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公开(公告)号：US4371542A
公开(公告)日：1983-02-01
申请号：US236634
申请日：1981-02-20
IPC分类号： A61K31/40 , A61K31/403 , A61P43/00 , C07D209/52 , C07D307/935 , C07D309/12 , C07D405/12 , C07D409/06 , C07D409/12
CPC分类号： C07D307/935 , C07D209/52 , C07D309/12
摘要： What are disclosed are prostacylin PGI.sub.2 analogs of the formula ##STR1## having a more specific or longer lasting pharmacological action than PGI.sub.2, methods of making these analogs; and methods and pharmaceutical preparations for inhibiting blood platelet aggregation, for treating hypertension, for the treatment or prophylaxis of gastrointestinal ulcers, and for the treatment of asthma.
摘要翻译： 所公开的是具有比PGI2更具体或更持久的药理作用的式“IMAGE”的前列腺酰基PGI2类似物，制备这些类似物的方法; 以及用于抑制血小板聚集，治疗高血压，治疗或预防胃肠溃疡以及用于治疗哮喘的方法和药物制剂。
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2.发明授权Thienyl, thienyloxy or furyl substituted prostaglandin derivatives in the 6-keto-PGE.sub.1 series 失效噻吩基，噻吩基氧基或呋喃基取代的前列腺素衍生物在6-keto-PGE1系列中
公开(公告)号：US4304783A
公开(公告)日：1981-12-08
申请号：US136819
申请日：1980-04-03
IPC分类号： C07D333/16 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/557 , A61K31/5575 , A61P7/02 , A61P9/08 , A61P9/10 , A61P9/12 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/42 , C07D307/937 , C07D307/54 , C07D333/24
CPC分类号： C07D307/937 , C07C405/00 , Y10S514/822
摘要： The invention relates to new prostaglandin derivatives of the 6-keto-PGE.sub.1 series, to processes and intermediates for their manufacture and to their use as medicaments.
摘要翻译： 本发明涉及6-酮基PGE1系列的新型前列腺素衍生物，其制备方法和中间体以及作为药物的用途。
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公开(公告)号：US5648333A
公开(公告)日：1997-07-15
申请号：US487442
申请日：1995-06-07
申请人： Stephan Henke , Hiristo Anagnostopulos , Gerhard Breipohl , Jochen Knolle , Jens Stechl , Bernward Scholkens , Hans-Wolfram Fehlhaber , Hermann Gerhards , Franz Hock
发明人： Stephan Henke , Hiristo Anagnostopulos , Gerhard Breipohl , Jochen Knolle , Jens Stechl , Bernward Scholkens , Hans-Wolfram Fehlhaber , Hermann Gerhards , Franz Hock
CPC分类号： C07K7/18 , A61K38/00 , Y10S514/803
摘要： Peptides of the formula IA-B-C-E-F-K-P-G-M-F'-I (I),wherein the terms A, B, C, E, F, K, P, G, M, F', and I are defined in the specification, have bradykinin antagonist action. Their therapeutic utility includes all pathological states which are mediated, caused or supported by bradykinin and bradykinin-related peptides.
摘要翻译： 其中术语A，B，C，E，F，K，P，G，M，F'和I在本说明书中定义的式IA-BCEFKPGM-F'-I（I）的肽具有缓激肽 拮抗作用。 它们的治疗用途包括缓激肽和缓激肽相关肽介导，引起或支持的所有病理状态。
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公开(公告)号：US5597803A
公开(公告)日：1997-01-28
申请号：US373464
申请日：1995-01-17
申请人： Gerhard Breipohl , Stephan Henke , Jochen Knolle , Bernward Scholkens , Hans-Georg Alpermann , Hermann Gerhards , Klaus Wirth
发明人： Gerhard Breipohl , Stephan Henke , Jochen Knolle , Bernward Scholkens , Hans-Georg Alpermann , Hermann Gerhards , Klaus Wirth
摘要： Peptides of the formula IZ-P-A-B-C-E-F-K-(D)Q-G-M-F'-I (I)and the physiologically tolerated salts thereof, are described.They have an excellent bradykinin-antagonistic action.They are obtained by reacting reacting a fragment with a C-terminal free carboxyl group or its activated derivative with a corresponding fragment with an N-terminal free amino group or assembling the peptide stepwise, where appropriate eliminating in the compound obtained in this way one or more protective groups introduced temporarily to protect other functionalities, and where appropriate converting the compounds of the formula I obtained in this way into the physiologically tolerated salt thereof.
摘要翻译： 描述了式I Z-P-A-B-C-E-F-K-（D）Q-G-M-F'-I（I）的肽及其生理上耐受的盐。 它们具有优异的缓激肽拮抗作用。 它们是通过使片段与C末端游离羧基或其活化衍生物与具有N-末端游离氨基的相应片段反应或逐步组装肽而得到的，如果合适，则以这种方式获得的化合物中的一种或 临时引入更多的保护基团以保护其它官能团，并且在适当的地方将由此获得的式I化合物转化为其生理上耐受的盐。
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5.发明授权Peptides with vasorelaxant, natriuretic and diuretic effects a process for their preparation, agents containing them, and their use 失效具有血管舒张剂，利尿钠和利尿剂的肽会影响其制备过程，含有它们的药剂及其用途
公开(公告)号：US4861755A
公开(公告)日：1989-08-29
申请号：US3237
申请日：1987-01-14
摘要： The invention relates to new peptides of the formula ##STR1## in which X, A, B, C, N', E, F, G and Z have the meanings indicated in the description, to a process for their preparation, to agents containing them, and to their use.
摘要翻译： 本发明涉及式“IMAGE”的新肽，其中X，A，B，C，N'，E，F，G和Z具有说明书中所示的含义，其制备方法，含有 他们和他们的使用。
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公开(公告)号：US4198429A
公开(公告)日：1980-04-15
申请号：US809432
申请日：1977-06-23
IPC分类号： A61K31/215 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： Prostaglandin esters of the formula ##STR1## have valuable therapeutical properties.
摘要翻译： 式“IMAGE”的前列腺素酯具有有价值的治疗特性。
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公开(公告)号：US4182773A
公开(公告)日：1980-01-08
申请号：US816207
申请日：1977-07-15
IPC分类号： C07D339/08 , A61K31/19 , A61K31/215 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D317/72 , C07D339/06 , C07C177/00
CPC分类号： C07D317/72 , C07C405/00 , C07D339/06
摘要： What is disclosed are prostaglandin-analogous cyclopentane derivatives of the formula I ##STR1## wherein R.sup.1 is hydrogen or a linear or branched, saturated or unsaturated aliphatic or cycloaliphatic radical having from 1 to 8 carbon atoms, or an araliphatic radical having from 7 to 9 carbon atoms, or a physiologically tolerable metal, NH.sub.4 or substituted ammonium ion derived from a primary, secondary or tertiary amine;R.sup.2 is a linear or branched, saturated or unsaturated aliphatic hydrocarbon radical having from 1 to 8 carbon atoms;R.sup.3 is hydrogen or a R.sup.4 CO group wherein R.sup.4 is a hydrogen atom or a linear or branched alkyl group having up to 10 carbon atoms;A is a saturated, linear or branched alkylene group having from 2 to 5 carbon atoms, and a process for the manufacture thereof.
摘要翻译： 公开的是具有式I的前列腺素类似环戊烷衍生物，其中R 1是氢或具有1至8个碳原子的直链或支链，饱和或不饱和的脂族或脂环族基团，或具有7至9个 碳原子或生理上可耐受的金属，NH 4或衍生自伯，仲或叔胺的取代的铵离子; R2是具有1至8个碳原子的直链或支链饱和或不饱和的脂族烃基; R3是氢或R4CO基，其中R4是氢原子或具有至多10个碳原子的直链或支链烷基; A是具有2至5个碳原子的饱和直链或支链亚烷基及其制备方法。
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公开(公告)号：US4079145A
公开(公告)日：1978-03-14
申请号：US698491
申请日：1976-06-22
申请人： Dieter-Bernd Reuschling , Klaus Kuhlein , Bernward Scholkens , Rudolf Kunstmann , Ulrich Lerch , Wilhelm Bartmann , Hermann Teufel , Gerhard Beck
发明人： Dieter-Bernd Reuschling , Klaus Kuhlein , Bernward Scholkens , Rudolf Kunstmann , Ulrich Lerch , Wilhelm Bartmann , Hermann Teufel , Gerhard Beck
IPC分类号： C07D207/26 , C07D207/27
CPC分类号： C07D207/27
摘要： The present invention relates to pyrrolidones which are analogues of prostaglandins and to a process for their manufacture. The compounds of the invention have prostaglandin-like pharmacological properties and can therefore be used as pharmaceutical compositions.
摘要翻译： 本发明涉及前列腺素类似物的吡咯烷酮及其制备方法。 本发明的化合物具有前列腺素样药理学性质，因此可用作药物组合物。
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9.发明申请PHARMACEUTICAL FORMULATIONS AND USE THEREOF IN THE PREVENTION OF STROKE, DIABETES AND/OR CONGESTIVE HEART FAILURE 审中-公开药物制剂及其用于预防冲击，糖尿病和/或焦虑性心脏衰竭的药物制剂及其用途公开(公告)号：US20080125472A1
公开(公告)日：2008-05-29
申请号：US12027938
申请日：2008-02-07
申请人： Bernward Scholkens , Norbert Bender , Badrudin Rangoonwala , Gilles Dagenais , Hertzel Gerstein , Anders Ljunggren , Salim Yusuf
发明人： Bernward Scholkens , Norbert Bender , Badrudin Rangoonwala , Gilles Dagenais , Hertzel Gerstein , Anders Ljunggren , Salim Yusuf
CPC分类号： A61K31/519 , A61K31/403 , A61K31/41 , A61K31/4178 , A61K31/4184
摘要： The present invention relates to use of an inhibitor of the renin-angiotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF).
摘要翻译： 本发明涉及肾素 - 血管紧张素系统抑制剂（RAS）或其药学上可接受的衍生物如雷米普利或雷米普利在预防中风，糖尿病和/或充血性心力衰竭（CHF）中的用途。
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公开(公告)号：US5360791A
公开(公告)日：1994-11-01
申请号：US1221
申请日：1993-01-06
CPC分类号： C07D401/12 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/06078 , A61K38/00
摘要： The invention relates to compounds of the formula I ##STR1## in which A denotes a radical of the formula II ##STR2## in which E denotes a CH.sub.2 group or an NR.sup.9 radical,G denotes a radical from the group comprising S, SO, SO.sub.2, O, CO, CS or a direct bond,B denotes an amino acid,D denotes a heterocycle andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.9 are defined in the description, and their salts.The invention in addition relates to a process for the preparation of the compounds of the formula I and their use as pharmaceuticals.
摘要翻译： 本发明涉及式I的化合物，其中A表示式II的基团，其中E表示CH 2基团或NR 9基团，G表示包括S，SO的基团 ，SO 2，O，CO，CS或直接键，B表示氨基酸，D表示杂环，R 1，R 2，R 3，R 4，R 5，R 6和R 9在说明书中定义，及其盐。 本发明还涉及制备式I化合物及其作为药物的用途的方法。
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