C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 405/12 (2006.01) A61K 31/35 (2006.01) A61K 31/44 (2006.01) A61K 31/4433 (2006.01) A61K 31/4436 (2006.01) A61P 31/18 (2006.01) C07C 43/23 (2006.01) C07C 245/18 (2006.01) C07D 307/93 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 407/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 487/00 (2006.01)
Patent
CA 2438524
Compounds of Formula (I), where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1- C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is -(CHR8)n--D-(CHR8)m-; D is -NR9-, -O-, -S-, -S(=O)- or -S(=O)2-; R8 is independently H, C1-C3 alkyl, halo substitutedC1-C3alkyl;R9 is H, C1-C3 alkyl; n and m are independently 0, 1 or 2; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.
L'invention concerne les composés représentés par la formule (I), dans laquelle; R¿1? est O, S; R¿2? est un hétérocycle contenant de l'azote éventuellement substitué, l'azote étant placé en position 2 par rapport à la liaison (thio)urée; R¿3? est H, alkyle C¿1?-C¿3?, R¿4?-R¿7? sont choisis indépendamment parmi H, alkyle C¿1?-C¿6?, alcényle C¿2?-C¿6?, alcynyle C¿2?-C¿6?, halo-alkyle C¿1?-C¿6?, alcanoyle C¿1?-C¿6?, halo-alcanoyle C¿1?-C¿6?, alcoxy C¿1?-C¿6?, halo-alcoxy C¿1?-C¿6?, alkyloxy C¿1?-C¿6? alkyle C¿1?-C¿6?, halo-alkyloxy C¿1?-C¿6? alkyle C¿1?-C¿6? hydroxy-alkyle C¿1?-C¿6?, amino-alkyle C¿1?-C¿6?, carboxy-alkyle C¿1?-C¿6?, cyano-alykle C¿1?-C¿6?, amino, carboxy, carbamoyle, cyano, halo, hydroxy, céto; X est -(CHR¿8?)¿n-?-D-(CHR¿8?)¿m?-; D est -NR¿9?-, -O-, -S-, -S(=O)- ou -S(=O)2-; R¿8? est indépendamment H, alkyle C¿1?-C¿3?, halo alkyle C¿1?-C¿3? substitué; R¿9? est H, alkyle C¿1?-C¿3?; n et m sont indépendamment 0, 1 ou 2; ainsi que des promédicaments et des sels pharmaceutiquement acceptables de ceux-ci. Ces composés sont utiles en tant qu'inhibiteurs de la transcriptase inverse de HIV-1, en particulier des mutants pharmacorésistants.
Kalyanov Genaidy
Lindstroem Stefan
Naeslund Lotta
Oden Lourdes Salvador
Sahlberg Christer
Gowling Lafleur Henderson Llp
Medivir Ab
LandOfFree
Cyclopropaheterocycles as non-nucleoside reverse... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Cyclopropaheterocycles as non-nucleoside reverse..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Cyclopropaheterocycles as non-nucleoside reverse... will most certainly appreciate the feedback.
Profile ID: LFCA-PAI-O-1626375