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1. 发明申请

WO2008039420A3 NOVEL INHIBITORS OF BETA-LACTAMASE 审中-公开
公开(公告)号：WO2008039420A3
公开(公告)日：2008-04-03
申请号：PCT/US2007/020608
申请日：2007-09-24
申请人： MERCK & CO., INC. , BLIZZARD, Timothy, A. , CHEN, Helen, Y. , WU, Jane, Yang , KIM, Seongkon , HA, Sookhee , MORTKO, Christopher, J. , VARIANKAVAL, Narayan , CHIU, Anna
发明人： BLIZZARD, Timothy, A. , CHEN, Helen, Y. , WU, Jane, Yang , KIM, Seongkon , HA, Sookhee , MORTKO, Christopher, J. , VARIANKAVAL, Narayan , CHIU, Anna
IPC分类号： C07D487/04 , A61K31/407 , A61P31/04
摘要： A class of 7-oxo-2,6-diazabicyclo-[3.2.0]-heptane-6-sulfonic acid compounds substituted at the two position of the bicyclic ring with a heterocyclylaminocarbonyl group or a carbocyclylaminocarbonyl group are β-lactamase inhibitors. The compounds and their prodrugs and pharmaceutically acceptable salts are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds are suitable for use with β-lactam antibiotics (e.g., imipenem and ceftazidime) against micro-organisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.

2. 发明申请

WO2009014676A1 NOVEL CRYSTALLINE FORM OF A DIHYDROCHLORIDE SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR 审中-公开
标题翻译：一种DIPEPTIDYL PEPTIDASE-IV抑制剂二氢氯化物盐的新型结晶形式
公开(公告)号：WO2009014676A1
公开(公告)日：2009-01-29
申请号：PCT/US2008/008859
申请日：2008-07-21
申请人： MERCK & CO., INC. , ELLISON, Martha, E. , VARIANKAVAL, Narayan , WENSLOW, Robert, M.
发明人： ELLISON, Martha, E. , VARIANKAVAL, Narayan , WENSLOW, Robert, M.
IPC分类号： A01N43/56 , A61K31/415
CPC分类号： C07D487/04
摘要： The present invention relates to a novel crystalline form of the dihydrochloride salt of (2 R ,3 S ,5 S )-2-(2,5-difluorophenyl)-5-(4,6-dihydropyrrolo[3,4-c]pyrazol-5(1 H )-yl)tetrahydro-2 H -pyran-3-amine as well as a process for its preparation, pharmaceutical compositions containing this novel form, and methods of use of the novel form and pharmaceutical compositions for the treatment of Type 2 diabetes, hyperglycemia, insulin resistance, obesity, and high blood pressure.
摘要翻译：本发明涉及（2R，3S，5S）-2-（2,5-二氟苯基）-5-（4,6-二氢吡咯并[3,4-c]吡唑-5-基）二盐酸盐的新结晶形式（1H） - 基）四氢-2H-吡喃-3-胺及其制备方法，含有该新形式的药物组合物，以及用于治疗2型糖尿病的新形式和药物组合物的使用方法，高血糖症，胰岛素抵抗，肥胖和高血压。

3. 发明申请

WO2007081895A2 PREPARATION OF SUBSTITUTED 2-HYDROXYGIBBA-1(10A), 2, 4, 4B-TETRAEN-6-ONES 审中-公开
标题翻译：取代的2-羟基甘氨酸-1（10A），2,4,4B-四烯-6-酮的制备
公开(公告)号：WO2007081895A2
公开(公告)日：2007-07-19
申请号：PCT/US2007000431
申请日：2007-01-05
申请人： MERCK & CO INC , MERCK SHARP & DOHME , BREWER SARAH ELIZABETH , OLIVER STEVEN FRASER , SCOTT JEREMY PETER , STEWART GAVIN WILLIAM , VARIANKAVAL NARAYAN , WALLACE DEBRA JANE
发明人： BREWER SARAH ELIZABETH , OLIVER STEVEN FRASER , SCOTT JEREMY PETER , STEWART GAVIN WILLIAM , VARIANKAVAL NARAYAN , WALLACE DEBRA JANE
IPC分类号： C07C49/747
CPC分类号： C07C49/747 , C07C45/63 , C07C45/68 , C07C45/73 , C07C49/755 , C07C2603/86
摘要： The instant invention describes processes for synthesizing substituted 2-hydroxygibba-1(10a),2,4,4b-tetraen-6-ones.
摘要翻译：本发明描述了合成取代的2-羟基吉巴-1（10a），2,4,4b-四烯-6-酮的方法。

4. 发明申请

WO2013181174A2 SOLID DOSAGE FORMULATIONS OF AN OREXIN RECEPTOR ANTAGONIST 审中-公开
标题翻译： OREXIN受体拮抗剂的固体剂量配方
公开(公告)号：WO2013181174A2
公开(公告)日：2013-12-05
申请号：PCT/US2013/042959
申请日：2013-05-29
申请人： MERCK SHARP & DOHME CORP. , HARMON, Paul, A. , VARIANKAVAL, Narayan
发明人： HARMON, Paul, A. , VARIANKAVAL, Narayan
IPC分类号： A61K47/32 , A61K31/551
CPC分类号： A61K31/551 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K47/32 , A61K47/38
摘要： The present invention is directed to a pharmaceutical composition comprising the compound suvorexant, or a pharmaceutically acceptable salt thereof, a concentration-enhancing polymer, and optionally a pharmaceutically acceptable surfactant.
摘要翻译：本发明涉及一种药物组合物，其包含化合物促氧化剂或其药学上可接受的盐，浓度增强聚合物和任选的药学上可接受的表面活性剂。

5. 发明申请

WO2007081895A3 PREPARATION OF SUBSTITUTED 2-HYDROXYGIBBA-1(10A), 2, 4, 4B-TETRAEN-6-ONES 审中-公开
公开(公告)号：WO2007081895A3
公开(公告)日：2007-07-19
申请号：PCT/US2007/000431
申请日：2007-01-05
申请人： MERCK & CO., INC. , MERCK SHARP & DOHME LIMITED , BREWER, Sarah Elizabeth , OLIVER, Steven Fraser , SCOTT, Jeremy Peter , STEWART, Gavin William , VARIANKAVAL, Narayan , WALLACE, Debra Jane
发明人： BREWER, Sarah Elizabeth , OLIVER, Steven Fraser , SCOTT, Jeremy Peter , STEWART, Gavin William , VARIANKAVAL, Narayan , WALLACE, Debra Jane
IPC分类号： C07C49/747
摘要： The instant invention describes processes for synthesizing substituted 2-hydroxygibba-1(10a),2,4,4b-tetraen-6-ones.

6. 发明申请

WO2013181174A3 SOLID DOSAGE FORMULATIONS OF AN OREXIN RECEPTOR ANTAGONIST 审中-公开
标题翻译： OREXIN受体拮抗剂的固体剂量配方
公开(公告)号：WO2013181174A3
公开(公告)日：2014-01-30
申请号：PCT/US2013042959
申请日：2013-05-29
申请人： MERCK SHARP & DOHME , HARMON PAUL A , VARIANKAVAL NARAYAN
发明人： HARMON PAUL A , VARIANKAVAL NARAYAN
IPC分类号： A61K31/551
CPC分类号： A61K31/551 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K47/32 , A61K47/38
摘要： The present invention is directed to a pharmaceutical composition comprising the compound suvorexant, or a pharmaceutically acceptable salt thereof, a concentration-enhancing polymer, and optionally a pharmaceutically acceptable surfactant. The concentration-enhancing polymer is a polymer that forms an amorphous dispersion with suvorexant, that is insoluble or almost completely insoluble in water by (a) dissolving the suvorexant or (b) interacting with the suvorexant in such a way that the suvorexant does not form crystals or crystalline domains in the polymer. A concentration-enhancing polymer is water soluble or readily disperse in water, so that when the polymer is placed in water or an aqueous environment (e.g. fluids in the gastrointestinal (Gl) tract or simulated Gl fluids), the solubility and/or bioavailability of suvorexant is increased over the solubility or bioavailability in the absence of the polymer.
摘要翻译：本发明涉及一种药物组合物，其包含化合物促氧化剂或其药学上可接受的盐，浓度增强聚合物和任选的药学上可接受的表面活性剂。浓度增强聚合物是通过（a）将suvorexant溶解或（b）与suvorexant相互作用以使得suvorexant不形成的方式形成具有suvorexant的无定形分散体的聚合物，其不溶或几乎完全不溶于水聚合物中的晶体或结晶域。浓度增强聚合物是水溶性的或容易分散在水中，使得当聚合物置于水或水性环境（例如胃肠道（G1）道或模拟的Gl液中的流体）时，溶解度和/或生物利用度在不存在聚合物的情况下，苏维素增加超过溶解度或生物利用度。

7. 发明申请

WO2009054923A2 SYNTHESIS AND CRYSTALLINE FORMS OF CB-1 ANTAGONIST/INVERSE AGONIST 审中-公开
标题翻译： CB-1 ANTAGONIST / INVERSE AGONIST的合成和结晶形式
公开(公告)号：WO2009054923A2
公开(公告)日：2009-04-30
申请号：PCT/US2008011927
申请日：2008-10-20
申请人： MERCK & CO INC , CAMPOS KEVIN R , CHEN CHENG-YI , FOLEY JENNIFER R , HILLIER MICHAEL , JEN WENDY S , KASSIM AMUDE M , KLAPARS ARTIS , PERESYPKIN ANDREY V , ROSNER THORSTEN , SAVARIN CECILE G , TUDGE MATTHEW , VARIANKAVAL NARAYAN , VYDRA VICKY , ZHAO DALIAN
发明人： CAMPOS KEVIN R , CHEN CHENG-YI , FOLEY JENNIFER R , HILLIER MICHAEL , JEN WENDY S , KASSIM AMUDE M , KLAPARS ARTIS , PERESYPKIN ANDREY V , ROSNER THORSTEN , SAVARIN CECILE G , TUDGE MATTHEW , VARIANKAVAL NARAYAN , VYDRA VICKY , ZHAO DALIAN
IPC分类号： C07D413/10 , A61K31/4245 , A61P25/00 , C07D271/113
CPC分类号： C07D271/113 , C07C255/53 , C07D413/10
摘要： The present invention relates to a process for producing crystalline 3-[(1S)-1-(1-{(S)-(4-chlorophenyl)[3-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)phenyl]methyl} azetidin-3-yl)-2-fluoro-2-methylpropyl]-5-fluorobenzonitrile, and novel salts, solvates, hydrates and polymorphs thereof.
摘要翻译：本发明涉及3 - [（1S）-1-（1 - {（S） - （4-氯苯基）[3-（5-氧代-4,5-二氢-1,3， 4-二唑-2-基）苯基]甲基}氮杂环丁烷-3-基）-2-氟-2-甲基丙基] -5-氟苄腈及其新的盐，溶剂合物，水合物和多晶型物。

8. 发明申请

WO2008039420A2 NOVEL INHIBITORS OF BETA-LACTAMASE 审中-公开
标题翻译：新型β-内酰胺酶抑制剂
公开(公告)号：WO2008039420A2
公开(公告)日：2008-04-03
申请号：PCT/US2007020608
申请日：2007-09-24
申请人： MERCK & CO INC , BLIZZARD TIMOTHY A , CHEN HELEN Y , WU JANE YANG , KIM SEONGKON , HA SOOKHEE , MORTKO CHRISTOPHER J , VARIANKAVAL NARAYAN , CHIU ANNA
发明人： BLIZZARD TIMOTHY A , CHEN HELEN Y , WU JANE YANG , KIM SEONGKON , HA SOOKHEE , MORTKO CHRISTOPHER J , VARIANKAVAL NARAYAN , CHIU ANNA
IPC分类号： C07D487/04 , A61K31/407 , A61P31/04
CPC分类号： C07D487/04
摘要： A class of 7-oxo-2,6-diazabicyclo-[3.2.0]-heptane-6-sulfonic acid compounds substituted at the two position of the bicyclic ring with a heterocyclylaminocarbonyl group or a carbocyclylaminocarbonyl group are ß-lactamase inhibitors. The compounds and their prodrugs and pharmaceutically acceptable salts are useful in the treatment of bacterial infections in combination with ß-lactam antibiotics. In particular, the compounds are suitable for use with ß-lactam antibiotics (e.g., imipenem and ceftazidime) against micro-organisms resistant to ß-lactam antibiotics due to the presence of the ß-lactamases.
摘要翻译：一类在双环的两个位置被杂环基氨基羰基或碳环基氨基羰基取代的7-氧代-2,6-二氮杂双环 - [3.2.0] - 庚烷-6-磺酸化合物是β-内酰胺酶抑制剂。这些化合物及其前药和药学上可接受的盐可用于与β-内酰胺抗生素联合治疗细菌感染。特别地，由于β-内酰胺酶的存在，所述化合物适用于抗β-内酰胺抗生素耐药微生物的β-内酰胺抗生素（例如亚胺培南和头孢他啶）。

9. 发明申请

WO2009054923A3 SYNTHESIS AND CRYSTALLINE FORMS OF CB-1 ANTAGONIST/INVERSE AGONIST 审中-公开
公开(公告)号：WO2009054923A3
公开(公告)日：2009-04-30
申请号：PCT/US2008/011927
申请日：2008-10-20
申请人： MERCK & CO., INC. , CAMPOS, Kevin, R. , CHEN, Cheng-Yi , FOLEY, Jennifer, R. , HILLIER, Michael , JEN, Wendy, S. , KASSIM, Amude, M. , KLAPARS, Artis , PERESYPKIN, Andrey, V. , ROSNER, Thorsten , SAVARIN, Cecile, G. , TUDGE, Matthew , VARIANKAVAL, Narayan , VYDRA, Vicky , ZHAO, Dalian
发明人： CAMPOS, Kevin, R. , CHEN, Cheng-Yi , FOLEY, Jennifer, R. , HILLIER, Michael , JEN, Wendy, S. , KASSIM, Amude, M. , KLAPARS, Artis , PERESYPKIN, Andrey, V. , ROSNER, Thorsten , SAVARIN, Cecile, G. , TUDGE, Matthew , VARIANKAVAL, Narayan , VYDRA, Vicky , ZHAO, Dalian
IPC分类号： C07D413/10 , C07D271/113 , A61P25/00 , A61K31/4245
摘要： The present invention relates to a process for producing crystalline 3-[(1 S )-1-(1-{( S )-(4-chlorophenyl)[3-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)phenyl]methyl} azetidin-3-yl)-2-fluoro-2-methylpropyl]-5-fluorobenzonitrile, and novel salts, solvates, hydrates and polymorphs thereof.

10. 发明申请

WO2008123953A1 ANTI-HYPERCHOLESTEROLEMIC COMPOUND 审中-公开
标题翻译：抗高血压化合物
公开(公告)号：WO2008123953A1
公开(公告)日：2008-10-16
申请号：PCT/US2008/004140
申请日：2008-03-28
申请人： MERCK & CO., INC. , VARIANKAVAL, Narayan , VYDRA, Vicky, K. , WENSLOW, Robert, M.
发明人： VARIANKAVAL, Narayan , VYDRA, Vicky, K. , WENSLOW, Robert, M.
IPC分类号： A01N43/00 , A61K31/397
CPC分类号： C07D205/08
摘要： This invention provides a novel crystalline form of N-[3-(4-{(2S,3R)-2-{4-[3,4-dihydroxy-3-(hydroxymethyl)butyl]phenyl}-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-oxoazetidin-1-yl}phen yl)propyl]methanesulfonamide. The compound is useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating mixed hyperlipidemia.
摘要翻译：本发明提供N- [3-（4 - {（2S，3R）-2- {4- [3,4-二羟基-3-（羟甲基）丁基]苯基} -3 - [（3S ）-3-（4-氟苯基）-3-羟丙基] -4-氧代氮杂环丁烷-1-基}苯基）丙基]甲磺酰胺。该化合物可用于降低血浆胆固醇水平，特别是低密度脂蛋白胆固醇，以及治疗混合型高脂血症。

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