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1. 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。

2. 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。

3. 发明申请

WO2019118311A1 PHARMACEUTICAL COMPOSITIONS OF TEDIZOLID PHOSPHATE 审中-公开
公开(公告)号：WO2019118311A1
公开(公告)日：2019-06-20
申请号：PCT/US2018/064646
申请日：2018-12-10
申请人： MERCK SHARP & DOHME CORP. , CAI, Lixia , DUBOST, David , HARRIS, David , LI, Yongjun , MAHJOUR, Majid , ZHANG, Dan
发明人： CAI, Lixia , DUBOST, David , HARRIS, David , LI, Yongjun , MAHJOUR, Majid , ZHANG, Dan
IPC分类号： A61K31/4439 , A61K47/12 , A61K47/36 , A61P31/04
摘要： Disclosed are pharmaceutical compositions comprising tedizolid phosphate, methods of preparing such pharmaceutical compositions, and methods of treating bacterial infections with such pharmaceutical compositions. Specifically, a pharmaceutical composition comprising tedizolid phosphate, an acid; and a suspending agent; and wherein the pH of the composition upon constitution with water is between about pH 2 - 4.5, is provided, wherein the acid is not citric acid or malic acid.

4. 发明申请

WO2010042392A3 HIV INTEGRASE INHIBITORS 审中-公开
标题翻译： HIV整合酶抑制剂
公开(公告)号：WO2010042392A3
公开(公告)日：2010-06-03
申请号：PCT/US2009059308
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 , A61K31/55 , A61P31/18 , C07D281/10 , C07D487/04
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 X1, X2, Y, R1A, R1B, R2 and R3 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X 1，X 2，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。化合物及其盐可以用作药物组合物中的成分，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。还描述了制备式I化合物及其中间体的方法。

5. 发明申请

WO2010042391A3 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：WO2010042391A3
公开(公告)日：2010-06-03
申请号：PCT/US2009059306
申请日：2009-10-02
申请人： MERCK SHARP & DOHME , 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： A61K31/33 , A61P31/18 , C07D487/04 , C07D498/04
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 X1, X2, Y, R1A, R1B, R2 and R3 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。

6. 发明申请

WO2008013807A2 A NOVEL LACTIC ACID FORMULATION OF MK-0457 USEFUL FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的MK-0457的新型酸性配方
公开(公告)号：WO2008013807A2
公开(公告)日：2008-01-31
申请号：PCT/US2007016637
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 , A61K9/00 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/14 , A61K9/16 , A61K31/506
CPC分类号： A61K9/0019 , A61K9/10 , A61K9/107 , A61K9/1075 , A61K9/485 , A61K9/4858 , A61K31/506 , A61K47/12
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.
摘要翻译：公开了一种乳酸制剂及其制备方法：MK-0457。这样的制剂可用于治疗癌症。

7. 发明申请

WO1997015574A1 POLYMORPHIC FORMS OF A GROWTH HORMONE SECRETAGOGUE 审中-公开
标题翻译：生长激素密码子的多形态
公开(公告)号：WO1997015574A1
公开(公告)日：1997-05-01
申请号：PCT/US1996016955
申请日：1996-10-23
申请人： MERCK & CO., INC. , DRAPER, Jerome, P. , DUBOST, David, C. , KAUFMAN, Michael, J. , MCCAULEY, James, A. , VANDRILLA, Jennifer, L. , VARSOLONA, Richard, J.
发明人： MERCK & CO., INC.
IPC分类号： C07D471/10
CPC分类号： C07D471/10 , A61K38/00 , C07K5/06034
摘要： This invention is concerned with polymorphic forms of the compound N-[1(R)-[(1,2-dihydro-1-methanesulfonylspiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyloxy)ethyl]-2-amino-2-methylpropanamide methanesulfonate which is a growth hormone secretagogue that is useful in food animals to promote their growth thereby rendering the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, and to treat medical conditions which are improved by the anabolic effects of growth hormone. The instant polymorphic forms have advantages over the other known forms of N-[1(R)-[(1,2-dihydro-1-methanesulfonylspiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyloxy)-ethyl]-2-amino-2-methylpropanamide methanesulfonate in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations. The present invention is also concerned with processes for preparing these polymorphic forms, pharmaceutical formulations comprising these polymorphic forms as active ingredients and the use of the polymorphic form of the compound and their formulations in the treatment of certain disorders.
摘要翻译：本发明涉及化合物N- [1（R） - [（1,2-二氢-1-甲磺酰基螺[3H-吲哚-3,4'-哌啶] -1'-基）羰基] - 2-（苯基甲氧基）乙基] -2-氨基-2-甲基丙酰胺甲磺酸盐，其是生物激素促分泌素，其可用于食用动物以促进其生长，从而使食用肉制品的生产更有效，并且在人类中，或以生长激素分泌不足为特征的医疗状况，以及治疗由生长激素的合成代谢作用改善的医疗状况。本发明的多晶型物质具有优于其他已知形式的N- [1（R） - [（1,2-二氢-1-甲磺酰基螺[3H-吲哚-3,4'-哌啶] -1'-基）羰基 ] -2-（苯基甲氧基） - 乙基] -2-氨基-2-甲基丙酰胺甲磺酸盐的热力学稳定性和药物制剂中的适用性。本发明还涉及制备这些多晶型物的方法，包含这些多晶型形式作为活性成分的药物制剂以及化合物的多晶形式及其制剂在治疗某些疾病中的用途。

8. 发明申请

WO2009117278A3 PROCESSES FOR PREPARING (AMINO-PYRAZOLOPYRIDINYL)METHOXY SUBSTITUTED BIARYL ETHERS 审中-公开
标题翻译：（氨基吡唑并吡啶基）甲氧基取代的双烯基醚的制备方法
公开(公告)号：WO2009117278A3
公开(公告)日：2009-11-12
申请号：PCT/US2009036616
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。该方法包括使联芳基醚与适当保护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，以磺酸盐或硫酸盐形式得到所需的取代联芳基醚。还描述了较早的反应步骤和其中使用和获得的中间体。也描述了特定的（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。

9. 发明申请

WO2008013807A3 A NOVEL LACTIC ACID FORMULATION OF MK-0457 USEFUL FOR THE TREATMENT OF CANCER 审中-公开
标题翻译： MK-0457的新型乳酸配方用于治疗癌症
公开(公告)号：WO2008013807A3
公开(公告)日：2008-04-03
申请号：PCT/US2007016637
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 , A61K9/00 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/14 , A61K9/16 , A61K31/506 , A61P35/00 , A61P35/02
CPC分类号： A61K9/0019 , A61K9/10 , A61K9/107 , A61K9/1075 , A61K9/485 , A61K9/4858 , A61K31/506 , A61K47/12
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.
摘要翻译：公开了一种乳酸制剂和一种制备MK-0457制剂的方法。这种制剂可用于治疗癌症。

10. 发明申请

WO1997045430A1 CARBAPENEM ANTIBIOTIC, COMPOSITION AND METHOD OF PREPARATION 审中-公开
标题翻译：卡巴因抗生素，组合物和制备方法
公开(公告)号：WO1997045430A1
公开(公告)日：1997-12-04
申请号：PCT/US1997008831
申请日：1997-05-23
申请人： MERCK & CO., INC. , ZIMMERMAN, Jeffrey, A. , WILLIAMS, John, M. , BERGQUIST, Paul, A. , DiMICHELE, Lisa, M. , DuBOST, David, C. , KAUFMAN, Michael, J. , SIDLER, Daniel, R. , HUNKE, William, A.
发明人： MERCK & CO., INC.
IPC分类号： C07D477/20
CPC分类号： C07D477/20 , A61K31/407
摘要： A pharmaceutical composition is disclosed which contains a compound of formula (I) or a pharmaceutically acceptable salt, prodrug or hydrate thereof, in the stabilized form and/or in combination with a carbon dioxide source.
摘要翻译：公开了一种药物组合物，其含有稳定形式的和/或与二氧化碳源组合的式（I）化合物或其药学上可接受的盐，前药或水合物。

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