Abstract

Disclosed in the present invention are heterocyclic-substituted indazolone compounds, a preparation method therefor, a pharmaceutical composition and the use thereof. Specifically, provided are compounds of formula (I), or pharmaceutically acceptable salts, tautomers, stereoisomers, isotope compounds, pharmaceutically acceptable salts, esters, prodrugs or hydrates thereof, a preparation method therefor, a pharmaceutical composition and the use thereof. The compounds disclosed by the present invention serving as CRL4CRBNE3 ubiquitin ligase regulators have good anti-tumor activity, and thus can be used for preparing drugs for treating CRL4CRBN E3 ubiquitin ligase related diseases.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61K 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed in the present invention are an indazolone compound, a preparation method therefor, a pharmaceutical composition, and a use. Specifically, provided are a compound of formula (I), or a pharmaceutically acceptable salt, tautomer, stereoisomer, isotopic compound, pharmaceutically usable salt, ester, prodrug or hydrate thereof, a preparation method therefor, a pharmaceutical composition, and a use. The compound of the present invention has good anti-tumor activity as a CRL4CRBNE3 ubiquitin ligase modulator, and can be used in the preparation of a drug for treating CRL4CRBN E3 ubiquitin ligase-related diseases.

IPC Classes  ?

• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

Disclosed in the present invention are a steroid compound, and a preparation method therefor and the use thereof. The structure of the steroid compound is as shown in formula I, and the definition of each substituent in the formula are as described in the description and claims. The steroid compound of the present invention is a steroid compound having the dual functions of excellent AR antagonistic activity and AR degradative activity, has the characteristics of good druggability and safety, and can be used for treating diseases related to an AR signaling pathway. Disclosed in the present invention are a steroid compound, and a preparation method therefor and the use thereof. The structure of the steroid compound is as shown in formula I, and the definition of each substituent in the formula are as described in the description and claims. The steroid compound of the present invention is a steroid compound having the dual functions of excellent AR antagonistic activity and AR degradative activity, has the characteristics of good druggability and safety, and can be used for treating diseases related to an AR signaling pathway.

IPC Classes  ?

• A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton

Abstract

Provided are a cyclic 2-aminopyrimidine compound having a structure as shown in formula (I), or a pharmaceutically acceptable salt, stereoisomer or prodrug molecule thereof, and a use thereof. The compound can effectively inhibit the activity of EGFR protein kinase drug-resistant mutants (such as EGFRT790Mand EGFR19del/T790M/C797S), and can overcome the clinical drug resistance of patients suffering from tumors such as non-small cell lung cancer induced by existing third-generation selective EGFRT790M small molecule inhibitors Osimertinib(AZD9291), Olmutinib(HM6171), Rociletinib(CO-1686) and the like.

IPC Classes  ?

• C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are a class of compounds which have a structure as shown in the following general formula (I) and are used as somatostatin receptor subtype 5 (SSTR5) antagonists, and a pharmaceutical composition and the use thereof. The compounds have good SSTR5 antagonistic activities, and can be used for preparing drugs for treating related diseases mediated by SSTR5.

IPC Classes  ?

• C07D 471/10 - Spiro-condensed systems
• A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
• A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
• A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• A61K 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• C07D 205/12 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
• C07D 211/96 - Sulfur atom
• C07D 211/98 - Nitrogen atom
• C07D 221/20 - Spiro-condensed ring systems
• C07D 295/26 - Sulfur atoms
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 471/04 - Ortho-condensed systems
• C07D 487/10 - Spiro-condensed systems
• C07D 498/10 - Spiro-condensed systems

Abstract

The present invention relates to a cGAS inhibitor, a preparation method therefor, and a use thereof. Specifically, the compound has a structure represented by formula (I), wherein the definitions of groups and substituents are as stated in the description. Also disclosed are a preparation method for the compound and a use of the compound in the prevention and/or treatment of inflammation, autoimmune diseases, neurodegenerative diseases, and other diseases.

IPC Classes  ?

• C07D 487/10 - Spiro-condensed systems
• A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
• A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection

Abstract

Disclosed in the present invention are preparation and a use of a fluorescent probe targeting a GPR84 receptor. Specifically, the structure of the fluorescent probe is as shown in formula (I), wherein in the formula, the definitions of substituents are as stated in the description. The compound of formula (I) of the present invention can be used as a fluorescent probe for a GPR84 receptor on a cell membrane surface. The probe can specifically target a GPR84 receptor on a cell membrane surface, and emit specific fluorescence in a fat-soluble environment by means of a Nile red fluorescent group. The probe compound is simple to synthesize and has high yield, can quickly target a corresponding membrane receptor and generate signals, and achieves good specificity and a high signal-to-noise ratio.

IPC Classes  ?

• C07F 9/6574 - Esters of oxyacids of phosphorus
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate

Abstract

Disclosed in the present invention are a lignan derivative, a preparation method therefor and the use thereof. The structure of the lignan derivative is as shown in a formula I, wherein in the formula, the definition of each substituent is as described in the description and claims. The lignan derivative of the present invention can be used as an inhibitor of mitochondrial respiratory chain complex I to inhibit mitochondrial oxidative phosphorylation and ATP generation, and can also be used for preventing and/or treating diseases associated with the elevated activity or expression of the mitochondrial respiratory chain complex I or enhanced mitochondrial oxidative phosphorylation. Disclosed in the present invention are a lignan derivative, a preparation method therefor and the use thereof. The structure of the lignan derivative is as shown in a formula I, wherein in the formula, the definition of each substituent is as described in the description and claims. The lignan derivative of the present invention can be used as an inhibitor of mitochondrial respiratory chain complex I to inhibit mitochondrial oxidative phosphorylation and ATP generation, and can also be used for preventing and/or treating diseases associated with the elevated activity or expression of the mitochondrial respiratory chain complex I or enhanced mitochondrial oxidative phosphorylation.

IPC Classes  ?

• C07F 9/655 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
• A61K 31/365 - Lactones
• A61K 31/665 - Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• C07D 307/33 - Oxygen atoms in position 2, the oxygen atom being in its keto or unsubstituted enol form

Abstract

The present invention relates to an IRAK4 degrader as shown in formula I, and a preparation method therefor and the use thereof, in particular to a compound as shown in formula (I), and a deuterated compound, a stereoisomer, a geometric isomer, a tautomer, a solvate, a hydrate, a prodrug, a pharmaceutically acceptable salt or cocrystal, and a pharmaceutical composition thereof, a preparation method therefor, and the use thereof in the treatment of IRAK4-related diseases such as autoimmune diseases, inflammatory diseases, and cancers.

IPC Classes  ?

• C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

Disclosed in the present invention are a compound as shown in formula (I), a preparation method therefor and the pharmaceutical use thereof, comprising an optical isomer and a pharmaceutically acceptable salt thereof. The compound of the present invention has FLT3 and/or IRAK4 inhibitory activity, has proliferation inhibitory activity on various leukemia cell strains and IRAK4-related cell strains, and can be used in the preparation of drugs for resisting blood diseases, inflammation and autoimmune diseases.

IPC Classes  ?

• C07D 239/48 - Two nitrogen atoms
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

Disclosed are an aromatic heterocyclic compound and an application thereof. The aromatic heterocyclic compound is represented by formula I, and the compound has good LSD1 enzyme inhibitory activity, and can be used as an LSD1 inhibitor for treatment of tumors etc. Disclosed are an aromatic heterocyclic compound and an application thereof. The aromatic heterocyclic compound is represented by formula I, and the compound has good LSD1 enzyme inhibitory activity, and can be used as an LSD1 inhibitor for treatment of tumors etc.

IPC Classes  ?

• C07D 239/84 - Nitrogen atoms
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61P 35/00 - Antineoplastic agents
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 471/04 - Ortho-condensed systems
• C07D 471/10 - Spiro-condensed systems

Abstract

The present invention relates to an azetidine compound and a medical use thereof. Specifically, the compound has a structure as shown in formula (I), and can be used as a secretion regulator for type I interferons, especially as a cGAS/STING signal pathway-targeted inhibitor, and can be used for preparing drugs for preventing and/or treating inflammatory diseases and autoimmune diseases.

IPC Classes  ?

• C07D 513/04 - Ortho-condensed systems
• A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

A long-chain compound, a preparation method therefor and the use thereof are disclosed. The structure of said compound is represented by formula (I). The definition of each substituent in the formula is as set out in the description and claims. The compound can directly inhibit ACLY, inhibit lipid synthesis in primary hepatocytes, inhibit lipid de novo synthesis and histone acetylation in various cancer cells such as H358, and inhibit cancer cell proliferation. The compound may be used to prepare drugs that treat metabolic diseases such as hyperlipidemia and atherosclerosis or various cancers such as lung cancer, pancreatic cancer, breast cancer, ovarian cancer, liver cancer, intestinal cancer, brain cancer, and acute myeloid leukemia. A long-chain compound, a preparation method therefor and the use thereof are disclosed. The structure of said compound is represented by formula (I). The definition of each substituent in the formula is as set out in the description and claims. The compound can directly inhibit ACLY, inhibit lipid synthesis in primary hepatocytes, inhibit lipid de novo synthesis and histone acetylation in various cancer cells such as H358, and inhibit cancer cell proliferation. The compound may be used to prepare drugs that treat metabolic diseases such as hyperlipidemia and atherosclerosis or various cancers such as lung cancer, pancreatic cancer, breast cancer, ovarian cancer, liver cancer, intestinal cancer, brain cancer, and acute myeloid leukemia.

IPC Classes  ?

• C07C 57/42 - Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing six-membered aromatic rings having unsaturation outside the rings
• A61K 31/201 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having one or two double bonds, e.g. oleic or linoleic acid
• A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
• A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61P 35/00 - Antineoplastic agents
• C07C 57/13 - Dicarboxylic acids
• C07C 61/35 - Unsaturated compounds having unsaturation outside the rings
• C07C 61/39 - Unsaturated compounds containing six-membered aromatic rings
• C07C 69/75 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring of acids with a six-membered ring
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• C07D 295/192 - Radicals derived from carboxylic acids from aromatic carboxylic acids
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Disclosed are an application of a coronavirus SARS-CoV-2 vaccine polypeptide, a polypeptide composition and a nanoemulsion preparation thereof in the prevention of coronavirus SARS-CoV-2 wild and mutant strain infections. Specifically, provided is a coronavirus SARS-CoV-2 vaccine polypeptide having an amino acid sequence derived from an S protein of SARS-CoV-2 wild and mutant strains, the vaccine polypeptide can enable the body to generate high-level and durable humoral immune responses against SARS-CoV-2 and to produce high titers of RBD-binding antibodies and neutralizing antibodies that block the binding of RBD to ACE2. The vaccine polypeptide can be used to prevent infections of SARS-CoV-2 wild strain and B.1.1.7, B.1.351, B.1.617, B.1.1.529 and other mutant strains.

IPC Classes  ?

• A61K 39/215 - Coronaviridae, e.g. avian infectious bronchitis virus
• A61K 9/107 - Emulsions
• A61P 37/04 - Immunostimulants
• C07K 14/005 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from viruses

Abstract

Disclosed in the present invention are a FAP-targeting compound, and a radionuclide-labeled complex based thereon and a preparation method therefor and the use thereof. The FAP-targeting compound has a structure as shown in formula (I), and has high affinity for a FAP target. A radiopharmaceutical obtained by means of labeling the FAP-targeting compound with a radionuclide such as 68Ga shows higher tumor uptake and longer tumor retention time, and can be used for the application and further development of FAP-targeting drugs.

IPC Classes  ?

• C07K 5/097 - Tripeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp, e.g. thyroliberin, melanostatin
• C07K 5/117 - Tetrapeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp
• C07K 5/078 - Dipeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp
• C07K 5/033 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link in which at least an epsilon- or zeta-amino acid is involved
• A61K 51/08 - Peptides, e.g. proteins
• A61K 51/04 - Organic compounds
• A61P 35/00 - Antineoplastic agents
• C07K 1/06 - General processes for the preparation of peptides using protecting groups or activating agents
• C07K 1/13 - Labelling of peptides
• A61K 103/00 - Radioactive metals

Abstract

A protein degradation agent, and a pharmaceutical composition and the use thereof. The structure as shown in formula (A) is used as an LC3B recruitment compound, and a protein degradation agent is obtained by means of connecting the structure as shown in formula (A), particularly a 2,4-quinazolinedione structure with a ligand of a target protein, which enable the autophagy degradation of the target protein, generate a biological effect, and facilitate the treatment and prevention of related diseases. The protein degradation agent can be used for treating, preventing and/or improving diseases associated with CDK, EZH2, or RAS.

IPC Classes  ?

• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 487/04 - Ortho-condensed systems
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention provides a compound represented by formula I, a racemate, an enantiomer, a diastereoisomer and a pharmaceutically acceptable salt thereof, and their use in preventing or treating a related disease caused by coronavirus and/or picornavirus infection. The present invention provides a compound represented by formula I, a racemate, an enantiomer, a diastereoisomer and a pharmaceutically acceptable salt thereof, and their use in preventing or treating a related disease caused by coronavirus and/or picornavirus infection.

IPC Classes  ?

• A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
• A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61P 31/14 - Antivirals for RNA viruses
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
• C07D 495/10 - Spiro-condensed systems

Abstract

The present application relates to a Gastrodiae rhizoma oligosaccharide compound, and a preparation method therefor and the use thereof, and in particular, to a Gastrodiae rhizoma oligosaccharide compound having a structure as represented by formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof, a preparation method therefor, a pharmaceutical composition and the use of the Gastrodiae rhizoma oligosaccharide compound of formula (I) or the pharmaceutically acceptable salt or the stereoisomer thereof in the preparation of a drug for treating and/or preventing somnipathy caused by diseases.

IPC Classes  ?

• C08B 37/00 - Preparation of polysaccharides not provided for in groups Derivatives thereof
• A61K 31/715 - Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkagesDerivatives thereof, e.g. ethers, esters
• A61K 31/702 - Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
• A61P 25/20 - HypnoticsSedatives
• A61P 25/22 - Anxiolytics
• A61P 25/24 - Antidepressants

Abstract

The present invention relates to a phosphodiesterase-4 inhibitor, a pharmaceutical composition comprising same, and a use thereof. The phosphodiesterase-4 inhibitor has a structure as shown in formula I. Researches prove that the compound of formula I of the present application can effectively inhibit the activity of phosphodiesterase 4, can increase the accumulation of cAMP in cells, can significantly inhibit the secretion of inflammatory factors TNF-α in human peripheral blood mononuclear cells, is expected to be used as an active ingredient for preparing a drug for preventing and/or treating phosphodiesterase 4-related diseases or for preparing a cosmetic for improving skin sensitivity, and is particularly expected to be used for preparing a drug for preventing and/or treating psoriasis and atopic dermatitis. Therefore, the compound of the present application has significant medicinal value and wide application prospects.

IPC Classes  ?

• C07D 307/84 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• C07D 307/83 - Oxygen atoms
• C07D 209/18 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 333/64 - Oxygen atoms
• A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• A61K 31/404 - Indoles, e.g. pindolol
• A61P 17/00 - Drugs for dermatological disorders

Abstract

The present invention relates to a FAP (Fibroblast Activation Protein) inhibitor, a FAP-targeted nuclide probe, and an application thereof, and specifically to a compound shown in formula I, or its precursor compound, isotope compound, salt, or hydrate, the compound is labeled with a radionuclide to obtain a FAP-targeted nuclide probe, and can be used as a diagnostic and therapeutic agent in lesions with high expression of FAP protein in humans or animals, especially as a tumor imaging agent and a radionuclide therapeutic drug. In animal experiments, compared with the widely accepted 68Ga-FAPI-04, the radioactive complex of the present invention has higher tumor uptake and tumor/muscle ratio, longer tumor retention time, and has good application prospects.

IPC Classes  ?

• C07D 455/02 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing not further condensed quinolizine ring systems
• C07D 421/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having selenium, tellurium, or halogen atoms as ring hetero atoms containing three or more hetero rings
• A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed in the present invention is a pyridazinone TRPC4/5 inhibitor; the structure thereof is as shown in formula I. In the formula, the definition of each substituent is as stated in the description and the claims. The compound of the present invention has strong inhibitory activity on TRPC4 and TRPC5. After oral administration, the compound shows a remarkable treatment effect on a hypertensive nephropathy model and a hepatic fibrosis model, and therefore has good potential to be developed as a drug for treating kidney and liver diseases.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

55 site, comprising antibodies, polypeptides, sugars, nucleic acids, small molecule drugs, optical dyes, organic nanomaterials or fragments or derivatives thereof, and the reaction is more accurate and efficient. The macrocyclic chelating agent can be chelated with radionuclides for imaging such as PET, SPECT, MRI, etc., or for research on the application of radionuclide therapy.

IPC Classes  ?

• C07D 471/18 - Bridged systems
• C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
• A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
• C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
• A61K 51/04 - Organic compounds
• A61K 51/08 - Peptides, e.g. proteins
• A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 31/695 - Silicon compounds
• A61P 35/00 - Antineoplastic agents
• C07B 59/00 - Introduction of isotopes of elements into organic compounds
• C07K 7/64 - Cyclic peptides containing only normal peptide links
• G01N 33/534 - Production of labelled immunochemicals with radioactive label

Abstract

The present invention relates to a urea compound containing 2-heteroaromatic ring substitution represented by formula (I), its enantiomers, diastereomers, racemates or mixtures thereof, or pharmaceutically acceptable salts thereof, solvate, metabolite or prodrug. The compound of formula (I) of the present invention has inhibitory activity against CDK9, and representative compounds have significant anti-tumor activity against CDK9 high-expressing tumor cells. Representative compounds have plasma stability and low clearance. The present invention relates to a urea compound containing 2-heteroaromatic ring substitution represented by formula (I), its enantiomers, diastereomers, racemates or mixtures thereof, or pharmaceutically acceptable salts thereof, solvate, metabolite or prodrug. The compound of formula (I) of the present invention has inhibitory activity against CDK9, and representative compounds have significant anti-tumor activity against CDK9 high-expressing tumor cells. Representative compounds have plasma stability and low clearance.

IPC Classes  ?

• C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
• A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
• A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61P 35/00 - Antineoplastic agents
• C07D 239/42 - One nitrogen atom
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 487/04 - Ortho-condensed systems
• C07D 498/04 - Ortho-condensed systems

Abstract

Provided in the present invention are Nav1.8 inhibitors shown as formula I, a preparation method therefor and the use thereof. The compounds provided by the present invention have good Nav1.8 selective inhibitory activity, good pharmacokinetic properties and good druggability, can be used as Nav1.8 inhibitors for preventing and/or treating diseases related to abnormal Nav1.8 channel expression activity, and thus have significant clinical application value.

IPC Classes  ?

• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 213/78 - Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 213/82 - AmidesImides in position 3
• C07D 317/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• C07C 257/18 - Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
• C07C 259/18 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines having carbon atoms of hydroxyamidine groups bound to carbon atoms of six-membered aromatic rings
• C07C 257/20 - Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having nitrogen atoms of amidino groups acylated
• C07C 261/04 - Cyanamides
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
• A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis

Abstract

Provided are a class of alkylphenol compounds and a preparation method therefor. Specifically provided are a new alkyl polyphenol compound as represented by chemical formula I, and a preparation method therefor and the use thereof in the treatment of metabolic syndrome. Provided are a class of alkylphenol compounds and a preparation method therefor. Specifically provided are a new alkyl polyphenol compound as represented by chemical formula I, and a preparation method therefor and the use thereof in the treatment of metabolic syndrome.

IPC Classes  ?

• C07C 39/19 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring monocyclic with unsaturation outside the aromatic ring containing carbon-to-carbon double bonds but no carbon-to-carbon triple bonds
• A61K 31/05 - Phenols
• A61K 31/09 - Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
• A61K 31/136 - Amines, e.g. amantadine having aromatic rings, e.g. methadone having the amino group directly attached to the aromatic ring, e.g. benzeneamine
• A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N)Sulfinylamines (—N=SO)Sulfonylamines (—N=SO2)
• A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• C07C 43/215 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring having unsaturation outside the six-membered aromatic rings
• C07C 43/23 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
• C07C 215/76 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton of the same non-condensed six-membered aromatic ring
• C07C 233/88 - Carboxylic acid amides having nitrogen atoms of carboxamide groups bound to an acyclic carbon atom and to a carbon atom of a six-membered aromatic ring wherein at least one ortho-hydrogen atom has been replaced
• C07D 213/69 - Two or more oxygen atoms
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• C07D 239/10 - Oxygen or sulfur atoms
• C07D 307/36 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
• C07D 333/06 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulfur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
• C07D 333/34 - Sulfur atoms

Abstract

Provided are a conserved druggable pocket for class B GPCRs and the use thereof. Specifically, provided is a preliminary screening method for class B GPCR targeting drugs. The method can be used for efficiently screening class B GPCR targeting drugs.

IPC Classes  ?

• G16B 15/30 - Drug targeting using structural dataDocking or binding prediction

Abstract

A use of a combination of an LSD1 inhibitor and a drug to treat cancer. Specifically, provided is a composition comprising: a tranylcypromine compound and/or a derivative thereof; and a drug selected from a kinase inhibitor, an anti-cancer drug acting upon or affecting the DNA, an antiviral compound, an antihypertension compound, an antidiabetic compound, a JAK-STAT signaling pathway inhibitor, an NF-κB signaling pathway inhibitor, a protein synthesis inhibitor, a 5-hydroxytryptamine receptor agonist, a dystroglycan modulator, a GABA receptor modulator, or a combination thereof. The two active ingredients have a synergistic effect, and the synergistic treatment effect is significantly better than that of the two individually, thereby remarkably improving the cancer treatment effect.

IPC Classes  ?

• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 221/00 - Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups
• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a pharmaceutical composition for oral mucosal delivery, a pharmaceutical preparation thereof and the use thereof. The pharmaceutical composition for oral mucosal delivery comprises the following components in parts by weight: 5 to 40 parts of a pharmaceutical active ingredient and 5 to 90 parts of a functional oil matrix, wherein the pharmaceutical active ingredient comprises one or more of butylphthalide and butylphthalide derivatives; and the functional oil matrix comprises one or more fatty acid esters.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/365 - Lactones
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system

Abstract

Provided are a ROR1-targeting antibody, an antibody-drug conjugate comprising same, a preparation method therefor, and a use thereof. The ROR1-targeting antibody or an antigen-binding fragment thereof has a heavy chain variable region, a light chain variable region, and a complementarity determining region (CDR). Additionally provided are an antibody-drug conjugate comprising the ROR1-targeting antibody or an antigen-binding fragment thereof, a preparation method therefor, and a use thereof.

IPC Classes  ?

• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C12N 15/13 - Immunoglobulins
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents
• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer

Abstract

A double site-directed antibody-functional molecular conjugate, and a preparation method therefor and the use thereof. The double site-directed antibody-functional molecular conjugate comprises an antibody, linking fragments 1 and 2 and a functional molecule, wherein the functional molecule is coupled to a conserved glycosylation site in the Fc region of the antibody by the linking fragment 1 and is coupled to a lysine site at position 246 or 248 of the antibody by the linking fragment 2. The double site-directed antibody-functional molecular conjugate has good stability, cytotoxicity and in-vivo activity, has good druggability, etc., and can be used in the preparation of a drug, diagnostic and therapeutic reagents and a kit for treating tumors, diseases caused by inflammation, diseases caused by a virus infection and immune diseases. The preparation method has the advantages of simple operation, few purification steps, etc., and has a good druggability and is easy to industrialize.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
• C08B 37/00 - Preparation of polysaccharides not provided for in groups Derivatives thereof
• A61K 38/07 - Tetrapeptides
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
• C07K 16/22 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against growth factors
• A61K 39/44 - Antibodies bound to carriers
• A61K 31/542 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are a HER2 targeted peptide and the use thereof. The HER2 targeted peptide comprises a fragment having a sequence of RSLWSDF. The HER2 targeted peptide is a low-molecular-weight polypeptide, is convenient to synthesize and low in terms of cost, and can comprise modified non-natural amino acids, which introduction can greatly improve the stability of the series of polypeptides in vivo. Therefore, the polypeptide is not easy to degrade, has targeting activity not prone to suffering damage, and has higher potential to be aggregated and retained in tumor sites, thereby achieving better imaging and treatment effects, which is beneficial for being popularized and used clinically.

IPC Classes  ?

• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• C07K 7/56 - Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
• C07K 7/02 - Linear peptides containing at least one abnormal peptide link
• C07K 1/107 - General processes for the preparation of peptides by chemical modification of precursor peptides
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• G01N 33/533 - Production of labelled immunochemicals with fluorescent label
• G01N 33/534 - Production of labelled immunochemicals with radioactive label
• A61K 49/00 - Preparations for testing in vivo
• A61K 51/08 - Peptides, e.g. proteins
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are an isoquinoline compound represented by formula (I), a pharmaceutically acceptable salt thereof, an enantiomer thereof, a diastereomer, a racemate, a crystalline hydrate, and a solvate, as well as an application of a composition thereof in fighting a virus. R1, R2, R3, and R4 are as defined in the description. Further provided are a preparation method for the compound and uses thereof for preparing an inhibitor that inhibits a virus and/or a drug for prophylaxis and/or treatment of an illness related to a respiratory tract infection, pneumonia, etc. caused by a virus. Provided are an isoquinoline compound represented by formula (I), a pharmaceutically acceptable salt thereof, an enantiomer thereof, a diastereomer, a racemate, a crystalline hydrate, and a solvate, as well as an application of a composition thereof in fighting a virus. R1, R2, R3, and R4 are as defined in the description. Further provided are a preparation method for the compound and uses thereof for preparing an inhibitor that inhibits a virus and/or a drug for prophylaxis and/or treatment of an illness related to a respiratory tract infection, pneumonia, etc. caused by a virus.

IPC Classes  ?

• C07D 491/18 - Bridged systems
• A61K 31/4748 - QuinolinesIsoquinolines forming part of bridged ring systems
• A61P 31/14 - Antivirals for RNA viruses
• C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
• C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

Abstract

The present invention provides a use of a naphthylamide compound (I) or a pharmaceutically acceptable salt thereof in preparation for a drug for treating meningioma, and provides a corresponding treatment method. The structure of the compound (I) is as shown below. The compound (I) has an excellent inhibitory effect on meningioma, can effectively treat meningioma, and has good safety and tolerance.

IPC Classes  ?

• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• A61P 35/00 - Antineoplastic agents
• C07D 231/56 - BenzopyrazolesHydrogenated benzopyrazoles

Abstract

The present invention provides a use of Lys01 or a salt thereof in preparation of a Kir4.1 potassium channel inhibitor. Specifically, the present invention relates to a use of Lys01 or a salt thereof in preparation of a Kir4.1 inhibitor, a use of Lys01 or a salt thereof in preparation of a drug for treating and/or preventing a disease using a Kir4.1 potassium channel as a therapeutic target, and a use of Lys01 or a salt thereof in preparation of a diuretic. Trihydrochloride Lys05 of Lys01 shown in the present invention has strong Kir4.1 potassium channel inhibitory activity, can suppress an endogenous Kir4.1 potassium channel current, can depolarize the astrocyte resting membrane potential, and can alleviate depression-like behaviors induced by overexpression of the Kir4.1 potassium channel in the mouse lateral habenula. Lys05 achieves a rapid antidepressant effect on a series of depression mouse models such as an acute forced swimming model, a novelty-suppressed feeding model, a corticosterone-induced depression model, and an olfactory bulbectomy model.

IPC Classes  ?

• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• A61P 25/24 - Antidepressants
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• A61P 13/00 - Drugs for disorders of the urinary system
• A61P 7/10 - Antioedematous agentsDiuretics

Abstract

The present invention relates to the fields of medicinal chemistry and pharmaco therapeutics, and specifically to a method for preparing a compound of formula I and a chemically acceptable salt thereof. The present invention relates to the fields of medicinal chemistry and pharmaco therapeutics, and specifically to a method for preparing a compound of formula I and a chemically acceptable salt thereof.

IPC Classes  ?

• C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Provided in the present invention are an isoquinoline alkaloid compound selected from the group consisting of the compounds represented by the following structural formulas, and a preparation method therefor and the use thereof. The present invention proves for the first time that the isoquinoline alkaloid compound is an inhibitor of the IK potassium current and the background potassium current in the nervous system, the cardiovascular system and the pancreas, especially an inhibitor of the Kv2.1 channel and the TRESK channel, and can be used for treating a disease such as stroke, arrhythmia, atrial fibrillation, diabetes, pain, hypoventilation, and depression. Provided in the present invention are an isoquinoline alkaloid compound selected from the group consisting of the compounds represented by the following structural formulas, and a preparation method therefor and the use thereof. The present invention proves for the first time that the isoquinoline alkaloid compound is an inhibitor of the IK potassium current and the background potassium current in the nervous system, the cardiovascular system and the pancreas, especially an inhibitor of the Kv2.1 channel and the TRESK channel, and can be used for treating a disease such as stroke, arrhythmia, atrial fibrillation, diabetes, pain, hypoventilation, and depression.

IPC Classes  ?

• C07D 471/14 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present invention relates to a heterocyclic compound for inhibiting SHP2 activity that is represented by formula I, a preparation method therefor and use thereof. The compound of the present invention is effective in treating a disease or disorder or condition mediated by SHP2. The present invention relates to a heterocyclic compound for inhibiting SHP2 activity that is represented by formula I, a preparation method therefor and use thereof. The compound of the present invention is effective in treating a disease or disorder or condition mediated by SHP2.

IPC Classes  ?

• C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

Abstract

A xanthine compound and the use thereof. The structure of the compound is as shown in formula I-a, wherein the definition of each substituent is as described in the description and claims. The compound of formula I-a is an inhibitor or an agonist of TRPC4 and TRPC5 ion channels, and has a potential application value in preventing, delaying or treating diseases related to abnormal function or expression of TRPC4/5.

IPC Classes  ?

• C07D 473/04 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

The present invention provides a pentacyclic triterpenoid glycoside compound, and a preparation method therefor and a use thereof. Specifically, the present invention provides a compound as shown in formula I. The definition of each group is described in the description. The compound can be used for preparing a medicament for treating metabolic diseases such as diabetes and viral diseases caused by influenza virus, coronavirus and the like. The present invention provides a pentacyclic triterpenoid glycoside compound, and a preparation method therefor and a use thereof. Specifically, the present invention provides a compound as shown in formula I. The definition of each group is described in the description. The compound can be used for preparing a medicament for treating metabolic diseases such as diabetes and viral diseases caused by influenza virus, coronavirus and the like.

IPC Classes  ?

• C07J 63/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
• A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses

Abstract

Disclosed in the present invention are a 1,2,3,4-tetrahydropyridone compound, and a preparation method therefor and a use thereof. The 1,2,3,4-tetrahydropyridone compound has a structure as shown in formula I, wherein in the formula, the definitions of the substituents are as described in the description and the claims. The compound of the present invention can selectively inhibit the activity of Jmjd1c; using the compound to treat tumor-bearing mice can selectively inhibit tumor regulatory T cells without affecting regulatory T cells in peripheral immune organs, thereby achieving the purpose of tumor immunotherapy without affecting immune homeostasis in organisms.

IPC Classes  ?

• C07D 513/04 - Ortho-condensed systems
• C07D 498/04 - Ortho-condensed systems
• C07D 471/04 - Ortho-condensed systems
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a novel coronavirus vaccine using a TLR7 agonist conjugated peptide as an antigen and an emulsion as an adjuvant. An antigen polypeptide of the conjugated peptide is a polypeptide derived from an S protein of SARS-COV-2, and the adjuvant is an oil-in-water nanoemulsion containing squalene. The conjugated peptide nanoemulsion vaccine preparation of the present invention is thermally stable, and can induce a high level of protective humoral immune response in a cynomolgus monkey, and the neutralizing antibody titer of antiserum after immunization of cynomolgus monkey is high, such that invasion of wild-type strain and mutant novel coronavirus can be blocked. The vaccine of the present invention has a nearly complete protection effect on the upper and lower respiratory tracts of the cynomolgus monkey in a cynomolgus monkey SARS-COV-2 challenge test. The nanoemulsion vaccine of the present invention is fast and convenient to prepare, and can realize large-scale production in a short term for coping with the novel coronavirus outbreak.

IPC Classes  ?

• A61K 39/215 - Coronaviridae, e.g. avian infectious bronchitis virus
• A61K 39/00 - Medicinal preparations containing antigens or antibodies
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• C12N 7/00 - Viruses, e.g. bacteriophagesCompositions thereofPreparation or purification thereof

Abstract

The present invention provides a long-acting insulin-Fc fusion protein. The insulin-Fc fusion protein of the present invention has reduced insulin receptor affinity, improved selectivity to auxin receptors, and a prolonged half-life in vivo, and can prolong a glucose lowering duration in vivo, reduce the time interval of insulin usage, and reduce the side effects such as a hypoglycemia risk.

IPC Classes  ?

• C07K 19/00 - Hybrid peptides
• C12N 15/62 - DNA sequences coding for fusion proteins
• A61K 38/28 - Insulins
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 3/00 - Drugs for disorders of the metabolism

Abstract

The present invention relates to a conjugate of an asialoglycoprotein receptor ligand and a cytotoxin, the conjugate being shown as the following formula I, and the use thereof. The conjugate presents relatively high inhibition activity on cell proliferation related to the ASGPR receptor expression quantity and thus can effectively kill tumor cells. In addition, the conjugate has hepatocellular carcinoma targeting effects and thus can effectively reduce the toxic and side effects caused by potential off-target.

IPC Classes  ?

• A61K 47/61 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 35/00 - Antineoplastic agents

Abstract

Provided in the present invention are a paeoniflorin crystal form A, a preparation method therefor, and the use thereof. The crystal form A is represented by means of XRD, IR, DSC, TGA and the like. A powder diffraction pattern of the crystal form A obtained by the X-ray powder diffraction method using Cu-Kα has diffraction peaks at the following 2θ angles: 6.73°±0.2°, 7.94°±0.2°, 13.57°±0.2°, 15.53°±0.2°, 15.98°±0.2°, 17.16°±0.2°, 17.62°±0.2°, 20.45°±0.2° and 25.60°±0.2°. The paeoniflorin crystal form A of the present invention has low hygroscopicity and good physical stability and therefore is an ideal medicinal crystal form.

IPC Classes  ?

• C07H 17/04 - Heterocyclic radicals containing only oxygen as ring hetero atoms
• C07H 1/06 - SeparationPurification
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 3/08 - Drugs for disorders of the metabolism for glucose homeostasis
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

The present invention relates to a salt of a compound of formula (I), and a method for preparing the salt, a pharmaceutical composition containing the salt and the use thereof. The salt-forming acid of the salt of the compound of formula (I) is selected from a plurality of acids such as hydrochloric acid, maleic acid, hydrogen bromide, phosphoric acid and sulfuric acid. The salt of the compound of formula (I) has the advantages of a good stability, high solubility, low hygroscopicity, etc., and can be used for preparing a drug for treating and/or relieving depression.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61P 25/24 - Antidepressants
• A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine

Abstract

A self-emulsifying pharmaceutical composition of compound (I), which improves the solubility and oral bioavailability of the medicine, has stable properties, and can be made into a plurality of dosage forms such as oral liquids, capsules, and tablets.

IPC Classes  ?

• A61K 9/107 - Emulsions
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• A61P 35/00 - Antineoplastic agents
• A61P 27/02 - Ophthalmic agents
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 17/06 - Antipsoriatics

Abstract

The present invention provides a phthalazinone or quinazolinone derivative as shown in formula I, a pharmaceutical composition comprising same, and a use thereof. The compound of the present invention has excellent PARP enzyme inhibitory activity and moderate to excellent drug-resistant cell proliferation inhibitory activity, has significant inhibitory effects on the growth of drug-resistant transplanted tumors in mice, has good application prospects for overcoming the resistance to existing PARP inhibitors, and can thus be used for treating PARP-related diseases, and PARP-related diseases that are resistant to the existing PARP inhibitors, especially tumors.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07F 17/02 - Metallocenes of metals of Groups 8, 9 or 10 of the Periodic Table
• C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
• A61P 35/00 - Antineoplastic agents
• A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol

Abstract

Disclosed in the present invention is a 4-alkoxy benzimidazole-6-carboxylic acid derivative serving as a GLP-1 receptor agonist. The structure of the 4-alkoxy benzimidazole-6-carboxylic acid derivative is represented by general formula (II), and the definition of each substituent is as recited in the description and the claims. The compound in the present invention serves as a GLP-1 receptor agonist, and can be used to prevent and/or treat diseases or symptoms associated with dysregulation of GLP-1 receptor signaling pathway. (II)

IPC Classes  ?

• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 471/04 - Ortho-condensed systems
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone

Abstract

The present invention relates to an aurone derivative or analog as represented by formula (I), and a preparation method therefor, a pharmaceutical composition thereof and the use thereof. The aurone derivative or analog can be used as an estrogen-related receptor (ERR) modulator, particularly an estrogen-related receptor α (ERRα) modulator for preventing and/or treating diseases associated with abnormal expression of ERRα activity.

IPC Classes  ?

• C07C 13/465 - IndenesCompletely or partially hydrogenated indenes
• C07D 333/64 - Oxygen atoms
• C07D 307/83 - Oxygen atoms
• C07D 311/32 - 2, 3-Dihydro derivatives, e.g. flavanones
• C07D 221/04 - Ortho- or peri-condensed ring systems
• C07C 49/427 - Saturated compounds containing a keto group being part of a ring polycyclic a keto group being part of a condensed ring system having two rings
• A61K 31/085 - Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
• A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
• A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
• A61P 3/00 - Drugs for disorders of the metabolism
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 19/00 - Drugs for skeletal disorders
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to the fields of pharmaceutical chemistry and pharmacotherapeutics, and in particular to a compound as represented by general formula I, a racemate, an R-isomer, an S-isomer and a pharmaceutically acceptable salt thereof and a mixture of same, a preparation method therefor, a pharmaceutical composition containing the compound and the use thereof as an SIP receptor agonist. The oxadiazole compound involved in the present invention can be used for treating SIP receptor agonist related diseases. The present invention relates to the fields of pharmaceutical chemistry and pharmacotherapeutics, and in particular to a compound as represented by general formula I, a racemate, an R-isomer, an S-isomer and a pharmaceutically acceptable salt thereof and a mixture of same, a preparation method therefor, a pharmaceutical composition containing the compound and the use thereof as an SIP receptor agonist. The oxadiazole compound involved in the present invention can be used for treating SIP receptor agonist related diseases.

IPC Classes  ?

• C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
• A61K 31/4245 - Oxadiazoles
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 3/06 - Antihyperlipidemics
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system

Abstract

The present application relates to a disaccharide linker, a disaccharide-small molecule drug conjugate and a sugar chain fixed-point antibody-drug conjugate, a preparation method and the use thereof. The structure of the disaccharide linker is as shown in the following formula I. The present invention provides a new-type fixed-point and quantitative antibody-drug conjugate form, and the stability and cytotoxicity of the antibody-drug conjugate are improved. The present application relates to a disaccharide linker, a disaccharide-small molecule drug conjugate and a sugar chain fixed-point antibody-drug conjugate, a preparation method and the use thereof. The structure of the disaccharide linker is as shown in the following formula I. The present invention provides a new-type fixed-point and quantitative antibody-drug conjugate form, and the stability and cytotoxicity of the antibody-drug conjugate are improved.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents
• C12N 9/04 - Oxidoreductases (1.), e.g. luciferase acting on CHOH groups as donors, e.g. glucose oxidase, lactate dehydrogenase (1.1)
• C12N 9/24 - Hydrolases (3.) acting on glycosyl compounds (3.2)
• C12P 19/12 - Disaccharides

Abstract

Provided is a method for preparing tumor-associated antigen DSGb5 glycolipid. Specifically, provided is an effective chemoenzymatic preparation method for preparing DSGb5 glycolipid antigen, of which the artificial preparation is complicated. The present disclosure provides a material basis for the development of malignant renal cancer vaccines and related tumor immunotherapies.

IPC Classes  ?

• C12P 19/26 - Preparation of nitrogen-containing carbohydrates
• C07H 1/00 - Processes for the preparation of sugar derivatives
• C07H 15/10 - Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of a saccharide radical containing unsaturated carbon-to-carbon bonds
• C07H 23/00 - Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12
• C07H 13/06 - Fatty acids
• C12P 19/18 - Preparation of compounds containing saccharide radicals produced by the action of a glycosyl transferase, e.g. alpha-, beta- or gamma-cyclodextrins

Abstract

The present invention provides a bispecific antibody targeting CD47 and PD-1 and use thereof. The bispecific antibody has a structure represented by the following formula: IgG-Linker-scFv. The bispecific antibody can simultaneously bind to human PD-1 antigen and CD47 antigen, effectively inhibit the binding of PD-1 and CD47 to corresponding receptors, and exert the synergistic effect of T cells and macrophages in tumor immunity, leading to the targeted engagement of T cells with tumor cells without significant coagulation-related adverse effects, as well as enhanced antitumor efficacy and improved safety. The use of partial or complete gene of the antibody allows the modification and production of diverse forms of genetically engineered antibodies in eukaryotic cells or any expression systems. As such, the present invention is suitable for the treatment of a range of CD47-positive tumors and related diseases.

IPC Classes  ?

• C07K 16/46 - Hybrid immunoglobulins
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention belongs to the technical field of polysaccharides, and particularly relates to a seaweed-derived sulphated polysaccharide, a preparation method therefor, and use thereof. The seaweed-derived sulphated polysaccharide SPW-05-S2 comprises 62%-70% of polysaccharide, 27%-32% of acidophobe, 0.5%-1.5% of acetyl, and 2.0%-4.5% of protein, and has a weight-average molecular weight of 121.77 kDa. The composition of the polysaccharide mainly comprises mannose, glucuronic acid, galactose, xylose, and fucose. In-vivo experiments demonstrate that the polysaccharide can reduce pulmonary fibrosis induced by bleomycin, including recovering the lung tissue morphology, reducing a lung coefficient, and reducing animal lung injury and the expression of a fibrosis phenotype-related protein. Moreover, the seaweed-derived sulphated polysaccharide does not affect cell growth activity in vitro, and can significantly inhibit the expression of the fibrosis-related protein. Therefore, the polysaccharide has a potential effect of relieving lung injury, and is expected to be a candidate carbohydrate drug for treating pulmonary fibrosis.

IPC Classes  ?

• A61K 31/737 - Sulfated polysaccharides, e.g. chondroitin sulfate, dermatan sulfate
• A61K 36/03 - Phaeophycota or phaeophyta (brown algae), e.g. Fucus
• A61P 11/00 - Drugs for disorders of the respiratory system

Abstract

Disclosed in the present invention are a use of a combination of an anti-PD-L1 nanobody and a TLR7 small molecule agonist in anti-tumor treatment, and a PD-L1 and TLR7 double-targeting nanobody coupling drug, a preparation method therefor, and a use thereof. Specifically, disclosed in the present invention are a use and solution of a combination of an anti-PD-L1 nanobody and a derived protein thereof as well as a TLR7 small molecule agonist and a derived compound thereof in anti-tumor treatment. Meanwhile, disclosed in the present invention are design, preparation, and identification solutions for a novel PD-L1 and TLR7 double-targeting-nanobody drug conjugate and a derived molecule thereof, and an effect of the novel PD-L1 and TLR7 double-targeting nanobody drug conjugate in anti-tumor treatment. The PD-L1 and TLR7 double-targeting nanobody drug conjugate of the present invention can yield a significant antineoplastic efficacy in various transplantation tumor models.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61J 1/05 - Containers specially adapted for medical or pharmaceutical purposes for collecting, storing or administering blood, plasma or medical fluids
• A61P 35/00 - Antineoplastic agents
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

A yohimbine derivative, and a preparation method therefor and a pharmaceutical composition and use thereof. The biological structure of the yohimbine derivative is as shown by formula (I), wherein the definitions of the substituents in the formula are as stated in the description and claims. The yohimbine derivative is used as an α2A-AR antagonist, and can be used for treating diseases such as diabetes.

IPC Classes  ?

• C07D 459/00 - Heterocyclic compounds containing benz [g] indolo [2, 3-a] quinolizine ring systems, e.g. yohimbine16, 18-lactones thereof, e.g. reserpic acid lactone
• A61K 31/475 - QuinolinesIsoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors

Abstract

The present invention relates to a nucleoside analog represented by the following formula and a use thereof. Specifically, the present invention relates to a nucleoside analog represented by the following formula or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition thereof, and a use thereof in preparation of (a) an inhibitor for inhibiting replication of coronaviruses, paramyxoviruses, influenza viruses, flaviviruses, filoviruses, bunya viruses and/or arenaviruses, and/or (b) a medicine for treating and/or preventing or alleviating a disease caused by infection of coronaviruses, paramyxoviruses, influenza viruses, flaviviruses, filoviruses, bunya viruses and/or arenaviruses.

IPC Classes  ?

• C07H 19/23 - Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
• C07H 19/067 - Pyrimidine radicals with ribosyl as the saccharide radical
• C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids

Abstract

Disclosed in the present invention are an aryl-containing amine compound, a preparation method therefor and a use thereof. The aryl-containing amine compound is represented by formula (I), and has the function of regulating the activity of an NMDA receptor and/or a monoamine transporter and/or a sigma receptor. Thus, the compound can be used for preparing drugs for treating and/or preventing diseases associated with an NMDA receptor and/or a monoamine transporter and/or a sigma receptor, especially central nervous system diseases.

IPC Classes  ?

• C07D 277/60 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
• A61P 25/24 - Antidepressants

Abstract

The present invention relates to a spiro compound, and a preparation method and use thereof. The spiro compound is as shown in formula I, has 3CL protease inhibitory activity, can effectively inhibit RNA virus replication of protein complex hydrolysis relying on 3CL protease, and is further used for preventing or treating related diseases.

IPC Classes  ?

• C07K 5/065 - Dipeptides the side chain of the first amino acid containing carbocyclic rings, e.g. Phe, Tyr
• C07K 5/062 - Dipeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
• C07K 1/06 - General processes for the preparation of peptides using protecting groups or activating agents
• C07D 487/10 - Spiro-condensed systems
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
• A61K 38/05 - Dipeptides
• A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61P 31/14 - Antivirals for RNA viruses

Abstract

The invention relates to the field of pharmaceuticals. Specifically, the present application relates to a voltage-gated calcium ion channel α2δ subunit ligand comprising a polycyclic γ-aminobutyric acid structure represented by general formula I, a method for preparing same, and use thereof in the treatment of chronic neuropathic pain, epilepsy, and anxiety.

IPC Classes  ?

• C07C 229/32 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings other than six-membered aromatic rings
• C07C 227/04 - Formation of amino groups in compounds containing carboxyl groups
• A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 25/22 - Anxiolytics

Abstract

The present invention relates to an S-configuration-containing amino benzamide pyridazinone compound, a preparation method therefor, and a pharmaceutical composition and application thereof. Specifically, the present invention relates to a compound represented by the following general formula I or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition and application thereof. The S-configuration compound of the present application has very strong binding activity on class I histone deacetylase (HDAC1), and shows inhibitory activity on in-vitro proliferation of various tumor cells.

IPC Classes  ?

• C07D 237/14 - Oxygen atoms
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• C07C 67/00 - Preparation of carboxylic acid esters
• C07C 67/10 - Preparation of carboxylic acid esters by reacting carboxylic acids or symmetrical anhydrides with ester groups or with a carbon-halogen bond
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond

Abstract

The present invention relates to an antiviral application of nucleoside analogs. Specifically, the present invention relates to uses of nucleoside analogs and a pharmaceutical composition thereof as: (a) inhibitors for inhibiting the replication of coronaviruses, influenza viruses, respiratory syncytial viruses, flaviviridae viruses, filoviridae viruses and/or porcine epidemic diarrhea virus (PEDV); and/or (b) medicines for treating and/or preventing and mitigating diseases caused by coronavirus, influenza virus, respiratory syncytial virus, flaviviridae virus, filoviridae virus and/or porcine epidemic diarrhea virus (PEDV) infections. The nucleoside analogs according to the invention may treat and/or prevent and mitigate respiratory infection, pneumonia (COVID-19) and other related diseases caused by 2019 novel coronavirus infection.

IPC Classes  ?

• C07H 7/06 - Heterocyclic radicals
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses

Abstract

The present invention relates to a use of a naphthylamide compound in treating drug-resistant tumors. Specifically, disclosed in the present invention is a use of a compound (I) or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating drug-resistant tumors, especially temozolomide-resistant tumors and EGFR inhibitor-resistant tumors. Also disclosed in the present invention is that a compound (I) or a pharmaceutically acceptable salt thereof, when used in combination with an EGFR third-generation inhibitor ASK120067, can reverse EGFR inhibitor resistance.

IPC Classes  ?

• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a use of a naphthylamide compound in treatment of KRAS mutation-related diseases. Specifically, disclosed in the present invention are a use of a compound (I) or a pharmaceutically acceptable salt thereof for preparing a medication for treating KRAS mutation-related diseases, especially KRAS mutation tumors. The compound can effectively inhibit the growth of KRAS mutation tumors, especially KRAS G12C mutation tumors and KRAS G12D mutation tumors.

IPC Classes  ?

• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed in the present invention is a small molecular compound having a substituted phenylspiro[indoline-3,3'-pyrrolidine] structure. The structure thereof is as shown in general formula I, and the definition of each substituent is as described in the description and claims. The compound of the present invention can inhibit the protein-protein interaction between MDM2-p53 and MDMX-p53, is used as a small molecular inhibitor for the protein-protein interaction between MDM2-p53 and MDMX-p53, and is used in the preparation of a drug for preventing and/or treating diseases related to MDM2 and MDMX, especially tumors.

IPC Classes  ?

• C07D 487/10 - Spiro-condensed systems
• A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed in the present invention are a thiochroman derivative and a preparation method therefor and a use thereof. The structure of the thiochroman derivative is as shown in general formula (I), and the definition of each substituent is as described in the description and the claims. The thiochroman derivative of the present invention is used as a selective estrogen receptor degrader and antagonist for treating estrogen receptor positive diseases.

IPC Classes  ?

• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 495/04 - Ortho-condensed systems
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
• A61K 31/69 - Boron compounds
• A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
• A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
• A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
• A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 37/02 - Immunomodulators
• A61P 15/00 - Drugs for genital or sexual disordersContraceptives
• A61P 3/04 - AnorexiantsAntiobesity agents

Abstract

Disclosed in the present invention is a heparin pentasaccharide-based low molecular weight heparin mimetic, which is a heparin pentasaccharide dimer or heparin pentasaccharide trimer. Also disclosed in the present invention is a preparation method for a heparin pentasaccharide dimer or heparin pentasaccharide trimer. The heparin pentasaccharide dimer or heparin pentasaccharide trimer of the present invention has anticoagulant activity, and the heparin pentasaccharide trimer can be neutralized by protamine.

IPC Classes  ?

• C08B 37/10 - HeparinDerivatives thereof

Abstract

Disclosed is a biotinylated heparin pentasaccharide capable of being neutralized, which has a structure as represented by formula (I). The anti-coagulation activity of the biotinylated heparin pentasaccharide capable of being neutralized similar to that of fondaparinux is shown, and the biotinylated heparin pentasaccharide can be quickly neutralized by avidin.

IPC Classes  ?

• C07H 15/26 - Acyclic or carbocyclic radicals, substituted by hetero rings
• C07H 15/02 - Acyclic radicals, not substituted by cyclic structures
• C07H 1/00 - Processes for the preparation of sugar derivatives
• A61K 31/702 - Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
• A61K 31/7042 - Compounds having saccharide radicals and heterocyclic rings
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors

Abstract

The present invention provides a compound for preventing and treating vasodilator diseases, a preparation method therefor, and use thereof. Specifically, the present invention provides a compound of formula I and use thereof in treating vessel-related diseases. The compound of the present invention has the effects of slowing down the rate of progress of vasodilator diseases, inhibiting the expansion of arterial aneurysm, reducing the occurrence of intramural hematoma, inhibiting the occurrence of aortic dissection and further reducing arteriorrhexis, and is suitable for treating vascular dilation-related diseases. Treatment options other than surgical treatment are provided for aneurysms, intramural hematoma and/or aortic dissection patients. The compound of the present invention is safe in medication and small in toxic and side effects.

IPC Classes  ?

• C07C 69/734 - Ethers
• C07C 69/54 - Acrylic acid estersMethacrylic acid esters
• C07C 59/64 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
• C07C 59/68 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings the oxygen atom of the ether group being bound to a non-condensed six-membered aromatic ring
• A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
• A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
• A61K 31/085 - Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
• A61P 9/14 - VasoprotectivesAntihaemorrhoidalsDrugs for varicose therapyCapillary stabilisers

Abstract

Disclosed are a dibenzylbutyrolactone glycoside compound as shown in formula (I), a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition containing same, and the use thereof in the preparation of a drug for the prevention, treatment or adjuvant treatment of diseases associated with abnormal activity or expression levels of phosphodiesterase 4 (PDE4). The disclosed dibenzylbutyrolactone glycoside compound has a strong inhibitory activity against PDE4 and a strong anti-inflammatory activity, and can be used for the prevention, treatment or adjuvant treatment of diseases associated with abnormal activity and/or expression levels of PDE4. In addition, the disclosed method for preparing the dibenzylbutyrolactone glycoside compound can achieve the stereoselective preparation of the compound.

IPC Classes  ?

• C07D 315/00 - Heterocyclic compounds containing rings having one oxygen atom as the only ring hetero atom according to more than one of groups
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61P 17/00 - Drugs for dermatological disorders
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/24 - Antidepressants
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 11/06 - Antiasthmatics

Abstract

Provided is use of a heteroaryloxynaphthalene compound, in particular, use of compound A or a pharmaceutically acceptable salt thereof in preparing a medicament for treating a tumor-related disease. Compound A or the pharmaceutically acceptable salt thereof exhibits good efficacy against tumors and good tolerance, and thus has clinical potential for treating tumors.

IPC Classes  ?

• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
• C07D 213/63 - One oxygen atom
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a thyroid hormone receptor β selective agonist compound represented by formula I, a pharmaceutical composition and use thereof. The compound improves the selectivity to THR-α and the druggability of the compound while maintaining good THR-β agonistic activity, and shows a certain activity in in vivo pharmacological experiments.

IPC Classes  ?

• C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 471/04 - Ortho-condensed systems
• A61P 3/06 - Antihyperlipidemics

Abstract

123444'A, etc., have meanings as shown in the specification. The present invention also relates to a method for preparing the compounds, and further relates to the use of the compounds, pharmaceutically acceptable salts, solvates and stereoisomers including the mixtures in various proportions thereof, in particular to the use of the compounds in the preparation of antiviral drugs.

IPC Classes  ?

• C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
• C07D 239/545 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 211/76 - Oxygen atoms attached in position 2 or 6
• C07C 229/18 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to carbon atoms of six-membered aromatic rings
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• C07D 213/65 - One oxygen atom attached in position 3 or 5
• C07D 239/42 - One nitrogen atom
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 239/94 - Nitrogen atoms
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• C07K 5/078 - Dipeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp
• A61K 38/07 - Tetrapeptides
• A61P 31/14 - Antivirals for RNA viruses

Abstract

Provided is the following compound (I) or a pharmaceutically acceptable salt, ester, optical isomer, stereoisomer, polymorph, solvate, N-oxide, isotopically-labeled compound, metabolite, chelate, complex, inclusion complex, or prodrug thereof, as well as a pharmaceutical composition containing said compound of the present invention. Further provided is a use of a α-synuclein aggregation inhibitor of a compound of the present invention, as well as an application in alleviating and/or eliminating PD (Parkinson's disease). Further provided is an application of a compound of the present invention in the preparation of a drug for a neurodegenerative disease. Further provided is a method for treating a disease related to α-synuclein aggregation.

IPC Classes  ?

• A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
• C07D 493/04 - Ortho-condensed systems
• C07D 493/02 - Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
• A61P 25/16 - Anti-Parkinson drugs

Abstract

A YTH N6-Methyladenosine RNA Binding Protein 1 (YTHDF1) attenuating agent, with a compound, and when bound to YTHDF1, the compound binds to amino acid residues 372-392, 479-494 and 526-535 of SEQ ID NO: 1. A modified antigen presenting cell (mAPC), with the mAPC being treated with a YTHDF1 attenuating agent. A composition, with a YTHDF1 attenuating agent, a mAPC treated with the YTHDF1 attenuating agent, and optionally a pharmaceutically acceptable carrier. A method for attenuating an activity of YTHDF1, by administering an effective amount of a YTHDF1 attenuating agent. A method for determining whether or not a candidate agent is a YTHDF1 attenuating agent, by contacting the candidate agent with a YTHDF1 mutant. A method for treating a disease, disorder or condition associated with an expression of an antigen in a subject in need thereof.

IPC Classes  ?

• A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• A61K 35/15 - Cells of the myeloid line, e.g. granulocytes, basophils, eosinophils, neutrophils, leucocytes, monocytes, macrophages or mast cellsMyeloid precursor cellsAntigen-presenting cells, e.g. dendritic cells
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
• A61P 35/00 - Antineoplastic agents

Abstract

An osmotic pump controlled release preparation, which comprises the following structures sequentially arranged from inside out: a tablet core containing a drug-containing layer and a push layer, a controlled-release coating layer having a drug release hole, and an optional water-soluble coating film; wherein the drug release hole establishes communication between the drug-containing layer and the outside of the osmotic pump controlled-release preparation; the push layer is located at the side of the drug-containing layer away from the drug release hole; the drug-containing layer comprises an active pharmaceutical ingredient, the push layer comprises an osmopolymer, and the osmopolymer comprises hydroxyethyl cellulose and alginate.

IPC Classes  ?

• A61K 9/24 - Layered or laminated unitary dosage forms
• A61K 9/44 - Pills, lozenges or tablets printed, embossed, grooved, or perforated
• A61K 9/36 - Organic coatings containing carbohydrates or derivatives thereof
• A61K 31/4422 - 1,4-Dihydropyridines, e.g. nifedipine, nicardipine
• A61P 9/12 - Antihypertensives
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

Disclosed are compounds having general formula I, a method for preparing same, a pharmaceutical composition thereof, and use thereof. Specifically, the present invention provides a compound having a structure represented by general formula I, and a racemate, an R-isomer, an S-isomer and a pharmaceutically acceptable salt thereof, or a mixture thereof. The compound has a good effect on promoting transcription factor EB (TFEB) nuclear translocation and promoting lysosome generation, and can be used for preventing, treating, or assisting in treating various diseases related to lysosome dysfunction and biosynthesis insufficiency, especially neurodegenerative diseases caused by the accumulation of intracerebral pathological proteins (e.g., β-amyloid protein and α-synuclein), such as Alzheimer's disease (AD) and Parkinson's disease (PD).

IPC Classes  ?

• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/4741 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
• A61K 31/404 - Indoles, e.g. pindolol
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/16 - Anti-Parkinson drugs

Abstract

The present invention relates to an HER2 targeting peptide molecule and a use thereof. The HER2 targeting peptide molecule has the following general formulas: X-peptide, X-L-peptide, peptide-X, and peptide-L-X, wherein X represents a mark unit for a report function (fluorescence, diagnostic radionuclides, nuclear magnetic resonance, etc.) or a therapeutic function (therapeutic radionuclides, chemical drugs, etc.), L represents a linking group, peptide represents a unit derived from a polypeptide Herceptide, and the amino acid sequence of the polypeptide Herceptide is as shown in SEQ ID No.: 1. The HER2 targeting peptide molecule in the present invention can specifically recognize and target an HER2 receptor, can be effectively gathered and retained at a tumor site, and can be used for tumor targeted diagnosis and treatment.

IPC Classes  ?

• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• C07K 1/10 - General processes for the preparation of peptides using coupling agents
• C07K 1/04 - General processes for the preparation of peptides on carriers
• A61K 49/00 - Preparations for testing in vivo
• A61K 51/08 - Peptides, e.g. proteins
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention provides a class of compounds of general formula I and a preparation method therefor, and a pharmaceutical composition and the use thereof. Specifically, the present invention provides a compound having a structure as shown in general formula I, and a racemate, an R-isomer, an S-isomer, and a pharmaceutically acceptable salt thereof or a mixture thereof. The compounds have good inhibitory activities against PL protease, and thus can be used for treating, preventing and alleviating diseases related to PL protease, particularly for treating viral diseases in which PL protease is present, such as diseases caused by SARS-CoV-2, SARS-CoV, MERS-CoV, etc.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• A61K 31/415 - 1,2-Diazoles
• A61K 31/4164 - 1,3-Diazoles
• A61P 31/12 - Antivirals

Abstract

Provided in the present invention are an α,β-unsaturated amide compound, and a preparation method therefor, and a pharmaceutical composition and the use thereof. Specifically, provided in the present invention is a compound as represented by formula I, wherein the definition of each group is as described in the description. The compound can be used as a compound for improving cerebral blood flow and is used for preparing a pharmaceutical composition for treating neurodegenerative diseases such as Alzheimer's disease and vascular dementia and strokes.

IPC Classes  ?

• C07D 263/26 - Oxygen atoms attached in position 2 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom
• C07D 277/14 - Oxygen atoms
• C07D 277/18 - Nitrogen atoms
• C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 417/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
• A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• A61K 31/426 - 1,3-Thiazoles
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

The present invention provides a preparation method and use of a defective filovirus. Specifically, the present invention provides a defective recombinant filovirus, a coding sequence of one or more key viral proteins in a genome of the defective recombinant filovirus being replaced with a recombinase coding sequence, and a use of the defective recombinant filovirus in the aspects of antiviral drug research and development, virology research, vaccine development, and the like. The defective recombinant filovirus of the present invention has a good biosafety feature, is easy to produce, can completely simulate related immune response of host cells caused by virus infection, and is a tool virus having extremely high practicability.

IPC Classes  ?

• C12N 7/01 - Viruses, e.g. bacteriophages, modified by introduction of foreign genetic material
• C12N 15/11 - DNA or RNA fragmentsModified forms thereof
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• A61K 39/12 - Viral antigens
• C12R 1/93 - Animal viruses

Abstract

The present invention relates to use of a compound represented by formula (I) in resisting feline coronavirus or calicivirus infection. The compound represented by formula (I) efficiently inhibits the replication of feline coronavirus or calicivirus, and has low toxic and side effects, high oral bioavailability, and good druggability, thus being useful for the treatment of diseases caused by feline coronavirus or calicivirus infection.

IPC Classes  ?

• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
• A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 487/04 - Ortho-condensed systems
• C07H 19/23 - Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups
• C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
• A61P 31/14 - Antivirals for RNA viruses
• A61P 1/02 - Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 31/20 - Antivirals for DNA viruses
• A61P 31/12 - Antivirals
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
• A61P 11/00 - Drugs for disorders of the respiratory system

Abstract

The present invention relates to a substituted 4-aminoisoindoline compound, a preparation method therefor, a pharmaceutical composition thereof, and use thereof. The compound has a structure represented by formula (I). Specifically, the substituted 4-aminoisoindoline compound provided by the present invention has good anti-tumor activity as a CRL4CRBNE3 ubiquitin ligase modulator, and can be used for preparing a medicament for the treatment of CRL4CRBN E3 ubiquitin ligase-related diseases.

IPC Classes  ?

• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/433 - Thiadiazoles
• A61P 37/02 - Immunomodulators
• A61P 35/02 - Antineoplastic agents specific for leukemia
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

Provided is a pharmaceutical composition for treating hemorrhagic diseases, comprising: salvianolic acid as a first active ingredient; and ginsenoside as a second active ingredient. The pharmaceutical composition can be used for preventing and/or treating hemorrhagic diseases in tissues and organs, especially hemorrhagic stroke, and can ameliorate hemorrhagic stroke-related neural symptoms.

IPC Classes  ?

• A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
• A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• A61P 7/04 - AntihaemorrhagicsProcoagulantsHaemostatic agentsAntifibrinolytic agents
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

Provided is the use of a CSF1R kinase inhibitor compound or a pharmaceutically acceptable salt thereof in the preparation of drugs for treating diseases related to the CSF1R kinase signal transduction pathway or drugs for regulating immunization.

IPC Classes  ?

• C07D 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
• A61P 35/00 - Antineoplastic agents
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

Provided are an intestinal tract targeted pentacyclic triterpene TGR5 receptor agonist, a preparation method therefor and a use thereof. The structure is as shown in formula (I). The compound can be used for preparing drugs for treating diabetes, obesity, hyperlipidemia, liver injury and inflammatory diseases.

IPC Classes  ?

• C07J 63/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
• A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
• A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
• A61P 3/00 - Drugs for disorders of the metabolism
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 3/06 - Antihyperlipidemics
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

Disclosed in the present invention are a 5,6-dihydro-1,2,4-triazine compound and the pharmaceutical use thereof as a GLP-1 receptor agonist. A structure of the 5,6-dihydro-1,2,4-triazine compound is represented by formula (I), and in the formula, the definition of each substituent is as described in the description and the claims. The compound of the present invention can be used for treating diabetes, metabolic syndrome and the like when being used as a GLP-1 receptor agonist.

IPC Classes  ?

• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 3/00 - Drugs for disorders of the metabolism
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/16 - Anti-Parkinson drugs
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 9/00 - Drugs for disorders of the cardiovascular system

Abstract

Provided are a novel tetrahydroisoquinoline compound, a preparation method therefor, a pharmaceutical composition containing said compound, and a use thereof. Specifically, provided are a nitrogen-containing heterocyclic compound as represented by general formula (I), a pharmaceutically acceptable salt, an enantiomer, a diastereoisomer, or a racemate thereof. The compound may be used for preparing a pharmaceutical composition for treating a disease or condition related to the activity or expression levels of relaxin family receptor 4.

IPC Classes  ?

• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
• C07D 471/04 - Ortho-condensed systems
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/475 - QuinolinesIsoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 1/10 - Laxatives
• A61P 1/14 - Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

A strong FXR small-molecule agonist, and a preparation method therefor and use thereof, the structure of the agonist being represented by formula (I), are provided. In the formula, each substituent is as defined in the description and the claims. The compound provided has the advantages of high FXR agonist activity, simple synthesis, easily available raw materials and the like, and can be used for preparing medicines for treating FXR related diseases. A strong FXR small-molecule agonist, and a preparation method therefor and use thereof, the structure of the agonist being represented by formula (I), are provided. In the formula, each substituent is as defined in the description and the claims. The compound provided has the advantages of high FXR agonist activity, simple synthesis, easily available raw materials and the like, and can be used for preparing medicines for treating FXR related diseases.

IPC Classes  ?

• C07D 471/08 - Bridged systems

Abstract

Provided are an asymmetric donor-receptor type near-infrared region II probe molecule, a method for preparing same, and use thereof. The probe molecule is represented by the following general formula (1). The emission spectrum of the probe molecule can reach an NIR-II region, and compared with a probe with a D-A-D structure, a D-A structure of the probe reduces the molecular weight, such that the probe is easier for chemical modification and metabolism, and can be used for whole-body angiography, lymphatic imaging, diagnosis and detection of diseases, tumor imaging, surgical navigation, and the like.

IPC Classes  ?

• C07F 7/10 - Compounds having one or more C—Si linkages containing nitrogen
• C07D 513/04 - Ortho-condensed systems
• C09K 11/06 - Luminescent, e.g. electroluminescent, chemiluminescent, materials containing organic luminescent materials
• C08G 65/334 - Polymers modified by chemical after-treatment with organic compounds containing sulfur
• A61K 41/00 - Medicinal preparations obtained by treating materials with wave energy or particle radiation
• A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
• A61K 49/00 - Preparations for testing in vivo
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention provides a fused ring compound represented by formula I and use thereof. The fused ring compound of the present invention has a selective inhibitory activity against Nav1.8, and can be used as a Nav inhibitor and used for preparing drugs for treating and/or alleviating pain and pain-related diseases.

IPC Classes  ?

• C07C 311/46 - Y being a hydrogen or a carbon atom
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

Provided are a tandem epitope polypeptide vaccine for novel coronavirus and use thereof. Specifically, a vaccine polypeptide for novel coronavirus pneumonia is provided on the basis of analysis and study of the RBD sequence and structural information of the S protein of SARS-CoV-2. Said vaccine polypeptide comprises the following elements connected in series: a generic Th epitope sequence, a B cell epitope sequence and a T cell epitope sequence. The B cell epitope and the T cell epitope have an amino acid sequence from the RBM region of the S protein of SARS-CoV-2. Provided are a vaccine composition containing said vaccine polypeptide and use thereof. Experiments show that the vaccine polypeptide of the present invention can enable cynomolgus monkeys to initiate strong cellular and humoral immunity, and to generate neutralizing antibodies that block the binding of RBD and ACE2, and can be used for preventing and treating novel coronavirus pneumonia.

IPC Classes  ?

• A61P 31/14 - Antivirals for RNA viruses
• A61K 39/215 - Coronaviridae, e.g. avian infectious bronchitis virus
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The present invention falls within the technical field of medicinal chemistry, and specifically relates to an antiviral nucleoside analogue, and a pharmaceutical composition and the use thereof. The nucleoside analogue of the present invention has a structure as represented by formula (I), and has a good chemical stability, a high oral bioavailability, and a significant antiviral activity. The nucleoside analogue can be used in the preparation of an inhibitor for inhibiting viral replication and/or a drug for preventing, alleviating and/or treating diseases caused by viral infection.

IPC Classes  ?

• C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61P 31/14 - Antivirals for RNA viruses
• C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids

Abstract

The present invention provides a ClpP regulator and use thereof. Particularly, the present invention provides a cyclic peptide compound represented by the following formula (I) and a composition containing same. The compound can be used for preparing a pharmaceutical composition for the prevention and/or treatment of diseases or conditions related to ClpP protease activity or expression.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61P 35/00 - Antineoplastic agents

Abstract

A salt of nucleoside analog, and crystal form, pharmaceutical composition and use thereof. The salt of nucleoside analog has a structure shown in formula I, wherein X is hydrogen or deuterium; Y is an acid, n is 0.5 to 2, or n is 1. When X is hydrogen or deuterium, Y is hydrogen bromide, and n is 1, the salt of the nucleoside analog exists in the form of a crystal with crystal form I or crystal form A or exists in an amorphous form. A salt of nucleoside analog, and crystal form, pharmaceutical composition and use thereof. The salt of nucleoside analog has a structure shown in formula I, wherein X is hydrogen or deuterium; Y is an acid, n is 0.5 to 2, or n is 1. When X is hydrogen or deuterium, Y is hydrogen bromide, and n is 1, the salt of the nucleoside analog exists in the form of a crystal with crystal form I or crystal form A or exists in an amorphous form.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems

Abstract

Disclosed in the present invention are a triazolamide compound, a preparation method therefor, and a use thereof. Specifically, disclosed are a triazolamide compound as shown in formula I or a pharmaceutically acceptable salt thereof, and a use thereof in the preparation of a drug for treating and/or preventing HDAC-related diseases. The diseases may be cancers.

IPC Classes  ?

• C07D 249/06 - 1,2,3-TriazolesHydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
• C07D 249/04 - 1,2,3-TriazolesHydrogenated 1,2,3-triazoles
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61K 31/16 - Amides, e.g. hydroxamic acids
• A61K 31/4192 - 1,2,3-Triazoles
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61P 35/00 - Antineoplastic agents

Abstract

A peptidomimetic compound, and a preparation method, pharmaceutical composition and use therefor. Specifically, disclosed are a peptidomimetic compound represented by general formula (I), or a racemate, a cis-trans isomer, an enantiomer, a diastereomer or a mixture thereof, or a metabolite thereof, or a pharmaceutically acceptable salt, solvate or prodrug thereof. Also disclosed is a use of the compound in inhibiting coronaviruses comprising SARS-CoV-2, SARS-CoV, MERS-CoV, FIPV, as well as others including RNA viruses such as EV71, EV68 and norovirus.

IPC Classes  ?

• C07K 5/062 - Dipeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
• C07K 5/078 - Dipeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp
• C07K 5/083 - Tripeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
• C07K 5/097 - Tripeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp, e.g. thyroliberin, melanostatin
• C07K 5/117 - Tetrapeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp
• C07K 1/02 - General processes for the preparation of peptides in solution
• C07K 1/12 - General processes for the preparation of peptides by hydrolysis
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 38/05 - Dipeptides
• A61P 31/14 - Antivirals for RNA viruses

Abstract

Disclosed are preparation and anti-tumor application of a gene therapy vector interfering CKLF-like MARVEL transmembrane domain-containing protein 6 (CMTM6) expression. Specifically, disclosed are a gene therapy vector encoding a gene sequence targeting CMTM6 and a derivative thereof, a gene sequence encoded by a vector, a preparation method, and a use of a vector alone and in combination with other drugs in treating tumors. These gene therapy vectors comprise adeno-associated viruses and lentiviruses, etc., can inhibit the expression of CMTM6 in tumor tissues, can effectively inhibit the in-vivo growth of mouse and human colorectal cancer, melanoma, liver cancer, breast cancer, non-small cell lung cancer and the like by improving the tumor immunosuppression microenvironment, exhibit a strong anti-tumor effect in combination with immune checkpoint antibodies, chemotherapeutic drugs, immunoagonistic drugs, and metabolic regulation drugs, and have significant efficacy on PD-L1-deficient tumors and immune checkpoint antibody drug-resistant tumors.

IPC Classes  ?

• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are a compound for preventing and treating psychiatric disorders and the use thereof. In particular, provided is the use of a compound of formula I or a pharmaceutically acceptable salt thereof in (i) the preparation of a pharmaceutical composition or a preparation for preventing and/or treating TREK-1 ion channel-related diseases, (ii) the preparation of a pharmaceutical composition or a preparation for preventing and/or treating psychiatric disorders and/or (iii) the preparation of a TREK-1 ion channel inhibitor. Provided are a compound for preventing and treating psychiatric disorders and the use thereof. In particular, provided is the use of a compound of formula I or a pharmaceutically acceptable salt thereof in (i) the preparation of a pharmaceutical composition or a preparation for preventing and/or treating TREK-1 ion channel-related diseases, (ii) the preparation of a pharmaceutical composition or a preparation for preventing and/or treating psychiatric disorders and/or (iii) the preparation of a TREK-1 ion channel inhibitor.

IPC Classes  ?

• A61K 31/18 - Sulfonamides
• A61P 25/24 - Antidepressants

Abstract

Provided in the present invention are a cleavable fragment directed by an affinity fragment, the design and the synthesis thereof, and the use thereof in the preparation of a site-directed drug conjugate. Specifically, provided in the present invention is a conjugate with a ligand affinity directing group. The conjugate is as represented by formula I: AT-CL-R (I), wherein AT is an affinity moiety for a target protein (TP); CL is a cleavable fragment which has a self-cleaving reactivity; and R is a group to be modified to the target protein.

IPC Classes  ?

• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• C07K 7/50 - Cyclic peptides containing at least one abnormal peptide link
• A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
• A61K 38/00 - Medicinal preparations containing peptides
• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61K 31/00 - Medicinal preparations containing organic active ingredients