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31. 发明申请

US20080070868A1 Novel Thiazole Inhibitors of Fructose 1,6-bisphosphatase 审中-公开
标题翻译：新型噻唑果糖1,6-二磷酸酶抑制剂
公开(公告)号：US20080070868A1
公开(公告)日：2008-03-20
申请号：US11841840
申请日：2007-08-20
申请人： Qun Dang , Joseph Kopcho , Scott Hecker , Bheemarao Ugarkar
发明人： Qun Dang , Joseph Kopcho , Scott Hecker , Bheemarao Ugarkar
IPC分类号： A61K31/675 , A61P3/08 , C07F9/02
CPC分类号： C07F9/65586 , C12N9/99
摘要： Compounds of Formula I, their prodrugs and salts, their preparation and their uses are described.
摘要翻译：描述了式I化合物，其前体药物和盐，其制备方法及用途。

32. 发明申请

US20150274739A1 2'-CYANO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 有权
标题翻译： 2'-氰基取代的核苷衍生物及其用于治疗病毒性疾病的方法
公开(公告)号：US20150274739A1
公开(公告)日：2015-10-01
申请号：US14436697
申请日：2013-10-11
申请人： Vinay Girijavallabhan , Stephane Bogen , Weidong Pan , Qun Dang , Ian Davies
发明人： Vinay Girijavallabhan , Stephane Bogen , Weidong Pan , Qun Dang , Ian Davies
IPC分类号： C07D487/04 , C07F9/6561 , A61K31/7056 , A61K45/06 , A61K47/48 , A61K38/21 , A61K31/706 , C07F9/6574
CPC分类号： C07D487/04 , A61K31/7056 , A61K31/706 , A61K38/212 , A61K45/06 , A61K47/48215 , A61K47/60 , C07F9/65616 , C07F9/65744 , A61K2300/00
摘要： Compounds of Formula (I) are disclosed, wherein R1, R2, R3, R4, R5, and R18 are defined herein. The compounds encompassed by Formula (I) include compounds which are HCV NS5B inhibitors and other compounds which can be metabolized in vivo to HCV NS5B inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HCV and the prophylaxis, treatment, or delay in the onset of disease caused by HCV. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：公开了式（I）的化合物，其中R 1，R 2，R 3，R 4，R 5和R 18在本文中定义。由式（I）包括的化合物包括HCV NS5B抑制剂和可以在体内被代谢为HCV NS5B抑制剂的其它化合物。该化合物及其药学上可接受的盐可用于预防或治疗HCV的感染以及由HCV引起的疾病发作的预防，治疗或延迟。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

33. 发明授权

US09006433B2 Substituted pyrimidines 有权
公开(公告)号：US09006433B2
公开(公告)日：2015-04-14
申请号：US13635275
申请日：2011-04-18
申请人： Changyou Zhou , Wuxin Zou , Yuxia Hua , Qun Dang
发明人： Changyou Zhou , Wuxin Zou , Yuxia Hua , Qun Dang
IPC分类号： A61K31/506 , C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14
摘要： The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.

34. 发明申请

US20140249130A1 BIPYRIDYLAMINOPYRIDINES AS SYK INHIBITORS 有权
标题翻译： BIPYRIDYLAMINOPYRIDINES作为SYK抑制剂
公开(公告)号：US20140249130A1
公开(公告)日：2014-09-04
申请号：US14116199
申请日：2012-05-04
申请人： Denis Deschenes , Michael D. Altman , John Michael Ellis , Christian Fischer , Andrew M. Haidle , Solomon D. Kattar , Alan B. Northrup , Adam J. Schell , Graham F. Smith , Brandon M. Taoka , Corey Bienstock , Maria Emilia Di Francesco , Anthony Donofrio , Scott Peterson , Kerrie B. Spencer , James Patrick Jewell , Amjad Ali , David Jonathan Bennett , Qun Dang , John Wai
发明人： Denis Deschenes , Michael D. Altman , John Michael Ellis , Christian Fischer , Andrew M. Haidle , Solomon D. Kattar , Alan B. Northrup , Adam J. Schell , Graham F. Smith , Brandon M. Taoka , Corey Bienstock , Maria Emilia Di Francesco , Anthony Donofrio , Scott Peterson , Kerrie B. Spencer , James Patrick Jewell , Amjad Ali , David Jonathan Bennett , Qun Dang , John Wai
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D401/12 , C07D409/14 , C07D417/14 , C07D471/04
摘要： The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.
摘要翻译：本发明提供了式I的新型嘧啶胺，其是脾脏酪氨酸激酶的有效抑制剂，或其前药，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD和类风湿性关节炎和癌症。

35. 发明申请

US20140154211A1 2'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 有权
标题翻译： 2'-取代的核苷衍生物及其用于治疗病毒性疾病的方法
公开(公告)号：US20140154211A1
公开(公告)日：2014-06-05
申请号：US14111687
申请日：2012-04-11
申请人： Vinay Girijavallabhan , F. George Njoroge , Stephane Bogen , Vishal Verma , Frank Bennett , Angela Kereles , Ashok Arasappan , Dmitri Pissarnitski , Qun Dang , Ian Davies , David B. Olsen , Andrew Stamford , Joseph P. Vacca
发明人： Vinay Girijavallabhan , F. George Njoroge , Stephane Bogen , Vishal Verma , Frank Bennett , Angela Kereles , Ashok Arasappan , Dmitri Pissarnitski , Qun Dang , Ian Davies , David B. Olsen , Andrew Stamford , Joseph P. Vacca
IPC分类号： A61K31/7072 , A61K31/7068 , A61K45/06 , C07H17/02
CPC分类号： A61K31/7072 , A01N47/36 , A61K31/7042 , A61K31/7068 , A61K45/06 , A61P31/14 , C07H17/02 , C07H19/10 , C07H19/11 , C07H19/207 , C07H19/213 , A01N2300/00 , A01N43/54 , A01N43/56 , A01N43/653 , A01N43/76 , A01N43/82 , A01N43/84 , A01N43/90
摘要： The present invention relates to 2′-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Substituted Nucleoside Derivative, and methods of using the 2′-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的2'-取代的核苷衍生物及其药学上可接受的盐，其中A，B，X，R 1，R 2和R 3如本文所定义。本发明还涉及包含至少一种2'-取代的核苷衍生物的组合物，以及使用2'-取代的核苷衍生物治疗或预防患者HCV感染的方法。

36. 发明申请

US20110294758A1 NOVEL ACTIVATORS OF GLUCOKINASE 有权
标题翻译： GLUCOKINASE的新型激活剂
公开(公告)号：US20110294758A1
公开(公告)日：2011-12-01
申请号：US13115647
申请日：2011-05-25
申请人： Feng Tian , Qun Dang , G. Sridhar Prasad , Wenyu Li , Brett C. Bookser , Nicholas Brian Raffaele , Mark D. Erion
发明人： Feng Tian , Qun Dang , G. Sridhar Prasad , Wenyu Li , Brett C. Bookser , Nicholas Brian Raffaele , Mark D. Erion
IPC分类号： A61K31/675 , C07F9/38 , C07F9/44 , C07F9/36 , A61P3/00 , A61P3/10 , A61P3/08 , A61P5/50 , A61P1/16 , C07F9/30 , C07F9/6574
CPC分类号： C07F9/65586 , A61K31/44 , C07C233/11 , C07D213/81 , C07F9/3834 , C07F9/4021 , C07F9/58 , C07F9/65031 , C07F9/650952 , C07F9/6512 , C07F9/653 , C07F9/6539 , C07F9/65392 , C07F9/65395 , C07F9/65397 , C07F9/6541 , C07F9/655345 , C07F9/65583 , C07F9/6561 , C07F9/65616 , C07F9/657181
摘要： The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator 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 glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
摘要翻译：本发明提供具有葡糖多糖激活剂活性的新颖的式I和II化合物及其药学上可接受的盐和共结晶。本发明进一步提供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出一种或多种葡萄糖激酶激活剂的疾病或病症的发展或进展的风险的方法，包括 1型和2型糖尿病，糖耐量异常，胰岛素抵抗和高血糖。本发明还提供了制备式I和II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。

37. 发明授权

US07371739B2 Aryl fructose-1,6-bisphosphatase inhibitors 失效
标题翻译：芳基果糖-1,6-二磷酸酶抑制剂
公开(公告)号：US07371739B2
公开(公告)日：2008-05-13
申请号：US11043859
申请日：2005-01-25
申请人： Brett C. Bookser , Qun Dang , K. Raja Reddy
发明人： Brett C. Bookser , Qun Dang , K. Raja Reddy
IPC分类号： C07F9/38 , C07F9/547 , A61K31/662 , A61K31/675
CPC分类号： C07F9/3808 , C07F9/3826 , C07F9/6539 , C07F9/65515 , C07F9/65583 , C07F9/65586
摘要： Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
摘要翻译：式I的新型FBPase抑制剂可用于治疗与血糖升高相关的糖尿病和其它病症。

38. 发明授权

US06294672B1 Indole and azaindole inhibitors of Fructose-1,6-biphosphatase 有权
标题翻译：果糖-1,6-二磷酸酶的吲哚和azaindole抑制剂
公开(公告)号：US06294672B1
公开(公告)日：2001-09-25
申请号：US09479384
申请日：2000-01-05
申请人： K. Raja Reddy , Gerard R. Scarlato , Qun Dang , Mark D. Erion , Srinivas Rao Kasibhatla , M. Rami Reddy
发明人： K. Raja Reddy , Gerard R. Scarlato , Qun Dang , Mark D. Erion , Srinivas Rao Kasibhatla , M. Rami Reddy
IPC分类号： C07F924
CPC分类号： C07F9/5728 , C07F9/65586 , C07F9/6561
摘要： The present invention is directed towards novel azaindole compounds which bind to the AMP site and are potent FBPase inhibitors. The present invention also is directed towards the clinical use of the novel FBPase inhibitors as a method of treatment or prevention of diseases responsive to lowered blood glucose levels.
摘要翻译：本发明涉及与AMP位点结合并且是有效的FBP酶抑制剂的新颖的氮杂吲哚化合物。本发明还涉及新型FBP酶抑制剂作为治疗或预防对低血糖水平降低的疾病的方法的临床应用。

39. 发明授权

US06284748B1 Purine inhibitors of fructose 1,6-bisphosphatase 失效
标题翻译：果糖1,6-二磷酸酶的嘌呤抑制剂
公开(公告)号：US06284748B1
公开(公告)日：2001-09-04
申请号：US09036327
申请日：1998-03-06
申请人： Qun Dang , Mark D. Erion , M. Rami Reddy , Edward D. Robinson , Srinivas Rao Kasibhatla , K. Raja Reddy
发明人： Qun Dang , Mark D. Erion , M. Rami Reddy , Edward D. Robinson , Srinivas Rao Kasibhatla , K. Raja Reddy
IPC分类号： C07F96561
CPC分类号： C07F9/65616 , C07F9/657181
摘要： Novel purine compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described. wherein A is selected from the group consisting of —NR82, —NHSO2R3, —OR5, —SR5, halo, lower alkyl, —CON(R4)2, guanidino, amidino, —H, and perhaloalkyl; E is selected from the group consisting of —H, halo, lower alkylthio, lower perhaloalkyl, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, —CN, and —NR72; X is selected from the group consisting of -alk-NR—, alkylene, alkenylene, alkynylene, arylene, heteroarylene, -alk-NR-alk-, -alk-O-alk-, -alk-S-alk-, -alk-S—, alicyclicene, heteroalicyclicene, 1,1-dihaloalkylene, —C(O)-alk-, —NR—C(O)—NR′—, -alk-NR—C(O)—, -alk-C(O)—NR—, —Ar-alk-, and -alk-Ar—, all optionally substituted, wherein each R and R′ is independently selected from —H and lower alkyl, and wherein each “alk” and “Ar” is an independently selected alkylene or arylene, respectively; Y is selected from the group consisting of —H, alkyl, alkenyl, alkynyl, aryl, alicyclic, heteroalicyclic, aralkyl, aryloxyalkyl, alkoxyalkyl, —C(O)R3, —S(O)2R3, —C(O)—OR3, —CONHR3, —NR22, and —OR3, all except H are optionally substituted; and pharmaceutically acceptable prodrugs and salts thereof.
摘要翻译：描述了以下结构的新型嘌呤化合物及其作为果糖-1,6-二磷酸酶抑制剂的用途，其中A选自-NR82，-NHSO2R3，-OR5，-SR5，卤素，低级烷基，-CON（ R 4）2，胍基，脒基，-H和全卤代烷基; E选自-H，卤素，低级烷硫基，低级全卤代烷基，低级烷基，低级烯基，低级炔基，低级烷氧基，-CN和 - NR72; X选自-alk-NR-，亚烷基，亚烯基，亚炔基，亚芳基，亚杂芳基，-alk-NR-烷基， - 烷基-O-烷基， - 烷基-S-烷基，（O）-NR' - ，-NR-C（O） - ， - 烷基，（C 1 -C 6） - 烷基亚磺酰基，其中每个R和R'独立地选自-H和低级烷基，并且其中每个“烷基”和“烷氧基” Ar“分别是独立选择的亚烷基或亚芳基; Y选自-H，烷基，烯基，炔基，芳基，脂环，杂脂环，芳烷基，芳氧基烷基，烷氧基烷基，-C（O）R 3，-S（O）2 R 3，-C（O）-OR 3，-CONHR 3，-NR 22和-OR 3，和药学上可接受的前药及其盐。

40. 发明授权

US09150603B2 2′-cyano substituted nucleoside derivatives and methods of use thereof useful for the treatment of viral diseases 有权
标题翻译： 2'-氰基取代的核苷衍生物及其用于治疗病毒性疾病的方法
公开(公告)号：US09150603B2
公开(公告)日：2015-10-06
申请号：US14111688
申请日：2012-04-11
申请人： Vinay Girijavallabhan , F. George Njoroge , Stephane Bogen , Angela Kerekes , Frank Bennett , Ying Huang , Latha Nair , Dmitri Pissarnitski , Vishal Verma , Qun Dang , Ian Davies , David B. Olsen , Andrew Stamford , Joseph P. Vacca
发明人： Vinay Girijavallabhan , F. George Njoroge , Stephane Bogen , Angela Kerekes , Frank Bennett , Ying Huang , Latha Nair , Dmitri Pissarnitski , Vishal Verma , Qun Dang , Ian Davies , David B. Olsen , Andrew Stamford , Joseph P. Vacca
IPC分类号： C07H19/06 , C07H19/20 , C07H19/10 , C07H19/12 , C07H19/16 , C07H19/04 , C07H19/207 , C07H19/11 , C07H19/213 , A61K31/7056 , A61K31/7068 , A61K31/7076 , A61K45/06
CPC分类号： C07H19/16 , A61K31/7056 , A61K31/7068 , A61K31/7076 , A61K45/06 , C07H19/06 , C07H19/10 , C07H19/11 , C07H19/20 , C07H19/207 , C07H19/213 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395
摘要： The present invention relates to 2′-Cyano Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Cyano Substituted Nucleoside Derivative, and methods of using the 2′-Cyano Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的2'-氰基取代的核苷衍生物及其药学上可接受的盐，其中B，X，R 1，R 2和R 3如本文所定义。本发明还涉及包含至少一种2'-氰基取代的核苷衍生物的组合物，以及使用2'-氰基取代的核苷衍生物治疗或预防患者HCV感染的方法。

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