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1. 发明授权

US4734500A O-aminoalkylene (or aminoalkyleneoxy) phenylsulfone compounds having anti-ulcer effect 失效
标题翻译：具有抗溃疡作用的O-氨基亚烷基（或氨基亚烷氧基）苯基砜化合物
公开(公告)号：US4734500A
公开(公告)日：1988-03-29
申请号：US838569
申请日：1986-03-11
申请人： Akihiro Tobe , Shinichiro Fujimori , Tomoshi Yamazaki , Mamoru Sugano , Ryoji Kikumoto , Issei Nitta
发明人： Akihiro Tobe , Shinichiro Fujimori , Tomoshi Yamazaki , Mamoru Sugano , Ryoji Kikumoto , Issei Nitta
IPC分类号： A61K31/135 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/275 , A61K31/495 , A61P1/04 , C07C47/11 , C07C67/00 , C07C313/00 , C07C317/22 , C07C317/32 , C07C317/44 , C07C317/46 , C07C317/48 , C07D295/08 , C07D295/092 , C07D295/096 , C07D333/76 , C07D333/50
CPC分类号： C07D295/096 , C07D295/088 , C07D333/76
摘要： A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylene; Y is --(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.3 hydroxyalkyl or phenyl; or a pharmaceutically acceptable salt thereof is disclosed. The compound has anti-ulcer effect.
摘要翻译：由通式（I）表示的新型砜化合物其中R 1是环己基，苯基; 或被选自硝基，C 1 -C 3烷基，C 1 -C 3烷氧基和卤素的基团取代的苯基; R2，R3，R4和R5分别是氢，卤素，氰基或羰基，其中R1和R2可以形成被至少一个选自硝基C1-C3烷基，C1-C3烷氧基的基团取代的邻亚苯基或邻亚苯基和卤素; X是氧或亚甲基; Y是 - （CH 2）n - ，其中n是0或5或6的整数，或者其中m是整数1-3; R6是氢，C1-C3烷基，ω-烷基氨基烷基，其中每个烷基具有1-3个碳原子，或ω-二烷基氨基烷基，其中每个烷基具有1-3个碳原子; R7是氢或C1-C3烷基; 并且R 6和R 7可以与N或其中R 8是氢，C 1 -C 3羟基烷基或苯基形成环; 或其药学上可接受的盐。该化合物具有抗溃疡作用。

2. 发明授权

US4814507A Arylsulfone compounds as anti-ulcer agents 失效
标题翻译：芳砜化合物作为抗溃疡剂
公开(公告)号：US4814507A
公开(公告)日：1989-03-21
申请号：US95766
申请日：1987-09-14
申请人： Akihiro Tobe , Shinichiro Fujimori , Tomoshi Yamazaki , Mamoru Sugano , Ryoji Kikumoto , Issei Nitta
发明人： Akihiro Tobe , Shinichiro Fujimori , Tomoshi Yamazaki , Mamoru Sugano , Ryoji Kikumoto , Issei Nitta
IPC分类号： A61K31/135 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/275 , A61K31/495 , A61P1/04 , C07C47/11 , C07C67/00 , C07C313/00 , C07C317/22 , C07C317/32 , C07C317/44 , C07C317/46 , C07C317/48 , C07D295/08 , C07D295/092 , C07D295/096 , C07D333/76 , C07C87/28 , C07C147/00
CPC分类号： C07D295/096 , C07D295/088 , C07D333/76
摘要： A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylkene; Y is -(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.3 hydroxyalkyl or phenyl; or a pharmaceutically acceptable salt thereof is disclosed. The compound has anti-ulcer effect.

3. 发明授权

US4695568A Thieno[2,3-d]pyrimidine derivatives and salts thereof 失效
标题翻译：噻吩并[2,3-d]嘧啶衍生物及其盐
公开(公告)号：US4695568A
公开(公告)日：1987-09-22
申请号：US685768
申请日：1984-12-24
申请人： Kunihiro Ninomiya , Issei Nitta , Akihiro Tobe , Mitsuo Egawa , Ryoji Kikumoto
发明人： Kunihiro Ninomiya , Issei Nitta , Akihiro Tobe , Mitsuo Egawa , Ryoji Kikumoto
IPC分类号： A61K31/505 , A61K31/55 , A61P25/24 , A61P25/26 , A61P25/28 , C07D495/04 , A61K31/38 , C07D239/00
CPC分类号： C07D495/04
摘要： This invention relates novel thieno[2,3-d]pyrimidine derivatives represented by the following general formula (I): ##STR1## or salts thereof; wherein R.sup.1 and R.sup.2 independently represent hydrogen, halogen or alkyl group having 1 to 6 carbon atoms; or R.sup.1 and R.sup.2 may concatenate to form a cycloalkylene group having 5 or 6 ring carbon atoms; R.sup.3 and R.sup.4 independently represent hydrogen or alkyl group having 1 to 6 carbon atoms; R.sup.5 represents a member selected from(1) hydrogen or alkyl having 1 to 6 carbon atoms,(2) ##STR2## in which m is an integer of from 1 to 3 and X represents halogen, or (3) ##STR3## in which R.sup.6 represents alkyl group having 1 to 6 carbon atoms; Ar represents substituted or unsubstituted phenyl, or 2- or 3-thienyl group; and n is 2 or 3. The derivatives of the invention can be used in the treatment of the various depression disease or the higher dysfunction of the brain.
摘要翻译：本发明涉及由以下通式（I）表示的新颖的噻吩并[2,3-d]嘧啶衍生物或其盐; 其中R 1和R 2独立地表示氢，卤素或具有1至6个碳原子的烷基; 或者R1和R2可以连接形成具有5或6个环碳原子的亚环烷基; R3和R4独立地表示氢或具有1-6个碳原子的烷基; R5表示选自（1）氢或具有1至6个碳原子的烷基的成员，（2）其中m是1至3的整数，X表示卤素，或（3）其中 R6代表具有1-6个碳原子的烷基; Ar表示取代或未取代的苯基，或2-或3-噻吩基; 并且n为2或3.本发明的衍生物可用于治疗各种抑郁症或较高的脑功能障碍。

4. 发明授权

US4716161A Phenylpiperazine derivatives and their acid addition salts 失效
标题翻译：苯基哌嗪衍生物及其酸加成盐
公开(公告)号：US4716161A
公开(公告)日：1987-12-29
申请号：US719456
申请日：1985-04-03
申请人： Harukazu Fukami , Ryoji Kikumoto , Kenichiro Nakao , Issei Nitta , Shinya Inoue
发明人： Harukazu Fukami , Ryoji Kikumoto , Kenichiro Nakao , Issei Nitta , Shinya Inoue
IPC分类号： C07D239/96 , C07D285/32 , C07D491/04 , C07D491/056 , C07D513/04 , A61K31/54 , C07D417/06
CPC分类号： C07D491/04 , C07D239/96 , C07D285/32 , C07D513/04
摘要： A phenylpiperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or alkoxy group having 1 to 3 carbon atoms, orR.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 together with carbon atoms to which they are attached form --O(CH.sub.2).sub.m O-- wherein m is an integer of 1 to 3, oreither R.sup.1 or R.sup.2 is amine residue selected from the group consisting of --NH.sub.2 , --NHSO.sub.2 CH.sub.3, --NHCOCH.sub.3 and --NHCONH.sub.2 and the other is hydrogen or alkoxy group of 1 to 3 carbon atoms and R.sup.3 is hydrogen;R.sup.4 and R.sup.5 are independently hydrogen or alkyl group of 1 to 3 carbon atoms;Y is --CO-- or --SO.sub.2 -- provided that at least one of R.sup.1 and R.sup.2 is not hydrogen when Y is --CO--; andn is an integer of 2 to 4.An acid addition salt of the phenylpiperazine derivative having the general formula [I] is included in the present invention. The phenylpiperazine derivative as well as its acid addition salt according to the present invention have the ability to reduce the blood pressure.
摘要翻译：根据本发明的苯基哌嗪衍生物具有以下通式[I]：其中R 1，R 2和R 3独立地是氢或具有1至3个碳原子的烷氧基，或者R 1和R 2或R 2和R 3 与其连接的碳原子一起形成-O（CH 2）m O-，其中m是1至3的整数，或者R 1或R 2是选自-NH 2，-NHSO 2 CH 3，-NHCOCH 3和 -NHCONH 2，另一个是1或3个碳原子的氢或烷氧基，R 3是氢; R4和R5独立地是氢或1〜3个碳原子的烷基; Y是-CO-或-SO 2 - ，条件是当Y是-CO-时，R 1和R 2中的至少一个不是氢; n为2〜4的整数。本发明包括具有通式[I]的苯基哌嗪衍生物的酸加成盐。根据本发明的苯基哌嗪衍生物及其酸加成盐具有降低血压的能力。

5. 发明授权

US4613598A Piperazine derivatives and their acid addition salts 失效
标题翻译：哌嗪衍生物及其酸加成盐
公开(公告)号：US4613598A
公开(公告)日：1986-09-23
申请号：US708641
申请日：1985-03-06
申请人： Harukazu Fukami , Shinya Inoue , Issei Nitta , Kenichiro Nakao , Ryoji Kikumoto
发明人： Harukazu Fukami , Shinya Inoue , Issei Nitta , Kenichiro Nakao , Ryoji Kikumoto
IPC分类号： C07D213/74 , C07D265/36 , C07D267/14 , C07D279/16 , C07D295/084 , C07D295/108 , C07D417/12 , A61K31/55 , C07D417/10
CPC分类号： C07D295/108 , C07D213/74 , C07D265/36 , C07D267/14 , C07D279/16 , C07D295/092 , C07D417/12
摘要： A piperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1 is --OH, --OR.sup.3, --SR.sup.3, --SOR.sup.3 or --SO.sub.2 R.sup.3 wherein R.sup.3 is alkyl group having 1 to 3 carbon atoms;R.sup.2 is --SO.sub.2 NH.sub.2, --SO.sub.2 NHR.sup.4, --SO.sub.2 NR.sup.4 R.sup.5, --COOH, --COOR.sup.4, --CONH.sub.2, --CONHR.sup.4, --CONR.sup.4 R.sup.5, --NHCONH.sub.2, --NHCSNH.sub.2, --NHCONHR.sup.4, --NHCOR.sup.4 or --NHSO.sub.2 R.sup.4 wherein R.sup.4 and R.sup.5 are independently alkyl group having 1 to 3 carbon atoms; orR.sup.1 and R.sup.2 together with carbon atoms to which they are attached form ##STR2## Z is --CO-- or --CH(OH)--; Ar is pyridyl or substituted or unsubstituted phenyl; andn is an integer of 3 to 5.An acid addition salt of the piperazine derivative having the above formula [I] is included in the present invention. The piperazine derivative as well as its acid addition salt according to the present invention have the ability to reduce the blood pressure.
摘要翻译：根据本发明的哌嗪衍生物具有以下通式[I]：其中R 1是-OH，-OR 3，-SR 3，-SOR 3或-SO 2 R 3，其中R 3是具有1至3个碳原子的烷基原子 R2是-SO2NH2，-SO2NHR4，-SO2NR4R5，-COOH，-COOR4，-CONH2，-CONHR4，-CONR4R5，-NHCONH2，-NHCSNH2，-NHCONHR4，-NHCOR4或-NHSO2R4，其中R4和R5独立地为具有1 至3个碳原子; 或R 1和R 2与它们所连接的碳原子一起形成Z是-CO-或-CH（OH） - ; Ar为吡啶基或取代或未取代的苯基; n为3〜5的整数。上述式[I]的哌嗪衍生物的酸加成盐包括在本发明中。根据本发明的哌嗪衍生物及其酸加成盐具有降低血压的能力。

6. 发明授权

US4684739A Alkylenedioxybenzene derivatives and acid addition salts thereof 失效
标题翻译：亚烷基二氧基苯衍生物及其酸加成盐
公开(公告)号：US4684739A
公开(公告)日：1987-08-04
申请号：US326417
申请日：1981-12-01
申请人： Ryoji Kikumoto , Harukazu Fukami , Kenichiro Nakao , Mamoru Sugano
发明人： Ryoji Kikumoto , Harukazu Fukami , Kenichiro Nakao , Mamoru Sugano
IPC分类号： C07D317/64 , C07D319/20 , C07D407/12 , C07D321/10
CPC分类号： C07D407/12 , C07D317/64 , C07D319/20
摘要： Alkylenedioxybenzene derivatives are prepared and found to be useful as pharmaceutical agents, particularly as hypotensives.
摘要翻译：制备了亚烷基二氧基苯衍生物，发现其可用作药剂，特别是作为低渗剂。

7. 发明授权

US4562211A Pharmaceutically active 2-substituted-1-(omega-aminoalkoxy)benzenes 失效
标题翻译：药用活性2-取代-1-（ω-氨基烷氧基）苯
公开(公告)号：US4562211A
公开(公告)日：1985-12-31
申请号：US94762
申请日：1979-11-16
申请人： Ryoji Kikumoto , Akihiro Tobe , Shinji Tonomura , Hidenobu Ikoma
发明人： Ryoji Kikumoto , Akihiro Tobe , Shinji Tonomura , Hidenobu Ikoma
IPC分类号： C07D295/092 , A61K31/135 , A61K31/205
CPC分类号： C07D295/088
摘要： 2-Substituted-1-(omega-aminoalkoxy)benzenes are prepared and found useful as pharmaceutical agents, particularly as antidepressants.
摘要翻译： 2-取代的1-（ω-氨基烷氧基）苯被制备并发现可用作药剂，特别是作为抗抑郁剂。

8. 发明授权

US4217366A Pharmaceutically active 2-(4-aminobutoxy)stilbenes 失效
标题翻译：药用活性2-（4-氨基丁氧基）二苯乙烯
公开(公告)号：US4217366A
公开(公告)日：1980-08-12
申请号：US11998
申请日：1979-02-14
申请人： Ryoji Kikumoto , Akihiro Tobe , Harukazu Fukami , Kunihiro Ninomiya , Mitsuo Egawa
发明人： Ryoji Kikumoto , Akihiro Tobe , Harukazu Fukami , Kunihiro Ninomiya , Mitsuo Egawa
IPC分类号： A61K31/13 , A61K31/135 , A61K31/395 , A61K31/40 , A61K31/41 , A61K31/445 , A61K31/495 , A61K31/55 , A61P25/08 , C07C67/00 , C07C213/00 , C07C217/18 , C07D211/06 , C07D211/14 , C07D211/42 , C07D211/46 , C07D223/04 , C07D227/04 , C07D241/04 , C07D295/092 , C07C93/06
CPC分类号： C07D295/088
摘要： 2-(4-aminobutoxy)stilbenes are prepared and found useful as pharmaceutical agents, particularly as anticonvulsants and skeletal muscle relaxants.
摘要翻译：制备2-（4-氨基丁氧基）二苯乙烯，发现可用作药剂，特别是抗惊厥药和骨骼肌松弛剂。

9. 发明授权

US4060641A Pharmaceutically active 2-(3-alkylaminopropoxy)diphenylmethanes 失效
标题翻译：药用活性2-（3-烷基氨基丙氧基）二苯基甲烷
公开(公告)号：US4060641A
公开(公告)日：1977-11-29
申请号：US734521
申请日：1976-10-21
申请人： Ryoji Kikumoto , Akihiro Tobe , Shinji Tonomura , Hidenobu Ikoma
发明人： Ryoji Kikumoto , Akihiro Tobe , Shinji Tonomura , Hidenobu Ikoma
IPC分类号： C07D295/092 , A01N9/20 , A01N9/24 , C07C93/06
CPC分类号： C07D295/088
摘要： 2-(3-Alkylaminopropoxy) diphenylmethanes have been produced and have been found to possess antidepressant activity.
摘要翻译：已经制备了2-（3-烷基氨基丙氧基）二苯基甲烷并已被发现具有抗抑郁活性。

10. 发明授权

US4060612A Pharmaceutically active 2-omega-aminoalkoxydiphenyl sulfides 失效
标题翻译：药用活性2-ω-氨基二氧代二苯硫醚
公开(公告)号：US4060612A
公开(公告)日：1977-11-29
申请号：US704493
申请日：1976-07-12
申请人： Ryoji Kikumoto , Akihiro Tobe , Shinji Tonomura , Hidenobu Ikoma
发明人： Ryoji Kikumoto , Akihiro Tobe , Shinji Tonomura , Hidenobu Ikoma
IPC分类号： C07D295/092 , A01N9/22 , A01N9/24 , C07C93/06
CPC分类号： C07D295/088
摘要： 2-Omega-aminoalkoxydiphenyl sulfides are prepared and found useful as pharmaceutical agents, particularly as antidepressants.
摘要翻译：制备2-ω-氨基烷氧基二苯基硫化物，可用作药剂，特别是作为抗抑郁剂。

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