Mark L 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:

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.

US Patent:

60692650, May 30, 2000

Filed:

Aug 19, 1999

Appl. No.:

9/377391

Inventors:

Mark S. Jensen - Holmdel NJ
Chunhua Yang - Edison NJ
Nobuyoshi Yasuda - Mountainside NJ
David A. Colon - Plainsboro NJ
Yi Xiao - Fanwood NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07F 722

US Classification:

556 87

Abstract:

The present invention relates to a process for synthesizing novel intermediates of formula III: ##STR1## wherein R. sup. 1 is a halogen. The intermediate compounds described herein are useful for the preparation of carbapenem compounds.