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1. 发明公开

EP1637532A1 FUSED PYRIMIDINE DERIVATIVE 审中-公开
标题翻译： KONDENSIERTES PYRIMIDINDERIVAT
公开(公告)号：EP1637532A1
公开(公告)日：2006-03-22
申请号：EP04729197.6
申请日：2004-04-23
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： NAKAJIMA, Takao , UENO, Kimihisa , NOMOTO, Yuji , MATSUMOTO, Yuichi , YANO, Hiroshi , NAKANISHI, Satoshi , TAKASAKI, Kotaro , KUSAKA, Hideaki
IPC分类号： C07D487/14 , A61K31/519 , A61P3/10 , A61P9/10 , A61P13/12 , A61P25/00 , A61P27/02
CPC分类号： C07D487/14
摘要： The present invention provides a fused pyrimidine derivative having an insulin secretion stimulating activity represented by Formula (I):

{wherein R 1 represents a hydrogen atom, lower alkyl, or the like; n represents an integer of 0 to 3; and X 1 and X 2 may be the same or different and each represents a hydrogen atom, lower alkyl, or the like; and formula (II):

represents formula (III):

[wherein X--Y--Z represents R 2 C=CR 3 -NR 4 (wherein R 2 , R 3 and R 4 may be the same or different and each represents a hydrogen atom, lower alkyl, or the like)]}, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有由式（I）表示的胰岛素分泌刺激活性的稠合嘧啶衍生物：其中R 1表示氢原子，低级烷基等; n表示0〜3的整数， X 1和X 2可以相同或不同，各自表示氢原子，低级烷基等; 和式（II）表示式（III）：[其中X-Y-Z表示R 2 C = CR 3 -NR 4（其中R 2，R 3和R 4可以相同或不同，氢原子，低级烷基等）]}或其药学上可接受的盐。

2. 发明公开

EP1908755A1 THERAPEUTIC AGENT FOR RESTENOSIS 审中-公开
标题翻译：治疗MITTEL GEGEN RESTENOSE
公开(公告)号：EP1908755A1
公开(公告)日：2008-04-09
申请号：EP06767189.1
申请日：2006-06-22
申请人： KYOWA HAKKO KOGYO CO., LTD. , Fujifilm Corporation
发明人： NAKAI, Ryuichiro , SHIMOIKE, Emi , KUSAKA, Hideaki , MURAKATA, Chikara , YAMASHITA, Yoshinori
IPC分类号： C07D285/135 , A61K31/433 , A61P9/00 , C07D285/12
CPC分类号： A61K31/433 , C07D285/12 , C07D285/135 , C07D417/12 , C07D491/10
摘要： A therapeutic and/or prophylactic agent for restenosis, which comprises a thiadiazoline derivative represented by the general formula (0), or a pharmaceutically acceptable salt thereof:

[wherein, n represents an integer of 1 to 3, R 0 represents aryl, -NR 1 CONR 2 (wherein R 1 represents a hydrogen atom or the like, and R 2 represents lower alkyl or the like) or the like, R 3 represents lower alkyl, R 4 represents a hydrogen atom or the like, and R 5 represents aryl or the like].
摘要翻译：用于再狭窄的治疗和/或预防剂，其包含由通式（0）表示的噻二唑啉衍生物或其药学上可接受的盐：[其中，n表示1〜3的整数，R 0表示芳基，-NR 1 CONR 2（其中R 1表示氢原子等，R 2表示低级烷基等）等，R 3表示低级烷基，R 4表示氢原子等，R 5表示芳基等等]。

3. 发明公开

EP1092435A1 REMEDIES FOR DIABETES 有权
标题翻译：抗炎药物MEDIKAMENTE
公开(公告)号：EP1092435A1
公开(公告)日：2001-04-18
申请号：EP99926903.8
申请日：1999-07-02
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： SHIMADA, Junichi , OHTA, Yoshihisa , TAKASAKI, Kotaro , SUDA, Miho , KUSAKA, Hideaki , YANO, Hiroshi , NAKANISHI, Satoshi , MATSUDA, Yuzuru
IPC分类号： A61K31/505
CPC分类号： C07D487/14 , A61K31/505 , A61K31/519 , Y10S514/866
摘要： A medicament for the therapeutic treatment of diabetes which comprises as an active ingredient a compound represented by the general formula (I):
wherein R 1 represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, R 2 represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, R 3 represents a hydrogen atom, a lower alkyl group or a substituted or unsubstituted aralkyl group, X 1 and X 2 independently represent a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and the symbol "n" represents an integer of from 0 to 3, or a physiologically acceptable salt thereof.
摘要翻译：一种用于治疗糖尿病的药物，其包含作为活性成分的由通式（I）表示的化合物：其中R 1表示氢原子，低级烷基，取代或未取代的芳基，或取代或未取代的芳族杂环基，R 2表示氢原子，低级烷基，取代或未取代的芳烷基，取代或未取代的芳基或取代或未取代的芳族杂环基，R 3，表示氢原子，低级烷基或取代或未取代的芳烷基，X 1和X 2独立地表示氢原子，低级烷基，取代或未取代的芳烷基或取代或未取代的芳基组，符号“n”表示0〜3的整数，或其生理上可接受的盐。

4. 发明授权

EP1092435B1 REMEDIES FOR DIABETES 有权
标题翻译：抗糖尿病药物
公开(公告)号：EP1092435B1
公开(公告)日：2007-04-04
申请号：EP99926903.8
申请日：1999-07-02
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： SHIMADA, Junichi , OHTA, Yoshihisa , TAKASAKI, Kotaro , SUDA, Miho , KUSAKA, Hideaki , YANO, Hiroshi , NAKANISHI, Satoshi , MATSUDA, Yuzuru
IPC分类号： A61K31/505 , A61K31/519 , C07D487/14
CPC分类号： C07D487/14 , A61K31/505 , A61K31/519 , Y10S514/866
摘要： Remedies for diabetes which contain as the active ingredient compounds represented by general formula (I) or physiologically acceptable salts thereof wherein R1 represents hydrogen, lower alkyl, optionally substituted aryl or optionally substituted heteroaryl; R2 represents hydrogen, lower alkyl, optionally substituted aralkyl, optionally substituted aryl or optionally substituted heteroaryl; R3 represents hydrogen, lower alkyl or optionally substituted aralkyl; X?1 and X2¿ independently represent each hydrogen, lower alkyl, optionally substituted aralkyl or optionally substituted aryl; and n is an integer of from 0 to 3.

5. 发明公开

EP0711772A1 PROCESS FOR PRODUCING XANTHINE DERIVATIVE 失效
标题翻译：生产黄嘌呤衍生物的方法
公开(公告)号：EP0711772A1
公开(公告)日：1996-05-15
申请号：EP95918190.0
申请日：1995-05-16
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： SHIMADA, Junichi , EGUCHI, Tamotsu , MOCHIDA, Kenichi , HORIGUCHI, Akira , YASUZAWA, Tohru , KUSAKA, Hideaki , NONAKA, Hiromi , SUZUKI, Fumio
IPC分类号： C07D473/04 , C12P17/18
CPC分类号： C07D473/04 , C07D473/06 , C12P17/18
摘要： The present invention relates to a process for producing a xanthine derivative represented by formula (II), comprising converting a xanthine derivative represented by formula (I) {hereinafter, referred to as Compound (I)}:

(wherein R¹ and R² independently represent hydrogen, or hydroxy-substituted, oxo-substituted, or unsubstituted lower alkyl) into a xanthine derivative represented by formula (II) {hereinafter, referred to as Compound (II)}:

(wherein R³ and R⁴ independently represent hydrogen, or hydroxy-substituted, oxo-substituted, or unsubstituted lower alkyl; R⁵ and R⁶ independently represent hydrogen, hydroxy, or oxo; with the proviso that R⁵ and R⁶ are both hydrogen, at least one of R³ and R⁴ is hydroxy-substituted or oxo-substituted lower alkyl; and X and Y both represent hydrogen or are combined with each other to form a single bond) in the presence of an enzyme source for catalyzing hydroxylation or carbonylation of Compound (I) into Compound (II), and collecting the produced Compound (II).
摘要翻译：（I）表示的黄嘌呤衍生物{以下称为化合物（I）}：（式中，R 1和R 2分别独立地表示氢原子（II）所示的黄嘌呤衍生物{以下称为化合物（II）} :(其中R 3和R 4分别独立地表示氢或羟基取代的，氧代 - 取代的或未取代的低级烷基），氧代 - 取代的或未取代的低级烷基; R 5和R 6独立地代表氢，羟基或氧代;条件是R 5和R 7都是氢，R 3和R 4中至少一个是羟基取代的或氧代 - 取代的低级烷基 ;并且X和Y均代表氢或彼此结合形成单键）在催化化合物（I）羟化或羰基化成化合物（II）的酶源存在下，并收集生成的化合物（II）。

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