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41. 发明授权

US07022681B2 Partial and full agonists of A1 adenosine receptors 失效
标题翻译： A1腺苷受体的部分和全部激动剂
公开(公告)号：US07022681B2
公开(公告)日：2006-04-04
申请号：US10641930
申请日：2003-08-15
申请人： Jeff Zablocki , Venkata Palle , Elfatih Elzein , Xiaofen Li
发明人： Jeff Zablocki , Venkata Palle , Elfatih Elzein , Xiaofen Li
IPC分类号： A61K31/70 , C07H19/167
CPC分类号： C07H19/16
摘要： Disclosed are A1 adenosine receptor agonists of the formula: wherein: R1 is optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, or optionally substituted heteroaryl; R2 is hydrogen, halo, trifluoromethyl, or cyano; R3 is hydrogen, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl, R4 and R5 are independently hydrogen or optionally substituted acyl; X is a covalent bond or lower alkylene optionally substituted by cycloalkyl; X1 is a covalent bond or alkylene; Y is a covalent bond or lower alkylene optionally substituted by hedroxy or cycloalkyl; and Z is —C≡C—, —R6C═CR7—, or —CHR6CHR7—, in which R6 and R7 at each occurrence are hydrogen or lower alkyl.
摘要翻译：公开了下式的A 1 N 2腺苷受体激动剂：其中：R 1是任选取代的环烷基，任选取代的杂环基，任选取代的芳基或任选取代的杂芳基; R 2是氢，卤素，三氟甲基或氰基; R 3是氢，任选取代的环烷基，任选取代的芳基，任选取代的杂芳基或任选取代的杂环基，R 4和R 5独立地是氢或任选取代的酰基; X是共价键或任选被环烷基取代的低级亚烷基; X 1是共价键或亚烷基; Y是共价键或任选被羟基或环烷基取代的低级亚烷基; 并且Z是-C≡C-，-R 6 C-CR 7或-CHR 6 CHR 7，其中每次出现的R 6和R 7都是氢或低级烷基。

42. 发明申请

US20060281921A1 A2B adenosine receptor antagonists 有权
标题翻译： A2B腺苷受体拮抗剂
公开(公告)号：US20060281921A1
公开(公告)日：2006-12-14
申请号：US11508592
申请日：2006-08-22
申请人： Elfatih Elzein , Rao Kalla , Tim Marquart , Jeff Zablocki , Xiaofen Li
发明人： Elfatih Elzein , Rao Kalla , Tim Marquart , Jeff Zablocki , Xiaofen Li
IPC分类号： C07D403/02
CPC分类号： C07D473/06 , C07D239/545 , C07D403/12 , C07D473/00 , C07D473/08
摘要： Disclosed are processes for the synthesis of novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
摘要翻译：公开了用于合成可用于治疗各种疾病状态（包括哮喘和腹泻）的Aβ2A腺苷受体拮抗剂的新化合物的方法。

43. 发明申请

US20060135467A1 Partial and full agonists of A1 adenosine receptors 审中-公开
标题翻译： A1腺苷受体的部分和完全激动剂
公开(公告)号：US20060135467A1
公开(公告)日：2006-06-22
申请号：US11355656
申请日：2006-02-15
申请人： Jeff Zablocki , Venkata Palle , Elfatih Elzein , Xiaofen Li
发明人： Jeff Zablocki , Venkata Palle , Elfatih Elzein , Xiaofen Li
IPC分类号： A61K31/7076 , C07H19/16
CPC分类号： C07H19/16
摘要： Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular the supraventricular tachycardias, emesis, angina, myocardial infarction and hyperlipidemia.
摘要翻译：公开了可用于治疗各种疾病状态，特别是室上性心动过速，呕吐，心绞痛，心肌梗死和高脂血症的部分和全部A 1 N 2腺苷受体激动剂的新化合物。

44. 发明申请

US20140135317A1 FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS 有权
标题翻译：熔融杂环化合物作为离子通道调节剂
公开(公告)号：US20140135317A1
公开(公告)日：2014-05-15
申请号：US14038646
申请日：2013-09-26
申请人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Dmitry Koltun , Xiaofen Li , Rubin Martinez , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
发明人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Dmitry Koltun , Xiaofen Li , Rubin Martinez , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
IPC分类号： C07D243/14 , C07D403/06
CPC分类号： C07D413/06 , A61K31/5513 , A61K31/553 , C07B59/002 , C07B2200/05 , C07D243/14 , C07D243/24 , C07D267/08 , C07D267/14 , C07D291/08 , C07D403/06 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/14 , C07D419/06 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
摘要翻译：本公开涉及作为钠通道抑制剂的化合物及其用于治疗各种疾病状态（包括心血管疾病和糖尿病）的用途。在具体实施方案中，化合物的结构由式I给出：其中Z 1，Z 2，Z 3，Z 4，X，Y，R 2，R 3和R 4如本文所述，用于制备和使用该化合物的方法，含有该组合物的药物组合物。

45. 发明申请

US20130005706A1 FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS 有权
公开(公告)号：US20130005706A1
公开(公告)日：2013-01-03
申请号：US13538307
申请日：2012-06-29
申请人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Dmitry Koltun , Xiaofen Li , Ruben Martinez , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
发明人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Dmitry Koltun , Xiaofen Li , Ruben Martinez , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
IPC分类号： A61K31/553 , C07D413/04 , C07D267/14 , C07D413/12 , C07D413/14 , A61P25/06 , A61P25/08 , A61P25/00 , A61P3/10 , A61P9/10 , A61P9/00 , A61P9/06 , A61P9/04 , A61P9/12 , C07D498/04
CPC分类号： C07D498/04 , C07D267/14 , C07D413/04 , C07D413/12 , C07D413/14
摘要： The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

46. 发明授权

US07521554B2 A2B adenosine receptor antagonists 有权
标题翻译： A2B腺苷受体拮抗剂
公开(公告)号：US07521554B2
公开(公告)日：2009-04-21
申请号：US11508592
申请日：2006-08-22
申请人： Elfatih Elzein , Rao Kalla , Tim Marquart , Jeff Zablocki , Xiaofen Li
发明人： Elfatih Elzein , Rao Kalla , Tim Marquart , Jeff Zablocki , Xiaofen Li
IPC分类号： C07D239/54 , C07D403/12
CPC分类号： C07D473/06 , C07D239/545 , C07D403/12 , C07D473/00 , C07D473/08
摘要： Disclosed are processes for the synthesis of novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
摘要翻译：公开了用于合成可用于治疗各种疾病状态（包括哮喘和腹泻）的A2B腺苷受体拮抗剂的新化合物的方法。

47. 发明授权

US07125993B2 A2B adenosine receptor antagonists 有权
标题翻译： A2B腺苷受体拮抗剂
公开(公告)号：US07125993B2
公开(公告)日：2006-10-24
申请号：US10719102
申请日：2003-11-21
申请人： Elfatih Elzein , Rao Kalla , Tim Marquart , Jeff Zablocki , Xiaofen Li
发明人： Elfatih Elzein , Rao Kalla , Tim Marquart , Jeff Zablocki , Xiaofen Li
IPC分类号： C07D473/04 , C07D473/06 , C07D473/08 , C07D247/02 , C07D239/545
CPC分类号： C07D473/06 , C07D239/545 , C07D403/12 , C07D473/00 , C07D473/08
摘要： Disclosed are processes for the synthesis of novel compounds that are A2B adenosine receptor antagonists, having the structure of Formula I or Formula II: by cyclizing a compound of the formula (3):
摘要翻译：公开了具有式I或式II结构的通过使式（3）的化合物环化合成作为A 2 B 2腺苷受体拮抗剂的新化合物的方法：

48. 发明授权

US08586732B2 Fused heterocyclic compounds as ion channel modulators 有权
公开(公告)号：US08586732B2
公开(公告)日：2013-11-19
申请号：US13538847
申请日：2012-06-29
申请人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Dmitry Koltun , Xiaofen Li , Ruben Martinez , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
发明人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Dmitry Koltun , Xiaofen Li , Ruben Martinez , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
IPC分类号： A61K31/00 , C07D267/02
CPC分类号： C07D413/06 , A61K31/5513 , A61K31/553 , C07B59/002 , C07B2200/05 , C07D243/14 , C07D243/24 , C07D267/08 , C07D267/14 , C07D291/08 , C07D403/06 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/14 , C07D419/06 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

49. 发明申请

US20120289493A1 FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS 有权
标题翻译：熔融杂环化合物作为离子通道调节剂
公开(公告)号：US20120289493A1
公开(公告)日：2012-11-15
申请号：US13466995
申请日：2012-05-08
申请人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Ruben Martinez , Gregory Notte , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
发明人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Ruben Martinez , Gregory Notte , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
IPC分类号： A61K31/53 , C07D401/10 , C07D403/10 , C07D413/06 , C07D413/14 , A61K31/5377 , C07D401/14 , A61K31/501 , A61K31/506 , C07D265/22 , A61K31/536 , C07D498/10 , A61K31/4725 , C07D417/06 , A61K31/5415 , A61P9/00 , A61P9/10 , A61P9/12 , A61P3/10 , A61P25/08 , A61P25/00 , C07D253/08
CPC分类号： C07D498/10 , C07D217/26 , C07D237/32 , C07D239/88 , C07D239/90 , C07D253/08 , C07D263/58 , C07D265/22 , C07D279/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D498/04
摘要： The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
摘要翻译：本公开涉及作为钠通道抑制剂的化合物及其用于治疗各种疾病状态（包括心血管疾病和糖尿病）的用途。在具体实施方案中，化合物的结构由式I给出：其中Q，R 1，X 1，X 2，Y和R 2如本文所述，用于制备和使用该化合物的方法以及含有该化合物的药物组合物。

50. 发明授权

US09115096B2 Fused heterocyclic compounds as ion channel modulators 有权
标题翻译：稠合杂环化合物作为离子通道调节剂
公开(公告)号：US09115096B2
公开(公告)日：2015-08-25
申请号：US13466995
申请日：2012-05-08
申请人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Ruben Martinez , Gregory Notte , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
发明人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Ruben Martinez , Gregory Notte , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
IPC分类号： C07D265/22 , C07D401/10 , C07D401/14 , C07D403/10 , C07D403/14 , C07D413/06 , C07D413/14 , A61K31/536 , A61K31/506 , A61K31/4427 , A61P25/08 , C07D498/04 , C07D498/14 , C07D253/08 , C07D237/32 , C07D239/88 , C07D239/90 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D405/12 , C07D417/06 , C07D417/14 , C07D217/26 , C07D413/12 , C07D498/10
CPC分类号： C07D498/10 , C07D217/26 , C07D237/32 , C07D239/88 , C07D239/90 , C07D253/08 , C07D263/58 , C07D265/22 , C07D279/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D498/04
摘要： The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
摘要翻译：本公开涉及作为钠通道抑制剂的化合物及其用于治疗各种疾病状态（包括心血管疾病和糖尿病）的用途。在具体实施方案中，化合物的结构由式I给出：其中Q，R 1，X 1，X 2，Y和R 2如本文所述，用于制备和使用化合物的方法以及含有该化合物的药物组合物。

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