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21. 发明申请

WO2012154760A1 FUSED HETEROCYCLIC COMPOUNDS AS SODIUM CHANNEL MODULATORS 审中-公开
标题翻译：熔融杂环化合物作为钠通道调节剂
公开(公告)号：WO2012154760A1
公开(公告)日：2012-11-15
申请号：PCT/US2012/036976
申请日：2012-05-08
申请人： GILEAD SCIENCES, INC. , CORKEY, Britton Kenneth , ELZEIN, Elfatih , JIANG, Robert H. , KALLA, Rao V. , KOBAYASHI, Tetsuya , KOLTUN, Dmitry , LI, Xiaofen , MARTINEZ, Ruben , NOTTE, Gregory , PARKHILL, Eric Q. , PERRY, Thao , ZABLOCKI, Jeff , VENKATARAMANI, Chandrasekar , GRAUPE, Michael , GUERRERO, Juan
发明人： CORKEY, Britton Kenneth , ELZEIN, Elfatih , JIANG, Robert H. , KALLA, Rao V. , KOBAYASHI, Tetsuya , KOLTUN, Dmitry , LI, Xiaofen , MARTINEZ, Ruben , NOTTE, Gregory , PARKHILL, Eric Q. , PERRY, Thao , ZABLOCKI, Jeff , VENKATARAMANI, Chandrasekar , GRAUPE, Michael , GUERRERO, Juan
IPC分类号： C07D237/32 , C07D253/08 , C07D265/22 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D403/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06
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, R 1 , X 1 , X 2 , Y and R 2 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相同。

22. 发明申请

WO2009137201A1 TRIAZOLOPYRIDINONE DERIVATIVES FOR USE AS STEAROYL COA DESATURASE INHIBITORS 审中-公开
标题翻译：用作硬脂酸脱乙酰酶抑制剂的三唑吡啶酮衍生物
公开(公告)号：WO2009137201A1
公开(公告)日：2009-11-12
申请号：PCT/US2009/039503
申请日：2009-04-03
申请人： CV THERAPEUTICS, INC. , KOLTUN, Dmitry , ZABLOCKI, Jeff
发明人： KOLTUN, Dmitry , ZABLOCKI, Jeff
IPC分类号： C07D471/04 , A61P3/00 , A61K31/437 , A61P3/06 , A61P35/00 , A61P9/00
CPC分类号： C07D471/04
摘要： The present invention discloses triazolopyridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.
摘要翻译：本发明公开了用作具有式I结构的硬脂酰CoA去饱和酶抑制剂的三氮代吡啶酮衍生物：该化合物可用于治疗和/或预防由硬脂酰辅酶A去饱和酶（SCD）酶介导的各种人类疾病，特别是疾病相关心血管疾病，糖尿病，肥胖症，代谢综合症等。

23. 发明申请

WO2007002867A1 ABCA1 ELEVATING COMPOUNDS 审中-公开
标题翻译： ABCA1发光化合物
公开(公告)号：WO2007002867A1
公开(公告)日：2007-01-04
申请号：PCT/US2006/025468
申请日：2006-06-28
申请人： CV THERAPEUTICS, INC. , ABELMAN, Matthew , JIANG, Robert , ZABLOCKI, Jeff , KOLTUN, Dmitry
发明人： ABELMAN, Matthew , JIANG, Robert , ZABLOCKI, Jeff , KOLTUN, Dmitry
IPC分类号： C07D491/04 , A61K31/436 , A61P9/10 , C07D495/04
CPC分类号： C07D491/052
摘要： The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCAl production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
摘要翻译：本发明提供了可用于增加哺乳动物中细胞ATP结合盒转运蛋白ABCA1产生的化合物，以及使用这些化合物治疗冠状动脉疾病，血脂异常和代谢综合征的方法。本发明还涉及制备这些化合物的方法以及含有它们的药物组合物。

24. 发明申请

WO2006138376A1 PRODRUGS OF A2B ADENOSINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译： A2B腺苷受体拮抗剂的研究进展
公开(公告)号：WO2006138376A1
公开(公告)日：2006-12-28
申请号：PCT/US2006/023167
申请日：2006-06-14
申请人： CV THERAPEUTICS, INC. , KOLTUN, Dmitry , ZABLOCKI, Jeff , KALLA, Rao
发明人： KOLTUN, Dmitry , ZABLOCKI, Jeff , KALLA, Rao
IPC分类号： C07D473/06 , A61K31/522
CPC分类号： C07F9/65616 , C07D473/06
摘要： Disclosed are prodrugs of A 2B adenosine receptor antagonists, and their use in treating mammals for various disease states.
摘要翻译：公开了Aβ2A腺苷受体拮抗剂的前药，以及它们用于治疗各种疾病状态的哺乳动物。

25. 发明申请

WO2006125190A1 A1 ADENOSINE RECEPTOR AGONISTS 审中-公开
标题翻译： A1腺苷受体激动剂
公开(公告)号：WO2006125190A1
公开(公告)日：2006-11-23
申请号：PCT/US2006/019599
申请日：2006-05-19
申请人： CV THERAPEUTICS, INC. , ELZEIN, Elfatih , KALLA, Rao , PERRY, Thao , ZABLOCKI, Jeff , LI, Xiaofen
发明人： ELZEIN, Elfatih , KALLA, Rao , PERRY, Thao , ZABLOCKI, Jeff , LI, Xiaofen
IPC分类号： C07H19/16 , A61K31/7076
CPC分类号： C07H19/16
摘要： Disclosed are novel compounds that are partial and foil A 1 adenosine receptor agonists having the structure of Formula (I) : which are useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.
摘要翻译：公开了具有式（I）结构的部分和箔A 1 N 2腺苷受体激动剂的新化合物：其可用于治疗各种疾病状态，特别是心动过速和心房扑动，心绞痛和心肌梗死。

26. 发明申请

WO2005009445A1 A1 ADENOSINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译： A1腺苷受体拮抗剂
公开(公告)号：WO2005009445A1
公开(公告)日：2005-02-03
申请号：PCT/US2004/023632
申请日：2004-07-22
申请人： CV THERAPEUTICS, INC. , ZABLOCKI, Jeff , KALLA, Rao , ZENG, Dewan
发明人： ZABLOCKI, Jeff , KALLA, Rao , ZENG, Dewan
IPC分类号： A61K31/52
CPC分类号： A61K31/52
摘要： Disclosed are novel methods of antagonizing the A 1 adenosine receptor in a mammal, comprising administering to a mammal in need thereof a therapeutically effective dose of a compound of the formula: (Formula I ) wherein R 1 is optionally substituted C 1-4 alkyl; Y is C 1-4 alkylene; and Z is phenyl that is optionally substituted with halo, hydroxy, amino, cyano, or optionally substituted C 1-4 alkyl or a pharmaceutically acceptable salt, ester, or prodrug thereof. The A 1 adenosine receptors are antagonized in order to treat a disease state is chosen from renal failure, renal dysfunction, nephritis, hypertension, oedema, Alzheimers disease, stress, depression, cardiac arrhythmia, restoration of cardiac function, congestive heart failure, diabetes, asthma, respiratory disorders, ischaemia-induced injury of the brain, heart and kidney, and diarrhea.
摘要翻译：公开了一种拮抗哺乳动物中的A1腺苷受体的新方法，包括向有需要的哺乳动物施用治疗有效剂量的下式化合物（式I），其中R 1为任选取代的C 1-4烷基; Y为C 1-4亚烷基; 并且Z是任选被卤素，羟基，氨基，氰基或任选取代的C 1-4烷基取代的苯基或其药学上可接受的盐，酯或前药。 A1腺苷受体被拮抗以治疗疾病状态，选自肾衰竭，肾功能不全，肾炎，高血压，水肿，阿尔茨海默病，压力，抑郁，心律失常，心脏功能恢复，充血性心力衰竭，糖尿病，哮喘，呼吸障碍，局部缺血引起的脑，心脏和肾脏的损伤以及腹泻。

27. 发明申请

WO2005000826A1 UREA DERIVATIVES OF PIPERAZINES AND PIPERIDINES AS FATTY ACID OXIDATION INHIBITORS 审中-公开
标题翻译：作为脂肪酸氧化抑制剂的哌啶和哌啶的尿素衍生物
公开(公告)号：WO2005000826A1
公开(公告)日：2005-01-06
申请号：PCT/US2004/017999
申请日：2004-06-07
申请人： CV THERAPEUTICS, INC. , ZABLOCKI, Jeff , ELZEIN, Elfatih , MARQUART, Tim
发明人： ZABLOCKI, Jeff , ELZEIN, Elfatih , MARQUART, Tim
IPC分类号： C07D277/64
CPC分类号： C07D295/21 , C07D211/58 , C07D277/64 , C07D417/12
摘要： Disclosed are novel piperazine derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction.
摘要翻译：公开了可用于治疗各种疾病状态，特别是心血管疾病如心房和室性心律失常，间歇性跛行，Prinzmetal（变体）心绞痛，稳定和不稳定心绞痛，运动诱发的心绞痛，充血性心脏病和心肌的新型哌嗪衍生物梗死。

28. 发明申请

WO2004067506A2 SUBSTITUTED HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：取代的杂环化合物
公开(公告)号：WO2004067506A2
公开(公告)日：2004-08-12
申请号：PCT/US2004/001096
申请日：2004-01-16
申请人： CV THERAPEUTICS INC. , IBRAHIM, Prabha , SHENK, Kevin , ELZEIN, Elfatih , PALLE, Venkata , ZABLOCKI, Jeff , REHDER, Kenneth
发明人： IBRAHIM, Prabha , SHENK, Kevin , ELZEIN, Elfatih , PALLE, Venkata , ZABLOCKI, Jeff , REHDER, Kenneth
IPC分类号： C07D
CPC分类号： C07D233/70 , C07D235/04 , C07D235/18 , C07D263/57 , C07D271/06 , C07D277/34 , C07D277/64 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes, and for increasing HDL plasma levels in mammals.
摘要翻译：公开了可用于治疗各种疾病状态，特别是心血管疾病如心房和室性心律失常，间歇性跛行，Prinzmetal（变体）心绞痛，稳定和不稳定型心绞痛，运动诱发的心绞痛，充血性心脏病和心肌的新型杂环衍生物梗死。该化合物还可用于治疗糖尿病，并且用于增加哺乳动物的HDL血浆水平。

29. 发明申请

WO2013033377A1 ALDH-2 INHIBITORS IN THE TREATMENT OF ADDICTION 审中-公开
标题翻译： ALDH-2抑制剂在治疗中的应用
公开(公告)号：WO2013033377A1
公开(公告)日：2013-03-07
申请号：PCT/US2012/053110
申请日：2012-08-30
申请人： GILEAD SCIENCES, INC. , GRAUPE, Michael , VENKATARAMANI, Chandrasekar , ZABLOCKI, Jeff
发明人： GRAUPE, Michael , VENKATARAMANI, Chandrasekar , ZABLOCKI, Jeff
IPC分类号： C07D311/36 , C07D405/06 , A61K31/352 , A61K31/397 , A61K31/4178
CPC分类号： C07D311/36 , C07D405/06 , C07D405/10
摘要： Disclosed are novel isoflavone derivatives having the structure of Formula (I) which are ALDH-2 inhibitors, useful for treating a patient in need thereof, for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.
摘要翻译：公开了具有式（I）结构的新型异黄酮衍生物，其是用于治疗有需要的患者的依赖于成瘾药物的ALDH-2抑制剂，例如对多巴胺产生剂如可卡因，吗啡，安非他明，尼古丁和酒精。

30. 发明申请

WO2008077050A1 ADENOSINE DERIVATIVES AS PARTIAL AND FULL AGONISTS OF A1 ADENOSINE RECEPTORS 审中-公开
标题翻译：腺苷衍生物作为A1腺苷受体的部分和全部激素
公开(公告)号：WO2008077050A1
公开(公告)日：2008-06-26
申请号：PCT/US2007/087957
申请日：2007-12-18
申请人： CV THERAPEUTICS, INC. , DHALLA, Arvinder , ELZEIN, Elfatih , IBRAHIM, Prabha , PALLE, Venkata , VARKHEDKAR, Vaibhav , ZABLOCKI, Jeff
发明人： DHALLA, Arvinder , ELZEIN, Elfatih , IBRAHIM, Prabha , PALLE, Venkata , VARKHEDKAR, Vaibhav , ZABLOCKI, Jeff
IPC分类号： A61K31/52 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P15/08 , A61P25/08
CPC分类号： A61K31/52 , A61K31/7076
摘要： Disclosed are novel compounds a compound of Formula I that are partial and full A 1 adenosine receptor agonists, useful for treating various disease states, in particular dyslipidemia, diabetes, decreased insulin sensitivity, Polycystic Ovarian Syndrome, Stein-Leventhal syndrome, and obesity.
摘要翻译：公开了作为部分和全部A 1 N 2腺苷受体激动剂的新颖化合物，其可用于治疗各种疾病状态，特别是血脂异常，糖尿病，胰岛素敏感性降低，多囊卵巢综合征，Stein- Leventhal综合征和肥胖症。

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