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公开(公告)号：US07728135B2
公开(公告)日：2010-06-01
申请号：US11326154
申请日：2006-01-05
Applicant: Xiongwei Shi , Man Zhu , William Leong , Vilas Dahanukar , Ilia A. Zavialov , Cecelia Proietti , Shannon Zhao , Hong-Chang Lee , Yi Liu , Hoa N. Nguyen , Wenxue Wu , Bosco D'Sa , Feng Liang , Loc Thanh Tran
Inventor： Xiongwei Shi , Man Zhu , William Leong , Vilas Dahanukar , Ilia A. Zavialov , Cecelia Proietti , Shannon Zhao , Hong-Chang Lee , Yi Liu , Hoa N. Nguyen , Wenxue Wu , Bosco D'Sa , Feng Liang , Loc Thanh Tran
IPC: C07D401/14 , C07D403/12 , A61K31/506 , A61K31/18
CPC classification number: C07D211/96 , C07D211/26 , C07D401/14
Abstract: The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.
Abstract translation: 本发明涉及4- [4 - [（R） - [1- [环丙基磺酰基] -4-哌啶基]（3-氟苯基）甲基] -3（S） - 甲基-1-哌嗪基] 1 - [（4,6-二甲基-5-嘧啶基）羰基] -4-甲基哌啶]，以及通过新途径从容易获得的起始原料中间产物。
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公开(公告)号：US20100036125A1
公开(公告)日：2010-02-11
申请号：US12580855
申请日：2009-10-16
Applicant: Xiongwei Shi , Man Zhu , William Leong , Vilas Dahanukar , Ilia A. Zavialov , Cecilia Proietti , Shannon Zhao , Hong-Chang Lee , Yi Liu , Hoa N. Nguyen , Wenxue Wu , Bosco D'Sa , Feng Liang , Loc Thanh Tran
Inventor： Xiongwei Shi , Man Zhu , William Leong , Vilas Dahanukar , Ilia A. Zavialov , Cecilia Proietti , Shannon Zhao , Hong-Chang Lee , Yi Liu , Hoa N. Nguyen , Wenxue Wu , Bosco D'Sa , Feng Liang , Loc Thanh Tran
IPC: C07D401/06 , C07D211/30
CPC classification number: C07D211/96 , C07D211/26 , C07D401/14
Abstract: The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.
Abstract translation: 本发明涉及4- [4 - [（R） - [1- [环丙基磺酰基] -4-哌啶基]（3-氟苯基）甲基] -3（S） - 甲基-1-哌嗪基] 1 - [（4,6-二甲基-5-嘧啶基）羰基] -4-甲基哌啶]，以及通过新途径从容易获得的起始原料中间产物。
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公开(公告)号：US07521452B2
公开(公告)日：2009-04-21
申请号：US11326155
申请日：2006-01-05
Applicant: Wenxue Wu , Loc Thanh Tran , Bosco D'Sa , Feng Liang , William Leong , Hong-Chang Lee , Kevin Klopfer , Vijay Sabesen
Inventor： Wenxue Wu , Loc Thanh Tran , Bosco D'Sa , Feng Liang , William Leong , Hong-Chang Lee , Kevin Klopfer , Vijay Sabesen
IPC: A61K31/497 , C07D239/02
CPC classification number: C07D401/14
Abstract: The present invention is generally directed to a process to directly prepare pharmaceutically acceptable salts enriched with respect to selected rotameric salts of a basic compound, by creative choice of an acid and a solvent medium. The process is particularly useful in preparing specific rotamers of pharmaceutically useful salts in desired preponderance of a rotamer.
Abstract translation: 本发明一般涉及通过创造性地选择酸和溶剂介质来直接制备相对于选择的碱性化合物的旋转异构酸盐富集的药学上可接受的盐的方法。 该方法在制备旋转异构体所需优势的药学上有用的盐的特定旋转异构体时特别有用。
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Patent Agency Ranking
公开(公告)号：US06936718B2
公开(公告)日：2005-08-30
申请号：US10305100
申请日：2002-11-26
Applicant: Minzhang Chen , Bosco D'sa , William Leong , Suhan Tang
Inventor： Minzhang Chen , Bosco D'sa , William Leong , Suhan Tang
IPC: A61K31/444 , A61K31/4545 , A61P11/06 , A61P19/02 , A61P19/06 , A61P29/00 , A61P31/18 , A61P37/08 , A61P43/00 , C07D401/14 , C07D211/54 , C07D211/30
CPC classification number: C07D401/14 , A61K31/444
Abstract: In one embodiment, the present invention discloses a process to directly prepare an unequal ratio of specific, preferred rotamer or rotameric pair of an acid salt from a basic compound, by creative choice of a solvent medium. The process is particularly useful in preparing desired rotamers of pharmaceutically useful salts.
Abstract translation: 在一个实施方案中，本发明公开了一种通过创造性地选择溶剂介质来直接制备特定的，优选的旋转异构体或旋转异构体的一对酸性盐与碱性化合物的比例不等的方法。 该方法特别可用于制备药学上可用的盐的所需旋转异构体。
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公开(公告)号：US20090093496A1
公开(公告)日：2009-04-09
申请号：US12331948
申请日：2008-12-10
Applicant: Wenxue Wu , Loc Thanh Tran , Bosco D'Sa , Feng Liang , William Leong , Hong-Chang Lee , Kevin Klopfer , Vijay Sabesan
Inventor： Wenxue Wu , Loc Thanh Tran , Bosco D'Sa , Feng Liang , William Leong , Hong-Chang Lee , Kevin Klopfer , Vijay Sabesan
IPC: A61K31/506 , C07D401/14
CPC classification number: C07D401/14
Abstract: The present invention is generally directed to a process to directly prepare pharmaceutically acceptable salts enriched with respect to selected rotameric salts of a basic compound, by creative choice of an acid and a solvent medium. The process is particularly useful in preparing specific rotamers of pharmaceutically useful salts in desired preponderance of a rotamer.
Abstract translation: 本发明一般涉及通过创造性地选择酸和溶剂介质来直接制备相对于选择的碱性化合物的旋转异构酸盐富集的药学上可接受的盐的方法。 该方法在制备旋转异构体所需优势的药学上有用的盐的特定旋转异构体时特别有用。
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公开(公告)号：US20060258863A1
公开(公告)日：2006-11-16
申请号：US11326154
申请日：2006-01-05
Applicant: Xiongwei Shi , Man Zhu , William Leong , Vilas Dahanukar , Ilia Zavialov , Cecilia Proletei , Shannon Zhao , Hong-Chang Lee , Yi Liu , Hoa Nguyen , Wenxue Wu , Bosco D'Sa , Feng Liang , Loc Tran
Inventor： Xiongwei Shi , Man Zhu , William Leong , Vilas Dahanukar , Ilia Zavialov , Cecilia Proletei , Shannon Zhao , Hong-Chang Lee , Yi Liu , Hoa Nguyen , Wenxue Wu , Bosco D'Sa , Feng Liang , Loc Tran
IPC: C07D403/14
CPC classification number: C07D211/96 , C07D211/26 , C07D401/14
Abstract: The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.
Abstract translation: 本发明涉及4- [4 - [（R） - [1- [环丙基磺酰基] -4-哌啶基]（3-氟苯基）甲基] -3（S） - 甲基-1-哌嗪基] 1 - [（4,6-二甲基-5-嘧啶基）羰基] -4-甲基哌啶]，以及通过新途径从容易获得的起始原料中间产物。
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公开(公告)号：US20060241295A1
公开(公告)日：2006-10-26
申请号：US11326155
申请日：2006-01-05
Applicant: Wenxue Wu , Loc Tran , Bosco D'Sa , Feng Liang , William Leong , Hong-Chang Lee , Kevin Klopfer , Vijay Sabesen
Inventor： Wenxue Wu , Loc Tran , Bosco D'Sa , Feng Liang , William Leong , Hong-Chang Lee , Kevin Klopfer , Vijay Sabesen
IPC: C07D403/14
CPC classification number: C07D401/14
Abstract: The present invention is generally directed to a process to directly prepare pharmaceutically acceptable salts enriched with respect to selected rotameric salts of a basic compound, by creative choice of an acid and a solvent medium. The process is particularly useful in preparing specific rotamers of pharmaceutically useful salts in desired preponderance of a rotamer.
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8.发明申请公开(公告)号：US20050187248A1
公开(公告)日：2005-08-25
申请号：US11088585
申请日：2005-03-24
Applicant: 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
Inventor： 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: 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 classification number: C07D401/06 , C07D401/14
Abstract: In its several embodiments, this invention discloses novel processes to prepare the compounds of formula II and formula IV:
Abstract translation: 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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