US2014296228A1PendingUtilityA1
Inhibitors of human immunodeficiency virus replication
Est. expiryNov 16, 2027(~1.4 yrs left)· nominal 20-yr term from priority
Inventors:Youla S. TsantrizosMurray D. BaileyFrancois BilodeauRene CoulombeTeddy HalmosStephen KawaiSerge R. LandrySteven LaplanteSebastien MorinMarc-Andre PoupartBruno SimoneauLee FaderRebekah J. CarsonMathieu Parisien
A61P 31/12A61P 43/00A61P 31/18C07D 405/04C07D 221/16A61K 31/5383C07D 215/18C07D 491/06C07D 413/04C07D 498/06C07D 409/04A61K 31/538A61K 31/47A61K 31/4709C07D 215/14A61K 31/473C07D 417/04C07D 401/04A61K 31/4741
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Claims
Abstract
Compounds of formula I: wherein R 4 , R 6 and R 7 are defined herein, are useful as inhibitors of HIV replication.
Claims
exact text as granted — not AI-modified1 - 38 . (canceled)
39 . A method of treating an HIV infection in a mammal having or at risk of having the infection, the method comprising administering to the mammal a therapeutically effective amount of a combination of a compound of formula (I):
or a pharmaceutically acceptable salt thereof,
wherein:
R 4 is Het, wherein Het is optionally substituted with 1 to 3 substituents each independently selected from halo, (C 1-6 )alkyl, (C 2-6 )alkenyl, (C 1-6 )haloalkyl, (C 3-7 )cycloalkyl, —OH, —O(C 1-6 )alkyl, —SH, —S(C 1-6 )alkyl, —NH 2 , —NH(C 1-6 )alkyl and —N((C 1-6 )alkyl) 2 , wherein (C 1-6 )alkyl is optionally substituted with hydroxy, cyano or oxo;
R 6 and R 7 are each independently selected from H, halo, (C 1-6 )alkyl and (C 1-6 )haloalkyl; and
Het is a 4- to 7-membered saturated, unsaturated or aromatic heterocycle having 1 to 4 heteroatoms each independently selected from O, N and S, or a 7- to 14-membered saturated, unsaturated or aromatic heteropolycycle having wherever possible 1 to 5 heteroatoms, each independently selected from O, N and S;
or a salt thereof; and
at least one other antiviral agent.
40 . The method according to claim 39 wherein R 4 is Het optionally substituted with 1 to 2 substituents each independently selected from halo, (C 1-3 )alkyl and —O(C 1-3 )alkyl.
41 . The method according to claim 40 wherein R 4 is Het optionally substituted with 1 to 2 substituents each independently selected from Cl, F, CH 3 and CH 2 CH 3 wherein Het is a 7- to 14-membered saturated, unsaturated or aromatic heteropolycycle having wherever possible 1 to 2 heteroatoms, each independently selected from O, N and S.
42 . The method according to claim 39 wherein R 4 is selected from:
optionally substituted with 1 to 3 substituents each independently selected from halo, (C 1-3 )alkyl and —O(C 1-3 )alkyl.
43 . The method according to claim 42 wherein R 4 is selected from:
optionally substituted with 1 to 2 substituents each independently selected from halo, (C 1-3 )alkyl and —O(C 1-3 )alkyl.
44 . The method according to claim 39 wherein R 6 is H, F, Cl or (C 1-2 )alkyl.
45 . The method according to claim 44 wherein R 6 is H or CH 3 .
46 . The method according to claim 39 wherein R 7 is H, F, Cl or CH 3 .
47 . The method according to claim 46 wherein R 7 is H or CH 3 .
48 . The method according to claim 39 wherein the compound of formula (I) has following formula:
wherein R 4 , R 6 and R 7 are defined as:
R 4
R 6
R 7
H
H.
49 . The method according to claim 39 wherein the at least one other antiviral agent comprises at least one NNRTI.
50 . The method according to claim 39 wherein the at least one other antiviral agent comprises at least one NRTI.
51 . The method according to claim 39 wherein the at least one other antiviral agent comprises at least one protease inhibitor.
52 . The method according to claim 39 wherein the at least one other antiviral agent comprises at least one entry inhibitor.
53 . The method according to claim 39 wherein the at least one other antiviral agent comprises at least one integrase inhibitor.Cited by (0)
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