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61. 发明专利

DE10034623A1 New heterocyclic substituted pyridine derivatives useful as tumor necrosis factor-alpha inhibitors in treatment of e.g. atherosclerosis, arthritis, Crohn's disease, osteoporosis, transplant rejection and psoriasis 未知
公开(公告)号：DE10034623A1
公开(公告)日：2002-01-31
申请号：DE10034623
申请日：2000-07-17
申请人： BAYER AG
发明人： MUELLER ULRICH , HANDKE GABRIELE , FISCHER RUEDIGER , PETESCH NICOLE , SCHMECK CARSTEN , KRETSCHMER AXEL , NIELSCH ULRICH , BREMM KLAUS-DIETER , ZAISS SIEGFRIED
IPC分类号： C07D409/04 , C07D413/14 , A61K31/422 , C07D417/04 , C07D417/14 , C07D419/04
摘要： Heterocyclic substituted pyridine derivatives and their salts and s-oxides are new. The heterocyclic substituted pyridine derivatives of formula (I) and their salts and S-oxides: P and Q = S; N; O; or -CH-; R and R = H or hydrocarbyl, e.g. alkyl (optionally substituted with OH, alkoxy or alkoxycarbonyl); or R or R = -CO-O-R ; or NR R = R4 of formula: m = 0-1; R = hydrocarbyl, alkyl (optionally monosubstituted with aryl or with 1 or more OH, alkoxy (optionally monosubstituted with aryl) or -O-CO-N(R3,1)(R3,2)) or saturated or partly unsaturated heterocyclyl ( optionally substituted with alkyl); R3,1, R3,2 = H or hydrocarbyl; R4,1 = halo, OH, alkoxy or -X-CO-Y(R4,2,1)(R4,2,2); X, Y = N and/or O; R4,2,1, R4,2,2 = H, alkyl (optionally substituted or alkoxycarbonyl); and R4,2,2 = absent when Y=0.

62. 发明专利

DE10019755A1 New cyclic carboxylic acids are integrin antagonists, useful for treating inflammatory diseases, autoimmune and immune disorders, e.g. atherosclerosis, asthma and diabetes 未知
公开(公告)号：DE10019755A1
公开(公告)日：2001-11-08
申请号：DE10019755
申请日：2000-04-20
申请人： BAYER AG
发明人： LEHMANN THOMAS , FISCHER RUEDIGER , ALBERS MARKUS , ROELLE THOMAS , MUELLER GERHARD , HESLER GERHARD , TAJIMI MASAOMI , ZIEGELBAUER KARL , OKIGAMI HIROMI , BACON KEVIN , HASEGAWA HARUKI
IPC分类号： C07D215/08 , A61K31/185 , A61K31/192 , A61K31/198 , A61K31/216 , A61K31/222 , A61K31/27 , A61K31/405 , A61K31/41 , A61K31/426 , A61K31/433 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/06 , A61P25/28 , A61P29/00 , A61P37/00 , A61P37/04 , A61P37/08 , A61P43/00 , C07C237/20 , C07C271/22 , C07C273/18 , C07C275/42 , C07D209/42 , C07D215/48 , C07D257/04 , C07D277/20 , C07D277/46 , C07D285/12 , C07D285/135 , C07K5/08 , A61K38/06
摘要： Cyclic carboxylic acids (I) and their salts are new. Cyclic carboxylic acids of formula (I) and their salts are new. [Image] R1>e.g. a 4-9 membered heterocyclic residue containing 0-3 heteroatoms (N, O or S); where R1> is optionally annulated with a 4-8 membered cyclic residue, containing 0-2 heteroatoms (N, S or O); R2>e.g. H, 1-10C alkyl, 2-10C alkenyl, 2-10C alkynyl (all optionally substituted); R3>e.g. H, 1-10C alkyl, 2-10C alkenyl, 2-10C alkynyl (all optionally substituted); R4>e.g. H, 1-10C alkyl, 2-10C alkenyl, 2-10C alkynyl (all optionally substituted); R5>e.g. H, 1-10C alkyl, 2-10C alkenyl, 2-10C alkynyl (all optionally substituted); R6>e.g. phenyl or 5-6 membered aromatic heterocyclic residue; A : e.g. -C(O)-, -C(O)-C(O) , -SO-, -SO2-, -PO-, -PO2-, 2- or 4-pyrimidyl, or 2-pyridyl; X : -CRx1>Rx2>-; Rx1>, Rx2>e.g. H, 1-4C alkyl, 2-4C alkenyl or 2 4C alkynyl; Y : e.g. -C(O) , -S(O)-, -SO2-, -O- or -S-; D : N or CRD1>; RD1>e.g. a bond, H, 1-4C alkyl, 2-4C alkenyl or 2-4C alkynyl (all optionally substituted); with provisos. The full definitions are given in the DEFINITIONS (Full Definitions) Field. An independent claim is included for the preparation of protected compounds of formula (IV) comprising reacting a carboxylic acid of formula (II) with a carboxylic acid of formula (III), in the presence of a coupling agent and a base in inert solvent. [Image] PG : protecting group. - ACTIVITY : Antiarteriosclerotic; antiasthmatic; antiallergic; antiinflammatory; antidiabetic; neuroprotective; antirheumatic; antiarthritic; immunosuppressive. - MECHANISM OF ACTION : Integrin antagonists. In-vitro assays were carried out to determine adhesion of Jurkat or Ramos cells to immobilized VCAM-1 (domains 1-3). Test compounds typically had IC50 values less than 0.5 MicroM to 10 MicroM.

63. 发明专利

HRP960071B1 N-(3-BENZOFURANYL)UREA-DERIVATIVES 未知
公开(公告)号：HRP960071B1
公开(公告)日：2001-04-30
申请号：HRP960071
申请日：1996-02-13
申请人： BAYER AG
发明人： BRAEUNLICH GABRIELE , FISCHER RUEDIGER , ES-SAYED MAZEN , HENNING ROLF , SPERZEL MICHAEL , SCHLEMMER KARL-HEINZ , NIELSCH ULRICH , TUDHOPE STEPHEN , STURTON GRAHAM , ABRAM TREVOR S , FITZGERALD MARY F
IPC分类号： A61K31/34 , A61K31/343 , C07D307/04 , A61K31/40 , A61K31/44 , A61P1/00 , A61P11/00 , A61P13/12 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/02 , C07D307/82 , C07D307/86 , C07D405/04 , C07D405/12 , C07D407/12
摘要： N-(3-benzofuranyl)urea-derivatives are prepared by reacting of 3-amino-substituted benzofuranes with appropriate substituted isocyanates or isothiocyanates. The N(3-benzofuranyl)urea-derivatives can be used as active ingredients in medicaments particularly for the treatment of acute and chronic inflammatory processes.

64. 发明专利

HK1013285A1 N-(3-benzofuranyl) ureaderivatives 未知
公开(公告)号：HK1013285A1
公开(公告)日：1999-08-20
申请号：HK98114554
申请日：1998-12-22
申请人： BAYER AG
发明人： BRAEUNLICH GARIELE , FISCHER RUEDIGER , ES-SAYED MAZEN , HENNING ROLF , SPERZEL MICHAEL , SCHLEMMER KARL-HEINZ , NIELSCH ULRICH , TUDHOPE STEPHEN , STURTON GRAHAM , ABRAM TREVOR S , FITZGERALD MARY F
IPC分类号： A61K31/34 , C07D307/04 , A61K31/343 , A61K31/40 , A61K31/44 , A61P1/00 , A61P11/00 , A61P13/12 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/02 , C07D307/82 , C07D307/86 , C07D405/04 , C07D405/12 , C07D407/12 , C07D
摘要： N-(3-benzofuranyl)urea-derivatives are prepared by reacting of 3-amino-substituted benzofuranes with appropriate substituted isocyanates or isothiocyanates. The N(3-benzofuranyl)urea-derivatives can be used as active ingredients in medicaments particularly for the treatment of acute and chronic inflammatory processes.

65. 发明专利

HU9600549A2 N-(3-BENZOFURANYL)UREA-DERIVATIVES 未知
公开(公告)号：HU9600549A2
公开(公告)日：1997-07-28
申请号：HU9600549
申请日：1996-03-05
申请人： BAYER AG
发明人： ABRAM TREVOR , BRAEUNLICH GABRIELE , ES-SAYED MAZEN , FISCHER RUEDIGER , FITZGERALD MARY F , HENNING ROLF , NIELSCH ULRICH , SCHLEMMER KARL-HEINZ , SPERZEL MICHAEL , STURTON GRAHAM , TUDHOPE STEPHEN
IPC分类号： A61K31/34 , A61K31/343 , A61K31/40 , C07D307/04 , A61K31/44 , A61P1/00 , A61P11/00 , A61P13/12 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/02 , C07D307/82 , C07D307/86 , C07D405/04 , C07D405/12 , C07D407/12
摘要： N-(3-benzofuranyl)urea-derivatives are prepared by reacting of 3-amino-substituted benzofuranes with appropriate substituted isocyanates or isothiocyanates. The N(3-benzofuranyl)urea-derivatives can be used as active ingredients in medicaments particularly for the treatment of acute and chronic inflammatory processes.

66. 发明专利

HUT71597A OXALYL-AMINO-BENZO-FURANE- AND BENZO-THIENYL-DERIVATIVES, PROCESS FOR PRODUCING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：HUT71597A
公开(公告)日：1996-01-29
申请号：HU9501569
申请日：1995-05-30
申请人： BAYER AG
发明人： BRAEUNLICH GABRIELE , FISCHER RUEDIGER , ES-SAYED MAZEN , HANKO RUDOLF , TUDHOPE STEPHEN , STURTON GRAHAM , ABRAM TREVOR , MCDONALD-GIBSON WENDY J , FITZGERALD MARY F
IPC分类号： A61K31/34 , A61K31/343 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/535 , A61P1/00 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/08 , A61P29/00 , A61P43/00 , C07D307/80 , C07D307/83 , C07D307/84 , C07D333/56 , C07D333/68 , C07D403/12 , C07D405/06 , C07D405/10 , C07D407/12 , C07D409/10 , C07D409/12 , C07D417/12 , C07D405/00 , C07D407/00 , C07D409/00 , C07D413/00 , A61K31/395 , A61K31/425
摘要： The inventive Oxalylamino-benzofuran- and benzothienyl-derivatives are prepared by reacting the appropriate amino substituted benzofuranes and benzothiophenes with oxalic acid derivatives. The inventive compounds are suitable for the prevention and treatment of acute and chronic inflammatory processes, particularly of the airways.

67. 发明专利

AU2028695A Oxalylamino-benzofuran- and benzothienyl-derivatives 未知
公开(公告)号：AU2028695A
公开(公告)日：1995-12-07
申请号：AU2028695
申请日：1995-05-25
申请人： BAYER AG
发明人： BRAEUNLICH GABRIELE , FISCHER RUEDIGER , ES-SAYED MAZEN , HANKO RUDOLF , TUDHOPE STEPHEN , STURTON GRAHAM , ABRAM TREVOR , DONALD-GIBSON WENDY J , FITZGERALD MARY F
IPC分类号： A61K31/34 , A61K31/343 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/535 , A61P1/00 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/08 , A61P29/00 , A61P43/00 , C07D307/80 , C07D307/83 , C07D307/84 , C07D333/56 , C07D333/68 , C07D403/12 , C07D405/06 , C07D405/10 , C07D407/12 , C07D409/10 , C07D409/12 , C07D417/12 , C07D307/82
摘要： The inventive Oxalylamino-benzofuran- and benzothienyl-derivatives are prepared by reacting the appropriate amino substituted benzofuranes and benzothiophenes with oxalic acid derivatives. The inventive compounds are suitable for the prevention and treatment of acute and chronic inflammatory processes, particularly of the airways.

68. 发明专利

HUT67847A BENZOFURANYL- AND -THIOPHENYL-ALKANE-CARBOXYLIC ACID DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND PROCESS FOR PRODUCING THEM 未知
公开(公告)号：HUT67847A
公开(公告)日：1995-05-29
申请号：HU9401415
申请日：1994-05-06
申请人： BAYER AG
发明人： MOHRS KLAUS-HELMUT , HANKO RUDOLF , FISCHER RUEDIGER , BRAEUNLICH GABRIELE , BUTLER-RANSOHOFF JOHN-EDWARD , ES-SAYED MAZEN , STURTON GRAHAM , TUDHOPE STEVE , ABRAM TREVOR , MCDONALD-GIBSON WENDY J
IPC分类号： A61K31/34 , A61K31/343 , A61K31/38 , A61P43/00 , C07D307/80 , C07D307/81 , C07D333/60 , C07D405/06 , C07D405/10 , C07D405/12 , C07D407/12 , C07D413/06 , C07D407/06 , A61K31/35 , A61K31/40 , A61K31/41 , A61K31/435 , A61K31/535
摘要： The benzofuranyl- and -thiophenyl-alkane-carboxylic acid derivatives of the formula (I) wherein R1, R2, R3, T, V, and W are as defined in Claim 1 are prepared by cyclisation of hydroxy acetophenones and related compounds or by Wittig-reaction of benzofuranyl aldehydes. The compounds can be used to prepare medicaments showing antiinflammatory activity.

69. 发明专利

DE10226048A1 Treating cardiovascular diseases, e.g. left ventricular hypertrophy or arrhythmia, using new 2-amino-4-methyl-1,3-thiazole-5-sulfonamide derivatives having AT1 antagonist activity 未知
公开(公告)号：DE10226048A1
公开(公告)日：2003-12-24
申请号：DE10226048
申请日：2002-06-12
申请人： BAYER AG
发明人： BETZ ULRICH , STASCH JOHANNES-PETER , FISCHER RUEDIGER , HENDRIX MARTIN , SCHOHE-LOOP D RUDOLF
IPC分类号： A61K31/425 , C07D277/42 , C07D277/54
摘要： The use of 2-(N-methyl-N-(phenylacetyl or phenylcarbonyl)-amino)-4-methyl-1,3-thiazole-5-sulfonamide derivatives (I) for treating cardiovascular disorders is new. The use of 2-(N-methyl-N-(phenylacetyl or phenylcarbonyl)-amino)-4-methyl-1,3-thiazole-5-sulfonamide derivatives of formula (I) for treating cardiovascular disorders is new. [Image] R1>phenyl, pyridyl or alkoxy; R2>H, cyclopropyl or alkyl (optionally monosubstituted by cyclopropyl, OH, alkoxy, halo, trialkylsilyloxy, phenyl or alkoxyphenyl); and X : CH2 or NH. An independent claim is included for new compounds of formula (I; R2> other than H; X = CH2), with the exception of 2-(1,1'-biphenyl-4-yl)-N-methyl-N-(4-methyl-5-((methylamino)-sulfonyl)-1,3-thiazol-2-yl)-acetamide, 2-(1,1'-biphenyl-4-yl)-N-(5-(((2-ethoxyethyl)-amino)-sulfonyl)-4-methyl-1,3-thiazol-2-yl)-N-methylacetamide, 2-(1,1'-biphenyl-4-yl)-N-(5-(((3-methoxypropyl)-amino)-sulfonyl)-4-methyl-1,3-thiazol-2-yl)-N-methylacetamide, 2-(1,1'-biphenyl-4-yl)-N-(5-(((3-ethoxypropyl)-amino)-sulfonyl)-4-methyl-1,3-thiazol-2-yl)-N-methylacetamide (I'), N-methyl-N-(4-methyl-5-((methylamino)-sulfonyl)-1,3-thiazol-2-yl)-2-(4-(2- or 3-pyridinyl)-phenyl)-acetamide, N-(5-(((2-ethoxyethyl)-amino)-sulfonyl)-4-methyl-1,3-thiazol-2-yl)-2-(4-ethoxyphenyl)-N-methylacetamide, 2-(1,1'-biphenyl-4-yl)-N-(5-(((2-((tert. butyl-(dimethyl)-silyl)-oxy)-ethyl)-amino)-sulfonyl)-4-methyl-1,3-thiazol-2-yl)-N-methylacetamide and N-(5-(((2-((tert. butyl-(dimethyl)-silyl)-oxy)-ethyl)-amino)-sulfonyl)-4-methyl-1,3-thiazol-2-yl)-N-methyl-2-(4-(2-pyridinyl)-phenyl)-acetamide. ACTIVITY : Cardiant; Vasotropic; Antiarrhythmic; Antiarteriosclerotic; Nephrotropic; Cerebroprotective; Nootropic. MECHANISM OF ACTION : Angiotensin II AT1 receptor antagonist. AT1 antagonist IC50 values were 40 nM for the known compound (I') and 70 nM for the new compound N-(5-(cyclopropylaminosulfonyl)-4-methyl-1,3-thiazol-2-yl)-2-(4-(2-pyridinyl)-phenyl)-N-methyl-acetamide (Ia). [Image].

70. 发明专利

DE10210319A1 New thiazole-5-sulfonamide derivatives, useful for the treatment of viral infections in humans and animals, especially herpes simplex or human cytomegalovirus infections 未知
公开(公告)号：DE10210319A1
公开(公告)日：2003-09-18
申请号：DE10210319
申请日：2002-03-08
申请人： BAYER AG
发明人： BENDER WOLFGANG , BETZ ULRICH , KLEYMANN GERALD , BAUMEISTER JUDITH , ECKENBERG PETER , FISCHER RUEDIGER , HANDKE-ERGUEDEN GABRIELE , HENDRIX MARTIN , HENNINGER KERSTIN , JENSEN AXEL , KELDENICH JOERG , REEFSCHLAEGER JUERGEN , SCHMIDT THORSTEN , SCHNEIDER UDO , WEBER OLAF
IPC分类号： C07D277/48 , C07D277/66 , A61K31/426 , C07D417/00
摘要： Thiazole-5-sulfonamide derivatives (I) are new. Thiazole-5-sulfonamide derivatives of formula (I) and their salts are new. R1 = H, halo, R, OR, 1-6C aminoalkyl or 1-6C haloalkyl; R = 1-6C alkyl; R2, R3 = H, 3-8C cycloalkyl or biphenylaminocarbonyl; 1-6C alkyl (substituted with 0-3 of 3-6C cycloalkyl, OR, halo, OH, NH2, OSiR3, 3,4-methylenedioxyphenyl, tetrahydro-2-furyl or N(R21)COOtBu), 5- or 6-membered heteroaryl, 3- to 8-membered heterocyclyl, 6-10C aryl (optionally substituted with OH or OR), PO(OR22)(OR23), COCH(NH)R24 or CH(R25)OCOR26; or NR2R3 = 5- or 6-membered saturated heterocycle optionally containing O; R21-R23 = H or 1-4C alkyl; R24 = the side chain of a natural alpha-amino acid; R25 = 1-4C alkyl; R26 = H, 1-4C alkyl or CH(NH2)R27; R27 = the side chain of a natural alpha-amino acid; R6 = phenyl (substituted with 0-3 of halo), Ar, OR, SR, SCF3, OH, COOH, 1-6C fluoroalkoxy, 1-6C alkyl (optionally substituted with tetrahydro-2-furyl), Het1, Het2, 2-6C alkenyl, OR61, NR62R3, CONR64R5, carbazole, dibenzofuran, dibenzothiophene, xanthene or 9,10-dihydroacridine; Ar = 6-10C aryl (substituted with 0-3 of 1-6C alkanoyl, OR, R, halo, COOR, NO2, CN, 1-6C haloalkyl, 1-6C haloalkoxy, NH2, SR, OH, COOH, CONH2, CONHR, CONRR, mono- or di(1-6C alkanoyl)amino, NHCOOR, SOR, SO2R, OSiR3) or 3- to 8-membered heterocyclyl; Het1 = 5- or 6-membered heteroaryl (optionally substituted as for Ar); Het2 = 3- to 8-membered heterocyclyl (substituted with 0-3 of oxo, halo, OH, COOR, NHCOOR, R, 1-6C haloalkyl and 1-6C hydroxyalkyl); R61 = phenyl optionally substituted with NR66R67; or 1-6C alkyl substituted with 0-3 of OH and/or halo; R66, R67 = H, R or 1-6C acyl; R62, R63 = H, CONH2, CONHR, CONRR, phenyl, 1-6C acyl, or 1-6C alkyl (optionally substituted with OR, 1-6C acyl, Ph or 5- to 6-membered heteroaryl, where phenyl and heteroaryl are substituted with 0-3 of halo and OH); R64, R65 = H or R; R7, R8 = H, R, halo or NH2; A = CR4'R5'-CO-CR4R5, CR4'R5'-CO-NR9, NR9-CO-CR4R5 or NR9'-CO-NR9; R4, R4' = H, 1-6C acyl, 2-6C alkenyl, 3-8C cycloalkyl, COOR, or 1-6C alkyl (substituted with 0-3 of halo, OH, 1-6C acyl, OR, ethoxyethoxy, OPh, 6-10C aryl or NR41R42); R41, R42 = H, 1-6C acyl, R, CONH2, mono- or di(1-6C alkyl)amino(1-6C)alkyl, CONHR, CONRR, 6-10C aryl or COOR, or NR41R42 = optionally oxo-substituted 5- or 6-membered heterocyclyl optionally N-substituted with 1-4C alkyl; R5, R5' = H, R or 1-6C alkanoyl; R9, R9' = H, 1-6C acyl, 2-6 alkenyl, 3-8C cycloalkyl, or 1-6C alkyl substituted with 0-3 of halo, OH, 3-8C cycloalkyl, 1-6C acyl, OR, COOH, NHCOOtBu, ethoxyethoxy, OPh, 6-10C aryl, NR92R93, optionally benzo-fused 5- or 6-membered heteroaryl, 2-pyrrolidyl, 1-R-2pyrrolidinyl, tetrahydro-2-furyl, benzo(1,4)dioxan-2-yl, 2-oxopyrrolidino or OCONR96R97; R92, R93 = groups as defined for R41 and R42; R94 = H or 1-4C alkyl; and R96, R97 = H, or 1-6C alkyl or 6-10C aryl substituted with 0-3 of OH, OR and halo.

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