Mark S Jensen

US Patent:

6346617, Feb 12, 2002

Filed:

Jun 16, 1999

Appl. No.:

09/334397

Inventors:

John Y. Chung - Edison NJ
Nobuyoshi Yasuda - Mountainside NJ
Mark S. Jensen - Holmdel NJ
Kenneth M. Wells - Neshanic Station NJ
Chunhua Yang - Edison NJ

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

C07D47714

US Classification:

540302

Abstract:

A process for preparation of a compound of formula I: wherein: R represents CH or H; and P represents a protecting group; comprising reacting a compound of formula IV: âwherein R and P and are defined above and R represents triflate or SO F; in the presence of a catalyst and (R ) SnCH OPâ, wherein each R represents C lower alkyl, and Pâ represents H or a protecting group, to yield the compound of formula I.

US Patent:

6407241, Jun 18, 2002

Filed:

Nov 7, 2000

Appl. No.:

09/707403

Inventors:

Mark S Jensen - Holmdel NJ
Michael Palucki - Belle Mead NJ
Nelo R. Rivera - Scotch Plains NJ
Kenneth M. Wells - Neshanic Station NJ
Yi Xiao - Fanwood NJ
Yaling Wang - Westfield NJ
Chunhua Yang - Edison NJ
Nobuyoshi Yasuda - Mountainside NJ

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

C07D47104

US Classification:

546122, 546300, 546301, 544238, 544264, 544333, 544405

Abstract:

A novel process is provided for the preparation of imidazolidinone v3/v5 integrin antagonists, and the useful intermediates obtained therein. These compounds are antagonists of v3/v5 integrin receptors and thus useful for inhibiting bone resorption and treating and preventing osteoporosis. Also disclosed is 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid in the form of a hemihydrate.

US Patent:

7473696, Jan 6, 2009

Filed:

Oct 25, 2004

Appl. No.:

10/577584

Inventors:

Mark Jensen - Holmdel NJ, US
Robert Larsen - Bridgewater NJ, US
Daniel Richard Sidler - Whitehouse Station NJ, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31/4375
C07D 471/04

US Classification:

514300, 546122

Abstract:

An efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl} cyclopentyl)[(3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl]amine and its succinate salt are provided. The succinate salt is crystalline and has superior properties.

US Patent:

8110569, Feb 7, 2012

Filed:

Mar 20, 2007

Appl. No.:

11/726289

Inventors:

David Putman - Irvine CA, US
Derk Hogenkamp - Carlsbad CA, US
Olivier Dasse - Foothill Ranch CA, US
Edward R. Whittemore - Costa Mesa CA, US
Mark S. Jensen - Wake Forest NC, US

Assignee:

The Regents of the University of California - Oakland CA

International Classification:

C07D 265/18
A61K 31/536

US Classification:

5142305, 544 90

Abstract:

Enantiomerically pure S-etifoxine and pharmaceutically acceptable salts, solvates, hydrates or prodrugs thereof are provided. Also provided are pharmaceutical compositions comprising the compounds and methods of treating disorders associated with central nervous system using the compounds and pharmaceutical compositions.

US Patent:

7361765, Apr 22, 2008

Filed:

Oct 25, 2004

Appl. No.:

10/577587

Inventors:

Dongwei Cai - Edison NJ, US
Fred Fleitz - Franklin Park NJ, US
Min Ge - Edison NJ, US
Scott Hoerrner - Westfield NJ, US
Gary Javadi - Princeton NJ, US
Mark Jensen - Holmdel NJ, US
Robert Larsen - Newbury Park CA, US
Wenjie Li - Edison NJ, US
Dorian Nelson - St Paul MN, US
Elizabeth Szumigala - Somerville NJ, US
Lihu Yang - Edison NJ, US
Changyou Zhou - Plainsboro NJ, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D 471/02

US Classification:

546122

Abstract:

The present invention provides an efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-m ethoxytetrahydro-2H-pyran-4-yl]amine and its succinate salt. The present invention additionally provides an efficient syntheses for the preparation of intermediates (3R)-3-methoxytetrahydro-4H-pyran-4-one; (1S,4S)-4-(2,5-dimethyl-1H-pyrrol-1-yl)-1-isopropylcyclopent-2-ene-1-carboxylic acid; and 3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine; and for the preparation of the precursor (3S,4S)-N-((1S,4S)-4-isopropyl-4-{[3-(tri-fluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopent-2-en-1-yl)-3-methoxytetrahydro-2H-pyran-4-amine. The invention additionally resides in the superior properties of the succinate salt of ((1R,3S)-3-isopropyl-3-1{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl]amine.

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:

62358987, May 22, 2001

Filed:

Feb 23, 2000

Appl. No.:

9/511958

Inventors:

Mark S. Jensen - Holmdel NJ
Chunhua Yang - Edison NJ
Nobuyoshi Yasuda - Mountainside NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D47706
C07F 722

US Classification:

540302

Abstract:

A process of synthesizing a carbapenem compound of formula 6: ##STR1## is disclosed using a compound of formula 4': ##STR2## The intermediate compounds that are described herein are also included in the present invention.

US Patent:

60489782, Apr 11, 2000

Filed:

Sep 23, 1998

Appl. No.:

9/159158

Inventors:

Mark S. Jensen - Holmdel NJ
Chunhua Yang - Edison NJ
Nobuyoshi Yasuda - Mountainside NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D26722
C07D48700

US Classification:

540468

Abstract:

A process of synthesizing a carbapenem compound of formula 6: ##STR1## is disclosed using a compound of formula 4': ##STR2## The intermediate compounds that are described herein are also included in the present invention.