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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
Applicant: GILEAD SCIENCES, INC. , GRAUPE, Michael , VENKATARAMANI, Chandrasekar , ZABLOCKI, Jeff
Inventor： GRAUPE, Michael , VENKATARAMANI, Chandrasekar , ZABLOCKI, Jeff
IPC: C07D311/36 , C07D405/06 , A61K31/352 , A61K31/397 , A61K31/4178
CPC classification number: C07D311/36 , C07D405/06 , C07D405/10
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：WO2010144371A1
公开(公告)日：2010-12-16
申请号：PCT/US2010/037647
申请日：2010-06-07
Applicant: GILEAD COLORADO, INC. , GRAUPE, Michael , VENKATARAMANI, Chandrasekar
Inventor： GRAUPE, Michael , VENKATARAMANI, Chandrasekar
IPC: C07C271/22 , C07D211/76 , C07D333/46 , C07D207/27 , C07D295/108 , C07D295/125 , A61K31/4965
CPC classification number: C07C271/22 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/475 , A61K31/496 , A61K31/513 , A61K31/519 , A61K31/52 , A61K31/5375 , A61K31/5377 , A61K31/573 , A61K31/655 , A61K31/661 , A61K31/704 , A61K31/7068 , C07D207/27 , C07D211/76 , C07D295/108 , C07D295/125 , C07D333/46
Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
Abstract translation: 本发明提供具有组蛋白脱乙酰酶（HDAC）抑制活性的通式（I）的化合物，包含该化合物的药物组合物和可用于使用该化合物治疗疾病的方法。
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公开(公告)号：WO2010009155A2
公开(公告)日：2010-01-21
申请号：PCT/US2009050577
申请日：2009-07-14
Applicant: GILEAD COLORADO INC , MELVIN LAWRENCE S JR , GRAUPE MICHAEL , VENKATARAMANI CHANDRASEKAR
Inventor： MELVIN LAWRENCE S JR , GRAUPE MICHAEL , VENKATARAMANI CHANDRASEKAR
IPC: C07D471/04 , A61K31/506 , A61P35/00 , C07D487/04
CPC classification number: C07D487/04 , C07D471/04
Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound. Formula (I)
Abstract translation: 本发明提供具有组蛋白脱乙酰酶（HDAC）和/或细胞周期蛋白依赖性激酶（CDK）抑制活性的通式（I）的化合物，包含该化合物的药物组合物和可用于治疗使用该化合物的疾病的方法。 式（I）
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公开(公告)号：WO2010144378A3
公开(公告)日：2011-04-07
申请号：PCT/US2010037661
申请日：2010-06-07
Applicant: GILEAD COLORADO INC , VENKATARAMANI CHANDRASEKAR
Inventor： VENKATARAMANI CHANDRASEKAR
IPC: C07C235/78 , A61K31/167 , C07C235/84 , C07C237/28 , C07C237/42 , C07C271/24 , C07C275/26 , C07D207/26 , C07D211/58 , C07D333/20
CPC classification number: C07C271/24 , C07C237/42 , C07C275/26 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/26 , C07D207/27 , C07D211/58 , C07D211/66 , C07D333/20 , C07D333/24 , C07D333/28 , C07D401/04
Abstract: The present invention provides a compound of general Formula (I) having histone deacctylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
Abstract translation: 本发明提供具有组蛋白脱钙酶（HDAC）抑制活性的通式（I）的化合物，包含该化合物的药物组合物和可用于使用该化合物治疗疾病的方法。
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公开(公告)号：WO2010144378A2
公开(公告)日：2010-12-16
申请号：PCT/US2010/037661
申请日：2010-06-07
Applicant: GILEAD COLORADO, INC. , VENKATARAMANI, Chandrasekar
Inventor： VENKATARAMANI, Chandrasekar
IPC: C07C235/78
CPC classification number: C07C271/24 , C07C237/42 , C07C275/26 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/26 , C07D207/27 , C07D211/58 , C07D211/66 , C07D333/20 , C07D333/24 , C07D333/28 , C07D401/04
Abstract: The present invention provides a compound of general Formula (I) having histone deacctylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
Abstract translation: 本发明提供具有组蛋白脱钙酶（HDAC）抑制活性的通式（I）的化合物，包含该化合物的药物组合物和可用于使用该化合物治疗疾病的方法。
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Patent Agency Ranking6.发明申请
公开(公告)号：WO2010009139A3
公开(公告)日：2010-07-08
申请号：PCT/US2009050558
申请日：2009-07-14
Applicant: GILEAD COLORADO INC , VENKATARAMANI CHANDRASEKAR
Inventor： VENKATARAMANI CHANDRASEKAR
IPC: C07D403/04 , A61K31/506 , A61K31/53 , A61P3/00 , A61P25/00 , C07D409/14 , C07D417/14
CPC classification number: C07D403/04 , C07D409/14 , C07D417/14
Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin- dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
Abstract translation: 具有组蛋白脱乙酰酶（HDAC）和/或细胞周期蛋白依赖性激酶（CDK）抑制活性的通式（I）的化合物，包含该化合物的药物组合物和可用于使用该化合物治疗疾病的方法。
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公开(公告)号：WO2010009155A3
公开(公告)日：2010-01-21
申请号：PCT/US2009/050577
申请日：2009-07-14
Applicant: GILEAD COLORADO, INC. , MELVIN, Lawrence, S., Jr. , GRAUPE, Michael , VENKATARAMANI, Chandrasekar
IPC: C07D471/04 , C07D487/04 , A61K31/506 , A61P35/00
Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound. Formula (I)
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公开(公告)号：WO2013006463A1
公开(公告)日：2013-01-10
申请号：PCT/US2012/045021
申请日：2012-06-29
Applicant: GILEAD SCIENCES, INC. , CORKEY, Britton, Kenneth , ELZEIN, Elfatih , JIANG, Robert, H. , KALLA, Rao, V. , KOLTUN, Dmitry , LI, Xiaofen , MARTINEZ, Ruben , PARKHILL, Eric, Q. , PERRY, Thao , ZABLOCKI, Jeff , VENKATARAMANI, Chandrasekar , GRAUPE, Michael , GUERRERO, Juan
Inventor： CORKEY, Britton, Kenneth , ELZEIN, Elfatih , JIANG, Robert, H. , KALLA, Rao, V. , KOLTUN, Dmitry , LI, Xiaofen , MARTINEZ, Ruben , PARKHILL, Eric, Q. , PERRY, Thao , ZABLOCKI, Jeff , VENKATARAMANI, Chandrasekar , GRAUPE, Michael , GUERRERO, Juan
IPC: C07D267/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D498/04 , A61K31/553
CPC classification number: C07D498/04 , C07D267/14 , C07D413/04 , C07D413/12 , C07D413/14
Abstract: 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, R 1 and R 3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
Abstract translation: 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Y，Z，n，R 1和R 3如本文所述，涉及化合物的制备和使用方法以及含有该化合物的药物组合物。
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公开(公告)号：WO2013006400A1
公开(公告)日：2013-01-10
申请号：PCT/US2012/044809
申请日：2012-06-29
Applicant: GILEAD SCIENCES, INC. , CANNIZZARO, Carina, E. , GRAUPE, Michael , GUERRERO, Juan, A. , LU, Yafan , STRICKLEY, Robert, G. , VENKATARAMANI, Chandrasekar , ZABLOCKI, Jeff
Inventor： CANNIZZARO, Carina, E. , GRAUPE, Michael , GUERRERO, Juan, A. , LU, Yafan , STRICKLEY, Robert, G. , VENKATARAMANI, Chandrasekar , ZABLOCKI, Jeff
IPC: C07D213/64 , A61K31/4418 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36
CPC classification number: A61K31/675 , A61K31/4418 , C07D213/64 , C07F9/581 , C07F9/584
Abstract: Disclosed are novel compounds having the structure of Formula (I) : which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
Abstract translation: 公开了具有式（I）结构的新化合物：其可用于治疗依赖于成瘾物质的哺乳动物，例如对多巴胺产生剂如可卡因，吗啡，苯丙胺，尼古丁和/或醇的成瘾。 还公开了包含治疗有效量的式（I）化合物和使用式（I）化合物治疗对多巴胺生成剂成瘾的方法的药物组合物。
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公开(公告)号：WO2010132601A1
公开(公告)日：2010-11-18
申请号：PCT/US2010/034600
申请日：2010-05-12
Applicant: GILEAD SCIENCES, INC. , GUO, Hongyan , KATO, Darryl , KIRSCHBERG, Thorsten, A. , LIU, Hongtao , LINK, John, O. , MITCHELL, Michael, L. , PARRISH, Jay, P. , SQUIRES, Neil , SUN, Jianyu , TAYLOR, James , BACON, Elizabeth, M. , CANALES, Eda , CHO, Aesop , KIM, Choung, U. , COTTELL, Jeromy, J. , DESAI, Manoj, C. , HALCOMB, Randall, L. , KRYGOWSKI, Evan, S. , LAZERWITH, Scott, E. , LIU, Qi , MACKMAN, Richard , PYUN, Hyung-Jung , SAUGIER, Joseph, H. , TRENKLE, James, D. , TSE, Winston, C. , VIVIAN, Randall, W. , SCHROEDER, Scott, D. , WATKINS, William, J. , XU, Lianhong , YANG, Zheng-Yu , KELLAR, Terry , SHENG, Xiaoning , CLARKE, Michael, O'Neil, Hanrahan , CHOU, Chien-hung , GRAUPE, Michael , JIN, Haolun , MCFADDEN, Ryan , MISH, Michael, R. , METOBO, Samuel, E. , PHILLIPS, Barton, W. , VENKATARAMANI, Chandrasekar
Inventor： GUO, Hongyan , KATO, Darryl , KIRSCHBERG, Thorsten, A. , LIU, Hongtao , LINK, John, O. , MITCHELL, Michael, L. , PARRISH, Jay, P. , SQUIRES, Neil , SUN, Jianyu , TAYLOR, James , BACON, Elizabeth, M. , CANALES, Eda , CHO, Aesop , COTTELL, Jeromy, J. , DESAI, Manoj, C. , HALCOMB, Randall, L. , KRYGOWSKI, Evan, S. , LAZERWITH, Scott, E. , LIU, Qi , MACKMAN, Richard , PYUN, Hyung-Jung , SAUGIER, Joseph, H. , TRENKLE, James, D. , TSE, Winston, C. , VIVIAN, Randall, W. , SCHROEDER, Scott, D. , WATKINS, William, J. , XU, Lianhong , YANG, Zheng-Yu , KELLAR, Terry , SHENG, Xiaoning , CLARKE, Michael, O'Neil, Hanrahan , CHOU, Chien-hung , GRAUPE, Michael , JIN, Haolun , MCFADDEN, Ryan , MISH, Michael, R. , METOBO, Samuel, E. , PHILLIPS, Barton, W. , VENKATARAMANI, Chandrasekar
IPC: C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D495/04 , A61K31/4188 , A61K31/4178 , A61P31/12
CPC classification number: C07D403/14 , A61K31/4025 , A61K31/4178 , A61K31/4184 , A61K31/427 , A61K31/435 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K45/06 , A61P31/12 , C07D207/16 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D491/113 , C07D495/04 , C07F5/025
Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
Abstract translation: 本发明涉及抗病毒化合物，含有这些化合物的组合物和包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。
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