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1. 发明公开

EP1838695A2 PREPARATION OF KETONE AMIDES 审中-公开
标题翻译：酮酮的制备
公开(公告)号：EP1838695A2
公开(公告)日：2007-10-03
申请号：EP06717452.4
申请日：2006-01-05
申请人： Schering Corporation
发明人： KUO, Shen-Chun , TSAI, David, Jieh-Shyh , LIAO, Hongbiao
IPC分类号： C07D401/06
CPC分类号： C07D211/74 , C07D401/06 , C07D401/14
摘要： The present invention discloses a novel process to prepare ketone amides, which are useful intermediates for the preparation of antagonists of CCR5 receptor and therefore useful for the treatment of HIV virus infected mammals. It specifically discloses a novel process to synthesize 1 -(2,4-dimethylpyrimidine-5-carbonyl)-4-piperidone, 1 -[(2,4-dimethyl-3- pyridinyl)carbonyl]-4-piperidone and related compounds. A salient feature of the invention is the use of a three-phase reaction medium with an organic phase and a buffer salt slurry. (formule I)
摘要翻译：本发明公开了一种制备酮酰胺的新方法，它是用于制备CCR5受体拮抗剂并因此可用于治疗HIV病毒感染的哺乳动物的有用中间体。它具体公开了合成1-（2,4-二甲基嘧啶-5-羰基）-4-哌啶酮，1 - [（2,4-二甲基-3-吡啶基）羰基] -4-哌啶酮和相关化合物的新方法。本发明的显着特征是使用具有有机相和缓冲盐浆液的三相反应介质。（Formule I）

2. 发明授权

EP0734369B1 PROCESS FOR PREPARING INTERMEDIATES FOR THE SYNTHESIS OF ANTIFUNGAL AGENTS 失效
标题翻译：于制备中间体，用于合成抗真菌剂
公开(公告)号：EP0734369B1
公开(公告)日：1998-11-18
申请号：EP95905849.6
申请日：1994-12-09
申请人： SCHERING CORPORATION
发明人： KUO, Shen-Chun , HOU, Donald , ZHAN, Zheng-Yun
IPC分类号： C07C25/24 , C07C17/14 , C07C17/35
CPC分类号： C07C29/64 , C07C17/14 , C07C17/35 , C07C25/24 , C07C29/40 , C07C33/46
摘要： Disclosed is a process for preparing allylic halides of the formula (I), wherein X is Cl, Br or I, for use as intermediates in the synthesis of substituted tetrahydrofuran azole anti-fungal agents.

3. 发明授权

EP0690850B1 2-SUBSTITUTED MORPHOLINE AND THIOMORPHOLINE DERIVATIVES AS GABA-B ANTAGONISTS 失效
标题翻译： 2-取代的吗啉和硫代吗啉AS GABA-B拮抗剂
公开(公告)号：EP0690850B1
公开(公告)日：1997-11-12
申请号：EP94911608.1
申请日：1994-03-23
申请人： SCHERING CORPORATION
发明人： KUO, Shen-Chun , BLYTHIN, David, J. , KREUTNER, William
IPC分类号： C07D265/30 , C07D279/12 , C07D265/34 , C07F9/6533 , A61K31/535 , A61K31/54
CPC分类号： C07D265/30 , C07D265/34 , C07D279/12 , C07F9/6533 , C07F9/65335
摘要： Disclosed are compounds of Formula (I) wherein: Y represents -CO2H, -CO2R6, -C(O)NHR7, -SO2H, -SO3H, -SO3R6, -SO2NHR7, -C(O)-N(OH)-R8, or a group of formula (a), (b), (c), (d) or (e); or a pharmaceutically acceptable addition salt or solvate thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I). Further disclosed is a method for treating or preventing respiratory depression, epileptic seizures or other central nervous system disorders, and for enhancing cognitive performance, by administering an effective amount of a compound of Formula (I).

4. 发明公开

EP0734369A1 PROCESS FOR PREPARING INTERMEDIATES FOR THE SYNTHESIS OF ANTIFUNGAL AGENTS 失效
标题翻译：于制备中间体，用于合成抗真菌剂
公开(公告)号：EP0734369A1
公开(公告)日：1996-10-02
申请号：EP95905849.0
申请日：1994-12-09
申请人： SCHERING CORPORATION
发明人： KUO, Shen-Chun , HOU, Donald , ZHAN, Zheng-Yun
IPC分类号： B01J31 , C07C17 , C07C25 , C07C29 , C07C33
CPC分类号： C07C29/64 , C07C17/14 , C07C17/35 , C07C25/24 , C07C29/40 , C07C33/46
摘要： Disclosed is a process for preparing allylic halides of the formula (I), wherein X is Cl, Br or I, for use as intermediates in the synthesis of substituted tetrahydrofuran azole anti-fungal agents.

5. 发明公开

EP0690850A1 2-SUBSTITUTED MORPHOLINE AND THIOMORPHOLINE DERIVATIVES AS GABA- B? ANTAGONISTS 失效
标题翻译： 2-取代的吗啉和硫代吗啉AS GABA-B拮抗剂
公开(公告)号：EP0690850A1
公开(公告)日：1996-01-10
申请号：EP94911608.0
申请日：1994-03-23
申请人： SCHERING CORPORATION
发明人： KUO, Shen-Chun , BLYTHIN, David, J. , KREUTNER, William
IPC分类号： A61K31 , A61P11 , A61P25 , A61P43 , C07C229 , C07D265 , C07D279 , C07D413 , C07D417 , C07F9
CPC分类号： C07D265/30 , C07D265/34 , C07D279/12 , C07F9/6533 , C07F9/65335
摘要： Disclosed are compounds of Formula (I) wherein: Y represents -CO2H, -CO2R6, -C(O)NHR7, -SO2H, -SO3H, -SO3R6, -SO2NHR7, -C(O)-N(OH)-R8, or a group of formula (a), (b), (c), (d) or (e); or a pharmaceutically acceptable addition salt or solvate thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I). Further disclosed is a method for treating or preventing respiratory depression, epileptic seizures or other central nervous system disorders, and for enhancing cognitive performance, by administering an effective amount of a compound of Formula (I).

6. 发明公开

EP2125733A1 PROCESS FOR PREPARING CCR-5 RECEPTOR ANTAGONISTS UTILIZING 4-SUBSTITUTED 1-CYCLOPROPANE-SULFONYL-PIPERIDINYL COMPOUNDS 审中-公开
标题翻译：用于生产CCR-5受体拮抗剂使用4-取代的1- CYCLOPROPANSULFONYLPIPERIDINYLVERBINDUNGEN
公开(公告)号：EP2125733A1
公开(公告)日：2009-12-02
申请号：EP07863166.0
申请日：2007-12-20
申请人： Schering Corporation
发明人： TRAVERSE, John F. , KUO, Shen-Chun , LIANG, Feng , LEONG, William W.
IPC分类号： C07D211/98 , C07D401/14
CPC分类号： C07D401/14 , C07D211/96 , C07D401/10 , C07D403/10
摘要： The present invention discloses a novel process to prepare 4-substituted 1-Cyclopropane-sulfonyl-Piperidinyl compounds, which are useful intermediates for the preparation of antagonists of CCR5 receptor and therefore useful for the treatment of HIV virus infected mammals. It specifically discloses a novel process to synthesize 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine] compounds.

7. 发明公开

EP1131313A1 ENANTIOSELECTIVE ALKYLATION OF TRICYCLIC COMPOUNDS 有权
标题翻译：三环连接的对映选择性烷基化
公开(公告)号：EP1131313A1
公开(公告)日：2001-09-12
申请号：EP99958771.0
申请日：1999-11-18
申请人： SCHERING CORPORATION
发明人： KUO, Shen-Chun , BERNARD, Charles, F. , CHEN, Frank, Xing , HOU, Donald , KIM-MEADE, Agnes, S. , WU, George, G.
IPC分类号： C07D401/04 , C07B53/00
CPC分类号： C07D401/04 , C07D401/14 , Y02P20/55
摘要： Disclosed is a process for preparing a compound of formula (I) wherein X?1, X2, X3, X4 and X5¿ are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having formula (II) wherein X?1, X2, X3, X4 and X5¿ are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having formula (V) wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase.

8. 发明公开

EP2057166A2 PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF (3-ALKYL-5-PIPERIDIN-1-YL-3,3A-DIHYDRO- PYRAZOLOÝ1,5-A¨PYRIMIDIN-7-YL)-AMINO DERIVATIVES AND INTERMEDIATES 有权转让
标题翻译： VERFAHREN UND ZWISCHENPRODUKTE ZUR HERSTELLUNG VON（3-ALKYL-5-PIPERIDIN-1-YL-3,3A-二氢吡唑并[1,5-A]吡啶基-7-YL） - 氨基衍生物
公开(公告)号：EP2057166A2
公开(公告)日：2009-05-13
申请号：EP07837015.2
申请日：2007-08-17
申请人： Schering Corporation
发明人： CHEN, Frank Xing , KEERTIKAR, Kartik M. , KUO, Shen-Chun , LEE, Hong-Chang , RAGHAVAN, Ramani R. , WU, George G. , XIE, Ji
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Disclosed is a process for the synthesis of compounds of Formula I by sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1, wherein R1 is a linear, branched, or cyclic alkyloxy functional group of the structure (—R2a—OH), R2a is a linear, branched or cyclic alkyl group, R2 is a linear, branched or cyclic alkyl group, and R3 is an alkylene-heterocycle, said process comprising forming intermediate compound of Formula E1 by reacting, in a refluxing reaction solvent selected from alcohols having 5 or less carbon atoms and mixtures of two or more thereof, a methanol solution of a salt of a 4-alkyl-3-amino-pyrazole compound of Formula C1, with a diamidization reagent selected from dimethylmalonate, monomethylmalonyl-chloride, and malonyl dichloride in the presence of a Lewis base having sufficient proton affinity to abstract a proton from the 1-position nitrogen on the pyrazole ring.
摘要翻译：公开了一种合成式I化合物的方法，首先用伯胺，然后与仲胺，式E1结构的中间体化合物，其中R 1是直链，支链或环状烷氧基官能团（-R2a-OH）基团，R2a是直链，支链或环状的烷基，R2是直链，支链或环状的烷基，R3是亚烷基 - 杂环，所述方法包括形成式E1的中间体化合物通过使选自具有5个或更少碳原子的醇的回流反应溶剂及其两种或更多种的混合物，将式C1的4-烷基-3-氨基 - 吡唑化合物的盐与二酰胺化反应选自二甲基丙二酸二甲酯，单甲基丙二酸酰氯和丙二酰氯的试剂在具有足够质子亲和力的路易斯碱存在下从吡唑环上的1-位氮抽出质子。

9. 发明授权

EP1689749B1 PROCESS FOR PREPARING SUBSTITUTED 5-AMINO-PYRAZOLO-[4,3-E]-1,2,4-TRIAZOLO[1,5-C]PYRIMIDINES 有权
标题翻译： PROCESS FOR取代的5-氨基吡唑并[4,3-E] -1,2,4-三唑并[1,5-C]嘧啶的制备
公开(公告)号：EP1689749B1
公开(公告)日：2007-11-07
申请号：EP04812380.6
申请日：2004-11-29
申请人： Schering Corporation
发明人： KUO, Shen-Chun , TRAN, Loc, Thanh , ZHANG, Pengyi
IPC分类号： C07D487/00
CPC分类号： C07D487/14
摘要： A process for preparing substituted 5-amino-pyrazolo[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidine compounds having an aminoalkyl substituent at the 7-position is disclosed.

10. 发明授权

EP1678182B1 PROCESS FOR PREPARING SUBSTITUTED 5-AMINO-PYRAZOLO- [4,3-E]-1,2,4-TRIAZOLO [1,5-C]PYRIMIDINES 失效转让
标题翻译：用于生产取代的5-氨基吡唑并[4,3-E] -1,2,4-三唑并[1,5-C]嘧啶类
公开(公告)号：EP1678182B1
公开(公告)日：2007-02-07
申请号：EP04796445.7
申请日：2004-10-26
申请人： SCHERING CORPORATION
发明人： KUO, Shen-Chun , TSAI, David, Jieh-Shyh , TRAN, Loc, Thanh , ZHANG, Pengyi , JONES, Andrew, D.
IPC分类号： C07D487/14
CPC分类号： C07D487/14
摘要： A process for preparing substituted 5-amino-pyrazolo[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidine compounds having an aminoalkyl substituent at the 7-position is disclosed, wherein the pyrimidine ring is cyclized using a cyanating agent.

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