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71. 发明申请

WO00009480A1 NOVEL SULFONYL DERIVATIVES 审中-公开
标题翻译：新型磺化衍生物
公开(公告)号：WO00009480A1
公开(公告)日：2000-02-24
申请号：PCT/JP1999/004344
申请日：1999-08-11
IPC分类号： A61P7/02 , C07D207/08 , C07D207/12 , C07D207/22 , C07D211/34 , C07D211/70 , C07D213/56 , C07D213/61 , C07D213/73 , C07D213/75 , C07D213/82 , C07D213/84 , C07D213/89 , C07D233/18 , C07D233/54 , C07D233/64 , C07D233/88 , C07D239/42 , C07D239/48 , C07D243/08 , C07D277/28 , C07D277/40 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D491/048 , C07D207/04 , A61K31/415 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/53 , A61K31/535 , A61K31/54 , A61K31/55 , C07D209/44 , C07D215/48 , C07D217/26 , C07D233/26 , C07D235/08 , C07D295/22 , C07D307/85 , C07D333/68 , C07D471/04 , C07D495/04 , C07D498/04 , C07D513/04
CPC分类号： C07D207/08 , C07D207/12 , C07D207/22 , C07D211/34 , C07D211/70 , C07D213/56 , C07D213/61 , C07D213/73 , C07D213/75 , C07D213/82 , C07D213/84 , C07D213/89 , C07D233/18 , C07D233/64 , C07D233/88 , C07D239/42 , C07D239/48 , C07D243/08 , C07D277/40 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： Sulfonyl derivatives represented by the following general formula (I): Q -Q -T -Q -SO2-Q and drugs containing the same (wherein Q is an optionally substituted, saturated or unsaturated, five- or six-membered cyclic hydrocarbon group, a five- or six-membered heterocyclic group, or the like; Q is a single bond, oxygen, sulfur, C1-C6 alkylene or the like; Q is optionally substituted arylalkenyl, heteroarylalkenyl or the like; and T is carbonyl or the like). These compounds have potent FXa-inhibitory effects and promptly exert satisfactory and persistent antithrombotic effects through oral administration, thus being useful as anticoagulant agents little accompanied with side effects.
摘要翻译：由以下通式（I）表示的磺酰基衍生物：Q 1 -Q 2 -T 1 -Q 3 -SO 2 -Q A和含有它们的药物（其中Q 1是任选取代的，饱和或不饱和的五元或六元环烃基，五元或六元杂环基等; Q 2是单键，氧，硫，C 1 -C 6亚烷基或类似物; Q

72. 发明申请

WO99063930A3 NOVEL ANGIOTENSIN RECEPTOR MODULATORS AND THEIR USES 审中-公开
标题翻译：新型血管紧张素受体调节剂及其用途
公开(公告)号：WO99063930A3
公开(公告)日：2000-01-27
申请号：PCT/US1999/011805
申请日：1999-06-07
IPC分类号： G01N33/50 , A61K31/13 , A61K31/136 , A61K31/137 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/27 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/485 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/55 , A61K31/551 , A61K31/5517 , A61K31/662 , A61K38/00 , A61K45/00 , A61K47/48 , A61P9/02 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/02 , A61P13/08 , A61P15/06 , A61P17/04 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/16 , A61P43/00 , C07B61/00 , C07C211/00 , C07C213/00 , C07C215/00 , C07C215/34 , C07C215/60 , C07C217/00 , C07C217/08 , C07C217/10 , C07C217/48 , C07C217/58 , C07C217/90 , C07C237/08 , C07C271/12 , C07C311/37 , C07C323/44 , C07C323/62 , C07D207/06 , C07D207/08 , C07D207/26 , C07D209/08 , C07D211/14 , C07D211/18 , C07D211/42 , C07D211/52 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/84 , C07D213/30 , C07D213/38 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/80 , C07D215/22 , C07D215/48 , C07D221/26 , C07D221/28 , C07D223/04 , C07D235/18 , C07D235/30 , C07D239/95 , C07D241/44 , C07D249/12 , C07D257/04 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D295/02 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/02 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D495/04 , C07D519/00 , C07K1/04 , C07K2/00 , C07K4/00 , C07K7/14 , C07K16/28 , C40B20/00 , G01N33/15 , G01N33/53 , G01N33/543 , G01N33/566 , G01N33/94 , G01N37/00 , A61K39/00 , A61K39/395 , A61K39/44 , A61K51/00
CPC分类号： C07D213/74 , A61K47/55 , C07B2200/11 , C07C215/60 , C07C217/08 , C07C323/62 , C07D211/42 , C07D211/56 , C07D213/80 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D401/12 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07K1/047 , C40B40/00 , G01N33/9406 , G01N2333/62 , G01N2333/70578 , G01N2333/726 , G01N2500/00
摘要： This invention relates to novel multibinding compounds that bind to angiotensin (AT) receptors and modulate their activity. The compounds of this invention comprise 2-10 AT receptor ligands covalently connected by a linker or linkers, wherein the ligands in their monovalent (i.e., unlinked) state bind to one or more types of AT receptors. The manner of linking the ligands together is such that the multibinding agents thus formed demonstrate an increased biologic and/or therapeutic effect as compared to the same number of unlinked ligands made available for binding to AT receptors. The invention also relates to methods of using such compounds and to methods of preparing them. The compounds of this invention are particularly useful for treating diseases and conditions of mammals that are mediated by AT receptors. Accordingly, this invention also relates to pharmaceutical compositions comprising a pharmaceutically acceptable excipient and an effective amount of a compound of this invention.
摘要翻译：本发明涉及结合血管紧张素（AT）受体并调节其活性的新型多结合化合物。本发明的化合物包含通过接头或接头共价连接的2-10个AT受体配体，其中其一价（即未连接）状态的配体与一种或多种类型的AT受体结合。将配体连接在一起的方式使得如此形成的多结合剂与可用于与AT受体结合的相同数目的未连接的配体相比，显示增加的生物学和/或治疗效果。本发明还涉及使用这些化合物的方法及其制备方法。本发明的化合物特别可用于治疗由AT受体介导的哺乳动物的疾病和病症。因此，本发明还涉及包含药学上可接受的赋形剂和有效量的本发明化合物的药物组合物。

73. 发明申请

WO99064042A1 NOVEL THERAPEUTIC AGENTS THAT MODULATE ALPHA-1A ADRENERGIC RECEPTORS 审中-公开
标题翻译：调节ALPHA-1A ADRENERGIC受体的新型治疗药物
公开(公告)号：WO99064042A1
公开(公告)日：1999-12-16
申请号：PCT/US1999/012728
申请日：1999-06-07
IPC分类号： G01N33/50 , A61K31/13 , A61K31/136 , A61K31/137 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/27 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/485 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/55 , A61K31/551 , A61K31/5517 , A61K31/662 , A61K38/00 , A61K45/00 , A61K47/48 , A61P9/02 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/02 , A61P13/08 , A61P15/06 , A61P17/04 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/16 , A61P43/00 , C07B61/00 , C07C211/00 , C07C213/00 , C07C215/00 , C07C215/34 , C07C215/60 , C07C217/00 , C07C217/08 , C07C217/10 , C07C217/48 , C07C217/58 , C07C217/90 , C07C237/08 , C07C271/12 , C07C311/37 , C07C323/44 , C07C323/62 , C07D207/06 , C07D207/08 , C07D207/26 , C07D209/08 , C07D211/14 , C07D211/18 , C07D211/42 , C07D211/52 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/84 , C07D213/30 , C07D213/38 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/80 , C07D215/22 , C07D215/48 , C07D221/26 , C07D221/28 , C07D223/04 , C07D235/18 , C07D235/30 , C07D239/95 , C07D241/44 , C07D249/12 , C07D257/04 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D295/02 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/02 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D495/04 , C07D519/00 , C07K1/04 , C07K2/00 , C07K4/00 , C07K7/14 , C07K16/28 , C40B20/00 , G01N33/15 , G01N33/53 , G01N33/543 , G01N33/566 , G01N33/94 , G01N37/00 , A61K39/00 , A61K39/395 , A61K39/44 , A61K51/00 , C07D317/10
CPC分类号： C07D213/74 , A61K47/55 , C07B2200/11 , C07C215/60 , C07C217/08 , C07C323/62 , C07D211/42 , C07D211/56 , C07D213/80 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D401/12 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07K1/047 , C40B40/00 , G01N33/9406 , G01N2333/62 , G01N2333/70578 , G01N2333/726 , G01N2500/00
摘要： Disclosed are novel multi-binding compounds (agents) which bind alpha-1A adrenergic receptors. The compounds of this invention comprise a plurality of ligands each of which can bind to such receptors thereby modulating the biological processes/functions thereof. Each of the ligands is covalently attached to a linker or linkers which may be the same or different to provide for the multi-binding compound. The linker is selected such that the multi-binding compound so constructed demonstrates increased modulation of the biological processes mediated by the alpha-1A adrenergic receptor.
摘要翻译：公开了结合α-1A肾上腺素能受体的新型多重结合化合物（试剂）。本发明的化合物包含多个配体，每个配体可以与这些受体结合，从而调节其生物学过程/功能。每个配体共价连接到可以相同或不同以提供多重结合化合物的接头或接头。选择接头使得如此构建的多结合化合物显示由α-1A肾上腺素能受体介导的生物过程的增加的调节。

74. 发明申请

WO9963930A2 NOVEL ANGIOTENSIN RECEPTOR MODULATORS AND THEIR USES 审中-公开
标题翻译：新型血管紧张素受体调节剂及其用途
公开(公告)号：WO9963930A2
公开(公告)日：1999-12-16
申请号：PCT/US9911805
申请日：1999-06-07
申请人： ADVANCED MEDICINE INC , MARQUESS DANIEL , THOMAS G ROGER , GRIFFIN JOHN H
发明人： MARQUESS DANIEL , THOMAS G ROGER , GRIFFIN JOHN H
IPC分类号： G01N33/50 , A61K31/13 , A61K31/136 , A61K31/137 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/27 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/485 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/55 , A61K31/551 , A61K31/5517 , A61K31/662 , A61K38/00 , A61K45/00 , A61K47/48 , A61P9/02 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/02 , A61P13/08 , A61P15/06 , A61P17/04 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/16 , A61P43/00 , C07B61/00 , C07C211/00 , C07C213/00 , C07C215/00 , C07C215/34 , C07C215/60 , C07C217/00 , C07C217/08 , C07C217/10 , C07C217/48 , C07C217/58 , C07C217/90 , C07C237/08 , C07C271/12 , C07C311/37 , C07C323/44 , C07C323/62 , C07D207/06 , C07D207/08 , C07D207/26 , C07D209/08 , C07D211/14 , C07D211/18 , C07D211/42 , C07D211/52 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/84 , C07D213/30 , C07D213/38 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/80 , C07D215/22 , C07D215/48 , C07D221/26 , C07D221/28 , C07D223/04 , C07D235/18 , C07D235/30 , C07D239/95 , C07D241/44 , C07D249/12 , C07D257/04 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D295/02 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/02 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D495/04 , C07D519/00 , C07K1/04 , C07K2/00 , C07K4/00 , C07K7/14 , C07K16/28 , C40B20/00 , G01N33/15 , G01N33/53 , G01N33/543 , G01N33/566 , G01N33/94 , G01N37/00 , A61K
CPC分类号： C07D213/74 , A61K47/55 , C07B2200/11 , C07C215/60 , C07C217/08 , C07C323/62 , C07D211/42 , C07D211/56 , C07D213/80 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D401/12 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07K1/047 , C40B40/00 , G01N33/9406 , G01N2333/62 , G01N2333/70578 , G01N2333/726 , G01N2500/00
摘要： This invention relates to novel multibinding compounds that bind to angiotensin (AT) receptors and modulate their activity. The compounds of this invention comprise 2-10 AT receptor ligands covalently connected by a linker or linkers, wherein the ligands in their monovalent (i.e., unlinked) state bind to one or more types of AT receptors. The manner of linking the ligands together is such that the multibinding agents thus formed demonstrate an increased biologic and/or therapeutic effect as compared to the same number of unlinked ligands made available for binding to AT receptors. The invention also relates to methods of using such compounds and to methods of preparing them. The compounds of this invention are particularly useful for treating diseases and conditions of mammals that are mediated by AT receptors. Accordingly, this invention also relates to pharmaceutical compositions comprising a pharmaceutically acceptable excipient and an effective amount of a compound of this invention.
摘要翻译：本发明涉及结合血管紧张素（AT）受体并调节其活性的新型多结合化合物。本发明的化合物包含通过接头或接头共价连接的2-10个AT受体配体，其中其一价（即未连接）状态的配体结合一种或多种类型的AT受体。将配体连接在一起的方式使得如此形成的多结合剂与可用于结合AT受体的相同数目的未连接的配体相比，显示增加的生物学和/或治疗效果。本发明还涉及使用这些化合物的方法及其制备方法。本发明的化合物特别可用于治疗由AT受体介导的哺乳动物的疾病和病症。因此，本发明还涉及包含药学上可接受的赋形剂和有效量的本发明化合物的药物组合物。

75. 发明申请

WO9943285A3 SULPHONAMIDE DERIVATIVES 审中-公开
标题翻译：磺酰胺衍生物
公开(公告)号：WO9943285A3
公开(公告)日：1999-12-09
申请号：PCT/US9903449
申请日：1999-02-18
申请人： LILLY CO ELI , ARNOLD MACKLIN BRIAN , ESCRIBANO ANA MARIA , ORNSTEIN PAUL LESLIE , ZIMMERMAN DENNIS MICHAEL
发明人： ARNOLD MACKLIN BRIAN , ESCRIBANO ANA MARIA , ORNSTEIN PAUL LESLIE , ZIMMERMAN DENNIS MICHAEL
IPC分类号： C07D295/22 , A61K20060101 , A61K31/18 , A61K31/195 , A61K31/24 , A61K31/275 , A61K31/34 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/4433 , A61K31/4436 , A61K31/4453 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/695 , A61P25/00 , A61P43/00 , C07C20060101 , C07C69/616 , C07C255/45 , C07C255/50 , C07C303/38 , C07C303/40 , C07C311/03 , C07C311/04 , C07C311/05 , C07C311/06 , C07D20060101 , C07D207/30 , C07D207/325 , C07D213/30 , C07D213/36 , C07D213/40 , C07D213/42 , C07D213/56 , C07D277/10 , C07D277/12 , C07D277/22 , C07D277/24 , C07D277/28 , C07D295/26 , C07D307/02 , C07D307/52 , C07D307/88 , C07D307/94 , C07D311/96 , C07D333/10 , C07D333/16 , C07D333/18 , C07D333/20 , C07D333/24 , C07D333/38 , C07D401/04 , C07D409/04 , C07F7/08
CPC分类号： C07D213/40 , C07C311/03 , C07C311/04 , C07C311/05 , C07C311/06 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07D277/12 , C07D277/28 , C07D333/20 , C07D409/04
摘要： The present invention provides novel sulphonamide derivatives which are useful for potentiating glutamate receptor function in a mammal requiring treatment, processes for their preparation, and pharmaceutical compositions containing them.
摘要翻译：本发明提供了用于增强需要治疗的哺乳动物的谷氨酸受体功能的新型磺酰胺衍生物，它们的制备方法以及含有它们的药物组合物。

76. 发明申请

WO99047529A1 HETEROCYCLIC SIGNAL TRANSDUCTION INHIBITORS, COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：杂环信号传导抑制剂，它们的组合物
公开(公告)号：WO99047529A1
公开(公告)日：1999-09-23
申请号：PCT/US1999/005970
申请日：1999-03-18
IPC分类号： A61K31/4245 , A61K31/426 , A61K31/675 , A61P9/00 , A61P19/10 , A61P29/00 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D271/06 , C07D277/28 , C07D277/30 , C07D413/06 , C07D417/06 , C07F9/58 , C07F9/6506 , C07F9/653 , C07F9/6539 , C07F9/655 , C07F9/6553 , C07F9/6558 , A61K31/33
CPC分类号： C07D271/06 , C07D277/28 , C07D277/30 , C07D413/06 , C07D417/06 , C07F9/588 , C07F9/653 , C07F9/65318 , C07F9/6539 , C07F9/65515 , C07F9/655345 , C07F9/65583 , C07F9/65586
摘要： This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of formula (I) as defined herein.
摘要翻译：本发明涉及用于抑制细胞内信号转导的化合物，特别是涉及包含含磷酸酪氨酸的蛋白质的一种或多种分子相互作用介导的细胞内信号转导。本发明还涉及包含化合物的药物组合物和涉及化合物的药物和兽药施用的预防和治疗方法。化合物是如本文所定义的式（I）化合物。

77. 发明申请

WO99019300A1 PROSTAGLANDIN AGONISTS AND THEIR USE TO TREAT BONE DISORDERS 审中-公开
标题翻译： PROSTAGLANDIN AGONISTS及其用于治疗骨质疏松症的用途
公开(公告)号：WO99019300A1
公开(公告)日：1999-04-22
申请号：PCT/IB1998/001540
申请日：1998-10-05
IPC分类号： C07D233/06 , A61K20060101 , A61K31/138 , A61K31/18 , A61K31/195 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4174 , A61K31/4178 , A61K31/42 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/435 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4535 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/53 , A61K31/5377 , A61K31/557 , A61K31/663 , A61P13/12 , A61P19/00 , A61P19/08 , A61P19/10 , A61P27/06 , A61P43/00 , C07C20060101 , C07C311/06 , C07C311/08 , C07C311/13 , C07C311/19 , C07D20060101 , C07D207/38 , C07D213/38 , C07D213/70 , C07D213/71 , C07D231/12 , C07D233/84 , C07D239/24 , C07D239/26 , C07D241/12 , C07D261/10 , C07D265/30 , C07D265/32 , C07D271/08 , C07D271/12 , C07D277/20 , C07D277/28 , C07D277/36 , C07D277/56 , C07D277/84 , C07D285/10 , C07D307/81 , C07D317/58 , C07D317/60 , C07D319/18 , C07D333/34 , C07D333/40 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号： C07D213/71 , A61K31/18 , A61K31/185 , A61K31/415 , A61K31/4164 , A61K31/425 , A61K31/44 , A61K31/505 , A61K45/06 , C07C311/19 , C07C311/46 , C07D233/84 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , A61K2300/00
摘要： This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.
摘要翻译：本发明涉及前列腺素激动剂，使用这种前列腺素激动剂的方法，含有这种前列腺素激动剂的药物组合物和含有这种前列腺素激动剂的试剂盒。前列腺素激动剂可用于治疗包括骨质疏松症在内的骨疾病。

78. 发明申请

WO99011657A1 1-AMINO-7-ISOQUINOLINE DERIVATIVES AS SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：作为丝氨酸蛋白酶抑制剂的1-氨基-7-异喹啉衍生物
公开(公告)号：WO99011657A1
公开(公告)日：1999-03-11
申请号：PCT/GB1998/002600
申请日：1998-08-28
IPC分类号： A61K38/00 , C07D217/22 , C07D217/24 , C07D233/54 , C07D249/08 , C07D277/28 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/14 , C07K5/02 , C07K5/06 , A61K31/47 , A61K38/05 , A61K38/06 , A61K38/07 , C07D217/00 , C07K5/08
CPC分类号： C07D401/12 , A61K38/00 , C07D217/22 , C07D217/24 , C07D401/14 , C07D405/12 , C07D409/14 , C07K5/0207
摘要： The invention relates to serine protease inhibitor compounds of formula (I) where R1 is hydrogen, halo, cyano, nitro or hydroxyl, amino, alkoxy, alkyl, aminoalkyl, hydroxyalkyl, thiol, alkylthio, aminosulphonyl, alkoxyalkyl, alkoxycarbonyl, acyloxymethoxycarbonyl or alkylamino optionally substituted by hydroxy, alkylamino, alkoxy, oxo, aryl, cycloalkyl, amino, halo, cyano, nitro, thiol, alkylthio, alkylsulphonyl, alkylsulphenyl, alkylsulphonamido, alkylaminosulphonyl, haloalkoxy and haloalkyl; R2 is hydrogen, halo, methyl, amino, hydroxy, or oxo; and R is X-X-Y(R7)-L-Lp(D)n; wherein each X independently is a C, N, O or S atom or a CO, CR1, C(R1)2 or NR1 group, at least one X being C, CO, CR1 or a C(R1)2 group; Y (the alpha -atom) is a nitrogen atom or a CR1 group or Y and L taken together form a cyclic group; R7 is a lipophilic group selected from alkyl, alkenyl, mono- or bi-cycloalkyl, aryl, heteroaryl, mono- or bicycloalkylalkyl, mono- or bicycloalkylalkenyl, aralkyl, heteroaryl-alkyl, arylalkenyl, heteroarylalkenyl all optionally substituted by a group R1; L is an organic linker group containing 1 to 5 backbone atoms selected from C, N, O and S, or a branched alkyl or cyclic group; Lp is a lipophilic organic group selected from alkyl, heterocyclic, alkenyl, alkaryl, cycloalkyl, polycycloalkyl, cycloalkenyl, aryl, aralkyl or haloalkyl group or a combination of two or more such groups optionally substituted by one or more of oxa, thia, aza or R1 groups; D is a hydrogen bond donor group; and n is 0, 1 or 2 and salts thereof.
摘要翻译：本发明涉及式（I）的丝氨酸蛋白酶抑制剂化合物，其中R1是氢，卤素，氰基，硝基或羟基，氨基，烷氧基，烷基，氨基烷基，羟基烷基，硫醇，烷硫基，氨基磺酰基，烷氧基烷基，烷氧基羰基，酰氧基甲氧基羰基或烷基氨基被羟基，烷基氨基，烷氧基，氧代，芳基，环烷基，氨基，卤素，氰基，硝基，硫醇，烷硫基，烷基磺酰基，烷基亚磺酰基，烷基磺酰氨基，烷基氨基磺酰基，卤代烷氧基和卤代烷基取代。 R2是氢，卤素，甲基，氨基，羟基或氧代; R为X-X-Y（R7）-L-Lp（D）n; 其中每个X独立地为C，N，O或S原子或CO，CR1，C（R1）2或NR1基团，至少一个X为C，CO，CR1或C（R1）2基团; Y（α原子）是氮原子或CR 1基团，或Y和L一起形成环状基团; R 7是选自烷基，烯基，单 - 或双 - 环烷基，芳基，杂芳基，单 - 或双环烷基烷基，单或双环烷基烯基，芳烷基，杂芳基 - 烷基，芳基烯基，杂芳基烯基的亲油基团，全部任选被基团R 1取代; L是含有1至5个选自C，N，O和S的骨架原子或支链烷基或环基的有机连接基团; Lp是选自烷基，杂环，烯基，烷芳基，环烷基，多环烷基，环烯基，芳基，芳烷基或卤代烷基中的亲脂性有机基团或两个或更多个这样的基团的组合，其任选被一个或多个氧杂，硫杂，氮杂或 R1组; D是氢键供体基团; 和n为0,1或2及其盐。

79. 发明申请

WO99009002A1 PHENOL DERIVATIVES 审中-公开
标题翻译：苯酚衍生物
公开(公告)号：WO99009002A1
公开(公告)日：1999-02-25
申请号：PCT/JP1998/003647
申请日：1998-08-17
IPC分类号： C07C235/38 , C07C237/22 , C07C237/42 , C07C251/36 , C07D277/28 , C07D277/42 , C07D295/135 , A61K31/165 , A61K31/195 , A61K31/27 , A61K31/275 , A61K31/42 , A61K31/425 , A61K31/445 , A61K31/535 , A61K31/54 , C07C255/44 , C07C255/60 , C07D263/32 , C07D263/48 , C07D295/12
CPC分类号： C07D295/135 , C07C235/38 , C07C237/22 , C07C237/42 , C07C251/36
摘要： Phenol derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, exhibiting an excellent depressant activity against the oxidation of LDL and an inhibitory activity against ACAT, thus being useful as therapeutic or preventive drugs for arteriosclerotic diseases. In said formula (I) R is hydroxyl; R and R are each independently hydrogen or alkyl (provided either R or R is alkyl); R is alkyl; and R is a saturated heterocyclic group, heteroaryl, heteroarylamino, cyano, hydroxyl, hydroxyiminomethyl, carboxy, carbamoyl, monoalkylcarbamoyl, dialkylcarbamoyl or alkanoylamino; and A is a single bond or alkylene.
摘要翻译：由通式（I）表示的苯酚衍生物或其药理学上可接受的盐，对LDL的氧化具有优异的抑制活性和对ACAT的抑制活性，因此可用作动脉硬化性疾病的治疗或预防药物。在所述式（I）中，R 1a是羟基; R 1b和R 1c各自独立地为氢或烷基（提供R 1b或R 1c为烷基）; R 2是烷基; R 3是饱和杂环基，杂芳基，杂芳基氨基，氰基，羟基，羟基亚氨基甲基，羧基，氨基甲酰基，单烷基氨基甲酰基，二烷基氨基甲酰基或烷酰基氨基; 而A是单键或亚烷基。

80. 发明申请

WO99005107A1 VITRONECTIN RECEPTOR ANTAGONIST 审中-公开
标题翻译：维生素C受体拮抗剂
公开(公告)号：WO99005107A1
公开(公告)日：1999-02-04
申请号：PCT/US1998/015271
申请日：1998-07-23
IPC分类号： C07D233/60 , A61K31/4164 , A61K31/421 , A61K31/426 , A61K31/44 , A61K31/4458 , A61P3/14 , A61P7/02 , A61P9/10 , A61P11/00 , A61P17/06 , A61P19/02 , A61P19/10 , A61P29/00 , A61P37/06 , A61P43/00 , C07C69/738 , C07D213/74 , C07D233/61 , C07D233/64 , C07D235/02 , C07D239/42 , C07D263/32 , C07D263/62 , C07D277/20 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/60 , C07D471/04 , C07D211/72 , C07D211/84 , C07D213/72 , C07D213/78
CPC分类号： C07D213/74 , C07C69/738 , C07C2602/12
摘要： Compounds of formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis, or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了式（I）化合物，其是玻连蛋白受体拮抗剂，可用于治疗骨质疏松症或其药学上可接受的盐。

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