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1. 发明申请

WO2009020588A1 PROCESS FOR MAKING THIOPHENE CARBOXAMIDE DERIVATIVE 审中-公开
标题翻译：制备硫代羧酰胺衍生物的方法
公开(公告)号：WO2009020588A1
公开(公告)日：2009-02-12
申请号：PCT/US2008/009389
申请日：2008-08-05
申请人： MERCK & CO., INC. , MERCK FROSST CANADA LTD. , DAVIES, Ian , DOLMAN, Sarah , GAUVREAU, Danny , HUGHES, Greg , O'SHEA, Paul
发明人： DAVIES, Ian , DOLMAN, Sarah , GAUVREAU, Danny , HUGHES, Greg , O'SHEA, Paul
IPC分类号： C07D333/38
CPC分类号： C07D333/38
摘要： The invention encompasses a process for making a thiophene carboxamide derivative, which is an EP4 antagonist useful for treating pain and inflammation.
摘要翻译：本发明包括制备噻吩甲酰胺衍生物的方法，其是用于治疗疼痛和炎症的EP4拮抗剂。

2. 发明申请

WO2008088690A3 A PROCESS FOR PREPARING DIAZABICYCLO[3.3.1] NONANE COMPOUNDS 审中-公开
公开(公告)号：WO2008088690A3
公开(公告)日：2008-07-24
申请号：PCT/US2008/000224
申请日：2008-01-08
申请人： MERCK & CO., INC. , MERCK FROSST CANADA LTD. , GAUVREAU, Danny , HUFFMAN, Mark, A. , HUGHES, Greg , ITOH, Tetsuji , YIN, Jingjun , LAU, Stephen , O'SHEA, Paul
发明人： GAUVREAU, Danny , HUFFMAN, Mark, A. , HUGHES, Greg , ITOH, Tetsuji , YIN, Jingjun , LAU, Stephen , O'SHEA, Paul
IPC分类号： C07D471/08 , C07C237/20
摘要： The invention is a process for preparing a diazabicyclo compound of formula (I) process for preparing a diazabicyclo compound of formula (I):where X is selected from the group consisting of hydrogen, C 1 -C 6 alkoxycarbonyl, and carbobenzyloxy; R 6 is selected from the group consisting of C 1 -C 6 alkyl, C 2 -C 6 alkenyl, and benzyl; and R 9 , R 10 , and R 11 are independently selected from the group consisting of hydrogen, halogen, and C 1 -C 6 alkyl. wherein the process involves cyclizing I-I, formula (II).

3. 发明申请

WO2010114978A1 RENIN INHIBITORS 审中-公开
标题翻译：雷宁抑制剂
公开(公告)号：WO2010114978A1
公开(公告)日：2010-10-07
申请号：PCT/US2010/029588
申请日：2010-04-01
申请人： MERCK SHARP & DOHME CORP. , MERCK FROSST CANADA LTD. , MCKAY, Daniel, J. , ARBOUR, Melissa , ASPIOTIS, Renee , CHEN, Austin , DOLMAN, Sarah Jennifer , FOURNIER, Pierre-Andre , GALLANT, Michel , HAN, Yongxin , HUGHES, Greg , JANEY, Jacob , JUTEAU, Helene , LACOMBE, Patrick , LALIBERTE, Sebastien , LAUZON, Sophie , MACDONALD, Dwight , MACKAY, Bruce , MELLON, Christophe , MOLINARO, Carmela , MORLEY, Krista, L. , O'SHEA, Paul , RAMTOHUL, Yeeman, K. , SIMARD, Daniel , TSUI, Chit
发明人： MCKAY, Daniel, J. , ARBOUR, Melissa , ASPIOTIS, Renee , CHEN, Austin , DOLMAN, Sarah Jennifer , FOURNIER, Pierre-Andre , GALLANT, Michel , HAN, Yongxin , HUGHES, Greg , JANEY, Jacob , JUTEAU, Helene , LACOMBE, Patrick , LALIBERTE, Sebastien , LAUZON, Sophie , MACDONALD, Dwight , MACKAY, Bruce , MELLON, Christophe , MOLINARO, Carmela , MORLEY, Krista, L. , O'SHEA, Paul , RAMTOHUL, Yeeman, K. , SIMARD, Daniel , TSUI, Chit
IPC分类号： A61K31/535
CPC分类号： C07D211/26 , C07D211/22 , C07D211/28 , C07D211/52 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/14
摘要： The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.
摘要翻译：本发明涉及联芳基哌啶基肾素抑制剂化合物及其在治疗心血管事件和肾功能不全中的用途。

4. 发明申请

WO2009143033A1 PROCESS FOR THE PREPARATION OF AN OREXIN RECEPTOR ANTAGONIST 审中-公开
标题翻译：制备OREXIN受体拮抗剂的方法
公开(公告)号：WO2009143033A1
公开(公告)日：2009-11-26
申请号：PCT/US2009/044284
申请日：2009-05-18
申请人： MERCK & CO., INC. , MERCK FROSST CANADA LTD. , CAMPEAU, Louis-charles , HUGHES, Gregory , GAUVREAU, Danny , GIRARDIN-RONDEAU, Melina , MELLON, Christophe , MOORE, Jeffrey, C. , O'SHEA, Paul , QUELLET, Stephane, G.
发明人： CAMPEAU, Louis-charles , HUGHES, Gregory , GAUVREAU, Danny , GIRARDIN-RONDEAU, Melina , MELLON, Christophe , MOORE, Jeffrey, C. , O'SHEA, Paul , QUELLET, Stephane, G.
IPC分类号： C07D401/12 , C07D401/14 , C07D233/96
CPC分类号： C07D401/14 , C07D233/96 , C07D401/12
摘要： The present invention is directed to processes for preparing a pyridyl piperidine compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.
摘要翻译：本发明涉及制备食欲肽受体拮抗剂的吡啶基哌啶化合物的方法，其可用于治疗或预防涉及食欲素受体的神经和精神疾病及疾病。

5. 发明申请

WO2010011584A2 PROCESS FOR MAKING A RENIN INHIBITOR 审中-公开
标题翻译：制备阮宁抑制剂的方法
公开(公告)号：WO2010011584A2
公开(公告)日：2010-01-28
申请号：PCT/US2009/051101
申请日：2009-07-20
申请人： MERCK & CO., INC. , MERCK FROSST CANADA LTD. , ANGELAUD, Remy , DAVIES, Ian , MAGUIRE, Courtney , LAU, Stephen , O'SHEA, Paul , SHULTZ, Scott
发明人： ANGELAUD, Remy , DAVIES, Ian , MAGUIRE, Courtney , LAU, Stephen , O'SHEA, Paul , SHULTZ, Scott
IPC分类号： C07D213/643
CPC分类号： C07D213/643
摘要： A salt of the compound (3 'R ,4 'S )-6-[2-(2,6-Dichloro-4-methyl-phenoxy)-ethoxy]-1',2',3',4',5',6'-hexahydro-[3,4']bipyridinyl-3'-carboxylic acid [2-chloro-5-(2-methoxy-ethyl)-benzyl]-cyclopropyl-amide selected from the group consisting of monoacetate salt and bis-D-tartrate salt. In one embodiment of the invention, the salt is (3 ', 4' S )-6-[2-(2,6-Dichloro-4-methyl-phenoxy)-ethoxy]-1',2',3',4',5',6'-hexahydro-[3,4']bipyridinyl-3'-carboxylic acid [2-chloro-5-(2-methoxy-ethyl)-benzyl]-cyclopropyl-amide monoacetate. In one embodiment of the invention, the salt is (3 'R , 4 'S )-6-[2-(2,6-Dichloro-4-methyl-phenoxy)-ethoxy]-1',2',3',4',5',6'-hexahydro-[3,4']bipyridinyl-3'-carboxylic acid [2-chloro-5-(2-methoxy-ethyl)-benzyl]-cyclopropyl-amide bis-D-tartrate. The invention also describes a asymmetric synthesis of (3'R, 4'S)-6-[2-(2,6-Dichloro-4-methyl-phenoxy)-ethoxy]-1',2',3',4',5',6'-hexahydro-[3,4']bipyridinyl-3'-carboxylic acid [2-chloro-5-(2-methoxy-ethyl)-benzyl]-cyclopropyl-amide as a monoacetate salt or as a bis-D-tartrate salt.
摘要翻译：化合物（3'R，4'S）-6- [2-（2,6-二氯-4-甲基 - 苯氧基） - 乙氧基] -1'，2'，3'，4'，5' 6'-六氢 - [3,4']联吡啶基-3'-羧酸[2-氯-5-（2-甲氧基 - 乙基） - 苄基] - 环丙基酰胺，其选自单乙酸盐和双 - D-酒石酸盐。在本发明的一个实施方案中，盐是（3'，4'S）-6- [2-（2,6-二氯-4-甲基 - 苯氧基） - 乙氧基] -1'，2'，3'，4' ，5'，6'-六氢 - [3,4']联吡啶-3'-羧酸[2-氯-5-（2-甲氧基 - 乙基） - 苄基] - 环丙基 - 酰胺单乙酸酯。在本发明的一个实施方案中，盐是（3'R，4'S）-6- [2-（2,6-二氯-4-甲基 - 苯氧基） - 乙氧基] -1'，2'，3'，4 '，5'，6'-六氢 - [3,4']联吡啶-3'-羧酸[2-氯-5-（2-甲氧基 - 乙基） - 苄基] - 环丙基 - 酰胺双-D-酒石酸盐。本发明还描述了（3'R，4'S）-6- [2-（2,6-二氯-4-甲基 - 苯氧基） - 乙氧基] -1'，2'，3'，4' 5'，6'-六氢 - [3,4']联吡啶-3'-羧酸[2-氯-5-（2-甲氧基 - 乙基） - 苄基] - 环丙基 - 酰胺，为单乙酸盐或二 -D-酒石酸盐。

6. 发明申请

WO2006017455A2 DIASTEREOSELECTIVE REDUCTIVE AMINATION PROCESS 审中-公开
标题翻译：二氧化硅选择性还原胺化工艺
公开(公告)号：WO2006017455A2
公开(公告)日：2006-02-16
申请号：PCT/US2005/027308
申请日：2005-07-29
申请人： MERCK & CO., INC. , MERCK FROSST CANADA LTD. , CHEN, Cheng Yi , DEVINE, Paul, N. , FOSTER, Bruce, S. , HUGHES, Greg , O'SHEA, Paul
发明人： CHEN, Cheng Yi , DEVINE, Paul, N. , FOSTER, Bruce, S. , HUGHES, Greg , O'SHEA, Paul
IPC分类号： C07C227/00
CPC分类号： C07C227/32 , C07B2200/07 , C07C227/04 , C07C227/18 , C07C229/14 , C07C229/20 , C07C229/36 , C07C249/02 , C07C315/04 , C07C317/32 , C07C251/24
摘要： This invention describes a reductive amination process whereby perfluorinated ketones or ketals are combined with α-aminoesters under basic conditions to form metal carboxylates. Diastereoselective reductions of the metal carboxylates enable access to two diastereomers, depending on the reducing conditions.
摘要翻译：本发明描述了还原胺化方法，其中全氟化酮或缩酮在碱性条件下与α-氨基酯组合以形成金属羧酸盐。取决于还原条件，金属羧酸盐的非对映选择性还原使得能够获得两种非对映异构体。

7. 发明申请

WO2007136672A2 SYNTHESIS OF A BIARYL SYNTHETIC INTERMEDIATE 审中-公开
标题翻译：二元合成中间体的合成
公开(公告)号：WO2007136672A2
公开(公告)日：2007-11-29
申请号：PCT/US2007/011777
申请日：2007-05-16
申请人： MERCK & CO., INC. , MERCK FROSST CANADA LTD. , ANGELAUD, Remy , O'SHEA, Paul , OUELLET, Stephane , ROY, Amelie
发明人： ANGELAUD, Remy , O'SHEA, Paul , OUELLET, Stephane , ROY, Amelie
CPC分类号： C07C41/26 , C07C41/16 , C07C41/18 , C07C41/22 , C07C41/30 , C07C43/225 , C07C43/23
摘要： An efficient process for manufacturing a biphenyl chloride chemical intermediate is disclosed. The biphenyl chloride is a synthetic intermediate for manufacturing a chemical compound which is a CETP inhibitor. The process comprises a CH activation step in which a phenyl bromide is coupled to the phenyl ring of a phenyl oxazoline to make a biphenyl structure.
摘要翻译：公开了制备联苯氯化物化学中间体的有效方法。联苯氯化物是用于制造作为CETP抑制剂的化合物的合成中间体。该方法包括CH活化步骤，其中苯基溴与苯基恶唑啉的苯环偶合以形成联苯结构。

8. 发明申请

WO2006052514A1 ASYMMETRIC HYDROGENATION OF ENAMIDES 审中-公开
标题翻译：不对称加氢法
公开(公告)号：WO2006052514A1
公开(公告)日：2006-05-18
申请号：PCT/US2005/039332
申请日：2005-11-01
申请人： MERCK & CO., INC. , MERCK FROSST CANADA LTD. , MCWILLIAMS, James, C. , ALLWEIN, Shawn, P. , NELSON, Todd, D. , O'SHEA, Paul , SHULTZ, Clinton, S.
发明人： MCWILLIAMS, James, C. , ALLWEIN, Shawn, P. , NELSON, Todd, D. , O'SHEA, Paul , SHULTZ, Clinton, S.
IPC分类号： C07D213/61 , C07C233/13
CPC分类号： C07C231/18 , C07D213/61 , C07C233/13
摘要： The present invention provides a process for the preparation of acyl amines of formula (I), enantiomerically enriched at the carbon atom marked with an *; wherein Y is N or CH; R 1 and R 2 are independently selected from H, halogen, C l-4 alkyl, OH, OC 1 -4alkyl, OSO 2 CH 3 , OSO 2 CF 3 , NO 2 , and phenyl optionally substituted with 1 to 3 substituents independently selected from CN, halogen, C l-4 alkyl optionally substituted with 1 to 5 halogen atoms, OH, OC l-4 alkyl, CO 2 C l-4 alkyl, and OC 1-4 alkyl optionally substituted with 1 to 5 halogen atoms; and R 3 is C(O)H, C(O)C 1-4 alkyl optionally substituted with 1 to 5 halogen atoms, C(O)aryl, C(O)CH 2 -aryl, C(O)O-C 1-10 alkyl, C(O)O-aryl, or C(O)OCH 2 -aryl; which comprises hydrogenating in the presence of hydrogen gas a prochiral enamide of formula (II), in a suitable organic solvent in the presence of a rhodium metal precursor complexed to a chiral mono- or bidentate phosphine ligand. A process for the preparation of an enamide of formula (II) which comprises reaction an aryl nitrile of formula (III), with a methylating agent selected from methylmagnesiumbromide, methylmagnesium-chloride, methyllithium and methyllithium-lithium bromide complex, in a suitable organic solvent and in the presence of R 3 -Cl or (R 3 ) 2 O, wherein R I , R 2 and R 3 areas defined in Claim 1.
摘要翻译：本发明提供了制备式（I）的酰胺的方法，在用*标记的碳原子上对映体富集; 其中Y是N或CH; R 1和R 2独立地选自H，卤素，C 1-4烷基，OH，OC 1 H 2 > - - 烷基，OSO 2，CH 3，OSO 2，CF 3，NO 2，/ SO 2 和任选被1至3个独立地选自CN，卤素，任选被1至5个卤素原子取代的C 1-4烷基的取代基取代的苯基，OH，OC 1-4，任选被1至5个卤素原子取代的C 1-4烷基，C 1-4烷基，和C 1-4烷基，和R 3是C（O）H，任选被1至5个卤素原子取代的C（O）C 1-4烷基，C（O）芳基，C（O） C（O）OC 1-10烷基，C（O）O-芳基或C（O）OCH 2， / SUB> - 芳基; 其包括在氢气存在下在合适的有机溶剂中在与手性单 - 或二齿膦配体络合的铑金属前体的存在下，将式（II）的前手性烯酰胺氢化。制备式（II）的酰胺的方法，其包括使式（III）的芳基腈与选自甲基溴化镁，甲基氯化镁，甲基锂和甲基锂 - 溴化锂络合物的甲基化剂在合适的有机溶剂并且在R 3 -Cl或（R 3）2 O 2的存在下，其中R 1，R 2，权利要求1中限定的第二和第三区域。

9. 发明申请

WO2009158308A1 SYNTHESIS OF CHIRAL AMINES 审中-公开
标题翻译：合成氨基酸
公开(公告)号：WO2009158308A1
公开(公告)日：2009-12-30
申请号：PCT/US2009/048129
申请日：2009-06-22
申请人： MERCK FROSST CANADA LTD. , O'SHEA, Paul , GOSSELIN, Francis , MCWILLIAMS, James, C.
发明人： O'SHEA, Paul , GOSSELIN, Francis , MCWILLIAMS, James, C.
IPC分类号： C07B43/04 , C07B53/00
CPC分类号： C07B53/00 , C07B43/04
摘要： The instant invention involves the enantioselective hydrogenation of isomeric N-H imines (N-unsubstituted) using a transition metal based catalyst modified with a chiral phosphine derivative to produce enantiomerically enriched chiral amines.
摘要翻译：本发明涉及使用用手性膦衍生物改性的过渡金属基催化剂对异构N-H亚胺（N-未取代的）进行对映选择性氢化以产生对映体富集的手性胺。

10. 发明申请

WO2009052625A1 NOVEL CRYSTALLINE SALTS OF MONTELUKAST 审中-公开
标题翻译： MONTELUKAST的新型晶体盐
公开(公告)号：WO2009052625A1
公开(公告)日：2009-04-30
申请号：PCT/CA2008/001875
申请日：2008-10-23
申请人： MERCK FROSST CANADA LTD. , O'SHEA, Paul
发明人： O'SHEA, Paul
IPC分类号： C07D215/18 , A61K31/47 , A61K31/573 , A61K31/58 , A61P11/06
CPC分类号： C07D215/18
摘要： The present application relates to crystalline 1,2-ethanedisulfonic acid salt and N,N'-dibenzylethylenediamine salt of montelukast. The salts are useful as therapeutic agents for the treatment of leukotriene mediated diseases and disorders. This application also relates to processes and intermediates for preparing the said salts and pharmaceutical compositions comprising the salts and optionally other therapeutic agents.
摘要翻译：本申请涉及孟鲁司特的结晶1,2-乙烷二磺酸盐和N，N'-二苄基乙二胺盐。所述盐可用作治疗白三烯介导的疾病和病症的治疗剂。本申请还涉及用于制备所述盐和包含所述盐和任选的其它治疗剂的药物组合物的方法和中间体。

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