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Last Updated: March 19, 2024

Details for Patent: 7,037,917


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Summary for Patent: 7,037,917
Title:HIV replication inhibiting pyrimidines
Abstract:This invention concerns the use of compounds of formula ##STR00001## the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a.sup.1=a.sup.2-a.sup.3=a.sup.4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R.sup.1 is hydrogen, aryl, formyl, C.sub.1-6alkylcarbonyl, C.sub.1-6alkyl, C.sub.1-6alkyloxycarbonyl, substituted C.sub.1-6alkyl, or substituted C.sub.1-6alkyloxyC.sub.1-6alkylcarbonyl; each R.sup.2 independently is hydroxy, halo, optionally substituted C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, C.sub.1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, --S(.dbd.O).sub.pR.sup.6, --NH--S(.dbd.O).sub.pR.sup.6, --C(.dbd.O)R.sup.6, --NHC(.dbd.O)H, --C(.dbd.O)NHNH.sub.2, --NHC(.dbd.O)R.sup.6, --C(.dbd.NH)R.sup.6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C.sub.1-10alkyl, C.sub.2-10alkenyl, C.sub.2-10alkynyl or C.sub.3-7cycloalkyl; or L is --X--R.sup.3 wherein R.sup.3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is --NR.sup.1--, --NH--NH--, --N.dbd.N--, --O--, --C(.dbd.O)--, --CHOH--, --S--, --S(.dbd.O)-- or --S(.dbd.O).sub.2--; Q is hydrogen, C.sub.1-6alkyl, halo, polyhalo-C.sub.1-6alkyl or an optionally substituted amino group; Y represents hydroxy, halo, C.sub.3-7cycloalkyl, optionally substituted C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl, C.sub.1-6alkyloxy, C.sub.1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, --S(.dbd.O).sub.pR.sup.6, --NH--S(.dbd.O).sub.pR.sup.6, --C(.dbd.O)R.sup.6, --NHC(.dbd.O)H, --C(.dbd.O)NHNH.sub.2, --NHC(.dbd.O)R.sup.6, --C(.dbd.NH)R.sup.6 or aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.
Inventor(s): De Corte; Bart (Southampton, PA), De Jonge; Marc Rene (Tilburg, NL), Heeres; Jan (Vosselaar, BE), Ho; Chih Yung (Lansdale, PA), Janssen; Paul Adriaan Jan (Vosselaar, BE), Kavash; Robert W. (Maple Glen, PA), Koymans; Lucien Maria Henricus (Turnhout, BE), Kukla; Michael Joseph (Maple Glen, PA), Ludovici; Donald William (Quakertown, PA), Van Aken; Koen Jeanne Alfons (Turnhout, BE)
Assignee: Janssen Pharmaceutica, N.V. (BE)
Application Number:10/634,682
Patent Claim Types:
see list of patent claims
Compound; Composition; Process; Use; Dosage form;

Drugs Protected by US Patent 7,037,917

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

Foreign Priority and PCT Information for Patent: 7,037,917

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
PCT/EP99/07417Sep 24, 1999

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