Mark Greenlee

US Patent:

6630510, Oct 7, 2003

Filed:

Oct 26, 2000

Appl. No.:

09/697415

Inventors:

James M. Balkovec - Martinsville NJ
Mark L. Greenlee - Rahway NJ
Steven H. Olson - Metuchen NJ
Gregory P. Rouen - New Brunswick NJ

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

C07C 5510

US Classification:

514557, 560 76, 560155, 560171, 560190, 546235, 546349, 5483001

Abstract:

This invention relates to novel substituted succinic acid metallo--lactamase inhibitors which are useful potentiators of -lactam antibiotics. Accordingly, the present invention provides a method of treating bacterial infections in animals or humans which comprises administering, together with a b-lactam antibiotic, a therapeutically effective amount of a compound of formula I: including pharmaceutically acceptable salts, prodrugs, anhydrides, and solvates thereof.

US Patent:

7511152, Mar 31, 2009

Filed:

Dec 5, 2005

Appl. No.:

11/792729

Inventors:

Mark L. Greenlee - Plainfield NJ, US
Dongfang Meng - Westfield NJ, US
Donald M. Sperbeck - East Hanover NJ, US
Kenneth J. Wildonger - Bridgewater NJ, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D 249/16
C07D 403/00
C07D 249/04
A61K 31/41

US Classification:

548261, 548255, 548257, 548259, 514359

Abstract:

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, age-related mild cognitive impairment, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, irritable bowel syndrome, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.

US Patent:

7709508, May 4, 2010

Filed:

Feb 12, 2009

Appl. No.:

12/378198

Inventors:

Mark L. Greenlee - Plainfield NJ, US
Dongfang Meng - Westfield NJ, US
Donald M. Sperbeck - East Hanover NJ, US
Kenneth J. Wildonger - Bridgewater NJ, US

Assignee:

Merck Sharp & Dohme - Rahway NJ

International Classification:

A61K 31/4192

US Classification:

514359

Abstract:

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, age-related mild cognitive impairment, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, irritable bowel syndrome, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.

US Patent:

7732432, Jun 8, 2010

Filed:

Jan 16, 2004

Appl. No.:

10/540757

Inventors:

Amjad Ali - Piscataway NJ, US
James M. Balkovec - Martinsville NJ, US
Donald W. Graham - Mountainside NJ, US
Mark L. Greenlee - Plainfield NJ, US
Gayle E. Taylor - Jersey City NJ, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

A61K 31/56
C07J 5/00

US Classification:

514178, 514179, 552570

Abstract:

The present invention encompasses compounds of Formula (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.

US Patent:

7863465, Jan 4, 2011

Filed:

Mar 29, 2007

Appl. No.:

11/727927

Inventors:

James M. Balkovec - Martinsville NJ, US
Frances Aileen Bouffard - Scotch Plains NJ, US
Bruno Tse - San Diego CA, US
James Dropinski - Colts Neck NJ, US
Dongfang Meng - Westfield NJ, US
Mark L. Greenlee - Plainfield NJ, US
Michael Peel - Chapel Hill NC, US
Weiming Fan - Chapel Hill NC, US
Ahmed Mamai - Raleigh NC, US
Hao Liu - Raleigh NC, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ
Scynexis, Inc. - Research Triangle Park NC

International Classification:

C07D 311/00
C07D 315/00

US Classification:

549381, 417432

Abstract:

The present invention relates to novel enfumafungin derivatives of formula I and pharmaceutically acceptable salts thereof, their synthesis, and their use as inhibitors of (1,3)-β-D-glucan synthase. The present compounds and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the present compounds and pharmaceutically acceptable salts thereof, are useful for treating or preventing antifungal infections and associated diseases and conditions.

US Patent:

7923568, Apr 12, 2011

Filed:

Sep 29, 2006

Appl. No.:

11/992879

Inventors:

Mark L. Greenlee - Plainfield NJ, US
Dongfang Meng - Westfield NJ, US
Wanying Sun - Edison NJ, US
Kenneth J. Wildonger - Bridgewater NJ, US
Robert R. Wilkening - Maplewood NJ, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

C07D 249/16
A61K 31/416
A61K 31/4192

US Classification:

548257, 548259, 548261, 5483585, 514359, 514406

Abstract:

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.

US Patent:

8188085, May 29, 2012

Filed:

Aug 7, 2009

Appl. No.:

12/461318

Inventors:

Mark L. Greenlee - Plainfield NJ, US
Robert Wilkening - Maplewood NJ, US
James Apgar - Edison NJ, US
Donald Sperbeck - East Hanover NJ, US
Kenneth J. Wildonger - Bridgewater NJ, US
Dongfang Meng - Westfield NJ, US
Gregory J. Pacofsky - Raleigh NC, US
Brian H. Heasley - Wake Forest NC, US
Ahmed Mamai - Raleigh NC, US
Kingsley Nelson - Mebane NC, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NC
Seynexis, Inc. - Research Triangle Park NC

International Classification:

A61K 31/41
A61K 31/445
A61K 31/501
C07D 231/02
C07D 249/08
C07D 401/00
C07D 401/02
C07D 405/02
C07D 405/14

US Classification:

51425205, 514320, 514337, 514359, 514383, 514406, 546210, 5462724, 548256, 5482648, 5482662, 5482676, 5483644

Abstract:

Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.

US Patent:

20020019543, Feb 14, 2002

Filed:

Dec 20, 2000

Appl. No.:

09/741644

Inventors:

James Balkovec - Martinsville NJ, US
Mark Greenlee - Rahway NJ, US
Milton Hammond - Somerville NJ, US
James Heck - Rahway NJ, US

International Classification:

C07D333/76
C 07D 3 7/91
C07D213/32

US Classification:

549/043000, 549/461000, 546/301000, 562/426000, 562/427000, 549/499000, 549/079000

Abstract:

Ar is optionally substituted with 1 to 3 Rgroups, and where n is 0, 1, 2 or 3; and a group of formula III: herein: Ris selected from hydrogen; and straight or branched alkyl; Ris selected from hydrogen; straight, branched, unsaturated or alicyclic alkyl, optionally substituted with 1 to 3 Rgroups, where the alkyl group is optionally interrupted by X, where X is selected from O, S, NH and N(COCH); allyloxy and 9-fluorenylmethyloxy; and (CH)Ar, where Ar is selected from phenyl, furanyl, thienyl, pyridyl, naphthyl, biphenyl, dibenzofuranyl, dibenzothienyl, fluorenyl and fluorenonyl, where n is 0, 1, 2 or 3, and where Ar is optionally substituted with 1 to 3 Rgroups; and Ris selected from OR, CN, C(O)NH, C(O)NHR, C(O)N(R), OC(O)NH, OC(O)R, CHO, SONH, SOR, CF, C(O)R, COOR, F, Cl, Br, I, OCHPh, NHR, N(R),, NHCOR, NHCOt-Bu, NHCOallyl, NH, and R, where R is hydrogen, Cto Calkyl, or aryl. The invention is further directed to a pharmaceutical composition containing the compound, as well as a method for treating bacterial infections in animals or humans, wherein the composition can be administered in combination with a -lactam antibiotic.

Author:

Mark Greenlee

ISBN #:

0198505825

Author:

Mark Greenlee

ISBN #:

0889370133

Author:

Mark Greenlee

ISBN #:

3814208749