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31. 发明申请

US20140005191A1 SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF 有权
公开(公告)号：US20140005191A1
公开(公告)日：2014-01-02
申请号：US13884061
申请日：2011-11-09
申请人： Craig A. Coburn , Kun Liu , Ernest J. McEacher , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou
发明人： Craig A. Coburn , Kun Liu , Ernest J. McEacher , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou
IPC分类号： C07D513/14
CPC分类号： C07D513/14 , C07D513/04 , C07H9/06 , C07H13/04 , C07H13/12 , C07H15/18 , C12Q1/48 , G01N2500/02
摘要： The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

32. 发明申请

US20120251491A1 FUSED TRICYCLIC ARYL COMPOUNDS USEFUL FOR THE TREATMENT OF VIRAL DISEASES 有权
标题翻译：用于治疗病毒性疾病的融合的三酰甘油化合物
公开(公告)号：US20120251491A1
公开(公告)日：2012-10-04
申请号：US13320427
申请日：2010-05-12
申请人： Stuart B. Rosenblum , Kevin X. Chen , Joseph A. Kozlowski , F. George Njoroge , Craig A. Coburn
发明人： Stuart B. Rosenblum , Kevin X. Chen , Joseph A. Kozlowski , F. George Njoroge , Craig A. Coburn
IPC分类号： A61K31/4178 , C07D487/04 , C07D493/04 , A61K31/4184 , A61K31/4188 , C07D471/04 , A61K31/4745 , C07D491/044 , A61K31/55 , C07D401/14 , A61K31/473 , A61K31/498 , A61K38/21 , A61K31/7088 , A61K39/12 , A61K39/395 , A61K31/7056 , A61P31/14 , A61P37/04 , A61P31/12 , C07D403/14
CPC分类号： C07D403/14 , C07C403/04 , C07D403/04 , C07D471/04 , C07D487/04 , C07D491/044 , C07D493/04
摘要： The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及新的熔融三环芳基化合物，包含至少一种稠合三环芳基化合物的组合物，以及使用稠合三环芳基化合物治疗或预防患者HCV感染的方法。

33. 发明申请

US20110034483A1 2-AMINOIMIDAZOLE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权
标题翻译：用于治疗阿尔茨海默病的2-氨基咪唑β-分泌酶抑制剂
公开(公告)号：US20110034483A1
公开(公告)日：2011-02-10
申请号：US12919277
申请日：2009-02-18
申请人： Ivory D. Hills , Craig A. Coburn , Samuel L. Graham , Keith P. Moore , Philippe G. Nantermet , Hemaka A. Rajapakse , Shawn J. Stachel , Hong Zhu
发明人： Ivory D. Hills , Craig A. Coburn , Samuel L. Graham , Keith P. Moore , Philippe G. Nantermet , Hemaka A. Rajapakse , Shawn J. Stachel , Hong Zhu
IPC分类号： A61K31/506 , C07D233/88 , A61K31/4174 , C07D403/10 , A61K31/4178 , C07D403/06 , C07D413/10 , A61K31/42 , C07D401/10 , A61K31/4439 , A61K31/422 , A61P25/28
CPC分类号： C07D233/88 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/10 , C07D413/10
摘要： The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译：本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默病的式（I）的2-氨基咪唑化合物。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。

34. 发明申请

US20100298342A1 Spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's Disease 审中-公开
标题翻译：用于治疗阿尔茨海默病的Spiropiperidineβ-分泌酶抑制剂
公开(公告)号：US20100298342A1
公开(公告)日：2010-11-25
申请号：US12310573
申请日：2007-09-04
申请人： Melissa S. Egbertson , Shaun R. Stauffer , Craig A. Coburn , James C. Barrow , Lou Anne Neilson , Jenny M. Wai , Wenjin Yang , Wanli Lu , Bruce Fahr
发明人： Melissa S. Egbertson , Shaun R. Stauffer , Craig A. Coburn , James C. Barrow , Lou Anne Neilson , Jenny M. Wai , Wenjin Yang , Wanli Lu , Bruce Fahr
IPC分类号： A61K31/438 , C07D471/10 , A61K31/497 , A61P25/28
CPC分类号： C07D471/10 , C07D498/10
摘要： The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译：本发明涉及式（I）的螺哌啶化合物及其互变异构体，其是β-分泌酶的抑制剂，并且其可用于治疗涉及β-分泌酶的疾病，例如阿尔茨海默氏病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。

35. 发明申请

US20080287523A1 Pyrrolidin-3-Yl Compounds Useful as Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease 有权
标题翻译：可用作治疗阿尔茨海默病的β-分泌酶抑制剂的吡咯烷-3-基化合物
公开(公告)号：US20080287523A1
公开(公告)日：2008-11-20
申请号：US11629209
申请日：2005-06-10
申请人： Craig A. Coburn
发明人： Craig A. Coburn
IPC分类号： A61K31/40 , C07D207/50 , A61P25/28
CPC分类号： C07D207/14
摘要： The present invention is directed to pyrrolidin-3-yl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译：本发明涉及作为β-分泌酶的抑制剂并且可用于治疗涉及β-分泌酶的疾病如阿尔茨海默氏病的吡咯烷-3-基衍生物化合物。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。

36. 发明授权

US06350745B1 Thrombin inhibitors 失效
标题翻译：凝血酶抑制剂
公开(公告)号：US06350745B1
公开(公告)日：2002-02-26
申请号：US09585740
申请日：2000-06-02
申请人： Craig A. Coburn , Christopher S. Burgey
发明人： Craig A. Coburn , Christopher S. Burgey
IPC分类号： C07D49804
CPC分类号： C07D498/04
摘要： Compounds of the invention, useful as thrombin inhibitors and having therapeutic value in for example, preventing coronary artery disease, have the following structure: or a pharmaceutically acceptable salt thereof, wherein A is wherein Y1 and Y2 are independently hydrogen, C1-4 alkyl, C1-4 alkoxy, FuHvC(CH2)0-1 O—, wherein u and v are either 1 or 2, provided that when u is 1, v is 2, and when u is 2, v is 1, C3-7 cycloalkyl, thio C1-4 alkyl, C1-4 sulfinylalkyl, C1-4 sulfonylalkyl, halogen cyano, or trifluoromethyl, and wherein b is 0 or 1.
摘要翻译：可用作凝血酶抑制剂并具有例如预防冠状动脉疾病的治疗价值的本发明化合物具有以下结构：或其药学上可接受的盐，其中A在其中Y 1和Y 2独立地为氢，C 1-4烷基，C 1-4烷氧基（CH 2）0-1 O-，其中u和v为1或2，条件是当u为1时，v为2，当u为2时，v为1，C 3-7环烷基，硫代C1- C4烷基，C1-4亚磺酰基烷基，C1-4磺酰基烷基，卤代，三氟甲基，其中b为0或1。

37. 发明授权

US09504690B2 Tetracyclic xanthene derivatives and methods of use thereof for the treatment of viral diseases 有权
标题翻译：四环呫吨衍生物及其用于治疗病毒性疾病的方法
公开(公告)号：US09504690B2
公开(公告)日：2016-11-29
申请号：US14005430
申请日：2012-03-16
申请人： Craig A. Coburn , Stuart B. Rosenblum , Joseph A. Kozlowski , Richard Soll , Hao Wu , Bin Hu , Bin Zhong , Dahai Wang , Changmao Shen , Fei Sun
发明人： Craig A. Coburn , Stuart B. Rosenblum , Joseph A. Kozlowski , Richard Soll , Hao Wu , Bin Hu , Bin Zhong , Dahai Wang , Changmao Shen , Fei Sun
IPC分类号： A61K31/535 , A61K31/5383 , C07D491/06 , C07D498/06 , A61K31/4178 , A61K45/06 , C07D493/06
CPC分类号： A61K31/5383 , A61K31/4178 , A61K45/06 , C07D491/06 , C07D493/06 , C07D498/06
摘要： The present invention relates to novel Tetracyclic Xanthene Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, Y1, Y2, Z, Ra, Rb, R1a, R1b and R2 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Xanthene Derivative, and methods of using the Tetracyclic Xanthene Derivatives for treating or preventing HCV infection in a patient.

38. 发明申请

US20160108048A1 IMIDAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 有权
标题翻译：咪唑衍生物及其用于改善药物药物动力学的方法
公开(公告)号：US20160108048A1
公开(公告)日：2016-04-21
申请号：US14895406
申请日：2014-06-02
申请人： Craig A. COBURN , Milana MALETIC , Yunfu LUO , Zhiqi QI , Chunsing LI , Tingting YU , Richard SOLL , MERCK SHARP & DOHME CORP.
发明人： Craig A. Coburn , Milana Maletic , Yunfu Luo , Zhiqi Qi , Chunsing Li , Tingting Yu , Richard Soll
IPC分类号： C07D487/04 , A61K31/4545 , C07D498/04 , A61K31/5383 , A61K31/4985 , A61K45/06 , A61K31/496 , A61K31/551 , C07D405/14 , C07D401/06 , C07D413/14 , C07D401/14 , A61K31/454
CPC分类号： C07D487/04 , A61K31/4375 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/513 , A61K31/5365 , A61K31/5383 , A61K31/55 , A61K31/551 , A61K45/06 , C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D498/04 , A61K2300/00
摘要： The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R1 and R2 are as defined herein. The present invention also relates to compositions comprising at least one Imidazole Derivative, and methods of using the Imidazole Derivatives for inhibiting CYP450 3A. Inhibition of CYP450 3A can be used to improve the pharmacokinetics of a drug that is metabolized by CYP450 3A4.
摘要翻译：本发明涉及式（I）的咪唑衍生物及其药学上可接受的盐，其中A，B，Y，R 1和R 2如本文所定义。本发明还涉及包含至少一种咪唑衍生物的组合物，以及使用咪唑衍生物抑制CYP450A 3A的方法。 CYP450 3A的抑制可用于改善由CYP450 3A4代谢的药物的药代动力学。

39. 发明授权

US08927507B2 Selective glycosidase inhibitors and uses thereof 有权
公开(公告)号：US08927507B2
公开(公告)日：2015-01-06
申请号：US14006888
申请日：2012-03-16
申请人： Ernest J. McEachern , David J. Vocadlo , Yuanxi Zhou , Craig A. Coburn , Kun Liu , Harold G. Selnick
发明人： Ernest J. McEachern , David J. Vocadlo , Yuanxi Zhou , Craig A. Coburn , Kun Liu , Harold G. Selnick
IPC分类号： C08B37/00 , C07D487/02 , A61K31/70 , A61K31/425 , C12Q1/34 , C07H13/04 , C07H9/06
CPC分类号： C07H9/06 , C07H13/04 , C12Q1/34 , G01N2333/924 , G01N2500/04
摘要： The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

40. 发明申请

US20140213584A9 SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF 有权
公开(公告)号：US20140213584A9
公开(公告)日：2014-07-31
申请号：US13884061
申请日：2011-11-08
申请人： Craig A. Coburn , Kun Liu , Ernest J. McEachern , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou
发明人： Craig A. Coburn , Kun Liu , Ernest J. McEachern , Changwei Mu , Harold G. Selnick , David J. Vocadlo , Yaode Wang , Zhongyong Wei , Yuanxi Zhou
IPC分类号： C07D513/14
CPC分类号： C07D513/14 , C07D513/04 , C07H9/06 , C07H13/04 , C07H13/12 , C07H15/18 , C12Q1/48 , G01N2500/02
摘要： The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

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