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1. 发明申请

US20130053345A1 BICYCLIC HETEROARLY ANALOGUES AS GPR119 MODULATORS 有权
标题翻译：作为GPR119调制器的双相异常模拟器
公开(公告)号：US20130053345A1
公开(公告)日：2013-02-28
申请号：US13696103
申请日：2011-05-04
申请人： Xiang-Yang Ye , Dean A. Wacker , Jeffrey A. Robl , Ying Wang
发明人： Xiang-Yang Ye , Dean A. Wacker , Jeffrey A. Robl , Ying Wang
IPC分类号： C07D417/14 , A61K31/4545 , C07D513/04 , C07D413/14 , C07F9/6558 , A61K31/675 , A61K31/5377 , A61K31/497 , C07D417/12 , A61K31/454 , C07D401/14 , A61K31/4439 , A61K31/496 , A61P3/10 , A61P3/08 , A61P9/10 , A61P25/00 , A61P13/12 , A61P17/02 , A61P9/00 , A61P3/00 , A61P9/12 , A61P3/04 , A61P3/06 , A61P1/18 , A61P25/28 , A61P19/08 , A61P27/06 , A61P9/04 , A61P29/00 , A61K31/4985 , A61K31/513 , A61K31/506
CPC分类号： C07D417/14 , C07D401/14 , C07D413/14 , C07D417/12
摘要： Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
摘要翻译：其中A，D，D，E，J，L，n，Q，R 2和R 4在本文中定义的结构式I的新型化合物或其对映异构体，非对映异构体，互变异构体，前药或其盐是GPR119G 蛋白偶联受体调节剂。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。因此，本公开还涉及包含这些新化合物的组合物以及通过使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与GPR119G蛋白偶联受体的活性有关的疾病或病症的方法。

2. 发明授权

US08940716B2 Bicyclic heteroaryl compounds as GPR119 modulators 有权
标题翻译：双环杂芳基化合物作为GPR119调节剂
公开(公告)号：US08940716B2
公开(公告)日：2015-01-27
申请号：US13696103
申请日：2011-05-04
申请人： Xiang-Yang Ye , Dean A. Wacker , Jeffrey A. Robl , Ying Wang
发明人： Xiang-Yang Ye , Dean A. Wacker , Jeffrey A. Robl , Ying Wang
IPC分类号： C07D417/14 , A61K31/4545 , C07D401/14 , C07D413/14 , C07D417/12
CPC分类号： C07D417/14 , C07D401/14 , C07D413/14 , C07D417/12
摘要： Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
摘要翻译：其中A，D，D，E，J，L，n，Q，R 2和R 4在本文中定义的结构式I的新型化合物或其对映异构体，非对映异构体，互变异构体，前药或其盐是GPR119G 蛋白偶联受体调节剂。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。因此，本公开还涉及包含这些新化合物的组合物以及通过使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与GPR119G蛋白偶联受体的活性有关的疾病或病症的方法。

3. 发明授权

US08729084B2 Benzofuranyl analogues as GPR119 modulators 有权
标题翻译：苯并呋喃基类似物作为GPR119调节剂
公开(公告)号：US08729084B2
公开(公告)日：2014-05-20
申请号：US13696131
申请日：2011-05-04
申请人： Xiang-Yang Ye , Dean A. Wacker , Jeffrey A. Robl
发明人： Xiang-Yang Ye , Dean A. Wacker , Jeffrey A. Robl
IPC分类号： C07D405/14 , A61K31/506
CPC分类号： C07D405/14
摘要： Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, L, m, n, o, p, R2, R3, R3, R4 and R5 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
摘要翻译：其中A，L，m，n，o，p，R 2，R 3，R 3，R 4和R 5在本文中定义的结构式I的新型化合物或其对映体，非对映异构体，互变异构体，前药或其盐， GPR119 G蛋白偶联受体调节剂。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。因此，本公开还涉及包含这些新化合物的组合物以及通过使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与GPR119G蛋白偶联受体的活性有关的疾病或病症的方法。

4. 发明申请

US20130059858A1 BENZOFURANYL ANALOGUES AS GPR119 MODULATORS 有权
标题翻译： BENZOFURANYL模拟器作为GPR119调制器
公开(公告)号：US20130059858A1
公开(公告)日：2013-03-07
申请号：US13696131
申请日：2011-05-04
申请人： Xiang-Yang Ye , Dean A. Wacker , Jeffrey A. Robl
发明人： Xiang-Yang Ye , Dean A. Wacker , Jeffrey A. Robl
IPC分类号： C07D405/14 , A61K31/4545 , A61K31/4985 , A61K31/513 , A61P19/08 , A61P9/10 , A61P9/12 , A61P3/04 , A61P3/06 , A61P1/18 , A61K31/506 , A61P3/10
CPC分类号： C07D405/14
摘要： Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, where-in A, L, m, n, o, p, R2, R3, R3, R4 and R5 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
摘要翻译：提供结构式I的新型化合物或其对映体，非对映体，互变异构体，前药或其盐，其中A，L，m，n，o，p，R 2，R 3，R 3，R 4和R 5在本文中定义其是GPR119G蛋白偶联受体调节剂。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。因此，本公开还涉及包含这些新化合物的组合物以及通过使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与GPR119G蛋白偶联受体的活性相关的疾病或病症的方法。

5. 发明授权

US08299054B2 Cyclic 11-beta hydroxysteroid dehydrogenase type 1 inhibitors 有权
标题翻译：环状11-β羟基类固醇脱氢酶1型抑制剂
公开(公告)号：US08299054B2
公开(公告)日：2012-10-30
申请号：US12759867
申请日：2010-04-14
申请人： Xiang-Yang Ye , Jeffrey A. Robl , Ronald L. Hanson , Zhiwei Guo , Ramesh N. Patel
发明人： Xiang-Yang Ye , Jeffrey A. Robl , Ronald L. Hanson , Zhiwei Guo , Ramesh N. Patel
IPC分类号： A61K31/397 , C07D206/00
CPC分类号： C07C61/40 , C07B2200/07 , C07C57/50 , C07C57/62 , C07C59/54 , C07C59/56 , C07C59/72 , C07C59/88 , C07C61/39 , C07C62/38 , C07C2603/66 , C07C2603/74 , C07D203/18 , C07D205/04 , C07D205/06 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/42 , C07D211/46 , C07D213/40 , C07D217/02 , C07D241/08 , C07D257/04 , C07D261/02 , C07D261/08 , C07D263/04 , C07D277/04 , C07D277/46 , C07D277/64 , C07D277/82 , C07D285/135 , C07D295/185 , C07D295/205 , C07D401/12 , C07D403/04 , C07D407/06 , C07D413/04 , C07D471/04 , C07D493/08
摘要： Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.
摘要翻译：提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。这些新化合物具有以下结构：其中A，W，X和Z如本文所定义，其对映异构体，非对映体，溶剂合物或其盐。

6. 发明申请

US20100204199A1 CYCLIC 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS 有权
标题翻译：循环11-羟基脱氢酶脱氢酶I型抑制剂
公开(公告)号：US20100204199A1
公开(公告)日：2010-08-12
申请号：US12759867
申请日：2010-04-14
申请人： Xiang-Yang Ye , Jeffrey A. Robl , Ronald L. Hanson , Zhiwei Guo , Ramesh N. Patel
发明人： Xiang-Yang Ye , Jeffrey A. Robl , Ronald L. Hanson , Zhiwei Guo , Ramesh N. Patel
IPC分类号： A61K31/397 , A61K31/496 , A61K31/45 , A61K31/41 , A61K31/40 , A61K31/192 , C07D241/08 , C07D471/04 , C07D211/22 , C07D401/12 , C07D413/04 , C07D257/04 , C07D403/04 , C07D207/08 , C07D205/04 , C07C59/56 , C07C57/50 , C07C57/62 , A61P3/00 , A61K31/4245 , A61K31/437 , A61K31/4427 , A61P3/10 , A61P9/12 , A61P25/28 , A61P19/02 , A61P27/06
CPC分类号： C07C61/40 , C07B2200/07 , C07C57/50 , C07C57/62 , C07C59/54 , C07C59/56 , C07C59/72 , C07C59/88 , C07C61/39 , C07C62/38 , C07C2603/66 , C07C2603/74 , C07D203/18 , C07D205/04 , C07D205/06 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/42 , C07D211/46 , C07D213/40 , C07D217/02 , C07D241/08 , C07D257/04 , C07D261/02 , C07D261/08 , C07D263/04 , C07D277/04 , C07D277/46 , C07D277/64 , C07D277/82 , C07D285/135 , C07D295/185 , C07D295/205 , C07D401/12 , C07D403/04 , C07D407/06 , C07D413/04 , C07D471/04 , C07D493/08
摘要： Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.
摘要翻译：提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。这些新化合物具有以下结构：其中A，W，X和Z如本文所定义，其对映异构体，非对映异构体，溶剂合物或其盐。

7. 发明授权

US07727978B2 Cyclic 11-beta hydroxysteroid dehydrogenase type I inhibitors 有权
标题翻译：环状11-β羟基类固醇脱氢酶I型抑制剂
公开(公告)号：US07727978B2
公开(公告)日：2010-06-01
申请号：US11843015
申请日：2007-08-22
申请人： Xiang-Yang Ye , Jeffrey A. Robl
发明人： Xiang-Yang Ye , Jeffrey A. Robl
IPC分类号： A61K31/397 , C07D206/00
CPC分类号： C07C61/40 , C07B2200/07 , C07C57/50 , C07C57/62 , C07C59/54 , C07C59/56 , C07C59/72 , C07C59/88 , C07C61/39 , C07C62/38 , C07C2603/66 , C07C2603/74 , C07D203/18 , C07D205/04 , C07D205/06 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/42 , C07D211/46 , C07D213/40 , C07D217/02 , C07D241/08 , C07D257/04 , C07D261/02 , C07D261/08 , C07D263/04 , C07D277/04 , C07D277/46 , C07D277/64 , C07D277/82 , C07D285/135 , C07D295/185 , C07D295/205 , C07D401/12 , C07D403/04 , C07D407/06 , C07D413/04 , C07D471/04 , C07D493/08
摘要： Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.
摘要翻译：提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。这些新化合物具有以下结构：其中A，W，X和Z如本文所定义，其对映异构体，非对映异构体，溶剂合物或其盐。

8. 发明申请

US20080234249A1 CYCLIC 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS 有权
标题翻译：循环11-羟基脱氢酶脱氢酶I型抑制剂
公开(公告)号：US20080234249A1
公开(公告)日：2008-09-25
申请号：US11843015
申请日：2007-08-22
申请人： Xiang-Yang Ye , Jeffrey A. Robl , Ronald L. Hanson , Zhiwei Guo , Ramesh N. Patel
发明人： Xiang-Yang Ye , Jeffrey A. Robl , Ronald L. Hanson , Zhiwei Guo , Ramesh N. Patel
IPC分类号： A61K31/00
CPC分类号： C07C61/40 , C07B2200/07 , C07C57/50 , C07C57/62 , C07C59/54 , C07C59/56 , C07C59/72 , C07C59/88 , C07C61/39 , C07C62/38 , C07C2603/66 , C07C2603/74 , C07D203/18 , C07D205/04 , C07D205/06 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/42 , C07D211/46 , C07D213/40 , C07D217/02 , C07D241/08 , C07D257/04 , C07D261/02 , C07D261/08 , C07D263/04 , C07D277/04 , C07D277/46 , C07D277/64 , C07D277/82 , C07D285/135 , C07D295/185 , C07D295/205 , C07D401/12 , C07D403/04 , C07D407/06 , C07D413/04 , C07D471/04 , C07D493/08
摘要： Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.
摘要翻译：提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。这些新化合物具有以下结构：其中A，W，X和Z如本文所定义，其对映异构体，非对映异构体，溶剂合物或其盐。

9. 发明申请

US20070287713A1 SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 有权
公开(公告)号：US20070287713A1
公开(公告)日：2007-12-13
申请号：US11779319
申请日：2007-07-18
申请人： Peter Cheng , Sean Chen , Pratik Devasthale , Charles Ding , Timothy Herpin , Shung Wu , Hao Zhang , Wei Wang , Xiang-Yang Ye
发明人： Peter Cheng , Sean Chen , Pratik Devasthale , Charles Ding , Timothy Herpin , Shung Wu , Hao Zhang , Wei Wang , Xiang-Yang Ye
IPC分类号： A61K31/41 , A61K31/42 , A61K31/44 , A61K31/445 , A61K31/4965 , A61K31/497 , A61K31/505 , A61P3/10 , C07D239/02 , C07D257/00 , C07D263/30 , C07D271/06 , C07D401/02 , C07D403/02 , C07D413/02
CPC分类号： C07D413/12 , C07D413/14
摘要： wherein Z1 is (CH2)q or C═O; Z2 is (CH2)p or C═O; D is —CH═ or C═O or (CH2)m where m is 0, 1, 2 or 3; n=0, 1 or 2; p=1 or 2; q=0, 1 or 2; Q is C or N; A is (CH2)x where x is 1 to 5, or A is (CH2)x1, where x1 is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is —(CH2)x2—O—(CH2)x3— where x2 is 0 to 5 and x3 is 0 to 5, provided that at least one of x2 and x3 is other than 0; B is a bond or is (CH2)x4 where x4 is 1 to 5; X is CH or N; X2 is C, N, O or S; X3 is C, N, O or S; X4 is C, N, O or S; X5 is C, N, O or S; X6 is C, N, O or S; provided that at least one of X2, X3, X4 X5 and X6 is N; and at least one of X2, X3, X4 X5 and X6 is C. R1 is H or alkyl; R2 is H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; R2a, R2b and R2c may be the same or different and are selected from H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; and R3, E, Z and Y are as defined herein.

10. 发明授权

US07951793B2 Substituted heterocyclic derivatives useful as antidiabetic and antiobesity agents and method 有权
标题翻译：用作抗糖尿病和抗肥胖剂的取代的杂环衍生物和方法
公开(公告)号：US07951793B2
公开(公告)日：2011-05-31
申请号：US11779319
申请日：2007-07-18
申请人： Peter T. W. Cheng , Sean Chen , Pratik Devasthale , Charles Z. Ding , Timothy F. Herpin , Shung Wu , Hao Zhang , Wei Wang , Xiang-Yang Ye
发明人： Peter T. W. Cheng , Sean Chen , Pratik Devasthale , Charles Z. Ding , Timothy F. Herpin , Shung Wu , Hao Zhang , Wei Wang , Xiang-Yang Ye
IPC分类号： A61K31/397 , C07D205/08 , A01N43/00
CPC分类号： C07D413/12 , C07D413/14
摘要： Compounds are provided which have the structure wherein Z1 is (CH2)q or C═O; Z2 is (CH2)p or C═O; D is —CH═ or C═O or (CH2)m where m is 0, 1, 2 or 3; n=0, 1 or 2; p=1 or 2; q=0, 1 or 2; Q is C or N; X is CH or N; X2 is C, N, O or S; X3 is C, N, O or S; X4 is C, N, O or S; X5 is C, N, O or S; X6 is C, N, O or S; provided that at least one of X2, X3, X4 X5 and X6 is N; and at least one of X2, X3, X4 X5 and X6 is C; and A, B, R1, R2, R2a, R4, R3, E, Z and Y are as defined herein, which compounds are useful in treating diabetes and related diseases.
摘要翻译：提供具有其中Z 1是（CH 2）q或C = O的结构的化合物; Z2是（CH2）p或C = O; D是-CH =或C = O或（CH 2）m，其中m为0,1,2或3; n = 0,1或2; p = 1或2; q = 0,1或2; Q是C或N; X是CH或N; X2是C，N，O或S; X3为C，N，O或S; X4为C，N，O或S; X5为C，N，O或S; X6为C，N，O或S; 条件是X 2，X 3，X 4 X 5和X 6中的至少一个为N; X2，X3，X4，X5和X6中的至少一个为C; 并且A，B，R1，R2，R2a，R4，R3，E，Z和Y如本文所定义，该化合物可用于治疗糖尿病和相关疾病。

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