C07D 209/48 - Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
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 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 37/00 - Drugs for immunological or allergic disorders
2.
PIPERIDINE-2,6-DIKETONE DERIVATIVE AND TREATMENT FOR CROHN'S DISEASE
C07D 209/48 - Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
C07D 211/88 - Oxygen atoms attached in positions 2 and 6, e.g. glutarimide
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 37/00 - Drugs for immunological or allergic disorders
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
Disclosed are a compound as shown in formula (I) and pharmaceutically acceptable salts thereof. R1, R2, R3, R4, R5, W, and n are defined as in the description of the present application.
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
TIANJIN MICHELE SCI-TECH DEVELOPMENT CO., LTD. (China)
Inventor
Zhang, Hesheng
Chen, Xin
Abstract
Disclosed are a polymorph I-VI of N-(6-(4-chlorophenoxy)hexyl)-N'-cyano-N''-(4-pyridyl)guanidine or solvate thereof, a preparation method therefor, and a use thereof as a biological active ingredient. The polymorph is useful in treatment of cancers, and diseases or disorders caused by abnormal cell proliferation.
TIANJIN MICHELE SCI-TECH DEVELOPMENT CO., LTD. (China)
Inventor
Zhang, Hesheng
Chen, Xin
Abstract
Provided are polymorphs I to VIII of a dalfampridine or of its solvates, a preparation method therefor, and applications thereof as an active component of a medicine. Said polymorphs I to VIII of the dalfampridine or of its solvates can be used to prepare formulations for improving the walking speed of patients of multiple sclerosis and for alleviating other symptoms of multiple sclerosis.
Disclosed are compounds of general formula I, stereisomers, cis-/trans-isomers, tautomers or mixtures thereof, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein R1, R2, R3 and R4 are defined as in the application.
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 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
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
TIANJIN MICHELE SCI-TECH DEVELOPMENT CO., LTD (China)
Inventor
Chen, Xin
Chen, Yingwei
Cong, Junjie
Li, Xingwen
Abstract
Compounds of formula (I) or pharmaceutically acceptable salts thereof, and use for treating cancer thereof are disclosed, wherein, the definitions of X, Y, R1, R2 and n are described in description.
A61P 35/02 - Antineoplastic agents specific for leukemia
A61P 35/04 - Antineoplastic agents specific for metastasis
C07C 277/08 - Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups of substituted guanidines
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07C 279/28 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to cyano groups, e.g. cyanoguanidines, dicyandiamides
TIANJIN MICHELE SCI-TECH DEVELOPMENT CO., LTD. (China)
Inventor
Zhang, Hesheng
Abstract
Compounds represented by general formula (I), pharmaceutically acceptable salts and solvates thereof or solvates of pharmaceutically acceptable salts are disclosed. wherein R1, R2, R3, R4, W and formula (II) are defined as in the application.
TIANJIN MICHELE SCI-TECH DEVELOPMENT CO., LTD. (China)
Inventor
Zhang, Hesheng
Zeng, Guanghuai
Gao, Yifei
Abstract
Compounds of formula (I), preparation method thereof and pharmaceutical compositions containing such compounds are disclosed, wherein R1, R2, R3, R4, R5, R6, R7 and R8 are defined in the description. The uses of said compounds for manufacturing a medicament for the treatment of PDE4-mediated diseases or conditions 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
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
TIANJIN MICHELE SCI-TECH DEVELOPMENT CO., LTD (China)
Inventor
Zhang, Hesheng
Zhang, Qinghua
Chen, Yingwei
Huo, Aihong
Abstract
The compositions formed from pyridyl cyanoguanidines and cyclodextrins, cyclodextrin derivatives and/or surfactants with solubilization, preparation methods and uses thereof.
Co-crystals of atorvastatin hemi-calcium and butanone, the preparation processes and uses as HMG-CoA enzyme inhibitor thereof. The dihydrate formed from atorvastatin hemi-calcium and butanone of formula I and water exists in the steady crystal form(crystal H) whose water-solubility(0.46 mg/ml) is far higher than that of atorvastatin hemi-calcium trihydrate available from market as the later's is only 0.198 mg/ml under the same testing conditions.
C07D 207/34 - 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 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 carbon atoms
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
12.
ANTHRACYCLINE ANTIBIOTIC DERIVATIVES WITH HIGH ACTIVITY, PREPARATION METHODS AND USES THEREOF
TIANJIN MICHELE SCI-TECH DEVELOPMENT CO., LTD (China)
Inventor
Zhang, Hesheng
Abstract
Anthracycline antibiotic derivatives with anticancer activity, i.e. the compounds of formula (I). The present anthracycline antibiotic derivatives has the same activity as or higher activity than that of the known medicaments such as doxorubicin, daunorubicin in the cellular level and at the same time the present derivatives have better tolerance than doxorubicin in animal body.
C07H 15/252 - Naphthacene radicals, e.g. daunomycins, adriamycins
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 31/7042 - Compounds having saccharide radicals and heterocyclic rings
THE SALTS OF 3-(4-AMINO-1-OXO-1,3-DIHYDRO-ISOINDOL-2-YL)PIPERIDINE-2,6-DIONE OR ITS DERIVATIVES, THEIR POLYMORPHS, PREPARATION METHODS AND USES THEREOF
TIANJIN MICHELE SCI-TECH DEVELOPMENT CO., LTD (China)
Inventor
Zhang, Hesheng
Abstract
The present invention provides the pharmaceutically acceptable strong acid addition salts of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione, their solvates, preparation methods and uses of treating the diseases or abnormities of inhibiting inflammatory gene or new blood vessel formation . The water-solubility of the pharmaceutically acceptable strong acid addition salts of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione is higher than 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione. The present invention also provides the polymorphs of the pharmaceutically acceptable strong acid addition salts of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione and their solvates.
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 31/454 - 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 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 13/00 - Drugs for disorders of the urinary system
C07D 211/32 - 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 doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
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
15.
THE TETRACYCLIC ANTHRAQUINONES POSSESSING ANTI-CANCER EFFECT
The present invention provides aminoside tetracyclic anthraquinones represented by formula I or II, wherein the piptides are introduced to connect tetracyclic anthraquinones and fatty acid saturated or unsaturated in order to make the anticancer agents to be absorbed and released selectively; meanwhile some water-solubility groups are also introduced into the branched chain, aminosaccharide and tetracyclic moiety of the compounds to improve the water-solubility. The present invention also provides the preparative method and the use thereof as pharmaceutically active components for treating the diseases cured by aminoside tetracyclic anthraquinone, for example cancer, such as intestines, liver, gastric, breast, lung, ovary, prostate, brain glioma, lymph, skin, pigment, thyroid gland, multiple bone marrow cancer and leukemia.
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
Compounds represented by formula (I) or (II) against cell releasing TNF α, their pharmaceutically acceptable salts or hydrates and preparation methods and uses thereof, in which A and B represent CH2, CO, SO, SO2 respectively; D represents S, NH, NC1-6 alkyl; R1 represents H, one-two same or different radical(s) selected from the group consisting of F, Cl, Br, C1-4 alkyl,OH,OC1-4 alkyl,NO2,NHC(O)C1-4 alkyl,NH2,NH(C1-4 alkyl),N(C1-4 alkyl)2.
A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
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
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
A61P 37/00 - Drugs for immunological or allergic disorders
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
A61P 5/00 - Drugs for disorders of the endocrine system
17.
PYRROLINE-2-ONE DERIVATIVES AGAINST CELL RELEASING TUMOR NECROSIS FACTOR, PREPARATION METHODS AND USES THEREOF
Compounds represented by formula (I) or (II) against cell releasing TNF α, their pharmaceutically acceptable salts or hydrates and preparation methods and uses thereof, in which A, B and E represent CH2, CO respectively; D represents S, NH, NC1-6 alkyl; R represents H, R3 ; R1 represents 1-4 same or different radical(s) selected from the group consisting of F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, NO2, NHC(O)C1-4 alkyl, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2; R2 represents F, CF3, H or C1-4 alkyl.
A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
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
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
A61P 37/00 - Drugs for immunological or allergic disorders
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
A61P 5/00 - Drugs for disorders of the endocrine system
A combined antibiotics preparation comprising piperacillin, sulbactam or clavulanic acid, ion chelants and/or buffers, which can be used to prepare a stable solution preparation, and can be used to prepare a stable solution preparation together with aminoglycoside antibiotics in one container.
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 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
The antibiotics composition comprising at least one of beta-lactam antibiotics and buffers, further comprising at least one of beta-lactamase inhibitors. The composition can be formulated with at least one of aminoglycoside antibiotics into solution for controlling microbial infection in a container.
A61K 31/545 - 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
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
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 31/431 - 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 containing further heterocyclic ring systems, e.g. ticarcillin, azlocillin, oxacillin
A61K 31/424 - Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
A61K 47/18 - Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
A61K 47/12 - Carboxylic acids; Salts or anhydrides thereof
The antibiotics composition comprising at least one of beta-lactam antibiotics and at least one of ionic chelating agents used for inhibiting particulate formation, further comprising at least one of beta-lactamase inhibitors or buffers, or at least one of beta-lactamase inhibitors and buffers simultaneously. The composition can be formulated with at least one of aminoglycoside antibiotics into solution for controlling microbial infection in a container.
A61K 31/545 - 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
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
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 31/431 - 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 containing further heterocyclic ring systems, e.g. ticarcillin, azlocillin, oxacillin
A61K 31/424 - Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
A61K 47/18 - Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
A61K 47/12 - Carboxylic acids; Salts or anhydrides thereof
The antibiotics composition comprising at least one of aminoglycoside antibiotics and at least one of ionic chelating agents used for inhibiting particulate formation, or at least one of buffers, or at least one of ionic chelating agents and buffers simultaneously. The composition can be formulated into solution, or combined with at least one of beta-lactam antibiotics, or combined with at least one of beta-lactam antibiotics and at least one of beta-lactamase inhibitors into solutions for controlling microbial infection in a container.
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
A61K 47/18 - Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
A61K 47/12 - Carboxylic acids; Salts or anhydrides thereof
The compounds which could inhibit protein tyrosine kinases activity or the pharmaceutical acceptable salts or hydrates thereof. The uses of the compounds in treating or preventing physiological abnormal induced by protein tyrosine kinases overexpression in mammal. The preparation methods of the compounds.
C07D 215/54 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/4706 - 4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
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
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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
23.
ANALGESIC 5, 9 - METHANOCYCLOOCTA (b) PYRIDIN - 2 (1H) - ONE DERIVATIVES, THEIR PREPARATION METHOD AND USE
Compounds represented by the formula (I) or salts, hydrates thereof, wherein R1, R8, R11 and R12 are H or C1-4 hydrocarbonyl respectively; R2, R3, R6 and R7 are H, halogen or C1-4 hydrocarbonyl respectively; R4 is C1-6 hydrocarbonyl or Ar; or =CR4R3 is cyclopentylidene, cyclohexylidene, 1-methylpiperidyl-4-idene or indenyl-1-idene; R5 is H, 1-4 same or different F, Cl, Br, CF3, R9, OR9, NR9R10, NO2, CN, COOR9, O2CR9, CONR9R10, NR9C(O)R10, heterocyclic, aryl or groups represented by the formula (II) respectively; R9 and R10 are H or C1-6 hydrocarbonyl; Ar is aromatic ring; m is 0, 1 or 2; n is 0, 1, 2, 3 or 4, for treating mammal pain, functional painful syndrome, organic painful syndrome or tissue painful syndrome, and their preparation method.
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
The invention relates to 5H-thieno⏧3,4-c]pyrrole-4,6-dione derivatives represented by formula (`), its various pharmaceutically acceptable salts, its preparation and its use as active ingredient in the medicament which can inhibit release of tumor necrosis factor (TNF) in organism: (`) in which R1 represents H, C1-6 alkyl, OR4, OC(O)R5, NO2, NHC(O)R6, NR7R8; R2 represents H, halogen, C1-6 alkyl; R3 represents H, methyl, isopropyl, allyl, benzyl, CH2CO2(C1-6 alkyl), CH2(CH2)nR9; in which R4, R5, R6, R7 and R8 represent H, C1-6 alkyl; R9 represents H, C1-6 alkyl, OH, OC1-6 alkyl, NH2, NHC1-6 alkyl, N(C1-6 alkyl)2, CO2(C1-6 alkyl); n is 1, 2, 3, 4.
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
C07D 333/00 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
C07D 209/00 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
The present invention discloses a method of treating pain, functional painful syndrome or organic painful syndrome, which characterized in using compound of formula (I) and the salts thereof to alleviate or treat the pain, functional painful syndrome or organic painful syndrome in mammals, wherein: R1 represents H or C1-6 Hydrocarbonyl; R2 represents H or C1-6 Hydrocarbonyl; R3 represents C1-6 Hydrocarbonyl, heterocycle group or aryl; R4 represents C1-6 Hydrocarbonyl, heterocycle group or aryl; and R5 represents C1-6 Hydrocarbonyl, heterocycle group or aryl.
A61K 31/48 - Ergoline derivatives, e.g. lysergic acid, ergotamine
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
The present invention is directed to piperidyl-2,6-dione derivatives of formula (I) and inorganic or organic acid salts thereof, methods of producing these compounds, and the use of the compounds as active ingredient in medicine to inhibit cells from releasing TNF&agr;: (I) Wherein, n represents 1, 2, 3, 4, 5, or 6; R1 represents F, Cl, Br, C1-4alkyl, OH, OC1-4alkyl, NO2, NHC (O) C1-4alkyl, NH2, NH (C1-4alkyl), N (C1-4alkyl)2, there are 1-4 R1 and each R1 may be the same or different; R2 represent OR3, NR3R4, N(R3)COR4, O2CR5, wherein R3 or R4 represents H or C1-4alkyl, R5 represents CHR6NR7R8, CHR6NR9C(O)CHR10NR7R8, heterocycle W or CHR6NR9C(O)W, where R6, R9, R10 independently represents H or C1-4alkyl, R7 and R8 independently represents H or C1-4alkyl or R7 and R8 together represent 1,3-propilidene, 1,4-butylidene, 1,5-pentamethylene, 1,6-hexamethylene, W represents four-, five-, six-, seven-, or eight-membered saturated or unsaturated heterocycles.
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
patents