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    2.
    发明专利
    失效

    公开(公告)号：JPH05310744A

    公开(公告)日：1993-11-22

    申请号：JP11286392

    申请日：1992-05-01

    Applicant: KOWA CO

    Inventor： KYOTANI YOSHINORI ,  TAIMA TSUTOMU ,  KURIHARA YUJI ,  KITAMURA TAKAHIRO ,  YAMAGUCHI TAKASHI ,  KAMIYA KAZUHIRO ,  ONOKI KAZUHIRO ,  SATO SEIICHI ,  OTA TOMIO ,  UCHIDA YASUYOSHI

    IPC: A61K31/47 ,  A61K31/4741 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  C07D491/052

    Abstract: PURPOSE:To provide a new pyrano[2,3-f]quinoline derivative having excel lent antiarrhythmic action, cardiac action, vasodilative action, etc., and useful as a cardiac disease therapeutic agent represented by cardiac failures. CONSTITUTION:The compound of formula 1 (R is lower alkyl; R is H, halogen, OH, lower alkylsulfonyloxy, lower alkanoyloxy, lower alkoxy, azido, amino; R is H, lower alkyl; R is H, lower alkyl, OH, lower alkylamino, pyrrolidinyl or piperazinyl which may have a substituent; when a double bond exists between the 3,4 positions, the substituent R does not exist), e.g. 3acetoxy-6-methyl-3,4,7,8- tetrahydro-2H-pyrano[2,3-f]quinoline. The compound of formula 1-1 among the compounds of formula 1 is obtained by reacting a quinoline compound with an allyl halide compound, thermally subjecting the obtained compound of formula 3 to a Claisen rearrangement, reacting the reaction product with an aliphatic acid anhydride, reacting the obtained compound of formula 5 with a peracid, and subsequently treating the produced epoxy compound of formula 6 with an alkali halide.

    Hdl increasing agent
    3.
    发明专利
    Hdl increasing agent 审中-公开
    HDL增加剂

    公开(公告)号：JP2009196901A

    公开(公告)日：2009-09-03

    申请号：JP2008037390

    申请日：2008-02-19

    Applicant: Kowa Co ,  興和株式会社

    Inventor： ABE KAZUTOYO ,  TAIMA TSUTOMU

    IPC: A61K31/427 ,  A61P3/06 ,  A61P9/10 ,  C07D471/04

    Abstract: PROBLEM TO BE SOLVED: To provide an HDL (high-density lipoprotein) increasing agent useful as a prophylactic and/or a therapeutic agent of arteriosclerosis, cardiovascular disorders, particularly myocardial infarction and cerebral infarction.
    SOLUTION: The HDL increasing agent comprises a 2-phenylimidazo[1,2-a]pyridine derivative represented by general formula (1) [wherein, R
    1 represents a hydrogen atom or a 1-6C alkyl group; R
    2 , R
    3 , R
    4 and R
    5 are each same or different and represent each a hydrogen atom, a halogen atom, a 1-6C alkyl group which may be substituted with a 1-6C acyloxy group, a halo-1-6C alkyl group, a 2-6C alkenyl group, a 2-6C alkynyl group, a 1-6C alkoxy group, a halo-1-6C alkoxy group, a 1-6C acyl group, a nitro group, a cyano group, a carboxy group, a 1-6C alkoxycarbonyl group, or a carbamoyl group; or R
    2 and R
    3 or R
    4 and R
    5 together may form a 1-3C alkylenedioxy group] or a salt thereof or a solvate thereof as an active ingredient.
    COPYRIGHT: (C)2009,JPO&INPIT

    Abstract translation: 要解决的问题：提供可用作动脉硬化，心血管疾病，特别是心肌梗死和脑梗死的预防和/或治疗剂的HDL（高密度脂蛋白）增加剂。 解决方案：HDL增加剂包含由通式（1）表示的2-苯基咪唑并[1,2-a]吡啶衍生物[其中R 1表示氢原子或1- 6C烷基; R 2 ，R 3 ，R 4 和R 5 各自相同或不同，表示氢原子 卤素原子，可被1-6个碳酰氧基取代的1-6C烷基，卤代-1,6- C烷基，2-6C烯基，2-6C炔基，1-6C 烷氧基，卤代-C 1-6烷氧基，1-6C酰基，硝基，氰基，羧基，1-6C烷氧基羰基或氨基甲酰基; 或R 2 和R 3 或R 4 和R 5 可以形成1-3C亚烷基二氧基] 或其盐或其溶剂合物作为活性成分。 版权所有（C）2009，JPO＆INPIT

    PYRIMIDINE DERIVATIVE AND MANUFACTURE OF THE SAME
    5.
    发明专利
    PYRIMIDINE DERIVATIVE AND MANUFACTURE OF THE SAME 失效

    公开(公告)号：JP2000143637A

    公开(公告)日：2000-05-26

    申请号：JP24715699

    申请日：1999-09-01

    Applicant: KOWA CO

    Inventor： TAKAHASHI YOSHIO ,  TAIMA TSUTOMU ,  OSHIMA TAKESHI ,  ISHIKAWA TETSUYA ,  YAMAGUCHI TAKASHI ,  HIRATA MITSUTERU ,  SATO YUKIHIRO ,  YAMADA HAJIME

    IPC: C07D239/52 ,  A61K31/505 ,  A61K31/5377 ,  A61P9/00 ,  A61P9/12 ,  A61P43/00

    Abstract: PROBLEM TO BE SOLVED: To obtain a new pyrimidine derivative having potent endothelin antagonism useful for medicine as a therapeutic agent of circulatory system disease or the like. SOLUTION: This derivative is expressed by formula I [R1 is a lower alkyl; R2 is a (substituted) pyrimidyl, morpholino; n is 1 to 3], preferably, 3-[6-(4-t- butylphenylsulfonylamino)-5-(2-methoxyphenoxy)-2-(2-pyrimidyl)-4-pyrim idyloxy) propanal or the like. The compound of formula I is preferably obtained by reacting a compound expressed by formula III [R3 is a (substituted) alkyl, an aralkyl or the like] (for example; 3,3-diethoxy-1-propanol or the like) to a compound expressed by formula II (X is a halogen) for example; 4-t-butyl-N-[6- chloro-5-(2-methoxyphenoxy)-2-(2-pyrimidyl)-4-pyrimidyl]benzenesulfona mide or the like} to obtain the compound of formula IV, and deprotecting the product.

    Benzoic acid derivative and medicine containing the same
    7.
    发明专利
    Benzoic acid derivative and medicine containing the same 有权
    苯甲酸衍生物和含有它们的药物

    公开(公告)号：JP2004323426A

    公开(公告)日：2004-11-18

    申请号：JP2003121227

    申请日：2003-04-25

    Applicant: Kowa Co ,  興和株式会社

    Inventor： YAMAZAKI YUKIYOSHI ,  TAIMA TSUTOMU ,  NISHIKAWA MASAHIRO ,  YAMADA HAJIME ,  OZAWA HIDESHI ,  ABE KAZUTOYO

    IPC: A61P3/06 ,  A61K31/192 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P29/00 ,  A61P43/00 ,  C07C317/44 ,  C07C323/62

    Abstract: PROBLEM TO BE SOLVED: To provide a PPARα-selective activated compound useful as a medicine for preventing and/or treating hyperlipemia, arteriosclerosis, diabetes, diabetic complication, inflammation, heart disease or the like not accompanying weight gain and overweight.
    SOLUTION: The benzoic acid derivative represented by general formula (1) [wherein, -A- is a -CH
    2 -CH
    2 - group, a -CH=CH- group, a -CH(OH)-CH
    2 - group or a -C(O)-CH
    2 - group; X is an oxygen atom, an NH group or an S(O)
    n group (wherein, n is an integer of 0, 1 or 2)] or a salt thereof, and a medicine using the derivative or the salt thereof are provided. The medicine has an activity for selectively activating the α type in the PPAR, and is effective as the medicine for preventing and/or treating the hyperlipemia, the arteriosclerosis, the diabetes, the diabetic complication, the inflammation, the heart disease or the like not accompanying the weight gain and the overweight.
    COPYRIGHT: (C)2005,JPO&NCIPI

    Abstract translation: 待解决的问题：提供一种PPARα选择性活化化合物，其可用作预防和/或治疗高脂血症，动脉硬化，糖尿病，糖尿病并发症，炎症，心脏病等的药物，不伴随体重增加和超重。 解决方案：由通式（1）表示的苯甲酸衍生物[其中，-A-为-CH 2 SB 2 -CH SB 2 - 基团，-CH = CH-基，-CH（OH）-CH 2 SB 2 - 或-C（O）-CH 2 SB 2 - ; X是氧原子，NH基或S（O） n 基（其中n是0,1或2的整数）]或其盐，以及使用该衍生物的药物 或其盐。 该药具有选择性活化PPAR中的α型活性，作为预防和/或治疗高脂血症，动脉硬化，糖尿病，糖尿病并发症，炎症，心脏病等的药物不起作用 伴随体重增加和超重。 版权所有（C）2005，JPO＆NCIPI

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