Kevin G Gilbert

US Patent:

6387893, May 14, 2002

Filed:

Sep 27, 2000

Appl. No.:

09/671520

Inventors:

Ben E. Evans - Lansdale PA
Jacob M. Hoffman - Lansdale PA
Kevin F. Gilbert - Barto PA
Kenneth E. Rittle - Green Lane PA

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

A61K 3155

US Classification:

51421202, 51421103, 51421104, 51421204, 5142245, 514267, 514278, 540485, 540495, 540543, 540547, 544249, 544315, 544318

Abstract:

Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

US Patent:

8461107, Jun 11, 2013

Filed:

Apr 16, 2009

Appl. No.:

12/989672

Inventors:

Nigel J. Liverton - Harleysville PA, US
John A. McCauley - Maple Glen PA, US
John W. Butcher - Telford PA, US
Kevin F. Gilbert - Barto PA, US
Charles J. McIntyre - Lansdale PA, US
Michael T. Rudd - Collegeville PA, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

A61K 38/00

US Classification:

514 37

Abstract:

The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

US Patent:

20100099695, Apr 22, 2010

Filed:

Oct 23, 2007

Appl. No.:

12/447342

Inventors:

Nigel J. Liverton - Harleysville PA, US
Vincenzo Summa - Rome, IT
Maria Emilia Di Francesco - Rome, IT
Marco Ferrara - Rome, IT
Kevin F. Gilbert - Barto PA, US
Steven Harper - Rome, IT
John A. McCauley - Maple Glen PA, US
Charles A. McIntyre - Lansdale PA, US
Alessia Petrocchi - Rome, IT
Marco Pompei - Rome, IT
Joseph J. Romano - Rome, IT
Michael T. Rudd - Collegeville PA, US
John W. Butcher - Telford PA, US
M. Katharine Holloway - Lansdale PA, US

International Classification:

A61K 31/439
C07D 513/18
C07D 513/08
A61K 31/407
A61K 31/4748
A61P 31/12

US Classification:

514281, 540456, 514293, 514411, 514286

Abstract:

The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

US Patent:

20130178413, Jul 11, 2013

Filed:

Sep 16, 2011

Appl. No.:

13/825245

Inventors:

John A. McCauley - Maple Glen PA, US
Nigel J. Liverton - Harleysville PA, US
Michael T. Rudd - Collegeville PA, US
Kevin F. Gilbert - Barto PA, US
Marco Ferrara - Milanese, IT
Vincenzo Summa - Roma, IT
Benedetta Crescenzi - Paris, FR

International Classification:

A61K 38/07
C07K 5/103
A61K 45/06
C07K 5/107

US Classification:

514 43, 530330

Abstract:

The present invention relates to macrocyclic compounds of formula I that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

US Patent:

54647886, Nov 7, 1995

Filed:

Mar 24, 1994

Appl. No.:

8/217270

Inventors:

Mark G. Bock - Hatfield PA
Ben E. Evans - Lansdale PA
J. Christopher Culberson - Hatfield PA
Kevin F. Gilbert - Bechtelsville PA
Kenneth E. Rittle - Green Lane PA
Peter D. Williams - Harleysville PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D27300
C07D41300
C07D45100

US Classification:

514252

Abstract:

Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO. sub. 2 --, --(CH. sub. 2). sub. p -- or --CO--(CH. sub. 2). sub. p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R. sup. 5, R. sup. 6 or R. sup. 7 ; R. sup. 1 is hydrogen, cyano, phenyl,--CONHR. sup. 2, --CONR. sup. 2 R. sup. 2, --(CH. sub. 2). sub. m --OR. sup. 2, --(CH. sub. 2). sub. p --S(O). sub. r --R. sup. 2, --(CH. sub. 2). sub. m --CO. sub. 2 R. sup. 2, --(CH. sub. 2). sub. m --N. sub. 3, --(CH. sub. 2). sub. m --NH. sub. 2 or --(CH. sub. 2). sub. m --NR. sup. 2 R. sup. 2 ; R. sup. 2 is hydrogen, C. sub. 3-8 cycloalkyl or C. sub. 1-5 alkyl; R. sup. 5 and R. sup. 6 are each independently selected from hydrogen, C. sub.

US Patent:

57565040, May 26, 1998

Filed:

Sep 23, 1996

Appl. No.:

8/718415

Inventors:

Mark G. Bock - Hatfield PA
Ben E. Evans - Lansdale PA
J. Christopher Culberson - Hatfield PA
Kevin F. Gilbert - Bechtelsville PA
Kenneth E. Rittle - Green Lane PA
Peter D. Williams - Harleysville PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31495
C07D24104
C07D40112
C07D40312

US Classification:

514252

Abstract:

Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO. sub. 2 --, --(CH. sub. 2). sub. p -- or --CO--(CH. sub. 2). sub. p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R. sup. 5, R. sup. 6 or R. sup. 7 ; R. sup. 1 is hydrogen, cyano, phenyl, --CONHR. sup. 2, --CONR. sup. 2 R. sup. 2, --(CH. sub. 2). sub. m --OR. sup. 2, --(CH. sub. 2). sub. p --S(O). sub. r --R. sup. 2, --(CH. sub. 2). sub. m --CO. sub. 2 R. sup. 2, --(CH. sub. 2). sub. m --N. sub. 3, --(CH. sub. 2). sub. m --NH. sub. 2 or --(CH. sub. 2). sub. m --NR. sup. 2 R. sup. 2 ; R. sup. 2 is hydrogen, C. sub. 3-8 cycloalkyl or C. sub. 1-5 alkyl; R. sup. 5 and R. sup. 6 are each independently selected from hydrogen, C. sub.

US Patent:

52043495, Apr 20, 1993

Filed:

Sep 16, 1991

Appl. No.:

7/760284

Inventors:

Mark G. Bock - Hatfield PA
Ben E. Evans - Lansdale PA
Roger M. Freidinger - Lansdale PA
Kevin Gilbert - Bechtelsville PA
Doug W. Hobbs - Lansdale PA
James B. Hoffman - King of Prussia PA
George F. Lundell - Blue Bell PA
Douglas J. Pettibone - Chalfont PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31495
C07D47100
C07D40112

US Classification:

514253

Abstract:

Compounds of the formula: ##STR1## where R. sup. 1 is hydrogen or hydroxy and R. sup. 2 is a substituted amino group, a substituted heterocyclic ring or a substituted alkyl. These compounds are oxytocin and vasopressin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery, timing of parturition, uterine hyperactivity, endometriosis, hypertension, congestive heart failure, hyponatremia and cognitive disorders. Also disclosed are pharmaceutical compositions containing these compounds, methods of their use and methods of their preparation.

US Patent:

63263726, Dec 4, 2001

Filed:

Sep 27, 2000

Appl. No.:

9/671407

Inventors:

Ben E. Evans - Lansdale PA
Kevin F. Gilbert - Barto PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D23982
C07D48722
C07D48714
A61K 31517
A61K 31519

US Classification:

514258

Abstract:

Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.