-
公开(公告)号:US20170334926A1
公开(公告)日:2017-11-23
申请号:US15524872
申请日:2015-11-05
申请人: Daniel A. DIROCCO , Ian DAVIES , Feng PENG , Mark MCLAUGHLIN , Louis-Charles CAMPEAU , Yingju XU , Merck Sharp & Dohme Corp.
发明人: Daniel A . DiRocco , Ian Davies , Feng Peng , Mark McLaughlin , Louis-Charles Campeau , Yingju Xu
IPC分类号: C07D498/04 , B01J31/18 , B01J35/00
CPC分类号: C07D498/04 , B01J31/00 , B01J31/181 , B01J35/004 , B01J2231/766 , B01J2531/827
摘要: The present invention is directed to a process for preparing Substituted Indole Compounds of Formula (I): wherein R1, R2, R3 and R4 are as defined herein. These indole compounds are useful as synthetic intermediates for making inhibitors of HCV NS5A.
-
公开(公告)号:US09862725B2
公开(公告)日:2018-01-09
申请号:US15325100
申请日:2015-07-16
发明人: John Y. L. Chung , Feng Peng , Yonggang Chen , Amude Mahmoud Kassim , Cheng-yi Chen , Mathew Maust , Mark McLaughlin , Michael J. Zacuto , Qinghao Chen , Lushi Tan , Zhiguo Jake Song , Yang Cao , Feng Xu
IPC分类号: C07D231/56 , C07D405/04 , C07C69/73 , C07F5/04 , C07D487/04 , A61K31/4162
CPC分类号: C07D487/04 , A61K31/4162 , C07D309/30
摘要: A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of, reductive amination of:
-
公开(公告)号:US20190022115A1
公开(公告)日:2019-01-24
申请号:US15761742
申请日:2016-09-16
发明人: Vinay M. Girijavallabhan , Mark McLaughlin , Edward Cleator , Jongrock Kong , Andrew William Gibson , David R. Lieberman , Alejandro Dieguez Vazquez , Stephen Philip Keen , Michael J. Williams , Jeffrey C. Moore , Erika M. Milczek , Feng Peng , Kevin M. Belyk , Zhiguo Jake Song
IPC分类号: A61K31/7064 , C07D307/33 , A61P31/18
摘要: The present invention is directed to 4′-substituted nucleoside derivatives of Formula (I) and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4′-substituted nucleoside derivatives of Formula (I) and derivatives thereof.
-
公开(公告)号:US20170158701A1
公开(公告)日:2017-06-08
申请号:US15325100
申请日:2015-07-16
发明人: John Y. L. Chung , Feng Peng , Yonggang Chen , Amude Mahmoud Kassim , Cheng-yi Chen , Mathew Maust , Mark McLaughlin , Michael J. Zacuto , Qinghao Chen , Lushi Tan , Zhiguo Jake Song , Yang Cao , Feng Xu
IPC分类号: C07D487/04 , A61K31/4162
CPC分类号: C07D487/04 , A61K31/4162 , C07D309/30
摘要: A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of, reductive amination of:
-
公开(公告)号:US11584724B2
公开(公告)日:2023-02-21
申请号:US17048833
申请日:2019-04-18
发明人: Kevin M. Maloney , Kallol Basu , Michael James Di Maso , Guy R. Humphrey , Alfred Y. Lee , Feng Peng , Hong Ren , Siwei Zhang
IPC分类号: C07D239/48 , C07C41/09 , C07C41/30 , C07C253/30 , C07D487/18
摘要: Disclosed herein is a novel process for preparing Compound A free base, 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-iso-propyl-2-methoxybenzenesulfonamide, and a citrate salt of Compound A with simplified chemistry and a high overall yield: Compound A. In one embodiment, the overall yield from the starting material 2-isopropylphenol to Compound A citrate salt is greater than 50%. In another embodiment, the overall yield is greater than 60%. Also disclosed herein are novel salts and solvates of Compound A.
-
公开(公告)号:US20210154221A1
公开(公告)日:2021-05-27
申请号:US17166512
申请日:2021-02-03
发明人: Mark McLaughlin , Edward Cleator , Jongrock Kong , Andrew William Gibson , David R. Lieberman , Alejandro Diequez Vazquez , Stephen Philip Keen , Michael J. Williams , Jeffrey C. Moore , Erika M. Milczek , Feng Peng , Kevin M. Belyk , Zhiguo Jake Song
IPC分类号: A61K31/7064 , C07D307/33 , A61K45/06 , C07H1/00 , C07H19/14 , C07H23/00 , C07H19/16 , A61P31/18
摘要: The present invention is directed to 4′-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4′-substituted nucleoside derivatives of Formula I and derivatives thereof.
-
公开(公告)号:US20180093992A1
公开(公告)日:2018-04-05
申请号:US15831895
申请日:2017-12-05
发明人: John Y. L. Chung , Feng Peng , Yonggang Chen , Amude Mahmoud Kassim , Cheng-yi Chen , Mathew Maust , Mark McLaughlin , Michael J. Zacuto , Qinghao Chen , Lushi Tan , Zhiguo Jake Song , Yang Cao , Feng Xu
IPC分类号: C07D487/04 , A61K31/4162
CPC分类号: C07D487/04 , A61K31/4162 , C07D309/30
摘要: A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of: and reductive amination of:
-
公开(公告)号:US20210122717A1
公开(公告)日:2021-04-29
申请号:US17048833
申请日:2019-04-18
发明人: Kevin M. Maloney , Kallol Basu , John Y.L. Chung , Richard Desmond , Michael James Di Maso , Guy R. Humphrey , Alfred Y. Lee , Dan Lehnherr , Feng Peng , Hong Ren , Mark Weisel , Siwei Zhang , Patrick Larpent
IPC分类号: C07D239/48 , C07D487/18 , C07C41/09 , C07C41/30 , C07C253/30
摘要: Disclosed herein is a novel process for preparing Compound A free base, 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-iso-propyl-2-methoxybenzenesulfonamide, and a citrate salt of Compound A with simplified chemistry and a high overall yield: Compound A. In one embodiment, the overall yield from the starting material 2-isopropylphenol to Compound A citrate salt is greater than 50%. In another embodiment, the overall yield is greater than 60%. Also disclosed herein are novel salts and solvates of Compound A.
-
公开(公告)号:US10131674B2
公开(公告)日:2018-11-20
申请号:US15524872
申请日:2015-11-05
发明人: Daniel A. DiRocco , Ian Davies , Feng Peng , Mark McLaughlin , Louis-Charles Campeau , Yingju Xu
IPC分类号: C07D498/04 , B01J31/18 , B01J35/00
摘要: The present invention is directed to a process for preparing Substituted Indole Compounds of Formula (I): wherein R1, R2, R3 and R4 are as defined herein. These indole compounds are useful as synthetic intermediates for making inhibitors of HCV NS5A.
-
公开(公告)号:US10053466B2
公开(公告)日:2018-08-21
申请号:US15831895
申请日:2017-12-05
发明人: John Y. L. Chung , Feng Peng , Yonggang Chen , Amude Mahmoud Kassim , Cheng-yi Chen , Mathew Maust , Mark McLaughlin , Michael J. Zacuto , Qinghao Chen , Lushi Tan , Zhiguo Jake Song , Yang Cao , Feng Xu
IPC分类号: C07D487/04 , A61K31/4162
摘要: A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of: and reductive amination of:
-
-
-
-
-
-
-
-
-