公开(公告)号：US08975447B2

公开(公告)日：2015-03-10

申请号：US14003248

申请日：2012-03-06

Applicant: Wenjie Li ,  Zhi-Hui Lu ,  Chris Hugh Senanayake ,  Yongda Zhang

Inventor： Wenjie Li ,  Zhi-Hui Lu ,  Chris Hugh Senanayake ,  Yongda Zhang

IPC: C07C33/48 ,  C07C39/38 ,  C07C29/38 ,  C07C29/40 ,  C07C39/14 ,  C07C37/055 ,  C07C41/48 ,  C07C29/143 ,  C07C37/62

CPC classification number: C07C39/14 ,  C07B2200/07 ,  C07C29/143 ,  C07C29/38 ,  C07C37/055 ,  C07C37/62 ,  C07C39/38 ,  C07C41/48 ,  C07C43/313 ,  C07C33/483

Abstract: Disclosed are a process and catalysts useful for carrying out asymmetric methlyallylations. The catalysts used in the invention have the formula (IV): wherein X1, X2, R3 and R4 are as defined herein. Compounds made by the process of the invention can be used to prepare pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors including 1,3-disubstituted oxazinan-2-ones.

Abstract translation: 公开了用于进行不对称甲基化反应的方法和催化剂。 用于本发明的催化剂具有式（Ⅳ）：其中X 1，X 2，R 3和R 4如本文所定义。 通过本发明的方法制备的化合物可用于制备药物活性化合物，例如11-＆bgr-羟基类固醇氢化酶1型（11-＆amp; bgr-HSD1）抑制剂，包括1,3-二取代的恶嗪烷-2-酮。

公开(公告)号：US08916701B2

公开(公告)日：2014-12-23

申请号：US13921145

申请日：2011-12-15

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

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

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

CPC classification number: C07D413/10 ,  C07C271/48 ,  C07D213/64 ,  C07D265/10

Abstract: 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.

Abstract translation: 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：US20090264655A1

公开(公告)日：2009-10-22

申请号：US12487910

申请日：2009-06-19

Applicant: Ahmad KHODABOCUS ,  Zhi-Hui Lu ,  Chris Hugh Senanayake ,  Hanxun Wei ,  Yongda Zhang

Inventor： Ahmad KHODABOCUS ,  Zhi-Hui Lu ,  Chris Hugh Senanayake ,  Hanxun Wei ,  Yongda Zhang

IPC: C07D403/04 ,  C07D209/18 ,  C07D403/12

CPC classification number: C07D209/10 ,  C07D209/08 ,  C07D209/12 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04

Abstract: Disclosed are processes for making 2, 3 disubstituted indole compounds such as compounds of general formula I comprised of the steps of a) reacting a bromoindole compound (i) with a dialkoxyl C1-5 borane in the presence of a ligand, a palladium catalyst and a base to make a compound of general formula (ii); or alternatively reacting compound (i) with a trialkyl magnesiate reagent, followed by treatment with a borate; b) reacting the product of step a with a R2-Hal where R2-Hal is defined herein.

Abstract translation: 公开了制备2,3,4-二取代吲哚化合物的方法，例如通式I的化合物，其包括以下步骤：a）在配体，钯催化剂和钯催化剂存在下使溴吲哚化合物（i）与二烷氧基C1-5硼烷反应， 制备通式（ii）的化合物的碱; 或者使化合物（i）与三烷基氧化镁试剂反应，然后用硼酸盐处理; b）使步骤a的产物与本文定义R 2 Hal的R 2-Hal反应。

公开(公告)号：US07332610B2

公开(公告)日：2008-02-19

申请号：US11514141

申请日：2006-09-01

Applicant: Zhengxu Han ,  Dhileepkumar Krishnamurthy ,  Chris Hugh Senanayake ,  Zhi-Hui Lu

Inventor： Zhengxu Han ,  Dhileepkumar Krishnamurthy ,  Chris Hugh Senanayake ,  Zhi-Hui Lu

IPC: C07D291/04

CPC classification number: C07D291/04 ,  C07B2200/07 ,  C07C209/52 ,  C07C249/02 ,  C07C303/34 ,  C07C2601/04 ,  C07D453/04 ,  C07C307/02 ,  C07C211/29 ,  C07C251/16

Abstract: This invention provides intermediates useful in a method of preparing amine stereoisomers. It also provides a method of preparing sulfoxide and sulfinylamine stereoisomers using certain of the intermediates.

Abstract translation: 本发明提供了可用于制备胺立体异构体的方法的中间体。 它还提供了使用某些中间体制备亚砜和亚磺酰胺立体异构体的方法。

公开(公告)号：US07125845B2

公开(公告)日：2006-10-24

申请号：US10613206

申请日：2003-07-03

Applicant: Frank X. H. Wu ,  Suanne Nakajima ,  Zhi-Hui Lu ,  Ying Sun ,  Zhenwei Miao ,  Yat Sun Or ,  Zhe Wang

Inventor： Frank X. H. Wu ,  Suanne Nakajima ,  Zhi-Hui Lu ,  Ying Sun ,  Zhenwei Miao ,  Yat Sun Or ,  Zhe Wang

IPC: A61K38/00

CPC classification number: C07K5/06139 ,  A61K38/00 ,  C07K5/06165

Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract translation: 本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）NS3-NS4A蛋白酶活性的式I化合物或其药学上可接受的盐，酯或前药。 因此，本发明的化合物干扰丙型肝炎病毒的生命周期，也可用作抗病毒剂。 本发明还涉及药物组合物，其包含用于给患有HCV感染的受试者施用的上述化合物。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的HCV感染的方法。

公开(公告)号：US08598183B2

公开(公告)日：2013-12-03

申请号：US13241551

申请日：2011-09-23

Applicant: Rolf-Stefan Brickl ,  Shirlynn Chen ,  Jihchin Chung ,  Mayur Suryakant Dudhedia ,  Danping Li ,  Zhi-Hui Lu ,  Siddharthya Mujumdar ,  Chitra Telang ,  Richard J. Varsolona ,  Zeren Wang

Inventor： Rolf-Stefan Brickl ,  Shirlynn Chen ,  Jihchin Chung ,  Mayur Suryakant Dudhedia ,  Danping Li ,  Zhi-Hui Lu ,  Siddharthya Mujumdar ,  Chitra Telang ,  Richard J. Varsolona ,  Zeren Wang

IPC: C07D235/04

CPC classification number: C07D403/14

Abstract: This invention relates to novel sodium salt forms of the following Compound (1), and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:

Abstract translation: 本发明涉及以下化合物（1）的新型钠盐形式及其制备方法，其药物组合物及其在治疗丙型肝炎病毒（HCV）感染中的用途：

公开(公告)号：US20120122887A1

公开(公告)日：2012-05-17

申请号：US13241551

申请日：2011-09-23

Applicant: Rolf-Stefan BRICKL ,  Shirlynn CHEN ,  Jihchin CHUNG ,  Mayur Suryakant DUDHEDIA ,  Danping LI ,  Zhi-Hui LU ,  Siddharthya MUJUMDAR ,  Chitra TELANG ,  Richard J. VARSOLONA ,  Zeren WANG

Inventor： Rolf-Stefan BRICKL ,  Shirlynn CHEN ,  Jihchin CHUNG ,  Mayur Suryakant DUDHEDIA ,  Danping LI ,  Zhi-Hui LU ,  Siddharthya MUJUMDAR ,  Chitra TELANG ,  Richard J. VARSOLONA ,  Zeren WANG

IPC: A61K31/506 ,  A61P31/12 ,  C07D403/14

CPC classification number: C07D403/14

Abstract: This invention relates to novel sodium salt forms of the following Compound (1), and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:

Abstract translation: 本发明涉及以下化合物（1）的新型钠盐形式及其制备方法，其药物组合物及其在治疗丙型肝炎病毒（HCV）感染中的用途：

公开(公告)号：US20080214870A1

公开(公告)日：2008-09-04

申请号：US12032727

申请日：2008-02-18

Applicant: Zhengxu Han ,  Dhileepkumar Krishnamurthy ,  Chris Hugh Senanayake ,  Zhi-Hui Lu

Inventor： Zhengxu Han ,  Dhileepkumar Krishnamurthy ,  Chris Hugh Senanayake ,  Zhi-Hui Lu

IPC: C07C251/00

CPC classification number: C07D291/04 ,  C07B2200/07 ,  C07C209/52 ,  C07C249/02 ,  C07C303/34 ,  C07C2601/04 ,  C07D453/04 ,  C07C307/02 ,  C07C211/29 ,  C07C251/16

Abstract: This invention provides intermediates useful in a method of preparing amine stereoisomers. It also provides a method of preparing sulfoxide and sulfinylamine stereoisomers using certain of the intermediates.

Abstract translation: 本发明提供了可用于制备胺立体异构体的方法的中间体。 它还提供了使用某些中间体制备亚砜和亚磺酰胺立体异构体的方法。

公开(公告)号：US07408076B2

公开(公告)日：2008-08-05

申请号：US11468185

申请日：2006-08-29

Applicant: Guisheng Li ,  Jianxiu Liu ,  Zhi-Hui Lu ,  Frank Roschangar ,  Chris Hugh Senanayake ,  Ming Shen

Inventor： Guisheng Li ,  Jianxiu Liu ,  Zhi-Hui Lu ,  Frank Roschangar ,  Chris Hugh Senanayake ,  Ming Shen

IPC: C07C229/54 ,  C07D263/42

CPC classification number: C07C237/38 ,  C07C2601/04 ,  C07D209/12 ,  C07D401/04

Abstract: Disclosed are 2-bromoaniline or 2-chloroaniline compounds of formula (I): wherein R, R1 and X are as defined. The compounds are useful as intermediates for preparing indole compounds.

Abstract translation: 公开了式（I）的2-溴苯胺或2-氯苯胺化合物：其中R 1，R 1和X如上所定义。 该化合物可用作制备吲哚化合物的中间体。

公开(公告)号：US07332614B2

公开(公告)日：2008-02-19

申请号：US11074194

申请日：2005-03-07

Applicant: Ahmad Khodabocus ,  Guisheng Li ,  Zhi-Hui Lu ,  Frank Roschangar ,  Chris Hugh Senanayake ,  Ming Shen

Inventor： Ahmad Khodabocus ,  Guisheng Li ,  Zhi-Hui Lu ,  Frank Roschangar ,  Chris Hugh Senanayake ,  Ming Shen

IPC: C07D209/10 ,  A61K31/404

CPC classification number: C07D209/30

Abstract: The present invention provides a process for making a compound of general formula I: wherein: R=H or C1-8alkyl X=C3-C8cycloalkyl, C3-C8aryl or C3-C8alkyl; Y=heteroaryl or aryl; Z=H, HO2C—, C1-8alkyl O2C—, C1-6alkyl HNC(O)—, and as described herein.

Abstract translation: 本发明提供制备通式I化合物的方法：其中：R = H或C 1-8烷基X = C 3 -C 8 C 3 -C 8环烷基，C 3 -C 8芳基或C 3 -C 8烷基; Y =杂芳基或芳基; Z = H，HO 2 C，C 1-8烷基，O 2 C，C 1-6，N， 烷基HNC（O） - ，并如本文所述。