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    Remedy for integration dysfunction syndrome
    1.
    发明申请
    Remedy for integration dysfunction syndrome 有权
    整合功能障碍综合征的补救措施

    公开(公告)号：US20060025422A1

    公开(公告)日：2006-02-02

    申请号：US10525021

    申请日：2003-08-20

    申请人： Mitsutaka Nakamura ,  Masaaki Ogasa ,  Shunsuke Sami

    发明人： Mitsutaka Nakamura ,  Masaaki Ogasa ,  Shunsuke Sami

    IPC分类号： A61K31/496

    CPC分类号： C07D417/12 ,  A61K31/496

    摘要： The present invention provides a novel method for treatment of schizophrenia which can improve wide-ranging symptoms of schizophrenia, especially positive symptoms and negative symptoms without being accompanied by extrapyramidal symptoms, which comprises orally administering as an active compound (1R,2S,3R,4S)—N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboxyimide or a pharmaceutically acceptable salt thereof (e.g., hydrochloride) at a daily dose of 5 mg to 120 mg once a day to a patient with schizophrenia, and a therapeutic agent to be used in said method.

    摘要翻译： 本发明提供一种治疗精神分裂症的新方法，其可以改善精神分裂症的广泛症状，特别是阳性症状和阴性症状，而不伴有锥体束外症状，其包括口服给药作为活性化合物（1R，2S，3R，4S ）-N - [（1R，2R）-2- [4-（1,2-苯并异噻唑-3-基）-1-哌嗪基甲基] -1-环己基甲基] -2,3-二环[2.2.1]庚烷二酰亚胺或 其药学上可接受的盐（例如，盐酸盐），每日一次给予精神分裂症患者5mg至120mg，以及用于所述方法的治疗剂。

    Bicyclooctane derivatives
    2.
    发明授权
    Bicyclooctane derivatives 失效
    双环辛烷衍生物

    公开(公告)号：US4493846A

    公开(公告)日：1985-01-15

    申请号：US243570

    申请日：1981-03-13

    申请人： Keiichi Ono ,  Akihiko Sugie ,  Hajime Kawakami ,  Shunsuke Sami ,  Atsuyuki Kojima ,  Junki Katsube

    发明人： Keiichi Ono ,  Akihiko Sugie ,  Hajime Kawakami ,  Shunsuke Sami ,  Atsuyuki Kojima ,  Junki Katsube

    IPC分类号： C07C69/708 ,  A61K31/557 ,  C07C29/09 ,  C07C29/128 ,  C07C35/32 ,  C07C43/196 ,  C07C47/198 ,  C07C47/277 ,  C07C51/00 ,  C07C51/08 ,  C07C59/125 ,  C07C59/13 ,  C07C59/31 ,  C07C59/46 ,  C07C59/62 ,  C07C67/00 ,  C07C67/08 ,  C07C69/734 ,  C07C405/00 ,  C07D211/32 ,  C07D295/08 ,  C07D295/18 ,  C07C69/608 ,  C07C61/13 ,  C07C61/28 ,  C07C69/616

    CPC分类号： C07C255/00 ,  C07C29/095 ,  C07C29/1285 ,  C07C35/32 ,  C07C405/0083 ,  C07C43/196 ,  C07D211/32 ,  C07B2200/07 ,  C07B2200/09 ,  C07C2102/24 ,  Y10S514/925

    摘要： A compound of the formula ##STR1## wherein X.sup.1 is a free or esterified carboxyl group, a hydroxymethyl group, a cyano group, a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7-membered saturated heterocyclic group) or a group of the formula: ##STR3## (R.sup.a and R.sup.b are each as defined above), Y is an ethylene group or a vinylene group, R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sub.1 and R.sub.2, when taken together, means a single linkage to form a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, R.sup.5 is a hydrogen atom, a C.sub.3 -C.sub.8 alkenyl group, a C.sub.3 -C.sub.8 alkynyl group, a C.sub.1 -C.sub.8 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group or a group of the formula: --(CH.sub.2).sub.n --B (n is 1 or 2 and B is a C.sub.1 -C.sub.4 alkoxyl group, a C.sub.3 -C.sub.7 cycloalkyl group, or a phenyl or phenoxy group optionally substituted with a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a trifluoromethyl group or a C.sub.1 -C.sub.4 alkoxyl group), A is a group of either one of the formulae: ##STR4## (R.sup.6 and R.sup.7 are each independently a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and ##STR5## m.sub.1 is 1 or 2 and m.sub.2 is 0, 1 or 2, and the non-toxic pharmaceutically acceptable salts threreof. Said compounds have strong anti-ulcerogenic activity and are useful in treatment of gastraintestinal ulcer.

    摘要翻译： 下式的化合物其中X1是游离或酯化的羧基，羟甲基，氰基，下式的基团：（R a和R b各自独立地是氢原子，C 1 -C 4 烷基，C3-C7环烷基，苄基，苯基，被卤素原子或C1-C4烷基取代的苯基，或者当与它们所连接的相邻氮原子一起时， 它们表示5至7元饱和杂环基）或下式的基团：（R a和R b各自如上所定义），Y是亚乙基或亚乙烯基，R 1是氢原子， 羟基或受保护的羟基，R2是氢原子或R1和R2，当它们一起表示在它们连接的碳原子之间形成双键的单键，R3是羟基或被保护的羟基 R4是氢原子或C1-C4烷基，R5是氢原子，C3-C8链烯基，C3-C8烷基 正丁基，C 1 -C 8烷基，C 3 -C 7环烷基或下式基团： - （CH 2）n B（n为1或2，B为C 1 -C 4烷氧基，C 3 -C 7环烷基 或任选被卤素原子取代的苯基或苯氧基，C 1 -C 4烷基，三氟甲基或C 1 -C 4烷氧基），A是以下基团之一： R 7各自独立地为氢原子或C 1 -C 4烷基），并且M 1为1或2，m 2为0,1或2，以及无毒的药学上可接受的盐。 所述化合物具有强的抗溃疡活性，可用于治疗胃肠溃疡。

    Remedy for integration dysfunction syndrome
    3.
    发明授权
    Remedy for integration dysfunction syndrome 有权
    整合功能障碍综合征的补救措施

    公开(公告)号：US09174975B2

    公开(公告)日：2015-11-03

    申请号：US10525021

    申请日：2003-08-20

    申请人： Mitsutaka Nakamura ,  Masaaki Ogasa ,  Shunsuke Sami

    发明人： Mitsutaka Nakamura ,  Masaaki Ogasa ,  Shunsuke Sami

    IPC分类号： A61K9/00 ,  C07D417/12 ,  A61K31/496

    CPC分类号： C07D417/12 ,  A61K31/496

    摘要： The present invention provides a novel method for treatment of schizophrenia which can improve wide-ranging symptoms of schizophrenia, especially positive symptoms and negative symptoms without being accompanied by extrapyramidal symptoms, which comprises orally administering as an active compound (1R,2S,3R,4S)—N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboxyimide or a pharmaceutically acceptable salt thereof (e.g., hydrochloride) at a daily dose of 5 mg to 120 mg once a day to a patient with schizophrenia, and a therapeutic agent to be used in the method.

    摘要翻译： 本发明提供一种治疗精神分裂症的新方法，其可以改善精神分裂症的广泛症状，特别是阳性症状和阴性症状，而不伴有锥体束外症状，其包括口服给药作为活性化合物（1R，2S，3R，4S ）-N - [（1R，2R）-2- [4-（1,2-苯并异噻唑-3-基）-1-哌嗪基甲基] -1-环己基甲基] -2,3-二环[2.2.1]庚烷二酰亚胺或 其药学上可接受的盐（例如，盐酸盐），每日一次给予精神分裂症患者5mg至120mg，以及用于该方法的治疗剂。