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    2-CARBONYLTHIAZOLE DERIVATIVES AND USE OF THE SAME
    2.
    发明授权
    2-CARBONYLTHIAZOLE DERIVATIVES AND USE OF THE SAME 失效
    2-羰基噻唑衍生物及其用途

    公开(公告)号：EP0940401B1

    公开(公告)日：2002-11-06

    申请号：EP97940436.5

    申请日：1997-09-19

    申请人： TAISHO PHARMACEUTICAL CO. LTD ,  Nihon Nohyaku Co., Ltd.

    发明人： NAKAZATO, Atsuro ,  KUMAGAI, Toshihito ,  CHAKI, Shigeyuki ,  TOMISAWA, Kazuyuki ,  NAGAMINE, Masashi, Nihon Nohyaku Co., Ltd ,  GOTOH, Makoto, Nihon Nohyaku Co., Ltd. ,  YOSHIDA, Masanori, Nihon Nohyaku Co., Ltd.

    IPC分类号： C07D417/06 ,  A61K31/445

    CPC分类号： C07D417/06

    摘要： 2-Carbonylthiazole derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof (wherein Ar?1 and Ar2¿ represent each phenyl optionally having one or two substituents selected from among halogeno, C¿1-5? alkyl, trifluoromethyl, C1-5 alkoxy and hydroxy or thienyl; R?1¿ represents C¿1-5? alkoxy, hydroxy or amino represented by the formula N(R?3)R4¿ (wherein R?3 and R4¿ represent each hydrogen or C¿1-5? alkyl, or R?3 and R4¿ together with the nitrogen atom to which they are bonded may form pyrrolidino, piperidino, morphorino or piperazino optionally having one to four substituents selected from among C¿1-5? alkyl, C1-5 alkoxy and hydroxy); Y?1-Y2¿ represents CH-CO or C=C(R2) (wherein R2 represents hydrogen or C¿1-5? alkyl); and n is an integer of 1 to 4); drugs comprising the derivatives represented by the above general formula (I) or pharmaceutically acceptable salts thereof; and dopamine D4 receptor antagonists containing as the active ingredient the same. These drugs are useful as preventives and remedies for various diseases in which dopamine D4 receptors participate, for example, schizophrenia, cerebrovascular disorders and problematic behaviors accompanying senile dementia without showing any extrapyramidal disorders as the side effect.

    摘要翻译： （I）表示的2-羰基噻唑衍生物或其药学上可接受的盐（其中Ar 1和Ar 2代表各自任选具有一个或两个选自卤素，C 1-5烷基，三氟甲基， R 5代表C 1-5烷氧基，羟基或由式N（R 3）R 4表示的氨基（其中R 3和R 4各自代表氢或C 1 -5烷基或R 3和R 4与它们所连接的氮原子一起可形成吡咯烷基，哌啶子基，吗啉代或哌嗪子基，其任选地具有一至四个选自C 1-5 - 烷基，C 1-6 - 5烷氧基和羟基）; Y 1 -Y 2'代表CH-CO或C = C（R 2）（其中R 2代表氢或C 1-5-5烷基）;并且n是1至4的整数。 包含由上述通式（I）表示的衍生物或其药学上可接受的盐的药物; 和含有相同作为活性成分的多巴胺D4受体拮抗剂。 这些药物可用作多巴胺D4受体参与的各种疾病的预防和治疗药物，例如精神分裂症，脑血管障碍和伴随老年性痴呆的有问题的行为，而不显示任何锥体外系疾病作为副作用。

    PROCESS FOR PRODUCTION OF CIS-4-FLUORO-L-PROLINE DERIVATIVES
    3.
    发明公开
    PROCESS FOR PRODUCTION OF CIS-4-FLUORO-L-PROLINE DERIVATIVES 审中-公开
    VERFAHREN ZUR HERSTELLUNG VON CIS-4-FLUOR-L-PROLINDERIVATEN

    公开(公告)号：EP1657237A1

    公开(公告)日：2006-05-17

    申请号：EP04771788.9

    申请日：2004-08-18

    申请人： Taisho Pharmaceutical Co. Ltd.

    发明人： TOMISAWA, Kazuyuki ,  TATSUTA, D., c/o Taisho Pharmaceutical Co., Ltd. ,  YOSHIDA, T., c/o Taisho Pharmaceutical Co.,Ltd. ,  YOKOO, C., c/o Taisho Pharmaceutical Co., Ltd

    IPC分类号： C07D207/16

    CPC分类号： C07D207/16 ,  Y02P20/55

    摘要： The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]:

    (wherein R 1 represents a protecting group for an α-amino group, and R 2 represents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.

    摘要翻译： 本发明提供了一种在更温和的条件下生产顺式-4-氟-L-脯氨酸衍生物的更安全的方法，并以良好的产率，以低成本在工业规模上得到高纯度的产物。 即，本发明提供顺式-4-氟-L-脯氨酸衍生物的制造方法，其包括使下式[I]的反式-4-羟基-L-脯氨酸衍生物：其中R 1表示 保护基为± - 氨基，R 2表示羧基的保护基）与N，N-二乙基-N-（1,1,2,3,3,3-六氟丙基）胺在存在下 氟化氢清除剂。

    2-CARBONYLTHIAZOLE DERIVATIVES AND USE OF THE SAME
    5.
    发明公开
    2-CARBONYLTHIAZOLE DERIVATIVES AND USE OF THE SAME 失效
    2-羰基噻唑衍生物及其用途

    公开(公告)号：EP0940401A1

    公开(公告)日：1999-09-08

    申请号：EP97940436.5

    申请日：1997-09-19

    申请人： TAISHO PHARMACEUTICAL CO. LTD ,  Nihon Nohyaku Co., Ltd.

    发明人： NAKAZATO, Atsuro ,  KUMAGAI, Toshihito ,  CHAKI, Shigeyuki ,  TOMISAWA, Kazuyuki ,  NAGAMINE, Masashi, Nihon Nohyaku Co., Ltd ,  GOTOH, Makoto, Nihon Nohyaku Co., Ltd. ,  YOSHIDA, Masanori, Nihon Nohyaku Co., Ltd.

    IPC分类号： C07D417/06 ,  A61K31/445

    CPC分类号： C07D417/06

    摘要： This invention provides a 2-carbonylthiazole derivative represented by formula (I):
    [wherein each of Ar 1 and Ar 2 represents a phenyl group, a phenyl group having one or two substituents selected from "a halogen atom, an alkyl group having 1 to 5 carbon atoms, a trifluoromethyl group, an alkoxy group having 1 to 5 carbon atoms and a hydroxyl group" or a thienyl group; R 1 represents an alkoxy group having 1 to 5 carbon atoms, a hydroxyl group or an amino group represented by formula N(R 3 )R 4 (wherein each of R 3 and R 4 represents a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, or R 3 and R 4 , together with the nitrogen atom to which they are bound, form a pyrrolidino, piperidino, morpholino or piperazino group, or a pyrrolidino, piperidino, morpholino or piperazino group having one to four substituents selected from "an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms and a hydroxyl group"); Y 1 -Y 2 represents CH-CO or C=C(R 2 ) (wherein R 2 represents a hydrogen atom or an alkyl group having 1 to 5 carbon atoms); and n is an integer of from 1 to 4] or a pharmaceutically acceptable salt thereof. It also provides a medicament which comprises the 2-carbonylthiazole derivative of formula (I) or a pharmaceutically acceptable salt thereof and a dopamine D 4 receptor antagonist which contains the same as the active ingredient, which are useful as drugs for preventing and treating dopamine D 4 receptor-related morbid states such as schizophrenia and problematic behavior caused by cerebrovascular accidents and senile dementia, and also as the drugs which do not induce extrapyramidal disorders as side effects.

    摘要翻译： 本发明提供了由式（I）表示的2-羰基噻唑衍生物：[其中Ar 1和Ar 2各自表示苯基，具有一个或两个选自下列取代基的苯基：卤素原子，具有1至5个碳的烷基 原子，三氟甲基，具有1至5个碳原子和羟基的烷氧基“或噻吩基; R1表示具有1至5个碳原子的烷氧基，羟基或由式N（R3）R4表示的氨基（其中R3和R4各自表示氢原子或具有1至5个碳原子的烷基，或 R3和R4与它们所连接的氮原子一起形成吡咯烷基，哌啶子基，吗啉代或哌嗪子基，或具有1-4个取代基的吡咯烷子基，哌啶子基，吗啉代或哌嗪子基，所述取代基选自“具有1至 5个碳原子，具有1至5个碳原子的烷氧基和羟基“）; Y 1 -Y 2表示CH-CO或C = C（R 2）（其中R 2表示氢原子或具有1至5个碳原子的烷基）。 并且n是1至4的整数]或其药学上可接受的盐。 它还提供了一种药物，其包含式（I）的2-羰基噻唑衍生物或其药学上可接受的盐和含有该化合物作为活性成分的多巴胺D4受体拮抗剂，其可用作预防和治疗多巴胺D4受体 相关病态如精神分裂症和由脑血管意外和老年性痴呆引起的问题行为，以及作为不引起锥体外系疾病的药物作为副作用。

    CARBAMOYL TETRAHYDROPYRIDINE DERIVATIVES
    8.
    发明公开
    CARBAMOYL TETRAHYDROPYRIDINE DERIVATIVES 有权
    氨基甲酰四氢吡啶衍生物

    公开(公告)号：EP1176146A1

    公开(公告)日：2002-01-30

    申请号：EP00907999.7

    申请日：2000-03-10

    申请人： TAISHO PHARMACEUTICAL CO., LTD

    发明人： NAKAZATO, Atsuro ,  OKUBO, Taketoshi ,  KUMAGAI, Toshihito ,  TOMISAWA, Kazuyuki

    IPC分类号： C07D473/34 ,  C07D487/04 ,  C07D211/78 ,  C07D207/34 ,  A61K31/52 ,  A61K31/519 ,  A61P43/00 ,  A61P25/24 ,  A61P25/22 ,  A61P25/28 ,  A61P25/16 ,  A61P25/30 ,  A61P25/08 ,  A61P1/00 ,  A61P7/10 ,  A61P9/10 ,  A61P9/12 ,  A61P17/02 ,  A61P29/00 ,  A61P37/02

    CPC分类号： A61K31/519 ,  C07D473/00 ,  C07D487/04

    摘要： Carbamoyl tetrahydropyridine derivatives represented by the formula:
    [in the formula, R 1 and R 2 are identical or different, and each represents a hydrogen atom, a C 1 -C 5 alkyl group, or the like; Y 1 -Y 2 represents (R 4 )C=C(R 5 ), (R 6 )C=N, N=N, (R 7 )N-CO, or N=C(R 8 ); X 1 , X 2 , and X 3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R 3 , R 4 , R 5 , and R 6 are identical or different, and each represents a hydrogen atom or an alkyl group; R 7 represents a hydrogen atom, a C 1 -C 5 alkyl group, or the like; and R 8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided.
    The derivatives described above are effective for diseases which are believed to involve CRF.

    摘要翻译： 由下式表示的氨基甲酰基四氢吡啶衍生物[式中，R1和R2相同或不同，且各自表示氢原子，C1-C5烷基等; Y1-Y2表示（R4）C = C（R5），（R6）C = N，N = N，（R7）N-CO或N = C（R8）。 X 1，X 2和X 3相同或不同，并且各自表示氢原子，卤素原子等; R3，R4，R5和R6相同或不同，并且各自表示氢原子或烷基; R7代表氢原子，C1-C5烷基等; 并且R 8表示氢原子或氨基甲酰基]或其药学上可接受的盐，以及用于其制备的中间体。 上述衍生物对于认为涉及CRF的疾病是有效的。

    1,2-DIHYDRO-2-OXOQUINOLINE DERIVATIVES
    9.
    发明公开
    1,2-DIHYDRO-2-OXOQUINOLINE DERIVATIVES 有权
    1,2-二氢-2- OXOCHINOLIN衍

    公开(公告)号：EP1048655A1

    公开(公告)日：2000-11-02

    申请号：EP98957145.0

    申请日：1998-12-03

    申请人： TAISHO PHARMACEUTICAL CO., LTD ,  Nihon Nohyaku Co., Ltd.

    发明人： NAKAZATO, Atsuro ,  OKUBO, Taketoshi ,  KUMAGAI, Toshihito ,  CHAKI, Shigeyuki ,  TOMISAWA, Kazuyuki ,  NAGAMINE, Masashi ,  GOTOH, Makoto ,  YOSHIDA, Masanori

    IPC分类号： C07D215/54 ,  C07D215/56 ,  C07D241/44 ,  C07D491/056 ,  A61K31/47 ,  A61K31/495

    CPC分类号： C07D401/06 ,  C07D215/54 ,  C07D241/44

    摘要： A 1,2-dihydro-2-oxoquinoline derivative represented by the formula:
    wherein Ar is a pyridyl group or a group represented by the formula:
    (wherein X 3 and X 4 are the same or different, and are each a hydrogen atom, a halogen atom, a C 1-5 alkyl group, a C 1-5 alkoxy group, a hydroxyl group or a trifluoromethyl group), Y is a nitrogen atom, CH or C(OH), R 1 and R 2 are the same or different, and are each a hydrogen atom, a C 1-10 alkyl group, a C 3-15 alkoxyalkyl group or a C 3-15 alkylaminoalkyl group, or R 1 and R 2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X 1 and X 2 are the same or different, and are each a hydrogen atom, a C 1-5 alkyl group, a C 1-5 alkoxy group or a halogen atom, or X 1 and X 2 taken together form an alkylenedioxy group, and n is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 由下式表示的1,2-二氢-2-氧代喹啉衍生物：其中Ar为吡啶基或由下式表示的基团：其中X 3和X 4相同 或不同，并且各自为氢原子，卤素原子，C 1-5烷基，C 1-5烷氧基，羟基或三氟甲基），Y为氮原子，CH或C（OH） R 1和R 2相同或不同，各自为氢原子，C 1-10烷基，C 3-15烷氧基烷基或C 3-15烷基氨基烷基，或R 1和R 2 与它们所连接的氮原子一起形成环状氨基，X 1和X 2相同或不同，分别为氢原子，C 1-5烷基， C 1-5烷氧基或卤原子，或X 1和X 2一起形成亚烷基二氧基，n为1〜3的整数。 或其药学上可接受的盐。