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1. 发明授权

US5716989A Bicyclo�3.3.0!octane derivatives, process for their production and their pharmaceutical use 失效
标题翻译：双环[3.3.0]辛烷衍生物，其生产工艺及其药物用途
公开(公告)号：US5716989A
公开(公告)日：1998-02-10
申请号：US777363
申请日：1991-11-27
申请人： Ulrich Klar , Hartmut Rehwinkel , Helmut Vorbruggen , Karl Heinz Thierauch , Peter Verhallen
发明人： Ulrich Klar , Hartmut Rehwinkel , Helmut Vorbruggen , Karl Heinz Thierauch , Peter Verhallen
IPC分类号： A61K31/335 , A61K31/357 , A61K31/41 , A61K31/42 , A61K31/421 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/47 , A61K31/557 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/08 , C07C251/42 , C07C281/10 , C07C311/49 , C07C335/40 , C07C405/00 , C07D257/04 , C07D263/10 , C07D263/14 , C07D263/16 , C07D263/22 , C07D319/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D493/08 , A61K31/21
CPC分类号： C07C405/0083
摘要： The invention relates to bicyclo�3.3.0!octane compounds of formula I, ##STR1## wherein the variable are defined in this specification, as well as their enantiomers, and their salts with physiologically compatible bases. .alpha.-, .beta.-, or .tau.-Cyclodextrin clathrates of the compounds and the compounds encapsulated with liposomes are also included. The invention is further directed to processes for production of the compounds and their pharmaceutical use.
摘要翻译：本发明涉及式I的双环[3.3.0]辛烷化合物，其中变体在本说明书中定义，以及它们的对映体及其与生理上相容的碱基的盐。也包括化合物和用脂质体包封的化合物的α-，β-或τ-环糊精包合物。本发明进一步涉及化合物的制备方法及其药物用途。

2. 发明授权

US5489613A Carbacyclin derivatives, process for their preparation and compositions containing them 失效
标题翻译：卡巴环素衍生物，其制备方法和含有它们的组合物
公开(公告)号：US5489613A
公开(公告)日：1996-02-06
申请号：US824696
申请日：1992-01-21
申请人： Kazuo Koyama , Shigeo Amemiya , Koichi Kojima , Shinsaku Kobayashi
发明人： Kazuo Koyama , Shigeo Amemiya , Koichi Kojima , Shinsaku Kobayashi
IPC分类号： C07C405/00 , C07D317/72 , A61K31/557
CPC分类号： C07D317/72 , C07C405/0083 , Y02P20/55
摘要： Compounds of formula (I): ##STR1## have valuable platelet-aggregation inhibitory activities and may be used for the prophylaxis and treatment of such diseases as thrombosis.
摘要翻译：式（I）化合物：（I）具有有价值的血小板聚集抑制活性，可用于预防和治疗诸如血栓形成之类的疾病。

3. 发明授权

US5405870A Carbacyclin compounds; pharmaceutical compositions and method of use 失效
标题翻译：卡巴环素化合物; 药物组合物和使用方法
公开(公告)号：US5405870A
公开(公告)日：1995-04-11
申请号：US147892
申请日：1993-11-04
申请人： Kazuo Koyama , Shigeo Amemiya , Koichi Kojima , Shinsaku Kobayashi
发明人： Kazuo Koyama , Shigeo Amemiya , Koichi Kojima , Shinsaku Kobayashi
IPC分类号： C07C405/00 , C07D317/72 , A61K31/557 , C07C69/732
CPC分类号： C07D317/72 , C07C405/0083 , Y02P20/55
摘要： Compounds of formula (Ic): ##STR1## having valuable platelet-aggregation inhibitory activities useful for the prophylaxis and treatment of such diseases as thrombosis and pharmaceutical compositions containing said compounds.
摘要翻译：式（Ic）化合物：具有有用的预防和治疗诸如血栓形成的疾病和含有所述化合物的药物组合物的有价值的血小板聚集抑制活性的图像（Ic）。

4. 发明授权

US5124343A Carbacyclins, process for the preparation thereof, and use thereof as medicinal agents 失效
标题翻译：卡巴菌素，其制备方法及其作为药剂的用途
公开(公告)号：US5124343A
公开(公告)日：1992-06-23
申请号：US141233
申请日：1988-01-06
申请人： Helmut Vorbrueggen , Hernd Raduechel , Werner Skuballa , Norbert Schwarz , Jorge Casals-Stenzel , Gerda Mannesmann , Michael H. Town
发明人： Helmut Vorbrueggen , Hernd Raduechel , Werner Skuballa , Norbert Schwarz , Jorge Casals-Stenzel , Gerda Mannesmann , Michael H. Town
IPC分类号： C07C45/59 , C07C57/26 , C07C57/60 , C07C405/00 , C07D263/14 , C07D317/72 , C07F9/40
CPC分类号： C07D317/72 , C07C405/0083 , C07C45/59 , C07C57/26 , C07C57/60 , C07D263/14 , C07F9/4018
摘要： The invention relates to carbacyclins of general Formula I ##STR1## wherein R.sub.1 is the residue CH.sub.2 OH or ##STR2## with R.sub.2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl residue, a ##STR3## or heterocyclic residue, or R.sub.1 is the residue ##STR4## with R.sub.3 meaning an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms or the residue R.sub.2, orR.sub.1 is the residue ##STR5## wherein m is the number 1 or 2, X is an oxygen atom or a CH.sub.2 -group,A is a trans--CH.dbd.CH- or --.tbd.C--group,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.- position,n is the number 1, 2, or 3,D is a straight-chain alkylene group of 1-5 carbon atoms,E is a --C.tbd.C---bond or a --CR.sub.6 =CR.sub.7 --group wherein R.sub.6 and R.sub.7 are different from each other and mean a hydrogen atom or an alkyl group of 1-5 carbon atoms or a hydrogen atom or a halogen atom, preferably chlorine,R.sub.4 is an alkyl, cycloalkyl, or optionally substituted arly group, or a heterocyclic group,R.sub.5 is a free or functionally modified hydroxy group, andif R.sub.2 means a hydrogen atom, the salts thereof with physiologically compatible bases;to processes for the preparation thereof, and to the use thereof as blood-pressure-lowering agents.
摘要翻译：本发明涉及通式I的碳霉素，其中R 1是残基CH 2 OH或R 2，其中R 2表示氢原子，烷基，环烷基，芳基，芳基或杂环残基，或者R 1是残基其中R3表示分别为1-10个碳原子的烷酰基或烷磺酰基残基或残基R2，或R1为残基，其中m为数1或2，X为氧原子或CH2- 基团，A是反式-CH = CH-或 - 3BOND C-基团，W是游离或官能改性的羟基亚甲基基团，其中OH-基团可以是α或β位置，n是数1，2 或3，D是1-5个碳原子的直链亚烷基，E是-C3OND C键或-CR6 = CR7-基团，其中R6和R7彼此不同，意指氢原子或1-5个碳原子的烷基或氢原子或卤素原子，优选氯，R4是烷基，环烷基或任选取代的芳基或杂环基团 p，R5是游离或功能改性的羟基，如果R 2表示氢原子，则其与生理上相容的碱的盐; 其制备方法及其作为降血压剂的用途。

5. 发明授权

US5109021A Prostaglandin analogues, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：前列腺素类似物，其制备方法和含有它们的药物组合物
公开(公告)号：US5109021A
公开(公告)日：1992-04-28
申请号：US528865
申请日：1990-05-25
申请人： Katsuhiro Imaki , Hajimu Miyake , Tadao Okegawa
发明人： Katsuhiro Imaki , Hajimu Miyake , Tadao Okegawa
IPC分类号： C07D307/935 , A61K31/557 , A61K31/5575 , A61P7/02 , A61P9/12 , A61P43/00 , C07C51/00 , C07C59/46 , C07C67/00 , C07C69/732 , C07C401/00 , C07C405/00 , C07D209/52 , C07D307/937 , C08B37/00
CPC分类号： C07D307/937 , C07C405/00 , C07C405/0083 , C07D209/52 , C08B37/0015
摘要： The present invention relates to novel isomers of PGAs, PGDs, PGEs, PGFs, 6-keto-PGE.sub.1 s, 6-keto-PGF.sub.1 s, PGI.sub.2 s, 6,9.alpha.-nitrilo-PGI.sub.1 s and 6,9.alpha.-methano-PGI.sub.2 s, having a specific steric configuration, which are replaced by an alkyl (C.sub.1 to C.sub.8)-substituted cycloalkyl (C.sub.4 to C.sub.7) group in (1S,S) form, in (1S,R) form or in cis form at the 15-, 16- or 17-position of the PG skeleton, and, alkyl esters thereof, non-toxic salts thereof, non-toxic acid addition salts thereof and cyclodextrin clathrates thereof, possessing more potent PG-like pharmacological activity than other isomers.

6. 发明授权

US5107014A Prostaglandin I analogue 失效
标题翻译：前列腺素I类似物
公开(公告)号：US5107014A
公开(公告)日：1992-04-21
申请号：US521621
申请日：1990-05-10
申请人： Ryuzo Ueno , Ryuji Ueno , Tomio Oda
发明人： Ryuzo Ueno , Ryuji Ueno , Tomio Oda
IPC分类号： C07C59/90 , C07C405/00
CPC分类号： C07C405/0083 , C07C59/90
摘要： The present invention relates to a new prostagrandine I analogous compounds represented by the following formula (I) and (II). ##STR1## wherein R.sub.1 is a hydrogen atom or alkyl group, at least one of R.sub.2 and/or R.sub.2 ' are a halogen atom, an alkyl group, a group containing an aromatic group, a hydroxyl group or an alkoxy group providing that the R.sub.2 and R.sub.2 ' are not simultaneously hydrogen atoms or salt thereof, which compound is expected as hypotensives.
摘要翻译：本发明涉及由下式（I）和（II）表示的新的前列腺素I类似物。（Ⅰ）其中R1是氢原子或烷基，R2和/或R2'中的至少一个是卤素原子，烷基，含芳基的基团，羟基基团或烷氧基，条件是R2和R2'不同时为氢原子或其盐，该化合物预期作为低渗剂。

7. 发明授权

US4978775A Process for producing bicyclo[3.3.0]octanes 失效
标题翻译：制备双环[3.3.0]辛烷的方法
公开(公告)号：US4978775A
公开(公告)日：1990-12-18
申请号：US890690
申请日：1986-07-16
申请人： Shiro Ikegami , Yasuhiro Torizawa , Seizi Kurozumi
发明人： Shiro Ikegami , Yasuhiro Torizawa , Seizi Kurozumi
IPC分类号： C07F7/18 , C07C51/377 , C07C67/00 , C07C401/00 , C07C405/00
CPC分类号： C07C405/0083 , C07C51/377 , Y02P20/55
摘要： This invention provides a process for producing bicyclo[3.3.0]octanes expressed by the following formula [II] ##STR1## wherein R.sub.11 represents H, a one-equivalent cation or R.sub.1, R.sub..omega.' , represents R.sub..omega.' , and R.sub.21 represents H or R.sub.2,from a thiol compound expressed by the following formula [I], ##STR2## wherein R.sub.1 represents a C.sub.1-10 alkyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted alicyclic group, a substituted or unsubstituted phenyl (C.sub.1-2)alkyl group or a tri(C.sub.1-7 hydrocarbyl)silyl group, Ar represents a substituted or unsubstituted aryl group, R.sub..omega. represents a substituted or unsubstituted C.sub.1-13 alkyl group or a substituted or unsubstituted C.sub.2-13 alkenyl group, and R.sub.2 represents a hydroxyl-protecting group.This process enables to obtain isocarbacyclines or synthetic intermediates therefor with industrial advantages.
摘要翻译： PCT No.PCT / JP85 / 00636 Sec。 371日期：1986年7月16日 102（e）日期1986年7月16日PCT提交1985年11月14日PCT公布。公开号WO86 / 02923 日本公开日1986年5月22日。本发明提供一种由下式[II]表示的双环[3.3.0]辛烷的方法。其中R11表示H，单当量阳离子或R 1，R“ ，由下式[I]表示的硫醇化合物表示R omega'，R 21表示H或R 2，其中R 1表示C 1-10烷基，取代或未取代的苯基，取代或未取代的脂环基，取代或未取代的苯基（C1-2）烷基或三（C1-7烃基）甲硅烷基，Ar表示取代或未取代的芳基，R表示取代或未取代的C1-13烷基或取代或未取代的C 2-3烯基，R 2表示羟基保护基。该方法能够获得具有工业优势的异卡途菌素或其合成中间体。

8. 发明授权

US4971987A New carbacycline, process for their production and their use as a drug 失效
标题翻译：新的碳青霉烯，其生产过程及其作为药物的使用
公开(公告)号：US4971987A
公开(公告)日：1990-11-20
申请号：US164758
申请日：1988-03-07
申请人： Helmut Vorbrueggen , Bob Nieuweboer , Claus-Steffen Stuerzebecher , Ulrich Klar
发明人： Helmut Vorbrueggen , Bob Nieuweboer , Claus-Steffen Stuerzebecher , Ulrich Klar
IPC分类号： C07C59/62 , C07C405/00
CPC分类号： C07C59/62 , C07C405/0083
摘要： The invention also relates to carbacyclin derivatives of general formula I' ##STR1## wherein R.sub.9 is an alkyl group of 1-10 carbon atoms or the group --C.dbd.C--(CH.sub.2).sub.m --R.sub.6 whereinm is 1 to 16 andR.sub.6 is hydroxy on amino.
摘要翻译：本发明还涉及通式Ⅰ'其中R9为1-10个碳原子的烷基或基团-C = C-（CH2）m -R6，其中m为1至16，R6为是氨基上的羟基。

9. 发明授权

US4788319A Novel isocarbacyclins and processes for production thereof 失效
标题翻译：新型异卡波菌素及其制备方法
公开(公告)号：US4788319A
公开(公告)日：1988-11-29
申请号：US44957
申请日：1987-05-01
申请人： Atsuo Hazato , Toshio Tanaka , Noriaki Okamura , Kiyoshi Bannai , Kurozumi, Seizi , Suzuki, Masaaki , Noyori, Ryoji
发明人： Atsuo Hazato , Toshio Tanaka , Noriaki Okamura , Kiyoshi Bannai , Kurozumi, Seizi , Suzuki, Masaaki , Noyori, Ryoji
IPC分类号： C07C405/00 , C07C147/107
CPC分类号： C07C405/0025 , C07C405/0083
摘要： A novel isocarbacyclin which is a compound represented by the following formula ##STR1## wherein R.sup.1 represents a hydrogen atom, or a C.sub.1 -C.sub.4 alkyl or alkenyl group; R.sup.2 and R.sup.3 are identical or different and each represents a hydrogen atom, a tri(C.sub.1 -C.sub.7)hydrocarbon-silyl group or a group forming an acetal linkage together with the oxygen atom of the hydroxyl group; R.sup.4 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.5 represents an unsubstituted linear or branched C.sub.3 -C.sub.8 alkyl group which may be interrupted by an oxygen atom, a substituted linear or branched C.sub.1 -C.sub.5 group in which the substituent is a C.sub.1 -C.sub.6 alkoxy group or a phenyl, phenoxy or C.sub.3 -C.sub.10 cycloalkyl group which may be substituted further, a phenyl group which may be substituted, a phenoxy group which may be substituted, or a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted; n is 0 or 1; and Ar represents a substituted or unsubstituted phenyl group, its enantiomorph, or a mixture both in an arbitrary ratio.
摘要翻译：一种新颖的异卡巴环素，它是由下式表示的化合物：其中R 1表示氢原子或C 1 -C 4烷基或烯基; R2和R3相同或不同，各自表示氢原子，三（C1-C7）烃 - 甲硅烷基或与羟基的氧原子一起形成缩醛键的基团; R4表示氢原子，甲基或乙烯基; R5表示可被氧原子取代的未取代的直链或支链C 3 -C 8烷基，其中取代基为C 1 -C 6烷氧基的取代的直链或支链C 1 -C 5基或苯基，苯氧基或C 3 -C 10 可以被取代的环烷基，可被取代的苯基，可被取代的苯氧基或可被取代的C3-C10环烷基; n为0或1; Ar表示取代或未取代的苯基，其对映体或任意比例的混合物。

10. 发明授权

US4764528A 2,4-pentadienoic acid derivatives and platelet aggregation inhibitors containing the same 失效
标题翻译： 2,4-戊二烯酸衍生物和含有它们的血小板聚集抑制剂
公开(公告)号：US4764528A
公开(公告)日：1988-08-16
申请号：US026993
申请日：1987-03-10
申请人： Keiko Chiba , Makoto Takai , Toshio Wakabayashi
发明人： Keiko Chiba , Makoto Takai , Toshio Wakabayashi
IPC分类号： C07C57/13 , C07C405/00 , C07C59/46 , A61K31/19
CPC分类号： C07C405/0083
摘要： Novel 2,4-pentadienoic acid derivatives are disclosed. As the examples are mentioned 3-(4-carboxy-trans, trans-1,3-butadienyl)-6-exo-(3.alpha.-hydroxy-trans-1-octenyl)-7-endo-hydroxybicyclo[3.3.0]oct-2-ene, 3-(5-carboxy-trans, trans-2,4-pentadienyl)-6-exo-(3.alpha.-hydroxy-trans-1-octenyl)-7-endo-hydroxybicyclo[3.3.0]oct-2-ene and the like. These compounds are useful as a platelet aggregation inhibitor, especially as a thrombosis-prophylactic agent.

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