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1. 发明授权

US4183870A Cyclopentane derivatives 失效
标题翻译：环戊烷衍生物
公开(公告)号：US4183870A
公开(公告)日：1980-01-15
申请号：US835723
申请日：1977-09-22
申请人： Michael P. L. Caton , Edward C. J. Coffee , Gordon L. Watkins
发明人： Michael P. L. Caton , Edward C. J. Coffee , Gordon L. Watkins
IPC分类号： C07C405/00 , C07D309/12 , C07D317/72 , C07F7/18 , C07F9/54 , C07C49/76
CPC分类号： C07D317/72 , C07C405/0025 , C07D309/12 , C07F7/1804 , C07F9/54 , Y10S424/15
摘要： Cyclopentane derivatives of the formula: ##STR1## wherein R.sup.1 represents hydrogen or a carboxylic acyl group, and either (i) R.sup.2 represents a group of the formula:--CR.sup.3 R.sup.4 R.sup.5 II(wherein R.sup.3 and R.sup.4 represent hydrogen or alkyl, and R.sup.5 represents hydrogen, or alkyl, alkoxy, cycloalkyl or adamantyl, or R.sup.5 represents alkyl substituted by alkoxy, or by cycloalkyl or by adamantyl, or the group --CR.sup.3 R.sup.4 R.sup.5 together forms a cycloalkyl or adamantyl group, X represents trans-vinylene or ethylene and Y represents carbonyl or a group of the formula: ##STR2## wherein R.sup.6 represents hydrogen or alkyl, and R.sup.7 represents hydrogen or a carboxylic acyl group, or else(ii) R.sup.2 represents a group of the formula:--A--Z--R.sup.8 IV(wherein A represents alkylene, Z represents a direct bond or oxygen or sulphur, and R.sup.8 represents an aryl or heterocyclyl group which may be substituted by one or more of halogen, alkyl, alkoxy and trihalomethyl), X in formula I represents ethylene or trans-vinylene and Y in formula I represents carbonyl or a group of formula III, or else(iii) R.sup.2 represents a group R.sup.8 and X and Y in formula I represent simultaneously ethylene and carbonyl, trans-vinylene and carbonyl, or ethylene and --CH(OR.sup.7)-- groups respectively. The compounds are new and possess pharmacological properties similar to those of prostaglandins.
摘要翻译：下式的环戊烷衍生物：其中R 1表示氢或羧基酰基，和（i）R 2表示下式基团：-CR 3 R 4 R 5 II（其中R 3和R 4表示氢或烷基，R 5表示氢，或烷基，烷氧基，环烷基或金刚烷基，或R5表示被烷氧基取代的烷基，或环烷基或金刚烷基，或-CR3R4R5一起形成环烷基或金刚烷基，X表示反式 - 亚乙烯基或亚乙基，Y表示羰基或基团其中R 6表示氢或烷基，R 7表示氢或羧基酰基，或者（ⅱ）R 2表示下列基团：-AZ-R 8 IV（其中A表示亚烷基，Z 代表直接键或氧或硫，并且R 8表示可被卤素，烷基，烷氧基和三卤代甲基中的一个或多个取代的芳基或杂环基）。式I中的X表示亚乙基或反式亚乙烯基，式I中的Y 代表或（iii）R 2表示基团R 8，并且式I中的X和Y分别代表亚乙基和羰基，反亚乙烯基和羰基，或亚乙基和-CH（OR 7） - 基团。这些化合物是新的，具有与前列腺素类似的药理学性质。

2. 发明授权

US4325967A Cyclopentane derivatives 失效
标题翻译：环戊烷衍生物
公开(公告)号：US4325967A
公开(公告)日：1982-04-20
申请号：US36644
申请日：1979-05-07
申请人： Michael P. L. Caton , Edward C. J. Coffee , Gordon L. Watkins
发明人： Michael P. L. Caton , Edward C. J. Coffee , Gordon L. Watkins
IPC分类号： C07C405/00 , C07D309/12 , C07D317/72 , C07F7/18 , C07F9/54 , A61K31/12 , A61K31/22 , A61K31/235 , C07C49/723 , C07C49/743 , C07C49/753 , C07C69/003 , C07C69/007 , C07C69/16 , C07C69/78
CPC分类号： C07D317/72 , C07C405/0025 , C07D309/12 , C07F7/1804 , C07F9/54 , Y10S424/15
摘要： Cyclopentane derivatives of the formula: ##STR1## wherein R.sup.1 represents hydrogen or a carboxylic acyl group, and either (i) R.sup.2 represents a group of the formula:--CR.sup.3 R.sup.4 R.sup.5 II (wherein R.sup.3 and R.sup.4 represent hydrogen or alkyl, and R.sup.5 represents hydrogen, or alkyl, alkoxy, cycloalkyl or adamantyl, or R.sup.5 represents alkyl substituted by alkoxy, or by cycloalkyl or by adamantyl, or the group --CR.sup.3 R.sup.4 R.sup.5 together forms a cycloalkyl or adamantyl group), X represents trans-vinylene or ethylene and Y represents carbonyl or a group of the formula: ##STR2## wherein R.sup.6 represents hydrogen or alkyl, and R.sup.7 represents hydrogen or a carboxylic acyl group, or else(ii) R.sup.2 represents a group of the formula:--A--Z--R.sup.8 IV (wherein A represents alkylene, Z represents a direct bond or oxygen or sulphur, and R.sup.8 represents an aryl or heterocyclyl group which may be substituted by one or more of halogen, alkyl, alkoxy and trihalomethyl), X in formula I represents ethylene or trans-vinylene and Y in formula I represents carbonyl or a group of formula III, or else (iii) R.sup.2 represents a group R.sup.8 and X and Y in formula I represent simultaneously ethylene and carbonyl, trans-vinylene and carbonyl, or ethylene and --CH(OR.sup.7)-- groups respectively. The compounds are new and possess pharmacological properties similar to those of prostaglandins.
摘要翻译：式中：R 1表示氢或羧基酰基的环戊烷衍生物，和（i）R 2表示下列基团：-CR 3 R 4 R 5 II（其中R 3和R 4表示氢或烷基，R 5表示氢，或烷基，烷氧基，环烷基或金刚烷基，或R5表示被烷氧基取代的烷基，或由环烷基或金刚烷基取代，或基团-CR3R4R5一起形成环烷基或金刚烷基），X表示反式亚乙烯基或亚乙基，Y表示羰基或下式的基团：其中R6表示氢或烷基，R7表示氢或羧基酰基，或（ii）R2表示下列基团：-AZ-R8 IV（其中A表示亚烷基 Z表示直接键或氧或硫，R8表示可被卤素，烷基，烷氧基和三卤代甲基中的一个或多个取代的芳基或杂环基），式I中的X表示亚乙基或反 - 亚乙烯基，Y表示公式我代表羰基或式III的基团，或者（iii）R 2表示基团R 8，并且式I中的X和Y Y分别代表亚乙基和羰基，反亚乙烯基和羰基，或亚乙基和-CH（OR 7） - 基团。这些化合物是新的，具有与前列腺素类似的药理学性质。

3. 发明授权

US4171375A Cyclopentane derivatives and their pharmaceutical compositions 失效
标题翻译：环戊烷衍生物及其药物组合物
公开(公告)号：US4171375A
公开(公告)日：1979-10-16
申请号：US758797
申请日：1977-01-12
申请人： Michael P. L. Caton , Trevor Parker , Gordon L. Watkins
发明人： Michael P. L. Caton , Trevor Parker , Gordon L. Watkins
IPC分类号： A61K31/20 , A61K9/08 , A61K31/335 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , A61K31/19 , A61K31/215 , A61K31/22 , C07C61/38 , C07C69/145 , C07C69/74 , C07C69/78
CPC分类号： C07C405/00
摘要： Cyclopentane derivatives of the formula: ##STR1## wherein R.sup.1 represents hydrogen or a carboxylic acyl group, R.sup.2 represents hydrogen or alkyl of 1 through 12 carbon atoms, and n represents an integer from 4 through 8, are new compounds possessing pharmacological properties, more particularly the production of hypertension and inhibition of gastric acid secretion. They are also useful in the preparation of 10-hydroxyprostaglandins.
摘要翻译：下式的环戊烷衍生物：其中R1表示氢或羧酰基，R2表示氢或1至12个碳原子的烷基，n表示4至8的整数，是具有药理学性质的新化合物，更具体地说产生高血压和抑制胃酸分泌。它们也可用于制备10-羟基霜霉内酯。

4. 发明授权

US4088695A Cyclopentanone derivatives 失效
标题翻译：环戊烷酮衍生物
公开(公告)号：US4088695A
公开(公告)日：1978-05-09
申请号：US543552
申请日：1975-01-23
申请人： Michael P. L. Caton , Edward C. J. Coffee , Gordon L. Watkins
发明人： Michael P. L. Caton , Edward C. J. Coffee , Gordon L. Watkins
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D309/12 , C07D317/72 , C07F9/54 , C07C49/76 , C07C49/82 , C07C69/16 , C07C69/78
CPC分类号： C07D317/72 , C07C405/0025 , C07D309/12 , C07F9/54
摘要： Cyclopentane derivatives of the formula: ##STR1## wherein R.sup.1 represents hydrogen or a carboxylic acyl group, and either (I) R.sup.2 represents a group of the formula:--CR.sup.3 R.sup.4 R.sup.5 II(wherein R.sup.3 and R.sup.4 represent hydrogen or alkyl, and R.sup.5 represents hydrogen, or alkyl, alkoxy, cycloalkyl or adamantyl, or R.sup.5 represents alkyl substituted by alkoxy, or by cycloalkyl or by adamantyl, or the group --CR.sup.3 R.sup.4 R.sup.5 together forms a cycloalkyl or adamantyl group), X represents trans-vinylene or ethylene and Y represents carbonyl or a group of the formula: ##STR2## wherein R.sup.6 represents hydrogen or alkyl, and R.sup.7 represents hydrogen or a carboxylic acyl group, or else(ii) R.sup.2 represents a group of the formula:--A-Z-R.sup.8 IV(wherein A represents alkylene, Z represents a direct bond or oxygen or sulphur, and R.sup.8 represents an aryl or heterocyclyl group which may be substituted by one or more of halogen, alkyl, alkoxy and trihalomethyl), X in formula I represents ethylene or trans-vinylene and Y in formula I represents carbonyl or a group of formula III, or else(iii) R.sup.2 represents a group R.sup.8 and X and Y in formula I represent simultaneously ethylene and carbonyl, trans-vinylene and carbonyl, or ethylene and --CH(OR.sup.7)-- groups respectively. The compounds are new and possess pharmacological properties similar to those of prostaglandins.

5. 发明授权

US4158062A Cyclopentane derivatives 失效
标题翻译：环戊烷衍生物
公开(公告)号：US4158062A
公开(公告)日：1979-06-12
申请号：US909018
申请日：1978-05-24
申请人： Michael P. L. Caton , Edward C. J. Coffee , Gordon L. Watkins
发明人： Michael P. L. Caton , Edward C. J. Coffee , Gordon L. Watkins
IPC分类号： A61K31/12 , A61K31/557 , A61K31/5575 , A61P1/04 , B01J23/00 , C07B61/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D317/72 , C07C49/28
CPC分类号： C07D317/72 , C07C405/0025 , Y10S514/925
摘要： Compounds of the formula: ##STR1## wherein the two side chains are attached to the ring carbon atoms in the trans configuration, have pharmacological properties typical of prostaglandins, and are especially useful for the treatment of gastric ulceration and gastric hyperacidity.
摘要翻译：下式的化合物：其中两条侧链与反式构型中的环碳原子连接，具有典型的前列腺素的药理学特性，特别可用于治疗胃溃疡和胃酸过多。

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