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41. 发明授权

US08921359B2 Inhibitors of beta-secretase 有权
标题翻译： β-分泌酶抑制剂
公开(公告)号：US08921359B2
公开(公告)日：2014-12-30
申请号：US13867590
申请日：2013-04-22
申请人： Lawrence W. Dillard , Jing Yuan , Lanqi Jia , Yajun Zheng
发明人： Lawrence W. Dillard , Jing Yuan , Lanqi Jia , Yajun Zheng
IPC分类号： A61K31/54 , A61K31/415 , A61K31/44 , A61K31/41 , A61K31/4965 , A61K31/497 , A61K31/505 , C07D498/16 , C07D495/10 , C07D491/20 , C07D498/10 , C07D513/10 , C07D491/107 , C07D498/20
CPC分类号： C07D498/20 , C07D491/107 , C07D491/20 , C07D495/10 , C07D498/10 , C07D498/16 , C07D513/10
摘要： The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.
摘要翻译：本发明涉及由以下结构式表示的化合物或其药学上可接受的盐。还描述了包含由结构式（I）表示的化合物和这些化合物用于抑制需要这种治疗的受试者中的BACE活性的方法的药物组合物。

42. 发明申请

US20130317014A1 INHIBITORS OF BETA-SECRETASE 有权
标题翻译： BETA-SECRETASE的抑制剂
公开(公告)号：US20130317014A1
公开(公告)日：2013-11-28
申请号：US13867590
申请日：2013-04-22
申请人： Lawrence W. Dillard , Jing Yuan , Lanqi Jia , Yajun Zheng
发明人： Lawrence W. Dillard , Jing Yuan , Lanqi Jia , Yajun Zheng
IPC分类号： C07D498/20 , C07D513/10 , C07D498/10 , C07D495/10 , C07D491/107 , C07D491/20
CPC分类号： C07D498/20 , C07D491/107 , C07D491/20 , C07D495/10 , C07D498/10 , C07D498/16 , C07D513/10
摘要： The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.
摘要翻译：本发明涉及由以下结构式表示的化合物或其药学上可接受的盐。还描述了包含由结构式（I）表示的化合物和这些化合物用于抑制需要这种治疗的受试者中的BACE活性的方法的药物组合物。

43. 发明授权

US07084271B2 Pyrazolopyrimidines as cyclin dependent kinase inhibitors 失效
公开(公告)号：US07084271B2
公开(公告)日：2006-08-01
申请号：US10654163
申请日：2003-09-03
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Chad Knutson , Brian McKittrick , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Chad Knutson , Brian McKittrick , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

44. 发明授权

US5789172A Methods of determining the structure of a compound encoded by identifiers having tags 失效
标题翻译：确定具有标签的标识符编码的化合物的结构的方法
公开(公告)号：US5789172A
公开(公告)日：1998-08-04
申请号：US680716
申请日：1996-07-11
申请人： W. Clark Still , Michael H. Wigler , Michael H. J. Ohlmeyer , Lawrence W. Dillard , John C. Reader
发明人： W. Clark Still , Michael H. Wigler , Michael H. J. Ohlmeyer , Lawrence W. Dillard , John C. Reader
IPC分类号： G01N33/566 , C07B61/00 , C07C43/225 , C07C205/59 , C07C245/14 , C07C317/28 , C07D243/24 , C07D521/00 , C07H21/00 , C07K1/00 , C07K1/04 , C40B70/00 , G01N33/532 , G01N33/543 , G01N33/68 , C12Q1/68 , G01N33/53
CPC分类号： G01N33/68 , C07D243/24 , C07H21/00 , C07K1/047 , C40B50/16 , G01N33/532 , G01N33/54353 , B01J2219/00572 , C07B2200/11 , C40B40/00 , C40B70/00
摘要： Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produced in the multi-stage synthesis, such as oligomers and synthetic non-repetitive organic molecules. Conveniently, nested families of compounds can be employed as identifiers, where number and/or position of a substituent define the choice. Alternatively, detectable functionalities may be employed, such as radioisotopes, fluorescers, halogens, and the like, where presence and ratios of two different groups can be used to define stage or choice. Particularly, pluralities of identifiers may be used to provide a binary or higher code, so as to define a plurality of choices with only a few detachable tags. The particles may be screened for a characteristic of interest, particularly binding affinity, where the products may be detached from the particle or retained on the particle. The reaction history of the particles which are positive for the characteristic can be determined by the release of the tags and analysis to define the reaction history of the particle.
摘要翻译：提供了编码的组合化学，其中使用有机分子记录顺序合成方案，其定义了反应物的选择和阶段，作为相同或不同的信息位。可以在多级合成中产生各种产物，例如低聚物和合成的非重复有机分子。方便地，化合物的嵌套族可以用作标识符，其中取代基的数目和/或位置定义了选择。或者，可以使用可检测的官能团，例如放射性同位素，荧光剂，卤素等，其中两个不同基团的存在和比例可用于限定阶段或选择。特别地，可以使用多个标识符来提供二进制或更高代码，以便仅限定几个可拆卸标签来定义多个选择。可以筛选颗粒以获得感兴趣的特征，特别是结合亲和力，其中产物可以与颗粒分离或保留在颗粒上。对特征呈阳性的颗粒的反应历程可以通过标签的释放和分析来确定以确定颗粒的反应历程。

45. 发明授权

US6001579A Supports and combinatorial chemical libraries thereof encoded by non-sequencable tags 失效
标题翻译：由非可序列标签编码的支持体和组合化学文库
公开(公告)号：US6001579A
公开(公告)日：1999-12-14
申请号：US485018
申请日：1995-06-07
申请人： W. Clark Still , Michael H. Wigler , Michael H. J. Ohlmeyer , Lawrence W. Dillard , John C. Reader
发明人： W. Clark Still , Michael H. Wigler , Michael H. J. Ohlmeyer , Lawrence W. Dillard , John C. Reader
IPC分类号： C07D243/16 , G01N33/53 , G01N33/543 , G01N33/546 , G01N33/566 , G01N33/58
CPC分类号： C07D243/28 , C07D491/048 , C40B40/04 , C40B50/16 , C40B70/00 , G01N33/54313 , G01N33/54353 , C07B2200/11
摘要： Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produced in the multi-stage synthesis, such as oligomers and synthetic non-repetitive organic molecules. Conveniently, nested families of compounds can be employed as identifiers, where number and/or position of a substituent define the choice. Alternatively, detectable functionalities may be employed, such as radioisotopes, fluorescers, halogens, and the like, where presence and ratios of two different groups can be used to define stage or choice. Particularly, pluralities of identifiers may be used to provide a binary or higher code, so as to define a plurality of choices with only a few detachable tags. The particles may be screened for a characteristic of interest, particularly binding affinity, where the products may be detached from the particle or retained on the particle. The reaction history of the particles which are positive for the characteristic can be determined by the release of the tags and analysis to define the reaction history of the particle.
摘要翻译：提供了编码的组合化学，其中使用有机分子记录顺序合成方案，其定义了反应物的选择和阶段，作为相同或不同的信息位。可以在多级合成中产生各种产物，例如低聚物和合成的非重复有机分子。方便地，化合物的嵌套族可以用作标识符，其中取代基的数目和/或位置定义了选择。或者，可以使用可检测的官能团，例如放射性同位素，荧光剂，卤素等，其中两个不同基团的存在和比例可用于限定阶段或选择。特别地，可以使用多个标识符来提供二进制或更高代码，以便仅限定几个可拆卸标签来定义多个选择。可以筛选颗粒以获得感兴趣的特征，特别是结合亲和力，其中产物可以与颗粒分离或保留在颗粒上。对特征呈阳性的颗粒的反应历程可以通过标签的释放和分析来确定以确定颗粒的反应历程。

46. 发明授权

US07807683B2 N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors 有权
标题翻译： N-杂芳基吡唑并嘧啶作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US07807683B2
公开(公告)日：2010-10-05
申请号：US11396001
申请日：2006-03-31
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Alan Mallams , Carmen S. Alvarez , Kartik M. Keertikar , Jocelyn Rivera , Tin Yau Chan , Vincent Madison , Thierry O. Fischmann , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park , Vidyadhar M. Paradkar , Douglas Walsh Hobbs
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Alan Mallams , Carmen S. Alvarez , Kartik M. Keertikar , Jocelyn Rivera , Tin Yau Chan , Vincent Madison , Thierry O. Fischmann , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park , Vidyadhar M. Paradkar , Douglas Walsh Hobbs
IPC分类号： A61K31/519 , A61P35/04 , A61P35/02 , C07D487/04 , A61P35/00
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。

47. 发明授权

US07470695B2 N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors 有权
标题翻译： N-杂芳基吡唑并嘧啶作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US07470695B2
公开(公告)日：2008-12-30
申请号：US11395974
申请日：2006-03-31
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park
IPC分类号： C07D487/04 , A61K31/519 , A61P35/04
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。

48. 发明授权

US07078525B2 Pyrazolopyrimidines as cyclin dependent kinase inhibitors 有权
公开(公告)号：US07078525B2
公开(公告)日：2006-07-18
申请号：US10654157
申请日：2003-09-03
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

49. 发明授权

US07067661B2 Pyrazolopyrimidines as cyclin dependent kinase inhibitors 有权
公开(公告)号：US07067661B2
公开(公告)日：2006-06-27
申请号：US10653776
申请日：2003-09-03
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Carmen S. Alvarez , Tin-Yau Chan , Chad Knutson , Vincent Madison , Thierry O. Fischmann , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Carmen S. Alvarez , Tin-Yau Chan , Chad Knutson , Vincent Madison , Thierry O. Fischmann , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

50. 发明授权

US5968736A Methods for recording the reaction history of a solid support 失效
标题翻译：用于记录固体支持物的反应历史的方法
公开(公告)号：US5968736A
公开(公告)日：1999-10-19
申请号：US480821
申请日：1995-06-07
申请人： W. Clark Still , Michael H. Wigler , Michael H. J. Ohlmeyer , Lawrence W. Dillard , John C. Reader
发明人： W. Clark Still , Michael H. Wigler , Michael H. J. Ohlmeyer , Lawrence W. Dillard , John C. Reader
IPC分类号： G01N33/566 , C07B61/00 , C07C43/225 , C07C205/59 , C07C245/14 , C07C317/28 , C07D243/24 , C07D521/00 , C07H21/00 , C07K1/00 , C07K1/04 , C40B70/00 , G01N33/532 , G01N33/543 , G01N33/68 , G01N33/53
CPC分类号： G01N33/68 , C07D243/24 , C07H21/00 , C07K1/047 , C40B50/16 , G01N33/532 , G01N33/54353 , B01J2219/00572 , C07B2200/11 , C40B40/00 , C40B70/00
摘要： Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produced in the multi-stage synthesis, such as oligomers and synthetic non-repetitive organic molecules. Conveniently, nested families of compounds can be employed as identifiers, where number and/or position of a substituent define the choice. Alternatively, detectable functionalities may be employed, such as radioisotopes, fluorescers, halogens, and the like, where presence and ratios of two different groups can be used to define stage or choice. Particularly, pluralities of identifiers may be used to provide a binary or higher code, so as to define a plurality of choices with only a few detachable tags. The particles may be screened for a characteristic of interest, particularly binding affinity, where the products may be detached from the particle or retained on the particle. The reaction history of the particles which are positive for the characteristic can be determined by the release of the tags and analysis to define the reaction history of the particle.
摘要翻译：提供了编码的组合化学，其中使用有机分子记录顺序合成方案，其定义了反应物的选择和阶段，作为相同或不同的信息位。可以在多级合成中产生各种产物，例如低聚物和合成的非重复有机分子。方便地，化合物的嵌套族可以用作标识符，其中取代基的数目和/或位置定义了选择。或者，可以使用可检测的官能团，例如放射性同位素，荧光剂，卤素等，其中两个不同基团的存在和比例可用于限定阶段或选择。特别地，可以使用多个标识符来提供二进制或更高代码，以便仅限定几个可拆卸标签来定义多个选择。可以筛选颗粒以获得感兴趣的特征，特别是结合亲和力，其中产物可以与颗粒分离或保留在颗粒上。对特征呈阳性的颗粒的反应历程可以通过标签的释放和分析来确定以确定颗粒的反应历程。

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