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1. 发明专利

IL293839A Inhibitors of enl/af9 yeats 未知
公开(公告)号：IL293839A
公开(公告)日：2022-08-01
申请号：IL29383922
申请日：2022-06-12
申请人： UNIV ROCKEFELLER , BRIDGE MEDICINES LLC , KHAN TANWEER A , LIVERTON NIGEL , FUKASE YOSHIYUKI , MAYAKO MICHINO , STAMFORD ANDREW W , MICHAEL W MILLER , HUGGINS DAVID , MEINKE PETER
IPC分类号： A61K31/437 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/538 , A61K45/06 , A61P35/00
摘要： Methods and compositions for treating leukemia are disclosed. Acylated 6-aminoindoles, acylated 6-aminopyrrolopyridines and acylated 3-aminopyrrolo[3,2-c]pyridazines of the following formula inhibit ENL/AF9 YEATS and are therefore useful for treating leukemia.

2. 发明专利

AU2020407589A1 Inhibitors of ENL/AF9 YEATS 未知
公开(公告)号：AU2020407589A1
公开(公告)日：2022-07-21
申请号：AU2020407589
申请日：2020-12-17
申请人： BRIDGE MEDICINES LLC , FUKASE YOSHIYUKI , HUGGINS DAVID , KHAN TANWEER A , LIVERTON NIGEL , MEINKE PETER , MICHINO MAYAKO , MILLER MICHAEL W , STAMFORD ANDREW W , THE ROCKEFELLER UNIV
发明人： KHAN TANWEER A , LIVERTON NIGEL , FUKASE YOSHIYUKI , MICHINO MAYAKO , STAMFORD ANDREW W , MILLER MICHAEL W , HUGGINS DAVID , MEINKE PETER , ALLIS C DAVID , WAN LILING , VACCA JOSEPH , LADDUWAHETTY TAMMY
IPC分类号： A61K31/409 , A61P35/00 , C07D209/00 , C07D487/04
摘要： Methods and compositions for treating leukemia are disclosed. Acylated 6-aminoindoles, acylated 6-aminopyrrolopyridines and acylated 3-aminopyrrolo[3,2-c]pyridazines of the following formula inhibit ENL/AF

3. 发明申请

WO2013048916A1 SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT 审中-公开
标题翻译：取代的环丙基化合物，包含这些化合物的组合物和处理方法
公开(公告)号：WO2013048916A1
公开(公告)日：2013-04-04
申请号：PCT/US2012/056792
申请日：2012-09-24
申请人： MERCK SHARP & DOHME CORP. , MILLER, Micheal, W. , STAMFORD, Andrew, W. , BASU, Kallol , GEISS, William, B. , EDMONDSON, Scott, D. , GUO, Zhiqiang
发明人： MILLER, Micheal, W. , STAMFORD, Andrew, W. , BASU, Kallol , GEISS, William, B. , EDMONDSON, Scott, D. , GUO, Zhiqiang
IPC分类号： C07D401/08
CPC分类号： C07D401/12 , C07D211/96 , C07D401/14
摘要： Substituted cyclopropyl compounds of the formula I and the pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the g-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. Another aspect of the invention that is of interest relates to compounds of formula la.
摘要翻译：公开了取代的式I的环丙基化合物及其药学上可接受的盐，用于治疗或预防2型糖尿病和类似病状。该化合物可用作g-蛋白偶联受体GPR-119的激动剂。还包括药物组合物和治疗方法。感兴趣的本发明的另一方面涉及式Ia的化合物。

4. 发明申请

WO2012138845A1 SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT 审中-公开
标题翻译：取代的环丙基化合物，包含这些化合物的组合物和处理方法
公开(公告)号：WO2012138845A1
公开(公告)日：2012-10-11
申请号：PCT/US2012/032303
申请日：2012-04-05
申请人： MERCK SHARP & DOHME CORP. , EDMONDSON, Scott , GUO, Zhiqiang , GEISS, William, B. , WOOD, Harold, B. , STAMFORD, Andrew, W. , MILLER, Michael, W. , DEMONG, Duane, E. , MORRIELLO, Gregori, J. , ANAND, Rajan , COLANDREA, Vincent, J. , MACALA, Megan , MALETIC, Milana , ZHU, Cheng , ZHU, Yuping , SUN, Wanying , ZHAO, Kake , HUANG, Yong , HARRIS, Joel, M. , CHANG, Lehua , KAR, Nam Fung , HU, Zhiyong , WANG, Liping , WANG, Bowei , LIU, Ping , SZEWCZYK, Jason, W.
发明人： EDMONDSON, Scott , GUO, Zhiqiang , GEISS, William, B. , WOOD, Harold, B. , STAMFORD, Andrew, W. , MILLER, Michael, W. , DEMONG, Duane, E. , MORRIELLO, Gregori, J. , ANAND, Rajan , COLANDREA, Vincent, J. , MACALA, Megan , MALETIC, Milana , ZHU, Cheng , ZHU, Yuping , SUN, Wanying , ZHAO, Kake , HUANG, Yong , HARRIS, Joel, M. , CHANG, Lehua , KAR, Nam Fung , HU, Zhiyong , WANG, Liping , WANG, Bowei , LIU, Ping , SZEWCZYK, Jason, W.
IPC分类号： A01N43/54 , A61K31/505 , A01N43/40 , A61K31/445
CPC分类号： C07D513/04 , A61K9/4858 , C07D211/22 , C07D401/12 , C07D405/04 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04
摘要： Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included
摘要翻译：公开了取代的式I的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病症。该化合物可用作G蛋白偶联受体GPR-119的激动剂。还包括药物组合物和治疗方法

5. 发明申请

WO2012138734A1 C5-C6 OXACYCLIC-FUSED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
标题翻译： C5-C6氧化亚铜二氧化物作为BACE抑制剂，组合物及其使用的化合物
公开(公告)号：WO2012138734A1
公开(公告)日：2012-10-11
申请号：PCT/US2012/032135
申请日：2012-04-04
申请人： MERCK SHARP & DOHME CORP. , CUMMING, Jared, N. , GILBERT, Eric, J. , STAMFORD, Andrew, W.
发明人： CUMMING, Jared, N. , GILBERT, Eric, J. , STAMFORD, Andrew, W.
IPC分类号： C07D285/00 , A61K31/54
CPC分类号： C07D513/04 , A61K31/54 , A61K31/549 , A61K45/06 , A61K2300/00
摘要： In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula : (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of ring A, ring B, ring C, R 2 , R 3 , R 4 , m, n, p, and -L 1 - is as defined herein. The novel compounds of the invention may be useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供了某些亚氨基二嗪二氧化物化合物，包括式（I）化合物及其互变异构体和立体异构体，以及所述化合物，所述互变异构体和所述立体异构体的药学上可接受的盐，其中环A，环B，环C，R 2，R 3，R 4，m，n，p和-L 1如本文所定义。本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括阿尔茨海默氏病。

6. 发明申请

WO2010144664A1 THIOPHENES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE 审中-公开
标题翻译：作为GLUCAGON受体拮抗剂的THIOPHENES，组合物及其使用方法
公开(公告)号：WO2010144664A1
公开(公告)日：2010-12-16
申请号：PCT/US2010/038113
申请日：2010-06-10
申请人： SCHERING CORPORATION , GILBERT, Eric, J. , MILLER,, Michael, W. , STAMFORD, Andrew, W. , GREENLEE, William, J.
发明人： GILBERT, Eric, J. , MILLER,, Michael, W. , STAMFORD, Andrew, W. , GREENLEE, William, J.
IPC分类号： C07D409/06 , A61K31/4155 , A61P3/10
CPC分类号： C07D409/06 , A61K31/4155 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds of the general formula (I): wherein R 1 , R 2 , R 3 , R 5 , s, and Z are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
摘要翻译：本发明涉及通式（I）的化合物：其中R 1，R 2，R 3，R 5，S和Z彼此独立地选自并且如本文所定义，包括该化合物的组合物，以及使用化合物作为胰高血糖素受体拮抗剂并用于治疗或预防2型糖尿病及其相关病症。

7. 发明申请

WO2009131974A1 THIOPHENYL-SUBSTITUTED 2-IMINO-3-METHYL PYRROLO PYRIMIDINONE COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
标题翻译：作为BACE-1抑制剂，组合物及其使用的噻吩基取代的2-亚氨基-3-甲基吡咯烷酮吡啶酮化合物
公开(公告)号：WO2009131974A1
公开(公告)日：2009-10-29
申请号：PCT/US2009/041201
申请日：2009-04-21
申请人： SCHERING CORPORATION , STAMFORD, Andrew, W. , ZHU, Zhaoning , MANDAL, Mihirbaran , LIU, Xiaoxiang
发明人： STAMFORD, Andrew, W. , ZHU, Zhaoning , MANDAL, Mihirbaran , LIU, Xiaoxiang
IPC分类号： C07D487/04 , A61P25/28 , A61K31/519
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides provides certain thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds (or tautomers or a pharmaceutically acceptable salts thereof) having the structural Formula (III): wherein R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and R 9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's Disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供某些噻吩基取代的2-亚氨基-3-甲基吡咯并嘧啶酮化合物，包括具有结构式（III）的化合物（或互变异构体或其药学上可接受的盐）：其中R2，R3， R 4，R 5，R 6，R 7，R 8和R 9各自独立地如本文所定义。还公开了包含一种或多种这样的化合物的药物组合物及其制备和用于治疗与淀粉样蛋白β（Aβ）蛋白质（包括阿尔茨海默病）相关的病理学的方法。

8. 发明申请

WO2007053506A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2007053506A1
公开(公告)日：2007-05-10
申请号：PCT/US2006/042193
申请日：2006-10-30
申请人： SCHERING CORPORATION , ZHU, Zhaoning , STAMFORD, Andrew, W. , MCKITTRICK, Brian
发明人： ZHU, Zhaoning , STAMFORD, Andrew, W. , MCKITTRICK, Brian
IPC分类号： C07D411/04 , A61K31/553
CPC分类号： C07D413/04 , C07F9/65848
摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein (W, R1, R2, R3, R4, R5, R6, and R7) are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula (I). Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin (D) and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula (I) in combination with a cholinesterase inhibitor or a muscarinic antagonist.
摘要翻译：公开了式（I）的化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物，其中（W，R 1，R 2，R 3，R 4，R 5，R 6和R 7）如说明书中所定义; 和包含式（I）化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法，以及抑制人类免疫缺陷病毒，plasmepins，组织蛋白酶（D）和原生动物酶的方法。还公开了使用式（I）化合物与胆碱酯酶抑制剂或毒蕈碱拮抗剂组合来治疗认知或神经退行性疾病的方法。

9. 发明申请

WO2006014944A1 MACROCYCLIC BETA-SECRETASE INHIBITORS 审中-公开
标题翻译：大分子β-分泌酶抑制剂
公开(公告)号：WO2006014944A1
公开(公告)日：2006-02-09
申请号：PCT/US2005/026468
申请日：2005-07-26
申请人： SCHERING CORPORATION , STAMFORD, Andrew, W. , HUANG, Ying , LI, Guoqing , STRICKLAND, Corey, O. , VOIGT, Johannes, H.
发明人： STAMFORD, Andrew, W. , HUANG, Ying , LI, Guoqing , STRICKLAND, Corey, O. , VOIGT, Johannes, H.
IPC分类号： C07D413/06
CPC分类号： C07D498/04 , C07D413/06
摘要： Disclosed are novel compounds of the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 , R 2 , R 3 , n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula (I). Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula (I) and at least one compound selected from the group consisting of -secretase inhibitors other than those of formula (I), HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
摘要翻译：公开了式（I）的新化合物或其药学上可接受的盐或溶剂化物，其中R

10. 发明申请

WO2017113288A1 FUSED TRICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：融合三环杂环化合物作为HIV整合酶抑制剂
公开(公告)号：WO2017113288A1
公开(公告)日：2017-07-06
申请号：PCT/CN2015/100106
申请日：2015-12-31
申请人： MERCK SHARP & DOHME CORP. , YU, Tao , WADDELL, Sherman T. , GRAHAM, Thomas H. , MCCAULEY, John A. , STAMFORD, Andrew W. , CAI, Jiaqiang , QI, Zhiqi
发明人： YU, Tao , WADDELL, Sherman T. , GRAHAM, Thomas H. , MCCAULEY, John A. , STAMFORD, Andrew W. , CAI, Jiaqiang , QI, Zhiqi
IPC分类号： C07D471/16 , C07D487/16 , A61K31/5025 , A61P31/18
CPC分类号： C07D471/16 , A61K31/427 , A61K31/4402 , A61K31/4985 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/5365 , A61K31/635 , A61K31/683
摘要： The present invention relates to Fused Tricyclic Heterocyclic Compounds of Formula (I) :and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocyclic Compound, and methods of using the Fused Tricyclic Heterocyclic Compounds for treating or preventing HIV infection in a subject.
摘要翻译：本发明涉及式（I）的稠合三环杂环化合物及其药学上可接受的盐，其中R 1，R 2和 R 3如本文所定义。本发明还涉及包含至少一种稠合三环杂环化合物的组合物，以及使用稠合三环杂环化合物治疗或预防受试者HIV感染的方法。

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