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1. 发明授权

US4367237A Prostacyclin analogues 失效
公开(公告)号：US4367237A
公开(公告)日：1983-01-04
申请号：US097675
申请日：1979-11-27
申请人： Hirohisa Wakatsuka , Katsuichi Shimoji , Sadahiko Iguchi , Yoshitaka Konishi , Hisashi Suga , Yasuyuki Miyata , Yoichi Iguchi , Hajimu Miyake , Masaki Hayashi
发明人： Hirohisa Wakatsuka , Katsuichi Shimoji , Sadahiko Iguchi , Yoshitaka Konishi , Hisashi Suga , Yasuyuki Miyata , Yoichi Iguchi , Hajimu Miyake , Masaki Hayashi
IPC分类号： C07C405/00 , C07D333/78 , C07D335/04 , A61K31/38
CPC分类号： C07C405/0033 , C07C405/00 , C07D333/78 , C07D335/04
摘要： Prostaglandin analogues of the general formula: ##STR1## [wherein the ring A represents: ##STR2## the ring B represents: ##STR3## (wherein R.sup.6 represents hydrogen, methyl or ethyl, and r is zero, one or two), Y represents ethylene, cis- or trans-vinylene or ethynylene, Z represents a grouping of the formula: --(CH.sub.2).sub.m --, --(CH.sub.2).sub.3 --CHR.sup.7 --, --(CH.sub.2).sub.2 --CHR.sup.7 --CH.sub.2 --, --CH.sub.2 --CHR.sup.7 --(CH.sub.2).sub.2 --, --CHR.sup.7 --(CH.sub.2).sub.3 --, or trans--(CH.sub.2).sub.2 --CH.dbd.CH-- (wherein m is 3, 4 or 5, and R.sup.7 represents methyl or ethyl), R.sup.1 represents a grouping of the formula: --COOR.sup.8, ##STR4## or --CH.sub.2 OR.sup.11 (wherein R.sup.8 represents hydrogen, alkyl, aralkyl, cycloalkyl which is unsubstituted or substituted by at least one alkyl group, or R.sup.8 represents phenyl which is unsubstituted or substituted by halogen, trifluoromethyl, alkyl, alkoxy, alkylthio or phenyl, or represents naphthyl, 2,3- or 1,3-dihydroxypropyl, 2,3- or 1,3-bisalkanoyloxypropyl, a grouping of the formula: -D.sub.1 --COOR.sup.12, ##STR5## -D.sub.2 -R.sup.15 or -D.sub.3 -R.sup.16, wherein D.sub.1 represents alkylene, D.sub.2 represents alkylene, D.sub.3 represents a single bond or alkylene, R.sup.12, R.sup.13 and R.sup.14, each represent alkyl, R.sup.15 represents hydroxy, alkoxy or alkylthio and R.sup.16 represents a heterocyclic ring, or R.sup.8 represents a grouping of the formula: ##STR6## R.sup.9 and R.sup.10, each represent hydrogen, alkyl, alkylsulphonyl, alkanoyl or ##STR7## represents a heterocyclic ring, and R.sup.11 represents hydrogen or alkanoyl, R.sup.2 represents hydrogen, methyl or ethyl, R.sup.3 represents a single bond or alkylene, R.sup.4 represents hydrogen, alkyl, alkoxy, cycloalkyl or cycloalkyloxy unsubstituted or substituted by alkyl, or represents phenyl or phenoxy unsubstituted or substituted by halogen, trifluoromethyl or alkyl with the proviso that, when R.sup.3 represents a single bond, R.sup.4 does not represent alkoxy, cycloalkyloxy or phenoxy, R.sup.5 represents hydrogen, methyl or ethyl and with the proviso that, when one of the groups R.sup.5, R.sup.6 and R.sup.7 represents methyl or ethyl the other two groups are hydrogen atoms] and cyclodextrin clathrates, non-toxic salts and non-toxic acid addition salts thereof, possess selective strong stimulatory activity on uterine contraction in female mammals.

2. 发明授权

US4245099A 2-Acyl-6-aminomethylphenol derivatives 失效
标题翻译： 2-酰基-6-氨基甲基苯酚衍生物
公开(公告)号：US4245099A
公开(公告)日：1981-01-13
申请号：US60113
申请日：1979-07-24
申请人： Hiroyuki Itoh , Mitoshi Konno , Takao Tokuhiro , Sadahiko Iguchi , Masaki Hayashi
发明人： Hiroyuki Itoh , Mitoshi Konno , Takao Tokuhiro , Sadahiko Iguchi , Masaki Hayashi
IPC分类号： A61K31/135 , A61K31/16 , A61K31/165 , A61P29/00 , C07C43/205 , C07C45/00 , C07C45/46 , C07C45/54 , C07C45/67 , C07C49/825 , C07C49/84 , C07C67/00 , C07C213/00 , C07C225/16 , C07C225/18 , C07C233/31 , C07C313/00 , C07C317/00 , C07C323/29 , C07C323/32 , C07C323/41 , C07D213/50
CPC分类号： C07D213/50 , C07C323/00 , C07C43/205 , C07C45/004 , C07C45/46 , C07C45/54 , C07C45/673 , C07C49/825 , C07C49/84 , Y10S514/87
摘要： A 2-acyl-6-aminomethylphenol derivative having the formula (I): ##STR1## wherein R.sup.1 represents a straight chain or branched chain alkyl group of 1 to 6 carbon atoms unsubstituted or substituted with 1 to 3 halogen atoms; a hydrogen atom or a group having the formula (II):--C.sub.n H.sub.2n --R.sup.7 (II)wherein n represents 0 or an integer of 1 to 6; R.sup.7 represents a cycloalkyl group of 3 to 8 carbon atoms unsubstituted or substituted with at least one lower alkyl group; a phenyl group unsubstituted or substituted with at least one lower alkyl group, a halogen atom, a lower alkoxy group or a lower alkylthio group; a lower alkoxy group; a lower alkylthio group; a lower alkylsulfinyl group; a lower alkylsulfonyl group; an N-lower alkylamino group; an N,N-di-lower alkylamino group; or a pyridyl, furyl or thienyl group; R.sup.2 represents a straight chain or branched chain alkyl group of 1 to 6 carbon atoms; a cycloalkyl group of 4 to 8 carbon atoms unsubstituted or substituted with at least one lower alkyl group; a phenyl group unsubstituted or substituted with at least one lower alkyl group, a lower alkoxy group, a lower alkylthio group or a halogen atom; or a lower alkylthio group; R.sup.3 and R.sup.4 each represents a hydrogen atom or R.sup.2 and R.sup.3 or R.sup.2 and R.sup.4 when taken together represent an alkylene group of 2 to 5 carbon atoms unsubstituted or substituted with 1 or 2 lower alkyl groups; R.sup.5 represents a hydrogen atom or a lower alkyl group; and R.sup.6 represents a hydrogen atom, a lower alkyl group or an acyl group, and the pharmaceutically acceptable acid addition salt thereof having anti-inflammatory, analgesic, antipyretic, diuretic and hypotensive effects that can be used for preventing and curing diseases caused by inflammation, edema, hypertension, etc. are disclosed. Also disclosed is a process for preparing such derivative or a pharmaceutically acceptable acid addition salt thereof.
摘要翻译：具有式（I）的2-酰基-6-氨基甲基苯酚衍生物：其中R 1表示未被取代或被1至3个卤素原子取代的1至6个碳原子的直链或支链烷基; 氢原子或具有式（II）的基团：-C n H 2n-R 7（II）其中n表示0或1至6的整数; R7表示未被取代或被至少一个低级烷基取代的3-8个碳原子的环烷基; 未取代或被至少一个低级烷基，卤素原子，低级烷氧基或低级烷硫基取代的苯基; 低级烷氧基; 低级烷硫基; 低级烷基亚磺酰基; 低级烷基磺酰基; N-低级烷基氨基; N，N-二低级烷基氨基; 或吡啶基，呋喃基或噻吩基; R2表示1〜6个碳原子的直链或支链烷基; 未取代或被至少一个低级烷基取代的4-8个碳原子的环烷基; 未取代或被至少一个低级烷基，低级烷氧基，低级烷硫基或卤素原子取代的苯基; 或低级烷硫基; R 3和R 4各自表示氢原子或R 2，R 3或R 2和R 4一起表示未取代或被1或2个低级烷基取代的2至5个碳原子的亚烷基; R5表示氢原子或低级烷基; R6表示氢原子，低级烷基或酰基，及其药学上可接受的酸加成盐，其具有抗炎，镇痛，解热，利尿和降血压作用，可用于预防和治疗由炎症引起的疾病，水肿，高血压等。还公开了制备此类衍生物或其药学上可接受的酸加成盐的方法。

3. 发明授权

US4180675A 15-Cycloalkyl-prostaglandin derivatives 失效
标题翻译： 15-环烷基 - 前列腺素衍生物
公开(公告)号：US4180675A
公开(公告)日：1979-12-25
申请号：US857341
申请日：1977-12-05
申请人： Masaki Hayashi , Seiji Kori , Isao Ohyama , Sadahiko Iguchi , Takanori Okada
发明人： Masaki Hayashi , Seiji Kori , Isao Ohyama , Sadahiko Iguchi , Takanori Okada
IPC分类号： C07C405/00 , C07D309/12 , C07F9/40 , C08B37/00 , C07C177/00
CPC分类号： C08B37/0015 , C07C405/00 , C07D309/12 , C07F9/4006
摘要： The present invention relates to 15-cycloalkyl-prostaglandins of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## W represents ethylene or trans-vinylene, X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, R represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.1 represents a hydrogen atom or a methyl or ethyl group, R.sup.2 represents a straight- or branched-chain alkyl group containing from 2 to 8 carbon atoms or a phenyl group unsubstituted or substituted by an alkyl group containing from 1 to 3 carbon atoms, R.sup.3 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 3 carbon atoms, and n represents 4 or 5 and cyclodextrin clathrates of such acids and esters and, when R represents a hydrogen atom, non-toxic salts thereof.These new compounds exhibit characteristic prostaglandin-like activities.
摘要翻译：本发明涉及下式的15-环烷基 - 前列腺素：其中A表示下式的基团：W表示亚乙基或反式亚乙烯基，X表示亚乙基或顺式亚乙烯基，Y表示亚乙基或反式亚乙烯基 - 亚乙烯基，R表示氢原子或含有1至12个碳原子的直链或支链烷基，R1表示氢原子或甲基或乙基，R2表示直链或支链烷基， 2至8个碳原子的苯基或未被取代或被含有1至3个碳原子的烷基取代的苯基，R 3表示氢原子或含有1至3个碳原子的直链或支链烷基，n 代表这些酸和酯的4或5和环糊精包合物，当R代表氢原子时，其无毒性盐。这些新化合物表现出特征性的前列腺素样活性。

4. 发明授权

US4087620A 15-Cycloalkyl-prostaglandin derivatives 失效
标题翻译： 15-环烷基 - 前列腺素衍生物
公开(公告)号：US4087620A
公开(公告)日：1978-05-02
申请号：US703158
申请日：1976-07-07
申请人： Masaki Hayashi , Seiji Kori , Isao Ohyama , Sadahiko Iguchi , Takanori Okada
发明人： Masaki Hayashi , Seiji Kori , Isao Ohyama , Sadahiko Iguchi , Takanori Okada
IPC分类号： A61K31/557 , A61K31/19 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D309/12 , C07F9/40 , C08B37/00 , C07C177/00
CPC分类号： C07F9/4018 , C07C405/00 , C07D309/12 , C08B37/0015
摘要： The present invention relates to 15-cycloalkyl-prostaglandins of the formula: ##STR1## WHEREIN A represents a grouping of the formula: ##STR2## W represents ethylene or trans-vinylene, X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, R represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.1 represents a hydrogen atom or a methyl or ethyl group, R.sup.2 represents a straight- or branched-chain alkyl group containing from 2 to 8 carbon atoms or a phenyl group unsubstituted or substituted by an alkyl group containing from 1 to 3 carbon atoms, R.sup.3 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 3 carbon atoms, and n represents 4 or 5) and cyclodextrin clathrates of such acids and esters and, when R represents a hydrogen atom, non-toxic salts thereof.These new compounds exhibit characteristic prostaglandin-like activities.
摘要翻译：本发明涉及下式的15-环烷基 - 前列腺素：其中A表示下式的基团：W表示亚乙基或反 - 亚乙烯基，X表示亚乙基或顺式 - 亚乙烯基，Y表示亚乙基或反式 - 亚乙烯基，R表示氢原子或含有1至12个碳原子的直链或支链烷基，R1表示氢原子或甲基或乙基，R2表示直链或支链烷基， 2至8个碳原子的苯基或未被取代或被含有1至3个碳原子的烷基取代的苯基，R 3表示氢原子或含有1至3个碳原子的直链或支链烷基，n 代表4或5）和这些酸和酯的环糊精包合物，当R代表氢原子时，其无毒性盐。

5. 发明授权

US4294849A Prostaglandin analogues 失效
标题翻译：前列腺素类似物
公开(公告)号：US4294849A
公开(公告)日：1981-10-13
申请号：US114804
申请日：1980-01-24
申请人： Masaki Hayashi , Sadahiko Iguchi , Takanori Okada , Akiyoshi Kawasaki
发明人： Masaki Hayashi , Sadahiko Iguchi , Takanori Okada , Akiyoshi Kawasaki
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07F9/40 , C07C177/00
CPC分类号： C07C405/00 , C07F9/4006
摘要： Prostaglandin analogues of the formula:- ##STR1## (wherein R represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms, the wavy line indicates attachment in .alpha.- or .beta.-configuration or a mixture thereof, and the double bonds between C.sub.2 -C.sub.3 and C.sub.13 -C.sub.14 are trans), and cyclodextrin clathrates of such acids and esters, and when R represents a hydrogen atom, non-toxic salts of such acids, possess hypotensive activity, inhibitory activity on blood platelet aggregation and vasodilator activity, and weak diarrhoea-producing activity.
摘要翻译：具有下式的前列腺素类似物： - （其中R表示氢原子或含有1至4个碳原子的直链或支链烷基，波浪线表示以α-或β-构型或混合物的连接其中C2-C3和C13-C14之间的双键是反式的）和这些酸和酯的环糊精包合物，当R代表氢原子时，这种酸的无毒盐具有低血压活性，抑制活性血小板聚集和血管扩张剂活性，以及腹泻产生活性低。

6. 发明授权

US5013734A Novel esters of phenylalkanoic acid 失效
标题翻译：苯基链烷酸的新型酯
公开(公告)号：US5013734A
公开(公告)日：1991-05-07
申请号：US521962
申请日：1990-05-11
申请人： Sadahiko Iguchi , Masanori Kawamura , Tsumoru Miyamoto
发明人： Sadahiko Iguchi , Masanori Kawamura , Tsumoru Miyamoto
IPC分类号： A61K31/44 , A61K31/443 , A61K31/495 , A61K31/535 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , C07D317/24 , C07D317/72 , C07D405/12
CPC分类号： C07D317/72 , C07D317/24
摘要： The esters of phenylalkanoic acid of the formula: ##STR1## wherein R.sup.1 is 4-10 membered, saturated or unsaturated, mono- or bi-cyclic hetero ring containing as hetero atoms:(i) one or two nitrogen,(ii) two or three of nitrogen and sulfur in total, or(iii) one or two sulfur;R.sup.2 is hydrogen; orR.sup.1 and R.sup.2, taken together with a nitrogen to which they are attached, form 4-7 membered, saturated or unsaturated, mono-cyclic hetero ring containing as hetero atoms:(i) one or two nitrogen, or(ii) two or three of nitrogen and oxygen in total, the aforementioned hetero rings, represented by R.sup.1 or formed by R.sup.1 and R.sup.2, taken together with a nitrogen to which they are attached, may be substituted by one substituent selected from C1-4 alkyl and C2-5 acyl;R.sup.3 each, independently, is hydrogen or C1-4 alkyl;R.sup.4 is hydrogen, halogen, trihalomethyl, C1-4 alkyl, C1-4 alkoxy, C2-5 acyl, cyano, nitro or nitroxy;R.sup.5 each, independently, is hydrogen, C1-4 alkyl or phenyl; or the two R.sup.5 's, taken together with a carbon to which they are attached, form cyclopentane or cyclohexane;and the pharmaceutically acceptable acid addition salts thereof, have .beta..sub.1 -adrenergic receptor blocking activity, and therefore, are useful for the prevention of and/or in the treatment of cardiovascular diseases such as angina pectoris, myocardial infarction, congestive heart failure, hypertension, arrhythmia, etc.

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