RATE-CONTROLLED PARTICLES

1 . (canceled)

2 . Particles according to claim 16 , wherein the copolymer of N-vinylpyrrolidone is a copolymer with vinyl acetate.

3 . Particles according to claim 16 , further comprising a surfactant.

4 . Particles according to claim 3 , wherein the surfactant is a PEG-n-hydrogenated castor oil.

5 . Particles according to claim 16 , wherein the surfactant is a low molecular weight poly-oxyethylene polyoxypropylene block copolymer.

6 . Particles according to claim 16 , further comprising citric acid in amounts of up to 5% b.w.

7 . Particles according to claim 16 , wherein the home- or copolymer of N-vinylpyrrolidone is used in amounts of from 40 to 70% b.w. of the total weight of the dosage form.

8 . Particles according to claim 7 , wherein the homo- or copolymer of N-vinylpyrrolidone is used in amounts of from 50 to 65% b.w.

9 . Particles according to claim 16 , wherein the controlled release is an instant release of the drug.

10 . Particles according to a claim 16 , wherein the controlled release is a sustained release.

11 . Particles according to claim 10 , further comprising hydroxypropyl methyl cellulose in amounts of from 5 to 10% b.w.

12 . Particles according to claim 16 , obtained by forming a homogeneous mixture of the components in the form of a melt, extruding said mixture and shaping of the extrudate.

13 . Particles according to claim 16 , comprising a compound selected from the group consisting of

4-[[4-amino-5-chloro-6-[(2,4,6-trimethylphenyl)amino]-2-pyrimidinyl]-amino]benzonitrile;

4-[[5-chloro-4-[(2,4,6-trimethylphenyl)amino]-2-pyrimidinyl]amino]benzonitrile;

4-[[5-bromo-4-(4-cyano-2,6-dimethylphenoxy)-2-pyrimidin]amino]-benzonitrile;

4-[[4-amino-5-chloro-6-[(4-cyano-2,6-dimethylphenyl)amino]-2-pyrimidinyl]amino]benzonitrile;

4-[[5-bromo-6-[(4-cyano-2,6-dimethylphenyl)amino]-2-pyrimidinyl]-amino]benzonitrile;

4-[[4-amino-5-chloro-6-[(4-cyano-2,6-dimethylphenoxy)-2-pyrimidinyl]amino]benzonitrile;

4-[[4-amino-5-bromo-6-(4-cyano-2,6-dimethylphenyloxy)-2-pyrimidinyl]amino]benzonitrile;

a N-oxide, a pharmaceutically acceptable addition salt or a stereochemically isomeric form thereof.

14 . Pharmaceutical dosage form, comprising particles according to claim 16 .

15 . Pharmaceutical dosage forms according to claim 14 , further comprising one or more pharmaceutically acceptable excipients

16 . Rate-controlled release particles, comprising a compound of formula II

an N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein

-b 1 =b 2 -C(R 2a )=b 3 -b 4 =represents a bivalent radical of formula

—CH═CH—C(R 2a )═CH—CH═  (b-1);

—N═CH—C(R 2a )═CH—CH═  (b-2);

—CH═N—C(R 2a )═CH—CH═  (b-3);

—N═CH—C(R 2a )═N—CH═  (b-4);

—N═CH—C(R 2a )═CH—N═  (b-5);

—CH═N-c(R 2a )═N—CH═  (b-6);

—N═N—C(R 2a )═CH—CH═  (b-7);

q is 0, 1, 2; or where possible q is 3 or 4;

R 1 is hydrogen, aryl, formyl, C 1-6 alkylcarbonyl, C 1-6 alkyl, C 1-6 alkyloxycarbonyl, C 1-6 alkyl substituted with formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl;

R 2a is cyano, aminocarbonyl, mono- or di(methyl)aminocarbonyl, C 1-6 alkyl substituted with cyano, aminocarbonyl or mono- or di(methyl)aminocarbonyl, C 2-6 alkenyl substituted with cyano, or C 2-6 alkynyl substituted with cyano;

each R 2 independently is hydroxy, halo, C 1-6 alkyl optionally substituted with cyano or —C(═O)R 6 , C 3-7 cycloalkyl, C 2-6 alkenyl optionally substituted with one or more halogen atoms or cyano, C 2-6 alkynyl optionally substituted with one or more halogen atoms or cyano, C 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C 1-6 alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)R 6 , —NH—S(═O) p R 6 , —C(═O)R 6 , —NHC(═O)H, —C(═O)NHNH 2 , —NHC(═O)R 6 , —C(═NH)R 6 or a radical of formula

wherein each A independently is N, CH or CR 6 ;

B is NH, O, S or NR 6 ;

p is 1 or 2; and

R 6 is methyl, amino, mono- or dimethylamino or polyhalomethyl;

L is C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, C 3-7 cycloalkyl, whereby each of said aliphatic group may be substituted with one or two substituents independently selected from

C 3-7 cycloalkyl,

indolyl or isoindolyl, each optionally substituted with one, two, three or four substituents each independently selected from halo, C 1-6 alkyl, hydroxy, C 1-6 alkyloxy, cyano, aminocarbonyl, nitro, amino, polyhalomethyl, polyhalomethyloxy and C 1-6 alkylcarbonyl,

phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl, wherein each of said aromatic rings may optionally be substituted with one, two, three, four or five substituents each independently selected from the substituents defined in R 2 ; or

L is —X—R 3 wherein

R 3 is phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl, wherein each of said aromatic rings may optionally be substituted with one, two, three, four or five substituents each independently selected from the substituents defined in R 2 ; and

X is —NH—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O) 2 —;

Q represents hydrogen, C 1-6 alkyl, halo, polyhaloC 1-6 alkyl or —NR 4 R 5 ; and

R 4 and R 5 are each independently selected from hydrogen, hydroxy, C 1-12 alkyl, C 1-12 alkyloxy, C 1-12 alkylcarbonyl, C 1-2 alkyloxycarbonyl, aryl, amino, mono- or di(C 1-12 alkyl)amino, mono- or di(C 1-2 alkyl)aminocarbonyl

wherein each of the aforementioned C 1-2 alkyl groups may optionally and each individually be substituted with one or two substituents each independently selected from hydroxy, C 1-6 alkyloxy, hydroxyc 1-6 alkyloxy, carboxyl, C 1-6 alkyloxycarbonyl, cyano, amino, imino, mono- or di(C 1-6 alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(O) p R 6 , —NH—S(═O) p R 6 , —C(═O)R 6 , —NHC(═O)H, —C(═O)NHNH 2 , —NHC(O)R 6 , —C(═NH)R 6 , aryl and Het; or

R 4 and R 5 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C 1-2 alkyl)aminoC 1-4 -alkylidene;

Y represents hydroxy, halo, C 3-7 cycloalkyl, C 2-6 alkenyl optionally substituted with one or more halogen atoms, C 2-6 alkynyl optionally substituted with one or more halogen atoms, C 1-6 alkyl substituted with cyano or —C(═O)R 6 , C 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C 1-6 alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O) p R 6 , —NH—S(═O) p R 6 , —C(═O)R 6 , —NHC(═O)H, —C(═O)NHNH 2 , —NHC(═O)R 6 , —C(NH)R 6 or aryl;

aryl is phenyl or phenyl substituted with one, two, three, four or five substituents each independently selected from halo, C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkyloxy, cyano, nitro, polyhaloC 1-6 alkyl and polyhaloC 1-6 alkyloxy;

Het is an aliphatic or aromatic heterocyclic radical;

said aliphatic heterocyclic radical is selected from pyrrolidinyl, piperidinyl, homopiperidinyl, piperazinyl, morpholinyl-, tetrahydrofuranyl and tetrahydrothienyl wherein each of said aliphatic heterocyclic radical may optionally be substituted with an oxo group; and said aromatic heterocyclic radical is selected from pyrrolyl, furanyl, thienyl, pyridinyl, pyrimidinyl, pyrazinyl and pyridazinyl wherein each of said aromatic heterocyclic radical may optionally be substituted with hydroxy,

as a solid dispersion in a polymeric matrix, wherein the polymeric matrix is consisting of a homo- or copolymer of N-vinylpyrrolidone.