Abstract

Disclosed are a 2-(2-chloro-4-methylphenyl)quinazoline-4(3H)-ketone compound represented by formula (I), a preparation method therefor, and use thereof in, for example, sedative hypnotic, anticonvulsant, antidepressant, anti-anxiety drugs.

IPC Classes  ?

• C07D 239/91 - Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
• C07D 405/06 - 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 only aliphatic carbon atoms
• 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
• A61P 25/20 - Hypnotics; Sedatives
• A61P 25/08 - Antiepileptics; Anticonvulsants
• A61P 35/00 - Antineoplastic agents
• A61P 31/04 - Antibacterial agents
• A61P 31/18 - Antivirals for RNA viruses for HIV
• A61P 31/06 - Antibacterial agents for tuberculosis
• A61P 25/16 - Anti-Parkinson drugs
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine

Abstract

The present invention relates to a pharmaceutical composition of Tecovirimat for injection, comprising Tecovirimat as an active ingredient, cyclodextrin and an additive. The present invention also relates to a method for preparing the pharmaceutical composition. The composition improves the solubility of Tecovirimat in water by using cyclodextrin and meglumine in combination, as compared with the solubility of Tecovirimat in water by using cyclodextrin or meglumine alone.

IPC Classes  ?

• 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 47/40 - Cyclodextrins; Derivatives thereof
• A61K 9/19 - Particulate form, e.g. powders lyophilised
• A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin

Abstract

The present invention provides a compound of a general formula I, a stereomeride, pharmaceutically acceptable salt or a solvate thereof, a preparation method thereof, and usages in preparing medicines for preventing and/or treating diseases or symptoms caused by drug-resistant tumors or drug-resistant bacteria and in preparing medicines for preventing and/or treating diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection. Preferably, the diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection are diseases or symptoms caused by a heat shock protein 70 (Hsp70). The compound in the present invention is used for overcoming a difficult problem of drug resistance of tumors, improves the effect of tumor treatment, and provides a new medical strategy for clinical tumor treatment.

IPC Classes  ?

• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• 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
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• 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
• 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 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

Abstract

The present invention pertains to field of pharmaceutical chemicals, and relates to thiazole inner salt compounds, preparation methods and uses thereof. Specifically, the present invention relates to a compound of Formula I, hydrates or pharmaceutically acceptable salts thereof. The compound of Formula I of the present invention is a potent cross-linking protein cleavage agent, has a stable structure, good physical and chemical properties, and good pharmacological activities, and is suitable for large scale production to obtain samples with stable, controllable and reliable quality, thereby being suitable for pharmaceutical development.

IPC Classes  ?

• C07D 277/22 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings 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, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• A61K 31/426 - 1,3-Thiazoles
• C07D 277/30 - 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
• A61K 8/49 - Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
• A61K 31/4422 - 1,4-Dihydropyridines, e.g. nifedipine, nicardipine
• A61Q 11/00 - Preparations for care of the teeth, of the oral cavity or of dentures, e.g. dentifrices or toothpastes; Mouth rinses
• A61Q 19/08 - Anti-ageing preparations

Abstract

A cyanoacrylate material for loading an antitumor drug, a composition comprising the cyanoacrylate material and the antitumor drug, and a pharmaceutical formulation comprising said composition, for example, a pharmaceutical formulation useful for intratumoral injection.

IPC Classes  ?

• A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
• A61K 9/08 - Solutions
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed in the present invention is a compound of Formula (I), a geometric or optical isomer, a pharmaceutically acceptable salt, a solvate or a polymorph thereof. Also disclosed in the present invention is a composition comprising the compound of Formula (I), the geometric or optical isomer, the pharmaceutically acceptable salt, the solvate or the polymorph thereof. Also disclosed in the present invention is a use of the compound of Formula (I), the geometric or optical isomer, the pharmaceutically acceptable salt, the solvate or the polymorph thereof in the treatment of a disease or disorder such as a hypoglutamatergic condition, a neurodegenerative disease or respiratory depression, particularly in the treatment of a disease or disorder associated with AMPA receptor.

IPC Classes  ?

• C07H 13/04 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals attached to acyclic carbon atoms
• C07D 413/12 - 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 chain containing hetero atoms as chain links
• C07D 271/12 - Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
• A61P 11/00 - Drugs for disorders of the respiratory system
• 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
• C07H 1/00 - Processes for the preparation of sugar derivatives
• A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
• A61K 31/4245 - Oxadiazoles

Abstract

The present invention relates to a 2,3-epoxy succinyl derivative, a preparation method and a use thereof, in particular, the present invention relates to a compound represented by Formula (1), a racemate or an optical isomer thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof. The compound according to the present invention has good inhibitory activity and/or selectivity against cathepsin, especially Cathepsin B, can be used in the treatment of multiple diseases associated with cathepsin, for example, osteoporosis, rheumatoid arthritis and osteoarthritis that are associated with Cathepsin K, Ebola virus infection, a degenerative disease and an autoimmune disease that are associated with Cathepsin L, S, especially Cathepsin B-related tumor diseases, such as gastric cancer, cervical cancer, lung cancer, breast cancer, prostate cancer, bladder cancer, colon cancer, neuroglioma, and melanoma.

IPC Classes  ?

• C07D 303/48 - Compounds containing oxirane rings with 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, e.g. ester or nitrile radicals
• 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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
• A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
• 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 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic 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
• A61P 19/00 - Drugs for skeletal disorders
• A61P 37/02 - Immunomodulators
• A61P 35/00 - Antineoplastic agents
• C07D 301/27 - Condensation of epihalohydrins or halohydrins with compounds containing active hydrogen atoms

Abstract

A sustained-release nanoparticle for targeting a neurodegenerative disease, a preparation method thereof, a pharmaceutical composition comprising the same, and a use thereof in preparing a drug for preventing and/or treating a neurodegenerative disease in a subject. The nanoparticle comprises a carrier material, an active ingredient, and a targeting molecule. The carrier material is human serum albumin, and the active ingredient can prevent and/or treat the neurodegenerative disease.

IPC Classes  ?

• A61K 9/50 - Microcapsules
• A61K 47/42 - Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
• A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
• A61K 31/221 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
• 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 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 37/02 - Immunomodulators
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system

Abstract

The invention belongs to the technical field of medicines. In particular, the invention relates to a thiazideamide derivative compound or a pharmaceutically acceptable salt or solvate thereof, a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt or solvate thereof, a method for preparing the compound or a pharmaceutically acceptable salt or solvate thereof, and a use of the compound or a pharmaceutically acceptable salt or solvate thereof. For example, the compound or a pharmaceutically acceptable salt or solvate thereof according to the invention can be used to prevent and/or treat a neurodegenerative disease or a neuropathic disease caused by a physical trauma or a related disease.

IPC Classes  ?

• C07D 279/12 - 1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
• A61K 31/54 - 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
• 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 invention relates to a homoserine lactone derivative of Formula I, preparation method and use thereof. The compound has an effect of regulatory of bacterial quorum sensing, and is useful for preventing and/or treating a disease caused by infection of a bacterium

IPC Classes  ?

• C07D 307/33 - Oxygen atoms in position 2, the oxygen atom being in its keto or unsubstituted enol form
• 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
• 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
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen 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
• C12Q 1/02 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving viable microorganisms
• 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 31/4025 - 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 31/365 - Lactones

Abstract

The present invention pertains to the field of pharmaceutical chemicals, and relates to a substituted acethydrazide derivative, preparation method and use thereof; preferably, relates to a compound of Formula I or a pharmaceutically acceptable salt thereof. The compound of the present invention or a pharmaceutically acceptable salt thereof can effectively inhibit proline hydroxylase, stabilize HIF-α, particularly HIF-1α, and has potency in the manufacture of a medicament for treatment and/or prophylaxis and/or adjuvant therapy of anemia, acute ischemic reperfusion injury.

IPC Classes  ?

• C07C 251/86 - Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to carbon atoms of six-membered aromatic rings
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61K 31/277 - Nitriles; Isonitriles having a ring, e.g. verapamil
• C07C 255/58 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
• C07C 249/16 - Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of hydrazones
• C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups

Abstract

The present invention provides a compound of a general formula I, a stereomeride, pharmaceutically acceptable salt or a solvate thereof, a preparation method thereof, and usages in preparing medicines for preventing and/or treating diseases or symptoms caused by drug-resistant tumors or drug-resistant bacteria and in preparing medicines for preventing and/or treating diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection. Preferably, the diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection are diseases or symptoms caused by a heat shock protein 70 (Hsp70). The compound in the present invention is used for overcoming a difficult problem of drug resistance of tumors, improves the effect of tumor treatment, and provides a new medical strategy for clinical tumor treatment.

IPC Classes  ?

• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• 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 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
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• 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 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

Abstract

Disclosed is a pharmaceutical composition, comprising an active ingredient tecovirimat, a cyclodextrin and an additive, and optionally, a pharmaceutically acceptable excipient. Also disclosed is a method for preparing the pharmaceutical composition. The composition improves the solubility of the tecovirimat in water by using a combination of the cyclodextrin and meglumine, compared with the use of cyclodextrin alone or meglumine alone.

IPC Classes  ?

• 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 47/18 - Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• A61K 9/08 - Solutions
• A61P 31/20 - Antivirals for DNA viruses

Abstract

Disclosed is an injectable pharmaceutical composition of tecovirimat, comprising an active ingredient tecovirimat, a cyclodextrin and an additive. Also disclosed is a method for preparing the pharmaceutical composition. The composition improves the solubility of the tecovirimat in water by using the combination of the cyclodextrin and meglumine, compared to the use of cyclodextrin alone or meglumine alone.

IPC Classes  ?

• 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 47/18 - Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• A61K 9/08 - Solutions
• A61K 9/19 - Particulate form, e.g. powders lyophilised
• A61P 31/20 - Antivirals for DNA viruses

Abstract

The invention relates to tizoxanide phosphate or alkane sulfonate compounds represented by Formula I, and pharmaceutically acceptable salts thereof, isomers thereof, hydrates thereof or solvates thereof, and pharmaceutical applications of the compounds.

IPC Classes  ?

• C07D 277/58 - Nitro radicals
• C07F 9/6539 - Five-membered rings
• A61K 31/426 - 1,3-Thiazoles
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61P 31/20 - Antivirals for DNA viruses
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
• A61P 31/06 - Antibacterial agents for tuberculosis
• A61P 33/02 - Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
• A61P 33/04 - Amoebicides
• A61P 33/10 - Anthelmintics
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system

Abstract

Disclosed in the present invention are a compound represented by formula (I), a geometric or optical isomer, a pharmaceutically acceptable salt, a solvate or a polymorph thereof. Also disclosed in the present invention is a composition of the compound represented by formula (I), the geometric or optical isomer, the pharmaceutically acceptable salt, the solvate or the polymorph thereof. Also disclosed in the present invention are applications of the compound represented by formula (I), the geometric or optical isomer, the pharmaceutically acceptable salt, the solvate or the polymorph thereof in diseases related to glutamic acid hypofunction, neurodegenerative diseases, and respiratory depression diseases or symptoms, and especially applications in the diseases or symptoms related to an AMPA receptor.

IPC Classes  ?

• C07D 271/12 - Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
• C07D 413/12 - 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 chain containing hetero atoms as chain links
• C07H 13/04 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals attached to acyclic carbon atoms
• C07H 1/00 - Processes for the preparation of sugar derivatives
• A61K 31/4245 - Oxadiazoles
• A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
• 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 25/18 - Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 11/00 - Drugs for disorders of the respiratory system

Abstract

Disclosed are a pillararene complex as shown in formula I, a preparation method, a pharmaceutical composition and a use thereof. The complex improves the stability of drugs, and increases the inhibitory effects of drugs on tumour cells.

IPC Classes  ?

• A61K 47/58 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting 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 by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed in the present invention are a 2,3-epoxy succinyl derivative, a preparation method therefor, and uses thereof. Specifically, disclosed in the present invention are a compound represented by formula (1), a raceme thereof, an optical isomer thereof, a solvate thereof or a pharmaceutical acceptable salt thereof. The compound in the present invention has good inhibitory activity and/or selectivity on cathepsins and especially on cathepsin B, and can be used for treating multiple kinds of diseases related to cathepsins, such as osteoporosis, rheumatoid arthritis and osteoarthritis related to cathepsin K, Ebola virus infection, degenerative diseases and autoimmune diseases related to cathepsins L and S, especially tumor diseases related to cathepsin B, such as stomach cancer, cervical cancer, lung cancer, breast cancer, prostate cancer, bladder cancer, colon cancer, glioma and melanoma.

IPC Classes  ?

• C07D 303/48 - Compounds containing oxirane rings with 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, e.g. ester or nitrile radicals
• C07D 301/00 - Preparation of oxiranes
• 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 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
• A61K 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
• 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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention pertains to the field of pharmaceutical chemicals, and relates to a rapamycin derivative of Formula I, and a preparation method, pharmaceutical composition and use thereof. The compounds of the present invention overcome the defects of rapamycin in terms of water solubility and metabolic properties, and some of the compounds have an in vitro anti-tumor activity superior to rapamycin, have less toxicity to normal cells than rapamycin, and have very good druggability.

IPC Classes  ?

• C07D 491/18 - Bridged systems
• A61L 31/16 - Biologically active materials, e.g. therapeutic substances
• A61L 31/08 - Materials for coatings
• A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins

Abstract

Disclosed are a hydroquinone compound, a preparation method therefor, and an application in tumour resistance or immunomodulation. The structural formula of the hydroquinone compound is as shown in formula I, wherein: X is C=O or CH2; Y is NH, O or absent; R is selected from any one of the following groups: a substituted or unsubstituted alkyl group having at least one carbon atom, a substituted or unsubstituted cycloalkyl group having at least three carbon atoms, and a substituted or unsubstituted alkenyl group or alkynyl group having at least two carbon atoms; a substituted or unsubstituted aryl group or heteroaryl group at least containing four carbon atoms. The compound slowly releases 2-tert-butyl-4-methoxyphenol in the body, overcomes the shortcoming that the half-life of 2-tert-butyl-4-methoxyphenol directly administered in the body is short (T1/2 = 0.5-1h), and maintains a stable 2-tert-butyl-4-methoxyphenol plasma concentration (T1/2 = 12-24h). The compound protects the phenolic hydroxyl group of 2-tert-butyl-4-methoxyphenol, prevents oxidation in the environment, and increases the environmental stability of a drug.

IPC Classes  ?

• C07C 271/44 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
• C07C 271/56 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
• C07C 69/28 - Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with dihydroxylic compounds
• C07D 265/30 - 1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
• C07C 69/78 - Benzoic acid esters
• C07C 69/16 - Acetic acid esters of dihydroxylic compounds
• A61K 31/325 - Carbamic acids; Thiocarbamic acids; Anhydrides or salts thereof
• A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a compound as shown by general formula (I), a racemate or optical isomer thereof, a pharmaceutically acceptable salt, solvate or hydrate thereof, a pharmaceutical composition comprising the compound, and a use thereof in the preparation of drugs for preventing and/or treating diseases or conditions associated with viral infections.

IPC Classes  ?

• C07D 277/52 - Nitrogen atoms bound to hetero atoms to sulfur atoms, e.g. sulfonamides
• A61K 31/426 - 1,3-Thiazoles
• A61P 31/12 - Antivirals
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
• A61P 11/04 - Drugs for disorders of the respiratory system for throat disorders
• 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 31/18 - Antivirals for RNA viruses for HIV
• A61P 31/14 - Antivirals for RNA viruses

Abstract

The invention relates to a drug sustained-release composition, particularly a sustained-release composition comprising metoprolol and preparation method thereof. The invention also relates to a combination product comprising a sustained-release composition comprising metoprolol and a pharmaceutical composition comprising hydrochlorothiazide. The sustained-release composition comprising metoprolol according to the invention eliminates the phenomena of delayed release of such sustained-release compositions in the prior art, has a better drug release curve, and also have the advantages such as simple formula, easy operation, stable quality, strong controllability, and good reproducibility, and therefore have good application prospects.

IPC Classes  ?

• A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 9/50 - Microcapsules
• A61K 31/549 - 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 having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
• A61K 9/16 - Agglomerates; Granulates; Microbeadlets

Abstract

Provided in the present invention are a complex prepared from antimicrobial peptides in combination with polymers, the preparation method of the complex, and the use of the complex for preparing drugs for preventing or treating diseases or infections caused by bacteria (such as gram-positive bacteria or gram-negative bacteria), fungi or viruses. While the complex of the present invention maintains the antimicrobial peptide activity, the hemolytic toxicity thereof significantly decreases.

IPC Classes  ?

• A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61K 38/08 - Peptides having 5 to 11 amino acids
• A61K 38/10 - Peptides having 12 to 20 amino acids
• A61K 47/42 - Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
• A61P 31/04 - Antibacterial agents
• A61P 31/10 - Antimycotics
• A61P 31/12 - Antivirals

Abstract

Provided are a compound represented in Formula I or Formula II, or a physiologically non-toxic salt thereof, a pharmaceutical composition containing the compound, and a use of the compound in preparing drugs for treating and/or preventing and/or assisting in the treatment of diseases caused by HIV infection, AIDS in particular. Z-X1X2IX3X4IEQX5IX6X7IEQRIQQIEQX8X9X10X11X12X13X14X15X16X17X18X19X20X21LLQLTVWGIKQLQARIL-B(I) (Z-X1X2IX3X4IEQX5IX6X7IEQRIQQIEQX8X9X10X11X12X13X14X15X16X17X18X19X20X21LLQLTVWGIKQLQARIL-B)3(II)

IPC Classes  ?

• C07K 14/16 - HIV-1
• C12N 15/49 - Lentiviridae, e.g. immunodeficiency viruses such as HIV, visna-maedi virus, equine infectious anaemia virus
• C12N 15/63 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
• A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61P 31/18 - Antivirals for RNA viruses for HIV

Abstract

The present invention falls within the technical field of medicines. In particular, the present invention relates to a thiazideamide derivative compound, a pharmaceutically acceptable salt or solvate thereof, a pharmaceutical composition comprising the compound, the pharmaceutically acceptable salt or the solvate thereof, a method for preparing the compound, the pharmaceutically acceptable salt or the solvate thereof, and a use of the compound, the pharmaceutically acceptable salt or the solvate thereof. For example, the compound, the pharmaceutically acceptable salt or the solvate thereof in the present invention can be used to prevent and/or treat neurodegenerative diseases and neuropathic diseases caused by physical trauma, or related diseases.

IPC Classes  ?

• C07D 279/12 - 1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
• A61K 31/54 - 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
• A61P 25/00 - Drugs for disorders of the nervous system
• 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 21/00 - Drugs for disorders of the muscular or neuromuscular system

Abstract

The invention relates to a tizoxanide carbamate compound of Formula I and a pharmaceutically acceptable salt, a hydrate or a solvate thereof, and their pharmaceutical use.

IPC Classes  ?

• C07D 277/58 - Nitro 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 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

The present invention relates to 4-methyl-1H-diaryl pyrazole derivatives, and specifically relates to the compounds represented by formula (I) and stereoisomers, solvates or pharmaceutically acceptable salts thereof. The present invention also relates to a preparation method of the compounds, a pharmaceutical composition containing them, and use of said compounds as cannabine type I (CB1) receptor inhibitor in brain in preparing drugs for preventing, treating or alleviating diseases or symptoms relating to excessive activity of CBI receptor, such as obesity, memory or cognition impairment and smoke addiction, etc..

IPC Classes  ?

• C07D 231/40 - Acylated on said nitrogen atom
• 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 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
• A61K 31/415 - 1,2-Diazoles
• A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• 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 31/5377 - 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
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61P 3/04 - Anorexiants; Antiobesity agents
• 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 relates to a compound of formula (I), a stereomeride, pharmaceutically acceptable salt, a solvate or an N-oxide thereof, a medicine composition comprising the compound, a method for preparing the compound, and a usage of the compound in treating diseases related to Hsp70. The diseases are preferably selected from tumors, neurodegenerative diseases, and allogeneic transplantation rejection and infection.

IPC Classes  ?

• 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 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• 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 417/06 - 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 only aliphatic carbon atoms
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present invention provides a compound of a general formula I, a stereomeride, pharmaceutically acceptable salt or a solvate thereof, a preparation method thereof, and usages in preparing medicines for preventing and/or treating diseases or symptoms caused by drug-resistant tumors or drug-resistant bacteria and in preparing medicines for preventing and/or treating diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection. Preferably, the diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection are diseases or symptoms caused by a heat shock protein 70 (Hsp70). The compound in the present invention is used for overcoming a difficult problem of drug resistance of tumors, improves the effect of tumor treatment, and provides a new medical strategy for clinical tumor treatment.

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
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• 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
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• 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 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

Abstract

Provided is an inhibitor of human immunodeficiency virus type 1. The inhibitor is a site-specific covalently cross-linked N-terminal peptide compound, derivative, stereoisomer or salt having physiological toxicity thereof. Also provided are a pharmaceutical composition of the compound and use of the compound in preparing related medicine for preventing and/or treating a human immunodeficiency virus infection.

IPC Classes  ?

• C07K 14/00 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61K 38/00 - Medicinal preparations containing peptides

Abstract

The invention provides a compound of Formula I, an isomer, a pharmaceutically acceptable salt, or a solvate thereof, and use thereof in manufacture of a medicament for preventing and/or treating a drug-resistant tumor or disease or disorder caused by a drug-resistant bacterium, or use thereof in manufacture of a medicament for preventing and/or treating a tumor, a neurodegenerative disease, an allogeneic graft rejection, or an infection-associated disease or disorder; preferably, the tumor, neurodegenerative disease, allogeneic graft rejection, or infection-associated disease or disorder is a disease or disorder caused by Heat shock protein 70 (Hsp70). The compounds of the invention, which are a class of Hsp70 inhibitors having a novel structure and a high activity, solve the problem concerning drug resistance of tumors, enhance the effect of treating tumors, and provide a new medical strategy for treatment of tumors in clinic.

IPC Classes  ?

• A61K 31/155 - Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (HN=C(OH)NH2), isothiourea (HN=C(SH)—NH2)
• A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
• C07C 335/04 - Derivatives of thiourea
• C07C 391/00 - Compounds containing selenium
• C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
• C07C 335/08 - Derivatives of thiourea having nitrogen atoms of thiourea groups bound to acyclic carbon atoms of a saturated carbon skeleton
• C07C 335/14 - Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of rings other than six-membered aromatic rings
• C07C 335/16 - Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
• C07C 335/18 - Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms
• C07D 295/16 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
• C07C 335/20 - Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
• C07D 211/06 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members

Abstract

A pegylated artesunate derivative, a pharmaceutical composition and uses thereof, the pegylated artesunate derivative is represented by the general formula (I): The pegylated artesunate derivative has activity comparable to that of artesunate, increased water solubility and stability, and an extended half-life in vivo.

IPC Classes  ?

• A61K 31/335 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
• A61K 31/35 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
• C07D 323/00 - Heterocyclic compounds containing more than two oxygen atoms as the only ring hetero atoms
• A61K 31/765 - Polymers containing oxygen
• A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
• C08G 65/332 - Polymers modified by chemical after-treatment with organic compounds containing oxygen containing carboxyl groups, or halides or esters thereof
• A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
• C08G 65/333 - Polymers modified by chemical after-treatment with organic compounds containing nitrogen

Abstract

The present invention relates to tizoxanide phosphate or alkane sulfonate type compounds represented by the type of Formula I, pharmaceutically acceptable salts thereof, isomers thereof, hydrates thereof or solvates thereof, and pharmaceutical applications of the type of compounds.

IPC Classes  ?

• C07F 9/6539 - Five-membered rings
• C07D 277/58 - Nitro radicals
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 31/426 - 1,3-Thiazoles
• A61P 33/02 - Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
• A61P 33/10 - Anthelmintics
• A61P 31/20 - Antivirals for DNA viruses
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
• A61P 31/06 - Antibacterial agents for tuberculosis
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 33/04 - Amoebicides

Abstract

Provided is a pentacyclic triterpene-peptide conjugate, and a preparation method, a pharmaceutical composition and a use thereof. The pentacyclic triterpene-peptide conjugate has an antibacterial effect, and in particular has a significant antibacterial effect on gram-positive bacteria.

IPC Classes  ?

• C07K 5/068 - Dipeptides the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
• C07K 5/09 - Tripeptides the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
• C07K 5/11 - Tetrapeptides the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• C07J 61/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by contraction of only one ring by one or two atoms
• A61K 38/05 - Dipeptides
• A61K 38/06 - Tripeptides
• A61K 38/07 - Tetrapeptides
• A61K 38/08 - Peptides having 5 to 11 amino acids
• A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• A61P 31/04 - Antibacterial agents

Abstract

Provided are a compound of formula I which can be used as a drug against small RNA virus infections, and optical isomers, pharmaceutically acceptable salts, solvates or hydrates thereof. Also provided are the preparation method of the compound, the method for using the compound for treating bacterial infections and the use of the compound in the preparation of a drug for preventing and/or treating viral diseases caused by small RNA viruses.

IPC Classes  ?

• 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 303/48 - Compounds containing oxirane rings with 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, e.g. ester or nitrile radicals
• 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

Abstract

The present invention relates to polysaccharides extracted from Poria, specifically relates to polysaccharide components A and B extracted from Poria, polysaccharide ingredients I and II extracted from Poria, and compositions thereof. The present invention also relates to a method for preparing polysaccharide components A and B, and polysaccharide ingredients I and II. The present invention also relates to the use of the polysaccharide components or ingredients as adjuvants, vaccine excipients or immunomodulators, and the use in the preparation of vaccine formulations or antibodies. Activity experiments show that Poria polysaccharide components A and B, and polysaccharide ingredients I and II have an immune adjuvant activity and an immunomodulating activity, which provides new choices of adjuvants, immunomodulators and vaccine excipients, and for preparing vaccine formulations or antibodies.

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 linkages; Derivatives thereof, e.g. ethers, esters
• A61P 37/02 - Immunomodulators

Abstract

The present invention relates to a drug delivery system, comprising a drug-loaded carbon nanotube formed by a carbon nanotube and drug molecules adsorbed to the surface of the carbon nanotube, a modifying material capable of enhancing the water solubility and biocompatibility of the drug delivery system, and a targeting molecule. The present invention also relates to a preparation method, and use, of the drug delivery system. The present invention provides a new type of strategy for selective targeting and effective removal of cancer stem cells, which is advantageous to the fundamental prevention of cancer recurrence and metastasis caused by cancer stem cells.

IPC Classes  ?

• A61K 47/36 - Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
• A61K 47/38 - Cellulose; Derivatives thereof
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a drug delivery system, comprising: a drug-loaded carbon nanotube forn-ied by a carbon nanotube and a drug molecule adsorbed on the surface of the carbon nanotube, a modifying material capable of enhancing water solubility and biocompatibility of the drug delivery systern, and a targeting molecule. The present invention further relates to preparation and use of the drug delivery system. The present invention provides a new strategy for selectively targeting and effectively eliminating cancer stem cells, which is conducive to fundamentally preventing recurrence and metastasis of a cancer induced by cancer stem cells.

IPC Classes  ?

• A61K 47/04 - Non-metals; Compounds thereof
• A61K 9/18 - Adsorbates
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are a polypeptide nucleic acid vector containing a cell-penetrating peptide and an antimicrobial peptide having an α-helix amphiphilic structure. Also provided are a composite containing said nucleic acid vector and nucleic acid molecule, and a method for preparation of said nucleic acid vector and composite, and a use of said nucleic acid vector and composite.

IPC Classes  ?

• C12N 15/63 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
• C07K 19/00 - Hybrid peptides
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
• A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
• A61P 35/00 - Antineoplastic agents

Abstract

The invention relates to a compound of formula I, and a preparation method and use thereof. The compound has a bacterial quorum-sensing regulatory effect, and can be used for prevention and/or treatment of a disease caused by a bacterial infection.

IPC Classes  ?

• C07D 263/26 - Oxygen atoms attached in position 2 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom
• A61K 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

Dislcosed are a metoprolol sustained-release composition, comprising a blank pellet core, an active constitutent layer and a sustained-release coating layer containing the active constitutent, a method for preparing the metoprolol sustained-release composition, a combination product containing the metoprolol sustained-release composition and hydrochlorothiazide, and a use of the metoprolol sustained-release composition and the joint product in the preparation of drugs for treating or preventing diseases such as hypertension and the like.

IPC Classes  ?

• A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• A61K 9/16 - Agglomerates; Granulates; Microbeadlets
• A61P 9/12 - Antihypertensives
• A61P 9/00 - Drugs for disorders of the cardiovascular system

Abstract

Provided are a GnRH analog-cytotoxic molecule conjugate as shown by the following formula (I), and a preparation method and a use thereof in the preparation of drugs for treating tumours. The cytotoxic molecule is a taxol derivative or a docetaxel derivative. The conjugate can maintain the binding activity with GnRH receptors, and has a relatively good plasma stability and the growth inhibition activity on tumour cells. (X)Aaa1Aaa2-Aaa3-Ser-Aaa5-Aaa6(Y)-Leu-Aaa8-Pro-Aaa10-NH2

IPC Classes  ?

• C07K 7/23 - Luteinising hormone-releasing hormone (LHRH); Related peptides
• A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
• A61P 35/00 - Antineoplastic agents
• C07K 1/107 - General processes for the preparation of peptides by chemical modification of precursor peptides
• C07K 1/06 - General processes for the preparation of peptides using protecting groups or activating agents
• C07K 1/04 - General processes for the preparation of peptides on carriers

Abstract

A derivative of homoserine lactone represented by formula I, and a preparation method and use thereof. The compound has a bacterial quorum-sensing regulatory effect, and can be used for prevention and/or treatment of a disease caused by a bacterial infection.

IPC Classes  ?

• C07D 307/33 - Oxygen atoms in position 2, the oxygen atom being in its keto or unsubstituted enol form
• A61K 31/365 - Lactones
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present invention relates to the field of pharmaceutical chemicals. Provided are a rapamycin derivative represented by formula I, a preparation method therefor, and a pharmaceutical composition and uses thereof. The compounds of the present invention alleviate defects of rapamycin in water solubility and metabolic properties, and a part of the compounds are superior to rapamycin in the aspect of antitumor activity in vitro, have less toxicity to normal cells than rapamycin and have good druggability.

IPC Classes  ?

• A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
• 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 405/00 - 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

Abstract

Substituted acetohydrazide derivatives represented by formula I, or pharmaceutically acceptable salts thereof. The compounds and pharmaceutically acceptable salts of formula I effectively inhibit prolyl hydroxylase, and have stable hypoxia-inducible factor HIF-α activity.

IPC Classes  ?

• C07C 251/86 - Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to carbon atoms of six-membered aromatic rings
• C07C 249/16 - Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of hydrazones
• C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
• C07C 255/58 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
• A61K 31/277 - Nitriles; Isonitriles having a ring, e.g. verapamil
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61P 7/06 - Antianaemics
• A61P 7/08 - Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock

Abstract

The present invention relates to homoserine lactone derivatives represented by formula I, a preparation method therefor and a use. The present compounds have a bacterial quorum sensing regulatory effect, and may be used for preventing and/or treating related diseases caused by bacterial infection.

IPC Classes  ?

• C07D 405/00 - 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
• 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
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

Abstract

The present invention belongs to the field of biomedicine and provides a class of antimicrobial peptides having free thiols or dimers thereof, and pharmaceutical compositions and uses thereof.

IPC Classes  ?

• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• C07K 14/00 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• C12N 15/11 - DNA or RNA fragments; Modified forms thereof
• C12N 15/63 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• A61K 38/10 - Peptides having 12 to 20 amino acids
• A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61P 31/04 - Antibacterial agents
• A61P 31/10 - Antimycotics
• A61P 31/12 - Antivirals

Abstract

Provided is a triterpene-polypeptide conjugate, stereoisomer or pharmaceutically acceptable salt thereof. Also provided are a pharmaceutical composition containing the conjugate, stereoisomer or pharmaceutically acceptable salt thereof, and use of the conjugate, stereoisomer or pharmaceutically acceptable salt thereof in treating or preventing related diseases caused by HIV infection, especially the acquired immunodeficiency syndrome (AIDS).

IPC Classes  ?

• C07K 14/16 - HIV-1
• A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61P 31/18 - Antivirals for RNA viruses for HIV

Abstract

The present invention relates to a thiazine amide derivative and a pharmaceutical use thereof, and particularly to a compound of formula I (in the formula, variables are as described in the specification), a pharmaceutically acceptable salt, solvate or hydrate thereof. The present invention further relates to a method for preparing the compound, a pharmaceutical composition containing the compound, and a method or use thereof for prevention or treatment of neurodegenerative diseases.

IPC Classes  ?

• C07D 279/12 - 1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings

Abstract

The present invention relates to the biomedical field, and provides polypeptide for inhibiting HIV infection. The polypeptide comprises an amino acid sequence as expressed by SEQ ID NO: 1-10. The present invention also provides uses of the polypeptide in the preparation of drugs for resisting to HIV infection or preventing or treating aids. The polypeptide of the present invention is a monomer fusion inhibitor directly derived from NHR, has an activity higher than that of an original sequence, and needs low synthesis cost.

IPC Classes  ?

• C07K 14/16 - HIV-1
• C12N 15/49 - Lentiviridae, e.g. immunodeficiency viruses such as HIV, visna-maedi virus, equine infectious anaemia virus
• C12N 15/63 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
• C12N 1/15 - Fungi ; Culture media therefor modified by introduction of foreign genetic material
• C12N 1/19 - Yeasts; Culture media therefor modified by introduction of foreign genetic material
• A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
• A61P 31/18 - Antivirals for RNA viruses for HIV
• C12N 1/21 - Bacteria; Culture media therefor modified by introduction of foreign genetic material

Abstract

The present invention provides compounds of general formula I, isomers thereof, non-toxic pharmaceutically acceptable salts or solvates thereof. The compounds have remarkably strengthened analgesic activity, reduce the acute toxicity obviously, have no inhibition to heart Herg channel, and reduce side effects on coordination movement of mice remarkably. The present invention realizes the separation of activity and side effects, and has a good application prospect.

IPC Classes  ?

• C07D 317/64 - Oxygen atoms
• A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

Provided are a linear lipopeptide with an end group having a lipophilic structure, a preparation method for the lipopeptide, and a use thereof in preparing an anti-radiation injury medicament. The lipopeptide is one lipophilic structural unit and one linear polypeptide chain connected via an amide bond, where the lipophilic structural unit is located at either the N-terminus or the C-terminus of the linear polypeptide chain. The lipopeptide provides significant radiation injury protection activity.

IPC Classes  ?

• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• C07K 5/11 - Tetrapeptides the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
• A61K 38/08 - Peptides having 5 to 11 amino acids
• A61K 38/07 - Tetrapeptides
• A61P 39/00 - General protective or antinoxious agents
• A61P 17/16 - Emollients or protectives, e.g. against radiation
• A61P 37/04 - Immunostimulants
• A61P 37/02 - Immunomodulators

Abstract

Provided in the present invention are a general formula I compound, the isomers, pharmaceutically-acceptable salt or solvate thereof, and application thereof to manufacturing medicine for preventing and/or treating drug-resistant tumours, or diseases or conditions caused by drug-resistant bacteria, or manufacturing medicine for preventing and/or treating tumours, neurodegenerative disease, allogeneic transplant rejection, infection-related diseases or symptoms; preferably, the tumour, neurodegenerative disease, allogeneic transplant rejection, infection-related disease or symptom is a disease or symptom caused by Heat shock protein 70 (Hsp70). The compound of the present invention is a highly-active Hsp70 inhibitor having an entirely new structure, used for overcoming the problem of drug-resistant tumours, improving the effects of tumour treatment, and providing a medical strategy for clinical oncology.

IPC Classes  ?

• C07C 391/00 - Compounds containing selenium
• C07D 295/16 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
• C07C 335/16 - Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
• C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
• C07C 335/08 - Derivatives of thiourea having nitrogen atoms of thiourea groups bound to acyclic carbon atoms of a saturated carbon skeleton
• C07C 335/18 - Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms
• C07C 335/14 - Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of rings other than six-membered aromatic rings
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61K 31/5375 - 1,4-Oxazines, e.g. morpholine
• A61K 31/4453 - Non-condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
• A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
• A61K 31/4406 - Non-condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
• A61K 31/4402 - Non-condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
• A61P 35/00 - Antineoplastic agents
• 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 37/06 - Immunosuppressants, e.g. drugs for graft rejection
• A61P 31/04 - Antibacterial agents

Abstract

The present invention provides a compound of a general formula I, a stereomeride, pharmaceutically acceptable salt or a solvate thereof, a preparation method thereof, and usages in preparing medicines for preventing and/or treating diseases or symptoms caused by drug-resistant tumors or drug-resistant bacteria and in preparing medicines for preventing and/or treating diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and inflection. Preferably, the diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and inflection are diseases or symptoms caused by a heat shock protein 70 (Hsp70). The compound in the present invention is used for overcoming a difficult problem of drug resistance of tumors, improves the effect of tumor treatment, and provides a new medical strategy for clinical tumor treatment.

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 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
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• 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 37/06 - Immunosuppressants, e.g. drugs for graft rejection
• A61P 31/04 - Antibacterial agents

Abstract

The present invention relates to a compound of formula (I), a stereomeride, pharmaceutically acceptable salt, a solvate or an N-oxide thereof, a medicine composition comprising the compound, a method for preparing the compound, and a usage of the compound in treating diseases related to Hsp70. The diseases are preferably selected from tumors, neurodegenerative diseases, and allogeneic transplantation rejection and infection.

IPC Classes  ?

• C07D 417/06 - 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 only aliphatic carbon 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
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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 35/00 - Antineoplastic agents
• 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 37/06 - Immunosuppressants, e.g. drugs for graft rejection
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

Abstract

2 are defined as those stated in the description.

IPC Classes  ?

• C07D 473/40 - Heterocyclic compounds containing purine ring systems with halogen atoms or perhalogeno-alkyl radicals directly attached in position 2 or 6
• 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 473/32 - Nitrogen atom
• C07D 215/20 - Oxygen atoms
• C07D 473/00 - Heterocyclic compounds containing purine ring systems
• 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 413/04 - 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 directly linked by a ring-member-to-ring- member bond
• C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine

Abstract

The present invention relates to a compound of Formula (I), or an isomer, pharmaceutically acceptable salt and solvate thereof; the present invention further relates to a pharmaceutical composition, which comprises the compound of Formula (I), or isomer, pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents; the present invention further relates to the use of the compound of Formula (I), or isomer, pharmaceutically acceptable salt or solvate thereof, for anti-apoptosis, prophylaxis or treatment of a disease or symptom associated with apoptosis, especially for protecting myocardial cells, and prophylaxis or treatment of a disease or symptom associated with cardiomyocyte apoptosis.

IPC Classes  ?

• C07D 277/42 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals

Abstract

The present invention provides a decapeptide derivative with LHRH receptor antagonist activity: R-D-Nal-D-Cpa-D-Pal-Ser-Aph(Hor)-D-Aph(Cbm)-Aaa7-Ilys-Pro-Aaa10-NH2. The present invention further provides a preparation method of the decapeptide derivative, a pharmaceutical composition containing the decapeptide derivative, and use of the decapeptide derivative in preparing medicine that can inhibit hypophysis from secreting gonnadotrophin, medicine that can inhibit gonad from secreting steroid hormones, and medicine for treatment of prostatic cancer, endometrial cancer, and sex hormone-dependent diseases associated with reproduction, contraception, and the like.

IPC Classes  ?

• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• C07K 1/04 - General processes for the preparation of peptides on carriers
• A61K 38/09 - Luteinising hormone-releasing hormone [LHRH]; Related peptides
• A61P 5/04 - Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
• A61P 5/06 - Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
• A61P 5/24 - Drugs for disorders of the endocrine system of the sex hormones
• A61P 13/08 - Drugs for disorders of the urinary system of the prostate
• A61P 15/00 - Drugs for genital or sexual disorders; Contraceptives
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention provides a joint product comprising synephrine and topiramate, in which the synephrine or salt thereof is administered in form of rapid-release preparation, preferably rapid-release pellet, having daily dose of 2 mg to 25 mg, preferably 5 mg to 20 mg; the topiramate is administered in form of sustained-release or controlled-release preparation, preferably sustained-release pellet, having daily dose of 20 mg to 100 mg, preferably 23 mg to 92 mg. The composition is used for treatment of obesity or other diseases associated with obesity.

IPC Classes  ?

• A61K 9/50 - Microcapsules
• A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
• A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
• A61K 9/16 - Agglomerates; Granulates; Microbeadlets
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present invention provides a combination product, which comprises immediate release pellet of phentermine and sustained-release pellet of topiramate, wherein the pellet of topiramate includes: a) a blank pellet core; b) an active drug layer that contains topiramate and is free of binding agent, the layer being located on surface of the blank pellet core; c) a sustained-release coating layer containing ethyl cellulose and PVP K30, the sustained-release coating layer being located on external of the active drug layer. The present invention further discloses a method for preparing the combination product.

IPC Classes  ?

• A61K 9/50 - Microcapsules
• A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
• A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

The present invention relates to a matrix metalloproteinase inhibitor and a use thereof. In particular, the matrix metalloproteinase inhibitor has a structure as shown in formula (I) or a pharmaceutically acceptable salt thereof, and can be used for the prevention or treatment of diseases regulated by matrix metalloproteinases, especially acute lung damage caused by asphyxiating gas or chronic obstructive pulmonary disease (COPD) caused by other reasons.

IPC Classes  ?

• C07C 259/06 - 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 without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
• C07D 307/52 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
• C07D 295/195 - Radicals derived from nitrogen analogues of carboxylic acids
• C07D 237/20 - Nitrogen atoms
• C07D 239/18 - Nitrogen atoms not forming part of a nitro radical with hetero atoms attached to said nitrogen atoms, except nitro radicals, e.g. hydrazine radicals
• C07D 213/40 - Acylated substituent nitrogen atom
• C07C 255/60 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
• 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 213/56 - Amides
• C07D 215/14 - Radicals substituted by oxygen atoms
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• 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 31/5375 - 1,4-Oxazines, e.g. morpholine
• A61K 31/4402 - Non-condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
• A61K 31/277 - Nitriles; Isonitriles having a ring, e.g. verapamil
• A61K 31/443 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/4406 - Non-condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
• A61K 31/4409 - Non-condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
• A61K 31/47 - Quinolines; Isoquinolines
• A61P 11/00 - Drugs for disorders of the respiratory system

Abstract

Disclosed in the present invention are a divalent polypeptide of formula I or formula II for resisting the HIV infection, and a derivative, stereoisomer or pharmaceutically acceptable salt thereof. Also disclosed in the present invention are a pharmaceutical composition comprising the polypeptide, or a derivative, stereoisomer or pharmaceutically acceptable salt thereof, and the use thereof in the preparation of a drug for the treatment or prevention of diseases resulting from HIV infection. Formula I: (C-L1-Z)2　Formula II: (Z-L1-C)2

IPC Classes  ?

• C07K 19/00 - Hybrid peptides
• C07K 14/16 - HIV-1
• A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61P 31/18 - Antivirals for RNA viruses for HIV

Abstract

The present invention belongs to the field of pharmaceuticals and chemicals, and relates to thiazole inner salt compounds, and a preparation method and use thereof. In particular, the present invention relates to compounds as shown by formula I, and hydrates or pharmaceutically acceptable salts thereof. The compounds of formula I of the present invention are potent crosslinking protein cleavage agent, and have a stable structure, good physical and chemical properties, and good pharmacological action; large-scale production can obtain samples with stable, controllable and reliable quality, and are suitable for developing into a drug.

IPC Classes  ?

• C07D 277/30 - 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
• A61K 31/426 - 1,3-Thiazoles
• A61P 17/00 - Drugs for dermatological disorders
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• 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
• A61P 27/12 - Ophthalmic agents for cataracts
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
• A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure

Abstract

Provided are a tizoxanide (TIZ) carbamate compound as represented by formula I, pharmaceutically acceptable salt, hydrate or solvate thereof, and pharmaceutical use of the compound.

IPC Classes  ?

• C07D 277/58 - Nitro radicals
• 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
• A61K 31/426 - 1,3-Thiazoles
• 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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
• A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61P 31/20 - Antivirals for DNA viruses
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
• A61P 31/04 - Antibacterial agents
• A61P 33/02 - Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
• A61P 33/10 - Anthelmintics
• C07F 9/6539 - Five-membered rings

Abstract

Disclosed are pyridazine derivatives represented by Formula I or pharmaceutically acceptable salts or hydrates thereof, pharmaceutical compositions comprising the compounds, methods of treating and/or preventing diseases or disorders associated with viral infections in patients using the compounds, and the use of the compounds in preparing the medicaments for treating and/or preventing diseases or disorders associated with viral infections. The compounds represented by Formula I have antiviral activity, especially anti-microRNA viral activity. Symbols in the compounds represented are described in the specification.

IPC Classes  ?

• C07D 237/20 - Nitrogen atoms

Abstract

A medical adhesive with good biodegradable performance capable of undergoing crosslinking copolymerization, comprising a mono-alpha-cyanoacrylate and a bis-alpha-cyanoacrylic acid diol ester monomer molecule. The olefinic bonds in the mono-alpha-cyanoacrylate structure are polymerized in the presence of infinitesimal anions to form a solid 3D high polymer; the 3D high polymer is provided with degradation sites on the web-like backbone chain, with clear degradation path and absorbable degradation products. The medical adhesive can be used for wound adhesive, large area wound hemostasia, and visceral and soft tissue wound closure.

IPC Classes  ?

• A61L 24/06 - Surgical adhesives or cements; Adhesives for colostomy devices containing macromolecular materials obtained by reactions only involving carbon-to-carbon unsaturated bonds
• C08F 28/02 - Homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a bond to sulfur or by a heterocyclic ring containing sulfur by a bond to sulfur
• A61L 24/00 - Surgical adhesives or cements; Adhesives for colostomy devices
• C08F 222/32 - Alpha-cyano-acrylic acid; Esters thereof
• C09J 4/00 - Adhesives based on organic non-macromolecular compounds having at least one polymerisable carbon-to-carbon unsaturated bond
• A61L 24/04 - Surgical adhesives or cements; Adhesives for colostomy devices containing macromolecular materials
• C09J 133/14 - Homopolymers or copolymers of esters of esters containing halogen, nitrogen, sulfur or oxygen atoms in addition to the carboxy oxygen
• C08F 283/02 - Macromolecular compounds obtained by polymerising monomers on to polymers provided for in subclass on to polycarbonates or saturated polyesters
• C09J 133/20 - Homopolymers or copolymers of acrylonitrile

Abstract

Disclosed are erythropoietin mimic peptide chemical dimmer and an application thereof, and especially, disclosed are erythropoietin mimic peptide chemical dimmer shown in formula (I) or medicinal salt thereof, and a composition containing the erythropoietin mimic peptide chemical dimmer or the medicinal salt thereof. Also disclosed is an application of the erythropoietin mimic peptide chemical dimmer or the medicinal salt thereof. The erythropoietin mimic peptide chemical dimmer or the medicinal salt thereof of the present invention has desirable erythropoiesis activity.

IPC Classes  ?

• C07K 14/505 - Erythropoietin (EPO)
• A61K 38/18 - Growth factors; Growth regulators
• A61P 7/06 - Antianaemics

Abstract

Provided are a compound of formula I which can be used as a drug against small RNA virus infections, and optical isomers, pharmaceutically acceptable salts, solvates or hydrates thereof. Also provided are the preparation method of the compound, the method for using the compound for treating bacterial infections and the use of the compound in the preparation of a drug for preventing and/or treating viral diseases caused by small RNA viruses.

IPC Classes  ?

• C07D 303/48 - Compounds containing oxirane rings with 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, e.g. ester or nitrile radicals
• C07D 301/00 - Preparation of oxiranes
• 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 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 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/428 - Thiazoles condensed with carbocyclic rings
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses

Abstract

Disclosed are a derivative of homoserine lactone shown in formula I, and a preparation method and use thereof. The compound has a function of sensing and regulating a bacterial colony, and can be used for prevention and/or treatment of related diseases caused by bacterial infection.

IPC Classes  ?

• C07D 307/33 - Oxygen atoms in position 2, the oxygen atom being in its keto or unsubstituted enol form
• A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
• A61P 31/04 - Antibacterial agents

Abstract

A compound in formula I, and a preparation method and use thereof. The compound has a function of sensing and regulating a bacterial colony, and can be used for prevention and/or treatment of related diseases caused by bacterial infection.

IPC Classes  ?

• C07D 263/26 - Oxygen atoms attached in position 2 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom
• A61K 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione
• A61P 31/04 - Antibacterial agents

Abstract

Disclosed is as a substituted thiazolamine derivative represented by Formula I or a pharmaceutically acceptable salt thereof or a hydrate thereof (the definitions of each group in the formula are as presented in the description), and the application thereof in the prevention and/or treatment of viral diseases induced by picornavirus. Also disclosed is a pharmaceutical composition containing the compound.

IPC Classes  ?

• C07D 417/04 - 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 directly linked by a ring-member-to-ring- member bond
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
• C07D 277/42 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals

Abstract

A metoprolol sustained-release drug composition and a preparation method therefor. The composition comprises: a. a blank sucrose pill core; b.an active drug layer containing metoprolol, the layer being located on the surface of the blank sucrose pill core; and c. a sustained-release coating layer containing ethyl cellulose and hydroxypropyl cellulose, the sustained-release coating layer being located outside the active drug layer.

IPC Classes  ?

• A61K 9/16 - Agglomerates; Granulates; Microbeadlets
• A61K 9/20 - Pills, lozenges or tablets
• A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• A61K 47/38 - Cellulose; Derivatives thereof
• A61P 9/00 - Drugs for disorders of the cardiovascular system

Abstract

The present invention relates to a thiazine amide derivative and a pharmaceutical use thereof, and particularly to a compound of formula I (in the formula, variables are as described in the specification), a pharmaceutically acceptable salt, solvate or hydrate thereof. The present invention further relates to a method for preparing the compound, a pharmaceutical composition containing the compound and a method or a use thereof for preventing or treating a neurodegenerative disease.

IPC Classes  ?

• C07D 279/12 - 1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
• A61K 31/54 - 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
• 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 25/00 - Drugs for disorders of the nervous system
• A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

Abstract

Provided are compounds of diarylanilines and diarylpyridinamines, a preparation method therefor, and uses thereof. The compounds have strong inhibitory activity (nM level) for a wild-type and multiple drug-resistant HIV strains, have good druggability, and are easy to synthesize.

IPC Classes  ?

• C07C 255/58 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
• C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• C07D 295/135 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• A61K 31/277 - Nitriles; Isonitriles having a ring, e.g. verapamil
• A61K 31/44 - Non-condensed pyridines; Hydrogenated derivatives thereof
• 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 31/18 - Antivirals for RNA viruses for HIV

Abstract

Provided is a diarylaniline or diarylpyridinamine compound and the preparation method and use thereof for preparing a drug. The compound has strong inhibition activity against wild-type and various resistant HIV viral strains (nM level) and good druggability, and can be convieniently synthesized.

IPC Classes  ?

• C07C 255/58 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
• C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
• C07C 311/39 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
• C07C 303/40 - Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• A61K 31/277 - Nitriles; Isonitriles having a ring, e.g. verapamil
• A61K 31/44 - Non-condensed pyridines; Hydrogenated derivatives thereof
• A61P 31/18 - Antivirals for RNA viruses for HIV

Abstract

Disclosed in the present invention are cyclopeptide derivatives with LHRH acceptor antagonistic activity of general formula I, the preparation method thereof, the pharmaceutical composition containing them and uses thereof in the preparation of medicines for treating prostate cancer, endometrial cancer, ovarian cancer, breast cancer and other sexual hormone dependent diseases related to reproduction, and of contraceptives.

IPC Classes  ?

• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• A61K 38/09 - Luteinising hormone-releasing hormone [LHRH]; Related peptides
• A61P 5/08 - Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
• A61P 5/28 - Antiandrogens
• A61P 5/32 - Antioestrogens
• A61P 5/36 - Antigestagens
• A61P 13/08 - Drugs for disorders of the urinary system of the prostate
• A61P 15/00 - Drugs for genital or sexual disorders; Contraceptives
• A61P 35/00 - Antineoplastic agents
• C07K 1/06 - General processes for the preparation of peptides using protecting groups or activating agents
• C07K 1/04 - General processes for the preparation of peptides on carriers

Abstract

Disclosed is anti-HIV infection polypeptide. The present invention relates to polypeptide expressed in formula I, derivative thereof, stereisomer thereof, or salt thereof with no physiological toxicity. Also disclosed are a pharmaceutical composition containing the polypeptide in formula I, the derivative thereof, the stereisomer thereof, or the salt thereof with no physiological toxicity, and use of the polypeptide in formula I, the derivative thereof, the stereisomer thereof, or the salt thereof with no physiological toxicity in treating or preventing related diseases caused by HIV infection, especially acquired immunodeficiency syndrome (AIDS).

IPC Classes  ?

• C07K 14/16 - HIV-1
• A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61P 31/18 - Antivirals for RNA viruses for HIV

Abstract

The present invention relates to a mimetic peptide of erythropoietin as shown in Formula (I) and uses thereof. The mimetic peptide of erythropoietin or pharmaceutically acceptable salts thereof can be used as alternatives to erythropoietin, and can be used in drugs for preventing and/or treating diseases and/or conditions related to the low activity of EPO or EPO receptors.

IPC Classes  ?

• C07K 14/505 - Erythropoietin (EPO)
• A61K 38/18 - Growth factors; Growth regulators
• C12P 21/04 - Cyclic or bridged peptides or polypeptides, e.g. bacitracin

Abstract

An N-aryl unsaturated fused ring tertiary amine compound, a preparation method thereof, a pharmaceutical composition containing the compound, and an application thereof in preparing medicine for treating tumors.

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 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 413/04 - 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 directly linked by a ring-member-to-ring- member bond
• C07D 215/20 - Oxygen atoms
• A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/47 - Quinolines; Isoquinolines
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic 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

Abstract

The present invention belongs to the field of pharmaceutical chemicals, and relates to a pegylated artesunate derivative, pharmaceutical composition and use thereof. In particular, the present invention relates to a pegylated artesunate derivative as shown by the general formula (I). The pegylated artesunate derivative of the present invention has activity comparable to that of an artesunate, significantly increased water solubility and stability, and a significantly extended half life in vivo.

IPC Classes  ?

• C08G 65/332 - Polymers modified by chemical after-treatment with organic compounds containing oxygen containing carboxyl groups, or halides or esters thereof
• A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
• A61P 33/06 - Antimalarials

Abstract

The present invention relates to a compound as represented by formula I or to an isomer, a pharmaceutically acceptable salt, and a solvate of the compound. The present invention also relates to a composition comprising the compound of formula I, or to the isomer, the pharmaceutically acceptable salt, and the solvate of the compound, and to a pharmaceutically acceptable carrier, excipient or diluent. The present invention also relates to a use of the compound of formula I, or the isomer, the pharmaceutically acceptable salt, and the solvate of the compound in resisting apoptosis, in the prevention or treatment of apoptosis-related diseases or symptoms, specifically a use for the protection of cardiomyocytes and in the prevention or treatment of the apoptosis-related diseases or symptoms.

IPC Classes  ?

• C07D 277/42 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• A61K 31/426 - 1,3-Thiazoles
• A61P 9/00 - Drugs for disorders of the cardiovascular system

Abstract

Provided in the present invention is a joint product comprising a phentermine immediate-release pellet and a topiramate sustained-release pellet. The topiramate pellet comprises: a. a blank pellet core; b. an active medicament layer without adhesive agents and containing only topiramate, where the layer is arranged on the surface of the blank pellet core; and, c. a sustained-release coating layer containing an ethyl cellulose and PVP K30, where the sustained-release coating layer is arranged on the exterior of the active medicament layer. Also disclosed is a preparation method for the joint product.

IPC Classes  ?

• A61K 9/16 - Agglomerates; Granulates; Microbeadlets
• A61K 9/52 - Sustained or differential release type
• A61K 31/35 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
• A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel

Abstract

Provided in the present invention is a joint product containing synephrine and topiramate, where the synephrine or a salt thereof is administered in the form of an immediate-release preparation, preferably an immediate-release pellet, with a daily dosage between 2 mg and 25 mg, preferably between 5 mg and 20 mg, and where the topiramate is administered in the form of a sustained-release or controlled-release preparation, preferably a sustained-release pellet, with a daily dosage between 20 mg and 100 mg, preferably between 23 mg and 92 mg. The composition is for use in treatment of obesity and other diseases related to obesity.

IPC Classes  ?

• A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
• A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
• A61K 9/30 - Organic coatings
• A61K 9/16 - Agglomerates; Granulates; Microbeadlets
• A61P 3/04 - Anorexiants; Antiobesity agents

Abstract

A 3-oxo-3,4-dihydro-2-pyrazine-formamide derivative, a pharmaceutical composition of same, a method for preparing same, and a use thereof. Specifically, a compound as represented by formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof, where R1 is either hydrogen or a halogen, where R2 and R3 are independently selected from: hydrogen, (C1-6 alkyl acyloxy)-C1-6 alkyl, 1-(C1-6 alkyl acyloxy)-C1-6 alkyl, tetrahydrofuranyl, tetrahydropyranyl, and hydroxy- or halogen-substituted C1-6 alkyl, and where the halogen is selected from fluorine, chlorine, bromine, and iodine, also, when R2 and R3 simultaneously are hydrogen, R1 can neither be hydrogen nor fluorine. The compound as represented by formula (I) can be in vivo converted into the corresponding 6-R1-3-oxo-3,4-dihydro-2-pyrazine-formamide and thus exerting antiviral efficacy. Compared with 6-R1-3-oxo-3,4-dihydro-2-pyrazine-formamide, the parent medicament, the compound as represented by formula (I) has increased bioavailability and extended period of in vivo efficacy.

IPC Classes  ?

• C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• 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 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 31/4965 - Non-condensed pyrazines
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61P 31/12 - Antivirals
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses

Abstract

A topiramate sustained-release pharmaceutical composition comprising no binders. The topiramate sustained-release pharmaceutical composition is a sustained-release pellet, comprising a blank pill core, a medicament layer, and a sustained-release coating layer.

IPC Classes  ?

• A61K 9/22 - Sustained or differential release type
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61K 47/38 - Cellulose; Derivatives thereof
• A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
• A61P 25/06 - Antimigraine agents
• A61P 25/08 - Antiepileptics; Anticonvulsants
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/24 - Antidepressants
• A61P 25/18 - Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• A61P 9/12 - Antihypertensives

Abstract

Provided in the present invention is a polypeptide, which is capable of inhibiting fusion of the HIV or other related enveloped viruses with a target cell, while the polypeptide has a sequence as expressed by SEQ ID NO: 1-42. Also provided in the present invention are a use of the polypeptide in preparing an HIV fusion inhibitor, a use in preparing a medicament for use in the treatment or prevention of HIV infection-related diseases, particularly the acquired immunodeficiency syndrome, and a use in preparing a medicament for use in the treatment or prevention of infections by the other related enveloped viruses.

IPC Classes  ?

• C07K 14/08 - RNA viruses
• C07K 14/16 - HIV-1
• C12N 15/40 - Proteins from RNA viruses, e.g. flaviviruses
• C12N 15/49 - Lentiviridae, e.g. immunodeficiency viruses such as HIV, visna-maedi virus, equine infectious anaemia virus
• C12N 15/63 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/18 - Antivirals for RNA viruses for HIV

Abstract

Disclosed are an HIV-inhibiting polypeptide and a target site thereof. The polypeptide comprises 11 amino acid residues in direct contact with the NHR of the HIV-1, where two of the amino acid residues are located respectively at the N-end and the C-end of the polypeptide. Also disclosed are a target site of the polypeptide and a medicinal use thereof. The polypeptide does not comprise a binding-pocket domain generally recognized as necessary for maintaining a high activity, is capable of inhibiting the HIV, particularly HIV strains having drug resistance against existing fusion inhibitors, and can be used in combating HIV infections.

IPC Classes  ?

• C07K 14/16 - HIV-1
• C07K 1/04 - General processes for the preparation of peptides on carriers
• C07K 1/16 - Extraction; Separation; Purification by chromatography
• C12N 15/49 - Lentiviridae, e.g. immunodeficiency viruses such as HIV, visna-maedi virus, equine infectious anaemia virus
• A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61P 31/18 - Antivirals for RNA viruses for HIV
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

Disclosed are a polypeptide for use in inhibiting the HIV, a pharmaceutical composition comprising the polypeptide, and a use thereof. The polypeptide comprises the sequence as expressed by SEQ ID NO: 8 or by SEQ ID NO: 9. The polypeptide comprise neither a pocket-binding domain nor a lipid membrane-binding domain generally recognized as necessary for high activity polypeptide fusion inhibitors, and the polypeptide is of a reduced length, but the polypeptide exhibits an increased anti-HIV activity.

IPC Classes  ?

• C07K 14/16 - HIV-1
• C12N 15/49 - Lentiviridae, e.g. immunodeficiency viruses such as HIV, visna-maedi virus, equine infectious anaemia virus
• C12N 15/63 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
• C12N 1/19 - Yeasts; Culture media therefor modified by introduction of foreign genetic material
• C12N 1/21 - Bacteria; Culture media therefor modified by introduction of foreign genetic material
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61P 31/18 - Antivirals for RNA viruses for HIV

Abstract

Provided are N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof. The above compounds have the dual activities of 5-hydroxytryptamine 1A receptor ligand and selective serotonin reuptake inhibitor. The preparation methods of the above compounds, the uses of these compounds for the prevention or treatment of nervous system diseases related to 5-hydroxytryptamine system dysfunction and the pharmaceutical compositions containing these compounds are also provided.

IPC Classes  ?

• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
• A61K 31/505 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• C07D 211/68 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
• C07D 239/02 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
• 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

Abstract

4 are defined as in the specification. Preparation methods of said compounds and use of said compounds in treating and/or preventing central nervous system disease associated with TSPO functional disorder

IPC Classes  ?

• A61K 31/535 - 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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
• C07D 471/04 - Ortho-condensed systems

Abstract

Provided are piperazinyl pyrimidine derivatives of formula I having CCR4 antagonism, and the preparation method, pharmaceutical composition and use thereof in the preparation of a medicament. The medicament is useful for the treatment and prevention of CCR4-related diseases. (see formula I)

IPC Classes  ?

• 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
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 11/06 - Antiasthmatics
• A61P 17/00 - Drugs for dermatological disorders

Abstract

Disclosed are pyridazine derivatives represented by Formula I or pharmaceutically acceptable salts or hydrates thereof, pharmaceutical compositions comprising the compounds, methods of treating and/or preventing diseases or disorders associated with viral infections in patients using the compounds, and the use of the compounds in preparing the medicaments for treating and/or preventing diseases or disorders associated with viral infections. The compounds represented by Formula I have antiviral activity, especially anti-microRNA viral activity. Symbols in the compounds represented are described in the specification.

IPC Classes  ?

• A61K 31/501 - Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
• C07D 237/20 - Nitrogen atoms

Abstract

Provided are piperazinyl pyrimidine derivatives of formula I having CCR4 antagonism, and the preparation method, pharmaceutical composition and use thereof in the preparation of a medicament. The medicament is useful for the treatment and prevention of CCR4-related diseases.

IPC Classes  ?

• 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
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 11/06 - Antiasthmatics
• A61P 17/00 - Drugs for dermatological disorders

Abstract

Provided in the present invention are a polypeptide and the derivative and stereoisomer or salt without physiological toxicity thereof as shown in formula I. The polypeptide is an artificially designed anti-HIV infection polypeptide. Also provided in the present invention are pharmaceutical compositions containing the polypeptide and the derivative and stereoisomer or salt without physiological toxicity thereof, and the use of the polypeptide and the derivative and stereoisomer or salt without physiological toxicity thereof in treating or preventing related diseases caused by the HIV infection.

IPC Classes  ?

• C07K 19/00 - Hybrid peptides
• C07K 14/00 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61P 31/18 - Antivirals for RNA viruses for HIV

Abstract

Disclosed is a small molecule-polypeptide conjugate resisting HIV infection as shown in formula I, or a stereoisomer or physiologically non-toxic salt thereof. Also disclosed are a pharmaceutical composition containing the conjugate, or the stereoisomer or physiologically non-toxic salt thereof, and the use of the conjugate, or the stereoisomer or physiologically non-toxic salt thereof in treating or preventing diseases resulting from an HIV infection, especially Acquired Immunodeficiency Syndrome (AIDS).

IPC Classes  ?

• C07K 14/16 - HIV-1
• A61K 38/16 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
• A61P 31/18 - Antivirals for RNA viruses for HIV

Abstract

Provided is a medical adhesive with good biodegradable performance capable of cross-linking and copolymerizing, comprising a mono-α-cyanoacrylate and a bis-α-cyanoacrylic acid diol ester monomer molecule. The olefinic bonds in the mono-α-cyanoacrylate structure are polymerized in the presence of infinitesimal anions to form a solid 3D type high polymer; the 3D type high polymer is provided with degradation sites on the web-like backbone chain, with clear degradation path and absorbable degradation products. The medical adhesive can be used for wound adhesive, large area wound hemostasia, and visceral and soft tissue wound closure. Furthermore, the medical adhesive also has the potential to be used as a tissue engineering material.

IPC Classes  ?

• A61L 24/06 - Surgical adhesives or cements; Adhesives for colostomy devices containing macromolecular materials obtained by reactions only involving carbon-to-carbon unsaturated bonds
• C09J 4/04 - Cyanoacrylate monomers
• C09J 135/04 - Homopolymers or copolymers of nitriles
• C08L 35/04 - Homopolymers or copolymers of nitriles
• C08F 222/32 - Alpha-cyano-acrylic acid; Esters thereof

Abstract

tubercle bacillus infection, is provided.

IPC Classes  ?

• C07C 215/08 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with only one hydroxy group and one amino group bound to the carbon skeleton
• C07C 215/30 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton
• C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
• A61K 31/045 - Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
• A61K 31/133 - Amines, e.g. amantadine having hydroxy groups, e.g. sphingosine

Abstract

Disclosed are 3-oxo-3, 4-dihydro-2-pyrazineformamide derivatives, pharmaceutical compositions, preparation methods, and uses thereof. Concretely, disclosed are the compounds shown as the formula Ⅰ, their pharmaceutically acceptable salts, their hydrates, or their solvates, wherein R1 is H or halogen; R2 and R3 are independently selected from H,(C1-6 alkylacyloxy)-C1-6 alkyl, 1-(C1-6 alkylacyloxy)-C1-6 alkyl, tetrahydrofuranyl, tetrahydropyranyl, and C1-6 alkyl substituted with OH or halogen, wherein the said halogen is selected from F, Cl, Br, and I; and when both of R2 and R3 are H, R1 cannot be H or F. The compounds of formula Ⅰ may be converted into corresponding 6-R1-3-oxo-3,4-dihydro-2-pyrazineformamide in vivo for treating virus. Compared with 6-R1-3-oxo-3,4-dihydro-2-pyrazineformamide, the compounds of formula Ⅰ show higher bioavailability and longer period of effect time in vivo.

IPC Classes  ?

• C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• 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 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 31/4965 - Non-condensed pyrazines
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61P 31/12 - Antivirals
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses

Abstract

Disclosed are a method for the preparation of 3-butoxy-2-pyrazineformamide and use thereof, specifically the use of 3-butoxy-2-pyrazineformamide, pharmaceutically acceptable salts, hydrates or solvates thereof in the preparation of anti-virus drugs. By transforming into T1105 in vivo, 3-butoxy-2-pyrazineformamide shows anti-virus activity, evidently improves oral bioavailability of T1105 and extends the duration of action of T1105 in vivo.

IPC Classes  ?

• C07D 241/18 - Oxygen or sulfur atoms
• C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 241/08 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
• A61K 31/4965 - Non-condensed pyrazines
• A61P 31/12 - Antivirals
• A61P 31/14 - Antivirals for RNA viruses

Abstract

Disclosed are a 3-alkoxy-substituted-2-pyrazinyl formamide compound having a structure represented by formula I and use thereof in preparing anti-viral medications. The compound disclosed exerts anti-viral effects in vivo by means of metabolism into T1105 or T705 through esterate or P450 enzyme.

IPC Classes  ?

• C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• A61K 31/4965 - Non-condensed pyrazines
• A61P 31/14 - Antivirals for RNA viruses