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公开(公告)号:US20090018056A1
公开(公告)日:2009-01-15
申请号:US12231856
申请日:2008-09-05
申请人: Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
发明人: Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号: A61K38/28 , C07D277/28 , C07D241/10 , C07D239/28 , C07D261/14 , A61K31/426 , A61K31/495 , A61K31/433 , A61K31/4439 , A61P3/10 , A61K31/501 , A61K31/4365 , A61K31/42 , A61K31/4965 , C07D285/08 , C07D471/04 , C07D401/10 , C07D403/10
CPC分类号: C07D213/75 , C07D231/40 , C07D237/20 , C07D239/42 , C07D241/20 , C07D249/04 , C07D261/14 , C07D271/07 , C07D275/03 , C07D277/18 , C07D277/46 , C07D277/60 , C07D277/82 , C07D285/08 , C07D285/10 , C07D285/135 , C07D401/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D513/04
摘要: Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): [wherein X1 represents oxygen, etc., X2 represents oxygen, etc., R1 represents a group on Ring A such as alkylsulfonyl, etc., R2 represents C3-7 cyclic alkyl optionally substituted with a halogen, etc., R3 represents a substituent on Ring B such as lower alkyl, etc., formula (II): [Chemical Formula 1] represents 6- to 10-membered aryl, etc., and formula (III): [Formula 1] represents monocyclic or bicyclic heteroaryl optionally having on Ring B a substituent represented by R3 above, wherein the carbon atom of Ring B which is bonded to the nitrogen atom of the amide group of formula (I) forms a C═N bond with the nitrogen atom of the ring], as well as their pharmaceutically acceptable salts.
摘要翻译: 具有葡糖激酶活化作用的化合物,可用作由下式(I)表示的糖尿病治疗:[其中X1表示氧等,X2表示氧等,R1表示环A上的基团,例如烷基磺酰基 等等,R 2表示任选被卤素取代的C 3-7环烷基等,R 3表示环B上的取代基,例如低级烷基等,式(II):[化学式1]表示6-至10 (III)表示:[式1]表示在环B上任选具有由上述R 3表示的取代基的单环或双环杂芳基,其中键合到氮原子上的环B的碳原子 式(I)的酰胺基与环的氮原子形成CN键,以及它们的药学上可接受的盐。
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公开(公告)号:US07994331B2
公开(公告)日:2011-08-09
申请号:US11988592
申请日:2006-07-12
IPC分类号: C07D413/14 , A61K31/44
CPC分类号: C07D409/14 , C07D401/14 , C07D405/14 , C07D413/14
摘要: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein X1 to X4 independently represent a carbon atom or the like; the ring A represents a 5- to 6-membered heteroaryl having 1 to 4 heteroatoms independently selected from the group consisting of a nitrogen atom, a sulfur atom and an oxygen atom; X5 represents an oxygen atom or the like; X represents a carbon atom or the like; Het represents a 5- or 6-membered aliphatic heterocycle; R1 represents an aryl or the like; R2 represents a formyl group or the like; and R3 represents a —C1-6 alkyl or the like. The compound or salt has a glucokinase activation effect and is useful as a therapeutic agent for diabetes.
摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐:(I)其中X 1至X 4独立地表示碳原子等; 环A表示具有1至4个独立地选自氮原子,硫原子和氧原子的杂原子的5-至6-元杂芳基; X 5表示氧原子等; X表示碳原子等; Het代表5-或6-元脂族杂环; R1表示芳基等; R2表示甲酰基等; 并且R 3表示-C 1-6烷基等。 化合物或盐具有葡糖激酶活化作用,可用作糖尿病的治疗剂。
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公开(公告)号:US07754743B2
公开(公告)日:2010-07-13
申请号:US12231856
申请日:2008-09-05
申请人: Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
发明人: Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号: A61K31/44 , A61K31/425 , C07D417/12
CPC分类号: C07D213/75 , C07D231/40 , C07D237/20 , C07D239/42 , C07D241/20 , C07D249/04 , C07D261/14 , C07D271/07 , C07D275/03 , C07D277/18 , C07D277/46 , C07D277/60 , C07D277/82 , C07D285/08 , C07D285/10 , C07D285/135 , C07D401/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D513/04
摘要: Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): [wherein X1 represents oxygen, etc., X2 represents oxygen, etc., R1 represents a group on Ring A such as alkylsulfonyl, etc., R2 represents C3-7 cyclic alkyl optionally substituted with a halogen, etc., R3 represents a substituent on Ring B such as lower alkyl, etc., formula (II): [Chemical Formula 1] represents 6- to 10-membered aryl, etc., and formula (III): [Formula 1] represents monocyclic or bicyclic heteroaryl optionally having on Ring B a substituent represented by R3 above, wherein the carbon atom of Ring B which is bonded to the nitrogen atom of the amide group of formula (I) forms a C═N bond with the nitrogen atom of the ring], as well as their pharmaceutically acceptable salts.
摘要翻译: 具有葡糖激酶活化作用的化合物,可用作由下式(I)表示的糖尿病治疗:[其中X1表示氧等,X2表示氧等,R1表示环A上的基团,例如烷基磺酰基 等等,R 2表示任选被卤素取代的C 3-7环烷基等,R 3表示环B上的取代基,例如低级烷基等,式(II):[化学式1]表示6-至10 (III)表示:[式1]表示在环B上任选具有由上述R 3表示的取代基的单环或双环杂芳基,其中键合到氮原子上的环B的碳原子 式(I)的酰胺基与环的氮原子形成C = N键,以及它们的药学上可接受的盐。
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公开(公告)号:US20100041660A1
公开(公告)日:2010-02-18
申请号:US12604835
申请日:2009-10-23
申请人: MORIHIRO MITSUYA , Makoto Bamba , Fumiko Sakai , Hitomi Watanabe , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki
发明人: MORIHIRO MITSUYA , Makoto Bamba , Fumiko Sakai , Hitomi Watanabe , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号: A61K31/53 , C07D417/14 , A61K31/4436 , C07D401/14 , A61K31/444 , C07D513/02 , A61K31/4365 , C07D403/02 , A61K31/501 , A61K31/497 , A61P3/10 , A61K31/506 , C07D253/065
CPC分类号: C07D471/04 , C07D417/14
摘要: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明涉及具有葡糖激酶活化作用并可用作糖尿病治疗剂的化合物,其由式(I)表示:[其中X1表示氮原子,硫原子,氧原子等 ; R1表示6-至10-元芳基,5-至7-元杂芳基等; D表示氧原子或硫原子; R2和R3相同或不同,各自表示氢原子,低级烷基等; 式(II)表示任选取代的5〜7元杂芳基等; 式(III)表示单环或双环杂芳基]或其药学上可接受的盐。
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公开(公告)号:US20050282815A1
公开(公告)日:2005-12-22
申请号:US10952471
申请日:2004-09-27
IPC分类号: A61K31/426 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/506 , A61P3/04 , A61P3/10 , A61P43/00 , C07D277/46 , C07D277/56 , C07D401/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/04 , A61K31/497 , A61K31/501 , C07D413/02 , C07D417/02 , C07D43/02
CPC分类号: C07D401/12 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/506 , C07D277/46 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/04
摘要: This invention relates to a novel compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is —S(O)p-A, —S—(O)q-B or —O-D, wherein p and q, which are the same or different, each represent an integer from 0 to 2, A is a straight chain C1-C10 alkyl group which may be substituted by R10, and B and D each independently represent R12 which may be substituted by R10; R2 is a hydrogen atom, a halogen atom, or a straight chain or branched C1-C6 alkyl group which may be substituted by R10; X1 and X2 each independently represent N or CH, but cannot both be N; the formula (II): shows a monocyclic or bicyclic heteroaryl group which has a nitrogen atom adjacent to the carbon atom bonded to the amide group, and the heteroaryl group may be substituted by R10; R10 is R11, or a hydrocarbon group which may be substituted by R11; R11 is, for example, a hydrogen atom or amino; and R12 is, for example, phenyl, thiazolyl, pyridyl or methylene dioxyphenyl. The compound according to this invention has a glucokinase activation effect, and for example, is useful in the treatment and prevention of diabetes mellitus, and in the prevention of its complications such as diabetic nephropathy, diabetic retinopathy, diabetic neuropathy and diabetic arteriosclerosis.
摘要翻译: 本发明涉及由式(I)表示的新化合物或其药学上可接受的盐,其中R 1是-S(O)p A,-S-(O)qB或-OD 其中相同或不同的p和q各自表示0至2的整数,A是可以被R 10取代的直链C 1 -C 10烷基,B和 D各自独立地表示可被R 10取代的R 12, R 2是氢原子,卤素原子或可被R 10取代的直链或支链C 1 -C 6烷基; X 1和X 2各自独立地表示N或CH,但不能都是N; 式(II)表示具有与结合到酰胺基上的碳原子相邻的氮原子的单环或双环杂芳基,杂芳基可以被R 10取代; R 10是R 11,或可被R 11取代的烃基; R 11是例如氢原子或氨基; R 12是例如苯基,噻唑基,吡啶基或亚甲基二氧苯基。 根据本发明的化合物具有葡糖激酶活化作用,例如可用于治疗和预防糖尿病,并且可用于预防其并发症如糖尿病性肾病,糖尿病性视网膜病,糖尿病性神经病和糖尿病性动脉硬化。
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公开(公告)号:US08344003B2
公开(公告)日:2013-01-01
申请号:US12604835
申请日:2009-10-23
申请人: Morihiro Mitsuya , Makoto Bamba , Fumiko Sakai , Hitomi Watanabe , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki
发明人: Morihiro Mitsuya , Makoto Bamba , Fumiko Sakai , Hitomi Watanabe , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号: A61K31/4436 , C07D417/14 , C07D401/14
CPC分类号: C07D471/04 , C07D417/14
摘要: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明涉及具有葡糖激酶活化作用并可用作糖尿病治疗剂的化合物,其由式(I)表示:[其中X1表示氮原子,硫原子,氧原子等 ; R1表示6-至10-元芳基,5-至7-元杂芳基等; D表示氧原子或硫原子; R2和R3相同或不同,各自表示氢原子,低级烷基等; 式(II)表示任选取代的5〜7元杂芳基等; 式(III)表示单环或双环杂芳基]或其药学上可接受的盐。
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公开(公告)号:US07687502B2
公开(公告)日:2010-03-30
申请号:US10593540
申请日:2005-03-23
申请人: Morihiro Mitsuya , Makoto Bamba , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki , Keisuke Arakawa
发明人: Morihiro Mitsuya , Makoto Bamba , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki , Keisuke Arakawa
IPC分类号: A61K31/519 , A61K31/497 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/14 , C07D419/12 , A61P3/04 , A61P3/10 , C07D471/04 , C07D513/04
CPC分类号: A61K31/513 , A61K31/517 , A61K31/519 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D513/04
摘要: The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is nitrogen atom, etc.; Y is oxygen atom, etc.; R1 is an optionally substituted five to six-membered heteroaryl group, etc.; R2 is hydrogen atom or fluorine atom; and ring A is a monocyclic or bicyclic heteroaryl group which may have a substituent represented by the formula (II)] or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明提供具有葡糖激酶活化作用的化合物,其可用于预防或治疗由式(I)表示的糖尿病等:X为氮原子等; Y是氧原子等; R1是任选取代的五至六元杂芳基等; R2是氢原子或氟原子; 环A是可以具有式(II)表示的取代基的单环或双环杂芳基]或其药学上可接受的盐。
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公开(公告)号:US07253188B2
公开(公告)日:2007-08-07
申请号:US10952471
申请日:2004-09-27
IPC分类号: C07D401/12 , C07D401/14 , A61K31/4427 , A61K31/506 , A61K31/5377 , A61P3/04 , A61P3/10 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , A61K31/47 , A61K31/497 , A61K31/501
CPC分类号: C07D401/12 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/506 , C07D277/46 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/04
摘要: This invention relates to a novel compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is —S(O)p-A, —S—(O)q-B or —O-D, wherein p and q, which are the same or different, each represent an integer from 0 to 2, A is a straight chain C1-C10 alkyl group which may be substituted by R10, and B and D each independently represent R12 which may be substituted by R10; R2 is a hydrogen atom, a halogen atom, or a straight chain or branched C1-C6 alkyl group which may be substituted by R10; X1 and X2 each independently represent N or CH, but cannot both be N; the formula (II): shows a monocyclic or bicyclic heteroaryl group which has a nitrogen atom adjacent to the carbon atom bonded to the amide group, and the heteroaryl group may be substituted by R10; R10 is R11, or a hydrocarbon group which may be substituted by R11; R11 is, for example, a hydrogen atom or amino; and R12 is, for example, phenyl, thiazolyl, pyridyl or methylene dioxyphenyl. The compound according to this invention has a glucokinase activation effect, and for example, is useful in the treatment and prevention of diabetes mellitus, and in the prevention of its complications such as diabetic nephropathy, diabetic retinopathy, diabetic neuropathy and diabetic arteriosclerosis.
摘要翻译: 本发明涉及由式(I)表示的新化合物或其药学上可接受的盐,其中R 1是-S(O)p A,-S-(O)qB或-OD 其中相同或不同的p和q各自表示0至2的整数,A是可以被R 10取代的直链C 1 -C 10烷基,B和 D各自独立地表示可被R 10取代的R 12, R 2是氢原子,卤素原子或可被R 10取代的直链或支链C 1 -C 6烷基; X 1和X 2各自独立地表示N或CH,但不能都是N; 式(II)表示具有与结合到酰胺基上的碳原子相邻的氮原子的单环或双环杂芳基,杂芳基可以被R 10取代; R 10是R 11,或可被R 11取代的烃基; R 11是例如氢原子或氨基; R 12是例如苯基,噻唑基,吡啶基或亚甲基二氧苯基。 根据本发明的化合物具有葡糖激酶活化作用,例如可用于治疗和预防糖尿病,并且可用于预防其并发症如糖尿病性肾病,糖尿病性视网膜病,糖尿病性神经病和糖尿病性动脉硬化。
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公开(公告)号:US06608098B1
公开(公告)日:2003-08-19
申请号:US10069376
申请日:2002-02-25
IPC分类号: A61K31403
CPC分类号: C07D498/04
摘要: This invention relates to compounds represented by the general formula [I] wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.
摘要翻译: 本发明涉及由通式[I]表示的化合物,其中R表示叠氮基等,R 1和R 2相同或不同,表示氢原子等,R 3和R 4相同或不同,表示 氢原子等,X1表示氧原子等,X2表示氧原子等,Y表示氧原子等,Z表示缩合芳基等,或其药学上可接受的盐 ,其制备方法和糖尿病治疗剂,用于糖尿病慢性并发症的预防剂或抗肥胖药物,含有作为有效成分的化合物或其药学上可接受的盐。
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公开(公告)号:US20080125429A1
公开(公告)日:2008-05-29
申请号:US11666555
申请日:2005-11-01
申请人: Noriaki Hashimoto , Keiji Takahashi , Chisato Nakama , Yoshio Ogino , Fumiko Sakai , Teruyuki Nishimura , Jun-ichi Eiki
发明人: Noriaki Hashimoto , Keiji Takahashi , Chisato Nakama , Yoshio Ogino , Fumiko Sakai , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号: A61K31/5377 , C07D213/02 , C07D221/00 , C07D239/06 , C07D241/10 , C07D295/00 , A61P3/10 , A61K31/4439 , A61K31/4545 , A61K31/444 , A61K31/506 , A61K31/497
CPC分类号: A61K38/31 , A61K31/155 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K38/28 , A61K45/06 , C07D401/04 , C07D401/14 , C07D413/06 , C07D413/14 , A61K2300/00
摘要: A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided.The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; Z represents an oxygen atom, a sulfur atom or a nitrogen atom; Ar represents an aryl or heteroaryl group optionally mono to tri-substituted with a group selected from the substituent group β; ring A represents a 5- or 6-membered nitrogen-containing heteroaromatic group; m indicates an integer of from 1 to 6; n indicates an integer of from 0 to 3; p indicates an integer of from 0 to 2 (provided that at least two of X1 to X4 are carbon atoms); q indicates 0 or 1] or its pharmaceutically-acceptable salt, which has an effect of glucokinase activation and is useful as a treatment for diabetes.
摘要翻译: 提供葡糖激酶活化剂; 提供糖尿病的治疗和/或预防,或治疗和/或预防糖尿病如视网膜病,肾病,神经症,缺血性心脏病,动脉硬化,以及进一步的治疗和/或预防肥胖症。 本发明涉及式(I)的化合物:其中R 1和R 2代表氢等; R 3表示氢原子,卤素原子等; R 4各自独立地表示氢原子,低级烷基等; Q表示碳原子,氮原子或硫原子(硫原子可以被氧代基单取代或二取代)。 R 5和R 6各自表示氢原子,低级烷基等; X 1,X 2,X 3和X 4各自独立地表示碳原子或氮原子; Z表示氧原子,硫原子或氮原子; Ar表示任选被选自取代基组β的基团单取代至三取代的芳基或杂芳基; 环A表示5-或6-元含氮杂芳基; m表示1〜6的整数, n表示0〜3的整数, p表示0〜2的整数(条件是X 1〜X 4中的至少2个为碳原子); q表示0或1]或其药学上可接受的盐,其具有葡糖激酶活化的作用,并且可用作糖尿病的治疗。
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