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1. 发明授权

US4103030A Novel cyclopropylmethylamine derivatives 失效
标题翻译：新型环丙基甲胺衍生物
公开(公告)号：US4103030A
公开(公告)日：1978-07-25
申请号：US635331
申请日：1975-11-26
申请人： Atsuyuki Kojima , Yoshito Kameno , Junki Katsube , Shigeho Inaba , Hisao Yamamoto
发明人： Atsuyuki Kojima , Yoshito Kameno , Junki Katsube , Shigeho Inaba , Hisao Yamamoto
IPC分类号： A61K31/13 , A61K31/135 , A01N9/20 , A01N9/24 , C07C91/16 , C07C91/28
摘要： Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein Ar.sup.1 represents a phenyl group having one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and trifluoromethyl, of which at least one is present at the o- or m-position, Ar.sup.2 represents an unsubstituted phenyl group or a phenyl group substituted with one or more substituents selected from the group consisting of halogen and C.sub.1 -C.sub.4 alkyl, R represents hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl and R' represents C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reduction of the corresponding compounds of the formula: ##STR2## wherein Ar.sup.1, Ar.sup.2, R and R' are each as defined above or by condensation of the corresponding compounds of the formula: ##STR3## wherein Ar.sup.1 and Ar.sup.2 are each as defined above and X is a conventional leaving (removable) group with amines of the formula: ##STR4## wherein R and R' are each as defined above.
摘要翻译：新的下式的环丙基甲胺化合物：其中Ar 1表示具有一个或多个选自卤素，C 1 -C 4烷基，C 1 -C 4烷氧基和三氟甲基的取代基的苯基，其中至少一个存在于或位置，Ar 2表示未取代的苯基或被一个或多个选自卤素和C 1 -C 4烷基的取代基取代的苯基，R表示氢，C 1 -C 4烷基或C 2 -C 4羟烷基， R'表示C1-C4烷基或C2-C4羟基烷基及其无毒盐，它们具有各种有用的药理活性，可以通过还原相应的下式化合物来制备：其中Ar1，Ar2，R和 R'各自如上所定义，或通过下式的相应化合物的缩合：其中Ar 1和Ar 2各自如上所定义，X是具有下式的胺的常规离去（可除去）基团：其中 R和R'各自如上所定义。

2. 发明授权

US4110376A Cyclopropylmethylamine derivatives 失效
标题翻译：环丙基甲胺衍生物
公开(公告)号：US4110376A
公开(公告)日：1978-08-29
申请号：US605012
申请日：1975-08-15
申请人： Atsuyuki Kojima , Junki Katsube , Yoshito Kameno , Shigeho Inaba , Hisao Yamamoto
发明人： Atsuyuki Kojima , Junki Katsube , Yoshito Kameno , Shigeho Inaba , Hisao Yamamoto
IPC分类号： A61K31/135 , A61K31/13 , C07C20060101 , C07C67/00 , C07C209/00 , C07C209/50 , C07C211/26 , C07C87/32
CPC分类号： C07D401/12
摘要： Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or halogen and R.sup.3 is hydrogen or methyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reduction of the corresponding compounds of the formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are each as defined above or their non-toxic salts, or by condensation of the corresponding compounds of the formula: ##STR3## wherein R.sup.1 and R.sup.2 are each defined above, and X is a conventional interchangeable group such as halogen or sulfonyloxy with methylamine or dimethylamine.
摘要翻译：下式的新型环丙基甲胺化合物：其中R 1和R 2各自为氢或卤素，R 3为氢或甲基，及其无毒盐，其具有各种有用的药理活性，可通过还原相应化合物其中R 1，R 2和R 3各自如上所定义，或其无毒盐，或通过下式的相应化合物的缩合：其中R 1和R 2各自如上所定义，X为常规的可互换基团如卤素或磺酰氧基与甲胺或二甲胺。

3. 发明授权

US4085210A Novel morpholine derivatives and the treatment of mental depression 失效
标题翻译：新型吗啉衍生物和精神抑郁症的治疗
公开(公告)号：US4085210A
公开(公告)日：1978-04-18
申请号：US646908
申请日：1976-01-06
申请人： Junki Katsube , Atsuyuki Kojima , Makoto Sunagawa , Yoshinori Takashima , Yoshito Kameno , Hisao Yamamoto
发明人： Junki Katsube , Atsuyuki Kojima , Makoto Sunagawa , Yoshinori Takashima , Yoshito Kameno , Hisao Yamamoto
IPC分类号： C07D265/30 , C07D267/10 , C07D409/06 , A61K31/535 , C07D405/06
CPC分类号： C07D265/30 , C07D267/10
摘要： Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4)alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D --E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.
摘要翻译：式中：R1代表氢或C1-C4烷基，R2代表氢，C1-C4烷基，C3-C5烯基，C3-C5炔基，芳基 - （C1-C4）烷基，（C3 -C 6）环烷基（C 1 -C 4）烷基，多卤代（C 2 -C 4）烷基或羟基（C 2 -C 4）烷基，A表示直链或支链C 2 -C 4亚烷基，B表示选自-CH 2 -CH 2 - ， - CH = CH-， -CH 2 -O-，-CH 2 -S-，-S-和-O-，> D-E-代表选自下组的三价基团：CH -CH 2 - 和> C = CH-且C 1和C 2各自表示任选被一个或多个选自卤素，C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的1,2-亚苯基，它们的无毒盐，其可用作抗抑郁药并且可以通过各种方法制备。

4. 发明授权

US4418079A Conjugated ketone compounds in preventing platelet thrombosis 失效
标题翻译：共轭酮化合物预防血小板血栓形成
公开(公告)号：US4418079A
公开(公告)日：1983-11-29
申请号：US335522
申请日：1981-12-29
申请人： Atsuyuki Kojima , Tsunemasa Irie , Shuichi Harada , Yoshito Kameno , Junki Katsube , Hisao Yamamoto
发明人： Atsuyuki Kojima , Tsunemasa Irie , Shuichi Harada , Yoshito Kameno , Junki Katsube , Hisao Yamamoto
IPC分类号： C07C29/42 , C07D209/44 , C07D295/108 , C07D307/52 , C07D317/58 , C07D333/22 , A61K27/00 , A61K31/135 , A61K31/34 , A61K31/36 , A61K31/38 , A61K31/40 , A61K31/44 , A61K31/445
CPC分类号： C07D295/108 , C07C29/42 , C07D209/44 , C07D307/52 , C07D317/58 , C07D333/22
摘要： Conjugated ketone compounds of the formula: ##STR1## wherein Ar is naphthyl, furyl, thienyl, or phenyl optionally bearing one or more substituents selected from the group consisting of chlorine, bromine, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, trifluoromethyl and methylenedioxy, R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.7 -C.sub.8 aralkyl or adamantyl, R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.5 alkenyl or C.sub.3 -C.sub.6 cycloalkyl, or when R.sub.1 and R.sub.2 are taken together with the nitrogen atom to which they are attached, they form a heterocyclic amino group containing up to 8 carbon atoms, A is straight or branched C.sub.1 -C.sub.3 alkylene, N-[4-(p-chlorophenyl)-4-oxo-2-trans-butenyl]morpholine and N-[4-(p-methoxyphenyl)-4-oxo-2-trans-butenyl]piperidine being excluded, and their non-toxic salts, which are useful as blood platelet anti-aggregative agents.
摘要翻译：具有下式的共轭酮化合物：其中Ar是萘基，呋喃基，噻吩基或任选具有一个或多个选自氯，溴，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4 烷基硫基，三氟甲基和亚甲二氧基，R 1是C 1 -C 6烷基，C 3 -C 5烯基，C 3 -C 6环烷基，C 7 -C 8芳烷基或金刚烷基，R 2是C 1 -C 6烷基，C 3 -C 5链烯基或C 3 -C 6环烷基，并且R 2与它们所连接的氮原子一起形成含有至多8个碳原子的杂环氨基，A是直链或支链C1-C3亚烷基，N- [4-（对氯苯基）-4 - 氧代-2-反式 - 丁烯基]吗啉和N- [4-（对甲氧基苯基）-4-氧代-2-反式 - 丁烯基]哌啶，以及它们的无毒盐，其可用作血小板抗体聚集代理。

5. 发明授权

US4169146A Novel morpholine derivatives and treating depression therewith 失效
标题翻译：新型吗啉衍生物和治疗抑郁症
公开(公告)号：US4169146A
公开(公告)日：1979-09-25
申请号：US811944
申请日：1977-06-30
申请人： Junki Katsube , Atsuyuki Kojima , Makoto Sunagawa , Yoshinori Takashima , Yoshito Kameno , Hisao Yamamoto
发明人： Junki Katsube , Atsuyuki Kojima , Makoto Sunagawa , Yoshinori Takashima , Yoshito Kameno , Hisao Yamamoto
IPC分类号： C07D265/30 , C07D267/10 , A61K27/00
CPC分类号： C07D265/30 , C07D267/10
摘要： Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4) alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D--E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.
摘要翻译：式中：R1代表氢或C1-C4烷基，R2代表氢，C1-C4烷基，C3-C5烯基，C3-C5炔基，芳基 - （C1-C4）烷基，（C3 -C 6）环烷基（C 1 -C 4）烷基，多卤代（C 2 -C 4）烷基或羟基（C 2 -C 4）烷基，A表示直链或支链C 2 -C 4亚烷基，B表示选自-CH 2 -CH 2 - ， - CH = CH-， -CH 2 -O-，-CH 2 -S-，-S-和-O-，> DE-表示选自下组的三价基团：CH-CH 2 - 和> C = CH-和C1和C2各自表示任选被一个或多个选自卤素，C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的1,2-亚苯基及其无毒盐，其可用作抗抑郁药并且可以通过各种方法制备。

6. 发明授权

US4348386A Protease inhibitors 失效
标题翻译：蛋白酶抑制剂
公开(公告)号：US4348386A
公开(公告)日：1982-09-07
申请号：US249984
申请日：1981-04-01
申请人： Shinichi Kojima , Ten Koide , Shigeo Ogino , Toshiro Tsuchiya , Yoshito Kameno
发明人： Shinichi Kojima , Ten Koide , Shigeo Ogino , Toshiro Tsuchiya , Yoshito Kameno
IPC分类号： C07K7/02 , A61K33/06 , A61K35/74 , A61K38/55 , A61P1/04 , C07K5/02 , C07K14/81 , A61K37/00 , C07C103/52
CPC分类号： C07K5/0205
摘要： An acidic protease inhibitor obtained by allowing a compound of ##STR1## wherein X and Y are L-leucine or L-valine, or its salt, to react with an aluminum compound in a medium containing water and/or an alcohol, and further continuing the reaction after adjusting the pH of the system within a range of 4.5 to 7. The protease can stay long in stomach, have an action to protect ulcerated areas and retain the antiulcer effect for a long period of time.
摘要翻译：通过使其中X和Y是L-亮氨酸或L-缬氨酸或其盐的化合物与含有水和/或其盐的介质中的铝化合物反应获得的酸性蛋白酶抑制剂酒精，并且在4.5至7的范围内将系统的pH调节后进一步继续反应。蛋白酶可以在胃中保持长时间，具有保护溃疡区域并长时间保持抗溃疡作用的作用。

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