Publication number: 20040198739
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=b4- represents 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—,
Type:
Application
Filed:
February 3, 2004
Publication date:
October 7, 2004
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
Publication number: 20040116431
Abstract: The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pyl
Type:
Application
Filed:
December 10, 2003
Publication date:
June 17, 2004
Applicant:
NitroMed, Inc.
Inventors:
Subhash P. Khanapure, David S. Garvey, Richard A. Earl, Maiko Ezawa, Xinqin Fang, Ricky D. Gaston