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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

US4517202A Prostaglandin analogues 失效
标题翻译：前列腺素类似物
公开(公告)号：US4517202A
公开(公告)日：1985-05-14
申请号：US498315
申请日：1983-05-26
申请人： Clive W. Bird , Helene I. Butler , Michael P. L. Caton , Edward C. J. Coffee , Geoffrey Darnbrough , Terance W. Hart
发明人： Clive W. Bird , Helene I. Butler , Michael P. L. Caton , Edward C. J. Coffee , Geoffrey Darnbrough , Terance W. Hart
IPC分类号： C07C69/67 , A61K31/557 , A61P43/00 , C07C43/196 , C07C45/59 , C07C45/69 , C07C49/743 , C07C49/753 , C07C51/00 , C07C59/11 , C07C59/205 , C07C59/46 , C07C59/76 , C07C67/00 , C07C69/73 , C07C313/00 , C07C323/53 , C07C323/55 , C07C405/00 , C07D317/72 , C07F7/18 , C07F9/40 , C07C177/00
CPC分类号： C07D317/72 , C07C405/0083 , C07C43/196 , C07C45/59 , C07C45/69 , C07C49/743 , C07C49/753 , C07F7/1856 , C07F9/4006
摘要： Prostaglandin analogues of the general formula: ##STR1## (wherein R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group, Y.sup.1 represents a carbonyl or hydroxymethylene group, represents a single or double bond, A.sup.1 represents an alkylene linkage containing 2 or 3 carbon atoms and optionally bearing a methyl or ethyl substituent, R.sup.2 represents a hydrogen atom or a methyl or ethyl group and R.sup.3 represents a hydrogen atom or else R.sup.2 and R.sup.3 form an alkylene linkage containing 2 or 3 carbon atoms, optionally bearing a methyl or ethyl substituent, such that the symbols A.sup.1, R.sup.2 and R.sup.3, together with the carbon atoms through which they are connected, form a cycloalkyl ring of 6, 7 or 8 carbon atoms, optionally bearing one or two methyl or ethyl substituents, X.sup.1 represents an ethylene or trans-vinylene group, Y.sup.2 represents a carbonyl or hydroxymethylene group, and either (i) A.sup.2 represents a straight- or branched-alkylene chain containing from 1 to 3 carbon atoms, Z.sup.1 represents a direct bond or an oxygen or sulphur atom, and R.sup.4 represents a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, optionally substituted by a cycloalkyl group containing from 3 to 8 carbon atoms, or represents a cycloalkyl group containing from 3 to 8 carbon atoms, or represents a phenyl group optionally substituted by a halogen atom or by a trifluoromethyl group or by a straight- or branched-chain alkyl or alkoxy group containing from 1 to 6 carbon atoms, or (ii) A.sup.2 and Z.sup.1 both represent direct bonds and R.sup.4 represents a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, optionally substituted by a cycloalkyl group containing from 3 to 8 carbon atoms, or represents a cycloalkyl group containing from 3 to 8 carbon atoms) and cyclodextrin clathrates thereof and, when R.sup.1 represents a hydrogen atom, non-toxic salts thereof, possess useful pharmacological properties.
摘要翻译：具有以下通式的前列腺素类似物：其中R1表示氢原子或直链或支链烷基，Y1表示羰基或羟基亚甲基，表示单键或双键，A1表示含有 2或3个碳原子，并且任选地带有甲基或乙基取代基，R 2表示氢原子或甲基或乙基，R 3表示氢原子，或者R 2和R 3形成含有2或3个碳原子的亚烷基键，甲基或乙基取代基，使符号A1，R2和R3与它们连接的碳原子一起形成6,7或8个碳原子的环烷基环，任选带有一个或两个甲基或乙基取代基，X1 代表乙烯或反亚乙烯基，Y2表示羰基或羟基亚甲基，和（i）A2表示含有1至3个碳原子的直链或支链亚烷基，Z1表示直接键或氧或硫原子，R4表示含有1至12个碳原子的直链或支链烷基，任选被含有3至8个碳原子的环烷基取代，或表示含有或者表示任选被卤素原子取代的苯基或三氟甲基或通过含有1至6个碳原子的直链或支链烷基或烷氧基，或（ii）A2和 Z1均表示直接键，R4表示含有1至12个碳原子的直链或支链烷基，任选被含有3至8个碳原子的环烷基取代，或表示含有3至8个碳原子的环烷基原子）和环糊精包合物，当R1表示氢原子时，其无毒盐具有有用的药理学性质。

3. 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。

4. 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。

5. 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。

6. 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.

7. 发明授权

US4243683A Tertiary alcohols 失效
标题翻译：叔醇
公开(公告)号：US4243683A
公开(公告)日：1981-01-06
申请号：US948156
申请日：1978-10-03
申请人： Barbara J. Broughton , Michael P. L. Caton , David J. Hambling
发明人： Barbara J. Broughton , Michael P. L. Caton , David J. Hambling
IPC分类号： A01N49/00 , A61K31/045 , A61K31/10 , A61K31/12 , A61P15/00 , C07C27/00 , C07C29/143 , C07C33/02 , C07C33/035 , C07C33/28 , C07C33/30 , C07C33/48 , C07C41/00 , C07C41/26 , C07C43/23 , C07C45/00 , C07C45/72 , C07C49/20 , C07C49/24 , C07C49/248 , C07C49/255 , C07C49/82 , C07C49/835 , C07C67/00 , C07C313/00 , C07C323/14 , C07C323/22 , C07F9/40 , C07F9/535
CPC分类号： C07F9/4006 , A01N49/00 , C07C29/143 , C07C321/00 , C07C33/035 , C07C33/30 , C07C41/26 , C07C43/23 , C07C45/72 , C07C49/24 , C07C49/248 , C07C49/835 , C07F9/4059 , C07F9/535 , C07B2200/07
摘要： Tertiary alcohols of the formula: ##STR1## wherein Y.sup.1 represents a carbonyl or hydroxymethylene group, and either(i) A.sup.1 represents a direct bond and R.sup.1 represents a phenyl group which may optionally carry one or more substituents selected from halogen atoms, straight- or branched-chain alkyl or alkoxy groups, each containing from 1 to 4 carbon atoms, and the trifluoromethyl group, or(ii) A.sup.1 represents a straight- or branched-chain alkylene group containing from 1 to 10 carbon atoms and R.sup.1 represents a hydrogen atom, or a phenyl, phenoxy or phenylthio group each of which may optionally carry one or more substituents selected from halogen atoms, straight- or branched-chain alkyl or alkoxy groups, each containing from 1 to 4 carbon atoms, and the trifluoromethyl group, are new compounds of use in the field of mammalian reproduction and also of use in the control of insects and acarines.
摘要翻译：具有下式的叔醇：其中Y 1表示羰基或羟基亚甲基，和（i）A 1表示直接键，并且R 1表示可任选地携带一个或多个选自卤素原子，直链 - 或支链烷基或烷氧基，每个含有1至4个碳原子，和三氟甲基，或（ii）A1表示含有1至10个碳原子的直链或支链亚烷基，R 1表示氢原子或苯基，苯氧基或苯硫基，其各自可以任选地带有一个或多个选自卤素原子，每个含有1至4个碳原子的直链或支链烷基或烷氧基的取代基，三氟甲基，是哺乳动物繁殖领域中使用的新化合物，也可用于控制昆虫和螨类。

8. 发明授权

US4424374A Bicycloheptane derivatives 失效
标题翻译：双环庚烷衍生物
公开(公告)号：US4424374A
公开(公告)日：1984-01-03
申请号：US243567
申请日：1981-03-13
申请人： Michael P. L. Caton , Keith A. J. Stuttle
发明人： Michael P. L. Caton , Keith A. J. Stuttle
IPC分类号： C07C69/73 , A61K31/19 , A61K31/215 , A61P9/08 , A61P9/10 , A61P15/04 , A61P43/00 , C07C45/67 , C07C51/00 , C07C59/42 , C07C59/46 , C07C59/80 , C07C67/00 , C07C405/00 , C07D307/20 , C07D309/12 , C07C61/38
CPC分类号： C07D309/12 , C07C405/0091 , C07C45/67 , C07C45/673 , C07C59/46 , C07C59/80
摘要： Compounds of the general formula: ##STR1## wherein R.sup.1 represents a straight- or branched-chain alkyl group containing from 1 to 6 carbon atoms or a phenoxy or benzyl group, and pharmaceutically acceptable salts and esters thereof, possess pharmacological properties of use in the fields of mammalian reproduction and cardiovascular disease.
摘要翻译：通式为：其中R 1表示含有1至6个碳原子的直链或支链烷基或苯氧基或苄基的化合物及其药学上可接受的盐和酯，具有用于哺乳动物繁殖和心血管疾病的领域。

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