.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 6,878,717

« Back to Dashboard

Claims for Patent: 6,878,717

Title: HIV replication inhibiting pyrimidines
Abstract:This invention concerns the use of compounds of formula: ##STR1## 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.1-6 alkylcarbonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy-carbonyl, substituted C.sub.1-6 alkyl, or substituted C.sub.1-6 alkyloxyC.sub.1-6 alkylcarbonyl; each R.sup.2 independently is hydroxy, halo, optionally substituted C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-methylthio, --S(.dbd.O).sub.p R.sup.6, --NH--S(.dbd.O).sub.p R.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.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl or C.sub.3-7 cycloalkyl; 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.1-6 alkyl, halo, polyhalo-C.sub.1-6 alkyl or an optionally substituted amino group; Y represents hydroxy, halo, C.sub.3-7 cycloalkyl, optionally substituted C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, --S(.dbd.O).sub.p R.sup.6, --NH--S(.dbd.O).sub.p R.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 (5045 CA Tilburg, NL), Heeres; Jan (Vosselaar, BE), Ho; Chih Yung (Lansdale, PA), Janssen; Paul Adriaan Jan (B2350 Vosselaar, BE), Kavash; Robert W. (Maple Glen, PA), Koymans; Lucien Maria Henricus (B-2300 Turnhout, BE), Kukla; Michael Joseph (Maple Glen, PA), Ludovici; Donald William (Quakertown, PA), Van Aken; Koen Jeanne Alfons (B-2300 Turnhout, BE)
Assignee:
Application Number:09/430,966
Patent Claims: 1. A method of treating subjects suffering from HIV (Human Immunodeficiency Virus) infection comprising administering to the subject a therapeutically effective amount of a compound of formula: ##STR32##

a N-oxide, a pharmaceutically acceptable addition salt, or a stereochemically isomeric form thereof, wherein -a.sup.1 =a.sup.2 -a.sup.3 =a.sup.4 - represents a bivalent radical of formula:

2. The method of claim 1, wherein R.sup.1 is hydrogen, aryl, formyl, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonyl, C.sub.1-6 alkyl substituted with formyl, C.sub.1-6 alkylcarbonyl, or C.sub.1-6 alkyloxycarbonyl.

3. A method of treating non-nucleoside reverse transcriptase inhibitor resistant HIV infection in a subject in need thereof comprising administering to the subject an effective amount of a compound having the formula: ##STR34##

a N-oxide, an addition salt, or a stereochemically isomeric form thereof, wherein -b.sup.1 =b.sup.2 -C(R.sup.2a)=b.sup.3 -b.sup.4 = represents a bivalent radical of formula:

4. A method of treating non-nucleoside reverse transcriptase inhibitor resistant HIV-1 infection in a subject in need thereof comprising administering to the subject an effective amount of a compound having the formula: ##STR36##

a N-oxide, an addition salt, or a stereochemically isomeric form thereof, wherein -b.sup.1 =b.sup.2 -C(R.sup.2a)=b.sup.3 -b.sup.4 = represents a bivalent radical of formula:

5. A method of treating subjects suffering from HIV (Human Immunodeficiency Virus) infection comprising administering to the subject a therapeutically effective amount of a compound of formula: ##STR38##

a N-oxide, an addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein -b.sup.1 =b.sup.2 -C(R.sup.2a)=b.sup.3 -b.sup.4 = represents a bivalent radical of formula:
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc