公开(公告)号：EP1007505B1

公开(公告)日：2003-04-16

申请号：EP98948872.1

申请日：1998-08-26

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： XU, Daqiang ,  FUJIMOTO, Roger, Aki ,  MCQUIRE, Leslie, Wighton ,  MUGRAGE, Benjamin, Biro ,  VAN DUZER, John, Henry

IPC分类号： C07C229/42

CPC分类号： C07C229/42

公开(公告)号：EP1373262B1

公开(公告)日：2010-05-12

申请号：EP02726168.4

申请日：2002-03-13

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： FUJIMOTO, Roger, Aki ,  MCQUIRE, Leslie, Wighton ,  MONOVICH, Lauren, G. ,  NANTERMET, Philippe ,  PARKER, David, Thomas ,  ROBINSON, Leslie, Ann ,  SKILES, Jerry, W. ,  TOMMASI, Ruben, Alberto

IPC分类号： C07D409/12

CPC分类号： C07D401/12 ,  C07D211/34 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12

摘要： Compounds of the formula (I) wherein R represents OH or NHOH; R1 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or acyl derived from a carboxylic acid, from a carbonic acid, from a carbamic acid of from a sulfonic acid; R2 represents biarylsulfonyl or aryloxyarylsufonyl; R3 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl or acyl derived from a carboxylic acid, from a carbonic acid or form a carbamic acid; R4 and R5 represent independently hydrogen, lower alkyl, lower alkoxycarbonyl, aryl-lower alkyl or cycloalkyl-lower alkyl; m is zero, 1, 2 or 3; pharmaceutically acceptable prodrug derivatives thereof; pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; and their use for inhibiting matrix degrading metalloproteinases and preventing or treating matrix metalloproteinase dependent conditions in mammals.

公开(公告)号：EP1567477B1

公开(公告)日：2009-09-09

申请号：EP03767652.5

申请日：2003-11-25

申请人： NOVARTIS AG ,  Novartis Pharma GmbH

发明人： FUJIMOTO, Roger, Aki ,  MCQUIRE, Leslie, Wighton ,  MONOVICH, Lauren, G. ,  MUGRAGE, Benjamin, Biro ,  PARKER, David, Thomas ,  VAN DUZER, John, Henry ,  WATTANASIN, Sompong

IPC分类号： C07C229/42 ,  C07D215/38 ,  C07D215/40 ,  C07D215/42 ,  C07D333/20 ,  C07D317/58 ,  A61K31/33 ,  A61K31/195

CPC分类号： C07D215/38 ,  C07C229/42 ,  C07D215/40 ,  C07D215/44 ,  C07D317/58 ,  C07D333/20 ,  C07D333/28

摘要： Compounds of formula (I) wherein R is hydrogen, lower alkyl, (C3-C8)cycloalkyl, hydroxy, halo, lower alkoxy, trifluoromethoxy, trifluoromethyl or cyano; and A is biaryl, optionally substituted β-naphthyl, bicyclic heterocyclic aryl, (C3-C6)cycloalkylmonocyclic carbocyclic aryl, or (C5 or C6)cycloalkane fused-monocyclic carbocyclic aryl; pharmaceutically acceptable salts thereof, and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.

公开(公告)号：EP1567477A1

公开(公告)日：2005-08-31

申请号：EP03767652.5

申请日：2003-11-25

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： FUJIMOTO, Roger, Aki ,  MCQUIRE, Leslie, Wighton ,  MONOVICH, Lauren, G. ,  MUGRAGE, Benjamin, Biro ,  PARKER, David, Thomas ,  VAN DUZER, John, Henry ,  WATTANASIN, Sompong

IPC分类号： C07C229/42 ,  C07D215/38 ,  C07D215/40 ,  C07D215/42 ,  C07D333/20 ,  C07D317/58 ,  A61K31/33 ,  A61K31/195

CPC分类号： C07D215/38 ,  C07C229/42 ,  C07D215/40 ,  C07D215/44 ,  C07D317/58 ,  C07D333/20 ,  C07D333/28

摘要： Compounds of formula (I) wherein R is hydrogen, lower alkyl, (C3-C8)cycloalkyl, hydroxy, halo, lower alkoxy, trifluoromethoxy, trifluoromethyl or cyano; and A is biaryl, optionally substituted β-naphthyl, bicyclic heterocyclic aryl, (C3-C6)cycloalkylmonocyclic carbocyclic aryl, or (C5 or C6)cycloalkane fused-monocyclic carbocyclic aryl; pharmaceutically acceptable salts thereof, and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.

公开(公告)号：EP1501491A2

公开(公告)日：2005-02-02

申请号：EP03725069.3

申请日：2003-04-22

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： FUJIMOTO, Roger, Aki ,  URBAN, Laszlo,Novartis Institues for Biomedical ,  GONZALEZ, Isabel

IPC分类号： A61K31/196 ,  C07C229/42

CPC分类号： A61K31/196

摘要： The invention provides a method of treating cancer pain, e.g. bone cancer pain, in a subject in need of such treatment which comprises administering to the subject an effective amount of a COX-2 inhibitor; advantageously a compound of formula (I); wherein R, R1 R2, R3, R4, and R5 are as defined; a pharmaceutically acceptable salts thereof; or a pharmaceutically acceptable prodrug ester thereof.

公开(公告)号：EP1373262A2

公开(公告)日：2004-01-02

申请号：EP02726168.4

申请日：2002-03-13

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： FUJIMOTO, Roger, Aki ,  MCQUIRE, Leslie, Wighton ,  MONOVICH, Lauren, G. ,  NANTERMET, Philippe ,  PARKER, David, Thomas ,  ROBINSON, Leslie, Ann ,  SKILES, Jerry, W. ,  TOMMASI, Ruben, Alberto

IPC分类号： C07D409/12

CPC分类号： C07D401/12 ,  C07D211/34 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12

摘要： Compounds of the formula (I) wherein R represents OH or NHOH; R1 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or acyl derived from a carboxylic acid, from a carbonic acid, from a carbamic acid of from a sulfonic acid; R2 represents biarylsulfonyl or aryloxyarylsufonyl; R3 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl or acyl derived from a carboxylic acid, from a carbonic acid or form a carbamic acid; R4 and R5 represent independently hydrogen, lower alkyl, lower alkoxycarbonyl, aryl-lower alkyl or cycloalkyl-lower alkyl; m is zero, 1, 2 or 3; pharmaceutically acceptable prodrug derivatives thereof; pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; and their use for inhibiting matrix degrading metalloproteinases and preventing or treating matrix metalloproteinase dependent conditions in mammals.

公开(公告)号：EP0942903A1

公开(公告)日：1999-09-22

申请号：EP97943901.0

申请日：1997-09-24

申请人： Novartis AG

发明人： GREENSPAN, Paul, David ,  FUJIMOTO, Roger, Aki

IPC分类号： A61K31 ,  A61P29 ,  A61P43 ,  C07C235 ,  C07C255 ,  C07C317 ,  C07C323 ,  C07D213 ,  C07D307 ,  C07D333

CPC分类号： C07D213/69 ,  C07C235/34 ,  C07C317/46 ,  C07C323/62 ,  C07D333/16 ,  C07D333/24

摘要： Disclosed are compounds of formula (I) wherein W is CH or N; R is (mono- or di-carbocyclic or heterocyclic aryl)-lower alkyl; R1 is hydrogen or lower alkyl; R?2 and R3¿ are hydrogen, lower alkyl, lower alkoxy-lower alkyl or aryl-lower alkyl; or R?2 and R3¿ joined together represent lower alkylene optionally interrupted by O, NH, N-lower alkyl or S so as to form a ring with the amide nitrogen; X is O, S, SO, SO¿2? or a direct bond; X?1¿ is O, S, SO, SO¿2? or a direct bond; Y is a direct bond, lower alkylene or lower alkylidene; and Z is carboxyl, 5-tetrazolyl, hydroxymethyl or carboxyl derivatized in the form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; which are useful as LTB-4 antagonists.

公开(公告)号：EP2170907A2

公开(公告)日：2010-04-07

申请号：EP08760422.9

申请日：2008-06-03

申请人： Novartis AG

发明人： FUJIMOTO, Roger, Aki ,  KRASTEL, Philipp ,  LAMARCHE, Matthew, J.

IPC分类号： C07D513/22 ,  A61K31/429 ,  A61K31/4353 ,  A61P31/04

CPC分类号： C07K7/64 ,  A61K38/12 ,  A61K45/06 ,  C07D513/22

摘要： The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.

公开(公告)号：EP1037617A1

公开(公告)日：2000-09-27

申请号：EP98966292.9

申请日：1998-12-10

申请人： Novartis AG ,  Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.

发明人： MARSHALL, Paul, James ,  FUJIMOTO, Roger, Aki

IPC分类号： A61K31/00

CPC分类号： A61K31/166

摘要： Use in medicaments for the treatment of chronic obstructive pulmonary disease of compounds of formula (I) wherein the C(=NH)-NHR3 group may be in tautomeric or isomeric form, or a pharmaceutically acceptable salt thereof, in which: R1 is amino which is mono- or disubstituted by a substitutent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen; R2 is hydrogen, halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy or is hydroxy which is etherified by an aliphatic, araliphatic or aromatic alcohol or by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy or which is esterified by an aliphatic or araliphatic carboxylic acid; R3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid; X1 and X3, independently or one another, are oxygen (-O-) or sulphur (-S-); and X2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical; wherein the phenyl rings of formula (I) may be, independently or one another, further substituted by one or more substituents selected from halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy, and hydroxy which is etherified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; wherein aryl in the above definitions may be, independently of one another, further substituted by one or more substitutents selected from halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy, and hydroxy which is ethereified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; wherein a cycloaliphatic hydrocarbon radical may be substituted by an aliphatic radical.

公开(公告)号：EP1007505A1

公开(公告)日：2000-06-14

申请号：EP98948872.1

申请日：1998-08-26

申请人： Novartis AG ,  Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.

发明人： XU, Daqiang ,  FUJIMOTO, Roger, Aki ,  MCQUIRE, Leslie, Wighton ,  MUGRAGE, Benjamin, Biro ,  VAN DUZER, John, Henry

IPC分类号： C07C229/42

CPC分类号： C07C229/42

摘要： Disclosed are the compounds of formula (I), wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; pharmaceutically acceptable salts thereof; and pharmaceutically acceptable prodrug esters thereof; as selective COX-2 cyclooxygenase inhibitors.

摘要翻译： 公开了式（I）的化合物，其中R是甲基或乙基; R1是氯或氟; R2是氢或氟; R3是氢，氟，氯，甲基，乙基，甲氧基，乙氧基或羟基; R4是氢或氟; 和R5是氯，氟，三氟甲基或甲基; 其药学上可接受的盐; 及其药学上可接受的前药酯; 作为选择性COX-2环加氧酶抑制剂。