David M 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:

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:

20060211687, Sep 21, 2006

Filed:

Mar 8, 2004

Appl. No.:

10/548781

Inventors:

Michael Palucki - Hillsborough NJ, US
David Askin - Warren NJ, US
Vincent Angelico - Edison NJ, US
Robert Wenslow Jr - East Windsor NJ, US

International Classification:

A61K 31/54
C07D 471/02

US Classification:

514222200, 544003000

Abstract:

A potassium salt of Compound A is disclosed, wherein Compound A is of formula (1): Compound A is an integrase inhibitor useful for preventing or treating HIV infection, for delaying the onset of AIDS, and for treating AIDS.

US Patent:

54461588, Aug 29, 1995

Filed:

Oct 12, 1990

Appl. No.:

7/596847

Inventors:

Todd K. Jones - Edison NJ
Sander G. Mills - Woodbridge NJ
David Askin - Edison NJ
Robert A. Reamer - Bloomfield NJ
Richard Desmond - Metuchen NJ
David M. Tschaen - Aberdeen NJ
Ralph P. Volante - East Windsor NJ
Ichiro Shinkai - Westfield NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07F 718

US Classification:

546 14

Abstract:

A process is described for the total synthesis of the macrolide immunosuppressant, FK-506, and important tricarbonyl process intermediates thereof. The tricarbonyl intermediates can be produced by the mild oxidation of 2,3-dihydroxy carboxylate compounds containing olefin moieties.

US Patent:

49202189, Apr 24, 1990

Filed:

Sep 5, 1989

Appl. No.:

7/403794

Inventors:

David Askin - Edison NJ
Todd K. Jones - Edison NJ
Robert A. Reamer - Bloomfield NJ
Ralph P. Volante - East Windsor NJ
Ichiro Shinkai - Westfield NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D49816
C07D49818

US Classification:

540456

Abstract:

A process is described involving an alkaline rearrangement of FK-506 producing a new decarbonylated 22-membered macrocycle rearrangement derivative of FK-506, i. e. C. 9, nor-keto FK-506.

US Patent:

51645254, Nov 17, 1992

Filed:

Jun 30, 1989

Appl. No.:

7/374508

Inventors:

David Askin - Edison NJ
Ralph P. Volante - East Windsor NJ
Daisy Joe - Union NJ
Ichiro Shinkai - Westfield NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07F 708
C07F 718

US Classification:

556444

Abstract:

A process for the conversion of FK-506 (I,R=allyl;1) to FK-525 (XV) and analogous 23-membered ring macrolides differing in the C. 1-N. 7 segment of the molecule (e. g. XVI) and is also applicable to the analogs FK-523 (XVII) and FK-520 (XVIII). The overall process consists of three stages: (a) initial degradation of the primary macrolide to an acyclic fragment containing a selectively protected C. 10-C. 34 framework with a protected aldehyde function at C. 10 and a free hydroxyl function at C. 26, (b) reacylation of the C. 26 hydroxyl function with an appropriately N-protected alpha-amino acid moiety, and (c) reintroduction of the C. 8 and C. 9 carbons followed by regeneration of the FK-macrolide system.

US Patent:

49804669, Dec 25, 1990

Filed:

Oct 26, 1989

Appl. No.:

7/427536

Inventors:

David Askin - Edison NJ
Todd K. Jones - Edison NJ
Robert A. Reamer - Bloomfield NJ
Ralph P. Volante - East Windsor NJ
Ichiro Shinkai - Westfield NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D49816

US Classification:

540456

Abstract:

A process is described involving an alkaline rearrangement of FK-506 producing a new decarbonylated 22-membered macrocycle rearrangement derivative of FK-506, i. e. C. 9, nor-keto FK-506.