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1.Preparation of salts of 4-[4-[(1R)-[4-(trifluoromethyl)phenyl]-2-methoxyethyl]-(3S)-methyl-1-piperazinyl]-4-methyl-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl] 失效
标题翻译: 制备4- [4 - [(1R) - [4-(三氟甲基)苯基] -2-甲氧基乙基] - (3S) - 甲基-1-哌嗪基] -4-甲基-1 - [(4,6 - 二甲基-5-嘧啶基)羰基]公开(公告)号:US06943251B2
公开(公告)日:2005-09-13
申请号:US10304674
申请日:2002-11-26
申请人: Dinesh Gala , Andrew J. Goodman , Gary Lee , Hongbiao Liao , Martin L. Schwartz , Suhan Tang , David Js Tsai , Wenxue Wu
发明人: Dinesh Gala , Andrew J. Goodman , Gary Lee , Hongbiao Liao , Martin L. Schwartz , Suhan Tang , David Js Tsai , Wenxue Wu
IPC分类号: C07D401/14 , A61K31/095 , A61K31/19 , A61K31/194 , A61K31/506 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D401/06
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.
摘要翻译: 在一个实施方案中,本发明公开了通过创造性地选择溶剂介质来直接制备酸性盐与碱性化合物的不等比例的旋转异构体的方法。 该方法特别可用于制备具有期望优势的药学上有用的盐的特定旋转异构体。
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公开(公告)号:US07534884B2
公开(公告)日:2009-05-19
申请号:US11093560
申请日:2005-03-30
申请人: Dinesh Gala , Andrew J. Goodman , Gary Lee , Hongbiao Liao , Martin L. Schwartz , Suhan Tang , David J. S. Tsai , Wenxue Wu
发明人: Dinesh Gala , Andrew J. Goodman , Gary Lee , Hongbiao Liao , Martin L. Schwartz , Suhan Tang , David J. S. Tsai , Wenxue Wu
IPC分类号: C07D401/14
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.
摘要翻译: 在一个实施方案中,本发明公开了通过创造性地选择溶剂介质来直接制备酸性盐与碱性化合物的不等比例的旋转异构体的方法。 该方法特别可用于制备具有期望优势的药学上有用的盐的特定旋转异构体。
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公开(公告)号:US20050171117A1
公开(公告)日:2005-08-04
申请号:US11093560
申请日:2005-03-30
申请人: Dinesh Gala , Andrew Goodman , Gary Lee , Hongbiao Liao , Martin Schwartz , Suhan Tang , David Tsai , Wenxue Wu
发明人: Dinesh Gala , Andrew Goodman , Gary Lee , Hongbiao Liao , Martin Schwartz , Suhan Tang , David Tsai , Wenxue Wu
IPC分类号: C07D401/14 , A61K31/095 , A61K31/19 , A61K31/194 , A61K31/506 , A61P1/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D401/06 , C07D43/14
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.
摘要翻译: 在一个实施方案中,本发明公开了通过创造性地选择溶剂介质来直接制备酸性盐与碱性化合物的不等比例的旋转异构体的方法。 该方法特别可用于制备具有期望优势的药学上有用的盐的特定旋转异构体。
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公开(公告)号:US20050171120A1
公开(公告)日:2005-08-04
申请号:US11089858
申请日:2005-03-25
申请人: Wenxue Wu , Hongbiao Liao , David Tsai , David Andrews , Dinesh Gala , Gary Lee , Martin Schwartz , Timothy McAllister , Xiaoyong Fu , Donal Maloney , Tiruvettipuram Thiruvengadam , Chou-Hang Tann
发明人: Wenxue Wu , Hongbiao Liao , David Tsai , David Andrews , Dinesh Gala , Gary Lee , Martin Schwartz , Timothy McAllister , Xiaoyong Fu , Donal Maloney , Tiruvettipuram Thiruvengadam , Chou-Hang Tann
IPC分类号: C07D241/04 , C07B53/00 , C07B61/00 , C07C45/51 , C07C303/28 , C07C309/73 , C07D295/084 , C07D295/088 , C07D295/185 , C07D295/192 , C07D295/205 , A61K31/495 , A61K31/496
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: In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process:
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5.Stereoselective alkylation of chiral 2-methyl-4-protected piperazines 失效
标题翻译: 手性2-甲基-4-保护的哌嗪的立体选择性烷基化公开(公告)号:US06872826B2
公开(公告)日:2005-03-29
申请号:US10400429
申请日:2003-03-27
申请人: Wenxue Wu , Hongbiao Liao , David J. S. Tsai , David R. Andrews , Dinesh Gala , Gary M. Lee , Martin Lawrence Schwartz , Timothy L. McAllister , Xiaoyong Fu , Donal Maloney , Tiruvettipuram K. Thiruvengadam , Chou-Hang Tann
发明人: Wenxue Wu , Hongbiao Liao , David J. S. Tsai , David R. Andrews , Dinesh Gala , Gary M. Lee , Martin Lawrence Schwartz , Timothy L. McAllister , Xiaoyong Fu , Donal Maloney , Tiruvettipuram K. Thiruvengadam , Chou-Hang Tann
IPC分类号: C07D241/04 , C07B53/00 , C07B61/00 , C07C45/51 , C07C303/28 , C07C309/73 , C07D295/084 , C07D295/088 , C07D295/185 , C07D295/192 , C07D295/205 , C07D295/067
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: In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process:
摘要翻译: 在说明性实施方案中,本发明通过新的立体选择性烷基化方法描述了具有高立体化学纯度的以下化合物和类似化合物的合成:
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6.Stereoselective alkylation of chiral 2-methyl-4-protected piperazines 失效
标题翻译: 手性2-甲基-4-保护的哌嗪的立体选择性烷基化公开(公告)号:US07745626B2
公开(公告)日:2010-06-29
申请号:US11089858
申请日:2005-03-25
申请人: Wenxue Wu , Hongbiao Liao , David J. Tsai , David R. Andrews , Dinesh Gala , Gary M. Lee , Martin Lawrence Schwartz , Timothy L. McAllister , Xiaoyong Fu , Donal Maloney , Tiruvettipuram K. Thiruvengadam , Chou-Hang Tann
发明人: Wenxue Wu , Hongbiao Liao , David J. Tsai , David R. Andrews , Dinesh Gala , Gary M. Lee , Martin Lawrence Schwartz , Timothy L. McAllister , Xiaoyong Fu , Donal Maloney , Tiruvettipuram K. Thiruvengadam , Chou-Hang Tann
IPC分类号: C07D295/023
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: In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process:
摘要翻译: 在说明性实施方案中,本发明通过新的立体选择性烷基化方法描述了具有高立体化学纯度的以下化合物和类似化合物的合成:
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7.Stereoselective Alkylation of Chiral 2-Methly-4 Protected Piperazines 审中-公开
标题翻译: 手性2-甲基-4保护的哌嗪的立体选择性烷基化公开(公告)号:US20100249411A1
公开(公告)日:2010-09-30
申请号:US12748882
申请日:2010-03-29
申请人: Wenxue Wu , Hongbiao Liao , David J.S. Tsai , David R. Andrews , Dinesh Gala , Gary M. Lee , Martin Lawrence Schwartz , Timothy L. McAllister , Xiaoyong Fu , Donal Maloney , Tiruvettipuram K. Thiruvengadam , Chou-Hang Tann
发明人: Wenxue Wu , Hongbiao Liao , David J.S. Tsai , David R. Andrews , Dinesh Gala , Gary M. Lee , Martin Lawrence Schwartz , Timothy L. McAllister , Xiaoyong Fu , Donal Maloney , Tiruvettipuram K. Thiruvengadam , Chou-Hang Tann
IPC分类号: C07D241/04 , C07C309/73 , C07C45/54
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: In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process:
摘要翻译: 在说明性实施方案中,本发明描述了通过新的立体选择性烷基化方法合成具有高立体化学纯度的以下化合物和类似化合物:
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8.
公开(公告)号:US06992189B2
公开(公告)日:2006-01-31
申请号:US10401070
申请日:2003-03-27
申请人: William Leong , Minzhang Chen , Bosco A. D'sa , Man Zhu , Tong Xiao , Xiongwei Shi , Suhan Tang , Dinesh Gala , Andrew J. Goodman , Christopher M. Nielsen , Gary M. Lee , Juan A. Gamboa , Andrew D. Jones
发明人: William Leong , Minzhang Chen , Bosco A. D'sa , Man Zhu , Tong Xiao , Xiongwei Shi , Suhan Tang , Dinesh Gala , Andrew J. Goodman , Christopher M. Nielsen , Gary M. Lee , Juan A. Gamboa , Andrew D. Jones
IPC分类号: C07D403/14
CPC分类号: C07D401/06 , C07D401/14
摘要: In its several embodiments, this invention discloses novel processes to prepare the compounds of formula II and formula IV:
摘要翻译: 在其几个实施方案中,本发明公开了制备式II和式IV化合物的新方法:
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9.Synthesis of piperidine and piperazine compounds as CCR5 antagonists 审中-公开
标题翻译: 哌啶和哌嗪化合物作为CCR5拮抗剂的合成公开(公告)号:US20050187248A1
公开(公告)日:2005-08-25
申请号:US11088585
申请日:2005-03-24
申请人: William Leong , Minzhang Chen , Bosco D'sa , Man Zhu , Tong Xiao , Xiongwei Shi , Suhan Tang , Dinesh Gala , Andrew Goodman , Christopher Nielsen , Gary Lee , Juan Gamboa , Andrew Jones
发明人: William Leong , Minzhang Chen , Bosco D'sa , Man Zhu , Tong Xiao , Xiongwei Shi , Suhan Tang , Dinesh Gala , Andrew Goodman , Christopher Nielsen , Gary Lee , Juan Gamboa , Andrew Jones
IPC分类号: A61K31/4545 , A61P11/06 , A61P17/02 , A61P17/06 , A61P19/02 , A61P29/00 , A61P31/18 , A61P37/08 , A61P43/00 , C07D401/06 , C07D401/14 , C07D41/14
CPC分类号: C07D401/06 , C07D401/14
摘要: In its several embodiments, this invention discloses novel processes to prepare the compounds of formula II and formula IV:
摘要翻译: 在其几个实施方案中,本发明公开了制备式II和式IV化合物的新方法:
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10.
公开(公告)号:US5545558A
公开(公告)日:1996-08-13
申请号:US211336
申请日:1994-03-29
申请人: Dinesh Gala
发明人: Dinesh Gala
CPC分类号: C12P41/004 , C12P7/26 , C12P7/62
摘要: A process for the preparation of a chiral .alpha.-hydroxylketone, or ester thereof, comprising hydrolyzing an ester of said .alpha.-hydroxyketone with an enzyme that has a specificity for one enantiomer, or by esterifying said .alpha.-hydroxyketone with an esterifying agent in the presence of an enzyme that favors one enantiomer.
摘要翻译: PCT No.PCT / US92 / 08168 Sec。 371日期:1994年3月29日 102(e)1994年3月29日PCT PCT于1992年10月1日提交一种制备手性α-羟基酮或其酯的方法,包括用所述α-羟基酮的酯水解具有特异性的酶 或通过在有利于一种对映异构体的酶存在下用酯化剂酯化所述α-羟基酮。
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