Abstract

1-61-6 alkyl. The present application also relates to the use of the compound or the pharmaceutically acceptable salt thereof for preparing a drug for resisting gram-negative bacteria, and a method for preparing the compound or the pharmaceutically acceptable salt thereof.

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
• A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
• A61P 31/04 - Antibacterial agents

Abstract

The chemotactic binding ability of CCL13 and an immune cell surface receptor such as DC cells is used to transport different antigenic proteins to the surface of the DC cells, the efficiency of phagocytosis, processing, and presentation of various antigenic proteins by the DC cells is improved, and the effect of preventing and treating related diseases of the antigenic proteins is enhanced. A T2 sequence is further added in an antigen, such that the immune effect can be enhanced.

IPC Classes  ?

• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• A61K 39/12 - Viral antigens
• C07K 14/52 - CytokinesLymphokinesInterferons
• C12N 7/00 - Viruses, e.g. bacteriophagesCompositions thereofPreparation or purification thereof
• C12N 15/62 - DNA sequences coding for fusion proteins

Abstract

A cyclic basic lipopeptide compound, and a preparation method therefor and a use thereof. The compound has a structure represented by general formula I, wherein AA represents amino acid. The preparation method for a cyclic lipopeptide compound comprises the following steps: (1) reacting an Fmoc-AA-OP side chain free amino group of a protected basic amino acid with a halogenated resin to obtain Fmoc-AA-OP-resin; (2) coupling Fmoc-AA-OP-resin one by one to obtain a linear polypeptide-resin; (3) selectively removing a protective group from the linear polypeptide-resin and carrying out solid-phase cyclization on the linear polypeptide-resin to obtain a cyclic polypeptide-resin; (4) carrying out acidolysis and ether precipitation on the cyclic polypeptide-resin to obtain a cyclic polypeptide crude product; and (5) carrying out purification and/or salt conversion and lyophilization on the cyclic polypeptide crude product to obtain a cyclic polypeptide pure product. The cyclic lipopeptide compound can be used for preparing antibacterial drugs, and particularly used for preparing antibacterial drugs having improved antibacterial activity and reduced renal toxicity, comprising an antibacterial drug against carbapenem drug-resistant "super bacteria". R0-CO-AA1-AA2-D/L-AA3-ring(4-10)[Dab4-AA5-D/L-AA6-AA7-AA8-AA9-AA10] I.

IPC Classes  ?

• C07K 7/62 - PolymyxinsRelated peptides
• A61K 38/12 - Cyclic peptides
• A61P 31/04 - Antibacterial agents

Abstract

The present invention relates to a pharmaceutical composition comprising a β-lactam compound of formula (I), or a stereoisomer, a solvate or a pharmaceutically acceptable salt or ester thereof, and a lactamase inhibitor or an efflux pump inhibitor, and the use thereof for inhibiting microorganisms, particularly bacteria, especially Gram-negative bacteria, wherein each symbol in formula (I) is as defined in the description. The present invention relates to a pharmaceutical composition comprising a β-lactam compound of formula (I), or a stereoisomer, a solvate or a pharmaceutically acceptable salt or ester thereof, and a lactamase inhibitor or an efflux pump inhibitor, and the use thereof for inhibiting microorganisms, particularly bacteria, especially Gram-negative bacteria, wherein each symbol in formula (I) is as defined in the description.

IPC Classes  ?

• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
• A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
• A61K 31/69 - Boron compounds
• A61P 31/04 - Antibacterial agents

Abstract

The present invention relates to a group of IMB-C5 series compounds having anti-coronavirus activity and the application thereof. The structure of the IMB-C5 series compounds is as shown in formula (1). The application is an application of the IMB-C5 series compounds in preparing a drug. The drug is a drug for inhibiting coronavirus, and is preferably a drug for treating human coronavirus infection. The coronavirus is preferably human α-coronavirus or human β-coronavirus, especially novel coronavirus (SARS-COV-2).

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• A61P 31/14 - Antivirals for RNA viruses
• C07D 487/14 - Ortho-condensed systems

Abstract

Disclosed in the present invention are a perinaphthenone compound and the use thereof. The compound can bind to E3 ubiquitin ligase tripartite motif 25 (TRIM25), thereby facilitating the recognition of TRIM25 to a pathogen and inducing proteasome-dependent ubiquitination degradation of the pathogen protein. The compound is expected to be used as a ligand for TRIM25 and have a broad application, for example, for preparing a PROTAC molecule. Therefore, the compound has good research and development value and application prospects.

IPC Classes  ?

• C07C 50/34 - Quinones containing groups having oxygen atoms singly bound to carbon atoms the quinoid structure being part of a condensed ring system having three rings
• A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
• A61K 31/202 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having three or more double bonds, e.g. linolenic acid
• 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 31/341 - 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 31/351 - 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 not condensed with another ring
• 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 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
• C07C 50/38 - Quinones containing —CHO or non-quinoid keto groups
• C07C 59/52 - Unsaturated compounds containing hydroxy or O-metal groups a hydroxy or O-metal group being bound to a carbon atom of a six-membered aromatic ring
• C07C 69/145 - Acetic acid esters of monohydroxylic compounds of unsaturated alcohols
• C07D 307/12 - Radicals substituted by oxygen atoms
• C07D 309/24 - Methylol radicals
• C07D 317/12 - Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
• C12N 1/14 - Fungi Culture media therefor
• C12R 1/66 - Aspergillus

Abstract

A biosynthetic gene cluster of tropolone compounds isatropolones, and a directed high-yield strain. The gene cluster comprises genes isaF, isaJ, and isaS; the gene sequence of isaF is as shown in SEQ ID NO 1; the gene sequence of isaJ is as shown in SEQ ID NO. 3; and the gene sequence of isaS is as shown in SEQ ID NO. 5. The directed high-yield strain is: (1) a strain of directed high-yield isatropolone A: a strain that uses Streptomyces sp.CGMCC No. 15540 as a host, and overexpresses isaF while disrupting gene isaJ of the host or disrupting gene isaS of the host; or (2) a strain of directed high-yield isatropolone C: a strain that uses Streptomyces sp.CGMCC No. 15540 as a host, and overexpresses genes isaF and isaS, or overexpresses genes isaJ and isaS, or overexpresses genes isaF, isaJ and isaS.

IPC Classes  ?

• C12N 15/31 - Genes encoding microbial proteins, e.g. enterotoxins
• C07K 14/36 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from bacteria from ActinomycesPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from bacteria from Streptomyces (G)
• C12N 15/76 - Vectors or expression systems specially adapted for prokaryotic hosts other than E. coli, e.g. Lactobacillus, Micromonospora for ActinomycesVectors or expression systems specially adapted for prokaryotic hosts other than E. coli, e.g. Lactobacillus, Micromonospora for Streptomyces
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• C12P 17/18 - Preparation of heterocyclic carbon compounds with only O, N, S, Se, or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin

Abstract

A biomarker miR-32533 for cognitive impairment-related diseases and use thereof. The miR-32533 comprises a nucleotide sequence represented by SEQ ID NO. 1, can be used as a biomarker for detecting cognitive disorder impairment-diseases, especially Alzheimer's disease (AD), and is able to specifically bind to a CREB5 gene, reduce the expression level of the CREB5 gene, and inhibit the generation of extracellular β-amyloid (Aβ), thus being capable of effectively preventing and treating AD.

IPC Classes  ?

• C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
• 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

Provided are an isolated monoclonal antibody or an antigen-binding fragment thereof against Trop2, and use of the antibody or fragment in tumor treatment and diagnosis.

IPC Classes  ?

• C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
• C12N 15/13 - Immunoglobulins
• A61P 35/00 - Antineoplastic agents
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• C12N 5/12 - Fused cells, e.g. hybridomas

Abstract

Provided in the present invention is a biomarker miR-25802 cluster for inflammation-related diseases, wherein the miR-25802 cluster can also be used as a target for treating inflammation-related diseases.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
• C12N 15/11 - DNA or RNA fragmentsModified forms thereof
• A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
• 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

This disclosure related to a group of peptide derivative Omicsynins with antiviral activity against influenza virus and coronavirus. It also related uses of these derivatives, the chemical formula of the peptide derivative Omicsynins is shown in formula (1): This disclosure related to a group of peptide derivative Omicsynins with antiviral activity against influenza virus and coronavirus. It also related uses of these derivatives, the chemical formula of the peptide derivative Omicsynins is shown in formula (1): This disclosure related to a group of peptide derivative Omicsynins with antiviral activity against influenza virus and coronavirus. It also related uses of these derivatives, the chemical formula of the peptide derivative Omicsynins is shown in formula (1): R1—R4 are shown in the following table. NO. substituent1 substituent2 substituent3 R1 Basic amino-acid side chains including lysine, histidine, citrulline residues, and etc. R2 —CH(CH3)2, —CH(CH3)CH2CH3 —CH2CH(CH3)2 Neutral amino-acid side chain including tryptophan, serine, threonine, cysteine residues and etc. R3 R3 including tyrosine, lysine, histidine, citrulline residues, and etc. R4 —CH2OH —CHO R4 including —CH2NH2, —CH═NH,— CH═NOH, —COOH, —COOR5 (R5 represents alkyl groups containing 1-3 carbons), -CONH2 and etc.

IPC Classes  ?

• C07K 14/36 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from bacteria from ActinomycesPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from bacteria from Streptomyces (G)
• A61P 31/12 - Antivirals

Abstract

The present invention provides use of berbamine dihydrochloride in preparation of an Ebola virus inhibitor. In the present invention, the primed glycoprotein of the Ebola virus (EBOV-GPcl) is taken as a target site, and an antiviral active compound with the capability of binding to the EBOV-GPcl, i.e., berbamine dihydrochloride, is obtained through structure-based virtual screening. Berbamine dihydrochloride can specifically inhibit the entry of an Ebola recombinant virus by binding to the target protein EBOV-GPcl, thereby achieving the effect of anti-Ebola virus infection. The half-maximum effect concentration (EC50) of berbamine dihydrochloride against EBOV is 0.49 μM, which indicates that berbamine dihydrochloride has a strong inhibition effect on EBOV.

IPC Classes  ?

• A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
• A61P 31/14 - Antivirals for RNA viruses

Abstract

A polypeptide compound and a preparation method therefor and an application thereof. The polypeptide compound has a structure as shown in formula I. The polypeptide compound can significantly improve the spatial learning and memory capabilities of an Aβ-mediated cognitive impairment mice. In addition, some of the polypeptide compounds have low toxicity, show relatively low toxicity in renal cell (Vero) toxicity detection and hemolytic (rabbit whole blood) detection, and can be used for preparing drugs having NK cell-related immunomodulatory effects, treating inflammation-related diseases or diagnosing and treating nervous system diseases. The polypeptide compound can be used alone or in combination with another or more other active ingredients for treatment, prevention, inhibition or amelioration of diseases or symptoms, wherein the combined use of the drugs is safer or more effective than the use of any one of the drugs alone.

IPC Classes  ?

• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• A61K 38/08 - Peptides having 5 to 11 amino acids
• A61K 38/04 - Peptides having up to 20 amino acids in a fully defined sequenceDerivatives thereof
• A61P 37/02 - Immunomodulators
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

Provided are a pyrimidinone derivative, and a preparation method therefor and the use thereof against Mycobacterium tuberculosis infection. The structure of the pyrimidinone derivative is represented by formula 1. Experiments prove that the pyrimidinone derivative has obvious anti-Mycobacterium tuberculosis activity and is particularly suitable for preparing a drug for preventing and/or treating related diseases caused by Mycobacterium tuberculosis. Provided are a pyrimidinone derivative, and a preparation method therefor and the use thereof against Mycobacterium tuberculosis infection. The structure of the pyrimidinone derivative is represented by formula 1. Experiments prove that the pyrimidinone derivative has obvious anti-Mycobacterium tuberculosis activity and is particularly suitable for preparing a drug for preventing and/or treating related diseases caused by Mycobacterium tuberculosis.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems

Abstract

A use of CCL26. Different antigen proteins are delivered to the surfaces of DC cells by utilizing a chemotactic binding capacity of CCL26 to surface receptors of immune cells such as the DC cells, so that the efficiency of phagocytosis, processing and presentation of different antigen proteins by the DC cells is improved, and the effect of preventing and treating related diseases is improved by further adding a T2 sequence into an antigen. The T2 sequence has a very strong immunological enhancement effect by means of experimental determination, and can further excite body fluid and cellular immune response in the process of promoting antigen presentation, thereby finally achieving the effect of inhibiting related tumor growth.

IPC Classes  ?

• C07K 19/00 - Hybrid peptides
• C12N 15/62 - DNA sequences coding for fusion proteins
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• A61K 39/12 - Viral antigens
• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants

Abstract

The present invention relates to the field of molecular biology, and in particular relates to the use of CXCL14. According to the present invention, different antigen proteins are transferred to the surface of a DC cell by means of the chemotactic binding capacity of CXCL14 and surface receptors of immune cells such as DC cells. A chemokine of CXCL14 can effectively induce the binding of an antigen molecule to a specific immune cell at the N-terminal of an antigen protein, such that the cross presentation effect of the antigen molecule is greatly enhanced, and CXCL14 can finally induce a stronger specific immune response of the antigen molecule. In addition, in the present invention, the T2 sequence is further added to the antigen to enhance the immune effect, and the T2 polypeptide can effectively enhance the immune intensity of an antigen molecule in the cell immune process at the C-terminal of the antigen protein, increases the number of specific T cells, achieves the decisive effect of an immune enhancer, improves the efficiency of phagocytosis, processing and presentation of various antigen proteins by DC cells, and improves the effect of DC cells in preventing and treating related diseases.

IPC Classes  ?

• C07K 19/00 - Hybrid peptides
• C07K 14/52 - CytokinesLymphokinesInterferons
• C12N 15/09 - Recombinant DNA-technology
• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• A61P 31/12 - Antivirals
• A61P 37/04 - Immunostimulants

Abstract

The chemotactic binding ability of CCL13 and an immune cell surface receptor such as DC cells is used to transport different antigenic proteins to the surface of the DC cells, the efficiency of phagocytosis, processing, and presentation of various antigenic proteins by the DC cells is improved, and the effect of preventing and treating related diseases of the antigenic proteins is enhanced. A T2 sequence is further added in an antigen, such that the immune effect can be enhanced.

IPC Classes  ?

• C07K 19/00 - Hybrid peptides
• C12N 15/62 - DNA sequences coding for fusion proteins
• C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
• C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
• A61K 39/12 - Viral antigens
• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• A61K 39/385 - Haptens or antigens, bound to carriers
• A61P 31/20 - Antivirals for DNA viruses
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to the technical field of vaccine preparation, and in particular to an immune-enhancing delivery system formed by targeted antigen delivery by CCL11. The system further enhances immunogenicity by fusing a chemokine CCL11 with a corresponding antigen molecule, and adding a T2 label at a terminal of the antigen molecule. The system can be a nucleic acid vector or a fusion protein or the like to be applied to prevention and/or treatment of diseases caused by a corresponding antigen. According to the present invention, by utilizing a chemotactic binding capacity of CCL11 with a surface receptor of an immune cell such as a DC, different antigen proteins are transported to the surface of the DC, so that the efficiency of phagocytosis, processing and presentation of the DC on various antigen proteins is improved, and the effect of preventing and treating related diseases is improved. The key point of the present invention is that a T2 sequence added to an antigen can enhance an immune response.

IPC Classes  ?

• C07K 19/00 - Hybrid peptides
• C07K 14/52 - CytokinesLymphokinesInterferons
• C12N 15/09 - Recombinant DNA-technology
• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• A61P 31/12 - Antivirals
• A61P 37/04 - Immunostimulants

Abstract

The present invention relates to a pharmaceutical composition containing a β-lactam compound of formula (I), or a stereoisomer, a solvate or a pharmaceutically acceptable salt or ester thereof, and a lactamase inhibitor or efflux pump inhibitor, and the use thereof for resisting microorganisms, particularly bacteria, especially gram-negative bacteria, wherein each code in formula (I) is as defined in the description.

IPC Classes  ?

• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
• 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
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
• A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
• A61K 31/69 - Boron compounds
• A61K 38/05 - Dipeptides
• A61P 31/04 - Antibacterial agents

Abstract

Disclosed in the present invention are a perinaphthenone compound and the use thereof. The compound can bind to E3 ubiquitin ligase tripartite motif 25 (TRIM25), thereby facilitating the recognition of TRIM25 to a pathogen and inducing proteasome-dependent ubiquitination degradation of the pathogen protein. The compound is expected to be used as a ligand for TRIM25 and have a broad application, for example, for preparing a PROTAC molecule. Therefore, the compound has good research and development value and application prospects.

IPC Classes  ?

• C07C 50/38 - Quinones containing —CHO or non-quinoid keto groups
• C07C 49/743 - Unsaturated compounds containing a keto group being part of a ring containing hydroxy groups having unsaturation outside the rings, e.g. humulones, lupulones
• C07C 50/34 - Quinones containing groups having oxygen atoms singly bound to carbon atoms the quinoid structure being part of a condensed ring system having three rings
• C07D 317/26 - Radicals substituted by doubly bound oxygen or sulfur atoms or by two such atoms singly bound to the same carbon atom
• C07D 309/22 - Radicals substituted by oxygen atoms
• A61P 31/12 - Antivirals
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/20 - Antivirals for DNA viruses
• A61P 31/22 - Antivirals for DNA viruses for herpes viruses
• C12R 1/66 - Aspergillus
• C12P 15/00 - Preparation of compounds containing at least three condensed carbocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are a benzyl piperazine compound, a preparation method there for and an application thereof in an antivirus. The benzyl piperazine compound has a structure represented by the following general formula(I). It is proven by experiments that the benzyl piperazine compound not only has significant antiviral activity, but also has the advantages of low cytotoxicity, a high selectivity index and soon.

IPC Classes  ?

• 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
• C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
• C07D 207/14 - Nitrogen atoms not forming part of a nitro radical
• C07D 207/325 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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 with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
• C07D 211/56 - Nitrogen atoms
• C07D 211/58 - Nitrogen atoms attached in position 4
• C07D 213/36 - Radicals substituted by singly-bound nitrogen atoms
• C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
• C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
• C07D 241/12 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
• 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

The disclosure relates to an indolo[2′,3′:3,4]pyrido[2,1-b]quinazoline compound represented by general formula (I) and use thereof in the manufacture of (1) a medicament for treating a cardiovascular and cerebrovascular disease, (2) a formulation for increasing expression of AMPK, ABCA1 and SR-BI, (3) a formulation for activating nuclear receptors (NRs), and inhibiting activity of NLRP3, IL-1β, NF-κB and MAPKs, (4) a formulation for promoting cellular cholesterol efflux; or (5) a medicament for anti-inflammation. The disclosure relates to an indolo[2′,3′:3,4]pyrido[2,1-b]quinazoline compound represented by general formula (I) and use thereof in the manufacture of (1) a medicament for treating a cardiovascular and cerebrovascular disease, (2) a formulation for increasing expression of AMPK, ABCA1 and SR-BI, (3) a formulation for activating nuclear receptors (NRs), and inhibiting activity of NLRP3, IL-1β, NF-κB and MAPKs, (4) a formulation for promoting cellular cholesterol efflux; or (5) a medicament for anti-inflammation.

IPC Classes  ?

• C07D 471/14 - Ortho-condensed systems
• C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
• C07D 498/14 - Ortho-condensed systems
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 3/06 - Antihyperlipidemics
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present invention relates to a group of IMB-C5 series compounds having anti-coronavirus activity and an application thereof. The structure of the IMB-C5 series compounds is as shown in formula (1). The application is an application of the IMB-C5 series compounds in preparing a drug. The drug is a drug for inhibiting coronavirus, and is preferably a drug for treating human coronavirus infection. The coronavirus is preferably human α-coronavirus or human β-coronavirus, especially novel coronavirus (SARS-CoV-2).

IPC Classes  ?

• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• C07D 473/04 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
• A61P 31/14 - Antivirals for RNA viruses

Abstract

The present invention relates to the use of an exogenous ATG10S protein in the preparation of an antiviral drug. The exogenous ATG10S is an rhATG10S protein, the coding nucleotide sequence thereof is as shown in SEQ ID NO: 1 or SEQ ID NO: 2, and the amino acid sequence of the rhATG10S protein is as shown in SEQ ID NO: 3. The present invention also relates to the use of the rhATG10S protein in the preparation of a drug for inhibiting viruses, and a method for screening antiviral drugs by means of taking the ATG10S protein as a target.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
• A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
• A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/18 - Antivirals for RNA viruses for HIV
• A61P 31/20 - Antivirals for DNA viruses
• C12R 1/19 - Escherichia coli

Abstract

The present disclosure is related to the field of enzyme inhibitors, and in particular to a hydroxamic acid derivative, a method for producing the same and use thereof. The hydroxamic acid group of the hydroxamic acid derivative can be chelated with zinc ions in the LpxC active area, and the derivative has a hydrophobic side chain which can bind to hydrophic channels in the enzyme LpxC. These guarantee that the hydroxamic acid derivative has good bactericidal activity against Gram-negative bacteria and low toxicity. The present disclosure also provides a method for producing the hydroxamic acid derivative, which requires a shorter reaction time and can provide the derivative with a high yield.

IPC Classes  ?

• A61P 31/04 - Antibacterial agents
• C07D 295/155 - 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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• C07D 295/195 - Radicals derived from nitrogen analogues of carboxylic acids
• C07D 295/215 - Radicals derived from nitrogen analogues of carbonic acid
• 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
• C07C 41/30 - Preparation of ethers by reactions not forming ether-oxygen bonds by increasing the number of carbon atoms, e.g. by oligomerisation
• C07C 51/09 - Preparation of carboxylic acids or their salts, halides, or anhydrides from carboxylic acid esters or lactones
• C07C 67/343 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisationPreparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by change of size of the carbon skeleton by increase in the number of carbon atoms
• C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
• C07C 269/06 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups

Abstract

11-121-61-3225521-121-61-3223244441-121-12; and V, W, X, Y, and Z are independently selected from carbon or nitrogen. The diarylamine compound provided in the present application has androgen receptor-inhibiting activity.

IPC Classes  ?

• C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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
• C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
• C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
• C07D 277/28 - Radicals substituted by nitrogen 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
• A61P 5/26 - Androgens
• A61P 35/00 - Antineoplastic agents
• A61P 13/08 - Drugs for disorders of the urinary system of the prostate
• A61P 15/00 - Drugs for genital or sexual disordersContraceptives
• A61P 17/08 - Antiseborrheics
• A61P 17/10 - Anti-acne agents
• A61P 17/00 - Drugs for dermatological disorders
• A61K 31/415 - 1,2-Diazoles
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/42 - Oxazoles
• A61K 31/426 - 1,3-Thiazoles

Abstract

Provided are a pyrimidinone derivative, and a preparation method therefor and the use thereof against Mycobacterium tuberculosis infection. The structure of the pyrimidinone derivative is represented by formula I. Experiments prove that the pyrimidinone derivative has obvious anti-Mycobacterium tuberculosis activity and is particularly suitable for preparing a drug for preventing and/or treating related diseases caused by Mycobacterium tuberculosis.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 31/06 - Antibacterial agents for tuberculosis

Abstract

12344 independently represents a hydrogen atom or a C1-10 linear or branched alkyl optionally having a substituent or a C6-12 aryl optionally having a substituent, or the two together form a cycloalkyl with 3 to 8 ring carbon atoms; X represents C or N; and Y represents a linear or branched alkenyl or alkynyl with 2 to 6 carbon atoms and optionally having a substituent, or a carboxyl). The compound has good antibacterial properties against bacteria, especially gram-negative bacteria, has low drug resistance, and has good prospects for the effective treatment of various conditions.

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
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/433 - Thiadiazoles
• A61P 31/04 - Antibacterial agents

Abstract

A novel stenotrophomonas species and an application thereof. The representative strain of the novel stenotrophomonas species is Stenotrophomonas nematodicola strain W5. The preservation number of the strain in the China General Microbiological Culture Collection Center is CGMCC No. 19401. The Stenotrophomonas nematodicola strain W5 has a nematode prebiotic function; a proper amount of nematodes are beneficial to maintain the stability of a soil ecosystem.

IPC Classes  ?

• C12N 1/20 - BacteriaCulture media therefor
• A01N 63/20 - BacteriaSubstances produced thereby or obtained therefrom
• A01P 19/00 - Pest attractants
• A01P 5/00 - Nematocides
• C12R 1/01 - Bacteria or actinomycetales

Abstract

144 are as shown in the following table. The viruses mentioned are influenza and coronavirus.

IPC Classes  ?

• A61K 38/05 - Dipeptides
• A61P 31/14 - Antivirals for RNA viruses
• C12N 1/20 - BacteriaCulture media therefor
• C12N 15/31 - Genes encoding microbial proteins, e.g. enterotoxins

Abstract

Disclosed is an anti-infection use of a class of thiazole-containing compounds. The thiazole-containing compounds can inhibit the production of virulence factors of Gram-negative bacteria and Gram-positive bacteria by means of interfering with the bacterial quorum-sensing system. ML364 can respectively increase the survival rate of mice with systemic infection caused by carbapenem-resistant Pseudomonas aeruginosa and methicillin-resistant Staphylococcus aureus by 60% .

IPC Classes  ?

• A61K 31/426 - 1,3-Thiazoles
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• C07D 277/46 - Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
• 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 31/04 - Antibacterial agents

Abstract

Disclosed are a benzyl piperazine compound, a preparation method therefor and an application thereof in an antivirus. The benzyl piperazine compound has a structure represented by the following general formula (I). It is proven by experiments that the benzyl piperazine compound not only has significant antiviral activity, but also has the advantages of low cytotoxicity, a high selectivity index and so on.

IPC Classes  ?

• 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
• C07D 295/155 - 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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• C07D 211/56 - Nitrogen atoms
• C07D 207/325 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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 with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
• C07D 211/26 - 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 with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
• C07D 207/09 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/20 - Antivirals for DNA viruses
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses

Abstract

The present invention relates to the technical field of natural medicine, and specifically relates to acquiring Secoemestrin C from microorganisms, particularly from fungal fermentation products, and the use of pharmaceutical salts thereof in the preparation and treatment of cancer-related diseases such as lung cancer, pancreatic cancer, colon cancer, breast cancer, gastric cancer, and liver cancer. The Secoemestrin C of the present invention or the pharmaceutical salt thereof have the structure shown in (I).

IPC Classes  ?

• C07D 513/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains four or more hetero rings
• A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
• A61P 35/00 - Antineoplastic agents
• C12N 1/14 - Fungi Culture media therefor
• C12P 17/18 - Preparation of heterocyclic carbon compounds with only O, N, S, Se, or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
• C12R 1/645 - Fungi

Abstract

The present invention relates a group of tetrahydroindoloquinazoline compounds and the use thereof, wherein the structure of the tetrahydroindoloquinazoline compounds is as shown in general formula (I). The tetrahydroindoloquinazoline compounds can be used in: (1) the preparation of a drug for treating cardiovascular and cerebrovascular diseases; (2) the preparation of a preparation for improving the expression of AMPK, ABCA1 and SR-BI; (3) the preparation of a preparation for activating the activity of a nuclear receptor NR, and inhibiting the activity of NLRP3, the activity of IL-1β, the activity of NF-κB and the activity of MAPKs; (4) the preparation of a preparation for promoting cholesterol efflux from cells; and (5) the preparation of an anti-inflammatory drug.

IPC Classes  ?

• C07D 471/14 - Ortho-condensed systems
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

Disclosed are a class of anti-human EGFR antibody drug conjugates and preparation method and application thereof. The anti-human EGFR antibody drug conjugate has the structure represented by formula (I). In the present invention, by means of using SCT-200 fully humanized monoclonal antibody, and coupling with Linker-MMAE by means of the chemical method of reducing the disulfide bonds between antibody chains, a class of anti-human EGFR antibody drug conjugates targeting EGFR for the treatment of solid tumors is constructed. The novel antibody drug conjugate SCT-200-Linker-MMAE provided by the present invention, in comparison with SCT-200 itself, does not affect the affinity, endocytic activity, and targeting of the antibody, better retains its biological function, and, in comparison with SCT-200, the activity is significantly improved, and can significantly inhibit the expression of related proteins during the process of tumor apoptosis, greatly improving the tumor inhibition effect.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
• A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to the technical field of enzyme inhibitors, and relates in particular to a hydroxamic acid derivative, a preparation method therefor and an application thereof. The hydroxamic acid group in the hydroxamic acid derivative provided in the present invention is chelated with an active zinc ion in an active region of an LpxC enzyme, and contains a hydrophobic side chain that binds to a hydrophobic channel in the LpxC enzyme. The described content in the two aspects ensures that a hydroxamic acid derivative has good bactericidal activity and low toxicity for LpxC. Also provided is a preparation method for the hydroxamic acid derivative, which has a short reaction time and a high yield.

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 295/195 - Radicals derived from nitrogen analogues of carboxylic acids
• C07D 295/155 - 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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• A61P 31/04 - Antibacterial agents
• C07C 45/29 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by oxidation of hydroxy groups
• C07C 47/37 - Saturated compounds having —CHO groups bound to carbon atoms of rings other than six-membered aromatic rings containing ether groups, groups, groups, or groups
• C07C 41/30 - Preparation of ethers by reactions not forming ether-oxygen bonds by increasing the number of carbon atoms, e.g. by oligomerisation
• C07C 43/192 - Ethers having an ether-oxygen atom bound to a carbon atom of a ring other than a six-membered aromatic ring containing halogen
• C07C 67/343 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisationPreparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by change of size of the carbon skeleton by increase in the number of carbon atoms
• C07C 69/78 - Benzoic acid esters
• C07C 51/09 - Preparation of carboxylic acids or their salts, halides, or anhydrides from carboxylic acid esters or lactones
• C07C 65/28 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups having unsaturation outside the aromatic rings
• C07C 269/06 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
• C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
• C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
• C07C 235/42 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton

Abstract

The present invention provides use of berbamine dihydrochloride in preparation of an Ebola virus inhibitor. In the present invention, the primed glycoprotein of the Ebola virus (EBOV-GPcl) is taken as a target site, and an antiviral active compound with the capability of binding to the EBOV-GPcl, i.e., berbamine dihydrochloride, is obtained through structure-based virtual screening. Berbamine dihydrochloride can specifically inhibit the entry of an Ebola recombinant virus by binding to the target protein EBOV-GPcl, thereby achieving the effect of anti-Ebola virus infection. The half-maximum effect concentration (EC50) of berbamine dihydrochloride against EBOV is 0.49 μM, which indicates that berbamine dihydrochloride has a strong inhibition effect on EBOV.

IPC Classes  ?

• A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
• A61P 31/14 - Antivirals for RNA viruses

Abstract

The present invention provides use of berbamine dihydrochloride in preparation of an Ebola virus inhibitor. In the present invention, the primed glycoprotein of the Ebola virus (EBOV-GPcl) is taken as a target site, and an antiviral active compound with the capability of binding to the EBOV-GPcl, i.e., berbamine dihydrochloride, is obtained through structure-based virtual screening. Berbamine dihydrochloride can specifically inhibit the entry of an Ebola recombinant virus by binding to the target protein EBOV-GPcl, thereby achieving the effect of anti-Ebola virus infection. The half-maximum effect concentration (EC50) of berbamine dihydrochloride against EBOV is 0.49 .mu.M, which indicates that berbamine dihydrochloride has a strong inhibition effect on EBOV.

IPC Classes  ?

• A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
• A61P 31/14 - Antivirals for RNA viruses

Abstract

Use of berbamine dihydrochloride in preparation of an Ebola virus inhibitor. An antiviral active compound having binding ability to EBOV-GPc1 is obtained by using an activated Ebola virus envelope glycoprotein (EBOV-GPcl) as a target and performing structure-based virtual screening, said compound being berbamine dihydrochloride. The berbamine dihydrochloride can achieve the effect of anti-Ebola virus infection by binding to the target protein EBOV-GPcl so as to specifically inhibit the entry of Ebola recombinant virus. The concentration for 50% of maximum effect (EC50) of berbamine hydrochloride against EBOV is 0.49 μM, indicating that berberamine dihydrochloride has a strong inhibitory effect on EBOV.

IPC Classes  ?

• A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
• A61P 31/14 - Antivirals for RNA viruses

Abstract

The invention belongs to the technical field of medicines. In particular, the invention relates to use of (benzenesulfonamido) benzamide compounds for inhibiting liver fibrosis, or preventing and/or treating a liver injury, or improving a liver function, or preventing and/or treating a liver disease associated with liver fibrosis, for modulating (e.g. reducing) the content of collagen (e.g. type I collagen) in liver tissue, for modulating (e.g. inhibiting) the activity of COL1A1 promoter in a cell, and for modulating (e.g. inhibiting) expression level of a gene associated with liver fibrosis in a cell.

IPC Classes  ?

• A61K 31/63 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide
• A61K 31/18 - Sulfonamides
• 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
• A61K 31/235 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group

Abstract

The present disclosure relates to the use of a compound as shown in formula (I), a stereoisomer thereof, or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating diabetes mellitus, or the use of same in the preparation of a drug for preventing or treating diabetic complications, or the use of same in the preparation of a drug as an insulin sensitizer.

IPC Classes  ?

• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 5/50 - Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• 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 27/02 - Ophthalmic agents

Abstract

Provided are a new aromatic cyanogen compound and a preparation method thereof. The present invention also relates to the use of such compound in antiviral drugs, in particular the use thereof in anti-HCV drugs.

IPC Classes  ?

• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
• C07C 255/50 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
• 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
• C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
• C07D 213/85 - Nitriles in position 3
• C07D 295/13 - 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 attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
• 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 211/56 - Nitrogen atoms
• C07D 295/155 - 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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings

Abstract

Provided are a polymyxin derivative having a general formula I structure, and a preparation method and an application thereof. The method for preparing the polymyxin derivative comprises the following steps: (1) an Fmoc-AA-OP side chain free amino group of a protected basic amino acid reacting with a halogenated resin to obtain an Fmoc-AA-OP-resin; (2) the Fmoc-AA-OP-resin being coupled one by one to obtain a linear peptide-resin; (3) the linear peptide-resin selectively removing a protective group, and carrying out solid-phase cyclization to obtain a cyclic peptide-resin; (4) the cyclic peptide-resin undergoing acidic hydrolysis and ether precipitation to obtain a crude product of a cyclic polypeptide; (5) the crude product being purified and/or salt transferred and lyophilized to obtain a pure product of the cyclic polypeptide. The polymyxin derivative may be used for preparing an antibacterial drug, and used in particular for preparing an antibacterial drug having an expanded antibacterial spectrum, improved antibacterial activity and reduced renal toxicity, comprising preparing an antibacterial drug against a "super bacteria" which carries the NDM-1 gene.

IPC Classes  ?

• C07K 7/62 - PolymyxinsRelated peptides
• A61K 38/12 - Cyclic peptides
• A61P 31/04 - Antibacterial agents

Abstract

The present invention relates to a preparation and purification method of a norvancomycin and a norvancomycin derivative. The method uses a salt-free liquid phase HPLC. The invention further relates to a method for acquiring the norvancomycin derivative (compounds 1-3). The invention further relates to a pharmaceutical preparation and application of the norvancomycin derivative (compounds 1-3).

IPC Classes  ?

• C07C 235/00 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
• C07K 1/20 - Partition-, reverse-phase or hydrophobic interaction chromatography
• C07K 9/00 - Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequenceDerivatives thereof
• A61K 38/00 - Medicinal preparations containing peptides
• A61P 31/04 - Antibacterial agents

Abstract

The present invention belongs to the technical field of medicine. In particular, the present invention relates to uses of benzenesulfonamido benzamide compounds for inhibiting liver fibrosis, or preventing and/or treating liver injury, or improving liver function, or preventing and/or treating liver diseases associated with liver fibrosis, a use thereof for regulating (i.e. reducing) the content of collagen in liver tissue (such as type I collagen), a use thereof for regulating (i.e. inhibiting) the activity of a COL1A1 promoter in cells, and a use thereof for regulating (i.e. inhibiting) the expression level of genes associated with liver fibrosis in cells.

IPC Classes  ?

• A61K 31/18 - Sulfonamides
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

Provided are a new aromatic cyanogen compound and a preparation method thereof. The present invention also relates to the use of such compound in antiviral drugs, in particular the use thereof in anti-HCV drugs.

IPC Classes  ?

• C07C 255/50 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
• C07D 213/84 - Nitriles
• C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
• A61K 31/44 - Non-condensed pyridinesHydrogenated 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 31/14 - Antivirals for RNA viruses
• A61P 31/20 - Antivirals for DNA viruses

Abstract

Disclosed are a use of a compound for up-regulating the transcriptional activity of Runx2 for preparing a medicine for preventing and treating osteoporosis. The compound N-(cyclopropylmethyl)-5-(thiophen-2-yl)-1,2-zole-3-carboxamide was obtained by a cell model of up-regulating the transcriptional activity of Runx2. The compound has the effects of up-regulating the transcriptional activity of Runx2, up-regulating the activity of alkaline phosphatase (ALP) of an osteoblast and promoting the expression of an osteogenic specific differentiation gene, and can increase the production of calcified nodules.

IPC Classes  ?

• A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
• A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis

Abstract

Provided is an application of gastrodin or gastrodin powder in preparing anti-hepaticfibrosis pharmaceutical. Systematic studies on I-type collagen α1 promoter activity inhibition, ALT and AST content in rat serum, a pathological structure in rat hepatic tissue, hydroxyproline content in rat hepatic tissue, an oxidative stress response in rat hepatic tissue, and influence on degree of rat hepaticfibrosis prove that gastrodin or gastrodin powder has a good anti-hepaticfibrosis activity.

IPC Classes  ?

• A61K 36/8988 - Gastrodia
• A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

The present invention relates to use of a microRNA or an inhibitor thereof, and specifically, the present invention relates to use of a microRNA or an inhibitor thereof in preparing a medicament for regulating lipid metabolism or preparing a medicament for preventing or treating a disease related to lipid metabolism. The microRNA is one or more of the following: miRNA-96, miRNA-185, and miRNA-223. The present invention also relates to use of the microRNA or the inhibitor thereof in regulating the expression level of a protein related to lipid metabolism. The present invention also relates to a composition comprising the microRNA or the inhibitor thereof. The microRNA or the inhibitor thereof in the present invention can be used as a pharmaceutical component, and can be applied in preventing or treating a disease caused by lipid metabolism disorders such as hyperlipidemia, atherosclerosis, coronary heart disease or other diseases.

IPC Classes  ?

• C12N 15/11 - DNA or RNA fragmentsModified forms thereof
• A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• G01N 33/92 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving lipids, e.g. cholesterol

Abstract

The present invention provides a bisamidine derivative containing bis(amidino) indole benzene, a preparation method and use thereof, and an antibacterial drug combination. The bisamidine derivative has a structure of the following formula [1], wherein R1 and R2 are independently selected from substituted or unsubstituted C1-12 linear alkyl, C3-12 branched alkyl or C3-12 cyclic alkyl; alternatively, R1 and R2 and N connected thereto are composed of a substituted or unsubstituted 3- to 6-membered ring; and R3 is independently selected from hydrogen, halogen, lower halogenated alkyl, lower alkoxy, amino or lower substituted amino. The bisamidine derivative containing bis(amidino) indole benzene provided by the present invention and a medicinal salt thereof have the activity of anti-drug-resistance bacteria, in particular having a strong activity of anti-drug-resistance gram positive and negative bacteria.

IPC Classes  ?

• C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61P 31/04 - Antibacterial agents

Abstract

Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.

IPC Classes  ?

• C07D 213/30 - Oxygen atoms
• C07D 213/68 - One oxygen atom attached in position 4
• C07D 213/55 - AcidsEsters
• C07D 213/64 - One oxygen atom attached in position 2 or 6
• C07D 213/65 - One oxygen atom attached in position 3 or 5
• C07D 213/69 - Two or more oxygen atoms
• C07C 65/28 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups having unsaturation outside the aromatic rings
• C07C 69/92 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with etherified hydroxyl groups
• C07C 51/09 - Preparation of carboxylic acids or their salts, halides, or anhydrides from carboxylic acid esters or lactones
• C07C 65/105 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic
• C07C 65/19 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups having unsaturation outside the aromatic ring
• C07C 43/215 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring having unsaturation outside the six-membered aromatic rings
• C07C 43/23 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
• C07D 213/80 - AcidsEsters in position 3
• C07D 311/58 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulfur atoms in position 2 or 4
• C07C 275/00 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
• C07C 275/54 - Y being a carbon atom of a six-membered aromatic ring, e.g. benzoylureas
• C07C 279/22 - Y being a hydrogen or a carbon atom, e.g. benzoylguanidines
• C07C 281/02 - Compounds containing any of the groups e.g. carbazates
• C07D 333/16 - Radicals substituted by singly bound hetero atoms other than halogen by oxygen atoms
• C07D 333/24 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 233/60 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
• C07D 233/90 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07C 217/20 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted by halogen atoms, by trihalomethyl, nitro or nitroso groups, or by singly-bound oxygen atoms
• C07C 217/22 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted by carbon atoms having at least two bonds to oxygen atoms
• C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
• C07C 229/08 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to hydrogen atoms
• C07C 235/46 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• C07C 235/62 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho- position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
• C07C 235/64 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho- position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
• C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 211/58 - Nitrogen atoms attached in position 4
• C07C 69/157 - Acetic acid esters of monohydroxylic compounds of unsaturated alcohols containing six-membered aromatic rings
• C07C 69/36 - Oxalic acid esters
• C07C 39/21 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic, containing only six-membered aromatic rings as cyclic part, with unsaturation outside the rings with at least one hydroxy group on a non-condensed ring
• C07C 51/353 - Preparation of carboxylic acids or their salts, halides, or anhydrides by reactions not involving formation of carboxyl groups by isomerisationPreparation of carboxylic acids or their salts, halides, or anhydrides by reactions not involving formation of carboxyl groups by change of size of the carbon skeleton
• C07C 51/36 - Preparation of carboxylic acids or their salts, halides, or anhydrides by reactions not involving formation of carboxyl groups by hydrogenation of carbon-to-carbon unsaturated bonds
• C07C 41/18 - Preparation of ethers by reactions not forming ether-oxygen bonds
• C07C 67/30 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
• C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups

Abstract

Provided are phenanthridine derivatives shown by general formula (I), pharmaceutical compositions comprising the derivatives, preparation methods therefor, and uses thereof for manufacturing medicines for the prophylaxis or treatment of diseases related to the activity of Wnt signal pathway, hepatitis C and hepatitis B.

IPC Classes  ?

• C07D 221/12 - Phenanthridines
• C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
• A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
• A61K 31/695 - Silicon compounds
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

The present invention provides an application of a microRNA or an inhibitor thereof, and specifically, the present invention provides an application of the microRNA or the inhibitor in preparing a medicine for regulating lipid metabolism or preparing a medicine for preventing or treating a disease related to lipid metabolism. The microRNA comprises one or more of the following: miRNA-96, miRNA-185, and miRNA-223. The present invention also provides an application of the microRNA or the inhibitor thereof in regulating a protein expression level related to lipid metabolism. The present invention also provides a composition comprising the microRNA or the inhibitor thereof. The microRNA or the inhibitor thereof in the present invention can be used as a pharmaceutical component, and can be applied in preventing or treating diseases related to hyperlipidemia, atherosclerosis, coronary heart disease or other diseases caused by lipid metabolism disorders.

IPC Classes  ?

• A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
• A61P 3/00 - Drugs for disorders of the metabolism
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 3/06 - Antihyperlipidemics
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• 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
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids

Abstract

Disclosed are phenyl-oxazolyl derivatives having a general formula (I), a preparation method thereof, and an application of the phenyl-oxazolyl derivatives as an inosine monophosphate dehydrogenase (IMPDH) inhibitor.

IPC Classes  ?

• C07D 263/32 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• A61P 31/12 - Antivirals
• A61P 35/00 - Antineoplastic agents
• A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection

Abstract

Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.

IPC Classes  ?

• C07C 65/03 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring
• C07C 65/05 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring o-Hydroxy carboxylic acids
• C07C 65/28 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups having unsaturation outside the aromatic rings
• C07C 69/78 - Benzoic acid esters
• C07C 69/88 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with esterified carboxyl groups
• C07C 69/92 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with etherified hydroxyl groups
• C07C 51/09 - Preparation of carboxylic acids or their salts, halides, or anhydrides from carboxylic acid esters or lactones
• C07C 67/14 - Preparation of carboxylic acid esters from carboxylic acid halides
• C07C 67/16 - Preparation of carboxylic acid esters from carboxylic acids, esters or anhydrides wherein one oxygen atom has been replaced by a sulfur, selenium or tellurium atom
• A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
• A61P 3/06 - Antihyperlipidemics
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 3/14 - Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 31/04 - Antibacterial agents
• A61P 31/12 - Antivirals

Abstract

Provided in the present invention are an unsaturated 5-membered benzo-heterocyclic compound with the structure as shown in general formula I or pharmaceutical salts thereof, and a preparation method, a pharmaceutical composition and the use thereof. Experiments have shown that the compound of the present invention has the effects of upregulating the expression activity of bone morphogenetic protein BMP-2 and anti-osteoporosis in vivo, and also has the effect of improving SAMP6 mice osteoporosis symptoms. Activity tests in vitro have shown that the compound of the present invention shows an obvious upregulation effect on bone morphogenetic protein BMP-2.

IPC Classes  ?

• C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 307/85 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
• C07D 333/70 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
• C07D 493/04 - Ortho-condensed systems
• C07D 495/04 - Ortho-condensed systems
• C07F 9/40 - Esters thereof
• A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/404 - Indoles, e.g. pindolol
• A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis

Abstract

The present invention belongs to the field of medical chemistry, and relates to an antitumour pharmaceutical composition with two active components and the use thereof. In particular, the pharmaceutical composition to which the present invention relates comprises a first independent group of active ingredients and a second independent group of active ingredients, wherein the first group of active ingredients comprises two or three ingredients of the following three ingredients A, B and C: A. dipyridamole and/or pharmaceutically acceptable derivatives thereof; B. ubenimex and/or pharmaceutically acceptable derivatives thereof; C. dexamethasone and/or pharmaceutically acceptable derivatives thereof. The second group of active ingredients comprises one or more ingredients selected from paclitaxel, adriamycin, cisplatinum, mitomycin, fluorouracil, gemcitabine, capecitabine and tyrosine kinase inhibitor; optionally, the pharmaceutical composition also comprises a pharmaceutically acceptable carrier or excipient. The antitumour pharmaceutical composition in the present invention acts on multiple targets and multiple paths, which has a clear and significant antitumour effect.

IPC Classes  ?

• A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
• A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• A61K 33/24 - Heavy metalsCompounds thereof
• A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention belongs to the field of medical chemistry, and relates to an antitumour pharmaceutical composition and use thereof. In particular, the pharmaceutical composition to which the present invention relates comprises two or three ingredients of the following three ingredients A, B and C: A. dipyridamole and/or pharmaceutically acceptable derivatives thereof; B. ubenimex and/or pharmaceutically acceptable derivatives thereof; C. dexamethasone and/or pharmaceutically acceptable derivatives thereof; optionally, the pharmaceutical composition also comprises a pharmaceutically acceptable carrier or excipient. The present invention also relates to a use of the pharmaceutical composition in preparing the antitumour drug and an antitumour method. The antitumour pharmaceutical composition in the present invention achieves the purpose of treating tumours effectively primarily by acting on the tumour microenvironment, and the features of the drug adjusting the tumour microenvironment are that it is acting on multiple targets and multiple paths, which can be expected to relieve the toxic and side effects caused by cytotoxic drugs.

IPC Classes  ?

• A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are compounds of formula(I),pharmaceutically acceptable salts and solvates thereof, wherein R can be COOR1,in which R1 can be H, substituted or unsubstituted C1~C10 straight chain or straight chain alkyl; preferred H, substituted or unsubstituted C1~C6 straight chain or straight chain alkyl. The compounds possess inhibiting effect on related tumour cells and may be developed hopefully as antitumour drugs.

IPC Classes  ?

• C07H 19/06 - Pyrimidine radicals
• C07H 1/00 - Processes for the preparation of sugar derivatives
• A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are a cell model and screening method for screening inhibitors of the tubercle bacillus. Provided is a cell which expresses the tubercle bacillus proteins L12 and L10, wherein the L12 encoding gene and the transcription activation domain of its transcription factor are located in one expression vector, and the L10 encoding gene and the DNA binding domain of its transcription factor are located in another expression vector. The present invention also relates to the use of the compound shown in formulae I or II in preparing a blocker of the interaction between proteins L12 and L10 of tubercle bacillus, an anti-tubercle bacillus drug, or a drug for treating and/or preventing tuberculosis.

IPC Classes  ?

• C12N 1/19 - YeastsCulture media therefor modified by introduction of foreign genetic material
• C12N 15/31 - Genes encoding microbial proteins, e.g. enterotoxins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• C12Q 1/18 - Testing for antimicrobial activity of a material
• A61K 31/03 - Halogenated hydrocarbons carbocyclic aromatic
• A61P 31/06 - Antibacterial agents for tuberculosis

Abstract

Provided are a rutaecarpine compound, a preparation method therefor, and a use thereof. The rutaecarpine compound, as represented in the compound of Formula (I) and the compound of Formula (2), is used in an up-regulator or an agonist for up-regulating ABCA1, SR-B1/CLA-1, and LXR α and for activating LXR α and PPAR γ, or in the preparation of drugs for treating or preventing atherosclerosis.

IPC Classes  ?

• C07D 471/14 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• 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 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

Disclosed are benzo 5-membered unsaturated heterocyclic compounds represented by formula I and their pharmaceutically acceptable salts, preparation methods and uses thereof in the preparation of the drugs for treating osteoporosis, wherein each substituent of formula (I) is defined as the description.

IPC Classes  ?

• C07D 333/70 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
• C07D 333/56 - Radicals substituted by oxygen atoms
• C07D 495/04 - Ortho-condensed systems
• C07D 307/85 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
• C07D 307/80 - Radicals substituted by oxygen atoms
• C07D 307/86 - Benzo [b] furansHydrogenated benzo [b] furans with an oxygen atom directly attached in position 7
• C07D 209/12 - Radicals substituted by oxygen atoms
• C07D 333/60 - 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 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
• A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis

Abstract

Provided is a method for preparing an acyclic nucleoside monophosphate compound as an antiviral drug, which comprises reacting an acyclic nucleoside antiviral drug such as adefovir or tenofovir as a raw material, with a aliphatic long-chain alkoxy-ethanol/propanol, to obtain a target compound. The present invention overcomes the disadvantage in the prior art, not only improves the quality of adefovir or tenofovir monophosphate, but also reduces the production cost, and meanwhile has the advantages of being convenient in operation and being easy for industrial production.

IPC Classes  ?

• C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

Abstract

N-substituted matrinic acid derivatives or matrine derivatives and preparation methods and uses thereof are disclosed. Specifically, compounds represented by formula (I) or (II), their pharmaceutically acceptable salts, geometric isomers, stereoisomer, solvates, esters and prodrugs are disclosed, wherein all the symbols are defined as in the description. The preparation methods of the present compounds, pharmaceutical compositions containing them and uses thereof in the manufacture of medicaments are also disclosed. The present compounds can be used in preventing and/or treating virus infection related diseases or disorders such as hepatitis B and/or hepatitis C and/or AIDS.

IPC Classes  ?

• C07D 471/16 - Peri-condensed systems
• C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
• A61P 31/14 - Antivirals for RNA viruses

Abstract

A group of amino substituted benzoyl derivatives, their preparation and their use. The screening and research on an antiviral drug with hA3G/Vif as a target point proves that the 3-amino benzoyl derivatives not only have the combined activity for the hA3G/Vif, but also have a function of inhibiting replication of viruses. The present invention provides the possible breakthrough progress for the problem of HIV drug resistance, thereby providing a novel clinical antiviral drug which has higher efficiency.

IPC Classes  ?

• A01N 47/10 - Carbamic acid derivatives, i.e. containing the group —O—CO—NThio-analogues thereof
• A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
• C07D 239/02 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
• C07C 261/00 - Derivatives of cyanic acid
• C07C 269/00 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
• C07C 271/00 - Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
• C07C 229/00 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton
• C07C 239/00 - Compounds containing nitrogen-to-halogen bondsHydroxylamino compounds or ethers or esters thereof

Abstract

Provided are a fusion protein of anti-CD20 antibody Fab fragment and lidamycin apoprotein (LDP) as well as coding gene, vector and host bacteria thereof; and the fusion protein functionally conjugated with lidamycin chromophore AE and method for the production thereof. Also provided are a pharmaceutical composition comprising said fusion protein and use of said fusion protein.

IPC Classes  ?

• C07K 19/00 - Hybrid peptides
• C12N 15/62 - DNA sequences coding for fusion proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
• A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
• A61P 35/00 - Antineoplastic agents

Abstract

A group of amino substituted benzoyl derivatives, their preparation and their use. The screening and research on an antiviral drug with hA3G/Vif as a target point proves that the 3-amino benzoyl derivatives not only have inhibiting the combined activity for the hA3G/Vif, but also have a function of inhibiting replication of viruses. The present invention provides the possible breakthrough progress for the problem of HIV drug resistance, thereby providing a novel clinical antiviral drug which has higher efficiency.

IPC Classes  ?

• C07C 237/44 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having carbon atoms of carboxamide groups, amino groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
• C07C 233/12 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
• C07C 229/54 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
• C07C 327/16 - Monothiocarboxylic acids having carbon atoms of thiocarboxyl groups bound to carbon atoms of six-membered aromatic rings
• C07C 307/02 - Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
• C07C 303/26 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids
• C07D 239/52 - Two oxygen atoms
• A61K 31/21 - Esters, e.g. nitroglycerine, selenocyanates
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61K 31/255 - Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
• A61P 31/12 - Antivirals

Abstract

A set of geldanamycin derivatives and their preparation methods. Pharmaceutical compositions comprising the said compounds as an active ingredient which are used as antivirus and antitumor agents. The said derivatives are used in the manufacture of heat shock protein 90(Hsp90) inhibiting agents which have the utility as antivirus and antitumor agents.

IPC Classes  ?

• C07D 225/06 - Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with one six-membered ring
• C07H 19/06 - Pyrimidine 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
• A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
• A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
• A61P 31/12 - Antivirals
• A61P 35/00 - Antineoplastic agents

Abstract

7-(4-oximino-3-amino-1-piperidyl)quinolinecarboxylic acid derivatives, their preparation methods, their pharmaceutical uses and antibacterial agents and feed additives comprising the said compounds. More specially, novel fluoroquinolone formic acid derivatives, wherein 7-position is 4-oximino-3-amino-1-piperidyl, 8-position is methoxyl and 1-position is cyclopropyl. Compared with conventional fluoroquinolone antibacterial medicine, the invention compounds show excellent gram-pos. bacteria resistance activity and broad-spectrum antibacterial activity.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed 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
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
• A61P 31/04 - Antibacterial agents

Abstract

Provided is a fusion protein NGR-LDP-AE, which comprises targeting peptide of CD13, lidamycin apoprotein LDP and activated form enediyne chromophore AE combined with the LDP. This fusion protein can be used for targeted cancer therapy.

IPC Classes  ?

• C07K 19/00 - Hybrid peptides
• C12N 15/62 - DNA sequences coding for fusion proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
• A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
• A61P 35/00 - Antineoplastic agents

Abstract

The invention provides new antitumor compounds, which are heterocyclic ketone (alcohol) or their derivatives having the structure of formula I. The compounds provided in the present invention can be used for preparing microtubulin protein inhibitors and have antitumor effect, and the invention also provides antitumor pharmaceutical compositions containing the said new compounds as active ingredient. The invention also provides the preparation method for the said compounds. The said compounds of formula I show the advantages of having a small molecular weight, being easy to synthesis and having less poison side effect.

IPC Classes  ?

• C07D 209/86 - CarbazolesHydrogenated carbazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
• 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 209/12 - Radicals substituted by oxygen atoms
• C07D 307/80 - Radicals substituted by oxygen atoms
• C07D 333/56 - Radicals substituted by oxygen atoms
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
• A61K 31/403 - 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
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention has disclosed a set of pentac unsaturated heterocycle compounds which can up accommodate the expression activity of Osteogenesis protein BMP-2 to increase the bone density, and inhibit cholesterol biosynthesis to reduce blood fats. The present invention has disclosed the synthesis of a set of pentac unsaturated heterocycle compounds and has measured their upper opsonization of Osteogenesis protein BMP-2 and inhibiting effect on key fat metabolism enzyme HMG-CoA. It lays the foundation of treatment of diseases relating to bone metabolic disorders or blood fat metabolic disorders of mentioned compounds.

IPC Classes  ?

• C07D 207/30 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
• C07D 207/323 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atoms
• C07D 307/34 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
• C07D 307/40 - Radicals substituted by oxygen atoms
• C07D 333/06 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulfur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
• A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61P 19/00 - Drugs for skeletal disorders

Abstract

The present application has disclosed carzole sulphamide derivatives and their pharmaceutically acceptable salts of formula (I). The compounds can be used as small molecular anti-mitotic agent. The compounds not only can inhibit tumor cell in the first mitosis, but also have remarkable antitumor activity. They have the advantage of small molecular and simple synthesis without drug resistance problems. The present application also provides pharmaceutical composition containing the carzole sulphamide derivatives as active ingredient.

IPC Classes  ?

• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/12 - 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 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 209/84 - Separation, e.g. from tarPurification
• C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
• 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 35/00 - Medicinal preparations containing materials or reaction products thereof with undetermined constitution
• A61P 35/00 - Antineoplastic agents