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Claims for Patent: 7,125,879

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Claims for Patent: 7,125,879

Title:HIV inhibiting pyrimidines derivatives
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 -a.sup.1=a.sup.2-a.sup.3=a.sup.4--and -b.sup.1=b.sup.2-b.sup.3=b.sup.4represents pheynl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sup.1-6alkyl; C.sub.1-6alkyloxycarbonyl, substituted C.sub.1-6alkyl, C.sub.1-6alkylcarbonyl; R.sup.2 is hydroxy, halo, optionally substituted C.sub.1-6alkyl, C.sub.3-7cycloalkyl, optionally substituted C.sub.2-6alkenyl, optionally substituted 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?2?, --NHC(.dbd.O)R.sup.6, --C(.dbd.NH)R.sup.6 or a 5-membered hetrocycl; X.sub.1 is --NR.sup.5--, --NH--NH--, --N.dbd.N--, --O--, --C(.dbd.O)--, C.sub.1-4alkanediyl, --CHOH--, --S--, --S(.dbd.O).sub.p--, --X.sub.2--C.sub.1-4alkanediyl- or --C.sub.1-4alkanediyl-X.sub.2--; R.sup.3 is NHR.sup.13, NR.sup.13R.sup.14; --C(.dbd.O)--NHR.sup.13; --C(.dbd.O)--NR.sup.13R.sup.14; --C(.dbd.O)--R.sup.15; --CH.dbd.N--NH--C(.dbd.O)--R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl; substituted C.sub.2-6alkynyl; substituted C.sub.2-6alkylenyl; C.sub.1-6alkyl substituted with hydroxy and a second substituent; --C(.dbd.N--O--R.sup.8)--C.sub.1-4alkyl; R.sup.7; or --X.sub.3--R.sup.7; R.sup.4 is halo, hydroxy, C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, cyano, nitro, polyhaloC.sub.1-6alkyl, polyhaloC.sub.1-6alkyloxy, aminocarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyl, formyl, amino, mono- or di(C.sub.1-4alkyl) amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them ##STR00001##
Inventor(s): Guillemont; Jeo (Ande, FR), Palandjian; Patrice (Louviers, FR), de Jonge; Marc Rene (Tilburg, NL), Koymans; Lucien Maria Henricus (Retie, BE), Vinkers; Hendrik Maarten (Antwerp, BE), Daeyaert; Frederik Frans Desire (Beerse, BE), Heeres; Jan (Vosselaar, BE), Van Aken; Koen Jeanne Alfons (Kortrijk, BE), Lewi; Paulus Joannes (Turnhout, BE), Arts, legal representative; Frank Xavier Josef Herwig (Beerse, BE), Janssen, deceased; Paul Adriaan Jan (Turnhout, BE)
Assignee: Janssen Pharmaceutica N.V. (Beerse, BE)
Application Number:10/485,636
Patent Claims: 1. A compound 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]- benzonitrile, an N-oxide, an addition salt, a quaternary amine or a stereochemically isomeric form thereof, said compound having the following structure: ##STR00253##

2. A compound 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]- benzonitrile, said compound having the following structure: ##STR00254##

3. A compound having the following structure: ##STR00255##

4. A compound having the following structure: ##STR00256##

5. A compound as claimed in claim 1, wherein the compound is an addition salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidiny- l]amino]benzonitrile.

6. A compound as claimed in claim 1, wherein the compound is an addition salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidiny- l]amino]benzonitrile (E).

7. A compound as claimed in claim 5, wherein the addition salt is the hydrochloride salt.

8. A compound as claimed in claim 6, wherein the additional salt is the hydrochloride salt.

9. A compound as claimed in claim 1, wherein the compound is an N-oxide of 4-[[4-[[4-(2cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amin- o]benzonitrile.

10. A compound as claimed in claim 1, wherein the compound is an N-oxide of 4-[[4-[[4-(2cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amin- o]benzonitrile (E).

11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and an effective amount of a compound according to any of claims 1, 2, 3, 10, 8.

12. A process for preparing a pharmaceutical composition, comprising mixing a therapeutically effective amount of a compound as claimed in any one of claims 1,2,3,10,8 with a pharmaceutically acceptable carrier.

13. A method of treating subjects suffering from HIV (Human Immunodeficiency Virus) infection comprising administering to the subject an effective amount of a compound according to any one of claims 1,2,3,10,8.

14. A pharmaceutical composition as claimed in claim 11, wherein the pharmaceutical composition is a tablet.

15. A pharmaceutical composition as claimed in claim 11, wherein the effective amount is between 1 to 1000 mg of active ingredient per unit dosage form.

16. A pharmaceutical composition as claimed in claim 11, wherein the effective amount is between 5 and 200 mg of active ingredient per unit dosage form.

17. A tablet as claimed in claim 14, wherein the effective amount is between 1 to 1000 mg of active ingredient.

18. A tablet asclaimed in claim 14, wherein the effective amount is between 5 to 200 mg of active ingredient.

19. A method of treating subjects suffering from HIV-1 (Human Immunodeficiency Virus) infection that have acquired resistance to art-known non-nucleoside reverse transcriptase inhibitors comprising administering to the subject an effective amount of a compound according to any of claims 1, 2, 3, 10, 8.
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