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公开(公告)号：US20090209481A1
公开(公告)日：2009-08-20
申请号：US12313992
申请日：2008-11-26
IPC分类号： A61K31/7076 , C07H19/213 , C07H19/11 , A61P31/12 , A61K31/7072
摘要： Compounds having the formula I or II wherein R1, R2, B, and V are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
摘要翻译： 具有式I或II的化合物，其中R 1，R 2，B和V如本文所定义，是丙型肝炎病毒NS5b聚合酶抑制剂。 还公开了用于治疗HCV感染和抑制HCV复制的组合物和方法。
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公开(公告)号：US08063025B2
公开(公告)日：2011-11-22
申请号：US12313992
申请日：2008-11-26
摘要： Compounds having the formula I or II wherein R1, R2, B, and V are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
摘要翻译： 具有式I或II的化合物，其中R 1，R 2，B和V如本文所定义，是丙型肝炎病毒NS5b聚合酶抑制剂。 还公开了用于治疗HCV感染和抑制HCV复制的组合物和方法。
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公开(公告)号：US20120214769A1
公开(公告)日：2012-08-23
申请号：US13083321
申请日：2011-04-08
申请人： Jorge E. Gomez-Galeno , K. Raja Reddy , Paul D. van Poelje , Robert Huerta Lemus , Thanh Huu Nguyen , Matthew P. Grote , Qun Dang , Scott J. Hecker , Venkat Reddy Mali , Mingwei Chen , Zhili Sun , Serge Henri Boyer , Haiqing Li , William Craigo
发明人： Jorge E. Gomez-Galeno , K. Raja Reddy , Paul D. van Poelje , Robert Huerta Lemus , Thanh Huu Nguyen , Matthew P. Grote , Qun Dang , Scott J. Hecker , Venkat Reddy Mali , Mingwei Chen , Zhili Sun , Serge Henri Boyer , Haiqing Li , William Craigo
IPC分类号： A61K31/675 , A61K31/185 , C07D307/81 , A61K31/343 , C07D295/185 , A61K31/4965 , C07D213/75 , A61K31/4418 , C07D405/04 , A61K31/443 , C07D235/30 , A61K31/4184 , C07F9/655 , A61K31/665 , C07D471/04 , A61K31/437 , C07F9/40 , A61K31/662 , C07D295/135 , A61K31/5375 , C07D261/08 , A61K31/42 , C07F9/653 , A61P3/10 , A61P3/08 , A61P1/16 , A61P3/06 , A61P9/10 , A61P3/04 , A61P3/00 , C07C309/15
CPC分类号： C07C309/15 , C07C307/02 , C07C309/11 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07C2603/74 , C07D209/20 , C07D213/53 , C07D213/75 , C07D235/30 , C07D261/08 , C07D263/56 , C07D277/66 , C07D307/68 , C07D307/81 , C07D317/66 , C07D333/38 , C07D405/04 , C07D409/12 , C07D413/04 , C07D471/04 , C07D498/04
摘要： The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
摘要翻译： 本发明提供具有胰高血糖素受体拮抗剂或反向激动剂活性的新颖的式（I）化合物及其药学上可接受的盐和共晶体。 本发明进一步提供了包含其的药物组合物以及治疗，预防，延迟发病时间或降低其中指示一种或多种胰高血糖素受体拮抗剂的疾病或病症的发展或进展的风险的方法， 包括I型和II型糖尿病，胰岛素抵抗和高血糖。 本发明还提供制备式I化合物的方法，包括其盐和共结晶，以及包含其的药物组合物。
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公开(公告)号：US08710236B2
公开(公告)日：2014-04-29
申请号：US13083321
申请日：2011-04-08
申请人： Jorge E. Gomez-Galeno , K. Raja Reddy , Paul D. van Poelje , Robert Huerta Lemus , Thanh Huu Nguyen , Matthew P. Grote , Qun Dang , Scott J. Hecker , Venkat Reddy Mali , Mingwei Chen , Zhili Sun , Serge Henri Boyer , Haiqing Li , William Craigo
发明人： Jorge E. Gomez-Galeno , K. Raja Reddy , Paul D. van Poelje , Robert Huerta Lemus , Thanh Huu Nguyen , Matthew P. Grote , Qun Dang , Scott J. Hecker , Venkat Reddy Mali , Mingwei Chen , Zhili Sun , Serge Henri Boyer , Haiqing Li , William Craigo
IPC分类号： C07D263/57 , C07D307/81 , C07C309/15
CPC分类号： C07C309/15 , C07C307/02 , C07C309/11 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07C2603/74 , C07D209/20 , C07D213/53 , C07D213/75 , C07D235/30 , C07D261/08 , C07D263/56 , C07D277/66 , C07D307/68 , C07D307/81 , C07D317/66 , C07D333/38 , C07D405/04 , C07D409/12 , C07D413/04 , C07D471/04 , C07D498/04
摘要： The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
摘要翻译： 本发明提供具有胰高血糖素受体拮抗剂或反向激动剂活性的新颖的式（I）化合物及其药学上可接受的盐和共晶体。 本发明进一步提供了包含其的药物组合物以及治疗，预防，延迟发病时间或降低其中指示一种或多种胰高血糖素受体拮抗剂的疾病或病症的发展或进展的风险的方法， 包括I型和II型糖尿病，胰岛素抵抗和高血糖。 本发明还提供制备式I化合物的方法，包括其盐和共结晶，以及包含其的药物组合物。
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5.发明授权Cyclic phosphate diesters of 1,3-propane-1-aryl diols and their use in preparing prodrugs 有权1,3-丙烷-1-芳基二醇的环磷酸二酯及其在制备前药中的用途公开(公告)号：US07498320B2
公开(公告)日：2009-03-03
申请号：US11528283
申请日：2006-09-28
申请人： K. Raja Reddy , William Craigo , Zhili Sun , Serge Boyer , Bheemarao G. Ugarkar
发明人： K. Raja Reddy , William Craigo , Zhili Sun , Serge Boyer , Bheemarao G. Ugarkar
IPC分类号： A61K31/665 , C07F9/02
CPC分类号： C07F9/65742 , C07H19/04
摘要： Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs: wherein: V and L are trans relative to one another; V is selected from group consisting of carbocyclic aryl, substituted carbocyclic aryl, heteroaryl, and substituted heteroaryl; and L is a leaving group selected from the group consisting of halogen, alkyl sulfonate, aryloxy optionally substituted with 1-2 substituents, N-containing heteroaryl, and N-hydroxy-nitrogen containing heteroaryl; and salts thereof.
摘要翻译： 式I化合物，其制备方法和合成中间体及其在前体药物合成中的应用：其中：V和L相对于彼此是反式的; V选自碳环芳基，取代的碳环芳基，杂芳基和取代的杂芳基; 并且L是选自卤素，烷基磺酸酯，任选被1-2个取代基取代的芳氧基，含N杂芳基和N-羟基 - 含氮杂芳基的离去基团; 及其盐。
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6.发明授权公开(公告)号：US07148349B2
公开(公告)日：2006-12-12
申请号：US10698924
申请日：2003-10-31
申请人： K. Raja Reddy , William Craigo , Zhili Sun , Serge Boyer , Bheemarao G. Ugarkar
发明人： K. Raja Reddy , William Craigo , Zhili Sun , Serge Boyer , Bheemarao G. Ugarkar
IPC分类号： C07D239/02 , C07D487/06 , C07C9/02
CPC分类号： C07F9/65742 , C07H19/04
摘要： Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs: wherein: V and L are trans relative to one another; V is selected from group consisting of carbocyclic aryl, substituted carbocyclic aryl, heteroaryl, and substituted heteroaryl; and L is a leaving group selected from the group consisting of halogen, alkyl sulfonate, aryloxy optionally substituted with 1–2 substituents, N-containing heteroaryl, and N-hydroxy-nitrogen containing heteroaryl; and salts thereof.
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公开(公告)号：US20130030029A1
公开(公告)日：2013-01-31
申请号：US13058604
申请日：2009-08-13
申请人： Jorge E. Gomez-Galeno , Scott J. Hecker , Qun Dang , Mali Venkat Reddy , Zhili Sun , Matthew P. Grote , Thanh Huu Nguyen , Robert Huerta Lemus , Haiqing Li
发明人： Jorge E. Gomez-Galeno , Scott J. Hecker , Qun Dang , Mali Venkat Reddy , Zhili Sun , Matthew P. Grote , Thanh Huu Nguyen , Robert Huerta Lemus , Haiqing Li
IPC分类号： A61K31/167 , A61P3/10 , A61K31/423 , C07C309/15 , C07D263/57
CPC分类号： C07C309/15 , A61K31/185 , A61K31/423 , A61K45/06 , C07B2200/07 , C07C2601/14 , C07C2601/16 , C07D263/57
摘要： Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or Co-crystals and prodrugs thereof. Formula I
摘要翻译： 本文提供了具有胰高血糖素受体拮抗剂或反向激动剂活性的化合物，包括其对映体纯的形式及其药学上可接受的盐或共晶体和前药。 此外，本文提供的是包含其的药物组合物以及治疗，预防，延迟发病时间或降低发生或进展一种或多种胰高血糖素受体拮抗剂的疾病或病症的风险的方法，包括 I型和II型糖尿病，胰岛素抵抗和高血糖。 此外，本文提供了制备或制备本文公开的化合物的方法，包括其对映体纯的形式，及其药学上可接受的盐或共晶体和前药。 一级方程式
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公开(公告)号：US08907103B2
公开(公告)日：2014-12-09
申请号：US13058604
申请日：2009-08-13
申请人： Jorge E. Gomez-Galeno , Scott J. Hecker , Qun Dang , Mali Venkat Reddy , Zhili Sun , Matthew P. Grote , Thanh Huu Nguyen , Robert Huerta Lemus , Haiqing Li
发明人： Jorge E. Gomez-Galeno , Scott J. Hecker , Qun Dang , Mali Venkat Reddy , Zhili Sun , Matthew P. Grote , Thanh Huu Nguyen , Robert Huerta Lemus , Haiqing Li
IPC分类号： C07D263/57 , C07D307/81 , C07C309/15
CPC分类号： C07C309/15 , A61K31/185 , A61K31/423 , A61K45/06 , C07B2200/07 , C07C2601/14 , C07C2601/16 , C07D263/57
摘要： Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or Co-crystals and prodrugs thereof. Formula I
摘要翻译： 本文提供了具有胰高血糖素受体拮抗剂或反向激动剂活性的化合物，包括其对映体纯的形式及其药学上可接受的盐或共晶体和前药。 此外，本文提供的是包含其的药物组合物以及治疗，预防，延迟发病时间或降低发生或进展一种或多种胰高血糖素受体拮抗剂的疾病或病症的风险的方法，包括 I型和II型糖尿病，胰岛素抵抗和高血糖。 此外，本文提供了制备或制备本文公开的化合物的方法，包括其对映体纯的形式，及其药学上可接受的盐或共晶体和前药。 一级方程式
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公开(公告)号：US08868988B2
公开(公告)日：2014-10-21
申请号：US13260045
申请日：2009-11-16
申请人： Zhili Sun , Jun Xu , Jin Xu , Zhifeng Yuan , Qianzi Xu , Xianwei Gong , Bo Sun , Huiying Fang
发明人： Zhili Sun , Jun Xu , Jin Xu , Zhifeng Yuan , Qianzi Xu , Xianwei Gong , Bo Sun , Huiying Fang
IPC分类号： G06F11/00
CPC分类号： H04L1/1819 , H04L1/0066 , H04L1/0068 , H04L1/0071
摘要： The present invention discloses a rate matching method and device. The method includes that: an information bit sequence is coded and interleaved to obtain a mother code codeword with a length NFB—Buffer; and bits are selected from the mother code codeword to generate a hybrid automatic repeat request (HARQ) subpacket for current transmission. By means of the present invention, the effect of covering the whole mother code area can be achieved as much as possible, and the performance of the HARQ multiple retransmission link can be enhanced.
摘要翻译： 本发明公开了一种速率匹配方法和装置。 该方法包括：对信息比特序列进行编码和交织以获得长度为NFB-Buffer的母码码字; 并且从母码码字中选择比特以产生用于当前传输的混合自动重传请求（HARQ）子分组。 通过本发明，可以尽可能地实现覆盖整个母码区域的效果，并且可以提高HARQ多重传输链路的性能。
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公开(公告)号：US20120110406A1
公开(公告)日：2012-05-03
申请号：US13260045
申请日：2009-11-16
申请人： Zhili Sun , Jun Xu , Jin Xu , Zhifeng Yuan , Qianzi Xu , Xianwei Gong , Bo Sun , Huiying Fang
发明人： Zhili Sun , Jun Xu , Jin Xu , Zhifeng Yuan , Qianzi Xu , Xianwei Gong , Bo Sun , Huiying Fang
CPC分类号： H04L1/1819 , H04L1/0066 , H04L1/0068 , H04L1/0071
摘要： The present invention discloses a rate matching method and device. The method includes that: an information bit sequence is coded and interleaved to obtain a mother code codeword with a length NFB—Buffer; and bits are selected from the mother code codeword to generate a hybrid automatic repeat request (HARQ) subpacket for current transmission. By means of the present invention, the effect of covering the whole mother code area can be achieved as much as possible, and the performance of the HARQ multiple retransmission link can be enhanced.
摘要翻译： 本发明公开了一种速率匹配方法和装置。 该方法包括：对信息比特序列进行编码和交织以获得长度为NFB-Buffer的母码码字; 并且从母码码字中选择比特以产生用于当前传输的混合自动重传请求（HARQ）子分组。 通过本发明，可以尽可能地实现覆盖整个母码区域的效果，并且可以提高HARQ多重传输链路的性能。
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