US 7,125,879 B2
HIV inhibiting pyrimidines derivativesGeneral
US 7,125,879 B2
HIV inhibiting pyrimidines derivatives
Tech Center:
1600 Biotechnology and Organic Chemistry
Examiner:
Deepak Rao
Art Unit:
1624 Organic Chemistry
Agent:
Laura Donnelly
Inventors:
Jerome Emile Georges Guillemont; Patrice Palandjian; Marc Rene de Jonge; Lucien Maria Henricus Koymans; Hendrik Maarten Vinkers; Frederik Frans Desire Daeyaert; Jan Heeres; Koen Jeanne Alfons Van Aken; Paulus Joannes Lewi; Paul Adriaan Jan Janssen
Assignee:
JANSSEN-CILAG S.A.
Priority:
08/13/01
Filed:
08/09/02
Granted:
10/24/06
Expiration:
04/14/23
Abstract
This invention concerns HIV replication inhibitors of formula (I) the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing −a1=a2−a3=a4—and −b1=b2−b3=b4represents pheynl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl, substituted C1-6alkyl, C1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH?2?, —NHC(═O)R6, —C(═NH)R6 or a 5-membered hetrocycl; X1 is —NR5—, —NH—NH—, —N═N—, —O—, —C(═O)—, C1-4alkanediyl, —CHOH—, —S—, —S(═O)p—, —X2—C1-4alkanediyl- or —C1-4alkanediyl-X2—; R3 is NHR13, NR13R14; —C(═O)—NHR13; —C(═O)—NR13R14; —C(═O)—R15; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl; substituted C2-6alkynyl; substituted C2-6alkylenyl; C1-6alkyl substituted with hydroxy and a second substituent; —C(═N—O—R8)—C1-4alkyl; R7; or —X3—R7; R4 is halo, hydroxy, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxy, cyano, nitro, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyl, formyl, amino, mono- or di(C1-4alkyl) amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them
Cooperative Patent Classification (CPC)
C07C07C255/42C07D239/48C07CA61K31/5377A61P31/18A61K