公开(公告)号：US08916701B2

公开(公告)日：2014-12-23

申请号：US13921145

申请日：2011-12-15

申请人： Daniel Robert Fandrick ,  Zhi-Hui Lu ,  Diana Reeves ,  Jonathan Reeves ,  Chris Hugh Senanayake ,  Jinhua Jeff Song ,  Yongda Zhang

发明人： Daniel Robert Fandrick ,  Zhi-Hui Lu ,  Diana Reeves ,  Jonathan Reeves ,  Chris Hugh Senanayake ,  Jinhua Jeff Song ,  Yongda Zhang

IPC分类号： C07D413/10 ,  C07D265/10 ,  C07D213/64

CPC分类号： C07D413/10 ,  C07C271/48 ,  C07D213/64 ,  C07D265/10

摘要： Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and R1 to R4 are as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors.

摘要翻译： 公开了制备式（I）的非对映体化合物的方法：其中m，n和R 1至R 4如本文所定义。 本发明的方法以高产率提供式（I）化合物，基本上不含相应的非对映异构体。 通过本发明的方法制备的式（I）化合物可用于制备药学活性化合物，例如11-羟基类固醇类氢化酶1型（11-＆amp; -HSD1）抑制剂。

公开(公告)号：US20140135493A1

公开(公告)日：2014-05-15

申请号：US13921145

申请日：2011-12-15

申请人： Daniel Robert Fandrick ,  Zhi-Hui Lu ,  Diana Crimhilda Reeves ,  Jonathan Timothy Reeves ,  Chris Hugh Senanayake ,  Jinhua J. Song ,  Yongda Zhang

发明人： Daniel Robert Fandrick ,  Zhi-Hui Lu ,  Diana Crimhilda Reeves ,  Jonathan Timothy Reeves ,  Chris Hugh Senanayake ,  Jinhua J. Song ,  Yongda Zhang

IPC分类号： C07D413/10 ,  C07D213/64 ,  C07C271/48 ,  C07D265/10

CPC分类号： C07D413/10 ,  C07C271/48 ,  C07D213/64 ,  C07D265/10

摘要： Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and R1 to R4 are as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors.

摘要翻译： 公开了制备式（I）的非对映体化合物的方法：其中m，n和R 1至R 4如本文所定义。 本发明的方法以高产率提供式（I）化合物，基本上不含相应的非对映异构体。 通过本发明的方法制备的式（I）化合物可用于制备药学活性化合物，例如11-羟基类固醇类氢化酶1型（11-＆amp; -HSD1）抑制剂。

公开(公告)号：US07879873B2

公开(公告)日：2011-02-01

申请号：US12564129

申请日：2009-09-22

申请人： Brian Nicholas Cook ,  Darren DiSalvo ,  Daniel Robert Fandrick ,  Christian Harcken ,  Daniel Kuzmich ,  Thomas Wai-Ho Lee ,  Pingrong Liu ,  John Lord ,  Can Mao ,  Jochen Neu ,  Brian Christopher Raudenbush ,  Hossein Razavi ,  Jonathan Timothy Reeves ,  Jinhua J. Song ,  Alan David Swinamer ,  Zhulin Tan

发明人： Brian Nicholas Cook ,  Darren DiSalvo ,  Daniel Robert Fandrick ,  Christian Harcken ,  Daniel Kuzmich ,  Thomas Wai-Ho Lee ,  Pingrong Liu ,  John Lord ,  Can Mao ,  Jochen Neu ,  Brian Christopher Raudenbush ,  Hossein Razavi ,  Jonathan Timothy Reeves ,  Jinhua J. Song ,  Alan David Swinamer ,  Zhulin Tan

IPC分类号： A61K31/437 ,  C07D515/04

CPC分类号： C07D471/04

摘要： Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.