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1. 发明授权

US07687502B2 Substituted quinazoline or pyridopyrimidine derivative 失效
标题翻译：取代喹唑啉或吡啶并嘧啶衍生物
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。

2. 发明申请

US20080032996A1 Substituted Quinazoline or Pyridopyrimidine Derivative 失效
标题翻译：取代喹唑啉或吡啶并嘧啶衍生物
公开(公告)号：US20080032996A1
公开(公告)日：2008-02-07
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 , A61K31/517 , A61K38/28 , A61P3/04 , A61P3/10 , C07D403/12 , C07D413/12 , C07D417/14 , 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; R 1是任选取代的五至六元杂芳基等; R 2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。

3. 发明授权

US08344003B2 2-pyridinecarboxamide derivatives 有权
标题翻译： 2-吡啶甲酰胺衍生物
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。

4. 发明授权

US07629362B2 2-pyridine carboxamide derivatives 有权
标题翻译： 2-吡啶甲酰胺衍生物
公开(公告)号：US07629362B2
公开(公告)日：2009-12-08
申请号：US10545424
申请日：2004-02-13
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。

5. 发明申请

US20060258701A1 Novel 2-pyridinecarboxamide derivatives 有权
标题翻译：新型2-吡啶甲酰胺衍生物
公开(公告)号：US20060258701A1
公开(公告)日：2006-11-16
申请号：US10545424
申请日：2004-02-13
申请人： Morihiro Mitsuya , Makoto Bamba , Fumio Sakai , Hitomi Watanabe , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Morihiro Mitsuya , Makoto Bamba , Fumio Sakai , Hitomi Watanabe , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： A61K31/4745 , A61K31/444 , A61K31/4439 , C07D498/02 , C07D417/14
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; R 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X 1表示氮原子，硫原子，氧原子等; R 1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; R和R 3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。

6. 发明申请

US20100041660A1 NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES 有权
标题翻译：新型2-吡啶甲酰胺衍生物
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。

7. 发明申请

US20080070928A1 Novel 2-Heteroaryl-Substituted Benzimidazole Derivative 有权
标题翻译：新型2-杂芳基取代的苯并咪唑衍生物
公开(公告)号：US20080070928A1
公开(公告)日：2008-03-20
申请号：US10582564
申请日：2004-12-28
申请人： Katsumasa Nonoshita , Makoto Ishikawa , Hiroshi Nakashima , Daisuke Tsukahara , Yoshio Ogino , Fumiko Sakai , Yoshikazu Nagae , Keisuke Arakawa , Teruyuki Nishimura , Jun-Ichi Eiki
发明人： Katsumasa Nonoshita , Makoto Ishikawa , Hiroshi Nakashima , Daisuke Tsukahara , Yoshio Ogino , Fumiko Sakai , Yoshikazu Nagae , Keisuke Arakawa , Teruyuki Nishimura , Jun-Ichi Eiki
IPC分类号： A61K31/497 , A61K31/4184 , A61K31/422 , A61K31/4245 , A61K31/427 , A61P3/04 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/02 , C07D413/02 , C07D403/02 , A61P3/10 , A61K31/506 , A61K31/433 , A61K31/4439 , A61K31/444
CPC分类号： C07D401/14 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/14 , C07D417/04
摘要： A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided.A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt: [in the formula, X represents a carbon atom or a nitrogen atom; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; the ring A represents a 5- or 6-membered nitrogen-containing aromatic hetero ring of a formula (II): (in the formula, X represents a carbon atom or a nitrogen atom); R1 represents an aryl, etc.; R2 represents a hydroxy, etc.; R3 represents a —C1-6 alkyl, etc.; R4 represents a —C1-6 alkyl, etc.; X5 represents —O—, etc.; a indicates an integer of 1, 2 or 3; q indicates an integer of from 0 to 2; m indicates an integer of from 0 to 2].
摘要翻译：提供葡糖激酶活化剂; 提供了糖尿病的补救措施和/或预防，糖尿病的补救和/或预防，如视网膜病变，肾病，神经症，缺血性心脏病，动脉硬化，以及进一步的补救措施和/或预防肥胖症。一种葡糖激酶活化剂，其特征在于含有通式（I-0）的2-杂芳基取代的苯并咪唑衍生物或其药学上可接受的盐：[式中X表示碳原子或氮原子; X 1，X 2，X 3和X 4各自独立地表示碳原子或氮原子; 环A表示式（II）的5-或6-元含氮芳族杂环：（式中，X表示碳原子或氮原子）; R 1表示芳基等; R 2表示羟基等; R 3表示-C 1-6烷基等; R 4表示-C 1-6烷基等; X 5表示-O-等; a表示1,2或3的整数; q表示0〜2的整数， m表示0〜2的整数]。

8. 发明申请

US20090018056A1 Heteroarylcarbamoylbenzene derivatives 有权
标题翻译：杂芳基氨基甲酰基苯衍生物
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。

9. 发明授权

US07253188B2 Aminobenzamide derivative 失效
标题翻译：氨基苯甲酰胺衍生物
公开(公告)号：US07253188B2
公开(公告)日：2007-08-07
申请号：US10952471
申请日：2004-09-27
申请人： Teruyuki Nishimura , Tomoharu Iino , Yasufumi Nagata , Jun-ichi Eiki
发明人： Teruyuki Nishimura , Tomoharu Iino , Yasufumi Nagata , Jun-ichi Eiki
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。

10. 发明授权

US06608098B1 Isoindole derivatives 失效
标题翻译：异吲哚衍生物
公开(公告)号：US06608098B1
公开(公告)日：2003-08-19
申请号：US10069376
申请日：2002-02-25
申请人： Toshio Nagase , Tomoharu Iino , Yoshiyuki Sato , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Toshio Nagase , Tomoharu Iino , Yoshiyuki Sato , Teruyuki Nishimura , Jun-ichi Eiki
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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