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1. 发明申请

WO2005097745A1 ASYMMETRIC HYDROGENATION PROCESS USEFUL FOR THE PREPARATION OF CYCLOALKANOINDOLE DERIVATIVES 审中-公开
标题翻译：用于制备环烷基衍生物的非对称加氢方法
公开(公告)号：WO2005097745A1
公开(公告)日：2005-10-20
申请号：PCT/US2005/010501
申请日：2005-03-29
申请人： MERCK & CO., INC. , TELLERS, David, M. , HUMPHREY, Guy, R.
发明人： TELLERS, David, M. , HUMPHREY, Guy, R.
IPC分类号： C07D209/30
CPC分类号： C07D209/80 , C07B53/00 , C07D209/94
摘要： The present invention provides an asymmetric hydrogenation process for the preparation of chiral cycloalkanoindole DP receptor antagonists of formula I in high enantiomeric excess.
摘要翻译：本发明提供了用于以高对映体过量制备式I的手性环烷基吲哚DP受体拮抗剂的不对称氢化方法。

2. 发明申请

WO2002102374A1 AMINE SALT OF AN INTEGRIN RECEPTOR ANTAGONIST 审中-公开
标题翻译：整合素受体拮抗剂的胺盐
公开(公告)号：WO2002102374A1
公开(公告)日：2002-12-27
申请号：PCT/US2002/018906
申请日：2002-06-14
申请人： MERCK & CO., INC. , HUMPHREY, Guy, R. , XU, Wei
发明人： HUMPHREY, Guy, R. , XU, Wei
IPC分类号： A61K31/407
CPC分类号： C07D471/04
摘要： The tris(hydroxymethyl)aminomethane ("TRIS") salt of 3-(pyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-nonanoic acid is a potent antagonist of the integrin αvβ3 receptor and is useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salt as well as pharmaceutical compositions containing the salt and methods of using the salt.
摘要翻译： 3-（嘧啶-5-基）-9-（5,6,7,8-四氢 - [1,8] - 萘啶-2-基） - 三烯（三羟甲基）氨基甲烷（“TRIS”）盐抗酸是整合素αvβ3受体的有效拮抗剂，可用于预防和/或治疗骨质疏松症和血管再狭窄，以及与过度血管生成相关的病症，如黄斑变性，糖尿病性视网膜病变，动脉粥样硬化，炎症关节炎，癌症和转移性肿瘤生长。本发明还涉及制备新型盐的方法以及含有盐的药物组合物和使用该盐的方法。

3. 发明申请

WO2003072042A2 MALONATE-CLAISEN REARRANGEMENT FOR PREPARATION OF INTEGRIN RECEPTOR ANTAGONIST INTERMEDIATES 审中-公开
标题翻译：用于制备INTEGRIN受体拮抗剂中间体的MALONATE-CLAISEN重组
公开(公告)号：WO2003072042A2
公开(公告)日：2003-09-04
申请号：PCT/US2003/005476
申请日：2003-02-21
申请人： MERCK & CO., INC. , HUMPHREY, Guy, R. , FARR, Roger, N. , LEE, Jaemoon
发明人： HUMPHREY, Guy, R. , FARR, Roger, N. , LEE, Jaemoon
IPC分类号： A61K
CPC分类号： C07D471/04
摘要： A novel process is provided for the preparation of chiral unsaturated ester intermediates useful in the asymmetric syntheses of α νβ 3 integrin receptor antagonists. The instant process involves an efficient Claisen rearrangement of a malonate ester of a chiral allylic alcohol precursor followed by hydrolysis and decarboxylation. The unsaturated ester intermediates can be converted in a 2-step sequence into the desired substituted nonanoic acid derivatives.
摘要翻译：提供了用于制备可用于αnubeta 3整联蛋白受体拮抗剂的不对称合成的手性不饱和酯中间体的新方法。本方法涉及手性烯丙醇前体的丙二酸酯的高效Claisen重排，然后水解和脱羧。不饱和酯中间体可以以2步顺序转化成所需的取代的壬酸衍生物。

4. 发明申请

WO2009088729A1 PROCESS FOR PREPARING N-SUBSTITUTED HYDROXYPYRIMIDINONE CARBOXAMIDES 审中-公开
标题翻译：制备N-取代羟基吡啶酮羧酰胺的方法
公开(公告)号：WO2009088729A1
公开(公告)日：2009-07-16
申请号：PCT/US2008/087929
申请日：2008-12-22
申请人： MERCK & CO., INC. , HUMPHREY, Guy, R. , MILLER, Ross, A. , MALIGRES, Peter, E. , WEISSMAN, Steven
发明人： HUMPHREY, Guy, R. , MILLER, Ross, A. , MALIGRES, Peter, E. , WEISSMAN, Steven
IPC分类号： C07D239/52 , C07D413/12
CPC分类号： C07D413/12 , C07D239/52 , Y02P20/55
摘要： Processes for preparing certain N -arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl- 5-hydroxy -6-oxo-1,6-dihydropyrimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N -arylalkyl-1-(alkyl or aralkyl)- 2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrimidinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N -arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed.
摘要翻译：公开了制备某些N-芳基烷基-1-（烷基或芳烷基）-2-酰基氨基烷基-5-羟基-6-氧代-1,6-二氢嘧啶-4-甲酰胺的方法。在一个实施方案中，该方法包括酰化相应的N-芳基烷基-1-（烷基或芳烷基）-2-氨基烷基-5-酯保护的羟基-6-氧代-1,6-二氢嘧啶-4-甲酰胺中的游离胺和然后通过碱水解脱保护5-羟基。该方法的羟基嘧啶酮羧酰胺产物是HTV整合酶抑制剂，其可用于治疗HTV感染，治疗AIDS或延缓AIDS的发作或进展。还公开了可用作过程中间体的某些酯化的N-芳基烷基羟基嘧啶酮甲酰胺。

5. 发明申请

WO2003072042A3 MALONATE-CLAISEN REARRANGEMENT FOR PREPARATION OF INTEGRIN RECEPTOR ANTAGONIST INTERMEDIATES 审中-公开
公开(公告)号：WO2003072042A3
公开(公告)日：2003-09-04
申请号：PCT/US2003/005476
申请日：2003-02-21
申请人： MERCK & CO., INC. , HUMPHREY, Guy, R. , FARR, Roger, N. , LEE, Jaemoon
发明人： HUMPHREY, Guy, R. , FARR, Roger, N. , LEE, Jaemoon
IPC分类号： C07D239/26
摘要： A novel process is provided for the preparation of chiral unsaturated ester intermediates useful in the asymmetric syntheses of α νβ 3 integrin receptor antagonists. The instant process involves an efficient Claisen rearrangement of a malonate ester of a chiral allylic alcohol precursor followed by hydrolysis and decarboxylation. The unsaturated ester intermediates can be converted in a 2-step sequence into the desired substituted nonanoic acid derivatives.

6. 发明申请

WO2014088983A1 REGIOSELECTIVE N-2 ARYLATION OF INDAZOLES 审中-公开
标题翻译：注射剂N-2芳族化合物
公开(公告)号：WO2014088983A1
公开(公告)日：2014-06-12
申请号：PCT/US2013/072710
申请日：2013-12-03
申请人： MERCK SHARP & DOHME CORP. , CHUNG, Cheol, K. , SCOTT, Mark, E. , BULGER, Paul Gerard , BELYK, Kevin Michael , LIMANTO, John , HUMPHREY, Guy, R.
发明人： CHUNG, Cheol, K. , SCOTT, Mark, E. , BULGER, Paul Gerard , BELYK, Kevin Michael , LIMANTO, John , HUMPHREY, Guy, R.
IPC分类号： A61K31/454
CPC分类号： C07D401/10
摘要： A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.
摘要翻译：提供了一种用于有效制备结构式I的不对称化合物的新方法：包括铜催化的碳 - 氮交叉偶联步骤。作为本发明一部分描述的方法可用于制备可用于治疗癌症的聚（ADP-核糖）聚合酶（PARP）抑制剂。特别地，本发明描述了制备PARP抑制剂2- {4 - [（3S） - 哌啶-3-基]苯基} -2H-吲唑-7-甲酰胺的方法。

7. 发明申请

WO2019209607A1 NOVEL PROCESS FOR SYNTHESIS OF A PHENOXY DIAMINOPYRIMIDINE COMPOUND 审中-公开
公开(公告)号：WO2019209607A1
公开(公告)日：2019-10-31
申请号：PCT/US2019/028014
申请日：2019-04-18
申请人： MERCK SHARP & DOHME CORP. , MSD WERTHENSTEIN BIOPHARMA GMBH , MALONEY, Kevin, M. , BASU, Kallol , CHUNG, John, Y.L. , DESMOND, Richard , DI MASO, Michael James , HUMPHREY, Guy, R. , LEE, Alfred, Y. , LEHNHERR, Dan , PENG, Feng , REN, Hong , WEISEL, Mark , ZHANG, Siwei , LARPENT, Patrick
发明人： MALONEY, Kevin, M. , BASU, Kallol , CHUNG, John, Y.L. , DESMOND, Richard , DI MASO, Michael James , HUMPHREY, Guy, R. , LEE, Alfred, Y. , LEHNHERR, Dan , PENG, Feng , REN, Hong , WEISEL, Mark , ZHANG, Siwei , LARPENT, Patrick
IPC分类号： A61K31/505
摘要： Disclosed herein is a novel process for preparing Compound A free base, 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-isopropyl-2-methoxybenzenesulfonamide, and a citrate salt of Compound A with simplified chemistry and a high overall yield: Compound A. In one embodiment, the overall yield from the starting material 2-isopropylphenol to Compound A citrate salt is greater than 50%. In another embodiment, the overall yield is greater than 60%. Also disclosed herein are novel salts and solvates of Compound A.

8. 发明申请

WO2015084763A2 PROCESS FOR MAKING REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：制备逆转录酶抑制剂的过程
公开(公告)号：WO2015084763A2
公开(公告)日：2015-06-11
申请号：PCT/US2014/068008
申请日：2014-12-02
申请人： MERCK SHARP & DOHME CORP. , CAO, Yang , GAUTHIER, Donald, R., Jr. , HUMPHREY, Guy, R. , ITOH, Tetsuji , JOURNET, Michel , QIAN, Gang , SHERRY, Benjamin, D. , TSCHAEN, David, M.
发明人： CAO, Yang , GAUTHIER, Donald, R., Jr. , HUMPHREY, Guy, R. , ITOH, Tetsuji , JOURNET, Michel , QIAN, Gang , SHERRY, Benjamin, D. , TSCHAEN, David, M.
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D213/69 , C07D213/78
摘要： The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase and HIV replication, and the treatment of human immunodeficiency virus infection in humans.
摘要翻译：本发明涉及合成3-（取代的苯氧基）-1 - [（5-氧代-4,5-二氢-1H-1,2,4-三唑-5-基）甲基]） - 吡啶-2（1H） - 酮衍生物。通过本发明方法合成的化合物是可用于抑制逆转录酶和HIV复制的HIV逆转录酶抑制剂，以及治疗人类免疫缺陷病毒感染。

9. 发明申请

WO2020263660A1 PROCESS FOR THE PREPARATION OF 2-FLUOROADENINE 审中-公开
公开(公告)号：WO2020263660A1
公开(公告)日：2020-12-30
申请号：PCT/US2020/038304
申请日：2020-06-18
申请人： MERCK SHARP & DOHME CORP. , CHUNG, John, Y. L. , HONG, Cynthia, Marilyn , HUMPHREY, Guy, R. , MALONEY, Kevin, M. , XU, Yingju , VARSOLONA, Richard, J.
发明人： CHUNG, John, Y. L. , HONG, Cynthia, Marilyn , HUMPHREY, Guy, R. , MALONEY, Kevin, M. , XU, Yingju , VARSOLONA, Richard, J.
IPC分类号： A61K31/7064 , A61P31/18 , C07D307/33
摘要： The present invention provides processes for the preparation of 2-fluoroadenine, as well as certain intermediates useful in the preparation of 2'-deoxy-4'-C-ethynyl-2-fluoroadenosine (EFdA): EFdA.

10. 发明申请

WO2017091453A1 NOVEL PROCESSES FOR MAKING SUBSTITUTED QUINAZOLINE COMPOUNDS USING HYDROGEN BONDING CATALYSTS 审中-公开
标题翻译：用氢键连接催化剂制备取代喹唑啉化合物的新工艺
公开(公告)号：WO2017091453A1
公开(公告)日：2017-06-01
申请号：PCT/US2016/062654
申请日：2016-11-18
申请人： MERCK SHARP & DOHME CORP. , CHUNG, Cheol, K. , HUMPHREY, Guy, R. , LIU, Zhijian , MCLAUGHLIN, Mark , XU, Yingju , YU, Younong
发明人： CHUNG, Cheol, K. , HUMPHREY, Guy, R. , LIU, Zhijian , MCLAUGHLIN, Mark , XU, Yingju , YU, Younong
IPC分类号： A61K31/517 , A61P31/12 , C07C309/30 , C07D239/72 , C07D239/84
CPC分类号： A61K31/517 , C07D239/84
摘要： Disclosed herein is a novel process for preparing substituted quinazoline compounds of formula (I) using a hydrogen bonding catalyst.
摘要翻译：本文公开了一种使用氢键催化剂制备式（I）的取代喹唑啉化合物的新方法。

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