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1.发明授权POLYMORPHIC, AMORPHOUS AND HYDRATED FORMS OF 5-CHLORO-3-(4-METHANESULFONYLPHENYL)-6'-METHYL- 2,3']BIPYRIDINYL 有权多晶型物，无定形和5-氯-3-（甲磺酰基 - 苯基）-6'-甲基 - 2,3“]联吡啶水合形式
公开(公告)号：EP1248618B1
公开(公告)日：2006-03-22
申请号：EP00980817.1
申请日：2000-11-27
发明人： CLAS, Sophie, Dorothee , O'SHEA, Paul , DALTON, Chad , CROCKER, Louis, S. , MCCAULEY, James, A. , TILLYER, Richard, D. , DAVIES, Ian
IPC分类号： A61K31/44 , C07D213/22 , A61K31/444
CPC分类号： A61K31/444 , C07D213/61
摘要： Polymorphic, amorphous and hydrated forms of the title compound having the following structure: are disclosed. The compound is a potent and selective cyclooxygenase -2 (COX-2) inhibitor.
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2.发明公开POLYMORPHIC, AMORPHOUS AND HYDRATED FORMS OF 5-CHLORO-3-(4-METHANESULFONYLPHENYL)-6'-METHYL- 2,3']BIPYRIDINYL 有权多晶型物，无定形和5-氯-3-（甲磺酰基 - 苯基）-6'-甲基 - 2,3“]联吡啶水合形式
公开(公告)号：EP1248618A1
公开(公告)日：2002-10-16
申请号：EP00980817.1
申请日：2000-11-27
发明人： CLAS, Sophie, Dorothee , O'SHEA, Paul , DALTON, Chad , CROCKER, Louis, S. , MCCAULEY, James, A. , TILLYER, Richard, D. , DAVIES, Ian
IPC分类号： A61K31/44 , C07D213/22
CPC分类号： A61K31/444 , C07D213/61
摘要： Polymorphic, amorphous and hydrated forms of the title compound having the following structure: are disclosed. The compound is a potent and selective cyclooxygenase -2 (COX-2) inhibitor.
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公开(公告)号：EP1442038A2
公开(公告)日：2004-08-04
申请号：EP02768879.5
申请日：2002-09-20
申请人： Merck & Co., Inc.
发明人： BRANDS, Karel, M., J. , CVETOVICH, Raymond , CROCKER, Louis, S. , WARD, Michael, D. , MAHAJAN, Amar, J. , WENSLOW, Robert, M. , WILLIAMS, John, M. , SIDLER, Daniel, R. , FISHER, Elizabeth, S. , JOBSON, Ronald , ORELLA, Charles
IPC分类号： C07D477/20
CPC分类号： C07D477/20
摘要： A process for preparing a crystalline, carbapenem monosodium salt of formula IIa, characterized by the steps a) adding about 10 to 30 % of an organic solvent to an aqueous solution of the carbapenem, b) cooling the resulting solution to less than -5 °C, c) adjusting the pH using a solution containing an acid in an organic solvent to give the appropriate pH for crystallization, and d) crystallizing the compound by adding methanol, and a C2-5 alcohol at between -5 and -25 °C.
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4.发明公开5-CHLORO-3-(4-METHANESULFONYLPHENYL)-6'-METHYL- [2,3']BIPYRIDINYL IN PURE CRYSTALLINE FORM AND PROCESS FOR SYNTHESIS 有权5-氯-3-（4-甲磺酰基苯基）的结晶形式-6'-甲基 - [2,3“]联吡啶及其方法
公开(公告)号：EP1296951A1
公开(公告)日：2003-04-02
申请号：EP01939267.9
申请日：2001-05-22
申请人： Merck & Co., Inc.
IPC分类号： C07D213/61 , A61K31/444 , A61P29/00
CPC分类号： C07D213/61
摘要： This invention encompasses the Form V polymorph of Compound A of structural formula (A) which is useful in the treatment of cyclooxygenase-2 mediated diseases. The invention encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising the Form V polymorph of Compound A. The invention also encompasses a process for synthesizing the Form V polymorph of Compound A.
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5.发明公开
公开(公告)号：EP1292582A1
公开(公告)日：2003-03-19
申请号：EP01944262.3
申请日：2001-06-04
申请人： Merck & Co., Inc.
发明人： CROCKER, Louis, S. , BRANDS, Karel, M., Jos , NELSON, Todd, D. , PYE, Philip, J. , ROSEN, Jonathan, D. , ROSSEN, Kai
IPC分类号： C07D265/32 , C07D263/06
CPC分类号： C07D263/04 , C07D265/32
摘要： The present invention is concerned with 4-benzyl-2-hydroxy-1,4-oxazin-3-one, and novel processes for the preparation therof. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
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6.发明公开PROCESS FOR THE CRYSTALLIZATION OF A REVERSE TRANSCRIPTASE INHIBITOR USING AN ANTI-SOLVENT 失效PROCESS FOR A逆转录酶抑制剂的结晶，其中抗溶剂USED
公开(公告)号：EP0975609A1
公开(公告)日：2000-02-02
申请号：EP98904853.3
申请日：1998-02-02
申请人： MERCK & CO., INC.
IPC分类号： C07D265/18
CPC分类号： C07D265/18
摘要： The instant invention describes a method for crystallizing (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one from a solvent and anti-solvent solvent system and producing the crystalline product. The desired final crystal form, Form I, can be produced when using methanol or ethanol. Form II is isolated from 2-propanol and can be converted to the desired crystal form at low drying temperatures, such as between about a temperature of 40 °C and 50 °C.
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7.发明公开5-CHLORO-3-(4-METHANESULFONYLPHENYL)-6'-METHYL- 2,3']BIPYRIDINYL IN PURE CRYSTALLINE FORM AND PROCESS FOR SYNTHESIS 审中-公开5-氯-3-（4-甲磺酰苯基）-6 - METHYLç2,3-联吡啶纯的晶形与综合过程！
公开(公告)号：EP1395562A1
公开(公告)日：2004-03-10
申请号：EP01973314.6
申请日：2001-09-21
申请人： Merck & Co., Inc.
IPC分类号： C07D213/62 , A61K31/44
CPC分类号： C07D213/61
摘要： This invention encompasses a pharmaceutical composition comprising the compound of formula A: A in combination with a pharmaceutically acceptable carrier, said compound being comprised of about 1-50%, 1-20% or 1-10% of the polymorphic form which is designated Form V and the remainder of the compound being comprised of at least one polymorphic form selected from the group consisting of: Form I, Form II, Form III and Form IV
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