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1. 发明授权

US4069387A 16-Chloro-substituted prostaglandins and derivatives thereof 失效
标题翻译： 16-氯取代的前列腺素及其衍生物
公开(公告)号：US4069387A
公开(公告)日：1978-01-17
申请号：US709847
申请日：1976-07-29
申请人： Masaki Hayashi , Seiji Kori , Katsuichi Shimoji
发明人： Masaki Hayashi , Seiji Kori , Katsuichi Shimoji
IPC分类号： A61K31/12 , A61K31/19 , A61K31/557 , A61K31/5575 , A61P1/04 , A61P3/04 , A61P3/06 , A61P7/02 , A61P7/10 , A61P9/12 , A61P11/08 , A61P15/00 , A61P15/04 , B01J31/00 , C07B61/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07F9/40 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0025 , C07F9/4006
摘要： The present invention relates to compounds of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## B represents a single bond or a straight- or branched-chain alkylene group containing from 1 to 9 carbon atoms, W represents ethylene or trans-vinylene, X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, R represents a hydroxymethyl group or a grouping of the formula --COOR.sup.4, in which R.sup.4 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 hydrogen atom or a methyl or ethyl group and R.sup.3 represents a hydrogen or chlorine atom or a hydroxy group and cyclodextrin clathrates of such alcohols, acids and esters and, when R.sup.4 in the formula --COOR.sup.4 represents a hydrogen atom, non-toxic salts thereof, and intermediates therefor. These compounds exhibit characteristic prostaglandin-like activity.
摘要翻译：本发明涉及下式的化合物：其中A表示下式的基团：B表示单键或含有1至9个碳原子的直链或支链亚烷基 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，R表示羟甲基或式-COOR4的基团，其中R4表示氢原子或直链，或含有1至12个碳原子的支链烷基，R1表示氢原子或甲基或乙基，R2表示氢原子或甲基或乙基，R3表示氢或氯原子或羟基，这些醇，酸和酯的环糊精包合物，以及当式-COOR 4中的R 4表示氢原子时，其无毒盐及其中间体。这些化合物表现出特征性的前列腺素样活性。

2. 发明授权

US4215142A Prostaglandin analogues 失效
公开(公告)号：US4215142A
公开(公告)日：1980-07-29
申请号：US940685
申请日：1978-09-08
申请人： Masaki Hayashi , Katsuichi Shimoji , Yoshinobu Arai
发明人： Masaki Hayashi , Katsuichi Shimoji , Yoshinobu Arai
IPC分类号： C08L5/00 , A61K31/20 , A61K31/215 , A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D307/937 , C07F1/02 , C07C177/00 , A61K31/14
CPC分类号： C07D307/935 , C07C405/00 , C07D307/937 , C07F1/02 , Y10S514/824 , Y10S514/826 , Y10S514/869 , Y10S514/926 , Y10S514/927
摘要： Prostaglandin E.sub.1 analogues of the general formula: ##STR1## [wherein Y represents ethylene or trans-vinylene, Z represents ethylene or trans-vinylene, R.sup.1 represents a hydrogen atom, an alkyl group containing from 1 to 12 carbon atoms, an aralkyl group containing from 7 to 12 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group containing from 1 to 6 carbon atoms, a phenyl group unsubstituted or substituted by at least one chlorine atom, trifluoromethyl group, alkyl group containing from 1 to 4 carbon atoms or phenyl group, a --C.sub.m H.sub.2m COOR.sup.5 group (wherein m represents an integer of from 1 to 12 and R.sup.5 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms), a --C.sub.n H.sub.2n OR.sup.6 group (wherein R.sup.6 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms and n represents an integer of from 2 to 12), or a ##STR2## group (wherein R.sup.7 and R.sup.8 each represent a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms and n is as hereinbefore defined), R.sup.2 represents a hydrogen atom or a methyl or ethyl group, R.sup.3 represents a single bond or an alkylene group containing from 1 to 4 carbon atoms, R.sup.4 represents a hydrogen atom, an alkyl group containing from 1 to 8 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group containing from 1 to 8 carbon atoms, or represents a phenyl or phenoxy group unsubstituted or substituted by at least one chlorine atom, trifluoromethyl group or alkyl group containing from 1 to 3 carbon atoms, and the wavy line attached to the C-11 and C-15 carbon atoms represents .alpha.- or .beta.- configuration or mixtures thereof] and cyclodextrin clathrates thereof, and, when R.sup.1 represents a hydrogen atom or a group C.sub.m H.sub.2m COOR.sup.5 in which R.sup.5 represents a hydrogen atom, non-toxic salts thereof and, when R.sup.1 represents a group ##STR3## non-toxic acid addition salts thereof, are new compounds and possess characteristic prostaglandin-like properties.

3. 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.

4. 发明授权

US4399147A Prostaglandin 12 analogues and their pharmaceutical compositions 失效
标题翻译：前列腺素12类似物及其药物组合物
公开(公告)号：US4399147A
公开(公告)日：1983-08-16
申请号：US872635
申请日：1978-01-26
申请人： Masaki Hayashi , Yoshinobu Arai , Yoshitaka Konishi , Katsuichi Shimoji , Shuichi Ohuchida , Hirohisa Wakatsuka , Hiroyuki Ito
发明人： Masaki Hayashi , Yoshinobu Arai , Yoshitaka Konishi , Katsuichi Shimoji , Shuichi Ohuchida , Hirohisa Wakatsuka , Hiroyuki Ito
IPC分类号： C07D307/935 , A61K31/34 , A61K31/343 , A61P43/00 , C07C405/00 , C07D307/937 , A61K31/557
CPC分类号： C07D307/937 , C07C405/00
摘要： Prostaglandin I.sub.2 analogues of the formula: ##STR1## [wherein X represents trans-vinylene or an ethylene group unsubstituted or substituted by a bromine atom at the C-5 position, Y represents trans-vinylene or ethylene, R.sup.1 represents hydrogen or an alkyl group containing from 1 to 12 carbon atoms, R.sup.2 represents hydrogen or methyl or ethyl, R.sup.3 represents a single bond or an alkylene group containing from 1 to 4 carbon atoms, R.sup.4 represents hydrogen, an alkyl group containing from 1 to 8 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group containing from 1 to 8 carbon atoms, or a phenyl or phenoxy group unsubstituted or carrying at least one substituent selected from halogen atoms, the trifluoromethyl group and alkyl groups containing from 1 to 3 carbon atoms, and the wavy line attached to the carbon atoms in positions 6, 11 and 15 depicted in the formula represents .alpha.- or .beta.-configuration or mixtures thereof] are new compounds possessing pharmacological properties typical of prostaglandins, for example PGI.sub.2, and are more stable than PGI.sub.2.
摘要翻译：前列腺素I2类似物，具有下式：其中X表示反式亚乙烯基或未被取代或被C-5位上的溴原子取代的亚乙基，Y表示反式亚乙烯基或亚乙基，R 1表示氢或烷基含有1至12个碳原子，R 2表示氢或甲基或乙基，R 3表示单键或含有1至4个碳原子的亚烷基，R 4表示氢，含有1至8个碳原子的烷基，环烷基含有未取代或被至少一个含有1至8个碳原子的烷基取代的4至7个碳原子的基团，或未取代或携带至少一个选自卤素原子的取代基的苯基或苯氧基，三氟甲基和含有 1至3个碳原子，并且连接在式中描述的6,11和15位的碳原子上的波浪线代表α-或β-构型或其混合物] 是具有典型的前列腺素的药理学性质的新化合物，例如PGI 2，并且比PGI2更稳定。

5. 发明授权

US4278688A Prostaglandin analogues 失效
公开(公告)号：US4278688A
公开(公告)日：1981-07-14
申请号：US112676
申请日：1980-01-16
申请人： Masaki Hayashi , Katsuichi Shimoji , Yoshinobu Arai
发明人： Masaki Hayashi , Katsuichi Shimoji , Yoshinobu Arai
IPC分类号： C08L5/00 , A61K31/20 , A61K31/215 , A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D307/937 , C07F1/02 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07D307/937 , C07F1/02 , Y10S514/824 , Y10S514/826 , Y10S514/869 , Y10S514/926 , Y10S514/927
摘要： Prostaglandin E.sub.1 analogues of the general formula: ##STR1## [wherein Y represents ethylene or trans-virylene, Z represents ethylene or trans-vinylene, R.sup.1 represents a hydrogen atom, an alkyl group containing 1 to 12 carbon atoms, an aralkyl group containing from 7 to 12 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group containing from 1 to 6 carbon atoms, a phenyl group unsubstituted or substituted by at least one chlorine atom, trifluoromethyl group, alkyl group containing from 1 to 4 carbon atoms or phenyl group, a--C.sub.m H.sub.2m COOR.sup.5 group (wherein m represents an integer of from 1 to 12 and R.sup.5 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms ), a --C.sub.n H.sub.2n OR.sup.6 group (wherein R.sup.6 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms and n represents an integer of from 2 to 12), or a ##STR2## group (wherein R.sup.7 and R.sup.8 each represent a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms and n is as hereinbefore defined), R.sup.2 represents a hydrogen atom or a methyl or ethyl group, R.sup.3 represents a single bond or an alkylene group containing from 1 to 4 carbon atoms, R.sup.4 represents a hydrogen atom, an alkyl group containing from 1 to 8 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group containing from 1 to 8 carbon atoms, or represents a phenyl or phenoxy group unsubstituted or substituted by at least one chlorine atom, trifuloromethyl group or alkyl group containing from 1 to 3 carbon atoms, and the wavy line attached to the C-11 and C-15 carbon atoms represents .alpha.- or .beta.-configuration or mixtures thereof] and cyclodextrin clathrates thereof, and, when R.sup.1 represents a hydrogen atom or a group C.sub.m H.sub.2m COOR.sup.5 in which R.sup.5 represents a hydrogen atom, non-toxic salts thereof and, when R.sup.1 represents a group ##STR3## non-toxic acid addition salts thereof, are new compounds and possess characteristic prostaglandin-like properties.

6. 发明授权

US4207332A Prostaglandin I.sub.2 analogues 失效
标题翻译：前列腺素I2类似物
公开(公告)号：US4207332A
公开(公告)日：1980-06-10
申请号：US944164
申请日：1978-09-20
申请人： Masaki Hayashi , Yoshinobu Arai , Katsuichi Shimoji , Yoshitaka Konishi , Shuichi Ohuchida , Shinsuke Hashimoto
发明人： Masaki Hayashi , Yoshinobu Arai , Katsuichi Shimoji , Yoshitaka Konishi , Shuichi Ohuchida , Shinsuke Hashimoto
IPC分类号： C07D307/935 , A61K31/34 , A61K31/343 , A61P43/00 , C07C405/00 , C07D307/937 , C07D307/93
CPC分类号： C07D307/937 , C07C405/00
摘要： Prostaglandin analogues of the general formula: ##STR1## [wherein Y represents ethylene or trans-vinylene, R.sup.1 represents a group --C.sub.m H.sub.2m COOR.sup.5, --C.sub.n H.sub.2n OR.sup.6 or ##STR2## (wherein R.sup.5 represents an alkyl group containing from 1 to 4 carbon atoms, R.sup.6 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, R.sup.7 and R.sup.8, which may be the same or different, each represents an alkyl group containing from 1 to 4 carbon atoms, m represents an integer of from 1 to 12 and n represents an integer of from 2 to 12), R.sup.2 represents a hydrogen atom or a methyl or ethyl group, R.sup.3 represents a single bond, or an alkylene group containing from 1 to 4 carbon atoms, R.sup.4 represents a hydrogen atom, an alkyl group containing from 1 to 8 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms in the ring, which may be unsubstituted or substituted by at least one alkyl group containing from 1 to 8 carbon atoms, or represents a phenyl or phenoxy group which may be unsubstituted or substituted by at least one chlorine atom, trifluoromethyl group or alkyl group containing from 1 to 3 carbon atoms, the wavy line attached to the carbon atoms in positions 11 and 15 represents .alpha.- or .beta.-configuration, or mixtures thereof, and the double bond between C.sub.5 -C.sub.6 is Z] and cyclodextrin clathrates thereof, and, when R.sup.1 represents a group ##STR3## in which n, R.sup.7 and R.sup.8 are as hereinbefore defined, non-toxic acid addition salts thereof, are new compounds and possess characteristic prostaglandin-like properties.
摘要翻译：前列腺素类似物具有以下通式：其中Y表示亚乙基或反式亚乙烯基，R1表示基团-CmH2mCOOR5，-CnH2nOR6或其中R5表示含有1至4个碳原子的烷基，R6表示含有1至4个碳原子的氢原子或烷基，可以相同或不同的R 7和R 8各自表示含有1至4个碳原子的烷基，m表示1至12的整数，m表示1至12的整数， n表示2〜12的整数），R2表示氢原子或甲基或乙基，R3表示单键或含有1〜4个碳原子的亚烷基，R4表示氢原子，烷基含有1至8个碳原子的环烷基，环中含有4至7个碳原子的环烷基，其可以是未取代的或被至少一个含有1至8个碳原子的烷基取代，或表示苯基或苯氧基，可以是未取代的或未取代的由至少一个氯原子，三氟甲基或含有1至3个碳原子的烷基取代，连接到位置11和15的碳原子的波浪线表示α或β构型，或其混合物，双键 C5-C6之间是Z]和环糊精包合物，当R1代表其中n，R7和R8如上所定义的基团“IMAGE”时，其无毒的酸加成盐是新的化合物，并且具有特征性的前列腺素 - 像属性。

7. 再颁专利

USRE36385E Glucopyranose derivatives 失效
标题翻译：吡喃葡萄糖衍生物
公开(公告)号：USRE36385E
公开(公告)日：1999-11-09
申请号：US64549
申请日：1993-05-20
申请人： Masaaki Toda , Yutaro Sasaki , Katsuichi Shimoji
发明人： Masaaki Toda , Yutaro Sasaki , Katsuichi Shimoji
IPC分类号： C07H13/04 , C07H13/06 , C07H15/04 , C07H15/18 , A61K31/00 , C07D309/00 , C07H11/00 , C07H13/00
CPC分类号： C07H13/04 , C07H13/06 , C07H15/04 , C07H15/18
摘要： This invention relates to glucopyranose compounds of formula (I) and (IA) ##STR1## and the non-toxic salts thereof wherein the substituents are as defined herein. Such materials possess enhancing activity of cellular immunity (e.g. mitogenic activity) to living tissue and therefore are useful as anti-tumor agents.
摘要翻译：本发明涉及式（I）和（IA）的吡喃葡萄糖化合物及其无毒盐，其中取代基如本文所定义。这样的物质具有提高活体组织的细胞免疫活性（例如有丝分裂活性），因此可用作抗肿瘤剂。

8. 发明授权

US4178367A Prostaglandin I.sub.2 analogues 失效
标题翻译：前列腺素I2类似物
公开(公告)号：US4178367A
公开(公告)日：1979-12-11
申请号：US878571
申请日：1978-02-16
申请人： Hayashi Masaki , Yoshinobu Arai , Yoshitaka Konishi , Katsuichi Shimoji , Shuichi Ohuchida , Hiroyuki Ito , Hirohisa Wakatsuka
发明人： Hayashi Masaki , Yoshinobu Arai , Yoshitaka Konishi , Katsuichi Shimoji , Shuichi Ohuchida , Hiroyuki Ito , Hirohisa Wakatsuka
IPC分类号： C07C405/00 , C07D307/937 , C07F9/40 , A61K31/34 , C07D307/93
CPC分类号： C07D307/937 , C07C405/00 , C07F9/4018
摘要： Prostaglandin I.sub.2 analogues of the formula: ##STR1## (wherein Y represents trans-vinylene or ethylene, R.sup.1 represents hydrogen or an alkyl group containing from 1 to 12 carbon atoms, R.sup.2 represents hydrogen, methyl or ethyl, R.sup.3 represents a single bond, or an alkylene group containing from 1 to 4 carbon atoms, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, each represent hydrogen or an alkyl group containing from 1 to 8 carbon atoms, n represents 3, 4, 5 or 6, the wavy line attached to the carbon atoms in positions 11 and 15 depicted in the formula represents .alpha.- or .beta.-configuration or mixtures thereof, and the double bond between C.sub.6 -C.sub.6 is Z or E) are new compounds possessing pharmacological properties typical of prostaglandins, for example PGI.sub.2.
摘要翻译：前列腺素I2类似物具有下式：其中Y表示反式亚乙烯基或亚乙基，R 1表示氢或含有1至12个碳原子的烷基，R 2表示氢，甲基或乙基，R 3表示单键，或含有1至4个碳原子的亚烷基，可以相同或不同的R 4，R 5和R 6各自表示氢或含有1至8个碳原子的烷基，n表示3,4,5或6 连接在式中描述的位置11和15处的碳原子的波浪线代表α-或β-构型或其混合物，并且C6-C6之间的双键是Z或E）是具有典型的药理学性质的新化合物前列腺素，例如PGI2。

9. 发明授权

US4925929A Glucopyranose derivatives 失效
标题翻译：吡喃葡萄糖衍生物
公开(公告)号：US4925929A
公开(公告)日：1990-05-15
申请号：US338090
申请日：1989-04-14
申请人： Masaaki Toda , Yutaro Sasaki , Katsuichi Shimoji
发明人： Masaaki Toda , Yutaro Sasaki , Katsuichi Shimoji
IPC分类号： C07D309/14 , C07H11/00 , C07H13/04 , C07H13/06 , C07H15/04 , C07H15/18
CPC分类号： C07H13/04 , C07D309/14 , C07H11/00 , C07H13/06 , C07H15/04 , C07H15/18 , Y10S514/885
摘要： This invention relates to glucopyranose compounds of formula (I) and (IA) ##STR1## and the non-toxic salts thereof wherein the substituents are as defined herein. Such materials possess enhancing activity of cellular immunity (e.g. mitogenic activity) to living tissue and therefore are useful as anti-tumor agents.
摘要翻译：本发明涉及式（I）和（IA）的吡喃葡萄糖化合物及其无毒盐，其中取代基如本文所定义。这样的物质具有提高活体组织的细胞免疫活性（例如有丝分裂活性），因此可用作抗肿瘤剂。

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