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1. 发明公开

EP1490352A1 SYNTHESIS OF PIPERIDINE AND PIPERAZINE COMPOUNDS AS CCR5 ANTAGONISTS 审中-公开
标题翻译：用于生产哌啶和哌嗪化合物作为CCR5拮抗剂
公开(公告)号：EP1490352A1
公开(公告)日：2004-12-29
申请号：EP03721466.5
申请日：2003-03-27
申请人： SCHERING CORPORATION
发明人： LEONG, William , CHEN, Minzhang , D'SA, Bosco A. , ZHU, Man , XIAO, Tong , SHI, Xiongwei , TANG, Suhan , GALA, Dinesh , GOODMAN, Andrew J. , NIELSEN, Christopher M. , LEE, Gary M. , GAMBOA, Juan A. , JONES, Andrew D.
IPC分类号： C07D401/14 , C07D401/06
CPC分类号： C07D401/06 , C07D401/14
摘要： This invention discloses novel processes to prepare the compounds of formula II and formula IV:

2. 发明公开

EP1490346A2 STEREOSELECTIVE ALKYLATION OF CHIRAL 2-METHYL-4-PROTECTED PIPERAZINES 有权
标题翻译：手性的STEREO选择性烷基化2-甲基-4-哌嗪PROTECTED
公开(公告)号：EP1490346A2
公开(公告)日：2004-12-29
申请号：EP03733842.3
申请日：2003-03-27
申请人： SCHERING CORPORATION
发明人： WU, Wenxue , LIAO, Hongbiao , TSAI, David, J. , ANDREWS, David, R. , GALA, Dinesh , LEE, Gary, M. , SCHWARTZ, Martin, Lawrence , MCALLISTER, Timothy, L. , FU, Xiaoyong , MALONEY, Donal , THIRUVENGADAM, T., K. , TANN, Chou-Hang
IPC分类号： C07D295/18 , C07D295/08 , C07B37/04
CPC分类号： C07D295/185 , C07B2200/07 , C07C45/512 , C07C67/343 , C07C309/73 , C07D295/088 , C07D295/092 , C07D295/192 , C07D295/205 , C07C49/255 , C07C69/734 , C07C49/84
摘要： The present invention describes the synthesis of the following compounds in high stereochemical purity by a novel stereoselective alkylation of 2-methyl-4-protected piperazines using an inorganic base. (I)

3. 发明授权

EP1490346B1 STEREOSELECTIVE ALKYLATION OF CHIRAL 2-METHYL-4-PROTECTED PIPERAZINES 有权
标题翻译：手性的STEREO选择性烷基化2-甲基-4-哌嗪PROTECTED
公开(公告)号：EP1490346B1
公开(公告)日：2009-12-02
申请号：EP03733842.3
申请日：2003-03-27
申请人： Schering Corporation
发明人： WU, Wenxue , LIAO, Hongbiao , TSAI, David, J. , ANDREWS, David, R. , GALA, Dinesh , LEE, Gary, M. , SCHWARTZ, Martin, Lawrence , MCALLISTER, Timothy, L. , FU, Xiaoyong , MALONEY, Donal , THIRUVENGADAM, T., K. , TANN, Chou-Hang
IPC分类号： C07D295/18 , C07D295/08 , C07B37/04
CPC分类号： C07D295/185 , C07B2200/07 , C07C45/512 , C07C67/343 , C07C309/73 , C07D295/088 , C07D295/092 , C07D295/192 , C07D295/205 , C07C49/255 , C07C69/734 , C07C49/84
摘要： The present invention describes the synthesis of the following compounds in high stereochemical purity by a novel stereoselective alkylation of 2-methyl-4-protected piperazines using an inorganic base. (I)

4. 发明公开

EP0362299A1 BICYCLIC COMPOUNDS, THEIR USE AS PHARMACEUTICALS, THEIR PREPARATION, AND INTERMEDIATES USEFUL IN THEIR PREPARATION 失效
标题翻译：双环化合物，它们的使用作为其生产药品，生产和中间体。
公开(公告)号：EP0362299A1
公开(公告)日：1990-04-11
申请号：EP88906692.0
申请日：1988-07-20
申请人： SCHERING CORPORATION
发明人： BLYTHIN, David, J. , SHUE, Ho-Jane , GALA, Dinesh , STEINMAN, Martin , GANGULY, Ashit
IPC分类号： C07D215 , A61K31 , A61P11 , A61P17 , A61P29 , A61P37 , A61P43 , C07D213 , C07D453 , C07D471 , C07D519
CPC分类号： C07D471/04 , C07D215/36 , C07D453/02
摘要： La présente invention décrit des composés bicycliques utiles comme agents anti-allergiques, anti-inflammatoires et/ou cytoprotecteurs et utiles dans le traitement des affections de la peau hyperprolifératives. Des compositions pharmaceutiques et des procédés de traitement utilisant de tels composés sont également décrits. Un grand nombre de ces composés sont nouveaux; des procédés originaux pour leur préparation et pour la préparation de composés intermédiaires sont également décrits.

5. 发明公开

EP1451174A2 PROCESS FOR THE PREPARATION OF COMPOSITIONS HAVING AN INCREASED AMOUNT OF PHARMACEUTICALLY ACTIVE SALTS OF ROTAMERS 有权
标题翻译：用于生产组合物含有活性药物成分的盐类旋转异构体含量提高
公开(公告)号：EP1451174A2
公开(公告)日：2004-09-01
申请号：EP02784638.5
申请日：2002-11-26
申请人： SCHERING CORPORATION
发明人： GALA, Dinesh , GOODMAN, Andrew, J. , LEE, Gary , LIAO, Hongbiao , SCHWARTZ, Martin, L. , TANG, Suhan , TSAI, David, J., S. , WU, Wenxue
IPC分类号： C07D401/06 , A61K31/506 , A61P37/08
CPC分类号： C07D401/06
摘要： In one embodiment, the present invention discloses a process to directly prepare an unequal ratio of rotamers of an acid salt from a basic compound, by creative choice of a solvent medium. The process is particularly useful in preparing specific rotamers of pharmaceutically useful salts in desired preponderance.

6. 发明公开

EP0923573A1 PREPARATION OF AMINOMETHYL-PHENYLIMIDAZOLES 失效
标题翻译：制造氨基甲基苯基咪唑
公开(公告)号：EP0923573A1
公开(公告)日：1999-06-23
申请号：EP97933820.0
申请日：1997-08-06
申请人： SCHERING CORPORATION
发明人： GALA, Dinesh , MERGELSBERG, Ingrid , STEINMAN, Martin , GIESINGER, Brigitte , SCHERER, Dominik
IPC分类号： C07D233 , A61K31 , A61P25 , A61P43 , C07D401 , C07D403
CPC分类号： C07D233/64 , C07D401/12 , C07D403/12
摘要： The present invention provides a process for the preparation of a compound of formula (II), which comprises condensing a compound of formula (III), wherein R is an acyl group of an alkanoic acid, an aromatic carboxylic acid, an aralkanoic acid, or an alkane- or aromatic-sulfonic acid; with a compound of the formula (IV): NHR5R6. A particularly preferred ester is the acetate ester. The aminomethyl-phenylimidazoles have useful properties as highly selective partial agonists or antagonists at brain dopamine receptor subtypes. A preferred compound prepared is 5-fluoro-2-[4-[(2-phenyl-1H-imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine. Esters of the hydroxymethyl-phenylimidazoles are useful intermediates.

7. 发明授权

EP1451174B1 PROCESS FOR THE PREPARATION OF COMPOSITIONS HAVING AN INCREASED AMOUNT OF PHARMACEUTICALLY ACTIVE SALTS OF ROTAMERS 有权
标题翻译：用于生产组合物含有活性药物成分的盐类旋转异构体含量提高
公开(公告)号：EP1451174B1
公开(公告)日：2010-08-18
申请号：EP02784638.5
申请日：2002-11-26
申请人： Schering Corporation
发明人： GALA, Dinesh , GOODMAN, Andrew, J. , LEE, Gary , LIAO, Hongbiao , SCHWARTZ, Martin, L. , TANG, Suhan , TSAI, David, J., S. , WU, Wenxue
IPC分类号： C07D401/06 , A61K31/506 , A61P37/08
CPC分类号： C07D401/06
摘要： In one embodiment, the present invention discloses a process to directly prepare an unequal ratio of rotamers of an acid salt from a basic compound, by creative choice of a solvent medium. The process is particularly useful in preparing specific rotamers of pharmaceutically useful salts in desired preponderance.

8. 发明公开

EP1021436A1 ETHYL 4-(8-CHLORO-5, 6-DIHYDRO-11H- BENZO 5,6]CYCLOHEPTA 1,2-b]PYRIDIN -11-YLIDENE)-1- PIPERIDENE CARBOXYLATE POLYMORPH 审中-公开
标题翻译：乙基-4-（8-氯-5,6-二氢-10H-苯并[5,6]嘧啶-2-基]吡啶-9-基] -1-哌啶氧基丙酸乙酯
公开(公告)号：EP1021436A1
公开(公告)日：2000-07-26
申请号：EP98950916.1
申请日：1998-10-08
申请人： SCHERING CORPORATION
发明人： GALA, Dinesh , DIBENEDETTO, Donald, J.
IPC分类号： C07D401/04 , A61K31/445
CPC分类号： C07D401/04
摘要： A polymorph form 2 of ethyl 4-(8-chloro-5, 6-dihydro-11H- benzo[5,6]cyclohepta [1,2-b]pyridin -11-ylidene)-1- piperidene carboxylate (hereinafter 'loratadine') represented by formula (I). Pharmaceutical composition containing the polymorph form 2, and methods of using the polymorph form 2 to treat allergic reactions in mammals such as man are disclosed.

9. 发明公开

EP0686157A1 2-BENZYL-POLYCYCLIC GUANINE DERIVATIVES AND PROCESS FOR PREPARING THEM 失效
标题翻译： 2 BENZYLPOLYCYCLISCH鸟嘌呤及其制备方法
公开(公告)号：EP0686157A1
公开(公告)日：1995-12-13
申请号：EP94910124.0
申请日：1994-02-24
申请人： SCHERING CORPORATION
发明人： TULSHIAN, Deen , McKITTRICK, Brian, A. , XIA, Yan , CHACKALAMANNIL, Samuel , GALA, Dinesh , DIBENEDETTO, Donald, J. , KUGELMAN, Max
IPC分类号： C07D239 , C07D473 , C07D487
CPC分类号： C07D487/14 , C07D239/54 , C07D473/40
摘要： Antihypertensive and bronchodilating compounds of formula (I) or a pharmaceutically acceptable salt thereof, and a process for preparing them are disclosed, wherein: R1, R2 and R3 are hydrogen, lower alkyl, lower alkoxy, halogeno, hydroxy, (di-lower alkyl)amino, 4-morpholinyl, 1-pyrrolidinyl, 1-pyrrolyl, -CF3, -OCF3, phenyl or methoxyphenyl; or R1 and R2 together are methylenedioxy; or R1 and R2 together with the carbon atoms to which they are attached form a benzene ring; and Ra is hydrogen and R?b and Rc¿, together with the carbon atoms to which they are attached, form a saturated ring of 5 carbons; or Ra is lower alkyl, Rb is hydrogen or lower alkyl, and Rc is hydrogen; or Ra, Rb and the carbon atom to which they are attached form a saturated ring of 5-7 carbons, and Rc is hydrogen; or Ra is hydrogen, and Rb, Rc and the carbon atoms to which they are attached form a tetrahydrofuran ring; or R?a and Rb¿, together with the carbon atom to which they are attached, and R?b and Rc¿, together with the carbon atoms to which they are attached, each form a saturated ring of 5-7 carbons; pharmaceutical compositions containing said compounds: methods of treatment using said compounds; and a process for preparing polycyclic guanines comprising a) reducing a nitrosopyrimidine, and treating the reduced nitrosopyrimidine with an acylating reagent to give the amidopyrimidine; b) reacting the amidopyrimidine with a halogenating/cyclizing reagent to give a halopurine; c) reacting, in the presence of a base, the halopurine with an amine to give the substituted aminopurine; and d) closing the ring of the substituted aminopurine with a suitable dehydrating agent.

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