Steven D. Young - Lansdale PA Melissa Egbertson - Ambler PA Linda S. Payne - Lansdale PA John S. Wai - Harleysville PA Thorsten E. Fisher - Hatfield PA Mark W. Embrey - North Wales PA Lekhanh Tran - Norristown PA Linghang Zhuang - Conshohocken PA Joseph P. Vacca - Telford PA H. Marie Langford - Lansdale PA Jeffrey Melamed - Warminster PA Juan C. Jaen - Burlingame CA David L. Clark - Albany CA Julio C. Medina - Belmont CA
Assignee:
Merck Co., Inc. - Rahway NJ Tularik Inc. - S. San Francisco CA
Certain six-membered aromatic and heteroaromatic-dioxobutyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
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
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 ).
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.
Hydroxy Pyridopyrrolopyrazine Dione Compounds Useful As Hiv Integrase Inhibitors
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
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.
Aza- And Polyaza-Naphthalenyl Carboxamides Useful As Hiv Integrase Inhibitors
Neville Anthony - Hatfield PA, US Robert Gomez - Perkasie PA, US Steven Young - Lansdale PA, US Melissa Egbertson - Ambler PA, US John Wai - Harleysville PA, US Linghang Zhuang - Chalfont PA, US Mark Embrey - North Wales PA, US LeKhanh Tran - Norristown PA, US Jeffrey Melamed - Doylestown PA, US H. Langford - Lansdale NJ, US James Guare - Quakertown PA, US Thorsten Fisher - Hatfield PA, US Samson Jolly - Quakertown PA, US Michelle Kuo - Gwynedd Valley PA, US Debra Perlow - East Greenville PA, US Jennifer Bennett - East Norriton PA, US Timothy Funk - Ephrata PA, US
Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
1-(Aromatic- Or Heteroaromatic-Substituted)-3-(Heteroaromatic Substituted)-1,3-Propanediones And Uses Thereof
Linda Payne - Lansdale PA, US Lekhanh Tran - Norristown PA, US Linghang Zhuang - Chalfont PA, US Steven Young - Lansdale PA, US Melissa Egbertson - Ambler PA, US John Wai - Harleysville PA, US Mark Embrey - North Wales PA, US Thorsten Fisher - Hatfield PA, US James Guare - Quakertown PA, US H. Marie Langford - Lansdale PA, US Jeffrey Melamed - Warminster PA, US David Clark - Albany CA, US
Certain 1-(aromatic- or heteroaromatic-substituted-3-(heteroaromatic substituted)-1,3-propanediones are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
Aza- And Polyaza-Naphthalenyl Carboxamides Useful As Hiv Integrase Inhibitors
Neville Anthony - Hatfield PA, US Robert Gomez - Perkasie PA, US Steven Young - Lansdale PA, US Melissa Egbertson - Ambler PA, US John Wai - Harleysville PA, US Linghang Zhuang - Chalfont PA, US Mark Embrey - North Wales PA, US Lekhanh Tran - Norristown PA, US Jeffrey Melamed - Doylestown PA, US H. Langford - Lansdale NJ, US James Guare - Quakertown PA, US Thorsten Fisher - Hatfield PA, US Samson Jolly - Quakertown PA, US Michelle Kuo - Gwynedd Valley PA, US Debra Perlow - East Greenville PA, US Jennifer Bennett - East Norriton PA, US Timothy Funk - Ephrata PA, US
International Classification:
A61K031/498 A61K031/4745 C07D471/02 C07D487/02
US Classification:
514249000, 514300000, 544350000, 546123000
Abstract:
Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
Neville J. Anthony - Hatfield PA Samuel L. Graham - Schwenksville PA Lekhanh O. Tran - Norristown PA Ian M. Bell - Harleysville PA S. Jane deSolms - Norristown PA Robert P. Gomez - Perkasie PA Michelle Sparks Kuo - Gwynedd Valley PA William C. Lumma - Pennsburg PA Debra S. Perlow - East Greenville PA Anthony W. Shaw - Lansdale PA John S. Wai - Harleysville PA Steven D. Young - Lansdale PA
Assignee:
Merck & Co., Inc. - Rahway NJ
International Classification:
C07D40104 A61K 3144
US Classification:
514333
Abstract:
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.