公开(公告)号：EP3219319A1

公开(公告)日：2017-09-20

申请号：EP17169940.8

申请日：2007-06-22

申请人： Nippon Chemiphar Co., Ltd.

发明人： HIRANO, Masuharu ,  YAMAKAWA, Tomio ,  ISHIKAWA, Toshihisa

IPC分类号： A61K31/519 ,  A61K31/426 ,  A61K31/444 ,  A61K31/4745 ,  A61P35/00 ,  C07D277/20 ,  C07D277/56 ,  C07D401/14 ,  C07D487/04 ,  C07D513/04

CPC分类号： C07D513/04 ,  A61K31/426 ,  A61K31/444 ,  A61K31/4745 ,  A61K31/519 ,  A61K45/06 ,  C07D277/20 ,  C07D277/56 ,  C07D401/14 ,  C07D487/04

摘要： An agent comprising, as an active ingredient, a xanthine oxidase inhibitor such as 2-[3-cyano-4-(4-fluorophenoxy)phenyl]-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-[3-cyano-4-(4-fluorophenoxy)phenyl]thiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-(3-cyano-4-phenoxyphenyl)thiazolo[5,4-d]pyrimidine, TMX-67, and FYX-051, which can be used as an agent for overcoming anti-cancer agent resistance.

摘要翻译： 含有黄嘌呤氧化酶抑制剂如2- [3-氰基-4-（4-氟苯氧基）苯基] -4-羟基噻唑并[5,4-d]嘧啶钾盐，2- [3 （4-氟苯氧基）苯基]噻唑并[5,4-d]嘧啶，2-（3-氰基-4-苯氧基苯基）-4-羟基噻唑并[5,4-d]嘧啶，2- （3-氰基-4-苯氧基苯基）噻唑并[5,4-d]嘧啶，TMX-67和FYX- 051，它可以用作克服抗癌剂抗性的药物。

公开(公告)号：EP1424330B1

公开(公告)日：2011-09-28

申请号：EP02755779.2

申请日：2002-08-02

申请人： NIPPON CHEMIPHAR CO., LTD.

发明人： SAKUMA, Shogo ,  YAMAKAWA, Tomio ,  KANDA, Takashi ,  MASUI, Seiichiro

IPC分类号： C07D263/32 ,  C07D277/24 ,  C07D277/26 ,  C07D233/54 ,  A61K31/421 ,  A61K31/426 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/14 ,  A61P9/00 ,  A61P9/10 ,  A61P19/10 ,  A61P21/04 ,  A61P25/28 ,  A61P31/00 ,  A61P35/00 ,  A61P43/00

CPC分类号： C07D263/62 ,  C07D263/32 ,  C07D277/24

摘要： A compound represented by the following general formula (I): (I) (wherein R1 represents optionally substituted phenyl, etc.; R2 represents C1-8 alkyl, etc.; A represents oxygen, etc.; X represents a C1-8 alkylene chain, etc.; Y represents C(=O), etc.; R3, R4, and R5 each represents hydrogen, C1-8 alkyl, etc.; B represents CH, etc.; Z represents oxygen or sulfur; R6 and R7 each represents hydrogen, etc.; and R8 represents hydrogen, etc.; provided that at least one of R3, R4, and R5 is not hydrogen) or a salt of the compound; and a PPAR-δ activator which contains the compound or salt as the active ingredient.

公开(公告)号：EP2036561A1

公开(公告)日：2009-03-18

申请号：EP07767849.8

申请日：2007-06-22

申请人： Nippon Chemiphar Co., Ltd.

发明人： HIRANO, Masuharu ,  YAMAKAWA, Tomio ,  ISHIKAWA, Toshihisa ,  SAITO, Hikaru

IPC分类号： A61K31/519 ,  A61K31/426 ,  A61K31/444 ,  A61K31/4745 ,  A61K45/00 ,  A61P19/06 ,  A61P35/00 ,  A61P43/00 ,  C07D277/20 ,  C07D277/56 ,  C07D401/14 ,  C07D487/04 ,  C07D513/04

CPC分类号： C07D513/04 ,  A61K31/426 ,  A61K31/444 ,  A61K31/4745 ,  A61K31/519 ,  A61K45/06 ,  C07D277/20 ,  C07D277/56 ,  C07D401/14 ,  C07D487/04

摘要： An agent comprising, as an active ingredient, a xanthine oxidase inhibitor such as 2-[3-cyano-4-(4-fluorophenoxy)phenyl]-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-[3-cyano-4-(4-fluorophenoxy)phenyl]thiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-(3-cyano-4-phenoxyphenyl)thiazolo[5,4-d]pyrimidine, TMX-67, and FYX-051, which can be used as an agent for overcoming anti-cancer agent resistance.

公开(公告)号：EP1310494A1

公开(公告)日：2003-05-14

申请号：EP01955606.7

申请日：2001-08-09

申请人： NIPPON CHEMIPHAR CO., LTD.

发明人： SAKUMA, Shogo ,  ENDO, Tsuyoshi ,  TENDO, Atsushi ,  TAKAHASHI, Toshihiro ,  YOSHIDA, Shinichi ,  KOBAYASHI, Kunio ,  MOCHIZUKI, Nobutaka ,  YAMAKAWA, Tomio ,  KANDA, Takashi ,  MASUI, Seiichiro

IPC分类号： C07D263/32 ,  C07D277/24 ,  C07D413/04 ,  C07D263/48 ,  C07D263/34 ,  C07D277/28 ,  C07D417/04 ,  C07D233/64 ,  C07D233/70 ,  C07D233/88 ,  C07D233/90 ,  A61K31/421 ,  A61K31/4439 ,  A61K31/426 ,  A61K31/4164 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/422 ,  A61K31/427

CPC分类号： C07D413/04 ,  C07D263/32 ,  C07D277/24

摘要： Compounds of the general formula (I) or salts thereof and activators of PPARδ (peroxisome proliferator activated receptor δ) containing the compounds or the salts as the active ingredient: wherein R 1 and R 2 each are hydrogen, C 1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X 1 and X 2 are each a free valency, oxygen, S(O) p (wherein p is an integer of 0 to 2), C(=O), C(=O)NH, NHC(=O), CH=CH, or the like; Y is optionally substituted C 1-8 alkylene; Z is oxygen or sulfur; R 3 and R 4 are each optionally substituted C 1-8 alkyl; and R 8 is hydrogen or C 1-8 alkyl, with the proviso that when X 1 is a free valency, X 2 is not O or S(O) p , while when X 1 is C(=O)NH, X 2 is not a free valency.

摘要翻译： 通式（I）化合物或其盐和含有化合物或其盐作为活性成分的PPARδ（过氧化物酶体增殖物激活受体δ）的活化剂：其中R 1和R 2各自为氢，C1- 8烷基，可被取代的芳基或杂环基等; A是氧，硫等; X 1和X 2各自为自由价，氧，S（O）p（其中p为0至2的整数），C（= O），C（= O）NH，NHC O），CH = CH等; Y为任选取代的C 1-8亚烷基; Z是氧或硫; R 3和R 4各自为任选取代的C 1-8烷基; 并且R 8是氢或C 1-8烷基，条件是当X 1是自由价时，X 2不是O或S（O）p，而当X 1是C（O） = O）NH，X 2不是自由价。

公开(公告)号：EP2014652B1

公开(公告)日：2014-08-06

申请号：EP07742334.1

申请日：2007-04-18

申请人： Nippon Chemiphar Co., Ltd.

发明人： SAKUMA, Shogo ,  MOCHIDUKI, Nobutaka ,  USHIODA, Masatoshi ,  TAKAHASHI, Rie ,  YAMAKAWA, Tomio ,  MASUI, Seiichiro

IPC分类号： C07D263/32 ,  A61K31/381 ,  A61K31/421 ,  A61K31/426 ,  A61P1/04 ,  A61P1/12 ,  A61P1/16 ,  A61P1/18 ,  A61P3/06 ,  A61P3/10 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P17/00 ,  A61P17/06 ,  A61P17/10 ,  A61P17/14

CPC分类号： C07D277/22 ,  C07D263/32 ,  C07D277/20 ,  C07D277/30 ,  C07D333/22

公开(公告)号：EP1445258B1

公开(公告)日：2009-06-24

申请号：EP02801515.4

申请日：2002-10-09

申请人： NIPPON CHEMIPHAR CO., LTD.

发明人： SAKUMA, Shogo ,  YAMAKAWA, Tomio ,  KANDA, Takashi ,  MASUI, Seiichiro

IPC分类号： C07D413/06 ,  C07D417/06 ,  A61K31/423 ,  A61K31/427 ,  A61K31/454 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P19/10 ,  C07D413/12 ,  C07D417/12

CPC分类号： C07D403/06 ,  A61K31/00 ,  A61K31/423 ,  A61K31/427 ,  A61K31/454 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： A compound represented by the general formula (I): (I) (wherein A represents oxygen, sulfur, etc.; B1 represents nitrogen, etc.; B2 represents oxygen, etc.; X1 and X2 each represents oxygen, sulfur, a bond, etc.; Y represents a C1-8 alkylene chain; Z represents oxygen or sulfur; R1 represents optionally substituted aryl, etc.; R2 represents C2-8 alkyl, etc.; R3 represents C1-8 alkyl, C2-8 alkenyl, etc.; R4 and R5 each represents hydrogen, C1-8 alkyl, etc.; and R6 represents hydrogen, etc.; provided that Z and R3 are bonded to the benzene ring and X2 is not bonded to the benzene ring) or a salt of the compound; and a PPARδ activator containing the compound or salt as an active ingredient.

公开(公告)号：EP1897872A1

公开(公告)日：2008-03-12

申请号：EP06756770.1

申请日：2006-05-24

申请人： Nippon Chemiphar Co., Ltd.

发明人： SAKUMA, Shogo ,  MOCHIDUKI, Nobutaka ,  TAKAHASHI, Rie ,  HIRAI, Toshitake ,  YAMAKAWA, Tomio ,  MASUI, Seiichiro

IPC分类号： C07D277/28 ,  A61K31/496 ,  A61P3/06 ,  A61P43/00

CPC分类号： C07D277/28

摘要： A compound having the following formula or its salt is used as an activator for PPAR:

[in which W 2 represents a bond, C(C=O) or CH 2 ; Z 2 represents an oxygen or sulfur atom; R 21 , R 22 and R 23 independently represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, a halogen atom, an alkyl group having 1 to 8 carbon atoms which is substituted with a halogen atom or the like; and R 24 and R 25 independently represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms or an alkyl group having 1 to 8 carbon atoms which is substituted with a halogen atom].

摘要翻译： 具有下式的化合物或其盐用作PPAR的活化剂：[其中W 2表示键，C（C = O）或CH 2; Z 2表示氧或硫原子; R 21，R 22和R 23独立地表示氢原子，碳原子数1〜8的烷基，碳原子数1〜8的烷氧基，卤素原子，碳原子数1〜8的烷基，被取代的 与卤素原子等; R 24和R 25独立地表示氢原子，碳原子数1〜8的烷基或被卤素原子取代的碳原子数1〜8的烷基。

公开(公告)号：EP1854784A1

公开(公告)日：2007-11-14

申请号：EP06715252.0

申请日：2006-02-28

申请人： Nippon Chemiphar Co., Ltd.

发明人： SAKUMA, Shogo ,  MOCHIDUKI, Nobutaka ,  TAKAHASHI, Rie ,  HIRAI, Toshitake ,  YAMAKAWA, Tomio ,  MASUI, Seiichiro

IPC分类号： C07D207/337 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/415 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P43/00 ,  C07D231/12 ,  C07D307/54 ,  C07D333/24 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04

CPC分类号： C07D231/12 ,  C07D207/325 ,  C07D207/333 ,  C07D231/22 ,  C07D307/42 ,  C07D307/46 ,  C07D333/16 ,  C07D333/22 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04

摘要： A compound or its salt having the following formula (II) is used as an activator for PPAR δ:

[in which each of R 11 and R 13 is a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, an alkyl group having 1 to 8 carbon atoms and a halogen atom substituent, etc.; R 12 is a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, an alkyl group having 1 to 8 carbon atoms and a halogen atom substituent, etc.; each of R 14 and R 15 is a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or an alkyl group having 1 to 8 carbon atoms and a halogen atom substituent; X 1 is CH or N; Z 1 is an oxygen atom or a sulfur atom; W 1 is an oxygen atom or CH 2 ; and q is an integer of 2 to 4].

摘要翻译： 使用具有下式（II）的化合物或其盐作为PPAR'的活化剂：[其中R 11和R 13各自为氢原子，具有1至8个碳原子的烷基，具有 1〜8个碳原子的烷基，碳原子数1〜8的烷基和卤素原子取代基等。 R 12为氢原子，碳原子数1〜8的烷基，碳原子数1〜8的烷氧基，碳原子数1〜8的烷基和卤原子取代基等。 R 14和R 15各自为氢原子，碳原子数1〜8的烷基或碳原子数1〜8的烷基和卤素原子取代基。 X 1为CH或N; Z 1是氧原子或硫原子; W 1是氧原子或CH 2; q为2〜4的整数]。

公开(公告)号：EP1619190A1

公开(公告)日：2006-01-25

申请号：EP04728921.0

申请日：2004-04-22

申请人： NIPPON CHEMIPHAR CO., LTD.

发明人： TENDO, Atsushi ,  TAKAHASHI, Toshihiro ,  YAMAKAWA, Tomio ,  OKAI, Kazuki ,  NIHASHI, Susumu

IPC分类号： C07D303/48

CPC分类号： C07D303/48

摘要： The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics:

DSC: exothermic peak observed at a temperature in the range of 170 to 175°C with weight decrease; and
characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm -1 .

摘要翻译： 本发明涉及（2S，3S）-3 - [[（1S）-1-异丁氧基甲基-3-甲基丁基]氨基甲酰基]环氧乙烷-2-羧酸[以下称为羧酸] 所述羧酸与选自哌嗪，金刚烷胺等的有机胺反应。 本发明还涉及提供羧酸的结晶钠盐。 钠盐可用作制备药物的材料并提高储存稳定性，具有以下特征：DSC：在170至175℃的温度范围内观察到的放热峰，重量减少; 和红外吸收光谱的特征吸收带（KBr片剂）：3255,2950,2860,1670,1630,1550,1460,1435,1395,1365,1310,1260,1110,890cm -1。

公开(公告)号：EP1445258A1

公开(公告)日：2004-08-11

申请号：EP02801515.4

申请日：2002-10-09

申请人： NIPPON CHEMIPHAR CO., LTD.

发明人： SAKUMA, Shogo ,  YAMAKAWA, Tomio ,  KANDA, Takashi ,  MASUI, Seiichiro

IPC分类号： C07D413/06 ,  C07D417/06 ,  A61K31/423 ,  A61K31/427 ,  A61K31/454 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P19/10 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D403/06 ,  A61K31/00 ,  A61K31/423 ,  A61K31/427 ,  A61K31/454 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： A compound represented by the formula (I) or a salt of the compound, and a PPAR-δ activator which contains the compound or salt as the active ingredient:
   (wherein A represents O or S; B 1 represents N, etc.; B 2 represents O, etc.; each of X 1 and X 2 represents O, S, a bond, etc.; Y represents C 1-8 alkylene chain; Z represents O or S; R 1 represents aryl, etc. which can have substituents; R 2 represents C 1-8 alkyl, etc.; R 3 represents C 1-8 alkyl, C 2-8 alkenyl, etc.; each of R 4 and R 5 represents hydrogen, C 1-8 alkyl, etc.; and R 6 represents hydrogen, etc.; provided that each of Z and R 3 is attached to the benzene ring, and X 2 is not attached to the benzene ring).

摘要翻译： 由式（I）表示的化合物或该化合物的盐和含有该化合物或盐作为活性成分的PPAR-δ活化剂：其中A表示O或S; B 1表示N 等等; B 2表示O等; X 1和X 2各自表示O，S，a等; Y表示C 1-8亚烷基链; Z表示O或S; R 1表示可以具有取代基的芳基等; R 2表示C 1-8烷基等; R 3表示C 1-8烷基，C 2-8链烯基等; R 4 并且R 5表示氢，C 1-8烷基等; R 6表示氢等;条件是Z和R 3各自连接到苯环上，X 2表示氢， 不附着于苯环）。