The present invention provides a novel antibiotic compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, an ester thereof, a prodrug thereof, a solvate thereof, or a deuterated analog thereof, or a stereoisomer thereof. The compound of the present invention exhibits excellent antibacterial activity, especially against Gram bacteria.
wherein each group is defined as in the description.
C07D 307/16 - 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 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 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 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
2.
METHOD FOR PREPARING TRICYCLIC COMPOUND, AND INTERMEDIATE THEREOF
Disclosed in the present application are a method for preparing a tricyclic compound, and an intermediate thereof, and in particular, a method for preparing (3S,3aR)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-pyrazolo[3,4-f]quinolone compound, an intermediate in the method, and a method for preparing the intermediate.
Provided are a new antimicrobial agent compound as shown in the following general formula (I), a pharmaceutically acceptable salt thereof, an ester thereof, a prodrug thereof, a solvate thereof, a deuterated compound thereof, or a stereoisomer thereof. The compound of the present invention exhibits an excellent antibacterial activity, in particular an excellent antibacterial activity against gram bacteria. In the formula, the definition of each group is as set forth in the description.
C07D 307/16 - 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 307/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 333/24 - 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 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
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
The present invention belongs to the field of pharmaceutical technology, and crystal forms of a 9-aminomethyl substituted tetracycline compound and a process for preparing the same. More specifically, the present invention relates to crystal forms of the compound represented by formula (1), a process for preparing crystal forms of the compound represented by formula (1) and use of said crystal forms in manufacture of medicament for treating and/or preventing an infection disease caused by tetracycline-sensitive bacteria and/or tetracycline-resistant bacteria.
C07D 209/02 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
Provided are a pharmaceutical composition comprising mineralocorticoid receptor antagonist and a use thereof. By orally administrating a pharmaceutical composition to a patient suffering from chronic kidney disease in need of treatment thereof, an effective and safe AUC of the pharmaceutical composition ranges from 188 ng*h/mL to 3173 ng*h/mL, with a bioavailability in mammals≥50%. AUC is controlled in a safe and effective range when the pharmaceutical composition is administered for the treatment of chronic kidney disease in a daily dose of 0.1 mg to 1.0 mg.
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 47/00 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient
A61K 9/00 - Medicinal preparations characterised by special physical form
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
6.
CRYSTAL FORM OF 9-AMINOMETHYL SUBSTITUTED TETRACYCLINE COMPOUNDS AND PREPARATION METHOD THEREFOR
The present invention relates to a crystal form of 9-aminomethyl substituted tetracycline compounds and a preparation method therefor, and in particular, to a crystal form of the compound represented by formula (I), a preparation method for a crystal form of the compound represented by formula (I) and use of the crystal form in the preparation of drugs for treating and/or preventing infectious diseases caused by tetracycline sensitive bacteria and/or tetracycline resistant bacteria.
The present invention relates to a compound represented by general formula (I), a method for preparing said compound, a pharmaceutical formulation containing said compound, and the use of said compound in manufacture of a medicament for treating or preventing the fibrous degeneration disease and treating the excessive proliferation disease:
9, a, b and n are defined as those in the description.
C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 401/12 - 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 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, 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
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 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
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 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention belongs to the field of pharmaceutical techniques, and in particular relates to JNK inhibitors as shown by general formulae (I), (1a) or (1b), pharmaceutically acceptable salts or stereoisomers thereof, the preparation method of these compounds, pharmaceutical preparations containing these compounds, and use of these compounds in the preparation of drugs for treating and/or preventing ischemia reperfusion injury, diabetes, neurodegenerative disorders, chronic inflammation, pulmonary fibrosis, liver fibrosis, fatty liver or liver cirrhosis.
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
9.
CRYSTAL FORM OF COMPOUND USED AS MINERALOCORTICOID RECEPTOR ANTAGONIST AND PREPARATION METHOD THEREFOR
The present invention belongs to the technical field of medicines, and relates to a crystal form of a compound used as a mineralocorticoid receptor antagonist and a preparation method therefor, and in particular, to a method for preparing a compound 2-chloro-4-[(3S,3a R)-3-cyclopentyl-7-(4-hydroxypiperidine-1-carbonyl)-3,3a,4,5-tetrahydro-2H-pyrazole[3,4-f]quinoline-2-yl]benzonitrile of formula (I), a crystal form thereof, a preparation method for the crystal form, and the use of the crystal form in the preparation of drugs for the treatment and/or prevention of renal injury or cardiovascular diseases.
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 25/00 - Drugs for disorders of the nervous system
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
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
The present invention relates to a compound shown in a formula (I), a method for preparing the compound, a pharmaceutical composition containing the compound, and applications of the compound in preparing drugs for preventing and/or treating B-cell related leukemia, inflammatory diseases and autoimmune diseases, wherein X, W, ring A, ring B, L1, L2, R1, R2, R3, ---, a, b, c, d, e, p and q are as defined in the specification.
A61P 25/00 - Drugs for disorders of the nervous system
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
A61P 11/00 - Drugs for disorders of the respiratory 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
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 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 21/04 - Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
11.
INDOLE FULL KETONE DERIVATIVE USED AS TYROSINE-KINASE INHIBITOR
The present invention relates to a compound having the general formula (I), a method of preparing the compound, a drug preparation containing the compound, and applications of the compound in preparing drugs used to preventing or treating fibrosis diseases and treating hyperplasia diseases. The ring A, X, R1, R2, R3, R4, R5, R6, R7, R8, R9, a, b, and n are as defined in the description.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 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 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/435 - 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 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61P 39/00 - General protective or antinoxious agents
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
Provided are a pyrimidineamide derivative as represented by general formula (I), pharmaceutically acceptable salt thereof, and stereoisomer thereof or solvent compound thereof, wherein X, Y, A, R1 and R2 are as defined in the specification; also provided are a preparation method of the compounds, pharmaceutical composition containing the compounds, and uses of the compounds in the preparation of drugs for treating and/or preventing syk-mediated signal-path-related diseases.
The present invention relates to compounds as represented by general formula (I) as tyrosine kinase inhibitors, preparation method thereof, pharmaceutical compositions containing the compounds, and uses thereof for preventing and/or treating instances of B-cell related leukemia, inflammatory diseases and autoimmune diseases, wherein A, ring B, L1, L2, R1, R2, R3, a, b, c, d, e, p and q are as defined in the specification.
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 401/02 - 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
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
Disclosed are a PI3Kδ inhibitor compound of formula (I), pharmaceutically acceptable salts, stereoisomers or deuterated compounds thereof, preparation methods of these compounds, a pharmaceutical preparation containing these compounds, and the use thereof for preparing a medicine for treating inflammatory disorders or tumours.
Nitrogen-containing fused ring compounds of general formula (I) for use as CRTH2 antagonists, and pharmaceutically acceptable salts and stereoisomers thereof, where X1, X2, X3, X4, X5, W, X, Y, L1, L2, L3, A, and B are as defined in the specification. Methods for preparing compounds of general formula (I), drug formulations and pharmaceutical compositions containing the compounds, and uses of the compounds in preparation of drugs for treatment and/or prevention of diseases related to CRTH2 activity.
C07D 209/22 - 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 with an aralkyl radical attached to the ring nitrogen atom
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
The invention belongs to the medicinal technical field, and in particular relates to a tigecycline derivative of general formula (I), a pharmaceutically acceptable salt, precursor drug, solvate or isomer thereof, wherein R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, R10, R11, R12, R13, X and W are defined as in the description; the invention also relates to a preparation method of these compounds, a pharmaceutical composition containing these compounds and the use of these compounds in preparing medicines for the treatment and/or prevention of diseases with a sensitivity to tetracycline medicines.
C07C 237/26 - 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 ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
C07D 205/12 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
C07D 209/52 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
C07D 305/08 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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 ring atoms
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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
The present invention relates to a 9-aminomethyl substituted tetracycline compound represented by general formula (I), pharmaceutically acceptable salts, solvates or isomers thereof, wherein R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, Rl0, R11, R12, R13a and R13b are as defined in the specification; the present invention also relates to a method for preparing the compounds; a pharmaceutical composition comprising the compounds; and use of the compounds in the preparation of medicaments for treatment and/or prevention of diseases responsive to tetracyclines.
C07C 235/66 - 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 bound to carbon atoms of six-membered aromatic rings being part of condensed ring systems and singly-bound oxygen atoms, bound to the same carbon skeleton
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 205/12 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
C07D 209/52 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/403 - 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 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
Provided are compounds of formula (I), pharmaceutically acceptable salts, esters, or solvates, or prodrugs or isomers thereof. Thereinto, Cy1, L, X, Y1, Y2, n1, n2, n3, n4, R1a, R1b, R3a, R3b, R4, R5 and m are defined as in the description.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
Provided are a dihydropyrazole compound as represented by general formula (Ia), a pharmaceutically acceptable salt or isomer thereof, a preparation process thereof, a pharmaceutical preparation containing such compounds and the use thereof. The definitions of the various substituents in formula (Ia) are as described in the specification. The compounds can be used for treating and/or preventing renal injury, cardiovascular diseases, especially hypertension, and/or endocrine diseases.
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 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 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 409/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 401/08 - 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 alicyclic rings
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
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
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/4439 - 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 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicaments for the treatment and/or prevention of kidney damage, cardiovascular diseases such as hypertension, and/or endocrine diseases. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy, and n are as presented in the description.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
Oxazolidinone compounds containing ring-fused bicyclic ring represented by the general formula (I), pharmaceutically acceptable salts and stereoisomers thereof are disclosed, wherein R1, R2, R3, R4, R5, R6, and -Y- are defined as in the description. Also disclosed are the preparation methods of such compounds, pharmaceutical compositions and pharmaceutical preparations containing the same and uses of the same in the manufacture of medicaments for treating and/or preventing infectious diseases, and in the treatment and/or prevention of infectious diseases.
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/428 - Thiazoles condensed with carbocyclic rings
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
Disclosed are oral carbapenem compounds containing aminosulfonyl azetidinyl represented by general formula (I), their stereoisomers, or their pharmaceutically acceptable salts or solvates, which belongs to the technical field of medicine. In the formula (I), R is defined as in the description. The preparation methods of the compounds, pharmaceutical compositions containing the compounds, the use of such compounds in the preparation of medicines for treating and/or preventing infectious diseases, and the method of treating and/or preventing infectious diseases using such compounds are also disclosed.
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
Compounds of formula I, pharmaceutically acceptable salts, esters, isomers or solvates thereof, wherein R1 and R2 are independently hydrogen, C1-6 alkyl or amino- protecting group; X is N and the like; R3 is H and the like；ring B is a ring with 3 to 8 members; R4 is H,C1-6 alkyl and the like；R5,R6 and R7 are independently hydrogen, C1-6 alkyl and the like or R6,R7 and the atom which they connect form a ring; n is an integer from 1 to 3；and the dotted line represents single bond or double bond. The compounds have good antimicrobial activities and can be effective ingredients of agents for preventing and/or treating infection of respiratory system, otolaryngological department, bone and arthrosis infection caused by bacterial pathogen.
C07D 501/57 - 7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with a further substituent in position 7, e.g. cephamycines
A61K 31/546 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine containing further heterocyclic rings, e.g. cephalothin
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
The invention provides a compound represented by formula (I), its pharmaceutically acceptable salts, easily hydrolyzed esters, isomers, hydrates and hydrates of such esters or salts, wherein R1, R2, R3 and A are defined as in the description. The invention also provides the preparation of such compounds, a pharmaceutical composition containing them, and the use of such compounds in preparation of medicaments for the treatment and/or prophylaxis of infective diseases.
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 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
25.
1&bgr;- METHYLCARBAPENEM ANTIBIOTICS,THE PHARMACEUTICAL COMPOSITION AND USE THEREOF
Antibiotic 1&bgr;-methylcarbapenem compounds of formula(I),pharmaceutically acceptable salts, in vivo hydrolysable esters, isomers, preparations or compositions thereof, or their use in the manufacturing of medicaments which prevent and/or treat infection diseases in mammals including human.
A61K 31/43 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems
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
Novel carbapenem derivatives, which belong to pharmaceutical art. In particular, compounds of Formula (1) and (2), pharmaceutical acceptable salts, hydrolysable esters, isomers and intermediates thereof: wherein R1, R2, R3 and R4 have the meanings as defined in the specification. Preparation methods of such compounds, pharmaceutical compositions containing such compounds and uses of such compounds in the preparation of drugs for the treatment and/or prophylaxis of infectious diseases.
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 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
27.
CRYSTAL FORMS OF A 9-AMINOMETHYL SUBSTITUTED TETRACYCLINE COMPOUND AND A PREPARATION METHOD THEREOF
The present invention relates to a crystal form of 9-aminomethyl substituted tetracycline compounds and a preparation method therefor, and in particular, to a crystal form of the compound represented by formula (I), a preparation method for a crystal form of the compound represented by formula (I) and use of the crystal form in the preparation of drugs for treating and/or preventing infectious diseases caused by tetracycline sensitive bacteria and/or tetracycline resistant bacteria.
The present invention relates to a 9-aminomethyl substituted tetracycline compound represented by general formula (I), pharmaceutically acceptable salts, solvates or isomers thereof, wherein R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, Rl0, R11, R12, R13a and R13b are as defined in the specification; the present invention also relates to a method for preparing the compounds; a pharmaceutical composition comprising the compounds; and use of the compounds in the preparation of medicaments for treatment and/or prevention of diseases responsive to tetracyclines.
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/403 - 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
C07C 235/66 - 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 bound to carbon atoms of six-membered aromatic rings being part of condensed ring systems and singly-bound oxygen atoms, bound to the same carbon skeleton
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 205/12 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
C07D 209/52 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
Provided are a new antimicrobial agent compound as shown in the following general formula (I), a pharmaceutically acceptable salt thereof, an ester thereof, a prodrug thereof, a solvate thereof, a deuterated compound thereof, or a stereoisomer thereof. The compound of the present invention exhibits an excellent antibacterial activity, in particular an excellent antibacterial activity against gram bacteria. In the formula, the definition of each group is as set forth in the description.
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
A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
C07D 307/16 - 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 307/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 333/24 - 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 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
patents
