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1. 发明申请

US20160297809A1 ARYL LINKED IMIDAZOLE AND TRIAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 有权
标题翻译：芳基链接的咪唑和三唑衍生物及其用于改善药物药代动力学的方法
公开(公告)号：US20160297809A1
公开(公告)日：2016-10-13
申请号：US15036274
申请日：2014-11-07
申请人： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Chun Sing Li , Tingting Yu
发明人： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Chun Sing Li , Tingting Yu
IPC分类号： C07D417/14 , C07D417/12 , A61K31/496 , C07D487/04 , A61K31/4985 , A61K31/4439 , A61K31/427 , C07D401/12 , C07D405/14 , A61K31/4178 , C07D403/10 , A61K31/5377 , A61K31/4545 , C07D401/14 , A61K45/06 , A61K31/4725
CPC分类号： C07D417/14 , A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K45/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/14 , C07D417/12 , C07D471/04 , C07D487/04 , A61K2300/00
摘要： The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
摘要翻译：本发明涉及芳基连接的咪唑和三唑衍生物，包含所述化合物单独或与其它药物组合的组合物，以及使用该化合物改善药物药代动力学的方法。本发明的化合物可用于抑制CYP3A4的人和兽医药物，并且用于改善由CYP3A4代谢的治疗化合物的药代动力学。

2. 发明授权

US08871759B2 Inhibitors of hepatitis C virus replication 有权
标题翻译：丙型肝炎病毒复制抑制剂
公开(公告)号：US08871759B2
公开(公告)日：2014-10-28
申请号：US13260684
申请日：2010-03-25
申请人： Craig A. Coburn , Steven W. Ludmerer , Kun Liu , Hao Wu , Richard Soll , Bin Zhong , Jian Zhu
发明人： Craig A. Coburn , Steven W. Ludmerer , Kun Liu , Hao Wu , Richard Soll , Bin Zhong , Jian Zhu
IPC分类号： A61K31/5365 , C07D413/14
CPC分类号： C07D498/04 , A61K31/4025 , A61K31/404 , A61K31/4178 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4985 , A61K31/506 , A61K31/5365 , A61K31/5377 , A61K31/5383 , A61K31/553 , A61K38/05 , A61K38/06 , A61K45/06 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D498/10 , C07K5/06 , C07K5/08
摘要： The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
摘要翻译：本发明涉及可用作丙型肝炎病毒（HCV）NS5A抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5A活性用于治疗或预防HCV感染的用途的式（I）化合物和抑制基于细胞的系统中的HCV病毒复制和/或病毒生产。

3. 发明申请

US20140170111A1 FUSED TETRACYCLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 有权
标题翻译：融合的四氢吡啶衍生物及其用于治疗病毒的方法
公开(公告)号：US20140170111A1
公开(公告)日：2014-06-19
申请号：US13876931
申请日：2011-09-28
申请人： Craig A. Coburn , Brian J. Lavey , Michael P. Dwyer , Joseph A. Kozlowski , Stuart B. Rosenblum
发明人： Craig A. Coburn , Brian J. Lavey , Michael P. Dwyer , Joseph A. Kozlowski , Stuart B. Rosenblum
IPC分类号： A61K31/553 , A61K31/4178 , C07D493/04 , A61K45/06 , C07D498/04 , C07D487/04 , A61K31/5517 , C07D403/14 , C07D405/14
CPC分类号： A61K31/553 , A61K31/4178 , A61K31/5517 , A61K45/06 , C07D403/14 , C07D405/14 , C07D487/04 , C07D493/04 , C07D498/04 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395
摘要： The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A′, B, G, R1, U, V, W, W′, X, X′, Y and Y′ are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的新型熔融四环衍生物及其药学上可接受的盐，其中A，A'，B，G，R 1，U，V，W，W'，X，X'，Y和Y '如本文所定义。本发明还涉及包含至少一种熔融四环衍生物的组合物，以及使用熔融四环衍生物治疗或预防患者HCV感染的方法。

4. 发明申请

US20140107044A1 SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF 有权
标题翻译：选择性糖苷酶抑制剂及其用途
公开(公告)号：US20140107044A1
公开(公告)日：2014-04-17
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： C07H9/06 , C12Q1/34
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.
摘要翻译：本发明提供了用于选择性抑制糖苷酶，化合物前药和包含化合物的化合物或前药的药物组合物的化合物。本发明还提供了治疗与O-GlcNAcase的缺乏或过度表达相关的疾病和障碍的方法，O-GlcNAc的积累或缺乏。

5. 发明授权

US07449599B2 Phenyl carboxamide compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease 失效
标题翻译：用作治疗阿尔茨海默病的β-分泌酶抑制剂的苯基甲酰胺化合物
公开(公告)号：US07449599B2
公开(公告)日：2008-11-11
申请号：US11579049
申请日：2005-05-09
申请人： Craig A. Coburn , Thomas G. Steele , Joseph P. Vacca , David Allen Annis, Jr. , Gergely M. Makara , Huw M. Nash , Praveen K. Tadikonda , Tong Wang
发明人： Craig A. Coburn , Thomas G. Steele , Joseph P. Vacca , David Allen Annis, Jr. , Gergely M. Makara , Huw M. Nash , Praveen K. Tadikonda , Tong Wang
IPC分类号： C07C233/05 , C07C233/65 , C07C305/18 , C07C255/50 , A61K31/16 , A61K31/255 , A61K31/275
CPC分类号： C07C235/84 , C07C255/57 , C07C309/67
摘要： The present invention is directed to phenyl carboxamide 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其中涉及β-分泌酶的疾病如阿尔茨海默氏病的苯甲酰胺化合物。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。

6. 发明申请

US20080153846A1 Aminomethyl Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease 有权
标题翻译：氨基甲基β-分泌酶抑制剂治疗阿尔茨海默病
公开(公告)号：US20080153846A1
公开(公告)日：2008-06-26
申请号：US11795283
申请日：2006-01-13
申请人： Craig A. Coburn , Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Shaun R. Stauffer
发明人： Craig A. Coburn , Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Shaun R. Stauffer
IPC分类号： A61K31/496 , C07C211/00 , A61K31/13 , A61K31/4245 , A61P25/28 , C07D271/06 , C07D413/06
CPC分类号： C07D413/06 , C07D271/10
摘要： The present invention is directed to aminomethyl 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-分泌酶的抑制剂并可用于治疗涉及β-分泌酶的疾病如阿尔茨海默氏病的氨基甲基化合物。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。

7. 发明授权

US07329746B2 Macrocyclic 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氏病的大环β-分泌酶抑制剂
公开(公告)号：US07329746B2
公开(公告)日：2008-02-12
申请号：US10568153
申请日：2004-08-10
申请人： Craig A. Coburn , Shawn J. Stachel , Joseph P. Vacca
发明人： Craig A. Coburn , Shawn J. Stachel , Joseph P. Vacca
IPC分类号： C07D225/04 , C07D267/22 , A61K31/33 , A61K31/395 , A61P25/28
CPC分类号： C07D267/00 , C07D225/08
摘要： The present invention is directed to compounds of formula I which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention 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 prevention or 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或预防其中涉及β-分泌酶的疾病如阿尔茨海默氏病的式I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预防或治疗涉及β-分泌酶的疾病中的用途

8. 发明授权

US5391745A Methods of preparation of camptothecin analogs 失效
标题翻译：喜树碱类似物的制备方法
公开(公告)号：US5391745A
公开(公告)日：1995-02-21
申请号：US2996
申请日：1993-01-11
申请人： Samuel J. Danishefsky , William G. Bornmann , Wang Shen , Craig A. Coburn
发明人： Samuel J. Danishefsky , William G. Bornmann , Wang Shen , Craig A. Coburn
IPC分类号： C07D491/14 , C07D491/147 , C07D491/22 , C07H17/00 , C07D491/52
CPC分类号： C07D491/14 , C07H17/00
摘要： Substituted analoguss of camptothecin possessing cytotoxic activity towards cancer cells, of the general structure: ##STR1## wherein E is H, CO.sub.2 R, CONH.sub.2, CONHR, CONR.sub.2, acyl, or CN; X is H OH, or OR; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, alkoxy, hydroxyalkyl, or aminoalkoxy group, or an aryl or aryloxy group, or a C-glycal, or CO.sub.2 R, nitro, cyano, Cl, F, Br, I, SR.sup.10, NR.sup.11 R.sup.12, or OR.sup.13 ; R is H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R.sup.10, R.sup.11 and R.sup.12 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, hydroxyalkyl, or acyl group, or an aryl group; R.sup.13 is glycosyl; n is 0 or 1; with the proviso that when R.sup. 1 is ethyl, and n is 0, E, R.sup.2, R.sup.3, and R.sup.4 are not all H. Intermediate compounds leading to the camptothecin analogues comprise substituted tricyclic compounds which consist of rings C, D, and E fused together. Methods for preparing the analoguss involve condensation of such intermediates with variably substituted protected .alpha.-aminobenzaldehydes.
摘要翻译：具有一般结构的具有对癌细胞的细胞毒性活性的喜树碱的取代类似物：其中E是H，CO 2 R，CONH 2，CONHR，CONR 2，酰基或CN; X是H OH或OR; R 1，R 2，R 3和R 4独立地相同或不同，为H，或直链或支链烷基，烷基芳基或羟烷基或芳基; R 5，R 6，R 7，R 8和R 9独立地相同或不同，为H，或直链或支链烷基，烷基芳基，烷氧基，羟基烷基或氨基烷氧基，或芳基或芳氧基或C- ，或CO 2 R，硝基，氰基，Cl，F，Br，I，SR10，NR 11 R 12或OR 13; R为H或直链或支链烷基，烷基芳基或羟烷基或芳基; R 10，R 11和R 12独立地相同或不同，为H，或直链或支链烷基，烷基芳基，羟基烷基或酰基或芳基; R13是糖基; n为0或1; 条件是当R 1为乙基且n为0时，E，R 2，R 3和R 4不全为H.导致喜树碱类似物的中间体化合物包括取代的三环化合物，其由环C，D和E稠合一起。制备类似物的方法涉及这种中间体与可变取代的保护的α-氨基苯甲醛的缩合。

9. 发明授权

US09254292B2 Fused tetracycle derivatives and methods of use thereof for the treatment of viral diseases 有权
标题翻译：熔融四环衍生物及其用于治疗病毒性疾病的方法
公开(公告)号：US09254292B2
公开(公告)日：2016-02-09
申请号：US13876931
申请日：2011-09-28
申请人： Craig A. Coburn , Brian J. Lavey , Michael P. Dwyer , Joseph A. Kozlowski , Stuart B. Rosenblum
发明人： Craig A. Coburn , Brian J. Lavey , Michael P. Dwyer , Joseph A. Kozlowski , Stuart B. Rosenblum
IPC分类号： A61K31/553 , C07D403/14 , C07D405/14 , C07D493/04 , C07D498/04 , A61K31/4178 , A61K31/5517 , A61K45/06 , C07D487/04
CPC分类号： A61K31/553 , A61K31/4178 , A61K31/5517 , A61K45/06 , C07D403/14 , C07D405/14 , C07D487/04 , C07D493/04 , C07D498/04 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395
摘要： The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A′, B, G, R1, U, V, W, W′, X, X′, Y and Y′ are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的新型熔融四环衍生物及其药学上可接受的盐，其中A，A'，B，G，R 1，U，V，W，W'，X，X'，Y和Y '如本文所定义。本发明还涉及包含至少一种熔融四环衍生物的组合物，以及使用熔融四环衍生物治疗或预防患者HCV感染的方法。

10. 发明授权

US08933040B2 Selective glycosidase inhibitors and uses thereof 有权
标题翻译：选择性糖苷酶抑制剂及其用途
公开(公告)号：US08933040B2
公开(公告)日：2015-01-13
申请号：US13884061
申请日：2011-11-08
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： C08B37/00 , C07D487/02 , A61K31/70 , A61K31/425 , C07D513/14 , C07D513/04 , C07H9/06 , C07H13/04 , C07H13/12 , C07H15/18 , C12Q1/48
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.
摘要翻译：本发明提供了用于选择性抑制糖苷酶，化合物前药和包含化合物的化合物或前药的药物组合物的化合物。本发明还提供了治疗与O-GlcNAcase的缺乏或过度表达相关的疾病和障碍的方法，O-GlcNAc的积累或缺乏。

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