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1. 发明申请

WO2010042392A2 HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：艾滋病毒整合抑制剂
公开(公告)号：WO2010042392A2
公开(公告)日：2010-04-15
申请号：PCT/US2009/059308
申请日：2009-10-02
申请人： MERCK & CO., INC. , ISAACS, Richard, C. A. , THOMPSON, Wayne, J. , WILLIAMS, Peter, D. , SU, Dai-Shi , VENKATRAMAN, Shankar , EMBREY, Mark, W. , FISHER, Thorsten, E. , WAI, John, S. , DUBOST, David, C. , BALL, Richard, G. , CHOI, Eric, J. , PEI, Tao , TRICE, Sarah, L. , CAMPBELL, Neil , MADDESS, Matthew , MALIGRES, Peter, E. , SHEVLIN, Michael , SONG, Zhiguo Jake , STEINHUEBEL, Dietrich, P. , STROTMAN, Neil, A. , YIN, Jingjun
发明人： ISAACS, Richard, C. A. , THOMPSON, Wayne, J. , WILLIAMS, Peter, D. , SU, Dai-Shi , VENKATRAMAN, Shankar , EMBREY, Mark, W. , FISHER, Thorsten, E. , WAI, John, S. , DUBOST, David, C. , BALL, Richard, G. , CHOI, Eric, J. , PEI, Tao , TRICE, Sarah, L. , CAMPBELL, Neil , MADDESS, Matthew , MALIGRES, Peter, E. , SHEVLIN, Michael , SONG, Zhiguo Jake , STEINHUEBEL, Dietrich, P. , STROTMAN, Neil, A. , YIN, Jingjun
IPC分类号： A61K31/553 , C07D487/04 , C07D281/10 , A61K31/55 , A61P31/18
CPC分类号： C07D498/04 , C07D487/04 , H01L2924/0002 , H01L2924/00
摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I), wherein X 1 , X 2 , Y, R 1A , R 1B , R 2 and R 3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.
摘要翻译：式I化合物是HIV整合酶抑制剂和HIV复制抑制剂：（I），其中X1，X2，Y，R1A，R1B，R2和R3如本文所定义。该化合物可用于预防或治疗艾滋病毒感染，并预防，治疗或延迟艾滋病的发病或进展。该化合物用作抗体作为化合物本身（或其水合物或溶剂化物）或以药学上可接受的盐形式的HIV感染和AIDS。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。还描述了制备式I化合物的方法及其中间体。

2. 发明申请

WO2010042391A2 HIV INTEGRASE INHIBITORS 审中-公开
标题翻译： HIV整合酶抑制剂
公开(公告)号：WO2010042391A2
公开(公告)日：2010-04-15
申请号：PCT/US2009/059306
申请日：2009-10-02
申请人： MERCK SHARP & DOHME CORP. , ISAACS, Richard, C. A. , THOMPSON, Wayne, J. , WILLIAMS, Peter, D. , SU, Dai-Shi , VENKATRAMAN, Shankar , EMBREY, Mark, W. , FISHER, Thorsten, E. , WAI, John, S. , DUBOST, David, C. , BALL, Richard, G. , CHOI, Eric, J. , PEI, Tao , TRICE, Sarah, L.
发明人： ISAACS, Richard, C. A. , THOMPSON, Wayne, J. , WILLIAMS, Peter, D. , SU, Dai-Shi , VENKATRAMAN, Shankar , EMBREY, Mark, W. , FISHER, Thorsten, E. , WAI, John, S. , DUBOST, David, C. , BALL, Richard, G. , CHOI, Eric, J. , PEI, Tao , TRICE, Sarah, L.
IPC分类号： A61K31/553 , C07D487/04 , C07D281/10 , A61K31/55 , A61P31/18
CPC分类号： C07D498/04 , C07D487/04 , H01L2924/0002 , H01L2924/00
摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I), wherein X 1 , X 2 , Y, R 1A , R 1B , R 2 and R 3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：式I化合物为HIV整合酶抑制剂和HIV复制抑制剂：（I）其中X 1，X 2，Y，Y， R 1A，R 1B，R 2和R 3如本文所定义。该化合物可用于预防或治疗HIV感染以及预防，治疗或延迟AIDS的发作或进展。这些化合物作为化合物本身（或其水合物或溶剂合物）或以药学上可接受的盐的形式用于抗HIV感染和AIDS。这些化合物及其盐可以用作药物组合物的成分，任选地与其他抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

3. 发明申请

WO2010088167A1 BRIDGED COMPOUNDS AS HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：桥联化合物作为HIV整合抑制剂
公开(公告)号：WO2010088167A1
公开(公告)日：2010-08-05
申请号：PCT/US2010/021920
申请日：2010-01-25
申请人： MERCK SHARP & DOHME CORP. , VENKATRAMAN, Shankar , WAI, John, S. , THOMPSON, Wayne , KIM, Boyoung , ISAACS, Richard C.A. , LOUGHRAN, H. Marie , SU, Dai-Shi , LIM, John , EMBREY, Mark, W. , WILLIAMS, Peter, D.
发明人： VENKATRAMAN, Shankar , WAI, John, S. , THOMPSON, Wayne , KIM, Boyoung , ISAACS, Richard C.A. , LOUGHRAN, H. Marie , SU, Dai-Shi , LIM, John , EMBREY, Mark, W. , WILLIAMS, Peter, D.
IPC分类号： A01N43/46 , A61K31/55
CPC分类号： C07D487/18 , C07D471/18 , C07D491/18
摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: the asterisk * in Q denotes the point of attachment to the rest of the compound; and n, L1, L2, X 1 , X 2 , χ 3 , Y, Z, R 1 , R 2 and R 3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：式I化合物是HIV整合酶和HIV复制抑制剂的抑制剂：Q中的星号*表示与化合物其余部分的连接点; 并且n，L1，L2，X1，X2，... 3，Y，Z，R1，R2和R3在本文中定义。该化合物可用于预防或治疗艾滋病毒感染，并预防，治疗或延迟艾滋病的发病或进展。该化合物用作抗体作为化合物本身（或其水合物或溶剂化物）或以药学上可接受的盐形式的HIV感染和AIDS。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

4. 发明申请

WO2008010964A1 1-HYDROXY NAPHTHYRIDINE COMPOUNDS AS ANTI-HIV AGENTS 审中-公开
标题翻译： 1-羟基萘啶化合物作为抗HIV药物
公开(公告)号：WO2008010964A1
公开(公告)日：2008-01-24
申请号：PCT/US2007/016052
申请日：2007-07-13
申请人： MERCK & CO., INC. , WILLIAMS, Peter, D. , VENKATRAMAN, Shankar , LANGFORD, H. Marie , KIM, Boyoung , BOOTH, Theresa, M. , GROBLER, Jay, A. , STAAS, Donnette , RUZEK, Rowena, D. , EMBREY, Mark, W. , WISCOUNT, Catherine, M. , LYLE, Terry, A.
发明人： WILLIAMS, Peter, D. , VENKATRAMAN, Shankar , LANGFORD, H. Marie , KIM, Boyoung , BOOTH, Theresa, M. , GROBLER, Jay, A. , STAAS, Donnette , RUZEK, Rowena, D. , EMBREY, Mark, W. , WISCOUNT, Catherine, M. , LYLE, Terry, A.
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： 1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and/or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and vaccines.
摘要翻译：式I的1-羟基萘啶化合物（例如，1-羟基萘啶-2（1H） - 酮化合物是HIV整合酶和/或HIV核糖核酸酶H和HIV复制抑制剂的抑制剂：（I）其中X和R 1 -R 6是这些化合物可用于预防和治疗艾滋病毒感染以及艾滋病的预防，延迟发作和治疗。该化合物用于抗艾滋病毒感染和艾滋病作为化合物本身或以其形式化合物及其盐可以用作药物组合物中的成分，任选地与其它抗HIV剂如HIV抗病毒剂，免疫调节剂，抗生素和疫苗组合使用。

5. 发明申请

WO2005051915A1 PYRIDIN-4-YLAMINE COMPOUNDS USEFUL IN THE TREATMENT OF NEUROPATHIC PAIN 审中-公开
标题翻译：用于治疗神经痛疼痛的吡啶-4-YLAMINE化合物
公开(公告)号：WO2005051915A1
公开(公告)日：2005-06-09
申请号：PCT/US2004/038669
申请日：2004-11-18
申请人： MERCK & CO., INC. , LIM, Jongwon , BOUERES, Julia, K. , MUNOZ, Benito , PRACITTO, Richard , STOCK, Nicholas , VENKATRAMAN, Shankar
发明人： LIM, Jongwon , BOUERES, Julia, K. , MUNOZ, Benito , PRACITTO, Richard , STOCK, Nicholas , VENKATRAMAN, Shankar
IPC分类号： C07D215/00
CPC分类号： C07D219/12 , C07D215/46
摘要： The present invention is directed to a method of use of triazolo-pyridazine compounds in the treatment of neuropathic pain. The present invention is also directed to the use of triazolo-pyridazine compounds in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson’s disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders - such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal and other diseases. The present invention is also directed to novel triazolo-pyridazine compounds that selectively bind to α 2 δ-1 subunit of Ca channels.
摘要翻译：本发明涉及使用三唑并哒嗪化合物治疗神经性疼痛的方法。本发明还涉及三唑并 - 哒嗪化合物在治疗精神病和情绪障碍（例如精神分裂症，焦虑症，抑郁症，双相性精神障碍和恐慌）以及治疗疼痛方面的应用，帕金森病疾病，认知功能障碍，癫痫，昼夜节律和睡眠障碍 - 如转移工作诱导的睡眠障碍和时差，吸毒成瘾，药物滥用，戒毒等疾病。本发明还涉及选择性结合Ca通道的α2dta-1亚基的新型三唑并哒嗪化合物。

6. 发明申请

WO2005041971A1 TRIAZOLO-PYRIDAZINE COMPOUNDS AND DERIVATIVES THEREOF USEFUL IN THE TREATMENT OF NEUROPATHIC PAIN 审中-公开
标题翻译：三唑并吡啶化合物及其衍生物可用于治疗神经性疼痛
公开(公告)号：WO2005041971A1
公开(公告)日：2005-05-12
申请号：PCT/US2004/034466
申请日：2004-10-15
申请人： MERCK & CO., INC. , LEBSACK, Alec D. , MUNOZ, Benito , PRACITTO, Richard , VENKATRAMAN, Shankar , WANG, Bowei , GUNZNER, Janet
发明人： LEBSACK, Alec D. , MUNOZ, Benito , PRACITTO, Richard , VENKATRAMAN, Shankar , WANG, Bowei , GUNZNER, Janet
IPC分类号： A61K31/5025
CPC分类号： C04B35/632 , C07D401/12 , C07D401/14 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The present invention is directed to a method of use of triazolo-pyridazine compounds in the treatment of neuropathic pain. The present invention is also directed to the use of triazolo-pyridazine compounds in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson’s disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders - such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal and other diseases. The present invention is also directed to novel triazolo-pyridazine compounds that selectively bind to α 2 δ-1 subunit of Ca channels.
摘要翻译：本发明涉及使用三唑并哒嗪化合物治疗神经性疼痛的方法。本发明还涉及三唑并 - 哒嗪化合物在治疗精神病和情绪障碍（例如精神分裂症，焦虑症，抑郁症，双相性精神障碍和恐慌）以及治疗疼痛中的应用，帕金森病疾病，认知功能障碍，癫痫，昼夜节律和睡眠障碍 - 如转移工作诱导的睡眠障碍和时差，吸毒成瘾，药物滥用，戒毒等疾病。本发明还涉及选择性结合Ca通道的α2dta-1亚基的新的三唑并哒嗪化合物。

7. 发明申请

WO2006023396A2 VLA-4 ANTAGONISTS 审中-公开
公开(公告)号：WO2006023396A2
公开(公告)日：2006-03-02
申请号：PCT/US2005/028768
申请日：2005-08-12
申请人： MERCK & CO., INC. , CHEN, Weichao , LESBACK, Alec, D. , MUNOZ, Benito , VENKATRAMAN, Shankar , WANG, Bowei
发明人： CHEN, Weichao , LESBACK, Alec, D. , MUNOZ, Benito , VENKATRAMAN, Shankar , WANG, Bowei
IPC分类号： C07K5/078 , A61K38/05 , A61P11/06 , A61P19/02 , A61P25/28
CPC分类号： C07K5/06139 , C07K5/06191
摘要： Compounds of Formula (I) are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of inflammatory bowel disease including ulcerative colitis and Crohn’s disease, multiple sclerosis, asthma, and rheumatoid arthritis.
摘要翻译：式（I）化合物是VLA-4的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。这些化合物可以配制成药物组合物，并且适用于治疗炎性肠病，包括溃疡性结肠炎和克罗恩病，多发性硬化，哮喘和类风湿性关节炎。

8. 发明申请

WO2020243519A1 COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY 审中-公开
公开(公告)号：WO2020243519A1
公开(公告)日：2020-12-03
申请号：PCT/US2020/035249
申请日：2020-05-29
申请人： IFM DUE, INC. , VENKATRAMAN, Shankar , KATZ, Jason , ROUSH, William R.
发明人： VENKATRAMAN, Shankar , KATZ, Jason , ROUSH, William R.
IPC分类号： C07D209/40 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D513/04 , A61P35/00 , A61K31/404 , A61K31/433 , A61K31/437 , A61K31/4427 , A61K31/506
摘要： This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

9. 发明申请

WO2009134747A1 METHOD AND APPARATUS FOR SPECTRALLY EFFICIENT LINK ADAPTATION USING HARQ IN OFDMA SYSTEMS 审中-公开
标题翻译：在OFDMA系统中使用HARQ的频谱效率链路适配的方法和装置
公开(公告)号：WO2009134747A1
公开(公告)日：2009-11-05
申请号：PCT/US2009/041899
申请日：2009-04-28
申请人： NORTEL NETWORKS LIMITED , NAMMI, Sairamesh , VENKATRAMAN, Shankar , CHHEDA, Ashvin
发明人： NAMMI, Sairamesh , VENKATRAMAN, Shankar , CHHEDA, Ashvin
IPC分类号： H04L12/26
CPC分类号： H04W72/04 , H04B7/024 , H04B7/0452 , H04J11/005 , H04L5/0023 , H04L5/0037
摘要： A method increases spectral efficiency in a communication system. The communication system includes at least one mobile station and is capable of transmitting messages encoded according to a plurality of available modulation coding schemes ("MCSs"). Each available MCS includes a modulation scheme and an effective coding rate. The MCSs are indexed according to increasing complexity. A signal-to-interference ratio ("SINR") is determined which is sufficient to satisfy a predetermined frame error rate ("FER"). A first MCS and a corresponding amount of transmissions needed to satisfy the predetermined FER at the SINR using the first MCS are determined. The first MCS has a higher effective coding rate than a second MCS. The second MCS sufficiently satisfies the predetermined FER at the SINR in a single transmission. A message encoded according to the first MCS is transmitted through the communication system using hybrid automatic repeat request ("HARQ")
摘要翻译：一种方法提高了通信系统中的频谱效率。通信系统包括至少一个移动站，并且能够发送根据多个可用调制编码方案（“MCS”）编码的消息。每个可用的MCS包括调制方案和有效的编码率。 MCS随着复杂性的增加而被索引。确定信号干扰比（“SINR”），其足以满足预定的帧错误率（“FER”）。确定使用第一MCS在SINR处满足预定FER所需的第一MCS和相应的传输量。第一MCS具有比第二MCS更高的有效编码率。第二MCS在单个传输中足够满足SINR下的预定FER。根据第一MCS编码的消息通过使用混合自动重传请求（“HARQ”）的通信系统被发送，

10. 发明申请

WO2009134742A1 METHOD AND APPARATUS FOR CANDIDATE LIST GENERATION FOR UPLINK V-MIMO 审中-公开
标题翻译：用于UPLINK V-MIMO的候选列表生成的方法和装置
公开(公告)号：WO2009134742A1
公开(公告)日：2009-11-05
申请号：PCT/US2009/041893
申请日：2009-04-28
申请人： NORTEL NETWORKS LIMITED , VENKATRAMAN, Shankar , CHEEDA, Ashvin , DEANE, Peter, Michael , CHEONG, Patrick, Lie, Chin
发明人： VENKATRAMAN, Shankar , CHEEDA, Ashvin , DEANE, Peter, Michael , CHEONG, Patrick, Lie, Chin
IPC分类号： H04J11/00
CPC分类号： H04W72/04 , H04B7/024 , H04B7/0452 , H04J11/005 , H04L5/0023 , H04L5/0037
摘要： A method selects mobile station candidates for use with virtual multiple-input multiple-output ("V-MIMO") in a communication system. The communication system includes at least one base station and a plurality of mobile stations. At least one downlink metric is determined for a first mobile station. The at least one downlink metric is used to determine eligibility for uplink V-MIMO candidate list selection. Responsive to determining that the first mobile station is eligible for uplink V-MIMO candidate list selection, the first mobile station is paired with a second mobile station eligible for uplink V-MIMO candidate list selection.
摘要翻译：一种方法选择在通信系统中使用虚拟多输入多输出（“V-MIMO”）的移动台候选。通信系统包括至少一个基站和多个移动台。为第一移动站确定至少一个下行链路度量。使用至少一个下行链路度量来确定上行链路V-MIMO候选列表选择的合格性。响应于确定第一移动台符合上行链路V-MIMO候选列表选择的条件，第一移动台与符合上行链路V-MIMO候选列表选择的第二移动台配对。

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