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公开(公告)号:US20090018331A1
公开(公告)日:2009-01-15
申请号:US12199982
申请日:2008-08-28
申请人: Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
发明人: Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
IPC分类号: C07D498/14 , C07D473/04 , C07D487/04
CPC分类号: C07D473/30 , C07D471/04 , C07D473/04 , C07D473/06 , C07D473/18 , C07D473/36 , C07D473/40 , C07D487/04 , C07D491/14
摘要: The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.
摘要翻译: 本发明涉及由下式表示的化合物或其盐或水合物,其中,T1表示在环中含有一个或两个氮原子的4至12元杂环基,其为单环或双环结构,其可以是 具有一个或多个取代基; X表示可以具有一个或多个取代基的C 1-6烷基; Z 1和Z 2各自独立地表示氮原子或由式-CR 2表示的基团; R1和R2独立地表示氢原子,可以具有一个或多个取代基的C 1-6烷基或可以具有一个或多个取代基的C 1-6烷氧基等。 这些是表现出优异的DPPIV抑制活性的新型化合物。
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公开(公告)号:US20060063787A1
公开(公告)日:2006-03-23
申请号:US11212407
申请日:2005-08-26
申请人: Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
发明人: Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
IPC分类号: A61K31/522 , C07D473/02 , A61K31/4745 , C07D471/02
CPC分类号: C07D473/30 , C07D471/04 , C07D473/04 , C07D473/06 , C07D473/18 , C07D473/36 , C07D473/40 , C07D487/04 , C07D491/14
摘要: The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.
摘要翻译: 本发明涉及由下式表示的化合物或其盐或水合物
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公开(公告)号:US07772226B2
公开(公告)日:2010-08-10
申请号:US12199982
申请日:2008-08-28
申请人: Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
发明人: Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
IPC分类号: A61K31/437 , A61K31/496 , C07D487/04 , C07D471/04 , C07D473/06 , C07D473/18 , C07D473/22 , C07D473/30 , C07D473/40 , C07D498/14 , A61K31/5025 , A61K31/522
CPC分类号: C07D473/30 , C07D471/04 , C07D473/04 , C07D473/06 , C07D473/18 , C07D473/36 , C07D473/40 , C07D487/04 , C07D491/14
摘要: The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.
摘要翻译: 本发明涉及由下式表示的化合物或其盐或水合物,其中,T1表示在环中含有一个或两个氮原子的4至12元杂环基,其为单环或双环结构,其可以是 具有一个或多个取代基; X表示可以具有一个或多个取代基的C 1-6烷基; Z 1和Z 2各自独立地表示氮原子或由式-CR 2表示的基团; R1和R2独立地表示氢原子,可以具有一个或多个取代基的C 1-6烷基或可以具有一个或多个取代基的C 1-6烷氧基等。 这些是表现出优异的DPPIV抑制活性的新型化合物。
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公开(公告)号:US07074798B2
公开(公告)日:2006-07-11
申请号:US10374918
申请日:2003-02-24
申请人: Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki , Mika Aoki
发明人: Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki , Mika Aoki
IPC分类号: C07D473/06 , C07D473/08 , C07D473/04 , A61K31/522 , A61P3/10
CPC分类号: C07D473/06 , C07D473/08
摘要: The present invention provides novel compounds exhibiting an excellent DPPIV inhibition effect.The compounds are represented by the formula: wherein, m is 0 or 1; n is 0; R31, R32, R33, R34, R35, R36, R37, R38, R39, R40, R41, and R42 each represent a hydrogen atom; X represents an alkynyl group, an aryl group, and such, which group may be substituted; and, R1 and R2 each independently represents a hydrogen atom, an alkyl group, an alkoxyl group, or such, or salts or hydrates thereof.
摘要翻译: 本发明提供具有优异DPPIV抑制作用的新化合物。 化合物由下式表示:其中,m为0或1; n为0; R 32,R 32,R 34,R 34,R 35,R 32, R< 36>,R< 37>,< 38>,R 39,R 40, R 41和R 42各自表示氢原子; X表示可以被取代的炔基,芳基等; R 1和R 2各自独立地表示氢原子,烷基,烷氧基等,或其盐或水合物。
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公开(公告)号:US06884821B1
公开(公告)日:2005-04-26
申请号:US10088916
申请日:2000-09-29
申请人: Masanobu Shinoda , Eita Emori , Fumiyoshi Matsuura , Toshihiko Kaneko , Norihito Ohi , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Sadakazu Miyashita , Taro Hibara , Takashi Seiki , Richard Clark , Hitoshi Harada
发明人: Masanobu Shinoda , Eita Emori , Fumiyoshi Matsuura , Toshihiko Kaneko , Norihito Ohi , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Sadakazu Miyashita , Taro Hibara , Takashi Seiki , Richard Clark , Hitoshi Harada
IPC分类号: C07C59/66 , C07C59/68 , C07C233/51 , C07C233/55 , C07C233/87 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/60 , C07C235/78 , C07C235/84 , C07C255/57 , C07D209/14 , C07D209/42 , C07D213/30 , C07D213/55 , C07D213/56 , C07D213/81 , C07D213/82 , C07D215/04 , C07D217/26 , C07D231/14 , C07D233/90 , C07D239/52 , C07D241/24 , C07D261/18 , C07D263/26 , C07D263/32 , C07D277/20 , C07D277/30 , C07D277/34 , C07D277/56 , C07D307/54 , C07D307/79 , C07D333/24 , C07D401/04 , C07D417/04 , C07D417/12 , C07D417/14 , A61K31/192 , C07C59/64
CPC分类号: C07D213/30 , C07C59/66 , C07C59/68 , C07C233/51 , C07C233/55 , C07C233/87 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/60 , C07C235/78 , C07C235/84 , C07C255/57 , C07C2601/08 , C07C2601/14 , C07D209/14 , C07D209/42 , C07D213/55 , C07D213/56 , C07D213/81 , C07D213/82 , C07D215/04 , C07D217/26 , C07D231/14 , C07D233/90 , C07D239/52 , C07D241/24 , C07D261/18 , C07D263/26 , C07D263/32 , C07D277/20 , C07D277/30 , C07D277/34 , C07D277/56 , C07D307/54 , C07D307/79 , C07D333/24 , C07D401/04 , C07D417/04 , C07D417/12 , C07D417/14
摘要: Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, R1 is hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, —CON(RW1)RW2, or the like; represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.
摘要翻译: 通式(I)的新型羧酸衍生物,它们的盐,它们的酯,或它们的水合物,其可用作胰岛素抵抗性改良剂; 和含有衍生物作为活性成分的药物。 在所述式中,R 1是氢,羟基,烷基等; L是单键,双键,亚烷基等; M是单键,亚烷基等; T是单键,亚烷基等; W是羧基,-CON(R W1),W 2,W 2等; <?img id =“CUSTOM-CHARACTER-00001”he =“2.46mm”wi =“6.01mm”file =“US06884821-20050426-P00900.TIF”alt =“custom character”img-content =“character”img- format =“tif”?>表示单键或双键; X是氧,亚烯基等; Y是可以含有杂原子的芳族烃基等; Z是可以含有杂原子的芳族烃基。
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公开(公告)号:US20050014833A1
公开(公告)日:2005-01-20
申请号:US10486396
申请日:2002-08-16
申请人: Richard Clark , Fumiyoshi Matsuura , Eita Emori , Masanobu Shinoda , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
发明人: Richard Clark , Fumiyoshi Matsuura , Eita Emori , Masanobu Shinoda , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
IPC分类号: A61P1/00 , A61P1/04 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P19/10 , A61P29/00 , A61P35/00 , A61P37/02 , C07C233/87 , C07C251/60 , C07D213/53 , C07D263/32 , C07D277/56 , C07D307/24 , C07D307/30 , C07D317/32 , C07D339/08 , C07D405/06 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07C229/02 , A61K31/195
CPC分类号: C07D213/53 , C07C233/87 , C07C251/60 , C07C2601/02 , C07C2601/14 , C07D263/32 , C07D277/56 , C07D307/24 , C07D307/30 , C07D317/32 , C07D339/08 , C07D405/06 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要: The present invention provides a novel compound having an excellent PPAR agonist action. More specifically, it provides a compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. Wherein a, b and c are the same as or different from one another and each represents 0 to 4; R1 to R6 are the same as or different from one another and each represents a hydrogen atom, a hydroxyl group, a cyano group, a halogen atom, etc.; A1 and A2 are the same as or different from each other and each represents a single bond, an oxygen atom, etc.; L, M and T each represent a single bond, an alkylene group having one to six carbon atoms, etc.; W represents a carboxyl group; the partial structure represented by the formula: represents a single bond or a double bond; X represents a single bond, an oxygen atom, —NRX1CQ1O—, etc.; Y represents Y1—Y2— (wherein Y1 represents a 5 to 14-membered aromatic ring having one to four substituents, etc.; and Y2 represents a single bond or a 5 to 14-membered aromatic ring); and the ring Z represents a 5 to 14-membered aromatic ring which have one to four substituents selected form the above-mentioned Group A, may have one or more hetero atoms and may be partially saturated.
摘要翻译: 本发明提供具有优异的PPAR激动剂作用的新化合物。 更具体地,它提供由下式表示的化合物,其盐,其酯或它们的水合物。 其中a,b和c彼此相同或不同,各自表示0〜4; R 1〜R 6彼此相同或不同,表示氢原子,羟基,氰基,卤素原子等; A 1和A 2彼此相同或不同,各自表示单键,氧原子等; L,M和T各自表示单键,具有1〜6个碳原子的亚烷基等; W表示羧基; 由式表示的部分结构表示单键或双键; X表示单键,氧原子,-NR X 1 C 10 O等; Y表示Y 1 -Y 2 - (其中Y 1表示具有1〜4个取代基的5〜14元芳环等,Y 2表示单键或5〜14个 芳环); 并且环Z表示具有一至四个选自上述A组的取代基的5至14元芳环,可具有一个或多个杂原子并且可部分饱和。
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公开(公告)号:US20110112109A1
公开(公告)日:2011-05-12
申请号:US13006004
申请日:2011-01-13
申请人: Richard CLARK , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
发明人: Richard CLARK , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
IPC分类号: A61K31/501 , A61K31/4196 , A61K31/506 , A61K31/4439 , A61K31/497 , A61K31/427 , A61K31/4245 , A61P7/02
CPC分类号: C07D249/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/04
摘要: A compound represented by the following general formula (1) or salts thereof or hydrates of the foregoing: wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen.
摘要翻译: 由下列通式(1)表示的化合物或其盐或上述的水合物:其中R1a,R1b,R1c和R1d各自独立地表示氢等; R2代表任选取代的苯基等; R3代表任选取代的C6-10芳基等; Z1和Z2各自独立地表示氢。
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公开(公告)号:US20080015199A1
公开(公告)日:2008-01-17
申请号:US11723893
申请日:2007-03-22
申请人: Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
发明人: Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
IPC分类号: A61K31/4196 , A61K31/427 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61P7/02 , A61P9/00 , C07D249/08 , C07D401/04 , C07D403/04 , C07D409/04 , C07D417/04
CPC分类号: C07D249/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/04
摘要: A Compound represented by the following general formula (1), salts thereof or hydrates of the foregoing is a novel compound useful for treatment and/or prevention of diseases associated with thrombus formation, and which is safer with suitable physicochemical stability. [wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen]
摘要翻译: 由以下通式(1)表示的化合物,其盐或其前体的水合物是可用于治疗和/或预防与血栓形成有关的疾病的新型化合物,其具有合适的理化稳定性更安全。 [其中R 1a,R 1b,R 1c和R 1d各自独立地表示氢等。 R 2表示任选取代的苯基等; R 3表示任选取代的C 6-10芳基等; Z 1和Z 2各自独立地表示氢]
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公开(公告)号:US07816522B2
公开(公告)日:2010-10-19
申请号:US11723893
申请日:2007-03-22
申请人: Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
发明人: Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
IPC分类号: A61K31/41 , A61K31/415 , C07D233/00 , C07D249/00
CPC分类号: C07D249/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/04
摘要: A Compound represented by the following general formula (1), salts thereof or hydrates of the foregoing is a novel compound useful for treatment and/or prevention of diseases associated with thrombus formation, and which is safer with suitable physicochemical stability. [wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen]
摘要翻译: 由以下通式(1)表示的化合物,其盐或其前体的水合物是可用于治疗和/或预防与血栓形成有关的疾病的新型化合物,其具有合适的理化稳定性更安全。 [其中R1a,R1b,R1c和R1d各自独立地表示氢等; R2代表任选取代的苯基等; R3代表任选取代的C6-10芳基等; 并且Z 1和Z 2各自独立地表示氢]
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公开(公告)号:US07253178B2
公开(公告)日:2007-08-07
申请号:US10469173
申请日:2002-03-27
申请人: Hitoshi Harada , Masanobu Shinoda , Richard Clark , Fumiyoshi Matsuura , Eita Emori , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
发明人: Hitoshi Harada , Masanobu Shinoda , Richard Clark , Fumiyoshi Matsuura , Eita Emori , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
IPC分类号: A61K31/435 , A61K31/44 , C07D211/72 , C07D211/70
CPC分类号: C07D213/64 , C07D213/79
摘要: The present invention provides a novel carboxylic acid derivative, a salt thereof or a hydrate of them which is useful as an insulin sensitizer, and a medicament comprising the derivative as the effective ingredient. More specifically, it provides a carboxylic acid compound represented by the formula (I), a salt thereof or a hydrate of them. In the formula, Ar represents a 6- to 14-membered aromatic ring group which may have at least one substituent; R1, R2, R3, R4, R5, R6, R7 and R8 are the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1-6 alkyl group or a C1-6 alkoxy group; X represents an oxygen atom or a methylene group; Y represents a group represented by the formula (II) or (III): (wherein Z represents a group represented by the formula (IV): (wherein R9, R10, R11 and R12 are the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1-6 alkyl group or a C1-6 alkoxy group)); m is 0 or 1; and n is 0 or 1.
摘要翻译: 本发明提供了可用作胰岛素敏化剂的新型羧酸衍生物,其盐或其水合物,以及包含该衍生物作为有效成分的药物。 更具体地,它提供由式(I)表示的羧酸化合物,其盐或它们的水合物。 在该式中,Ar表示可以具有至少一个取代基的6至14元芳环基团; R 1,R 2,R 3,R 4,R 5, R 6,R 7和R 8彼此相同或不同,并且各自表示氢原子,卤素原子, 羟基,C 1-6烷基或C 1-6烷氧基; X表示氧原子或亚甲基; Y表示由式(II)或(III)表示的基团:(其中Z表示由式(IV)表示的基团:(其中R 9,R 10, >,R 11和R 12彼此相同或不同,并且各自表示氢原子,卤素原子,羟基,C 1 -C 12烷基, 1-6烷基或C 1-6烷氧基)); m为0或1; n为0或1。
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