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1. 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。

2. 发明申请

WO1997039763A1 COMPOSITIONS COMPRISING ANTIFUNGAL AGENT AND ACETATE BUFFER 审中-公开
标题翻译：包含抗真菌剂和乙酸盐缓冲液的组合物
公开(公告)号：WO1997039763A1
公开(公告)日：1997-10-30
申请号：PCT/US1997006284
申请日：1997-04-15
申请人： MERCK & CO., INC. , NERURKAR, Maneesh, J. , HUNKE, William, A. , KAUFMAN, Michael, J.
发明人： MERCK & CO., INC.
IPC分类号： A61K38/12
CPC分类号： A61K38/12
摘要： The invention is a pharmaceutical composition for intravenous administration to a patient comprising a) a pharmaceutically effective amount of a compound having the formula (I) and the pharmaceutically acceptable salts thereof; b) a pharmaceutically acceptable amount of an excipient such as a bulking agent effective to form a lyophilized cake; and c) a pharmaceutically acceptable amount of acetate buffer effective to provide a pH of between about 4 and 7.
摘要翻译：本发明是用于静脉内施用于患者的药物组合物，其包含：a）药学有效量的具有式（I）的化合物及其药学上可接受的盐; b）药学上可接受量的赋形剂，例如有效形成冻干饼的填充剂; 和c）药学上可接受量的乙酸盐缓冲液，其有效提供约4至7的pH。

3. 发明申请

WO1997015191A1 WET GRANULATION FORMULATION OF A GROWTH HORMONE SECRETAGOGUE 审中-公开
标题翻译：生长激素密度的湿润造粒
公开(公告)号：WO1997015191A1
公开(公告)日：1997-05-01
申请号：PCT/US1996017196
申请日：1996-10-23
申请人： MERCK & CO., INC. , ASGHARNEJAD, Mandana , DRAPER, Jerome, P. , DUBOST, David, C. , KAUFMAN, Michael, J. , STOREY, David, E.
发明人： MERCK & CO., INC.
IPC分类号： A01N43/38
CPC分类号： A61K31/438 , A61K9/2004 , A61K9/2077
摘要： The present invention relates to a pharmaceutical composition and a process for the preparation of a tablet containing a growth hormone secretagogue as the active ingredient. The tablet is prepared by forming a powder blend of the active ingredient N-[1(R)-[(1,2-dihydro-1-methanesulfonyl-spiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyl-oxy)ethyl]-2-amino-2-methyl-propanamide, or a pharmaceutically acceptable salt thereof, in particular the methanesulfonate salt, with a binder/diluent, a first diluent, a second diluent, a first portion of a disintegrant, and a lubricant; wet granulating the powder blend with a solution of ethanol/water to form granules; drying the granules to remove the ethanol/water; adding a second portion of a disintegrant; lubricating the granules; and compressing the dried granules into the desired tablet form. The present invention further relates to a novel amorphous form of the compound N-[1(R)-[(1,2-dihydro-1-methanesulfonyl-spiro[3H-indole-3,4'-piperdin]-1'-yl)carbonyl]-2-(phenylmethyl-oxy)ethyl]-2-amino-2-methylpropanamide methanesulfonate which is produced directly as a result of the process of tablet formulation.
摘要翻译：本发明涉及药物组合物和制备含有生长激素促分泌素作为活性成分的片剂的方法。通过形成活性成分N- [1（R） - [（1,2-二氢-1-甲磺酰 - 螺[3H-吲哚-3,4'-哌啶] -1'- 吡啶-2-基）羰基] -2-（苯甲基 - 氧基）乙基] -2-氨基-2-甲基 - 丙酰胺或其药学上可接受的盐，特别是甲磺酸盐，与粘合剂/稀释剂，第一稀释剂，第二稀释剂，崩解剂的第一部分和润滑剂; 用乙醇/水的溶液湿粉碎混合物以形成颗粒; 干燥颗粒以除去乙醇/水; 加入第二部分的崩解剂; 润滑颗粒; 并将干燥的颗粒压缩成所需的片剂形式。本发明还涉及新型无定形形式的化合物N- [1（R） - [（1,2-二氢-1-甲磺酰 - 螺[3H-吲哚-3,4'-哌啶] -1'- 吡啶-2-基）羰基] -2-（苯基甲基 - 氧基）乙基] -2-氨基-2-甲基丙酰胺甲磺酸盐，其是由于片剂制剂的过程而直接制备的。

4. 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。

5. 发明申请

WO1998018800A1 STABILIZED CARBAPENEM ANTIBIOTIC COMPOSITIONS AND METHOD OF MAKING 审中-公开
标题翻译：稳定的碳水化合物抗生素组合物和制备方法
公开(公告)号：WO1998018800A1
公开(公告)日：1998-05-07
申请号：PCT/US1997019336
申请日：1997-10-24
申请人： MERCK & CO., INC. , ALMARSSON, Orn , KAUFMAN, Michael, J. , STONG, John, D. , WILLIAMS, John, M.
发明人： MERCK & CO., INC.
IPC分类号： C07D487/04
CPC分类号： C07D477/20 , C07D477/02
摘要： A method is presented for stabilizing carbapenem antibiotics by carboxylating the pyrrolidinyl amino with a carbon dioxide source. The resulting compounds and pharmaceutical compositions thereof can be used in the treatment of infectious diseases, including those resulting from gram positive and negative, aerobic and anaerobic bacteria. The compounds have favorable pharmaceutical properties and stability against beta -lactamases, and a favorable duration of action.
摘要翻译：提出了一种通过用二氧化碳源羧化吡咯烷基氨基来稳定碳青霉烯类抗生素的方法。所得化合物及其药物组合物可用于治疗感染性疾病，包括由革兰氏阳性和阴性，需氧和厌氧细菌产生的传染病。该化合物对β-内酰胺酶具有有利的药物性质和稳定性，并且具有有利的作用持续时间。

6. 发明申请

WO1997021687A1 PROCESS FOR MAKING DIHYDROPYRIMIDINONES 审中-公开
标题翻译：制备二氢嘧啶酮的方法
公开(公告)号：WO1997021687A1
公开(公告)日：1997-06-19
申请号：PCT/US1996019651
申请日：1996-12-12
申请人： MERCK & CO., INC. , HU, Essa, H. , SIDLER, Daniel, R. , DOLLING, Ulf, H. , PATANE, Michael, A.
发明人： MERCK & CO., INC.
IPC分类号： C07D239/36
CPC分类号： C07D239/22
摘要： The present invention provides a process for forming 5-(alkyl or alkoxy)carbonyl-6-alkyl-4-(aryl or alkyl)-3,4-2(1H)-dihydropyrimidinones by combining a beta -keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu2O) and a catalyst (e.g., acid). The reaction is typically run in one pot in a solvent to afford dihydropyrimidinones in higher yields and with easier work up than previously known methods.
摘要翻译：本发明提供了通过将β-酮酯或二酮组合形成5-（烷基或烷氧基）羰基-6-烷基-4-（芳基或烷基）-3,4-2（1H） - 二氢嘧啶酮的方法，醛和尿素在硼试剂，金属盐（例如Cu 2 O）和催化剂（例如酸）的存在下进行。该反应通常在一锅中在溶剂中进行，以更高的产率提供二氢嘧啶酮，并且比以前已知的方法更容易处理。

7. 发明申请

WO1995018107A1 PROCESS FOR THE PREPARATION OF LEUKOTRIENE ANTAGONISTS 审中-公开
标题翻译：制备白藜芦醇拮抗剂的方法
公开(公告)号：WO1995018107A1
公开(公告)日：1995-07-06
申请号：PCT/US1994014858
申请日：1994-12-22
申请人： MERCK & CO., INC. , BHUPATHY, Mahadevan , McNAMARA, James, M. , SIDLER, Daniel, R. , VOLANTE, Ralph, P. , BERGAN, James, J.
发明人： MERCK & CO., INC.
IPC分类号： C07D215/12
CPC分类号： C07D215/14 , C07C323/53 , C07C2601/02
摘要： The present invention relates to a process for the preparation of a compound of formula (I) or a sodium salt thereof, wherein HET is 7-chloroquinolin-2-yl or 6,7-difluoroquinolin-2-yl, which comprises: reacting the dilithium dianion of 1-(mercapto-methyl)cyclopropaneacetic acid with a compound of formula (II), wherein HET is as defined above and L is arylsulfonyl or alkylsulfonyl. The invention further provides the dicyclohexylamine salt of a compound of formula (I), an intermediate falling within (II) and a 1-(Mercaptomethyl)cyclopropaneacetic acid intermediate.
摘要翻译：本发明涉及制备式（I）化合物或其钠盐的方法，其中HET是7-氯喹啉-2-基或6,7-二氟喹啉-2-基，其包括：使 1-（巯基 - 甲基）环丙烷乙酸的二锂二阴离子与式（II）化合物，其中HET如上所定义，L是芳基磺酰基或烷基磺酰基。本发明还提供式（I）化合物的二环己胺盐，（II）中的中间体和1-（巯基甲基）环丙烷乙酸中间体。

8. 发明申请

WO1998002439A1 PROCESS FOR SYNTHESIZING CARBAPENEM ANTIBIOTICS 审中-公开
标题翻译：合成抗胆碱药物的方法
公开(公告)号：WO1998002439A1
公开(公告)日：1998-01-22
申请号：PCT/US1997011844
申请日：1997-07-08
申请人： MERCK & CO., INC. , WILLIAMS, John, M. , JOBSON, Ronald, B.
发明人： MERCK & CO., INC.
IPC分类号： C07D477/08
CPC分类号： C07D477/20 , C07D477/02 , Y02P20/55
摘要： A process for synthesizing a coumpond of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein each P independently represents H or a protecting group, and R and R independently represent H, C1-10 alkyl, aryl or heteroaryl, or substituted C1-10 alkyl, aryl or heteroaryl, comprising: reacting the compounds (II) or a pharmaceutically acceptable salt or ester thereof, and (III) or a pharmaceutically acceptable salt or ester thereof, wherein X represents OP(O)(OR)2, or OSO2R, wherein R represents C1-6 alkyl, aryl or perfluoro C1-6 alkyl, in the presence of an amine selected from the group consisting of: diisopropylamine (DIPA), dicyclohexylamine (DCHA), 2,2,6,6-tetramethylpiperidine (TMP), 1,1,3,3-tetramethylguanidine (TMG), 1,8-diazabicyclo[4.3.0]undec-7-ene (DBU) and 1,5-diazabicyclo[4.3.0]non-5-ene to produce a compound of formula (I).
摘要翻译：一种合成式（I）化合物或其药学上可接受的盐或酯的方法，其中每个P独立地表示H或保护基，R 1和R 2独立地表示H，C 1-10烷基，芳基或杂芳基，或取代的C 1-10烷基，芳基或杂芳基，其包括：使化合物（II）或其药学上可接受的盐或酯与（III）或其药学上可接受的盐或酯反应，其中X表示OP O）（OR）2或OSO 2 R，其中R表示C 1-6烷基，芳基或全氟C 1-6烷基，在选自二异丙胺（DIPA），二环己胺（DCHA），2 ，2,6,6-四甲基哌啶（TMP），1,1,3,3-四甲基胍（TMG），1,8-二氮杂双环[4.3.0]十一碳-7-烯（DBU）和1,5-二氮杂双环[ 4.3.0]壬-5-烯，得到式（I）化合物。

9. 发明申请

WO1998029441A1 HUMAN GALANIN RECEPTOR GALR2 AND NUCLEOTIDES ENCODING SAME 审中-公开
标题翻译：人类GALANIN受体GALR2和编码其的核苷酸
公开(公告)号：WO1998029441A1
公开(公告)日：1998-07-09
申请号：PCT/US1997023892
申请日：1997-12-18
申请人： MERCK & CO., INC. , UNIVERSITY OF TEXAS HEALTH SCIENCE CENTER AT SAN ANTONIO , UNIVERSITY OF TORONTO , SULLIVAN, Kathleen , KOLAKOWSKI, Lee, F., Jr. , O'DOWD, Brian
发明人： MERCK & CO., INC. , UNIVERSITY OF TEXAS HEALTH SCIENCE CENTER AT SAN ANTONIO , UNIVERSITY OF TORONTO
IPC分类号： C07K14/00
CPC分类号： C07K14/72 , G01N2333/72
摘要： A new galanin receptor, GALR2, is described. Also provided are nucleic acids encoding same and various assays to identify ligands particular to said receptor. Ligands so identified are useful for the treatment of obesity, treatment of pain, and treatment of cognitive disorders.
摘要翻译：描述了一种新的甘丙肽受体GALR2。还提供了编码相同的核酸和用于鉴定所述受体特异性的配体的各种测定法。如此鉴定的配体可用于治疗肥胖症，治疗疼痛和治疗认知障碍。

10. 发明申请

WO1998028000A1 STABILIZERS FOR LYOPHILIZED VACCINES 审中-公开
标题翻译： LYOPHILIZED VACCINES的稳定剂
公开(公告)号：WO1998028000A1
公开(公告)日：1998-07-02
申请号：PCT/US1997023668
申请日：1997-12-18
申请人： MERCK & CO., INC. , VOLKIN, David, B. , BURKE, Carl, J. , SHEU, Su-Pi
发明人： MERCK & CO., INC.
IPC分类号： A61K39/00
CPC分类号： A61K39/25 , A61K9/19 , A61K39/0015 , A61K39/12 , A61K39/13 , A61K39/165 , A61K39/20 , A61K47/26 , A61K47/42 , A61K2039/5254 , A61K2039/70 , C12N2710/16734 , C12N2760/18434 , C12N2760/18734 , C12N2770/36234 , Y02A50/466
摘要： Vaccine stabilizers, vaccine formulations and lyophilized vaccines with enhanced thermostability are disclosed. The vaccine formulations comprise an increased amount of a 6-carbon polyhydric alcohol (such as sorbitol), an increased amount of a disaccharide (such as sucrose) and an amount of a physiologically active buffer to adjust the pH from about 6.0 to about 7.0.
摘要翻译：公开了具有增强的热稳定性的疫苗稳定剂，疫苗制剂和冻干疫苗。疫苗制剂包含增加量的6-碳多元醇（例如山梨醇），增加量的二糖（例如蔗糖）和用于将pH调节至约6.0至约7.0的生理活性缓冲液的量。

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