公开(公告)号：US07439400B2

公开(公告)日：2008-10-21

申请号：US10551770

申请日：2003-06-16

Applicant: Biao Jiang ,  Yugui Si

Inventor： Biao Jiang ,  Yugui Si

IPC: C07C33/042 ,  C07C29/42 ,  C07C215/36 ,  C07D239/80

CPC classification number: C07C213/02 ,  C07B2200/07 ,  C07C217/48 ,  C07C2601/02 ,  C07D239/80 ,  C07F7/1804 ,  C07C215/68

Abstract: The invention disclosed a new process of asymmetric alkynylation of ketone or ketimine, involving the chiral ligand-mediated asymmetric addition of zinc or copper acetylide to a trifluoromethyl ketone or ketimine intermediate to give a chiral tertiary proparglic alcohols or amines. The adduct compounds include the key precursors to the potent HIV reverse transcriptase inhibitor Efavirenz (DMP 266), DPC 961 and DPC 083. The invention also disclosed a novel chiral amino alcohol ligand.

Abstract translation: 本发明公开了酮或酮亚胺的不对称炔基化的新方法，其涉及手性配体介导的不对称加成的锌或铜乙炔化物至三氟甲基酮或酮亚胺中间体，得到手性叔炔醇或胺。 加合物包括有效的HIV逆转录酶抑制剂依法韦仑（DMP 266），DPC 961和DPC 083的关键前体。本发明还公开了一种新的手性氨基醇配体。

公开(公告)号：US20120101124A1

公开(公告)日：2012-04-26

申请号：US13379214

申请日：2010-06-17

Applicant: Xichen Lin ,  Feng Ren ,  Yugui Si

Inventor： Xichen Lin ,  Feng Ren ,  Yugui Si

IPC: A61K31/437 ,  A61K31/4439 ,  C07D413/14 ,  C07D413/10 ,  A61K31/4245 ,  A61P25/00 ,  A61P29/00 ,  A61P11/06 ,  A61P19/02 ,  A61P1/00 ,  A61P17/06 ,  A61P35/00 ,  A61P35/04 ,  A61P31/12 ,  A61P3/10 ,  A61P9/00 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07D413/04 ,  C07D413/14

Abstract: 1,2,4-Oxadiazol derivatives represented by formula (I) useful as sphingosine 1-phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders mediated via S1P1 receptor are disclosed.

Abstract translation: 可用作鞘氨醇1-磷酸1（S1P1）受体激动剂的式（I）表示的1,2,4-恶二唑衍生物，其制备方法，含有它们的药物组合物及其用于治疗通过S1P1受体介导的各种病症的用途 披露

公开(公告)号：US20060217552A1

公开(公告)日：2006-09-28

申请号：US10551770

申请日：2003-06-16

Applicant: Biao Jiang ,  Yugui Si

Inventor： Biao Jiang ,  Yugui Si

IPC: C07C215/34 ,  C07D239/76

CPC classification number: C07C213/02 ,  C07B2200/07 ,  C07C217/48 ,  C07C2601/02 ,  C07D239/80 ,  C07F7/1804 ,  C07C215/68

Abstract: The invention disclosed a new process of asymmetric alkynylation of ketone or ketimine, involving the chiral ligand-mediated asymmetric addition of zinc or copper acetylide to a trifluoromethyl ketone or ketimine intermediate to give a chiral tertiary proparglic alcohols or amines. The adduct compounds include the key precursors to the potent HIV reverse transcriptase inhibitor Efavirenz (DMP 266), DPC 961 and DPC 083. The invention also disclosed a novel chiral amino alcohol ligand.

Abstract translation: 本发明公开了酮或酮亚胺的不对称炔基化的新方法，其涉及手性配体介导的不对称加成的锌或铜乙炔化物至三氟甲基酮或酮亚胺中间体，得到手性叔炔醇或胺。 加合物包括有效的HIV逆转录酶抑制剂依法韦仑（DMP 266），DPC 961和DPC 083的关键前体。本发明还公开了一种新的手性氨基醇配体。