公开(公告)号：US4598078A

公开(公告)日：1986-07-01

申请号：US543496

申请日：1983-10-19

申请人： Kikuo Ishizumi ,  Fujio Antoku ,  Yukio Asami

发明人： Kikuo Ishizumi ,  Fujio Antoku ,  Yukio Asami

IPC分类号： A61K31/495 ,  A61K31/505 ,  A61P25/20 ,  C07C51/567 ,  C07C61/09 ,  C07C61/24 ,  C07D209/48 ,  C07D239/42 ,  C07D295/073 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D403/04

CPC分类号： C07D209/48 ,  C07C51/567 ,  C07C61/09 ,  C07C61/24 ,  C07D239/42 ,  C07D295/073 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14

摘要： A succinimide derivative of the formula: ##STR1## wherein A is straight or branched C.sub.2 -C.sub.6 alkylene or alkenylene, B is straight or branched C.sub.3 -C.sub.5 alkylene, D is straight or branched C.sub.2 -C.sub.3 alkylene, E is straight or branched C.sub.2 -C.sub.3 alkylene, R.sup.1 and R.sup.2 are each hydrogen or C.sub.1 -C.sub.4 alkyl, or they may form a single bond and R.sup.3 is a phenyl group optionally substituted with C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen and/or trifluoromethyl, a 2-pyridyl group optionally substituted with halogen, a 2-pyrimidyl group optionally substituted with halogen, a group of the formula: ##STR2## (in which R.sup.4 is hydrogen or phenyl), a group of the formula: CO--R.sup.5 (in which R.sup.5 is adamantyl or furyl) or hydroxy (C.sub.2 -C.sub.4) alkyl, and an acid addition salt thereof, which are useful as anti-anxiety drugs and/or anti-allergic drugs.

摘要翻译： 下式的琥珀酰亚胺衍生物，其中A是直链或支链C 2 -C 6亚烷基或亚烯基，B是直链或支链C 3 -C 5亚烷基，D是直链或支链C 2 -C 3亚烷基，E是直链或支链C 2 -C 6亚烷基， C 3亚烷基，R 1和R 2各自为氢或C 1 -C 4烷基，或者它们可以形成单键，并且R 3是任选被C 1 -C 4烷基，C 1 -C 4烷氧基，卤素和/或三氟甲基取代的苯基， 任选被卤素取代的吡啶基，任选被卤素取代的2-嘧啶基，下式的基团：其中R 4是氢或苯基，其中R 5是 金刚烷基或呋喃基）或羟基（C 2 -C 4）烷基及其酸加成盐，其可用作抗焦虑药物和/或抗过敏药物。

公开(公告)号：US4507303A

公开(公告)日：1985-03-26

申请号：US446047

申请日：1982-12-01

申请人： Kikuo Ishizumi ,  Fujio Antoku ,  Yukio Asami

发明人： Kikuo Ishizumi ,  Fujio Antoku ,  Yukio Asami

IPC分类号： A61K31/40 ,  A61K31/505 ,  C07D209/76 ,  C07D401/12 ,  C07D403/02 ,  C07D403/06 ,  C07D403/12 ,  C07D491/18 ,  C07D403/04 ,  C07D403/14

CPC分类号： C07D401/12 ,  C07D209/76 ,  C07D403/12

摘要： Succinimide derivatives representable by the following formula: ##STR1## wherein X and Y are combined to form a group of the formula: ##STR2## (wherein A is an oxygen atom, a methylene group or an ethylene group and a full line accompanying a broken line ( ) is a single bond or a double bond) and Z is a hydrogen atom or, X and Z are combined to form a group of the formula: ##STR3## (wherein A and a full line are each as defined above) and Y is a hydrogen atom, R is a phenyl group, optionally substituted with halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, a 2-pyridyl group or a 2-pyrimidinyl group and n is an integer of 3 or 4, and pharmaceutically acceptable acid addition salts thereof, which are useful as antianxious substances.

摘要翻译： 可以由下式表示的琥珀酰亚胺衍生物：其中X和Y组合形成下式的基团：其中A是氧原子，亚甲基或亚乙基和全数 伴随虚线（）是单键或双键），Z是氢原子，或X和Z组合形成下式的基团：其中A和全部线各自如所定义 并且Y是氢原子，R是任选被卤素，C 1 -C 4烷基，C 1 -C 4烷氧基或三氟甲基取代的苯基，2-吡啶基或2-嘧啶基，n是3的整数 或4及其药学上可接受的酸加成盐，其可用作抗毒物质。

公开(公告)号：US4543355A

公开(公告)日：1985-09-24

申请号：US689776

申请日：1985-01-08

申请人： Kikuo Ishizumi ,  Fujio Antoku ,  Yukio Asami

发明人： Kikuo Ishizumi ,  Fujio Antoku ,  Yukio Asami

IPC分类号： A61K31/40 ,  A61K31/505 ,  C07D209/76 ,  C07D401/12 ,  C07D403/02 ,  C07D403/06 ,  C07D403/12 ,  C07D491/18 ,  C07D403/04 ,  C07D403/14

CPC分类号： C07D401/12 ,  C07D209/76 ,  C07D403/12

摘要： Succinimide derivatives representable by the following formula: ##STR1## wherein X and Y are combined to form a group of the formula: ##STR2## (wherein A is an oxygen atom, a methylene group or an ethylene group and a full line accompanying a broken line is a single bond or a double bond) and Z is a hydrogen atom or, X and Z are combined to form a group of the formula: ##STR3## (wherein A and a full line are each as defined above) and Y is a hydrogen atom, R is a phenyl group, optionally substituted with halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, a 2-pyridyl group or a 2-pyrimidinyl group and n is an integer of 3 or 4, and pharmaceutically acceptable acid addition salts thereof, which are useful as antianxious substances.

公开(公告)号：US4843078A

公开(公告)日：1989-06-27

申请号：US182085

申请日：1988-04-15

申请人： Kikuo Ishizumi ,  Fujio Antoku ,  Isamu Maruyama ,  Atsuyuki Kojima

发明人： Kikuo Ishizumi ,  Fujio Antoku ,  Isamu Maruyama ,  Atsuyuki Kojima

IPC分类号： C07D213/74 ,  A61K31/495 ,  A61K31/505 ,  A61P25/18 ,  A61P25/20 ,  C07D209/76 ,  C07D213/84 ,  C07D213/85 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12

CPC分类号： C07D401/12 ,  C07D209/76 ,  C07D403/12

摘要： A succinimide derivative of the formula: ##STR1## wherein R is a pyridyl or pyrimidinyl group substituted with at least one member selected from the group consisting of halogen, lower alkyl, lower alkoxy, cyano, benzyloxy, hydroxyl and amino, and n is an integer of 1 or 2, or a pharmaceutically acceptable acid addition salt thereof. The succinimide derivatives are useful as an anti-anxiety drugs.

摘要翻译： 下式的琥珀酰亚胺衍生物，其中R是被选自卤素，低级烷基，低级烷氧基，氰基，苄氧基，羟基和氨基中的至少一个取代的吡啶基或嘧啶基，n是 1或2的整数，或其药学上可接受的酸加成盐。 琥珀酰亚胺衍生物可用作抗焦虑药。

公开(公告)号：US4937249A

公开(公告)日：1990-06-26

申请号：US262575

申请日：1988-10-25

申请人： Fujio Antoku ,  Mayumi Yoshigi ,  Ikutaro Saji ,  Kikuo Ishizumi

发明人： Fujio Antoku ,  Mayumi Yoshigi ,  Ikutaro Saji ,  Kikuo Ishizumi

IPC分类号： C07D413/14 ,  C07D417/14 ,  C07D491/18

CPC分类号： C07D413/14 ,  C07D417/14

摘要： A compound of the formula: ##STR1## or its acid addition salt, which is useful as a psychotic drug.

公开(公告)号：US4745117A

公开(公告)日：1988-05-17

申请号：US844528

申请日：1986-03-27

申请人： Kikuo Ishizumi ,  Fujio Antoku ,  Isamu Maruyama ,  Atuyuki Kojima

发明人： Kikuo Ishizumi ,  Fujio Antoku ,  Isamu Maruyama ,  Atuyuki Kojima

IPC分类号： C07D209/48 ,  A61K31/425 ,  A61K31/428 ,  A61K31/435 ,  A61K31/495 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  C07D209/76 ,  C07D275/06 ,  C07D405/06 ,  C07D417/12 ,  C07D491/18 ,  C07D417/14

CPC分类号： C07D275/06 ,  C07D417/12

摘要： A compound of the formula: ##STR1## wherein A is a carbonyl group or a sulfonyl group;B is either one of the formulas: ##STR2## (in which E is a methylene group, an ethylene group or an oxygen atom and a full line accompanying a broken line ( ) indicates a single bond or a double bond), ##STR3## (in which F is a methylene group or an ethylene group and a full line accompanying a broken line ( ) is as defined above) and ##STR4## (in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each a hydrogen atom or a methyl group) when A represents a carbonyl group, or B is a 1,2-phenylene group when A represents a sulfonyl group;D is an ethylene group, an ethenylene group or an ethynylene group, of which one or more may be optionally substituted with hydroxyl; andn is an integer of 0, 1 or 2, or its acid addition salt. These compounds are useful for the treatment or psychosis.

摘要翻译： 下式的化合物：其中A是羰基或磺酰基; B是下列公式之一：（其中E是亚甲基，亚乙基或氧原子，伴随虚线的全部线表示单键或双键）， （其中F是亚甲基或亚乙基，虚线（）的全部线如上所定义）和（其中R 1，R 2，R 3，R 4，R 5和R 6各自为氢原子 或甲基），当A表示羰基时，或B表示1,2-亚苯基，当A表示磺酰基时; D是亚乙基，亚乙烯基或亚乙炔基，其中一个或多个可以任选被羟基取代; n为0,1或2的整数，或其酸加成盐。 这些化合物可用于治疗或精神病。

公开(公告)号：US4562263A

公开(公告)日：1985-12-31

申请号：US614246

申请日：1984-05-25

申请人： Naohito Ohashi ,  Shoji Nagata ,  Kikuo Ishizumi

发明人： Naohito Ohashi ,  Shoji Nagata ,  Kikuo Ishizumi

IPC分类号： C07D209/48 ,  C07D317/60 ,  C07D405/12 ,  C07C99/12

CPC分类号： C07D209/48 ,  C07D317/60 ,  C07D405/12

摘要： A process for producing racemic or optically active threo- or erythro-3-(3,4-dihydroxyphenyl)serine which comprises phthaloylating the amine group of a racemic or optically active threo- or erythro-3-(3,4-dihydroxyphenyl)serine derivative to yield a racemic or optically active threo- or erythro-N-phthaloyl-3-(3,4-dihydroxyphenyl)serine derivative and removing the phthaloyl group from the racemic or optically active threo- or erythro-N-phthaloyl-3-(3,4-dihydroxyphenyl)-serine to yield the racemic or optically active threo- or erythro-3-(3,4-dihydroxyphenyl)serine.

摘要翻译： 制备外消旋或光学活性的苏氨酸或赤式3-（3,4-二羟基苯基）丝氨酸的方法，其包括将外消旋或光学活性的苏氨酸或赤式3-（3,4-二羟基苯基）丝氨酸的胺基苯甲酰化 衍生物，得到外消旋或光学活性的苏氨酸或赤式-N-邻苯二甲酰基-3-（3,4-二羟基苯基）丝氨酸衍生物，并从外消旋或光学活性的苏氨酸或赤式-N-邻苯二甲酰基-3- （3,4-二羟基苯基） - 丝氨酸，得到外消旋或光学活性的苏氨酸或赤式3-（3,4-二羟基苯基）丝氨酸。

公开(公告)号：US4480109A

公开(公告)日：1984-10-30

申请号：US455254

申请日：1983-01-03

申请人： Naohito Ohashi ,  Shoji Nagata ,  Kikuo Ishizumi

发明人： Naohito Ohashi ,  Shoji Nagata ,  Kikuo Ishizumi

IPC分类号： C07D317/60 ,  C07C19/00 ,  C07D317/54 ,  C07D317/58

CPC分类号： C07D317/60

摘要： A process for producing an optically active threo-3-(3,4-dihydroxyphenyl)serine represented by the formula ##STR1## which is useful as a remedy for peripheral orthostatic hypotension or as an antidepressant, which process comprises treating threo-3-(3,4-methylenedioxyphenyl)serine or an N-carbobenzoxy derivative thereof represented by the formula ##STR2## wherein A represents a hydrogen atom or a carbobenzoxy group, with a Lewis acid to form threo-3-(3,4-dihydroxyphenyl)serine or an N-carbobenzoxy derivative thereof represented by the formula ##STR3## wherein A is as defined above, and, if A is a carbobenzoxy group, catalytically reducing the resulting compound of formula [2]; a racemic or optically active threo-N-carbobenzoxy-3-(3,4-methylenedioxyphenyl)serine represented by the formula ##STR4## which is a novel compound useful as an intermediate in the above synthesis; and a process for producing said novel compound.

摘要翻译： 用于制备由式 [1]表示的光学活性的苏氨酰-3-（3,4-二羟基苯基）丝氨酸的方法，其可用作周围直立性低血压的补救剂或作为抗抑郁药，该方法包括将苏氨酸 - 由式[IMAGE] [3]表示的3-（3,4-亚甲二氧基苯基）丝氨酸或N-苄氧羰基衍生物，其中A表示氢原子或苯甲酰氧基，与路易斯酸形成苏-3-（3 ，4-二羟基苯基）丝氨酸或其通式为“IMAGE”[2]所示的N-苄氧羰基衍生物，其中A如上所定义，如果A为苄氧羰基，则催化还原所得的式[2]化合物。 由上式合成中可用作中间体的新化合物，由式[IMAGE] [3“表示的外消旋或光学活性的苏氨酰-N-苄氧羰基-3-（3,4-亚甲二氧基苯基）丝氨酸; 以及制备所述新型化合物的方法。

公开(公告)号：US4545936A

公开(公告)日：1985-10-08

申请号：US607268

申请日：1984-05-04

申请人： Kikuo Ishizumi ,  Michihisa Muramatsu ,  Hiromi Sato ,  Norihiko Tanno ,  Noboru Yoshida

发明人： Kikuo Ishizumi ,  Michihisa Muramatsu ,  Hiromi Sato ,  Norihiko Tanno ,  Noboru Yoshida

IPC分类号： A61K31/135 ,  A61K31/22 ,  A61P35/00 ,  C07C225/32 ,  C07C15/24 ,  C07C50/22 ,  C07C50/36

CPC分类号： A61K31/135

摘要： An aminonaphthacene derivative of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a hydroxyl group or a lower alkoxy group, R.sup.2 is a hydrogen atom or a hydroxyl group, R.sup.3 is a hydrogen atom or a lower alkanoyl group and R.sup.4 and R.sup.5 are, same or different, each a hydrogen atom, a lower alkyl group, a lower hydroxyalkyl group or a group of the formula: ##STR2## wherein A is an alkylene group which may have one or more lower alkyl substituent(s) and R.sup.6 and R.sup.7 are, same or different, each a hydrogen atom, a lower alkyl group, a lower hydroxyalkyl group or a lower aminoalkyl group, and an acid addition salt thereof, which is useful as anti-tumor agent.

摘要翻译： 下式的氨基并萘系衍生物：其中R1是氢原子，羟基或低级烷氧基，R2是氢原子或羟基，R3是氢原子或低级烷酰基， R 4和R 5各自相同或不同，为氢原子，低级烷基，低级羟基烷基或下式基团：其中A为可具有一个或多个低级烷基的亚烷基 取代基和R6和R7各自为氢原子，低级烷基，低级羟烷基或低级氨基烷基，及其酸加成盐，可用作抗肿瘤剂。

公开(公告)号：US4544635A

公开(公告)日：1985-10-01

申请号：US579602

申请日：1984-02-13

申请人： Naohito Ohashi ,  Kozo Shimago ,  Takaharu Ikeda ,  Kikuo Ishizumi

发明人： Naohito Ohashi ,  Kozo Shimago ,  Takaharu Ikeda ,  Kikuo Ishizumi

IPC分类号： C07D233/32 ,  C07D491/04 ,  C07D491/048 ,  C12N9/18 ,  C12P17/10

CPC分类号： C07D491/04 ,  C07D233/32 ,  C12N9/18 ,  C12P17/10

摘要： A process for preparing an optically active cis-1,3-dibenzylhexahydro-1H-furo[3,4-d]imidazole-2,4-dione of the formula: ##STR1## wherein an asterisk (*) indicates an asymmetric carbon, Bzl represents a benzyl group and the 3a- and 6a-positions take the cis-configuration, which comprises reducing selectively an optically active cis-imidazolidinedicarboxylic acid monoester of the formula: ##STR2## wherein R is a C.sub.1 -C.sub.6 alkyl group and Bzl is as defined above with a reducing agent at either one of the carboxyl group and the alkoxycarbonyl group in the said monoester, followed by cyclization.