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公开(公告)号：US10233193B2
公开(公告)日：2019-03-19
申请号：US15575433
申请日：2016-05-20
Applicant: MERCK SHARP & DOHME CORP. , Tao Yu , Thomas H. Graham , Sherman T. Waddell , John A. McCauley , Andrew W. Stamford , John M. Sanders , Lihong Hu , Jiaqiang Cai , Lianyun Zhao
Inventor： Tao Yu , Thomas H. Graham , Sherman T. Waddell , John A. McCauley , Andrew W. Stamford , John M. Sanders , Lihong Hu , Jiaqiang Cai , Lianyun Zhao
IPC: A61K31/4375 , C07D491/147 , A61K31/4355 , A61K31/437 , C07D471/14 , A61K31/427 , A61K31/4402 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/635 , A61K31/675 , A61P31/18
Abstract: The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, m, R1, R2, R3, R3, R3, R4, R5 and R9 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject.
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2.发明申请公开(公告)号：US20140323519A1
公开(公告)日：2014-10-30
申请号：US14113382
申请日：2012-04-20
Applicant: M. Arshad Siddiqui , Lianyun Zhao , Amit K. Mandal
Inventor： M. Arshad Siddiqui , Lianyun Zhao , Amit K. Mandal
IPC: C07D263/22 , C07D233/36 , C07D217/24 , C07D207/27 , C07D209/46 , C07D235/26
CPC classification number: C07D263/22 , A01N43/36 , A01N43/38 , A01N43/42 , A01N43/76 , C07D207/27 , C07D209/46 , C07D217/24 , C07D233/36 , C07D235/26 , C07D263/20
Abstract: This invention relates to novel heterocyclic compounds that are useful for treating cancer and other cellular proliferative diseases and/or disorders associated with B-Raf activity. The compounds of the invention may be illustrated by the Formula (I). (Formula (I))
Abstract translation: 本发明涉及可用于治疗与B-Raf活性相关的癌症和其它细胞增殖性疾病和/或病症的新型杂环化合物。 本发明的化合物可以由式（I）说明。 （式（I））
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公开(公告)号：US08318735B2
公开(公告)日：2012-11-27
申请号：US12447710
申请日：2007-10-29
Applicant: Gerald W. Shipps, Jr. , Cliff C. Cheng , Xiaohua Huang , Thierry O. Fischmann , Jose S. Duca , Matthew Richards , Hongbo Zeng , Binyuan Sun , Panduranga Adulla Reddy , Lianyun Zhao , Shuyi Tang , Tzu T. Wong , Praveen K. Tadikonda , Luis E. Torres , M. Arshad Siddiqui , Michael P. Dwyer , Kartik M. Keertikar , Timothy J. Guzi
Inventor： Gerald W. Shipps, Jr. , Cliff C. Cheng , Xiaohua Huang , Thierry O. Fischmann , Jose S. Duca , Matthew Richards , Hongbo Zeng , Binyuan Sun , Panduranga Adulla Reddy , Lianyun Zhao , Shuyi Tang , Tzu T. Wong , Praveen K. Tadikonda , Luis E. Torres , M. Arshad Siddiqui , Michael P. Dwyer , Kartik M. Keertikar , Timothy J. Guzi
IPC: A61K31/5355 , A61K31/496 , C07D401/14 , C07D403/14 , C07D413/14
CPC classification number: C07D277/56 , A61K31/435 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04 , A61K2300/00
Abstract: The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
Abstract translation: 本发明涉及式（I）的新型苯胺基哌嗪衍生物，包含苯胺基哌嗪衍生物的组合物，以及使用苯胺基哌嗪衍生物治疗或预防增殖性病症，抗增殖病症，炎症，关节炎，中枢神经系统疾病 ，心血管疾病，脱发，神经元疾病，缺血性损伤，病毒性疾病，真菌感染或与蛋白激酶活性相关的病症。
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公开(公告)号：US08278337B2
公开(公告)日：2012-10-02
申请号：US12519731
申请日：2007-12-17
Applicant: David B. Belanger , M. Arshad Siddiqui , Patrick J. Curran , Blake Hamann , Lianyun Zhao , Panduranga Adulla P. Reddy , Praveen K. Tadikonda , Gerald W. Shipps, Jr. , Umar Faruk Mansoor
Inventor： David B. Belanger , M. Arshad Siddiqui , Patrick J. Curran , Blake Hamann , Lianyun Zhao , Panduranga Adulla P. Reddy , Praveen K. Tadikonda , Gerald W. Shipps, Jr. , Umar Faruk Mansoor
IPC: A61K31/44
CPC classification number: C07D417/12 , C07D213/81 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.
Abstract translation: 公开了式（I）的化合物，其中X是N或CH，Y是N或CR 5。 还公开了使用式1.0化合物治疗JNK和ERK介导的疾病的方法。
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公开(公告)号：US08293747B2
公开(公告)日：2012-10-23
申请号：US12669334
申请日：2008-07-17
Applicant: Panduranga Adulla P. Reddy , Lianyun Zhao , Praveen K. Tadikonda , Tzu Tshin Wong , Shuyi Tang , Luis E. Torres , David F. Cauble, Jr. , Timothy J. Guzi , M. Arshad Siddiqui
Inventor： Panduranga Adulla P. Reddy , Lianyun Zhao , Praveen K. Tadikonda , Tzu Tshin Wong , Shuyi Tang , Luis E. Torres , David F. Cauble, Jr. , Timothy J. Guzi , M. Arshad Siddiqui
IPC: A61K31/506 , C07D401/14 , A61K31/496 , A61K31/497 , A61K31/519 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04
CPC classification number: C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
Abstract: The present invention relates to novel heterocyclic amide compounds of Formula I: as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease.
Abstract translation: 本发明涉及式I的新型杂环酰胺化合物：本文所公开的或其药学上可接受的盐，溶剂化物，酯，前药或立体异构体。 还公开了包含所述化合物的组合物，以及使用所述化合物治疗或预防增殖性疾病，抗增殖性疾病，炎症，关节炎，神经性或神经变性疾病，心血管疾病，脱发，神经元疾病，缺血性疾病 损伤，病毒性疾病或真菌性疾病。
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Patent Agency Ranking
![PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS](/abs-image/US/2012/05/10/US20120114739A1/abs.jpg.150x150.jpg)
公开(公告)号：US20120114739A1
公开(公告)日：2012-05-10
申请号：US13263193
申请日：2010-04-08
Applicant: Yongqi Deng , Binyuan Sun , Hongbo Zeng , Matthew Richards , Gerald W. Shipps, JR. , Cliff C. Cheng , Yinyan Zhao , Andrew McRiner , Zhaoyang Meng , Yang Nan , Mehul F. Patel , Iwona E. Wrona , Panduranga Adulla Reddy , Brian M. Eklov , Shuyi Tang , Duan Liu , Amit K. Mandal , Lianyun Zhao , M. Asshad Siddiqui
Inventor： Yongqi Deng , Binyuan Sun , Hongbo Zeng , Matthew Richards , Gerald W. Shipps, JR. , Cliff C. Cheng , Yinyan Zhao , Andrew McRiner , Zhaoyang Meng , Yang Nan , Mehul F. Patel , Iwona E. Wrona , Panduranga Adulla Reddy , Brian M. Eklov , Shuyi Tang , Duan Liu , Amit K. Mandal , Lianyun Zhao , M. Asshad Siddiqui
IPC: A61K9/127 , A61K31/519 , A61K31/5377 , C07D491/048 , C07D495/04 , A61K31/538 , A61K31/551 , A61K31/553 , A61K31/541 , A61K31/554 , C07D498/04 , C12N9/99 , A61K31/704 , A61K39/395 , A61K33/36 , A61K38/50 , A61K33/24 , A61P29/00 , A61P37/08 , A61P11/00 , A61P37/06 , A61P35/00 , A61P35/02 , C07D487/04
CPC classification number: C07D487/04 , C07D519/00
Abstract: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.
Abstract translation: 本发明提供使用吡唑并[1,5-a]嘧啶化合物抑制mTOR的方法以及使用这些化合物治疗，预防，抑制或改善与mTOR相关的一种或多种疾病的方法。
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公开(公告)号：US20100286135A1
公开(公告)日：2010-11-11
申请号：US12669334
申请日：2008-07-17
Applicant: Panduranga Adulla P. Reddy , Lianyun Zhao , Praveen k. Tadikonda , Tzu Tshin Wong , Shuyi Tang , Luis E. Torres , David F. Cauble, JR. , Timothy J. Guzi , M. Arshad Siddiqui
Inventor： Panduranga Adulla P. Reddy , Lianyun Zhao , Praveen k. Tadikonda , Tzu Tshin Wong , Shuyi Tang , Luis E. Torres , David F. Cauble, JR. , Timothy J. Guzi , M. Arshad Siddiqui
IPC: A61K31/5383 , C07D401/14 , C07D413/14 , C07D417/14 , C07D409/14 , C07D405/14 , A61K31/5377 , A61K31/497 , A61K31/445
CPC classification number: C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
Abstract: The present invention relates to novel heterocyclic amide compounds of Formula I: as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease.
Abstract translation: 本发明涉及式I的新型杂环酰胺化合物：本文所公开的或其药学上可接受的盐，溶剂化物，酯，前药或立体异构体。 还公开了包含所述化合物的组合物，以及使用所述化合物治疗或预防增殖性疾病，抗增殖性疾病，炎症，关节炎，神经性或神经变性疾病，心血管疾病，脱发，神经元疾病，缺血性疾病 损伤，病毒性疾病或真菌性疾病。
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公开(公告)号：US20100179141A1
公开(公告)日：2010-07-15
申请号：US12519731
申请日：2007-12-17
Applicant: David B. Belanger , M. Arshad Siddiqui , Patrick J. Curran , Blake Hamann , Lianyun Zhao , Panduranga Adulla P. Reddy , Praveen K. Tadikonda , Gerald W. Shipps, JR. , Umar Faruk Mansoor
Inventor： David B. Belanger , M. Arshad Siddiqui , Patrick J. Curran , Blake Hamann , Lianyun Zhao , Panduranga Adulla P. Reddy , Praveen K. Tadikonda , Gerald W. Shipps, JR. , Umar Faruk Mansoor
IPC: A61K31/5377 , C07D417/12 , A61K31/4439 , A61K31/4545 , C07D417/14 , C07D401/12 , C07D413/14 , C07D405/12 , A61K31/444 , A61K31/502 , A61K31/497 , C07D213/81 , A61K31/44 , C07D401/14 , A61K31/506 , C07D513/04 , A61K31/517 , C07D471/04 , A61K31/496 , A61P19/02 , A61P29/00 , A61P11/06 , A61P25/28 , A61P1/00 , A61P3/10 , A61P17/06
CPC classification number: C07D417/12 , C07D213/81 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.
Abstract translation: 公开了式（I）的化合物，其中X是N或CH，Y是N或CR 5。 还公开了使用式1.0化合物治疗JNK和ERK介导的疾病的方法。
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公开(公告)号：US07652020B2
公开(公告)日：2010-01-26
申请号：US11142601
申请日：2005-06-01
Applicant: Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert D. Mazzola , Tin-Yau Chan , Henry A. Vaccaro , Brian McKittrick , Joseph A. Kozlowski , Brian J. Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline C. Ting , Kristin E. Rosner , Gerald W. Shipps, Jr. , M. Arshad Siddiqui , David B. Belanger , Chaoyang Dai , Dansu Li , Vinay M. Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
Inventor： Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert D. Mazzola , Tin-Yau Chan , Henry A. Vaccaro , Brian McKittrick , Joseph A. Kozlowski , Brian J. Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline C. Ting , Kristin E. Rosner , Gerald W. Shipps, Jr. , M. Arshad Siddiqui , David B. Belanger , Chaoyang Dai , Dansu Li , Vinay M. Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
IPC: A61K31/519 , A61K31/506 , A61K31/4709 , A61K31/43 , A61K31/4245 , C07D413/00 , C07D241/36 , C07D471/00 , C07D295/00 , C07D471/02 , C07D401/00 , C07D513/00 , C07D277/22 , C07D277/62 , C07D263/30 , C07D261/06 , C07D235/00 , C07D209/04 , C07D207/00 , C07D205/00 , C07D409/00 , C07D307/00
CPC classification number: C07D409/14 , C07C235/06 , C07C235/08 , C07C235/10 , C07C2601/08 , C07D207/20 , C07D207/26 , C07D209/44 , C07D215/14 , C07D217/06 , C07D263/32 , C07D295/185 , C07D307/52 , C07D333/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04
Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-α or combinations thereof.
Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或异构体，其可用于治疗由MMP，ADAM，TACE，TNF-α或其组合介导的疾病或病症。
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公开(公告)号：US07511040B2
公开(公告)日：2009-03-31
申请号：US11936380
申请日：2007-11-07
Applicant: David B. Belanger , M. Arshad Siddiqui , Timothy J. Guzi , Patrick J. Curran , Praveen K. Tadikonda , Blake Hamann , Panduranga Adulla P. Reddy , Lianyun Zhao
Inventor： David B. Belanger , M. Arshad Siddiqui , Timothy J. Guzi , Patrick J. Curran , Praveen K. Tadikonda , Blake Hamann , Panduranga Adulla P. Reddy , Lianyun Zhao
IPC: C07D471/02
CPC classification number: C07D487/04
Abstract: In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or Aurora kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or Aurora kinases using such compounds or pharmaceutical compositions. An illustrative compound of the invention is shown below:
Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的咪唑并吡嗪化合物作为蛋白质和/或极光激酶的抑制剂，制备这些化合物的方法，包含一种或多种这样的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 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与蛋白质或极光激酶相关的一种或多种疾病的方法。 本发明的说明性化合物如下所示：
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