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11. 发明申请

US20110009392A1 GAMMA SECRETASE MODULATORS 审中-公开
公开(公告)号：US20110009392A1
公开(公告)日：2011-01-13
申请号：US12671806
申请日：2008-08-04
申请人： Zhaoning Zhu , William J. Greenlee , John P. Caldwell , Robert D. Mazzola, JR. , Brian McKittrick , Chad E. Bennett , Xianhai Huang , Hubert B. Josien , Duane A. Burnett
发明人： Zhaoning Zhu , William J. Greenlee , John P. Caldwell , Robert D. Mazzola, JR. , Brian McKittrick , Chad E. Bennett , Xianhai Huang , Hubert B. Josien , Duane A. Burnett
IPC分类号： A61K31/55 , C07D487/04 , C07D235/02 , C07D498/04 , C07D491/04 , A61K31/4188 , A61K31/519 , A61K31/535 , A61K31/4353 , A61K31/435 , A61K31/47 , A61K31/505 , A61K31/397 , A61K31/4406 , A61K38/16 , A61P25/28
CPC分类号： C07D487/04 , C07D217/24 , C07D498/04
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, 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 central nervous system using such compounds or pharmaceutical compositions.

12. 发明申请

US20100298381A1 GAMMA SECRETASE MODULATORS 审中-公开
标题翻译： GAMMA秘密调节器
公开(公告)号：US20100298381A1
公开(公告)日：2010-11-25
申请号：US12676035
申请日：2008-09-25
申请人： Zhaoning Zhu , William J. Greenlee , John P. Caldwell , Robert D. Mazzola, JR. , Brian McKittrick , Chad E. Bennett , Duane A. Burnett
发明人： Zhaoning Zhu , William J. Greenlee , John P. Caldwell , Robert D. Mazzola, JR. , Brian McKittrick , Chad E. Bennett , Duane A. Burnett
IPC分类号： A61K31/454 , C07D403/10 , A61K31/4178 , C07D403/14 , A61P25/28 , A61P27/06 , A61P25/00
CPC分类号： C07D233/86 , C07D233/76 , C07D233/88 , C07D403/04
摘要： In its many embodiments, the present invention provides a novel class of 5-membered, nitrogen-containing heterocyclic compounds as modulators of gamma secretase, 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 central nervous system 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5元含氮杂环化合物作为γ-分泌酶的调节剂，制备这种化合物的方法，含有一种或多种这类化合物的药物组合物，制备药物制剂的方法，包括一种或更多这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。

13. 发明申请

US20130210805A1 QUINAZOLINONE-TYPE COMPOUNDS AS CRTH2 ANTAGONISTS 有权
标题翻译：喹诺酮类化合物作为CRTH2拮抗剂
公开(公告)号：US20130210805A1
公开(公告)日：2013-08-15
申请号：US13878654
申请日：2011-10-06
申请人： Robert G. Aslanian , Christopher W. Boyce , Robert D. Mazzola, JR. , Brian A. McKittrick , Kevin D. McCormick , Anandan Palani , Jun Qin , Haiqun Tang , Dong Xiao , Younong Yu , John P. Caldwell , Elizabeth Helen Kelley , Hongjun Zhang , Phieng Siliphaivanh , Rachel N. MacCoss , Joey L. Methot , Jolicia Polivina Gauuan , Qin Jiang , Andrew J. Leyhane , Johny Biju , Li Dong , Xian Huang , Ning Shao , Wei Zhou , Pawan K. Dhondi
发明人： Robert G. Aslanian , Christopher W. Boyce , Robert D. Mazzola, JR. , Brian A. McKittrick , Kevin D. McCormick , Anandan Palani , Jun Qin , Haiqun Tang , Dong Xiao , Younong Yu , John P. Caldwell , Elizabeth Helen Kelley , Hongjun Zhang , Phieng Siliphaivanh , Rachel N. MacCoss , Joey L. Methot , Jolicia Polivina Gauuan , Qin Jiang , Andrew J. Leyhane , Johny Biju , Li Dong , Xian Huang , Ning Shao , Wei Zhou , Pawan K. Dhondi
IPC分类号： C07D239/91 , A61K31/517 , A61K45/06 , C07D403/10 , C07D417/10 , C07D413/10 , C07D405/10 , C07D413/14 , C07D498/10 , C07D403/14 , A61K31/55 , C07D401/14 , A61K31/5395 , C07D471/04 , C07D401/10
CPC分类号： C07D239/91 , A61K31/517 , A61K31/5395 , A61K31/55 , A61K45/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/10 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/10 , C07D471/04 , C07D498/10
摘要： This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.
摘要翻译：本申请提供式I化合物或其药学上可接受的盐，其中各个变量在本文中定义，以及制备这些化合物的方法，包含其的药物组合物及其用于治疗与CRTH2相关的疾病状态受体。

14. 发明申请

US20150057246A1 SILYL-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 审中-公开
标题翻译：含有SILYL的杂环化合物及其用于治疗病毒性疾病的方法
公开(公告)号：US20150057246A1
公开(公告)日：2015-02-26
申请号：US14345130
申请日：2012-09-11
申请人： Michael P. Dwyer , Kartik M. Keertikar , Qingbei Zeng , Robert D. Mazzola, JR. , John P. Caldwell , Haiqun Tang , Anilkumar Gopinadhan Nair , Bandarpalle B. Shankar , Stuart B. Rosenblum , Joseph A. Kozlowski
发明人： Michael P. Dwyer , Kartik M. Keertikar , Qingbei Zeng , Robert D. Mazzola, JR. , John P. Caldwell , Haiqun Tang , Anilkumar Gopinadhan Nair , Bandarpalle B. Shankar , Stuart B. Rosenblum , Joseph A. Kozlowski
IPC分类号： C07F7/08 , A61K45/06 , A61K31/695
CPC分类号： C07F7/0816 , A61K31/695 , A61K45/06 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395
摘要： The present invention relates to novel Silyl-Containing Heterocyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, B, C, D and R2 are as defined herein. The present invention also relates to compositions comprising at least one Silyl-Containing Heterocyclic Compound, and methods of using the Silyl-Containing Heterocyclic Compounds for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的新的含甲硅烷基的杂环化合物：（I）及其药学上可接受的盐，其中A，B，C，D和R2如本文所定义。本发明还涉及包含至少一种含甲硅烷基的杂环化合物的组合物，以及使用含有甲硅烷基的杂环化合物治疗或预防患者HCV感染的方法。

15. 发明授权

US08927559B2 Quinazolinone-type compounds as CRTH2 antagonists 有权
标题翻译：喹唑啉酮类化合物作为CRTH2拮抗剂
公开(公告)号：US08927559B2
公开(公告)日：2015-01-06
申请号：US13878654
申请日：2011-10-06
申请人： Robert G. Aslanian , Christopher W. Boyce , Robert D. Mazzola, Jr. , Brian A. McKittrick , Kevin D. McCormick , Anandan Palani , Jun Qin , Haiqun Tang , Dong Xiao , Younong Yu , John P. Caldwell , Elizabeth Helen Kelley , Hongjun Zhang , Phieng Siliphaivanh , Rachel N. MacCoss , Joey L. Methot , Jolicia Polivina Gauuan , Qin Jiang , Andrew J. Leyhane , Purakkattle Johny Biju , Li Dong , Xianhai Huang , Ning Shao , Wei Zhou , Pawan K. Dhondi , Ashwin U. Rao
发明人： Robert G. Aslanian , Christopher W. Boyce , Robert D. Mazzola, Jr. , Brian A. McKittrick , Kevin D. McCormick , Anandan Palani , Jun Qin , Haiqun Tang , Dong Xiao , Younong Yu , John P. Caldwell , Elizabeth Helen Kelley , Hongjun Zhang , Phieng Siliphaivanh , Rachel N. MacCoss , Joey L. Methot , Jolicia Polivina Gauuan , Qin Jiang , Andrew J. Leyhane , Purakkattle Johny Biju , Li Dong , Xianhai Huang , Ning Shao , Wei Zhou , Pawan K. Dhondi , Ashwin U. Rao
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72 , C07D401/00
CPC分类号： C07D239/91 , A61K31/517 , A61K31/5395 , A61K31/55 , A61K45/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/10 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/10 , C07D471/04 , C07D498/10
摘要： This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.
摘要翻译：本申请提供式I化合物或其药学上可接受的盐，其中各个变量在本文中定义，以及制备这些化合物的方法，包含其的药物组合物及其用于治疗与CRTH2相关的疾病状态受体。

16. 发明授权

US11141403B2 Benzimidazoles and indoles as taro inhibitors 有权
公开(公告)号：US11141403B2
公开(公告)日：2021-10-12
申请号：US16061481
申请日：2016-12-13
申请人： MERCK SHARP & DOHME CORP. , John P. Caldwell , Ginny Dai Ho , Sookhee N. Ha , Sandra J. Koseoglu , Marc A. Labroli , Sang Ho Lee , Christina Madsen-Duggan , Mihir Mandal , Jianping Pan , Weidong Pan , Terry Roemer , Jing Su , Christopher Michael Tan , Zheng Tan , Hao Wang , Christine Yang , Shu-Wei Yang
发明人： John P. Caldwell , Ginny Dai Ho , Sookhee N. Ha , Sandra J. Koseoglu , Marc A. Labroli , Sang Ho Lee , Christina Madsen-Duggan , Mihir Mandal , Jianping Pan , Weidong Pan , Terry Roemer , Jing Su , Christopher Michael Tan , Zheng Tan , Hao Wang , Christine Yang , Shu-Wei Yang
IPC分类号： A61K31/397 , A61P31/04 , A61K31/407 , C07D235/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D471/04
摘要： Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a β-lactam antibiotic.

17. 发明授权

US07041666B2 Adenosine A2a receptor antagonists 有权
标题翻译：腺苷A2a受体拮抗剂
公开(公告)号：US07041666B2
公开(公告)日：2006-05-09
申请号：US10304504
申请日：2002-11-26
申请人： Julius J. Matasi , John P. Caldwell , Deen Tulshian , Lisa S. Silverman , Bernard R. Neustadt
发明人： Julius J. Matasi , John P. Caldwell , Deen Tulshian , Lisa S. Silverman , Bernard R. Neustadt
IPC分类号： C07D487/04 , A61K31/519 , A61P25/18 , A61P25/16 , A61P25/28
CPC分类号： C07D487/04
摘要： Disclosed are compounds having the structural formula or pharmaceutically acceptable salts or solvates thereof, wherein R is optionally substituted heteroaryl, optionally substituted phenyl, cycloalkenyl, —C(═CH2)CH3, —C≡C—CH3, —CH═C(CH3)2, or —CH═CH—CH3; R2 is —W—X, —NR19(CH2)m—W—X, and —NR19CH(CH3)—W—X, or R2 is alkyl, alkenyl and —NR18R19, each optionally substituted —W—X; R3 is H, halo, alkyl, trifluoromethyl, alkoxy, alkoxyalkyl, hydroxyalkyl, alkylamino, alkylaminoalkyl, dialkylamino, dialkylaminoalkyl, aminoalkyl, aryl, heteroaryl, or CN; R18 is a bond, —CH(OH)—, —CH(CH3)—, —C(CH3)n—, —(CH2)n—or —O(CH2)n—; W is aryl or heteroaryl, each optionally substituted; X is H, NH2, or substituted amino, or X is —R18—Y-Z; and n, R19, Y and Z are as defined in the specification; pharmaceutical compositions thereof, and methods of treating stroke or central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment.
摘要翻译：公开了具有结构式或其药学上可接受的盐或溶剂化物的化合物，其中R是任选取代的杂芳基，任选取代的苯基，环烯基，-C（-CH 2 CH 2）CH 3 ，-C≡C-CH 3，-CH-C（CH 3）2，或-CH-CH-CH _{3 ; R 2是-WX，-NR 19（CH 2）2 -WX和-NR O SUP CH 3（CH 3 CH 3）-WX或R 2是烷基，烯基和-NR 18 R 12， 19，每个任选取代的-WX; R 3是H，卤素，烷基，三氟甲基，烷氧基，烷氧基烷基，羟基烷基，烷基氨基，烷基氨基烷基，二烷基氨基，二烷基氨基烷基，氨基烷基，芳基，杂芳基或CN; -CH（OH） - ， - CH（CH 3） - ， - （CH 3 CH 3） - ， - （CH 3 CH 3） n - - （CH 2）n - 或 - （CH 2）n - / > - ; W是芳基或杂芳基，各自任选被取代; X是H，NH 2或取代的氨基，或X是-R 18 -Y-Z; 和n，R 19，Y和Z如说明书中所定义; 其药物组合物，以及通过将本发明化合物给予需要这种治疗的患者来治疗中风或中枢神经系统疾病的方法。}

18. 外观设计

USD385548S Icon for a computer housing 失效
公开(公告)号：USD385548S
公开(公告)日：1997-10-28
申请号：US20423
申请日：1994-03-25
申请人： Robert W. Paterson , John P. Caldwell
设计人： Robert W. Paterson , John P. Caldwell

19. 外观设计

USD374439S Front panel of a desktop personal computer 失效
公开(公告)号：USD374439S
公开(公告)日：1996-10-08
申请号：US36788
申请日：1995-03-27
申请人： Robert W. Paterson , Graham P. Marshall , John P. Caldwell , Scott M. Belliveau
设计人： Robert W. Paterson , Graham P. Marshall , John P. Caldwell , Scott M. Belliveau

20. 外观设计

USD314076S Night depository for use with automated teller machine or similar article 失效
公开(公告)号：USD314076S
公开(公告)日：1991-01-22
申请号：US033541
申请日：1987-04-01
申请人： Alex M. Tarkany , John P. Caldwell , Jay Sucre
设计人： Alex M. Tarkany , John P. Caldwell , Jay Sucre

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