Terry Alan Lyle

US Patent:

6376499, Apr 23, 2002

Filed:

Oct 28, 1999

Appl. No.:

09/428314

Inventors:

Philip E. Sanderson - Philadelphia PA
Terry Lyle - Lederach PA
Bruce Dorsey - Maple Glen PA
Matthew G. Stanton - Lansdale PA

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

A61K 31497

US Classification:

51425505, 544405

Abstract:

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is N Y or O; c is CY or N; d is CY ; e is CY or N; f is CY or N; g is CY or N; Y is hydrogen, C alkyl, or halogen; Y is hydrogen, C alkyl, C cycloalkyl, halogen, NH , OH or C alkoxy; A is âand W, X, Z, R , R and R are defined in the specification.

US Patent:

6455532, Sep 24, 2002

Filed:

Jun 1, 2000

Appl. No.:

09/585112

Inventors:

Christopher S. Burgey - Plymouth Meeting PA
Kyle A. Robinson - Elkins Park PA
Peter D. Williams - Harleysville PA
Craig Coburn - Royersford PA
Terry A. Lyle - Lederach PA
Philip E. Sanderson - Philadelphia PA

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

A61K 31497

US Classification:

51425502, 544405

Abstract:

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: A is âwherein Y and Y are independently hydrogen, C alkyl, C alkoxy, F H C(CH ) Oâ, wherein u and v are either 1 or 2, provided that when u is 1, v is 2, and when u is 2, v is 1, C cycloalkyl, thio C alkyl, C sulfinylalkyl, C sulfonylalkyl, halogen cyano, or trifluoromethyl, and wherein b is 0 or 1.

US Patent:

6515011, Feb 4, 2003

Filed:

Dec 18, 2001

Appl. No.:

10/023776

Inventors:

Harold G. Selnick - Ambler PA
James C. Barrow - Harleysville PA
Philippe G. Nantermet - Lansdale PA
Peter D. Williams - Harleysville PA
Kenneth J. Stauffer - Souderton PA
Philip E. Sanderson - Philadelphia PA
Kenneth E. Rittle - Green Lane PA
Matthew M. Morrissette - Pottstown PA
Catherine M. Wiscount - Allentown PA
Lekhanh O. Tran - Norristown PA
Terry A. Lyle - Lederach PA
Donnette D. Staas - Harleysville PA

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

A61K 3140

US Classification:

514423, 548538, 548528, 548518, 546111, 5462791, 514422, 514343, 514290

Abstract:

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e. g. where R is âCH NH , âCH CH NH , or âCH NHC(O)OC(CH ).

US Patent:

6528503, Mar 4, 2003

Filed:

Jun 14, 2002

Appl. No.:

10/171708

Inventors:

Peter D. Williams - Harleysville PA
Terry A. Lyle - Lederach PA
Matthew M. Morrissette - Pottstown PA
Lekhanh O. Tran - Norristown PA
Donnette D. Staas - Harleysville PA

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

A61K 31397

US Classification:

514210, 548953, 5462681, 514340

Abstract:

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e. g. 1-(3(S)-Cyclopropyl-2(R)-hydroxybutanoyl)azetidine-2(S)-N-(2-aminomethyl-5-chlorobenzyl)carboxamide, and 1-(3-Cyclopropyl-3-methyl-2(R)-hydroxybutanoyl)azetidine-2(S)-N-(2-aminomethyl-5-chlorobenzyl)carboxamide.

US Patent:

6610692, Aug 26, 2003

Filed:

Oct 28, 1999

Appl. No.:

09/429741

Inventors:

Philip E. Sanderson - Philadelphia PA
Bruce D. Dorsey - Maple Glen PA
Terry A. Lyle - Lederach PA
Matthew G. Stanton - North Wales PA
Donnette Staas - Lansdale PA
Craig Coburn - Skippack PA
Matthew M. Morrissette - Pottstown PA

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

A61K 31497

US Classification:

514248, 544405, 544236, 51425505, 514300, 514303, 514337, 514338, 514339, 546113, 546117, 546118, 546119, 546122, 5462684, 5462721, 5462734, 5462757, 5462771, 5462774

Abstract:

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is NY or O; c is CY or N; d is CY or N; e is CY or N; f is CY or N; g is CY or N; Y , Y , and Y are independently hydrogen, C alkyl, or halogen; Y and Y are independently hydrogen, C alkyl, C cycloalkyl, halogen, NH , OH or C alkoxy, and Y is hydrogen, C alkyl, C cycloalkyl, halogen, âCN, NH , OH or C alkoxy; A is and W, W , R , R , R , R , X and Z are defined in the specification.

US Patent:

7144899, Dec 5, 2006

Filed:

Feb 5, 2002

Appl. No.:

10/467439

Inventors:

Harold G. Selnick - Ambler PA, US
Mary Beth Young - Lansdale PA, US
Philippe G. Nantermet - Lansdale PA, US
James C. Barrow - Harleysville PA, US
Peter D. Williams - Harleysville PA, US
Terry A. Lyle - Lederach PA, US
Donnette D. Staas - Harleysville PA, US
Kenneth J. Stauffer - Souderton PA, US
Philip E. Sanderson - Philadelphia PA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31/4439
C07D 401/12

US Classification:

514340, 514361, 5462687, 5462691, 548127, 548131, 548134

Abstract:

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure Formula (I): wherein u is CH or N; Q is 1)—N(R)CH(R)— wherein the nitrogen atom is attached to R, and Rand Rare independently selected from the group consisting of hydrogen, Ccycloalkyl, and Calkyl, or 2) wherein the nitrogen atom is attached to R, and m is 0, 1, or 2.

US Patent:

7435735, Oct 14, 2008

Filed:

Oct 18, 2004

Appl. No.:

10/576328

Inventors:

John S. Wai - Harleysville PA, US
Thorsten E. Fisher - Hatfield PA, US
Linghang Zhuang - Chalfont PA, US
Donnette D. Staas - Harleysville PA, US
Terry A. Lyle - Lederach PA, US
Boyoung Kim - Lansdale PA, US
Mark W. Embrey - North Wales PA, US
Catherine M. Wiscount - Allentown PA, US
Lekhanh O. Tran - Norristown PA, US
Melissa Egbertson - Ambler PA, US
Kelly L. Savage - Schwenksville PA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A01N 43/58
A01N 43/60
A61K 31/50
A61K 31/495
C07D 471/00
C07D 487/00
C07D 241/36

US Classification:

514250, 544345

Abstract:

Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, R, R, R, R, R, R, Rand Rare 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:

7538112, May 26, 2009

Filed:

May 3, 2005

Appl. No.:

11/579772

Inventors:

John S. Wai - Harleysville PA, US
Joseph P. Vacca - Telford PA, US
Linghang Zhuang - Chalfont PA, US
Boyoung Kim - Lansdale PA, US
Terry A. Lyle - Lederach PA, US
Catherine M. Wiscount - Allentown PA, US
Melissa S. Egbertson - Ambler PA, US
Lou Anne Neilson - Sellersville PA, US
Mark Embrey - Harleysville PA, US
Thorsten E. Fisher - Hatfield PA, US
Donnette D. Staas - Harleysville PA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D 487/14
A61K 31/5025
A61K 31/4985

US Classification:

514250, 544234

Abstract:

Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R, R, R, R, R, Rand Rare 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.