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。

公开(公告)号：EP1156039A4

公开(公告)日：2002-04-17

申请号：EP00905344

申请日：2000-02-25

Applicant: KOWA CO

Inventor： OHKUCHI MASAO ,  KYOTANI YOSHINORI ,  SHIGYO HIROMICHI ,  YOSHIZAKI HIDEO ,  KOSHI TOMOYUKI ,  KITAMURA TAKAHIRO ,  MATSUDA TAKAYUKI ,  YASUOKA KYOKO ,  FURUYAMA TOMOKO

IPC: C07D237/14 ,  A61K31/00 ,  A61K31/50 ,  A61K31/501 ,  A61P1/00 ,  A61P1/04 ,  A61P9/00 ,  A61P9/10 ,  A61P19/00 ,  A61P19/02 ,  A61P19/10 ,  A61P29/00 ,  A61P37/00 ,  A61P37/06 ,  C07D209/00 ,  C07D213/00 ,  C07D237/00 ,  C07D237/24 ,  C07D401/12 ,  C07D403/06

CPC classification number: C07D237/24

Abstract: Pyridazin-3-one derivatives of general formula (1) or salts of the same, exhibiting an excellent interleukin-1β production inhibiting effect; and medicines containing the derivatives or the salts as the active ingredient wherein Ar1 is an optionally substituted aromatic group; Ar2 is phenyl substituted at least at the 4-position; R1 is linear or branched alkyl, alkyl having a cyclic structure, optionally substituted phenyl, or optionally substituted phenyl lower alkyl; and R2 is cyano, carboxyl, lower alkoxycarbonyl, optionally substituted lower alkyl, or optionally substituted carbamoyl.

公开(公告)号：EP2415764A4

公开(公告)日：2012-08-08

申请号：EP10758277

申请日：2010-03-31

Applicant: KOWA CO

Inventor： ASHIKAWA MASANORI ,  TAGASHIRA JUNYA ,  KOKETSU AKIYASU ,  MORIMOTO TOSHIHARU ,  KITAMURA TAKAHIRO ,  TAKEMURA SYUNJI ,  WATANABE GEN ,  NISHIYAMA TATSUAKI ,  GODA SATOSHI ,  YAMABI MASAKI ,  DOI TAKESHI ,  ISHIWATA HIROYUKI

IPC: C07D215/22 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61P7/06 ,  A61P43/00 ,  C07D215/44 ,  C07D215/46 ,  C07D215/48 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D215/42 ,  A61K31/47 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/69 ,  C07D215/233 ,  C07D215/44 ,  C07D215/46 ,  C07D215/48 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

公开(公告)号：EP1431294A4

公开(公告)日：2004-09-15

申请号：EP02760658

申请日：2002-08-19

Applicant: KOWA CO

Inventor： SHIBUYA KIMIYUKI ,  KAWAMINE KATSUMI ,  OOGIYA TADAAKI ,  KITAMURA TAKAHIRO ,  MIURA TORU ,  EDANO TOSHIYUKI ,  YOSHINAKA YASUNOBU ,  YAMADA YOUICHI

IPC: A61K31/496 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07D263/58 ,  C07C233/25

CPC classification number: C07D263/58 ,  A61K31/496

Abstract: It is intended to provide a novel compound, which sustains an ACAT inhibitory activity and a macrophage-selectivity to a certain degree as a practically usable drug and can maintain an excellent oral absorbability and a favorable drug concentration in case of tested in vivo; a process for producing the same; medicinal compositions comprising the same and its intermediate. Namely, 2-[4-[2[(7-trifluoromethylbenzoxazol-2-ylthio)ethyl]piperadin-1-yl]-N-(2,6-diisopropyl-4-hydroxyphenyl)acetamide represented by the following formula: salts thereof or solvates of the same; and medicinal compositions comprising the compound represented by the above formula, salts thereof or solvates of the same together with pharmaceutically acceptable carriers.

公开(公告)号：EP1431293A4

公开(公告)日：2004-12-22

申请号：EP02768055

申请日：2002-09-25

Applicant: KOWA CO

Inventor： KYOTANI YOSHINORI ,  KOSHI TOMOYUKI ,  SHIGYO HIROMICHI ,  YOSHIZAKI HIDEO ,  KITAMURA TAKAHIRO ,  TAKEMURA SHUNJI ,  YASUOKA KYOKO ,  TOTSUKA JUNKO ,  SATO SEIICHI

IPC: C07D237/14 ,  A61K31/50 ,  A61K31/501 ,  A61P1/04 ,  A61P9/00 ,  A61P19/02 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P37/02 ,  A61P43/00 ,  C07D237/24

CPC classification number: C07D237/14 ,  A61K31/50 ,  A61K31/501 ,  C07D237/24

Abstract: Compounds represented by the following general formula (1), which have an effect of inhibiting IL-β production, are highly soluble in water and have a favorable oral absorbability, and medicinal compositions containing the same: (1) wherein R1 represents alkyl, alkenyl, etc.; R2 and R3 represent each hydrogen, alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl, or R2 and R3 may form together with the adjacent nitrogen atom an optionally substituted nitrogen-containing saturated heterocyclic group; X, Y and Z represent each hydrogen, alkyl, halogeno, etc.; and n is from 1 to 5.

公开(公告)号：EP1043317A4

公开(公告)日：2003-03-05

申请号：EP98951732

申请日：1998-11-09

Applicant: KOWA CO

Inventor： OHKUCHI MASAO ,  KYOTANI YOSHINORI ,  SHIGYO HIROMICHI ,  KOSHI TOMOYUKI ,  KITAMURA TAKAHIRO ,  OHGIYA TADAAKI ,  MATSUDA TAKAYUKI ,  YAMAZAKI YUKIYOSHI ,  KUMAI NATSUYO ,  KOTAKI KYOKO ,  YOSHIZAKI HIDEO ,  HABATA YURIKO

IPC: A61K31/50 ,  A61K31/501 ,  A61P19/02 ,  A61P19/10 ,  A61P29/00 ,  A61P37/00 ,  C07D213/00 ,  C07D237/00 ,  C07D237/04 ,  C07D237/14 ,  C07D237/18 ,  C07D401/04 ,  C07D401/06

CPC classification number: C07D401/04 ,  C07D237/02 ,  C07D237/04 ,  C07D237/14 ,  C07D237/18 ,  C07D401/06 ,  C07D401/14 ,  C07D413/04

Abstract: Pyridazine derivatives represented by general formula (1) or salts thereof; and drugs containing the same as the active ingredient: wherein R1 is (substituted) aryl; R2 is phenyl substituted with lower alkoxy, lower alkylthio or the like at the position 4; R3 is H, lower alkoxy, lower haloalkyl, lower cycloalkyl, (substituted) aryl, (substituted) aryloxy, (substituted) nitrogenous heterocyclic residue, (substituted) aminocarbonyl or lower alkyl-carbonyl; A is a single bond, lower alkylene or lower alkenylene; X is O or S; and the broken line between the carbon atoms at the positions 4 and 5 represents a single or double bond. These compounds exhibit excellent inhibitory activity against the production of interleukin 1β, thus being useful as preventive and therapeutic drugs for immunologic diseases, inflammatory diseases, ischemic diseases and so on.

公开(公告)号：NO327425B1

公开(公告)日：2009-06-29

申请号：NO20041250

申请日：2004-03-25

Applicant: KOWA CO

Inventor： SHIGYO HIROMICHI ,  SATO SEIICHI ,  KYOTANI YOSHINORI ,  KOSHI TOMOYUKI ,  KITAMURA TAKAHIRO ,  YOSHIZAKI HIDEO ,  YASUOKA KYOKO ,  TAKEMURA SHUNJI ,  TOTSUKA JUNKO

IPC: C07D237/14 ,  C07D237/24 ,  A61K31/50 ,  A61K31/501 ,  A61P1/04 ,  A61P9/00 ,  A61P19/02 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P37/02 ,  A61P43/00

Abstract: Compounds having the formula (1): wherein R represents an alkyl or alkenyl group, R and R each independently represents a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or R and R may be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represents a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to pharmaceutical compositions containing them. These compounds have inhibitory activity against IL-1 beta production, high water solubility and good oral absorbability.

公开(公告)号：DE69840755D1

公开(公告)日：2009-05-28

申请号：DE69840755

申请日：1998-11-09

Applicant: KOWA CO

Inventor： OHKUCHI MASAO ,  KYOTANI YOSHINORI ,  SHIGYO HIROMICHI ,  KOSHI TOMOYUKI ,  KITAMURA TAKAHIRO ,  OHGIYA TADAAKI ,  MATSUDA TAKAYUKI ,  YAMAZAKI YUKIYOSHI ,  KUMAI NATSUYO ,  KOTAKI KYOKO ,  YOSHIZAKI HIDEO ,  HABATA YURIKO

IPC: C07D237/04 ,  A61K31/50 ,  A61K31/501 ,  A61P19/02 ,  A61P19/10 ,  A61P29/00 ,  A61P37/00 ,  C07D213/00 ,  C07D237/00 ,  C07D237/14 ,  C07D237/18 ,  C07D401/04 ,  C07D401/06

Abstract: A pyridazine derivative represented by the following formula (1): wherein R 1 represents a phenyl or pyridyl group which may be substituted by 1 to 3 substituents selected from a halogen atom and a C 1-6 alkoxyl group, R 2 represents a phenyl group substituted at least at 4-position by a C 1-6 alkoxyl group, C 1-6 alkylthio group, a C 1-6 alkylsulfinyl group, or a C 1-6 alkylsulfonyl group, and optionally has one or more substituents at the other position by 1 or 2 substituents selected from a halogen atom, a C 1-6 alkoxyl group, C 1-6 alkylthio group, a C 1-6 alkylsulfinyl group, or a C 1-6 alkylsulfonyl group, R 3 represents a C 1-6 alkoxyl group, a fluorinated C 1-6 alkyl group, C 1-6 alkyl group or a C 3-8 cycloalkyl group, A represents a single bond or linear or branched C 1-6 alkylene group or C 2-9 alkenylene group, X represents an oxygen atom or a sulfur atom; or a salt thereof.

公开(公告)号：PT1043317E

公开(公告)日：2009-05-11

申请号：PT98951732

申请日：1998-11-09

Applicant: KOWA CO

Inventor： OHKUCHI MASAO ,  KYOTANI YOSHINORI ,  YOSHIZAKI HIDEO ,  KOSHI TOMOYUKI ,  KITAMURA TAKAHIRO ,  MATSUDA TAKAYUKI ,  SHIGYO HIROMICHI ,  OHGIYA TADAAKI ,  YAMAZAKI YUKIYOSHI ,  KUMAI NATSUYO ,  KOTAKI KYOKO ,  HABATA YURIKO

IPC: C07D237/04 ,  A61K31/50 ,  A61K31/501 ,  A61P19/02 ,  A61P19/10 ,  A61P29/00 ,  A61P37/00 ,  C07D213/00 ,  C07D237/00 ,  C07D237/14 ,  C07D237/18 ,  C07D401/04 ,  C07D401/06

公开(公告)号：AT418532T

公开(公告)日：2009-01-15

申请号：AT04734380

申请日：2004-05-21

Applicant: KOWA CO

Inventor： INOUE KEISUKE ,  TOMA TSUTOMU ,  KITAMURA TAKAHIRO ,  YAMAZAKI YUKIYOSHI ,  ISHIKAWA TETSUYA

IPC: C07C59/56 ,  A61K31/20 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P29/00 ,  C07C59/40 ,  C07C59/88 ,  C07C69/732 ,  C07C69/738

Abstract: A compound represented by the following general formula (1), a salt thereof, or an ester thereof: wherein m represents an integer of 0 to 4, n represents an integer of 5 to 9, and W represents -CH(OR)- (wherein R represents hydrogen atom or a protective group of hydroxyl group) or -C(=O)-, which has reducing actions of blood glucose, plasma insulin, and triglyceride, and is useful for preventive and/or therapeutic treatment of diabetes, complications of diabetes, hyperlipemia and others.