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1. 发明专利

CA2588398A1 POTASSIUM SALT OF AN HIV INTEGRASE INHIBITOR 未知
公开(公告)号：CA2588398A1
公开(公告)日：2006-06-08
申请号：CA2588398
申请日：2005-12-02
申请人： MERCK & CO INC , ANGELETTI P IST RICHERCHE BIO , MERCK SHARP & DOHME
发明人： JONES PHILIP , TUNG HSIEN-HSIN , KUMKE DANIEL J , SUMMA VINCENZO , PYE PHILIP , ANGELAUD REMY , MORRISON HENRY G , MANCHENO DANNY , BELYK KEVIN M , PRUZINSKY VANESSA , WAI LAWRENCE , COOPER V BRETT , MAHAJAN AMAR J
IPC分类号： C07D239/557 , A61K31/513 , A61P31/18 , C07D413/12
摘要： Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.

2. 发明专利

AU2005311671A1 Potassium salt of an HIV integrase inhibitor 未知
公开(公告)号：AU2005311671A1
公开(公告)日：2006-06-08
申请号：AU2005311671
申请日：2005-12-02
申请人： MERCK SHARP & DOHME , MERCK & CO INC , ANGELETTI P IST RICHERCHE BIO
发明人： BELYK KEVIN M , COOPER V BRETT , SUMMA VINCENZO , WAI LAWRENCE , MAHAJAN AMAR J , MANCHENO DANNY , PRUZINSKY VANESSA , JONES PHILIP , KUMKE DANIEL J , PYE PHILIP , TUNG HSIEN-HSIN , MORRISON HENRY G , ANGELAUD REMY
IPC分类号： C07D239/557 , A61K31/513 , A61P31/18 , C07D413/12
摘要： Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.

3. 发明专利

AT518844T 未知
公开(公告)号：AT518844T
公开(公告)日：2011-08-15
申请号：AT05852866
申请日：2005-12-02
申请人： MERCK SHARP & DOHME , ANGELETTI P IST RICHERCHE BIO , MERCK SHARP & DOHME
发明人： PYE PHILIP , ANGELAUD REMY , MANCHENO DANNY
IPC分类号： C07D239/557 , A61K31/513 , A61P31/18 , C07D413/12
摘要： Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.

4. 发明专利

HK1115011A1 POTASSIUM SALT OF AN HIV INTEGRASE INHIBITOR HIV 未知
公开(公告)号：HK1115011A1
公开(公告)日：2008-11-14
申请号：HK08104747
申请日：2008-04-29
申请人： MERCK SHARP & DOHME , ANGELETTI P IST RICHERCHE BIO , MERCK SHARP & DOHME
发明人： BELYK KEVIN M , MORRISON HENRY G , JONES PHILIP , SUMMA VINCENZO , COOPER V BRETT , MAHAJAN AMAR J , KUMKE DANIEL J , TUNG HSIEN-HSIN , WAI LAWRENCE , PRUZINSKY VANESSA , PYE PHILIP , ANGELAUD REMY , MANCHENO DANNY
IPC分类号： A61K20060101 , A61P20060101 , C07D20060101
摘要： Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.

5. 发明专利

ES2370136T3 SAL DE POTASIO DE UN INHIBIDOR DE LA INTEGRASA DEL VIH. 未知
公开(公告)号：ES2370136T3
公开(公告)日：2011-12-13
申请号：ES05852866
申请日：2005-12-02
申请人： MERCK SHARP & DOHME , ANGELETTI P IST RICHERCHE BIO
发明人： PYE PHILIP , ANGELAUD REMY , MANCHENO DANNY
IPC分类号： C07D239/557 , A61K31/513 , A61P31/18 , C07D413/12
摘要： Un procedimiento para preparar un compuesto de fórmula Q: que comprende hacer reaccionar un haluro de alquilo de fórmula R 1 X con un compuesto de fórmula S: en un disolvente aprótico polar y en presencia de una base seleccionada de una base de magnesio y una base de calcio; en los que R 1 es alquilo C1-6; R 2 es O-alquilo C1-6 o N(R A )R B en la que R A y R B son cada uno independientemente H o alquilo C1-6; R 3 es H o alquilo C1-6; L es alquileno C1-6; W es un grupo protector de amina; y X es halógeno.

6. 发明申请

WO2006060730A3 POTASSIUM SALT OF AN HIV INTEGRASE INHIBITOR 审中-公开
标题翻译：一种HIV整合酶抑制剂的钾盐
公开(公告)号：WO2006060730A3
公开(公告)日：2006-08-17
申请号：PCT/US2005043781
申请日：2005-12-02
申请人： MERCK & CO INC , ELETTI S P A ISTITUTO DI RICER , MERCK SHARP & DOHME , BELYK KEVIN M , MORRISON HENRY G , JONES PHILIP , SUMMA VINCENZO , COOPER V BRETT , MAHAJAN AMAR J , KUMKE DANIEL J , TUNG HSIEN-HSIN , WAI LAWRENCE , PRUZINSKY VANESSA , PYE PHILIP , ANGELAUD REMY , MANCHENO DANNY
发明人： BELYK KEVIN M , MORRISON HENRY G , JONES PHILIP , SUMMA VINCENZO , COOPER V BRETT , MAHAJAN AMAR J , KUMKE DANIEL J , TUNG HSIEN-HSIN , WAI LAWRENCE , PRUZINSKY VANESSA , PYE PHILIP , ANGELAUD REMY , MANCHENO DANNY
IPC分类号： C07D239/557 , A61K31/513 , A61P31/18 , C07D413/12
CPC分类号： C07D239/557 , C07D313/12 , C07D413/12
摘要： Potassium salts of Coompound A and methods for their preparation are disclosed, wherein Compound A is of formula: (Compound A). Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.
摘要翻译：公开了化合物A的钾盐及其制备方法，其中化合物A具有下式：（化合物A）。化合物A是一种HIV整合酶抑制剂，用于治疗或预防HIV感染，延缓AIDS的发作以及治疗或预防AIDS。

7. 发明申请

WO2010011584A3 PROCESS FOR MAKING A RENIN INHIBITOR AND RELATED INTERMEDIATES 审中-公开
标题翻译：制备瑞宁抑制剂及相关中间体的方法
公开(公告)号：WO2010011584A3
公开(公告)日：2010-07-29
申请号：PCT/US2009051101
申请日：2009-07-20
申请人： MERCK SHARP & DOHME , 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。

8. 发明专利

AU2005222391B2 HIV integrase inhibitors 未知
公开(公告)号：AU2005222391B2
公开(公告)日：2010-11-11
申请号：AU2005222391
申请日：2005-03-09
申请人： MERCK SHARP & DOHME
发明人： RUZEK ROWENA D , PERLOW DEBRA S , KIM BOYOUNG , HOERRNER R SCOTT , MANCHENO DANNY E , PYE PHILIP J , MORRISSETTE MATTHEW M , PAYNE LINDA S , FOSTER BRUCE S , NEILSON LOU ANNE , EGBERTSON MELISSA , OBLIGADO VANESSA E , ANGELAUD REMY , ZHUANG LINGHANG , WILLIAMS PETER D , WAI JOHN S , ISAACS RICHARD C A , DOLLING ULF H , ASKIN DAVID , CAMERON MARK , HAN WEI
IPC分类号： C07D471/04 , A61K31/4375
摘要： Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, R 1?, R 2?, R 3?, R 4? and R 5? are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, 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 antivirals, immunomodulators, antibiotics or vaccines.

9. 发明申请

WO2007136672A3 SYNTHESIS OF A BIARYL SYNTHETIC INTERMEDIATE 审中-公开
标题翻译：二联合中间体的合成
公开(公告)号：WO2007136672A3
公开(公告)日：2008-04-03
申请号：PCT/US2007011777
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
IPC分类号： C07C41/30 , C07C43/225 , C07D263/12
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。联苯氯是制备作为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联以形成联苯结构。

10. 发明申请

WO2004087650A2 PROCESS AND INTERMEDIATES FOR THE PREPARATION OF BETA-AMINO ACID AMIDE DIPEPTIDYL PEPTIDASE-IV INHIBITORS 审中-公开
标题翻译：制备β-氨基酸酰胺二磷酸酯酶IV抑制剂的方法和中间体
公开(公告)号：WO2004087650A2
公开(公告)日：2004-10-14
申请号：PCT/US2004008826
申请日：2004-03-23
申请人： MERCK & CO INC , ANGELAUD REMY , ARMSTRONG JOSEPH D III , ASKIN DAVID , BALSELLS JAUME , HANSEN KARL , LEE JAEMOON , MALIGRES PETER E , RIVERA NELO R , XIAO YI , ZHONG YONG-LI
发明人： ANGELAUD REMY , ARMSTRONG JOSEPH D III , ASKIN DAVID , BALSELLS JAUME , HANSEN KARL , LEE JAEMOON , MALIGRES PETER E , RIVERA NELO R , XIAO YI , ZHONG YONG-LI
IPC分类号： C07C229/00 , C07C239/20 , C07D20060101 , C07D205/00 , C07D497/00 , C07D
CPC分类号： C07C239/20 , C07D205/08 , C07D487/04
摘要： A novel process is provided for the preparation of chiral beta-amino acid amide inhibitors of the dipeptidyl peptidase-IV and the useful intermediates obtained therein. The products resulting from the instant process are inhibitors of dipeptidyl peptidase-IV and thereby useful for the treatment of Type 2 diabetes.
摘要翻译：提供了用于制备二肽基肽酶-IV的手性β-氨基酸酰胺抑制剂及其中获得的有用的中间体的新方法。本发明产生的产物是二肽基肽酶-IV的抑制剂，因此可用于治疗2型糖尿病。

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