Alfred P Lee

US Patent:

20210122717, Apr 29, 2021

Filed:

Apr 18, 2019

Appl. No.:

17/048833

Inventors:

- Rahway NJ, US
- Werthenstein, CH
John Y.L. Chung - Edison NJ, US
Richard Desmond - Lebanon NJ, US
Michael James Di Maso - Hamilton NJ, US
Guy R. Humphrey - Hillsborough NJ, US
Alfred Y. Lee - Robbinsville NJ, US
Dan Lehnherr - Garwood NJ, US
Feng Peng - Dayton NJ, US
Hong Ren - Green Brook NJ, US
Mark Weisel - Stewartsville NJ, US
Siwei Zhang - Westfield NJ, US
Patrick Larpent - Luzern, CH

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ
Werthenstein BioPharma GmbH - Werthenstein

International Classification:

C07D 239/48
C07D 487/18
C07C 41/09
C07C 41/30
C07C 253/30

Abstract:

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.

US Patent:

20180000803, Jan 4, 2018

Filed:

Dec 14, 2015

Appl. No.:

15/536467

Inventors:

- Rahway NJ, US
Yung-Chi Lee - New Providence NJ, US
Alfred Lee - Robbinsville NJ, US
Dan Zhang - Watchung NJ, US
Tao Feng - Shanghai, CN

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

A61K 31/444
A61K 9/16

Abstract:

The invention includes a granular composition comprising the active ingredient (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3- carboxamide, wherein a total amount of active ingredient comprises by weight % about 60-90% (5)-N-(3-(6-isopro-poxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-di-hydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide Form 1 HCl, about 10-30% (5)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous HCl, and about 0-5% (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous free base.

US Patent:

20160311834, Oct 27, 2016

Filed:

Oct 24, 2014

Appl. No.:

15/032663

Inventors:

Michael McNEVIN - Basking Ridge NJ, US
Yong LIU - Princeton NJ, US
Ian MANGION - Cranford NJ, US
Alfred LEE - Robbinsville NJ, US
Joyce STELLABOTT - Perkasie PA, US
Benjamin D. SHERRY - New York NY, US
Gary MARTIN - Warren Township NJ, US
Kung-I FENG - Basking Ridge NJ, US
Scott SHULTZ - Maplewood NJ, US
Ryan COHEN - Piscataway NJ, US
Yanfeng ZHANG - Suzhou, CN

International Classification:

C07D 498/04
A61K 45/06
A61K 31/5383

Abstract:

The present invention relates to novel Pseudopolymorphs of Compound A, compositions comprising at least one Pseudopolymorph of Compound A, and methods of using the Pseudopolymorphs of Compound A for preparing compositions useful for treating or preventing HCV infection in a patient, wherein Compound A has the structure.

Author:

Alfred M. Lee

ISBN #:

0669055557

Author:

Alfred M. Lee

ISBN #:

0803909608

Author:

Alfred M. Lee

ISBN #:

0815623550

Author:

Alfred M. Lee

ISBN #:

0930390504

Author:

Alfred M. Lee

ISBN #:

0930390512

Author:

Alfred McClung Lee

ISBN #:

0139257764

Author:

Alfred McClung Lee

ISBN #:

0195023358

Author:

Alfred McClung Lee

ISBN #:

0195023366