公开(公告)号：US20070219382A1

公开(公告)日：2007-09-20

申请号：US11578283

申请日：2005-05-06

申请人： Spencer Dreher ,  Norihiro Ikemoto ,  Scott Shultz ,  Michael Williams

发明人： Spencer Dreher ,  Norihiro Ikemoto ,  Scott Shultz ,  Michael Williams

IPC分类号： C07D315/00 ,  C07C233/00 ,  C07C303/00

CPC分类号： C07D315/00 ,  C07C303/40 ,  C07C2601/14 ,  C07D309/04 ,  C07D309/06 ,  C07D309/20 ,  C07C311/13 ,  C07C311/19 ,  C07C311/16 ,  C07C311/29

摘要： This invention relates to a process for preparing optically active α-amino acid substrates which are used to make potent lethal factor (LF) inhibitors for the treatment of anthrax. This invention further relates to a process for synthesis of potent LF-inhibitors for the treatment of anthrax. Specifically, the invention concerns a novel, high-yielding and highly enantioselective asymmetric hydrogenation reaction of a tetrasubstituted ene-sulfonamide acid or ester.

摘要翻译： 本发明涉及用于制备用于治疗炭疽的有效的致死因子（LF）抑制剂的光学活性α-氨基酸底物的方法。 本发明还涉及一种合成用于治疗炭疽的强效LF抑制剂的方法。 具体地，本发明涉及四取代的烯 - 磺酰胺酸或酯的新颖的高产率和高度对映选择性的不对称氢化反应。

公开(公告)号：US20160304537A1

公开(公告)日：2016-10-20

申请号：US15103148

申请日：2014-12-05

申请人： Xiaoqing HAN ,  Alan WHITEHEAD ,  Subharekha RAGHAVAN ,  Timothy A. CERNAK ,  Spencer DREHER ,  Jonathan GROEPER ,  Jian GUO ,  Yong ZHANG ,  MERCK SHARP & DOHME CORP.

发明人： Xiaoqing Han ,  Alan Whitehead ,  Subharekha Raghavan ,  Timothy A. Cernak ,  Spencer Dreher ,  Jonathan Groeper ,  Jian Guo ,  Yong Zhang

IPC分类号： C07D519/00 ,  A61K45/06 ,  A61K31/519

CPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/52 ,  A61K45/06 ,  C07B2200/05 ,  A61K2300/00

摘要： A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20050090668A1

公开(公告)日：2005-04-28

申请号：US10954752

申请日：2004-09-30

申请人： Spencer Dreher

发明人： Spencer Dreher

IPC分类号： C07D239/36 ,  C07D413/04 ,  C07D239/02

CPC分类号： C07D239/36 ,  C07D413/04

摘要： 5-Hydroxy-6-oxo-1,6-dihydropyrimidine compounds are prepared by the condensation of dihydroxyfumarate derivatives with amidines. The pyrimidine compounds are useful as intermediates in the preparation of pharmacologically active compounds.

摘要翻译： 5-羟基-6-氧代-1,6-二氢嘧啶化合物通过二羟基富马酸盐衍生物与脒的缩合来制备。 嘧啶化合物可用作制备药理活性化合物的中间体。