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1. 发明授权

EP2053054B1 METHOD FOR INTRODUCING NUCLEIC-ACID-PROTECTING GROUP 有权转让
标题翻译：建立方法核酸保护组
公开(公告)号：EP2053054B1
公开(公告)日：2014-12-17
申请号：EP07791750.8
申请日：2007-08-01
申请人： Nippon Shinyaku Co., Ltd.
发明人： KITAGAWA, Hidetoshi , UETAKE, Kouichi
IPC分类号： C07H19/06
CPC分类号： C07H19/06 , C07H19/167 , Y02P20/55

2. 发明公开

EP2053054A4 METHOD FOR INTRODUCING NUCLEIC-ACID-PROTECTING GROUP 有权转让
标题翻译：建立方法核酸保护组
公开(公告)号：EP2053054A4
公开(公告)日：2013-11-06
申请号：EP07791750
申请日：2007-08-01
申请人： NIPPON SHINYAKU CO LTD
发明人： KITAGAWA HIDETOSHI , UETAKE KOUICHI
IPC分类号： C07H19/06
CPC分类号： C07H19/06 , C07H19/167 , Y02P20/55

3. 发明公开

EP2292231A1 THERAPEUTIC AGENT FOR SPINAL CANAL STENOSIS 有权转让
标题翻译： HEILMITTEL ZUR BEHANDLUNG VON螺丝刀STENOSE
公开(公告)号：EP2292231A1
公开(公告)日：2011-03-09
申请号：EP09770106.4
申请日：2009-06-22
申请人： Nippon Shinyaku Co., Ltd.
发明人： KUWANO, Keiichi
IPC分类号： A61K31/4965 , A61P25/00 , C07D241/20
CPC分类号： C07D241/20 , A61K31/4965
摘要： The main object of the present invention is to provide a novel agent for the treatment of spinal canal stenosis.
The present invention relates to an agent for the treatment of spinal canal stenosis containing the heterocyclic derivative represented by the following general formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient;

In the formula (1),
R 1 and R 2 are the same or different and each represents an optionally substituted aryl;
R 3 and R 4 are the same or different and each represents hydrogen atom or alkyl;
R 5 represents hydrogen atom, alkyl or halogen atom;
Y represents N or N→O;
A represents NR 6 , and R 6 represents hydrogen atom, alkyl, etc.;
D represents alkylene or alkenylene which is optionally substituted with hydroxy;
E represents phenylene or a single bond;
G represents O, S, etc.; and
Q represents carboxy, alkoxycarbonyl, etc.
摘要翻译：本发明的主要目的是提供一种用于治疗椎管狭窄的新型药剂。本发明涉及用于治疗含有由以下通式（1）表示的杂环衍生物或其药学上可接受的盐作为活性成分的椎管狭窄的药剂; 在式（1）中，R 1和R 2相同或不同，各自表示任选取代的芳基; R 3和R 4相同或不同，各自表示氢原子或烷基; R 5表示氢原子，烷基或卤素原子; Y表示N或N≠O; A表示NR 6，R 6表示氢原子，烷基等; D表示任选被羟基取代的亚烷基或亚烯基; E表示亚苯基或单键; G代表O，S等; Q表示羧基，烷氧基羰基等。

4. 发明公开

EP1400518A4 HETEROCYCLIC COMPOUND DERIVATIVES AND MEDICINES 有权转让
标题翻译：来自ARZNEIMITTEL的DERIVATE HETEROCYCLISCHER VERBINDUNGEN
公开(公告)号：EP1400518A4
公开(公告)日：2005-04-20
申请号：EP02722772
申请日：2002-04-25
申请人： NIPPON SHINYAKU CO LTD
发明人： ASAKI TETSUO , HAMAMOTO TAISUKE , KUWANO KEIICHI
IPC分类号： A61K31/4418 , A61K31/4965 , A61K31/497 , A61K31/505 , A61K31/53 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/06 , A61P11/08 , A61P13/12 , A61P17/02 , A61P37/02 , A61P37/08 , A61P43/00 , C07D213/74 , C07D239/42 , C07D241/12 , C07D241/18 , C07D241/20 , C07D253/07 , C07D401/04 , C07D403/04 , C07D409/12 , C07D253/06 , C07D239/34 , C07D239/38
CPC分类号： C07D409/12 , A61K31/4418 , A61K31/4965 , A61K31/497 , A61K31/505 , A61K31/53 , C07D213/74 , C07D239/42 , C07D241/12 , C07D241/18 , C07D241/20 , C07D253/07 , C07D401/04 , C07D403/04
摘要： The invention provides compounds useful as PGI2 receptor agonist and pharmaceutical compositions, particularly pharmaceutical compositions containing as the active ingredient compounds represented by the general formula (1) or pharmaceutically acceptable salts thereof: (1) wherein R1 and R2 are each independently optionally substituted aryl; Y is N, CH, or the like; Z is N, CH, or the like; A is NH, NR5, O, S, ethylene, or the like; R5 is alkyl or the like; D is alkylene or alkenylene; E is phenylene or a single bond; G is O, S, CH2, or the like; R3 and R4 are each independently hydrogen or alkyl; and Q is carboxyl, alkoxycarbonyl, tetrazolyl, carbamoyl, N-(alkylsulfonyl)carbamoyl, or the like.
摘要翻译：本发明提供了可用作PGI 2受体激动剂的化合物和药物组合物。本发明涉及包含由下式表示的化合物的药物组合物：＆lt; CHEM＆gt;（R 1和R 2相同或不同，各自表示任意取代的芳基，Y表示 N或CH，Z表示N或CH，A表示NH，NR 5，O，S或亚乙基，R 5表示烷基，D表示亚烷基或亚烯基，E表示亚苯基或单键，G表示O， S或CH 2，R 3和R 4相同或不同，各自表示氢或烷基，Q表示羧基，烷氧基羰基，四唑基，氨基甲酰基或N-（烷基磺酰基）氨基甲酰基）或其药学上可接受的盐作为活性成分。

5. 发明授权

EP1944298B1 QUINAZOLINE DERIVATIVE AND PHARMACEUTICAL 有权转让
标题翻译：喹唑啉衍生物和制药
公开(公告)号：EP1944298B1
公开(公告)日：2013-01-09
申请号：EP06811143.4
申请日：2006-10-03
申请人： Nippon Shinyaku Co., Ltd.
发明人： OKANO, Masahiko , OYAMA, Tatsuya
IPC分类号： C07D239/94 , A61K31/517 , A61P1/16 , A61P3/00 , A61P3/10 , A61P5/00 , A61P5/16 , A61P7/00 , A61P13/12 , A61P17/04 , A61P25/00 , A61P25/08 , A61P25/18
CPC分类号： C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14

6. 发明公开

EP2394999A4 AMINOPYRAZINE DERIVATIVE AND MEDICINE 有权转让
标题翻译：氨基嘧啶衍生物与医药
公开(公告)号：EP2394999A4
公开(公告)日：2012-10-10
申请号：EP10738621
申请日：2010-02-05
申请人： NIPPON SHINYAKU CO LTD
发明人： FUJIHARA HIDETAKA , ASAKI TETSUO , HORI KATSUTOSHI , NAITO HARUNA
IPC分类号： C07D401/14 , A61K31/497 , A61K31/506 , A61P7/00 , A61P35/02 , C07D403/12 , C07D403/14 , C07D413/14
CPC分类号： C07D401/14 , A61K31/497 , A61K31/506 , C07C57/145 , C07D403/12 , C07D403/14 , C07D413/14

7. 发明公开

EP1944298A4 QUINAZOLINE DERIVATIVE AND PHARMACEUTICAL 有权转让
标题翻译：喹唑啉衍生物和制药
公开(公告)号：EP1944298A4
公开(公告)日：2010-06-30
申请号：EP06811143
申请日：2006-10-03
申请人： NIPPON SHINYAKU CO LTD
发明人： OKANO MASAHIKO , OYAMA TATSUYA
IPC分类号： C07D239/94 , A61K31/517 , A61P1/16 , A61P3/00 , A61P3/10 , A61P5/00 , A61P5/16 , A61P7/00 , A61P13/12 , A61P17/04 , A61P25/00 , A61P25/08 , A61P25/18
CPC分类号： C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14

8. 发明公开

EP2053054A1 METHOD FOR INTRODUCING NUCLEIC-ACID-PROTECTING GROUP 有权转让
标题翻译： VERFAHREN ZUREINFÜHRUNGEINERNUKLEINSÄURESCHUTZGRUPPE
公开(公告)号：EP2053054A1
公开(公告)日：2009-04-29
申请号：EP07791750.8
申请日：2007-08-01
申请人： Nippon Shinyaku Co., Ltd.
发明人： KITAGAWA, Hidetoshi , UETAKE, Kouichi
IPC分类号： C07H19/06
CPC分类号： C07H19/06 , C07H19/167 , Y02P20/55
摘要： It is an object of the invention to provide a simple and economical method for introducing the following substituent (I) at the 2'-hydroxyl group of the ribose of a ribonucleic acid derivative whose 3'-hydroxyl group and 5'-hydroxyl group are protected with a silicon protecting group:

[in formula (I), WG 1 represents an electron-withdrawing group] and to provide a method for producing a ribonucleic acid derivative represented by the following general formula (3), comprising the reaction of a ribonucleic acid derivative represented by the following general formula (1) with a monothioacetal compound represented by the following general formula (2) to produce the ribonucleic acid derivative represented by the following general formula (3), using iodine as the reagent for halogenating the sulfur atom of the monothioacetal compound (2) in the presence of an acid:

[in formulae (1), (2), and (3), Bz represents a nucleobase which may or may not have a protecting group; WG 1 represents an electron-withdrawing group; R 3 represents alkyl or aryl; and A represents a silicon substituent].
摘要翻译：本发明的目的是提供一种在3'-羟基和5'-羟基为核苷酸的核糖核酸衍生物的核糖的2'-羟基上引入下述取代基（I）的简单和经济的方法用硅保护基保护：[在式（I）中，WG 1表示吸电子基团]，并提供由以下通式（3）表示的核糖核酸衍生物的制备方法，其包括核糖核酸由下述通式（1）表示的酸衍生物与下述通式（2）表示的一硫代缩醛化合物反应，制造下述通式（3）所示的核糖核酸衍生物，使用碘作为卤素化反应试剂的一硫代缩醛化合物（2）在酸存在下：[在式（1），（2）和（3）中，Bz表示可以具有或不具有保护基团的核碱基; WG 1表示吸电子基团; R 3表示烷基或芳基; A表示硅取代基]。

9. 发明公开

EP1944298A1 QUINAZOLINE DERIVATIVE AND PHARMACEUTICAL 有权转让
标题翻译： CHINAZOLINDERIVAT UND PHARMAZEUTIKUM
公开(公告)号：EP1944298A1
公开(公告)日：2008-07-16
申请号：EP06811143.4
申请日：2006-10-03
申请人： Nippon Shinyaku Co., Ltd.
发明人： OKANO, Masahiko , OYAMA, Tatsuya
IPC分类号： C07D239/94 , A61K31/517 , A61P1/16 , A61P3/00 , A61P3/10 , A61P5/00 , A61P5/16 , A61P7/00 , A61P13/12 , A61P17/04 , A61P25/00 , A61P25/08 , A61P25/18
CPC分类号： C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14
摘要： It is intended to provide a novel quinazoline derivative with less skin irritation and an excellent action of strongly suppressing scratching behavior and a pharmaceutical composition containing the quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivative represented by the general formula [1] or a pharmaceutically acceptable salt thereof. In the general formula [1], R 1 represents hydrogen or the like, R 2 represents hydrogen or the like, R 3 and R 4 are the same or different and represent hydrogen, alkyl, alkoxy or halogen, R 5 is combined with R 6 to represent alkylene or represents hydrogen, hydroxy, alkyl, phenyl or alkoxy, R 6 represents (1) alkyl, (2) cycloalkyl, (3) phenyl, (4) a 5- to 10-membered aromatic heterocyclic group containing one to three heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or (5) -N(R 61 ) (R 62 ).
摘要翻译：本发明提供一种新颖的喹唑啉衍生物，其具有较少的皮肤刺激性和强烈抑制刮擦行为的优异作用，以及含有喹唑啉衍生物作为活性成分的药物组合物。本发明涉及由通式[1]表示的喹唑啉衍生物或其药学上可接受的盐。在通式[1]中，R 1表示氢等，R 2表示氢等，R 3和R 4相同或不同，表示氢，烷基，烷氧基或卤素，R 5与R 6表示亚烷基或代表氢，羟基，烷基，苯基或烷氧基，R 6表示（1）烷基，（2）环烷基，（3）苯基，（4）5至10元芳族杂环基，三个选自氮原子，氧原子和硫原子的杂原子，或（5）-N（R 61）（R 62）。

10. 发明公开

EP1626051A1 CRYSTALS OF QUINOLINECARBOXYLIC ACID DERIVATIVE SOLVATE 有权转让
标题翻译：喹啉羧酸衍生物溶剂的晶体
公开(公告)号：EP1626051A1
公开(公告)日：2006-02-15
申请号：EP04730102.3
申请日：2004-04-28
申请人： Nippon Shinyaku Co., Ltd.
发明人： AKAI, Jun , NISHIDA, Hiroshi, 2-9-9-304, Oharano
IPC分类号： C07D513/04 , B01D9/02 , A61K31/496 , A61P31/04
CPC分类号： C07D513/04
摘要： A main object is to provide a crystal of 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)-methyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid acetonitrile solvate (Compound B) which is an intermediate for producing preferentially the type III crystal of 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl-1-piperazinyl]-4-oxo-4H-[1,3]-thiazeto[3,2-a]quinoline-3-carboxylic acid (Compound A).
A crystal of Compound B can be preferentially precipitated by controlling the supersaturation concentration in crystalization using acetonitrile as a solvent. Subsequently, the type III crystal of CompoundA can be produced by performing desolvation of the crystal.
摘要翻译：主要目的是提供6-氟-1-甲基-7- [4-（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基） - 甲基-1-哌嗪基] -4 - 氧代-4H- [1,3]硫氮杂[3,2-a]喹啉-3-羧酸乙腈溶剂化物（化合物B），其是用于优先生产6-氟-1-甲基-1- 7- [4-（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基）甲基-1-哌嗪基] -4-氧代-4H- [1,3] -thiazeto并〔3,2- ]喹啉-3-羧酸（化合物A）。化合物B的晶体可以通过使用乙腈作为溶剂控制结晶中的过饱和浓度而优先沉淀。随后，化合物A的III型晶体可以通过进行晶体的去溶剂化来制备。

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