David O Conlon

US Patent:

6506908, Jan 14, 2003

Filed:

Apr 20, 2001

Appl. No.:

09/838989

Inventors:

Nobuyoshi Yasuda - Mountainside NJ
Michael Palucki - Hillsborough NJ
Joann M. Um - Franklin Lakes NJ
David Alan Conlon - Plainsboro NJ
Barry M. Trost - Los Altos CA

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

C07D33302

US Classification:

549 78, 568715

Abstract:

Processes are disclosed for preparing 3-hydroxymethylcyclopentanone compounds, which are useful as intermediates in the preparation of HIV chemokine CCR-5 receptor antagonists. A process is described in which the compounds are prepared by opening the cyclopropyl ring of a (1-alkoxycarbonyl-2-oxo)-trans-bicyclo[3. 1. 0]hexane compound by addition of a nucleophile to the cyclopropyl ring, and then decarboxylating the resulting 2-alkoxycarbonyl-3-(Nu-methyl)-cyclopentanone (Nu=the added nucleophilic group) via base solvolysis. Also described is a process for preparing the bicyclo[3. 1. 0]hexane precursors by the catalyzed cyclopropanation of a suitable alpha-diazo-beta-ketoester. The preparation of the alpha-diazo-beta-ketoesters and precursors thereto are also disclosed.

US Patent:

20050192346, Sep 1, 2005

Filed:

Feb 25, 2005

Appl. No.:

11/066676

Inventors:

F. Conrad Engelhardt - Hoboken NJ, US
Cameron John Cowden - Stanstead Abbots, GB
David Conlon - Plainsboro NJ, US
Brenda Pipik - Edison NJ, US

International Classification:

C07C317/24
A61K031/21

US Classification:

514509000, 558482000

Abstract:

The invention encompasses a novel process for making compounds of Formula I which are prodrugs of cyclooxygenase-2 selective inhibitors that convert in vivo to diaryl-2-(5H)-furanones and also liberate nitric oxide in vivo. As such, the compounds made by the present invention may be co-dosed with low-dose aspirin to treat chronic cyclooxygenase-2 mediated diseases or conditions, effectively reduce the risk of thrombotic cardiovascular events and potentially renal side effects and at the same time reduce the risk of GI ulceration or bleeding. The present invention describes an efficient and economical process for the preparation of 2,3-disubstituted (2Z)-4-acetoxybut-2-enoate derivatives that is useful for the production of kilogram quantities of material for preclinical and clinical use.

US Patent:

20070142635, Jun 21, 2007

Filed:

Dec 8, 2004

Appl. No.:

10/582414

Inventors:

David Askin - Warren NJ, US
David Conlon - Plainsboro NJ, US
Yoshinori Kohmura - Okazaki, JP
Jaemoon Lee - Edison NJ, US
Brenda Pipik - Edison NJ, US
Yong-Li Zhong - Edison NJ, US

International Classification:

C07F 9/6512
C07D 487/04

US Classification:

544244000, 544281000

Abstract:

Processes for preparing 10-amino-3-hydroxy-4-oxo-4,6,7,8,9,10-hexahydropyrimido[1,2-a]azepine-2-carboxylates and related compounds are disclosed. The preparation of carboxamide derivatives from these carboxylates is also disclosed. The carboxamides are HIV integrase inhibitors and are useful for treating HIV infection and AIDS.

US Patent:

20160022675, Jan 28, 2016

Filed:

Mar 12, 2014

Appl. No.:

14/774522

Inventors:

- Princeton NJ, US
David Alan CONLON - New Brunswick NJ, US
Paul C. LOBBEN - New Brunswick NJ, US
Justin Lockheart BURT - Greenwood IN, US
Joshua ENGSTROM - New Brunswick NJ, US
Carolyn S. WEI - New Brunswick NJ, US
Jason J. ZHU - New Brunswick NJ, US
Yu FAN - New Brunswick NJ, US

International Classification:

A61K 31/501
A61K 9/20
A61K 9/48
C07D 217/04

Abstract:

Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and compositions comprising the tetrahydroisoquinolines and other compounds, e.g, intermediates and by-products of the processes described herein. Pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression are also disclosed.