David B Askin

US Patent:

6388083, May 14, 2002

Filed:

Jul 5, 2001

Appl. No.:

09/899633

Inventors:

Jaemoon Lee - Edison NJ
David Askin - Warren NJ
Thoa Hoang - Iselin NJ

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

C07D21102

US Classification:

546216

Abstract:

The present invention is concerned with novel processes for the preparation of (2S)-phenyl-3-piperidone. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.

US Patent:

6642237, Nov 4, 2003

Filed:

Nov 21, 2000

Appl. No.:

09/718223

Inventors:

James R. Tata - Westfield NJ
Kevin T. Chapman - Scotch Plains NJ
Joseph Leslie Duffy - Cranford NJ
Nancy J. Kevin - East Brunswick NJ
Yuan Cheng - Edison NJ
Thomas A. Rano - Somerville NJ
Fengqi Zhang - Edison NJ
Tracy Huening - Madison NJ
Brian Anthony Kirk - Basking Ridge NJ
Zhijian Lu - Clinton NJ
Subharekha Raghavan - Teaneck NJ
Fred J. Fleitz - Franklin Park NJ
Daniel E. Petrillo - Hoboken NJ
Richard J. Varsolona - Scotch Plains NJ
David Askin - Warren NJ
R. Scott Hoerrner - Westfield NJ
Robert Purick - Edison NJ

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

C07D491048

US Classification:

51425202, 544362, 544376, 544364, 544295, 51425304, 51425311, 51425301, 514252

Abstract:

-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

US Patent:

7598264, Oct 6, 2009

Filed:

Mar 9, 2005

Appl. No.:

10/587682

Inventors:

Wei Han - West Chester PA, US
Melissa Egbertson - Ambler PA, US
John S. Wai - Harleysville PA, US
Linghang Zhuang - Chalfont PA, US
Rowena D. Ruzek - North Wales PA, US
Debra S. Perlow - East Greenville PA, US
Mark Cameron - Brick NJ, US
Bruce S. Foster - Scoth Plains NJ, US
Ulf H. Dolling - Westfield NJ, US
R. Scott Hoerrner - Westfield NJ, US
Philip J. Pye - Guttenberg NJ, US
Remy Angelaud - Union NJ, US
Danny E. Mancheno - Rego Park NY, US
David Askin - Warren NJ, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A01N 43/42
A61K 31/44
C07D 471/02
C07D 491/02
C07D 498/02
C07D 513/02

US Classification:

514300, 546113

Abstract:

Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, R1?, R2?, R3?, R4? and R5? are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

US Patent:

20040186093, Sep 23, 2004

Filed:

Feb 10, 2004

Appl. No.:

10/486526

Inventors:

Jaemoon Lee - Edison NJ, US
David Askin - Warren NJ, US
Mark Jensen - Holmdel NJ, US
Yong-Li Zhong - Woodbridge NJ, US

International Classification:

A61K031/554
A61K031/54

US Classification:

514/211010, 514/222200, 544/001000, 540/544000

Abstract:

The preparation of sultams is disclosed. In one embodiment (e.g. scheme (I)), an alkanesulfonyl halide is reacted with a haloalkylamine to obtain the corresponding N-(haloalkyl)alkanesulfonamide which is then cyclized in the presence of a deprotonating agent to give the sultam. The sultams are useful as intermediates in the preparation of naphthyridine carboxamide compounds which are HIV integrase inhibitors.

US Patent:

20040267026, Dec 30, 2004

Filed:

Jun 4, 2004

Appl. No.:

10/860916

Inventors:

David Askin - Warren NJ, US
Jaemoon Lee - Edison NJ, US
Yong-Li Zhong - Edison NJ, US

International Classification:

C07D233/61

US Classification:

548/338100

Abstract:

The invention is a process for preparing an imidazole of formula I which comprises treating an N-acylated -amino nitrile with a phosphine and a carbon tetrahalide of the formula CX, wherein X is Cl or Br, to form a haloimidazole of the formula wherein Ris selected from the group consisting of hydrogen, Calkyl, —CH-aryl, and aryl; and Ris selected from the group consisting of hydrogen, Calkyl, —CH—O-aryl and aryl; and X is selected from the group consisting of Cl and Br.

US Patent:

20050014780, Jan 20, 2005

Filed:

Aug 13, 2002

Appl. No.:

10/486535

Inventors:

Peter Maligres - Fanwood NJ, US
David Askin - Warren NJ, US

International Classification:

C07D471/02
A61K031/4745

US Classification:

514300000, 546123000

Abstract:

The preparation of 5-sulfonamido-8-hydroxy-1,6-naphthyridine-7-carboxamides is disclosed. A 5-halo-8-hydroxy-1,6-napthyridine-7-carboxylic acid or acid ester in which the hydroxy is derivatized with a protecting group is reacted with a sulfonamide (e.g., an alkanesulfonamide, N-alkyl alkanesulfonamide, or alkanesultam) in the presence of a copper promoter and a chelating agent, followed by deprotection of the hydroxy group, and then coupling with an amine to obtain the 5-sulfonamido-8-hydroxy-1,6-naphthyridine-7-carboxamide. Alternatively, the hydroxy-protected 5-halo-8-hydroxy-1,6-napthyridine-7-carboxylic acid (or ester) is first coupled with an amine, the resulting carboxamide reacted with a sulfonamide followed by deprotection of the hydroxy group to obtain the 5-sulfonamido-8-hydroxy-1,6-naphthyridine-7-carboxamide. The 5-sulfonamido-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and are useful for treating HIV infection, preventing HIV infection, delaying the onset of AIDS, and treating AIDS.

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:

51699524, Dec 8, 1992

Filed:

Jul 2, 1991

Appl. No.:

7/724617

Inventors:

David Askin - Warren NJ
Ralph Volante - East Windsor NJ
Michael Wallace - Matawan NJ
Ichiro Shinkai - Westfield NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07C27120
C07D26352
C07D295104

US Classification:

544137

Abstract:

An efficient process for stereoselective preparation of a medicinally significant hydroxyamide compound of structural formula: ##STR1## comprises the addition of metalated amide enolates to chiral. alpha. -amino metalated epoxides. The hydroxyamide reaction products are useful as inhibitors of the HIV protease or of renin, or as intermediates in the preparation of inhibitors of the HIV protease or renin.