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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

WO2006115834A1 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO2006115834A1
公开(公告)日：2006-11-02
申请号：PCT/US2006/014092
申请日：2006-04-14
申请人： MERCK & CO., INC. , ALANI, Laman, L. , DUBOST, David, C. , FOSTER, Bruce, S. , GHOSH, Soumojeet , JAHANSOUZ, Hossain , POURKAVOOS, Nazaneen , REGE, Bhagwant , TATAVARTI, Aditya
发明人： ALANI, Laman, L. , DUBOST, David, C. , FOSTER, Bruce, S. , GHOSH, Soumojeet , JAHANSOUZ, Hossain , POURKAVOOS, Nazaneen , REGE, Bhagwant , TATAVARTI, Aditya
IPC分类号： A61K31/41 , C07D257/04
CPC分类号： C07D403/10
摘要： The compounds of the present invention are polymorphic crystalline forms of the compound 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid, which has the structure (I). Specifically, the compounds of the invention are selected from the group consisting of 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid of Claim 3 selected from the group consisting of 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form I, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form II, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form III, and 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form IV, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form V, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VI, 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VII, and 2-butyl-4-chloro-1-[(2’-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid monohydrate Form VIII.
摘要翻译：本发明的化合物是2-丁基-4-氯-1 - （（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-1-基的化合物的多晶型形式，其具有结构（I）。具体地说，本发明化合物选自2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑 -5-羧酸，其选自2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑 -5-甲酸盐酸盐形式I，2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸盐酸盐形式II，2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸盐酸盐形式III和 2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸一水合物形式IV，2-丁基-4 - 氯 - 1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸一水合物形式V，2-丁基-4-氯-1- 甲基] - 咪唑-5-羧酸一水合物形式VI，2-丁基-4-氯-1 - [（2' - （1H-四唑-5-基）联苯-4-基）（1-1H-四唑-5-基）联苯-4-基）甲基]咪唑-5--C 羧酸一水合物形式VII和2-丁基-4-氯-1 - [（2' - （1-H-四唑-5-基）联苯-4-基）甲基] - 咪唑-5-甲酸一水合物形式八。

4. 发明申请

WO2009117278A2 PROCESSES FOR PREPARING (AMINO-PYRAZOLOPYRIDINYL)METHOXY SUBSTITUTED BIARYL ETHERS 审中-公开
标题翻译：制备（氨基 - 吡唑并吡啶-2-基）甲氧基取代二异氰酸酯的方法
公开(公告)号：WO2009117278A2
公开(公告)日：2009-09-24
申请号：PCT/US2009/036616
申请日：2009-03-10
申请人： MERCK & CO., INC. , KUETHE, Jeffrey, T. , ZHONG, Yong Li , YASUDA, Nobuyoshi , TUCKER, Thomas, J. , PYE, Philip , ZHANG, Yangfeng , TYNEBOR, Robert , DUBOST, David, C. , BEUTNER, Gregory, L. , TELLERS, David, M.
发明人： KUETHE, Jeffrey, T. , ZHONG, Yong Li , YASUDA, Nobuyoshi , TUCKER, Thomas, J. , PYE, Philip , ZHANG, Yangfeng , TYNEBOR, Robert , DUBOST, David, C. , BEUTNER, Gregory, L. , TELLERS, David, M.
IPC分类号： A61P31/18 , C07D213/61 , C07D213/74 , C07D471/04
CPC分类号： C07D213/61 , C07D213/74 , C07D471/04 , Y02P20/55
摘要： Processes for preparing certain (amino-pyrazolopyridinyl)methoxy-substituted biaryl ethers and their salts are described. The substituted biaryl ethers are useful as HIV non-nucleoside reverse transcriptase inhibitors. The processes include coupling a biaryl ether with a suitably protected and activated pyrazolopyridinyl methanol and then removing the protective groups from the coupled product to provide the desired substituted biaryl ether in the form of a sulfonate salt or a sulfate salt. Earlier reaction steps and the intermediates employed and obtained therein are also described. Crystalline HCl and sulfate salts of a particular (amino-pyrazolopyridmyl)-methoxy~substituted biaryl ether are described as well.
摘要翻译：描述了制备某些（氨基 - 吡唑并吡啶基）甲氧基取代的联芳基醚及其盐的方法。取代的联芳基醚可用作HIV非核苷逆转录酶抑制剂。这些方法包括将联芳基醚与适当保护的和活化的吡唑并吡啶基甲醇偶联，然后从偶联产物中除去保护基团，以提供磺酸盐或硫酸盐形式的所需取代的联芳基醚。还描述了早期反应步骤及其中使用和获得的中间体。还描述了特定（氨基 - 吡唑并吡啶基） - 甲氧基 - 取代的联芳基醚的结晶HCl和硫酸盐。

5. 发明申请

WO2008013807A9 A NOVEL LACTIC ACID FORMULATION OF MK-0457 USEFUL FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2008013807A9
公开(公告)日：2008-01-31
申请号：PCT/US2007/016637
申请日：2007-07-24
申请人： MERCK & CO., INC. , DUBOST, David, C.
发明人： DUBOST, David, C.
IPC分类号： A61K47/12 , A61K31/506 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/14 , A61K9/16 , A61K9/00 , A61P35/00 , A61P35/02
摘要： A lactic acid formulation, and a process to prepare that formulation, of MK-0457 is disclosed:. Such a formulation is useful in the treatment of cancer.

6. 发明申请

WO2013025449A1 USE OF INORGANIC MATRIX AND ORGANIC POLYMER COMBINATIONS FOR PREPARING STABLE AMORPHOUS DISPERSIONS 审中-公开
标题翻译：无机基质和有机聚合物组合的使用制备稳定的无定形分散体
公开(公告)号：WO2013025449A1
公开(公告)日：2013-02-21
申请号：PCT/US2012/050221
申请日：2012-08-10
申请人： MERCK SHARP & DOHME CORP. , HIGGINS, John , DUBOST, David, C.
发明人： HIGGINS, John , DUBOST, David, C.
IPC分类号： A61K9/14
CPC分类号： A61K47/02 , A61K9/10 , A61K9/143 , A61K9/145 , A61K9/146 , A61K31/277 , A61K31/405 , A61K31/437 , A61K31/444 , A61K31/496 , A61K47/38
摘要： The present invention relates to methods for processing pharmaceutically active substances having poor water solubility in the presence of an inorganic matrix, e.g., magnesium aluminometasilicate, and a secondary polymer as a means of converting the crystalline API to substantially amorphous and stable form, i.e., the crystallinity is less than 5%. The methods of the invention result in more complete amorphization, increased solubility, drug loading and stability as compared to typical amorphization or literature methods.
摘要翻译：本发明涉及用于在无机基质例如硅铝酸镁的存在下加工具有差的水溶性的药物活性物质的方法，以及作为将结晶API转化成基本无定形和稳定形式的手段的方法，即，将结晶度小于5％。与典型的非晶化或文献方法相比，本发明的方法导致更完全的非晶化，增加的溶解度，药物负载和稳定性。

7. 发明申请

WO2011126969A1 PRODRUGS OF AN HIV REVERSE TRANSCRIPTASE INHIBITOR 审中-公开
标题翻译： HIV逆转录酶抑制剂的产品
公开(公告)号：WO2011126969A1
公开(公告)日：2011-10-13
申请号：PCT/US2011/031070
申请日：2011-04-04
申请人： MERCK SHARP & DOHME CORP. , JOLLY, Samson, M. , ANTHONY, Neville , GOMEZ, Robert , DUBOST, David, C. , WOODWARD, Rick, G.
发明人： JOLLY, Samson, M. , ANTHONY, Neville , GOMEZ, Robert , DUBOST, David, C. , WOODWARD, Rick, G.
IPC分类号： A61K31/44 , C07D471/02
CPC分类号： C07D471/04 , C07F9/6561
摘要： Compounds of Formula I are described: (I), wherein R P and R Q are defined herein. The compounds of Formula I are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV, and the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：描述了式I化合物：（I），其中RP和RQ在本文中定义。式I的化合物可用于抑制HIV逆转录酶，HIV的感染的预防和治疗以及预防，延缓发作或进展以及AIDS的治疗。该化合物可以用作药物组合物中的成分，任选地与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

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