David A 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:

6740666, May 25, 2004

Filed:

Nov 9, 2001

Appl. No.:

10/040993

Inventors:

Dwight Macdonald - Llle Bizard, CA
Helene Perrier - Burlingame CA
Roch Thibert - Outremont, CA
Guo-Jie Ho - Scotch Plains NJ
Anant Vailaya - North Brunswick NJ
David Conlon - Plainsboro NJ
Elizabeth Kwong - Pointe-Claire, CA
Sophie-Dorothee Clas - Montreal, CA

Assignee:

Merck Co., Inc. - Rahway NJ
Merck Frosst Canada Co. - Kirkland

International Classification:

A61K 3147

US Classification:

514314, 546172

Abstract:

Novel sulfuric acid, methanesulfonic acid, p-toluenesulfonic acid, 2-naphthalenesulfonic acid, hydrochloride acid, or benzenesulfonic acid salts of substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.

US Patent:

6835837, Dec 28, 2004

Filed:

May 15, 2003

Appl. No.:

10/433538

Inventors:

Richard Desmond - Bridgewater NJ
David A. Conlon - Plainsboro NJ
Antoinette Drahus - Hoboken NJ
Guo-Jie Ho - Scotch Plains NJ
Brenda Pipik - Edison NJ
Carl Leblond - Gilbertsville PA
Anant Vailaya - North Brunswick NJ

Assignee:

Merck Co. Inc. - Rahway NJ

International Classification:

C07D41310

US Classification:

546167, 546172, 546173, 514314, 514311, 514256

Abstract:

A substituted 8-aryl quinoline and its benzenesulfonic acid salt is synthesized.

US Patent:

7563807, Jul 21, 2009

Filed:

Sep 12, 2003

Appl. No.:

10/526782

Inventors:

Mirlinda Biba - Piscataway NJ, US
Paul Compton Collins - Bridgewater NJ, US
Christopher Joseph Welch - Cranbury NJ, US
David A. Conlon - Plainsboro NJ, US
Antoinette Drahus - Lexington MA, US

Assignee:

Merck & Co. Inc. - Rahway NJ

International Classification:

A61K 31/47
A61K 31/4709
C07D 215/14
C07D 401/10
C07D 413/10

US Classification:

514314, 514311, 514256, 51425306, 546167, 546172, 546 73

Abstract:

A purification method in the preparation of a substituted 8-arylquinoline, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, utilizes a polystyrene-based sulfonylhydrazine reactive resin to remove an aldehyde impurity.

US Patent:

20030097001, May 22, 2003

Filed:

Dec 18, 2001

Appl. No.:

10/023089

Inventors:

Richard Desmond - Bridgewater NJ, US
David Conlon - Plainsboro NJ, US
Antoinette Drahus - Hoboken NJ, US
Guo-Jie Ho - Scotch Plains NJ, US
Brenda Pipik - Edison NJ, US
Carl Leblond - Gilbertsville PA, US
Anant Vailaya - North Brunswick NJ, US

International Classification:

C07D413/02

US Classification:

546/176000

Abstract:

A substituted 8-aryl quinoline and its benzenesulfonic acid salt is synthesized.

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.