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Details for Patent: 7,015,221

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Details for Patent: 7,015,221

Title:2,4-disubstituted triazine derivatives
Abstract: This invention concerns the use of the 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 or substituted C.sub.1-6alkyl; 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.4, --NH--S(.dbd.O).sub.pR.sup.4, --C(.dbd.O)R.sup.4, --NHC(.dbd.O)H, --C(.dbd.O)NHNH.sub.2, --NHC(.dbd.O)R.sup.4, --C(.dbd.NH)R.sup.4 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(=O)--, --CHOH--, --S--, --S(.dbd.O)-- or --S(.dbd.O).sub.2--; aryl is optionally substituted phenyl; 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 (CA Tilburg, NL), Heeres; Jan (Vosselaar, BE), Janssen; Paul Adriaan Jan (Vosselaar, BE), Kavash; Robert W. (Glenside, PA), Koymans; Lucien Maria Henricus (Retie, BE), Kukla; Michael Joseph (Maple Glen, PA), Ludovici; Donald William (Quakertown, PA), Van Aken; Koen Jeanne Alfons (Turnhout, BE)
Assignee: Janssen Pharmaceutica, N.V. (Beerse, BE)
Filing Date:Aug 27, 2003
Application Number:10/649,017
Claims:1. A compound of formula ##STR00011## or a N-oxide, a pharmaceutically acceptable 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 TABLE-US-00006 --CH.dbd.CH--C(R.sup.2a).dbd.CH--CH.dbd. (b-1); --N.dbd.CH--C(R.sup.2a).dbd.CH--CH.dbd. (b-2); --CH.dbd.N--C(R.sup.2a).dbd.CH--CH.dbd. (b-3); --N.dbd.CH--C(R.sup.2a).dbd.N--CH.dbd. (b-4); --N.dbd.CH--C(R.sup.2a).dbd.CH--N.dbd. (b-5); --CH.dbd.N--C(R.sup.2a).dbd.N--CH.dbd. (b-6); or --N.dbd.N--C(R.sup.2a).dbd.CH--CH.dbd. (b-7);

q is 0, 1, 2, 3 or 4; R.sup.1 is hydrogen, aryl, formyl, C.sub.1-6alkylcarbonyl, C.sub.1-6alkyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkyl substituted with formyl, C.sub.1-6alkylcarbonyl, or C.sub.1-6alkyloxycarbonyl; R.sup.2a is cyano; aminocarbonyl; mono- or di(methyl)aminocarbonyl; C.sub.1-6alkyl substituted with cyano, aminocarbonyl or mono- or di(methyl)aminocarbonyl; C.sub.2-6alkenyl substituted with cyano; or C.sub.2-6alkynyl substituted with cyano; each R.sup.2 independently is hydroxy, halo, C.sub.1-6alkyl optionally substituted with cyano or --C(.dbd.O)R.sup.4, C.sub.3-7cycloalkyl, C.sub.2-6alkenyl optionally substituted with one or more halogen atoms or cyano, C.sub.2-6alkynyl optionally substituted with one or more halogen atoms or cyano, 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.4, --NH--S(.dbd.O).sub.pR.sup.4, --C(.dbd.O)R.sup.4, --NHC(.dbd.O)H, --C(.dbd.O)NHNH.sub.2, --NHC(.dbd.O)R.sup.4, --C(.dbd.NH)R.sup.4 or a radical of formula ##STR00012## wherein each A independently is N, CH or CR.sup.4; B is NH, O, S or NR.sup.4; p is 1 or 2; and R.sup.4 is methyl, amino, mono- or dimethylamino or polyhalomethyl; L is C.sub.4-10alkyl, C.sub.2-10alkenyl, C.sub.2-10alkynyl, or C.sub.3-7cycloalkyl, whereby each of said aliphatic groups is optionally substituted with one or two substituents independently selected from (i) C.sub.3-7cycloalkyl, (ii) indolyl or isoindolyl, each optionally substituted with one, two, three or four substituents each independently selected from halo, C.sub.1-6alkyl, hydroxy, C.sub.1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, polyhalomethyl, polyhalomethyloxy or C.sub.1-6alkylcarbonyl, (iii) phenyl, pyridinyl, pyrimidinyl pyrazinyl or pyridazinyl, wherein each of said aromatic rings is optionally substituted with one, two, three, four or five substituents each independently selected from the substituents defined in R.sup.2; or L is --X--R.sup.3 wherein R.sup.3 is phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl, wherein each of said aromatic rings is optionally substituted with two, three, four or five substituents each independently selected from the substituents defined in R.sup.2; and 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--; aryl is phenyl or phenyl substituted with one, two, three, four or five substituents each independently selected from halo, C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, cyano, nitro, polyhaloC.sub.1-6alkyl or polyhaloC.sub.1-6alkyloxy.

2. A compound as claimed in claim 1 wherein L is --X--R.sup.3, --X-- is --O-- or --NH-- and R.sup.3 is phenyl substituted with two or three substituents each independently selected from chloro, bromo, cyano or methyl.

3. A compound as claimed in claim 1 wherein R.sup.2a is cyano, aminocarbonyl, mono- or di(methyl)aminocarbonyl, C.sub.1-6alkyl substituted with cyano, aminocarbonyl or mono- or di(methyl)aminocarbonyl.

4. A method of treating a subject suffering from Human Immunodeficiency Virus (HIV) infection, comprising administering a therapeutically effective amount of a compound of claim 1 to said subject.

5. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of compound as claimed in claim 1.

6. A process for preparing a pharmaceutical composition as claimed in claim 5 comprising mixing a therapeutically effective amount of said compound with a pharmaceutically acceptable carrier.

7. The combination of a compound as defined in claim 1 and another antiretroviral compound.

8. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and as active ingredients (a) a compound as defined in claim 1, and (b) another antiretroviral compound.

9. The method of claim 4 further comprising administering a therapeutically effective amount of another antiretroviral compound to said subject.

10. The method of claim 9 wherein said compound and said another antiretroviral compound are administered simultaneously, separately, or sequentially to said subject.
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