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    QUINOLINE DERIVATIVE OR SALT THEREOF AND REMEDY FOR CARDIAC DISEASES CONTAINING THE SAME.
    1.
    发明公开
    QUINOLINE DERIVATIVE OR SALT THEREOF AND REMEDY FOR CARDIAC DISEASES CONTAINING THE SAME. 失效
    喹啉或它们的盐和含有心脏病的治疗。

    公开(公告)号：EP0638571A4

    公开(公告)日：1995-04-12

    申请号：EP93911951

    申请日：1993-04-28

    Applicant: KOWA CO

    Inventor： KYOTANI YOSHINORI ,  OGIYA TADAAKI ,  TOMA TSUTOMU ,  KURIHARA YUJI ,  KITAMURA TAKAHIRO ,  YAMAGUCHI TAKASHI ,  ONOGI KAZUHIRO ,  SATO SEICHI ,  SHIGYO HIROMICHI ,  OTA TOMIO ,  KAWADA MITSUO ,  UCHIDA YASUMI

    IPC: C07D491/04 ,  C07D491/048 ,  C07D491/056 ,  A61K31/47

    CPC classification number: C07D491/04

    Abstract: A quinoline derivative represented by general formula (1), a medicinally acceptable salt thereof, and a remedy for cardiac diseases containing the same, wherein ring A represents a furan, dihydrofuran or dioxolane ring, R1 represents hydroxy, carboxy, alkoxycarbonyl, etc., R2s may be the same or different from each other and each represents hydrogen, alkyl, etc., R?3 and R4¿ may be the same or different from each other and each represents hydrogen, halogen, alkyl, amino, alkoxy, etc., R?5, R6, R7 and R8¿ may be the same or different from one another and each represents hydrogen or alkyl, m represents an integer of 0 to 3, and symbol ...... means that there may be a double bond formed by R?6 and R8¿. The compound (1) has a positively inotropic effect on myocardia and an antiarrhythmic effect and can dilate blood vessels without extremely increasing the heart rate. Therefore, a remedy for cardiac diseases containing the same as the active ingredient is remarkably useful for treating cardiac insufficiency, arrhythmia, and so forth.

    Abstract translation: 由通式所表示的喹啉衍生物（1），其药物上可接受的盐，以及用于心脏病含有相同，worin环A darstellt呋喃，二氢呋喃或二氧戊环的补救，R <1> darstellt羟基，羧基，烷氧基羰基， 等，R <2> S可以是相同的或彼此和各darstellt氢，烷基等不同，R <3>和R <4>可以是从彼此，并且每个darstellt氢相同或不同， 卤素，烷基，氨基，烷氧基等，R <5> - [R <6> - [R <7>和R <8>可以相同或彼此不同，分别darstellt氢或烷基，米darstellt成整数 0至3，和符号...... bedeutet，DASS可能存在由R形成双键<6>和R <8>。 的化合物（1）对心肌和抗心律失常效果率的带正性肌力作用和可扩张血管，而不极端地增加的心脏。 因此，对于心脏病含有相同的活性成分的补救可用于治疗心功能不全，心律失常，等等非常有用。

    Novel compound having 3-(5-ethoxypyrimidin-2-yl)pyrimidine-4(3h)-one structure, and medicine containing the same
    2.
    发明专利
    Novel compound having 3-(5-ethoxypyrimidin-2-yl)pyrimidine-4(3h)-one structure, and medicine containing the same 审中-公开
    具有3-（5-乙氧基嘧啶-2-YL）嘧啶-4（3H） - 酮结构的新化合物和含有它们的药物

    公开(公告)号：JP2012041309A

    公开(公告)日：2012-03-01

    申请号：JP2010185007

    申请日：2010-08-20

    Applicant: Kowa Co ,  興和株式会社

    Inventor： MIURA TORU ,  TAGASHIRA JUNYA ,  SEKIMOTO RYOHEI ,  ISHIDA RIE ,  AOKI HITOMI ,  OGIYA TADAAKI

    IPC: C07D413/14 ,  A61K31/513 ,  A61P3/00 ,  A61P3/10 ,  A61P5/50 ,  A61P9/10 ,  A61P13/12 ,  A61P25/00 ,  A61P27/02 ,  A61P43/00

    Abstract: PROBLEM TO BE SOLVED: To provide a novel compound which has angiotensin II receptor antagonism and PPARγ activating action, and is useful as a preventing and/or therapeutic agent for hypertension, heart disease, angina pectoris, cerebrovascular disorder, cerebral circulation disorder, ischemia nature peripheral circulatory failure, kidney disease, arteriosclerosis, inflammatory disease, 2 type diabetes, diabetic complication, insulin resistance syndrome, syndrome X, metabolic syndrome, and high insulinemia.SOLUTION: A 3-(5-ethoxypyrimidin-2-yl)pyrimidine-4(3H)-one derivative, a salt thereof or a solvate thereof, and a pharmaceutical composition containing the same are disclosed.

    Abstract translation: 要解决的问题：提供具有血管紧张素II受体拮抗作用和PPARγ活化作用的新型化合物，可用作高血压，心脏病，心绞痛，脑血管障碍，脑循环障碍的预防和/或治疗剂 ，缺血性周围循环衰竭，肾脏疾病，动脉硬化，炎性疾病，2型糖尿病，糖尿病并发症，胰岛素抵抗综合征，综合征X，代谢综合征和高胰岛素血症。 解决方案：公开了3-（5-乙氧基嘧啶-2-基）嘧啶-4（3H） - 酮衍生物，其盐或其溶剂化物和含有它们的药物组合物。 版权所有（C）2012，JPO＆INPIT

    METHD OF PRODUCING 3,5-BISALKYLPHENOL
    3.
    发明专利
    METHD OF PRODUCING 3,5-BISALKYLPHENOL 失效

    公开(公告)号：JP2002167343A

    公开(公告)日：2002-06-11

    申请号：JP2001054802

    申请日：2001-02-28

    Applicant: KOWA CO

    Inventor： SHIBUYA MASAYUKI ,  OGIYA TADAAKI ,  MIURA TORU ,  ONOKI KAZUHIRO

    IPC: C07C37/01 ,  C07C37/00 ,  C07C37/11 ,  C07C37/50 ,  C07C39/06 ,  C07C39/11 ,  C07C39/235 ,  C07C43/23

    Abstract: PROBLEM TO BE SOLVED: To obtain, efficiently and safely in a short process, and further with high purity and in high yield, 3,5-diisopropylphenol or the like which are important as a synthetic intermediate for medicines and agrochemicals. SOLUTION: 3,5-bisalkylphenol (2) and a carbinol compound (1) are obtained by the following reaction formula. [wherein, R1 represents H, an alkali metal atom, an alkali earth metal atom or a hydroxyl protecting group (except a methyl group); R2 may represent a 1-5C lower alkyl group or a phenyl group which may have a substitute; R3 and R4 may represent the same or different lower alkyl, aralkyl or aryl groups].

    NEW PIPERIDINE DERIVATIVE AND PHARMACEUTICAL CONTAINING THE SAME
    4.
    发明专利
    NEW PIPERIDINE DERIVATIVE AND PHARMACEUTICAL CONTAINING THE SAME 审中-公开

    公开(公告)号：JP2013253019A

    公开(公告)日：2013-12-19

    申请号：JP2010217446

    申请日：2010-09-28

    Applicant: KOWA CO

    Inventor： MORIMOTO TOSHIHARU ,  KOSHIZAWA TOMOAKI ,  WATABE GEN ,  FUKUDA TOMOAKI ,  OGIYA TADAAKI ,  SHIMIZU NAHO ,  INOUE KUNIYUKI

    IPC: C07D498/04 ,  A61K31/519 ,  A61P3/10 ,  A61P5/50

    Abstract: PROBLEM TO BE SOLVED: To provide a new compound having an action to promote insulin secretion from pancreatic &bgr; cells, and useful as a prophylactic and/or therapeutic agent for disorders caused by hyperglycemia, e.g. diabetes mellitus.SOLUTION: There is disclosed a compound expressed by general formula (1) or salt thereof or solvates thereof. In formula, one of A and B represents a nitrogen atom and the other thereof represents a nitrogen atom or CR; X represents an oxygen atom, sulfur atom, -(CH)-N(R)- or -(CH)-CH(R)-; Z represents a nitrogen atom when Y is an oxygen atom or sulfur atom, or Z represents an oxygen atom or sulfur atom when Y is a nitrogen atom; Rto Reach represents a hydrogen atom or another substituent.

    Optically active dibenzylamine derivative and method for producing the same
    5.
    发明专利
    Optically active dibenzylamine derivative and method for producing the same 有权
    光活性二苯胺衍生物及其制备方法

    公开(公告)号：JP2013136572A

    公开(公告)日：2013-07-11

    申请号：JP2012263933

    申请日：2012-12-03

    Applicant: Kowa Co ,  興和株式会社

    Inventor： OGIYA TADAAKI ,  MURAKAMI TAKESHI ,  MIYOSAWA KATSUTOSHI ,  SHIBUYA MASAYUKI ,  YAMAZAKI KOICHI ,  KUSAKABE TAICHI

    IPC: C07D239/14 ,  A61K31/505 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  C12N15/09 ,  C12Q1/68

    Abstract: PROBLEM TO BE SOLVED: To provide a low-molecular compound which has such an action as to decrease the amount of PCSK9 protein and increase the amount of LDL receptor, and to provide a medicine including the low-molecular compound as an active ingredient.SOLUTION: The medicine includes (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetate which is substantially optically-pure or a salt thereof, or solvates of them as an active ingredient.

    Abstract translation: 要解决的问题：提供具有降低PCSK9蛋白质量和增加LDL受体量的作用的低分子化合物，并提供包含低分子化合物作为活性成分的药物。 ：该药物包括（S） - 反 - {4 - [（{2 - [（{1- [3,5-双（三氟甲基）苯基]乙基} {5- [2-（甲基磺酰基）乙氧基] - 基}氨基）甲基] -4-（三氟甲基）苯基}（乙基）氨基）甲基]环己基}乙酸乙酯，其基本上为光学纯的或其盐，或它们的溶剂合物作为活性成分。

    Advanced glycation end product formation inhibitor comprising pyrazine derivative as active ingredient
    6.
    发明专利
    Advanced glycation end product formation inhibitor comprising pyrazine derivative as active ingredient 审中-公开
    高效糖化终产物形成抑制剂包含吡嗪衍生物作为活性成分

    公开(公告)号：JP2008110921A

    公开(公告)日：2008-05-15

    申请号：JP2006293321

    申请日：2006-10-27

    Applicant: Kowa Co ,  興和株式会社

    Inventor： NAKAGAWA TAKASHI ,  SEKIMOTO RYOHEI ,  OGIYA TADAAKI ,  ONOKI KAZUHIRO ,  MIYATA TOSHIO

    IPC: C07D241/18 ,  A61K31/4965 ,  A61P3/10 ,  A61P9/12 ,  A61P13/12 ,  A61P43/00

    Abstract: PROBLEM TO BE SOLVED: To provide a novel AGE (advanced glycation end product) formation inhibitor.
    SOLUTION: The novel AGE formation inhibitor includes a compound represented by general formula (I) (wherein each of R
    1 , R
    2 , R
    3 , R
    4 , R
    5 and R
    6 independently represents a hydrogen atom, a halogen atom, 1-6C alkyl group or a 1-6C alkoxy group; R
    7 represents a hydrogen atom or a 1-6C alkyl group; and n represents an integer of 1 to 4), a salt thereof, and a solvate thereof. In particular, 5,6-bis(4-methoxyphenyl)-3-(2-carboxyethyl)-2H-pyrazin-2-one is preferable. The compounds according to the present invention have an excellent inhibiting action on AGE formation and are useful as a medicine for preventing and/or treating a glomerular disease, particularly for preventing and/or treating diabetic nephropathy.
    COPYRIGHT: (C)2008,JPO&INPIT

    Abstract translation: 要解决的问题：提供新型AGE（晚期糖基化终产物）形成抑制剂。 解决方案：新型AGE形成抑制剂包括由通式（I）表示的化合物（其中R 1，R 2，R 3，R 3， / SP>，R 4 ，R 5 和R 6 独立地表示氢原子，卤素原子，1-6C烷基或 1-6C烷氧基; R 7表示氢原子或1-6C烷基，n表示1〜4的整数），其盐及其溶剂合物。 特别优选5,6-双（4-甲氧基苯基）-3-（2-羧乙基）-2H-吡嗪-2-酮。 根据本发明的化合物对AGE形成具有优异的抑制作用，可用作预防和/或治疗肾小球疾病，特别是用于预防和/或治疗糖尿病肾病的药物。 版权所有（C）2008，JPO＆INPIT

    PRODUCTION OF INDOLE DERIVATIVE
    7.
    发明专利
    PRODUCTION OF INDOLE DERIVATIVE 失效

    公开(公告)号：JPH09176117A

    公开(公告)日：1997-07-08

    申请号：JP33684495

    申请日：1995-12-25

    Applicant: KOWA CO

    Inventor： KYOTANI YOSHINORI ,  SHIMIZU NOBORU ,  SATO SEIICHI ,  YAMAGUCHI TAKASHI ,  KITAMURA TAKAHIRO ,  OGIYA TADAAKI ,  KAWAMINE KATSUMI

    IPC: C07D209/34 ,  B01J31/24 ,  C07B61/00 ,  C07F7/10

    Abstract: PROBLEM TO BE SOLVED: To produce an indole derivative useful as a synthetic intermediate for a furo[2,3-e]indole derivative having treating action on cardiac diseases under mild reaction condition in high yield. SOLUTION: The objective indole derivative expressed by the formula I [R and R are each a (substituted)alkyl; R is an alkyl or an aralkyl; R and R are each H, a halogen, etc.; R is H, sec-butyl, etc.] can be produced by cyclizing a compound of the formula II (R is sec-butyl, t-butyl, etc.; X is a halogen) in the presence of a metal (e.g. copper or iron) or a metal complex (e.g. a palladium complex). The amounts of the metal catalyst and the metal complex in the reaction are preferably 1-2mol-equivalent and 0.01-0.1 mol- equivalent based on the compound of the formula II, respectively.

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