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公开(公告)号:EP1007033B1
公开(公告)日:2008-04-23
申请号:EP98951317.1
申请日:1998-08-26
申请人: Novartis AG , Novartis Pharma GmbH
发明人: BAUER, Wilfried , COTTENS, Sylvain , GEYL, Dieter , WEITZ-SCHMIDT, Gabriele , KALLEN, Jörg , HOMMEL, Ulrich
IPC分类号: A61K31/365 , A61K31/22 , A61K31/19 , A61K31/44 , C07D309/10 , C07D309/30 , C07D319/06 , C07D213/64
CPC分类号: C07D213/64 , A61K31/00 , A61K31/222 , A61K31/366 , C07C219/24 , C07C235/30 , C07C237/18 , C07C237/22 , C07C2601/08 , C07C2602/28 , C07D207/16 , C07D295/13 , C07D295/145 , C07D295/205 , C07D307/52 , C07D309/10 , C07D309/30 , C07D405/12 , C07D491/10
摘要: The present invention relates to compounds which bind to all or parts of the active binding 'south pole pocket' of the LFA-1 I-domain and their uses as LFA-1 antagonists.
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公开(公告)号:EP1154988B1
公开(公告)日:2004-08-11
申请号:EP00916832.9
申请日:2000-02-14
申请人: Novartis AG , Novartis Pharma GmbH
发明人: BAENTELI, Rolf , BAUER, Wilfried , COTTENS, Sylvain , EHRHARDT, Claus , HOMMEL, Ulrich , KALLEN, Jörg , MEINGASSNER, Josef, Gottfried , NUNINGER, François , WEITZ-SCHMIDT, Gabriele
IPC分类号: C07C235/26 , C07C237/18 , C07C235/30 , C07C237/20 , C07D211/76 , C07D265/24 , C07D401/06 , A61K31/4402 , A61K31/45 , A61K31/4545 , A61K31/535 , A61P9/10 , A61P3/06 , A61P29/00 , A61P37/00
CPC分类号: C07C271/12 , C07C235/26 , C07C235/30 , C07C237/18 , C07C2602/28 , C07D211/76 , C07D265/10
摘要: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.
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公开(公告)号:EP1307486B1
公开(公告)日:2008-04-30
申请号:EP01969555.0
申请日:2001-07-30
申请人: Novartis AG , Novartis Pharma GmbH
发明人: ALBERT, Rainer , BAUER, Wilfried , BODMER, David , BRUNS, Christian , FELNER, Ivo , HELLSTERN, Heribert , LEWIS, Ian , MEISENBACH, Mark , WECKBECKER, Gisbert , WIETFELD, Bernhard
IPC分类号: C07K14/655 , G01N33/74 , A61K51/08
CPC分类号: C07K7/64 , A61K38/00 , C07K14/655 , Y02P20/55
摘要: The invention provides cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.
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公开(公告)号:EP1307486A2
公开(公告)日:2003-05-07
申请号:EP01969555.0
申请日:2001-07-30
申请人: Novartis AG , Novartis Pharma GmbH
发明人: ALBERT, Rainer , BAUER, Wilfried , BODMER, David , BRUNS, Christian , FELNER, Ivo , HELLSTERN, Heribert , LEWIS, Ian , MEISENBACH, Mark , WECKBECKER, Gisbert , WIETFELD, Bernhard
IPC分类号: C07K14/655 , G01N33/74 , A61K51/08
CPC分类号: C07K7/64 , A61K38/00 , C07K14/655 , Y02P20/55
摘要: The invention provides cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.
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公开(公告)号:EP0672057B1
公开(公告)日:2000-09-20
申请号:EP93915814.3
申请日:1993-07-06
申请人: Novartis AG
发明人: BAUER, Wilfried , BRECKENRIDGE, Robin , CARDINAUX, François , GOMBERT, Frank , GRAM, Hermann , RAMAGE, Paul , SCHNEIDER, Helmut , WAELCHLI, Rudolf , ALBERT, Rainer , LEWIS, Ian
IPC分类号: C07K14/635 , C12N15/62 , C12P21/02 , C12N1/20 , A61K38/29
CPC分类号: C07K14/005 , A61K38/00 , C07K14/635 , C07K2319/00 , C07K2319/50 , C07K2319/75 , C12N2795/10222
摘要: PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1) at least one radical selected from an L- or D-α-amino acid, C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to one or more side chain amino groups of the PTH compound; or 2) at least one α-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the α-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form or in salt form, have pharmacological activity, e.g. for preventing or treating all bone conditions which are associated with increased calcium depletion or resorption or in which calcium fixation in the bone is desirable.
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公开(公告)号:EP1007033A1
公开(公告)日:2000-06-14
申请号:EP98951317.1
申请日:1998-08-26
发明人: BAUER, Wilfried , COTTENS, Sylvain , GEYL, Dieter , WEITZ-SCHMIDT, Gabriele , KALLEN, Jörg , HOMMEL, Ulrich
IPC分类号: A61K31/365 , A61K31/22 , A61K31/19 , A61K31/44 , C07D309/10 , C07D309/30 , C07D319/06 , C07D213/64
CPC分类号: C07D213/64 , A61K31/00 , A61K31/222 , A61K31/366 , C07C219/24 , C07C235/30 , C07C237/18 , C07C237/22 , C07C2601/08 , C07C2602/28 , C07D207/16 , C07D295/13 , C07D295/145 , C07D295/205 , C07D307/52 , C07D309/10 , C07D309/30 , C07D405/12 , C07D491/10
摘要: The present invention relates to compounds which bind to all or parts of the active binding 'south pole pocket' of the LFA-1 I-domain and their uses as LFA-1 antagonists.
摘要翻译: 美维林化合物,用于治疗或预防自身免疫疾病,炎症,缺血/再灌注损伤和移植排斥反应。 这样的化合物结合LFA-1 I结构域,从而抑制LFA-1 / ICAM-1或LFA-1 / ICAM-3相互作用。
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公开(公告)号:EP1154988A1
公开(公告)日:2001-11-21
申请号:EP00916832.9
申请日:2000-02-14
发明人: BAENTELI, Rolf , BAUER, Wilfried , COTTENS, Sylvain , EHRHARDT, Claus , HOMMEL, Ulrich , KALLEN, Jörg , MEINGASSNER, Josef, Gottfried , NUNINGER, François , WEITZ-SCHMIDT, Gabriele
IPC分类号: C07C235/26 , C07C237/18 , C07C235/30 , C07C237/20 , C07D211/76 , C07D265/24 , C07D401/06 , A61K31/4402 , A61K31/45 , A61K31/4545 , A61K31/535 , A61P9/10 , A61P3/06 , A61P29/00 , A61P37/00
CPC分类号: C07C271/12 , C07C235/26 , C07C235/30 , C07C237/18 , C07C2602/28 , C07D211/76 , C07D265/10
摘要: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.
摘要翻译: 其中内酯环被改性的美维诺林衍生物具有令人感兴趣的药物性质,特别是在预防或治疗由LFA-1 / ICAM-1相互作用介导的病症或疾病方面。
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公开(公告)号:EP0835263B9
公开(公告)日:2002-07-24
申请号:EP96924811.1
申请日:1996-06-28
发明人: ALBERT, Rainer , BAUER, Wilfried , BRUNS, Christian , CHANDRAMOULI, Nagarajan , LEWIS, Ian , WECKBECKER, Gisbert
IPC分类号: C07K14/655 , A61K38/31
CPC分类号: C07K14/6555 , A61K38/00 , A61K51/083 , A61K51/088
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公开(公告)号:EP0835263B1
公开(公告)日:2001-12-05
申请号:EP96924811.1
申请日:1996-06-28
发明人: ALBERT, Rainer , BAUER, Wilfried , BRUNS, Christian , CHANDRAMOULI, Nagarajan , LEWIS, Ian , WECKBECKER, Gisbert
IPC分类号: C07K14/655 , A61K38/31
CPC分类号: C07K14/6555 , A61K38/00 , A61K51/083 , A61K51/088
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公开(公告)号:EP0835263A2
公开(公告)日:1998-04-15
申请号:EP96924811.0
申请日:1996-06-28
发明人: ALBERT, Rainer , BAUER, Wilfried , BRUNS, Christian , CHANDRAMOULI, Nagarajan , LEWIS, Ian , WECKBECKER, Gisbert
IPC分类号: A61K38 , A61K51 , A61P3 , A61P5 , A61P9 , A61P27 , A61P29 , A61P35 , A61P37 , A61P43 , C07K5 , C07K14 , G06F13 , H04L9 , H04N7
CPC分类号: C07K14/6555 , A61K38/00 , A61K51/083 , A61K51/088
摘要: Somatostatin analogues comprising the amino acid sequence of the formula (I): -(D/L)Trp-Lys-X1-X2, wherein X1 is a substituted Thr, Ser, Tyr, Glu or Cys residue and X2 is an α-amino acid having an aromatic residue on the Cα side chain, or an amino acid unit selected from Dab, Dpr, Dpm, His (Bzl)HyPro, thienyl-Ala, cyclohexyl-Ala and t.-butyl-Ala, the residue Lys of said sequence corresponding to the residue Lys9 of the native somatostatin-14, in free form, in salt form or complexed with a detectable element have interesting pharmacological properties.
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