Compounds exhibiting jak-kinase activity (versions), method of treating jak-kinase mediated diseases, method of inhibiting jak-kinase activity (versions), pharmaceutical composition of said compounds

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of general formula III which possess the properties of JAK pathway inhibitors and JAK-kinase inhibitors. In formula III: X is specified in a group consisting of C1-C10alkyl, amino, halogen, carboxyl, carboxylic acid ester, C2alkynyl, substituted tri-C1-C6alkylsilyl; R represents hydrogen; the cycle A is specified in a group consisting of C6aryl, bicycloheptene, five-and sis-member mono- or 10-member bicyclic heteroaryl including 1 to 3 heteroatoms specified in a group of heteroatoms, including N, O or S, and five- or six-member mono- or 10-member bicyclic heterocycle, including 1 to 2 heteroatoms specified in a group of heteroatoms, including N or O; p means 0, 1, 2 or 3; each of R2 is independently specified in a group consisting of C1-C6alkyl, C1-C4alkyl substituted by 1 to 3 substitutes. The other substitute and radical values are specified in the patent claim.

EFFECT: compounds may be used in preparing a therapeutic agent for T-cell mediated autoimmune disease, for treating or preventing allograft rejection in a recipient, for treating or preventing a type IV hypersensitivity reactions, which includes administering the above agent containing the compound according to cl 1-11, in an amount effective to treat the autoimmune disease or the allograft rejection or the type IV hypersensitivity.

23 cl, 7 dwg, 12 tbl, 43 ex

 

The text descriptions are given in facsimile form.

1. The compounds of formula III:

where X is selected from the group consisting of C1-C10of alkyl, amino, halogen, carboxyl, complex ether carboxylic acid, With2the quinil, substituted three-C1-C6alkylsilane;
R represents a hydrogen:
cycle And selected from the group consisting of C6aryl, bicycloheptene, five or six-membered mono - or 10-membered bicyclic heteroaryl, including from 1 to 3 heteroatoms selected from the group of heteroatoms, including N, O or S, and five or six-membered mono - or 10-membered bicyclic heterocycle containing 1 to 2 heteroatoms selected from the group of heteroatoms, including N or O;
p denotes 0, 1, 2 or 3;
each of R2independently from each other selected from the group consisting of C1-C6of alkyl, C1-C4of alkyl, substituted from 1 to 3 substituents selected from the group comprising From1-C6alkoxy, C1-C10and the sludge C1-C10acylamino, amino, aminocarbonyl, aminocarbonyl,6aryl, ester of carboxylic acid (-C(O)O-C1-C10alkyl, -C(O)O-C2-C10alkenyl), aminocarbonyl, mono-C1-C6-alkylaminocarbonyl, di-C1-C6-alkylaminocarbonyl, cyano, halogen, hydroxyl, 5-6-membered heteroaryl, including from 1 to 3 heteroatoms selected from the group of heteroatoms, including N, O or S, a 5-6-membered heterocyclyl comprising 1 to 2 heteroatoms selected from the group of heteroatoms, including N, O or S, tios1-C10acyl, C1-C10alkylthio or three-From1-C10alkylsilane,
C1-C6alkoxy, C1-C6alkoxy, substituted from 1 to 3 substituents selected from the group comprising C1-C6alkoxy, C1-C10acylamino, aminocarbonyl, mono-C1-C4alkylaminocarbonyl, di-C1-C4alkylaminocarbonyl, aminocarbonyl, ester of carboxylic acid (-C(O)O-C1-C10alkyl, -C(O)O-C2-C10alkenyl, -C(O)O-C2-C10quinil)2-C4quinil, halogen, hydroxyl, cyano, 5-6-membered heteroaryl, including from 1 to 3 heteroatoms, represents N, a 5-6-membered heterocyclyl comprising 1 to 2 heteroatoms selected from the group of heteroatoms, including N, O or S,
and the Ino-, amino group substituted by the substituents R21and R22independently selected from the group comprising hydrogen, C1-C10alkyl, or both Deputy R21and R22together with the nitrogen atom form a C1-C6a heterocycle comprising 1 to 2 heteroatoms selected from the group of heteroatoms, including N, O or S, with R21and R22at the same time are not hydrogens, ceanography, bicycloheptene, halogen, 5-6-membered heteroaryl, including from 1 to 3 heteroatoms selected from the group of heteroatoms, including N, O or S,
With5-C15heteroaromatic including 1 heteroatom represents N, C1-C10heterocyclyl comprising 1 to 2 heteroatoms selected from the group of heteroatoms, including N, O or S,
C1-C10heterocyclics comprising 1 to 2 heteroatoms selected from the group of heteroatoms, including N, O or S
aminos1-C10acyl, amino1-C10acyloxy;
each of the Z1, Z2and Z3represents a carbon atom;
q is 0, 1, 2 or 3;
each of R3independently from each other selected from the group consisting of hydrogen, C1-C10of alkyl, C1-C6alkoxy, C1-C10of alkyl, substituted from 1 to 5 substituents selected from the group comprising C1-C10alkoxy, g is lågen, With5-C6heterocycle comprising 1 to 2 heteroatoms selected from the group of heteroatoms, including N, O or S and C5-C6heterocycle comprising 1 to 2 heteroatoms selected from the group of heteroatoms, including N, O or S, substituted by 1 Deputy selected from the group comprising C1-C6alkyl, ester of carboxylic acid (-C(O)O-C1-C10alkyl);
R4and R5independently from each other selected from the group consisting of hydrogen, C1-C6of alkyl, C2-C6the quinil, C1-C6of alkyl, substituted from 1 to 3 substituents selected from the group comprising From1-C10alkoxy, C1-C10acyl, C1-C10acylamino, amino, di-C1-C6-alkylamino, aminocarbonyl, ester of carboxylic acid (-C(O)O-C1-C10alkyl),
With5-C6heterocyclyl comprising 1 to 2 heteroatoms selected from the group of heteroatoms, including N, O, and
M+where M+is a metal counterion selected from the group consisting of K+, Na+Li+; or
R4and R5together with the nitrogen atom to which they are attached, form a group C5-C6heterocyclyl comprising 1 to 2 heteroatoms selected from the group of heteroatoms, including N, O, or C5-C6the heterocycle is, comprising 1 to 2 heteroatoms selected from the group of heteroatoms, including N, O, substituted 1 Deputy selected from the group comprising amino, C1-C6-alkyl, halogen, hydroxyl; or
when q is 1, 2 or 3, R5may be associated with one group R3through its α-position with the formation of condensed cycle, as illustrated in formula IV:

in which W is selected from the group consisting of C1-C3alkylene, in which one carbon atom is replaced by a group C(O), or is a bond participating in the centre of unsaturation-N=C<; and SO2NR4R5is meta - or para-position relative to the amino group in position 2 of the pyrimidine;
their pharmaceutically acceptable salts.

2. Compounds according to claim 1, in which:
X represents fluorine or methyl; and
R4and R5independently from each other selected from the group consisting of hydrogen, C1-C6of alkyl, C1-C6of alkyl, substituted from 1 to 3 substituents selected from the group comprising C1-C10alkoxy, C1-C10acyl, C1-C10acylamino, amino, di-C1-C6-alkylamino, aminocarbonyl, ester of carboxylic acid (-C(O)O-C1-C10alkyl); or
R4and R5together with the nitrogen atom to which they are connected, is formed will C 5-C6heterocyclic group containing 1 to 2 heteroatoms selected from the group of heteroatoms, including N or O5-C6heterocyclic group containing 1 to 2 heteroatoms selected from the group of heteroatoms, including N, or O substituted 1 Deputy selected from the group comprising C1-C6alkyl, amino, halogen, hydroxyl.

3. Compounds according to claim 1, in which the cycle And represents phenyl.

4. A compound selected from the group of compounds comprising N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(prop-2-ynyloxy)-phenyl]-2,4-pyrimidinediamine and 5-fluoro-N2-(4-methyl-3-propionamido-sulfanilyl)N4-[4-(prop-2-ynyloxy)phenyl]-2,4-pyrimidinediamine.

5. The Union, representing N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(prop-2-ynyloxy)-phenyl]-2,4-pyrimidinediamine.

6. The Union, which represents 5-fluoro-N2-(4-methyl-3-propionylthiocholine)-N4-[4-(prop-2-ynyloxy)phenyl]-2,4-pyrimidinediamine.

7. Compounds represented by formula V:

where X represents a fluorine or methyl;
R represents hydrogen;
q is 0, 1, 2 or 3;
each of R3independently from each other selected from the group consisting of hydrogen, C1-C6of alkyl, C1-C6alkoxy, halogen;
each of the Z1, Z2and Z3is the th carbon; and
SO2NR4R5is in meta-position to the amino group in position 2 of the pyrimidine; and
R4and R5independently from each other selected from the group consisting of hydrogen, C1-C6of alkyl, C1-C6of alkyl, substituted from 1 to 3 substituents selected from the group comprising C1-C10alkoxy, C1-C10acyl, C1-C10acylamino, amino, aminocarbonyl, ester of carboxylic acid (-C(O)O-C1-C10alkyl),
With5-C6heterocyclyl comprising 1 to 2 heteroatoms selected from the group of heteroatoms, including N, or O; or
R4and R5together with the nitrogen atom to which they are bound, form a5-C6heterocyclic group containing 1 to 2 heteroatoms selected from the group of heteroatoms, including N or O5-C6heterocyclic group containing 1 to 2 heteroatoms selected from the group of heteroatoms, including N, or O substituted 1 Deputy selected from the group comprising C1-C6alkyl, amino, halogen, hydroxyl;
R7selected from the group consisting of hydrogen, C1-C10the alkyl or C1-C10of alkyl, substituted 1 Deputy selected from the group comprising From6aryl, C1-C6alkalosis6aryl, cyano, C5-C6g is tetraaryl, comprising 1 to 2 heteroatoms selected from the group of heteroatoms, including N or O, and
V is selected from the group consisting of C1-C3alkylene or C1-C3alkylene substituted from 1 to 3 substituents selected from the group comprising C1-C6alkyl, halogen, in which one carbon atom is replaced by a heteroatom selected from oxygen, sulfur, S(O)2.

8. Compounds selected from the group consisting of:
I-2 N2-(3-aminosulfonyl-4-were)-N4-(3-cyanoethoxy-4,5-acid)-5-fluoro-2,4-pyrimidinediamine;
I-3 N2-(4-aminosulfonyl)phenyl-N4-(3-cyanoethoxy)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-4 N2-(3-aminosulfonyl)phenyl-N4-(3-cyanoethoxy)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-5 N4-(3-cyanoethoxy)phenyl-5-fluoro-N2-[3-(4-methylpiperazin-1-yl)sulfonyl]phenyl-2,4-pyrimidinediamine;
I-8 N2-(3-aminosulfonyl-4-ISO-propylphenyl)-N4-(4-cyanomethylation)-5-fluoro-2,4-pyrimidinediamine;
I-9 N2-[3-aminosulfonyl-4-(4-methylpiperazin-1-yl)phenyl]-5-fluoro-N4-(4-cyanomethylation)-2,4-pyrimidinediamine;
I-10 N2-[3-aminosulfonyl-4-(4-methylpiperazin-1-yl)phenyl]-5-fluoro-N4-(4-cyanomethylene-3-forfinal)-2,4-pyrimidinediamine;
I-11 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(4-cyanomethylene-3-forfinal)-2,4-pyrimidinediamine;
I-12 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(4-cyanomethylene-3-forfinal)-2,4-pyrimidinediamine;
I-13 N2-(3-aminosulfonyl enyl)-5-bromo-N4-(4-cyanomethylation)-2,4-pyrimidinediamine;
I-14 N2-(3-aminosulfonyl-4-were)-5-bromo-N4-(4-cyanomethylation)-2,4-pyrimidinediamine;
I-15 N2-(3-aminosulphonylphenyl)-N4-(4-cyanomethylation)-5-trimethylsilylethynyl-2,4-pyrimidinediamine;
I-17 N2-(3-aminosulfonyl)phenyl-N4-(4-cyanoethoxy)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-19 N4-(4-cyanoethoxy)phenyl-5-fluoro-N2-[3-(4-methylpiperazin-1-yl)sulfonyl]phenyl-2,4-pyrimidinediamine:
I-20 N2-(3-aminosulfonyl-4-methyl)phenyl-N4-(4-cyanoethoxy)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-21 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(4-cyanoethoxy)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-23 N2-(3-aminosulfonyl)phenyl-N4-(4-cyanoethoxy-3-methyl)phenyl-5-fluoro-2,4-pyrimidinediamine:
I-24 N2-(3-aminosulfonyl-4-methyl)phenyl-N4-(4-cyanoethoxy-3-methyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-26 N2-(3-aminosulfonyl)phenyl-N4-(4-cyanoethoxy-3,5-dimethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-27 N2-(3-aminosulfonyl-4-methyl)phenyl-N4-(4-cyanoethoxy-3,5-dimethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-30 N4-(4-cyanomethylene)phenyl-5-fluoro-N2-(4-methyl-3-propiomelanocortin)phenyl-2,4-pyrimidinediamine (68);
I-31 N4-(4-cyanomethylene)phenyl-5-fluoro-N2-(4-methyl-3-propiomelanocortin)phenyl-2,4-pyrimidinediamine sodium salt (69);
I-33 N2-(3-aminosulfonyl-4-fluoro)phenyl-N4-(4-cyanoethoxy)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-34 N2-(3-aminosulfonyl-4-fluoro)phenyl-N4-(4-cyanoethoxy-3-methyl)phenyl-5-fluoro-2,4-pyrimidine is yamina;
I-35 N2-(3-aminosulfonyl-4-fluoro)phenyl-N4-(4-cyanoethoxy-3,5-dimethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-36 N2-(3-acetylaminophenol-4-methyl)phenyl-N4-(4-cyanomethylene)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-37 N4-(4-cyanomethylene)phenyl-5-fluoro-N2-(3-isobutyryl aminosulfonyl-4-methyl)phenyl-2,4-pyrimidinediamine;
I-38 N2-(3-acetylaminophenol-4-methyl)phenyl-N4-(4-cyanomethylene)phenyl-5-fluoro-2,4-pyrimidinediamine sodium salt;
I-39 N4-(4-cyanomethylene)phenyl-5-fluoro-N2-(3-isobutylbenzene-4-methyl)phenyl-2,4-pyrimidinediamine sodium salt;
I-42 N2-(3-aminosulphonylphenyl)-N4-(3-chloro-4-cinematographer)-5-fluoro-2,4-pyrimidinediamine;
I-43 N2-(3-aminosulfonyl-4-were)-N4-(3-chloro-4-cyanoethoxy phenyl)-5-fluoro-2,4-pyrimidinediamine;
I-46 N2-(3-aminosulphonylphenyl)-N4-(4-cyanoethoxy-3-methoxy phenyl)-5-fluoro-2,4-pyrimidinediamine;
I-47 N2-(3-aminosulfonyl-4-were)-N4-(4-cyanoethoxy-3-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine:
I-48 N4-(4-cyanoethoxy-3-forfinal)-5-fluoro-N2-(4-methyl-3-propionylthiocholine)-2,4-pyrimidinediamine;
I-49 N4-(4-cyanoethoxy-3-forfinal)-5-fluoro-N2-(4-methyl-3-propionylthiocholine)-2,4-pyrimidinediamine sodium salt;
I-50 N2-(3-aminosulphonylphenyl)-N4-(4-cyanoethoxy-3-hydroxymethylene)-5-fluoro-2,4-pyrimidinediamine;
I-51 N2-(3-aminosulfonyl-4-were)-N4-(4-cyanoethoxy-3-hydroxymethylene)-5-fluoro-2,4-pyrimidin the amine;
I-53 N2-(3-aminosulphonylphenyl)-N4-[4-cyanoethoxy-3-(1-cyanomethylene-3-yl)phenyl]-5-fluoro-2,4-pyrimidinediamine;
I-54 N2-(3-aminosulfonyl-4-were]-N4-[4-cyanoethoxy-3-(1-cyanomethylene-3-yl)phenyl]-5-fluoro-2,4-pyrimidinediamine;
I-56 N2-(3-aminosulfonyl-4-methoxyphenyl)-N4-(4-cinematographer)-5-fluoro-2,4-pyrimidinediamine;
I-58 N2-(3-aminosulphonylphenyl)-N4-(4-cinematographer)-5-methyl-2,4-pyrimidinediamine;
I-59 N2-(3-aminosulfonyl-4-were)-N4-(4-cinematographer)-5-methyl-2,4-pyrimidinediamine;
I-61 racemic N2-(3-aminosulfonyl)phenyl-N4-[4-(1-cyano)ethoxy-3-methyl]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-62 racemic N2-(3-aminosulfonyl-4-methyl)phenyl-N4-[4-(1-cyano)ethoxy-3-methyl]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-65 racemic N2-(3-aminosulfonyl)phenyl-N4-[4-(1-cyano)ethoxy]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-67 racemic N2-(3-aminosulfonyl-4-methyl]phenyl-N4-[4-(1-cyano)ethoxy]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-68 racemic N2-(3-aminosulfonyl-4-fluoro)phenyl-N4-[4-(1-cyano)ethoxy]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-69 racemic N2-(3-aminosulfonyl-4-fluoro)phenyl-N4-[4-(1-cyano)ethoxy-3-methyl]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-71 racemic N2-(3-aminosulfonyl)phenyl-N4-[4-(1-cyano)ethoxy-3,5-dimethyl]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-72 racemic N2-(3-aminosulfonyl-4-methyl)phenyl-N4-[4-(1-cyano)ethoxy-3,5-dimethyl]phenyl-5-fluoro-2,4-Piri is inindiana;
I-73 N2-(3-aminosulfonyl-4-methyl)phenyl-N4-[4-(1-cyano-1-methyl)ethoxy]phenyl-5-fluoro-2,4-pyrimidinediamine:
I-74 N2-(3-aminosulfonyl-4-fluoro)phenyl-N4-[4-(1-cyano-1-methyl)ethoxy]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-76 N2-(3-aminosulfonyl)phenyl-N4-[4-(1-cyano-1-methyl)ethoxy]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-78 N2-(3-aminosulphonylphenyl)-N4-[4-(N-cyanoacetyl)AMINOPHENYL]-5-fluoro-2,4-pyrimidinediamine;
I-79 N2-(3-aminosulfonyl-4-were)-N4-[4-(N-cyanoacetyl)AMINOPHENYL]-5-fluoro-2,4-pyrimidinediamine;
I-80, N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[3-methyl-4-(N-cyanoacetyl)AMINOPHENYL]-2,4-pyrimidinediamine;
I-81 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-methyl-4-(N-cyanoacetyl)AMINOPHENYL]-2,4-pyrimidinediamine;
I-82 N2-(3-aminosulphonylphenyl)-N4-[3-chloro-4-(N-cyano-acetyl)AMINOPHENYL]-5-fluoro-2,4-pyrimidinediamine;
I-83 N2-(3-aminosulfonyl-4-were)-N4-[3-chloro-4-(N-cyanoacetyl)AMINOPHENYL]-5-fluoro-2,4-pyrimidinediamine;
I-84 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[3-methoxy-4-(N-cyanoacetyl)AMINOPHENYL]-2,4-pyrimidinediamine;
I-85 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-methoxy-4-(N-cyanoacetyl)AMINOPHENYL]-2,4-pyrimidinediamine;
I-86 N2-(3-aminosulphonylphenyl)-N4-[4-(N-cyanoacetyl-N-methyl)AMINOPHENYL]-5-fluoro-2,4-pyrimidinediamine;
I-87 N2-(3-aminosulfonyl-4-were)-N4-[4-(N-cyanoacetyl-N-methyl)AMINOPHENYL]-5-fluoro-2,4-pyrimidinediamine;
I-88 N4-(3-aminocarbonylmethyl)phenyl-N2-(3-aminosulfonyl)phenyl-5-fluoro-,4-pyrimidinediamine;
I-89 N4-(3-aminocarbonylmethyl)phenyl-5-fluoro-N2-[3-(4-methylpiperazin-1-yl)sulfonyl]phenyl-2,4-pyrimidinediamine;
I-90 N4-(3-aminocarbonylmethyl)phenyl-N2-(3-aminosulfonyl-4-methyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-92 N4-(4-aminocarbonylmethyl-3-methyl)phenyl-N2-(3-aminosulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-93 N4-(4-aminocarbonylmethyl-3,5-dimethyl)phenyl-N2-(3-aminosulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-94 N4-(4-aminocarbonylmethyl)phenyl-N2-(3-aminosulfonyl-4-methyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-95 N4-(4-aminocarbonylmethyl-3-methyl)phenyl-N2-(3-aminosulfonyl-4-methyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-96 N4-(4-aminocarbonylmethyl-3,5-dimethyl)phenyl-N2-(3-aminosulfonyl-4-methyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-98 N4-(4-aminocarbonylmethyl-3-chlorophenyl)-N2-(3-aminosulphonylphenyl)-5-fluoro-2,4-pyrimidinediamine;
I-99 N4-(4-aminocarbonylmethyl-3-chlorophenyl)-N2-(3-aminosulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
I-101 N4-(4-aminocarbonylmethyl-3-forfinal)-N2-(3-aminosulphonylphenyl)-5-fluoro-2,4-pyrimidinediamine;
I-102 N4-(4-aminocarbonylmethyl-3-forfinal)-N2-(3-aminosulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
I-104 N4-(4-aminocarbonylmethyl-3-methoxyphenyl)-N2-(3-aminosulphonylphenyl)-5-fluoro-2,4-pyrimidinediamine;
I-105 N4-(4-aminocarbonylmethyl-3-methoxyphenyl)-N2-(3-aminosulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
I-106 N4-4-aminocarbonylmethyl-3-hydroxymethylene)-N2-(3-aminosulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
I-107 N4-(4-aminocarbonylmethyl-3-hydroxymethylene]-N2-(3-aminosulphonylphenyl)-5-fluoro-2,4-pyrimidinediamine;
I-109 N4-(4-aminocarbonylmethyl)-N2-(3-amino-sulfanilyl)-5-methyl-2,4-pyrimidinediamine;
I-110 N4-(4-aminocarbonylmethyl)-N2-(3-aminosulfonyl-4-were)-5-methyl-2,4-pyrimidinediamine;
I-111 N4-(4-aminocarbonylmethyl)phenyl-N2-(3-aminosulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-112 N4-(4-aminocarbonylmethyl)phenyl-5-fluoro-N2-[3-(4-methylpiperazin-1-yl)sulfonyl]phenyl-2,4-pyrimidinediamine;
I-117 racemic N4-[4-(1-aminocarbonyl)ethoxy]phenyl-N2-(3-aminosulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-118 N4-[4-(1-aminocarbonyl)ethoxy]phenyl-N2-(3-aminosulfonyl-4-methyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-120 racemic N4-[4-(1-aminocarbonyl)ethoxy-3-methyl]phenyl-N2-(3-aminosulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-121 racemic N4-[4-(1-aminocarbonyl)ethoxy-3-methyl]phenyl-N2-(3-aminosulfonyl-4-methyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-123 racemic N4-[4-(1-aminocarbonyl)ethoxy-3,5-dimethyl]phenyl-N2-(3-aminosulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-124 racemic N4-[4-(1-aminocarbonyl)ethoxy-3,5-dimethyl]phenyl-N2-(3-aminosulfonyl-4-methyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-126 N4-[4-(1-aminocarbonyl-1-methyl)ethoxy]phenyl-N2-(3-aminosulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-127 N4-[4-(1-aminocarbonyl-1-methyl)ethoxy]phenyl-N2-(3-what aminosulfonyl-4-methyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-129 N2-(3-aminosulphonylphenyl)-N4-(4-dimethylamino-carbonylmethyl)-5-fluoro-2,4-pyrimidinediamine;
I-130 N2-(3-aminosulfonyl-4-were)-N4-(4-dimethylamino-carbonylmethyl)-5-fluoro-2,4-pyrimidinediamine;
I-132 N2-(3-aminosulphonylphenyl)-N4-(3-chloro-4-dimethyl-aminocarbonylmethyl)-5-fluoro-2,4-pyrimidinediamine;
I-133 N2-(3-aminosulfonyl-4-were)-N4-(3-chloro-4-dimethyl-aminocarbonylmethyl)-5-fluoro-2,4-pyrimidinediamine;
I-135 N2-(3-aminosulphonylphenyl)-N4-(3-chloro-4-dimethyl-aminocarbonylmethyl)-5-methyl-2,4-pyrimidinediamine;
I-136 N2-(3-aminosulfonyl-4-were)-N4-(3-chloro-4-dimethylaminocarbonylmethyl)-5-methyl-2,4-pyrimidinediamine;
I-138 N2-(3-aminosulphonylphenyl)-N4-(4-dimethylamino-carbonyloxy-3-forfinal)-5-methyl-2,4-pyrimidinediamine;
I-139 N2-(3-aminosulfonyl-4-were)-N4-(4-dimethylamino-carbonyloxy-3-forfinal)-5-methyl-2,4-pyrimidinediamine;
I-140 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(3-chloro-4-dimethyl-aminocarbonylmethyl)-5-fluoro-2,4-pyrimidinediamine;
I-141 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(3-chloro-4-dimethyl-aminocarbonylmethyl)-5-methyl-2,4-pyrimidinediamine;
I-142 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(4-dimethylamino-carbonyloxy-3-forfinal)-5-methyl-2,4-pyrimidinediamine;
I-144 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(4-methylamino-carbonylmethyl)-2,4-pyrimidinediamine;
I-145 N2-(3-aminosulfonyl-4-methylp the Nile)-5-fluoro-N4-(4-methylenedioxybenzyl)-2,4-pyrimidinediamine;
I-147 N2-(3-aminosulphonylphenyl)-N4-(3-chloro-4-methylenedioxybenzyl)-5-fluoro-2,4-pyrimidinediamine;
I-148 N2-(3-aminosulfonyl-4-were)-N4-(3-chloro-4-methylenedioxybenzyl)-5-fluoro-2,4-pyrimidinediamine;
I-150 N2-(3-aminosulphonylphenyl)-N4-(3-chloro-4-methyl-aminocarbonylmethyl)-5-methyl-2,4-pyrimidinediamine;
I-151 N2-(3-aminosulfonyl-4-were)-N4-(3-chloro-4-methylenedioxybenzyl)-5-methyl-2,4-pyrimidinediamine;
I-152 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(3-chloro-4-methylenedioxybenzyl)-5-fluoro-2,4-pyrimidinediamine;
I-153 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(3-chloro-4-methylenedioxybenzyl)-5-methyl-2,4-pyrimidinediamine;
I-155 N2-(3-aminosulphonylphenyl)-N4-(3-fluoro-4-methyl-aminocarbonylmethyl)-5-methyl-2,4-pyrimidinediamine;
I-156 N2-(3-aminosulfonyl-4-were)-N4-(3-fluoro-4-methylenedioxybenzyl)-5-methyl-2,4-pyrimidinediamine;
I-158 N4-(4-allylaminogeldanamycin)-N2-(3-amino-sulfanilyl)-5-fluoro-2,4-pyrimidinediamine;
I-159 N4-(4-allylaminogeldanamycin)-N2-(3-amino-sulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
I-160 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(2-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-161 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-5-fluoro-N4-[4-(2-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-162 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-166 N2-[3-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[4-(2-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-167 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[(4-((pyridin-2-yl)methoxy)-3-were)]-2,4-pyrimidinediamine;
I-168 N2-(3-amino-4-methylsulfinylphenyl)-5-fluoro-N4-[(4-((pyridin-2-yl)methoxy)-3-were)]-2,4-pyrimidinediamine;
I-169 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-pyridinyl)-3-permitidentifier]-2,4-pyrimidinediamine;
I-170 5-fluoro-N2-[3-N-(methyl)aminosulfonyl-4-were]-N4-[4-(2-pyridinyl)-3-methylethylenediamine]-2,4-pyrimidinediamine;
I-171 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-pyridinyl)-3-chloromethyloxirane]-2,4-pyrimidinediamine;
I-172 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(2-pyridinyl)-3-permitidentifier]-2,4-pyrimidinediamine;
I-173 5-fluoro-N2-[3-N-(methyl)aminosulfonyl-4-were]-N4-[4-(2-pyridinyl)-3-permitidentifier]-2,4-pyrimidinediamine;
I-174 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(2-pyridinyl)-3-chloromethyloxirane]-2,4-pyrimidinediamine;
I-178 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(3-pyridyloxy)phenyl]-2,4-pyrimidinediamine;
I-179 N2-(3-aminosulphonylphenyl)-5-methyl-N4-[4-(2-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-180 5-methyl-N2-[3-(N-methylaminomethyl)-4-were]-N4-[4-(2-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-182 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[3-(3-pyridinyl)-methylenedioxyphenyl]-24-pyrimidinediamine;
I-183 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-(3-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-184 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-5-fluoro-N4-[3-(3-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-187 N2-[3-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[3-(3-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-188 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(3-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-189 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(3-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-190 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-5-fluoro-N4-[4-(3-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-192 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(3-pyridinyl)-methylthiophenyl]-2,4-pyrimidinediamine;
I-193 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-194 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(4-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-195 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-5-fluoro-N4-[4-(4-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-196 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-4-[(2-pyridinyl)-methylenediphenyl]-2,4-pyrimidinediamine salt of hydrochloric acid;
I-197 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(3-methyl-(1H)-pyrazole-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-198 N2-(3-aminosulfonyl-4-were)-N4-[4-(1,3-dimethyl-(1H-pyrazole-5-yl)methylenediphenyl]-5-fluoro-2,4-pyrimidinediamine;
I-199 N2-(3-aminosulfonyl-4-were)-N4-[4-(1-benzyl-3-methyl-(1H)-pyrazole-5-yl)methylenediphenyl]-5-fluoro-2,4-pyrimidinediamine;
I-200 N2-(3-aminosulfonyl-4-forfinal)-5-fluoro-N4-[4-(2,4-dihydro-3-oxo-1,2,4-triazole-5-yl)methylenediphenyl]-2,4-pyrimidine-diamine (76);
I-201 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(2,4-dihydro-3-oxo-1,2,4-triazole-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-202 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(2,4-dihydro-3-oxo-1,2,4-triazole-5-yl)methylenediphenyl]-2,4-pyrimidine-diamine;
I-203 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-methyl-3-(2-morpholinoethoxy)phenyl]-2,4-pyrimidinediamine;
I-204 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-methyl-3-(2-morpholinoethoxy)phenyl]-2,4-pyrimidinediamine;
I-206 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-morpholino-ethyloxy)phenyl-2,4-pyrimidinediamine;
I-207 5-fluoro-N2-(3-morpholinosydnonimine)-N4-[4-(2-morpholino-ethyloxy)phenyl]-2,4-pyrimidinediamine;
I-208 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-methyl-3-(2-morpholinosydnonimine)phenyl]-2,4-pyrimidinediamine;
I-211 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-morpholine-4-yl-2-oxo-ethoxy)phenyl]-2,4-pyrimidinediamine;
I-212 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(2-morpholine-4-yl-2-oxo-ethoxy)phenyl]-2,4-pyrimidinediamine;
I-213 5-fluoro-N4-(4-methoxycarbonylaminophenyl)-N2-(4-methyl-3-propionylthiocholine)-2,4-pyrimidinediamine;
I-214 N2-(3-aminosulfonyl-4-were)-N4-[3-(5-m is Teal-isoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-215 5-fluoro-N2-[3-(N-methoxycarbonylmethylene)aminosulfonyl-phenyl]-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidine-diamine;
I-216 N2-(3-aminosulfonyl-5-chloro-4-were)-5-fluoro-N4-[3-methyl-4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidine-diamine;
I-217 N2-(3-aminosulfonyl-4-fluoro-5-were)-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-218 N2-(3-aminosulfonyl-4-chloro-5-were)-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-219 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-220 N2-(3-aminosulfonyl-4-chlorophenyl)-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-221 N2-(3-aminosulfonyl-4-were)-N4-[3-chloro-4-(5-methylisoxazol-3-yl)methylenediphenyl]-5-fluoro-2,4-pyrimidinediamine;
I-222 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-fluoro-4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-223 N2-(3-aminosulfonyl-5-chloro-4-were)-5-fluoro-N4-[3-fluoro-4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidine-diamine;
I-224 N2-(3-aminosulfonyl-4-fluoro-5-were)-5-fluoro-N4-[3-fluoro-4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidine-diamine;
I-225 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-methyl-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-226 N2-(3-aminosulfonyl-4-Mei is phenyl)-5-fluoro-N4-[3-fluoro-4-(5-methylisoxazol-3-yl)methylenediphenyl]-N4-methyl-2,4-pyrimidinediamine;
I-227 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-methoxy-carbonylmethyl-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-228 5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-N2-(4-methyl-3-propionylthiocholine)-2,4-pyrimidinediamine;
1-229 5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-N2-(4-methyl-3-(2-methylpropionyl)aminosulphonylphenyl)-2,4-pyrimidinediamine;
I-230 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine (59, X=H);
I-232 N2-(3-acetamidophenyl)-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-233 N2-(3-aminosulfonyl-4-forfinal)-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-234 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-methyl-4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine:
I-235 5-fluoro-N2-[3-(N-methyl)aminosulfonyl-4-were]-N4-[4-(5-methylisoxazol-3-yl)metalinox phenyl]-2,4-pyrimidinediamine;
I-236 5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-N2-(3-N-propanamide)sulfanilyl)]-2,4-pyrimidinediamine;
I-237 N2-(3-aminosulfonyl-4-forfinal)-5-fluoro-N4-[3-methyl-4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-238 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[3-methyl-4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-239 5-fluoro-N2-[3-N-(methyl)aminosulfonyl-4-methylphen the]-N4-[3-methyl-4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-241 N2-[3-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-242 5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-N2-(3-N-propanamide)sulfanilyl)]-2,4-pyrimidinediamine sodium salt;
I-243 N2-(3-acetamidophenyl)-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine sodium salt;
I-244 N2-[3-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[3-methyl-4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-247 N2-{3-[(N-5-methyl-1,3-dioxolan-2-he-4-yl)methylene]amino-sulfanilyl}-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-248 N2-{3-[N-N-di-[(5-methyl-1,3-dioxolan-2-he-4-yl)methylene]]-aminosulphonylphenyl}-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-249 N2-{3-[N-N-di-[(5-tert-butyl-1,3-dioxolan-2-he-4-yl)-methylene]]aminosulphonylphenyl}-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-250 N2-{3-[(N-5-tert-butyl-1,3-dioxolan-2-he-4-yl)methylene]-aminosulphonylphenyl}-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-251 N2-[3-aminosulfonyl-4-(4-methylpiperazin-1-yl)phenyl-5-fluoro-N4-[2-fluoro-4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-252 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[3-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine (60)
I-254 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-255 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-N4-[3-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-257 N2-{3-[(N-5-methyl-1,3-dioxolan-2-he-4-yl)methylene]-aminosulphonylphenyl}-5-fluoro-N4-[4-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-258 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-259 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-260 5-fluoro-N2-[3-N-(methyl)aminosulfonyl-4-were)-N4-[4-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-261 N2-[3-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[3-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-262 5-fluoro-N4-[4-(3-methyl-1,2,4-oxadiazol-3-yl)methylenediphenyl]-N2-[(3-N-propanamide)sulfanilyl)]-2,4-pyrimidinediamine;
I-264 5-fluoro-N4-[4-(3-methyl-1,2,4-oxadiazol-3-yl)metalinox-phenyl]-N2-[(3-N-propanamide)sulfanilyl)]-2,4-pyrimidinediamine;
I-265 N2-(3-aminosulfonyl-4-chloro-5-were)-5-fluoro-N4-[4-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-266 N2-(3-aminosulfonyl-4-forfinal)-5-fluoro-N4-[4-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-267 N-(3-aminosulfonyl-4-forfinal)-5-fluoro-N4-[4-(3-methyl-1,2,4-oxadiazol-5-yl)tilepanel]-2,4-pyrimidinediamine;
I-271 N2-(5-N,N-diethylaminomethyl-2-methoxyphenyl)-5-fluoro-N4-(4-[3-methyl-1,2,4-oxadiazol-5-yl]methylenedioxyphenyl)-2,4-pyrimidinediamine;
I-273 5-fluoro-N4-[4-(3-methyl-1,2,4-oxadiazol-3-yl)methylene oksifenil]-N2-[(3-N-propanamide)sulfanilyl)]-2,4-pyrimidinediamine sodium salt;
I-274 5-fluoro-N4-[4-(5-methyl-1,2,4-oxadiazol-3-yl)methoxy]phenyl-N2-[3-(4-methylpiperazin-1-yl)sulfonyl]phenyl-N2,4-pyrimidinediamine;
I-276 N2-(3-aminosulfonyl)phenyl-5-fluoro-N4-[4-(5-methyl-1,2,4-oxadiazol-3-yl)methoxy]phenyl-2,4-pyrimidinediamine;
I-277 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(5-methyl-1,3,4-oxadiazol-2-yl)methylenediphenyl]-2,4-pyrimidinediamine (71);
I-278 N2-(3-aminosulfonyl-4-forfinal)-5-fluoro-N4-[4-(5-methyl-1,3,4-oxadiazol-2-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-279 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(5-methyl-1,3,4-oxadiazol-2-yl)methoxyphenyl]-2,4-pyrimidinediamine;
I-280 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(2-methylthiazole-4-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-281 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-methylthiazole-4-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-282 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-N4-[4-(2-methylthiazole-4-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-283 N2-[3-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[4-(2-methylthiazole-4-yl)methylenediphenyl]-2,4-pyrimidinediamine;
II-1 racemic N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-{3-[(1-metile ridin-3-yl)oxy]phenyl}-2,4-pyrimidinediamine;
II-2 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-{3-[(1-methylpiperidin-4-yl)oxy]phenyl}-2,4-pyrimidinediamine;
II-3 racemic N2-(3-aminosulfonyl-4-were)-N4-{3-chloro-4-[(1-methylpiperidin-3-yl)oxy]phenyl}-5-fluoro-2,4-pyrimidinediamine;
II-4 racemic N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-{4-[(1-methylpiperidin-3-yl)oxy]phenyl}-2,4-pyrimidinediamine;
II-5 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-{3-methyl-4-[(1-methylpiperidin-4-yl)oxy]phenyl}-2,4-pyrimidinediamine;
II-6 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-{4-[(1-methylpiperidin-4-yl)oxy]-3-triptoreline}-2,4-pyrimidinediamine;
II-7 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-{4-[(1-methylpiperidin-4-yl)oxy]phenyl}-2,4-pyrimidinediamine;
II-8 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-{3-chloro-4-[(1-methylpiperidin-4-yl)oxy]phenyl}-2,4-pyrimidinediamine;
II-9 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(N-methylpyrrolidine-3-idoxifene)-2,4-pyrimidinediamine;
II-10 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(N-methylpyrrolidine-3-idoxifene)-2,4-pyrimidinediamine;
II-11 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(3-pyridyloxy)-phenyl]-2,4-pyrimidinediamine;
II-12 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(3-pyridyloxy)phenyl]-2,4-pyrimidinediamine;
II-13 5-fluoro-N2-[3-N-(methylaminomethyl)-4-were]-N4-[4-(3-pyridyloxy)phenyl]-2,4-pyrimidinediamine;
II-16 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(4-pyridyloxy)phenyl]-2,4-pyrimidine is yamina;
II-17 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-pyridyloxy)-phenyl]-2,4-pyrimidinediamine;
II-18 5-fluoro-N2-[3-N-methylaminomethyl)-4-were]-5-fluoro-N4-[4-(4-pyridyloxy)phenyl]-2,4-pyrimidinediamine;
II-19 N2-(3-aminocarbonyl-5-were)-5-fluoro-N2-[4-(1-methylpyrazole-3-yl)AMINOPHENYL)-2,4-pyrimidinediamine;
III-1 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-5-fluoro-N4-(4-cyanomethylene)-2,4-pyrimidinediamine;
III-2 N2-[4-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-(4-cyanomethylene)-2,4-pyrimidinediamine;
III-4 N2-(3-aminosulfonyl)phenyl-N4-(4-cyanomethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-5 N4-(4-cyanomethyl)phenyl-5-fluoro-N2-[3-(4-methylpiperazin-1-yl)sulfonyl]phenyl-2,4-pyrimidinediamine;
III-7 N2-(3-aminosulfonyl-4-methyl)phenyl-N4-(4-cyanomethyl)-phenyl-5-fluoro-2,4-pyrimidinediamine;
III-8 N2-(3-aminosulfonyl-4-chloro)phenyl-N4-(4-cyanomethyl)-phenyl-5-fluoro-2,4-pyrimidinediamine;
III-10 N2-(3-aminosulfonyl-4-fluoro)phenyl-N4-(4-cyanomethyl)-phenyl-5-fluoro-2,4-pyrimidinediamine;
III-11 N2-(3-aminosulfonyl-4-were)-N4-(4-cyanoethylene-phenyl)-5-methyl-2,4-pyrimidinediamine;
III-12 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-[4-(2-cyanoethyl)-phenyl-5-methyl-2,4-pyrimidinediamine;
III-13 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-[4-(2-cyanoethyl)-phenyl]-5-fluoro-2,4-pyrimidinediamine;
III-14 N2-(3-aminosulphonylphenyl)-N4-[4-(cyanoethyl)phenyl]-5-fluoro-2,4-pyrimidinediamine;
III-15 N2-(3-aminosulfonyl-4-were)-N4-[4-(cyanoethyl is)-phenyl]-5-fluoro-2,4-pyrimidinediamine;
III-16 N2-(3-aminosulfonyl-4-forfinal)-N4-[4-(cyanomethylene)-phenyl]-5-fluoro-2,4-pyrimidinediamine;
III-17 N2-(3-aminosulfonyl-4-were-5-fluoro-N4-[4-(2-cyanoethyl)-3-forfinal]-2,4-pyrimidinediamine;
III-18 N2-(3-aminosulphonylphenyl)-N4-[4-(2-cyanoethyl)-3-fluoro-phenyl]-5-fluoro-2,4-pyrimidinediamine;
III-19 N2-(3-aminosulfonyl-4-were)-N4-[4-(2-cyanoethyl)-3-were]-5-fluoro-2,4-pyrimidinediamine;
III-20 N2-(3-aminosulphonylphenyl)-N4-[4-(2-cyanoethyl)-3-were]-5-fluoro-2,4-pyrimidinediamine;
III-21 N2-(3-aminosulfonyl-4-were)-N4-[3-chloro-4-(2-cyanoethyl)phenyl]-5-fluoro-2,4-pyrimidinediamine;
III-22 N2-(3-aminosulphonylphenyl)-N4-[3-chloro-4-(2-cyanoethyl)-phenyl]-5-fluoro-2,4-pyrimidinediamine;
III-23 N2-(3-aminosulfonyl-4-were)-N4-(4-cyanoethyl-2-were)-5-fluoro-2,4-pyrimidinediamine;
III-24 N2-(3-aminosulphonylphenyl)-N4-(4-cyanoethyl-2-methyl-phenyl)-5-fluoro-2,4-pyrimidinediamine;
III-25 N2-(3-aminosulfonyl-4-were)-N4-(4-cyanomethylene-3-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
III-26 N2-(3-aminosulphonylphenyl)-N4-(4-cyanoethyl-2-methyl-phenyl)-5-fluoro-2,4-pyrimidinediamine;
III-28 N4-(3-chloro-4-cyanomethyl-phenyl)-5-fluoro-N2-(4-methyl-3-propionylthiocholine)-2,4-pyrimidinediamine;
III-29 N4-(3-chloro-4-cyanoethylene-phenyl)-5-fluoro-N2-(4-methyl-3-propionylthiocholine)-2,4-pyrimidinediamine sodium salt;
III-30 N4-(4-cyanomethylene-3-triptoreline)-5-fluoro-N2-(4-methyl-3-aminosulphonylphenyl)-2,4-pyrimido the diamine;
III-31 N4-(4-cyanomethylene-3-triptoreline)-5-fluoro-N2-(3-aminosulphonylphenyl)-2,4-pyrimidinediamine;
III-33 N4-(4-aminocarbonylmethyl)-N2-(3-aminosulphonylphenyl)-5-fluoro-2,4-pyrimidinediamine;
III-34 N4-(4-aminocarbonylmethyl)-N2-(3-aminosulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
III-36 N2-(3-aminosulfonyl)phenyl-N4-(4-ethylcarbodiimide)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-37 N2-(3-aminosulfonyl-4-methyl)phenyl-N4-(4-ethylcarboxyl-aminomethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-39 N2-(3-aminosulfonyl)phenyl-N4-(3-cyclopropanecarbonyl-aminomethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-40 N2-(3-aminosulfonyl-4-methyl)phenyl-N4-(3-cyclopropyl-carbonylmethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-42 N2-(3-aminosulfonyl)phenyl-N4-(4-cyclopropanecarbonyl-aminomethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-43 N2-(3-aminosulfonyl-4-methyl)phenyl-N4-(4-cyclopropyl-carbonylmethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-45 N4-(4-acrylamidoethyl)-N2-(3-aminosulphonylphenyl)-5-fluoro-2,4-pyrimidinediamine;
III-46 N4-(4-acrylamidoethyl)-N2-(3-aminosulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
III-47 N4-[4-(2-aminocarboxylate)phenyl]-5-fluoro-N2-(4-methyl-3-aminosulphonylphenyl)-2,4-pyrimidinediamine;
III-48 N4-[4-(2-aminocarboxylate)phenyl]-N2-(3-aminosulfonyl-phenyl)-5-fluoro-2,4-pyrimidinediamine;
III-50 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(1-meth is l-pyrazolyl-3-aminocarbonylmethyl)phenyl]-2,4-pyrimidinediamine;
III-51 N2-(3-aminosulphonylphenyl)-N4-[(1-ethylpyrazine-5-aminocarbonylmethyl)phenyl]-5-fluoro-2,4-pyrimidinediamine;
III-52 N2-(3-aminosulfonyl-4-were)-5-N4-[(1-ethylpyrazine-5-aminocarbonylmethyl)phenyl]-5-fluoro-2,4-pyrimidinediamine;
III-53 N4-{4-[2-(aminocarbonyl)ethyl]phenyl}-N2-(3-aminosulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
III-54 N4-{4-[2-(aminocarbonyl)ethyl]phenyl}-N2-(3-aminosulphonylphenyl)-5-fluoro-2,4-pyrimidinediamine;
III-55 N4-{4-[2-(aminocarbonyl)ethyl]phenyl}-N2-(3-aminosulfonyl-4-chlorophenyl)-5-fluoro-2,4-pyrimidinediamine;
III-56 N2-(3-aminosulfonyl-4-were)-N4-{4-[2-(dimethylaminoethoxy)ethyl]phenyl}-5-fluoro-2,4-pyrimidinediamine;
III-57 N2-(3-aminosulphonylphenyl)-N4-{4-[2-(dimethylaminoethoxy)ethyl]phenyl}-5-fluoro-2,4-pyrimidinediamine;
III-58 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-{4-[2-(dimethylaminoethoxy)ethyl]phenyl}-5-fluoro-2,4-pyrimidinediamine;
III-59 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-{4-[2-(methylaminorex)ethyl]phenyl}-2,4-pyrimidinediamine;
III-60 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-{4-[2-(methylaminorex)ethyl]phenyl}-2,4-pyrimidinediamine;
III-61 N2-(3-aminosulfonyl-4-chlorophenyl)-5-fluoro-N4-{4-[2-(methylaminorex)ethyl]phenyl}-2,4-pyrimidinediamine;
III-62 N2-(3-aminosulphonylphenyl)-N4-(4-benzoylphenyl)-5-fluoro-2,4-pyrimidinediamine;
III-63 N2-(3-aminosulfonyl-4-were)-N4-(4-benzoylphenyl)-5-fluoro-2,4-pyrimidinediamine;
III-64 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(4-benzoylphenyl)-5-fluoro-2,4-pyrimidinediamine;
III-65 N2-(3-aminosulfonyl-4-methoxy-5-were)-N4-(4-benzoylphenyl)-5-fluoro-2,4-pyrimidinediamine;
III-66 N2-(3-aminosulfonyl-4-methoxyphenyl)-5-fluoro-N4-[4-(4-pyridinylmethyl)phenyl]-2,4-pyrimidinediamine;
III-68 5-fluoro-N4-[4-(4-pyridinylmethyl]-N2-[(3-N-propanamide)sulfanilyl)]-2,4-pyrimidinediamine;
III-69 5-fluoro-N4-[4-(4-pyridinylmethyl)phenyl]-N2-[(3-N-propanamide)sulfanilyl)]-2,4-pyrimidinediamine sodium salt;
III-70 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-pyridinylmethyl)phenyl]-2,4-pyrimidinediamine;
III-73 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-pyridylmethyl)-phenyl]-2,4-pyrimidinediamine, salt of hydrochloric acid;
III-74 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(4-pyridinylmethyl)phenyl]-2,4-pyrimidinediamine;
III-75 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-5-fluoro-N4-[4-(4-pyridinylmethyl)phenyl]-2,4-pyrimidinediamine;
III-76 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-pyridinyl)-phenethyl]-2,4-pyrimidinediamine;
III-77 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(4-pyridinyl)phenethyl]-2,4-pyrimidinediamine;
III-78 5-fluoro-N2-[3-N-(methyl)aminosulfonyl-4-were]-N4-[4-(4-pyridinyl)phenethyl]-2,4-pyrimidinediamine;
III-80 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(1-oxido-4-pyridylmethyl)phenyl]-2,4-pyrimidinediamine;
111-81 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(1-imidazolidinyl)phenyl]-2,4-pyrimidinediamine;
III-82 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(1-imidazolidinyl)f the Nile]-2,4-pyrimidinediamine;
III-83 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-5-fluoro-N4-[4-(1-imidazolidinyl)phenyl]-2,4-pyrimidinediamine;
III-85 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-N4-[4-(1-imidazolidinyl)phenyl]-2,4-pyrimidinediamine hydrochloride;
III-86 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-N4-[4-(1-imidazolidinyl)phenyl]-2,4-pyrimidinediamine;
III-87 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(1-imidazolyl)phenethyl]-2,4-pyrimidinediamine;
III-88 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(1-imidazolyl)phenethyl]-2,4-pyrimidinediamine;
III-89 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-N4-[4-(1-imidazolyl)phenethyl]-2,4-pyrimidinediamine;
III-91 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(2-methyl-1-imidazolidinyl)phenyl]-2,4-pyrimidinediamine;
III-93 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-N4-[4-(2-methyl-1-imidazolidinyl)phenyl]-2,4-pyrimidinediamine;
III-94 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-methyl-1-imidazolidinyl)phenyl]-2,4-pyrimidinediamine;
III-95 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-{4-[1-(1,2,3-triazolyl)methyl]phenyl}-2,4-pyrimidinediamine;
III-97 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-{4-[1-(1,2,3-triazolyl)methyl]phenyl}-2,4-pyrimidinediamine;
III-98 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-N4-{4-[1-(1,2,3-triazolyl)methyl]phenyl}-2,4-pyrimidinediamine;
III-100 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-{4-[1-(1,2,4-triazolyl)methyl]phenyl}-2,4-pyrimidinediamine;
III-101 N2-(3-AMI is sulfonyl-4-were)-5-fluoro-N4-{4-[1-(1,2,4-triazolyl)methyl]phenyl}-2,4-pyrimidinediamine;
III-102 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-N4-{4-[1-(1,2,4-triazolyl)methyl]phenyl}-2,4-pyrimidinediamine;
III-103 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(4-N-morpholino-methylindenyl)-2,4-pyrimidinediamine;
III-104 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(4-N-morpholinomethyl)-2,4-pyrimidinediamine;
III-105 N2-(3-aminosulfonyl-4-methylenedioxyphenyl)-5-fluoro-N4-(4-N-morpholinomethyl)-2,4-pyrimidinediamine;
III-106 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(3-methyl-1,2,4-oxadiazol-5-yl)tilepanel]-2,4-pyrimidinediamine;
III-107 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(4-thiomorpholine-methylindenyl)-2,4-pyrimidinediamine;
III-108 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(4-thio-morpholinomethyl)-2,4-pyrimidinediamine;
III-109 N2-(3-aminosulfonyl-4-methoxyphenyl)-5-fluoro-N4-(4-thiomorpholine)-2,4-pyrimidinediamine;
III-110 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-{4-[(1,1-diocletianopolis-4-yl)-methyl]phenyl}-2,4-pyrimidinediamine;
III-111 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-{4-[(1,1-diocletianopolis-4-yl)-methyl]phenyl}-2,4-pyrimidinediamine;
III-112 N2-(3-aminosulfonyl-4-methoxyphenyl)-5-fluoro-N4-{4-[(1,1-diocletianopolis-4-yl)-methyl]phenyl}-2,4-pyrimidinediamine;
III-114 N4-(3-aminocarbonylmethyl)phenyl-N2-(3-amino-sulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-115 N4-(3-aminocarbonylmethyl)phenyl-N2-(3-amino-sulfonyl-4-methyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-117 N2-(3-AMI is sulfonyl)phenyl-N4-(3-ethylaminomethyl-aminomethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-118 N2-(3-aminosulfonyl-4-methyl)phenyl-N4-(3-ethylamino-carbonylmethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-120 N2-(3-aminosulphonylphenyl]-N4-(4-ethylaminomethyl-aminomethylphenol)-5-fluoro-2,4-pyrimidinediamine;
III-121 N2-(3-aminosulfonyl-4-were)-N4-(4-ethylamino-carbonylmethyl)-5-fluoro-2,4-pyrimidine;
III-123 N2-(3-aminosulfonyl)phenyl-N4-[4-(2-ethylamino-carbylamine)ethyl]phenyl-5-fluoro-2,4-pyrimidinediamine;
III-124 N2-(3-aminosulfonyl-4-methyl)phenyl-N4-[4-(2-ethylamino-carbylamine)ethyl]phenyl-5-fluoro-2,4-pyrimidinediamine;
III-126 N2-(3-aminosulfonyl)phenyl-N4-[4-(N-carbarnoyl-N-propyl)aminomethyl]phenyl-5-fluoro-2,4-pyrimidinediamine;
III-127 N2-(3-aminosulfonyl-4-methyl)phenyl-N4-[4-(N-carbarnoyl-N-propyl)aminomethyl]phenyl-5-fluoro-2,4-pyrimidinediamine;
III-128 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-pyridylmethyl)-phenyl]-2,4-pyrimidinediamine salt p-toluensulfonate acid;
III-129 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-pyridylmethyl)-phenyl]-2,4-pyrimidinediamine salt methanesulfonic acid;
IV-1 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[3-(1,3-oxazol-5-yl)-phenyl]-2,4-pyrimidinediamine;
IV-2 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-(1,3-oxazol-5-yl)phenyl]-2,4-pyrimidinediamine;
IV-4 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-N4-[3-(1,3-oxazol-5-yl)phenyl]-2,4-pyrimidinediamine;
IV-5 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(1,3-oxazol-5-yl)phenyl]-2,4-pyrimidinediamine;
IV-6 N2-(-aminosulfonyl-4-were)-5-fluoro-N4-[4-(1,3-oxazol-5-yl)phenyl]-2,4-pyrimidinediamine;
IV-7 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-N4-[4-(1,3-oxazol-5-yl)phenyl]-2,4-pyrimidinediamine;
IV-9 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[3-(N,N-dimethylaminomethyl)phenyl]-2,4-pyrimidinediamine;
IV-10 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-(N,N-dimethylaminomethyl)phenyl]-2,4-pyrimidinediamine;
IV-11 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[3-(N-methylaminomethyl)phenyl]-2,4-pyrimidinediamine;
IV-12 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-N-methylaminomethyl)phenyl]-2,4-pyrimidinediamine;
V-1 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[2-(5-methyl-isoxazol-3-yl)methylenechloride-5-yl]-2,4-pyrimidinediamine;
V-2 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-oxo-4-(2-pyridylmethyl)-benzo[1,4]oxazin-6-yl]-2,4-pyrimidinediamine;
V-5 racemic N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[2-methyl-3-oxo-4-(4-methoxybenzyl)-benzo[1,4]oxazin-6-yl]-2,4-pyrimidinediamine;
V-7 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(3-oxo-4-cyanomethyl-benzo[1,4]oxazin-6-yl)-2,4-pyrimidinediamine;
V-8 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-oxo-4-cyanomethyl-benzo[1,4]oxazin-6-yl]-2,4-pyrimidinediamine;
V-9 (R/S)-N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[2-methyl-3-oxo-4-(4-methoxybenzyl)-benzo[1,4]thiazin-6-yl]-2,4-pyrimidinediamine;
V-12 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(3-oxo-4-cyanomethyl-benzo[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
V-13 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(3-oxo-4-cyanomethyl be the AOR[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
V-14 N2-(3-aminosulfonyl-4-were)-N4-[2,2-dimethyl-3-oxo-4-cyanomethyl-5-pyrid[1,4]oxazin-7-yl]-5-fluoro-2,4-pyrimidinediamine;
V-15 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-[2,2-dimethyl-3-oxo-4-cyanomethyl-5-pyrid[1,4]oxazin-7-yl]-5-fluoro-2,4-pyrimidinediamine;
V-16 N2-(3-aminosulfonyl-4-were)-N4-(2-cyanoethylene-benzothiophen-5-yl)-5-fluoro-2,4-pyrimidinediamine;
V-17 N-2-(3-aminosulphonylphenyl)-N4-[2,2-dimethyl-3-oxo-4N-pyrid[1,4]oxazin-7-yl]-5-fluoro-2,4-pyrimidinediamine;
V-18 N-2-(3-aminosulfonyl-4-were)-N4-[2,2-dimethyl-3-oxo-4H-pyrid[1,4]oxazin-7-yl]-5-fluoro-2,4-pyrimidinediamine;
V-19 (4R)-N2-(3-aminosulfonyl-4-were)-N4-(1-cyano-methylennorbornan-4-methylpiperidin-3-yl)-5-fluoro-2,4-pyrimidinediamine) or (4S)-N2-(3-aminosulfonyl-4-were)-N4-(1-cyanomethylene-carbonyl-4-methylpiperidin-3-yl)-5-fluoro-2,4-pyrimidinediamine);
VIII-1 5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-N2-(saccharin-6-yl)-2,4-pyrimidinediamine; and
VIII-2 N4-(3-chloro-4-cyanomethylation)-5-fluoro-N2-(5-methyl-2H-1,1-dioxide-1,2,4-benzothiadiazin-7-yl)-2,4-pyrimidinediamine.

9. Compounds selected from the group consisting of:
VI-2 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(3-chloro-4-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-3 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(3,4-dichlorophenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-4 N2-(3-aminosulfonyl-4-were)-N4-(3-chloro-4-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-5 N2-(3-aminosulfonyl-4-methylphe who yl)-N4-(4-chloro-3-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-6 N2-(3-aminosulfonyl-4-were)-N4-(3,4-dichlorophenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-7 N4-(3-chloro-4-methoxyphenyl)-5-fluoro-N2-[3-(N-methoxycarbonyl-methylene)aminosulphonylphenyl]-2,4-pyrimidinediamine;
VI-8 N4-(3,4-dichlorophenyl)-5-fluoro-N2-[3-(N-methoxycarbonyl-methylene)aminosulphonylphenyl]-2,4-pyrimidinediamine;
VI-9 N4-(3-chloro-4-methoxyphenyl)-5-fluoro-N2-[3-(4-methylpiperidin-1-yl)aminosulphonylphenyl]-2,4-pyrimidinediamine;
VI-10 N4-(3,4-dichlorophenyl)-5-fluoro-N2-[3-(4-methylpiperidin-1-yl)aminosulphonylphenyl]-2,4-pyrimidinediamine;
VI-11 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(4-chloro-3-methoxy-phenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-12 N2-[3-(N-acetyl)aminosulfonyl-4-chlorophenyl]-N4-(3-chloro-4-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-13 N2-(3-aminosulfonyl-5-chloro-4-were)-N4-(3-chloro-4-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-14 N2-(3-aminosulfonyl-5-chloro-4-were)-N4-(3-chloro-4-trifloromethyl)-5-fluoro-2,4-pyrimidinediamine;
VI-15 N2-(3-aminosulfonyl-4-fluoro-5-were)-N4-(3-chloro-4-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-16 N2-(3-aminosulfonyl-4-fluoro-5-were)-N4-(3-chloro-4-trifloromethyl)-5-fluoro-2,4-pyrimidinediamine:
VI-17 N2-(3-aminosulfonyl-4-chloro-5-were)-N4-(3-chloro-4-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-18 N2-(3-aminosulfonyl-4-chloro-5-were)-N4-(3-chloro-4-trifloromethyl)-5-fluoro-2,4-pyrimidinediamine;
VI-19 N2-(3-aminosulfonyl-4-were)-N4-(3-chloro-methoxyphenyl)-5-fluoro-N4-methyl-2,4-pyrimidinediamine;
VI-20 N2-(3-aminosulfonyl-4-fluoro-5-were)-N4-(3-chloro-4-methoxyphenyl)-5-fluoro-N4-methyl-2,4-pyrimidinediamine;
VI-21 N2-(3-aminosulfonyl-4-chloro-5-were)-N4-(3-chloro-4-methoxyphenyl)-5-fluoro-N4-methyl-2,4-pyrimidinediamine;
VI-22 N2-(3-aminosulfonyl-4-were)-N4-(3-chloro-4-methoxy-phenyl)-5-fluoro-N4-propyl-2,4-pyrimidinediamine;
VI-23 N2-(3-aminosulfonyl-4-fluoro-5-were)-N4-(3-chloro-4-methoxyphenyl)-5-fluoro-N4-propyl-2,4-pyrimidinediamine;
VI-24 N2-(3-aminosulphonylphenyl)-5-carboethoxy-N4-(N-Carbo-ethoxymethylene-N-3-chloro-4-methoxyphenyl)-2,4-pyrimidinediamine;
VI-25 N2-(3-aminosulfonyl-4-were)-5-carboethoxy-N4-(N-carbomethoxyamino-N-3-chloro-4-methoxyphenyl)-2,4-pyrimidinediamine;
VI-26 N2-(3-aminosulphonylphenyl)-5-bromo-N4-(3-chloro-4-methoxy-phenyl)-2,4-pyrimidinediamine;
VI-27 2-(3-aminosulfonyl-4-were)-5-bromo-N4-(3-chloro-4-methoxyphenyl)-2,4-pyrimidinediamine;
VI-28 N2-(3-aminosulphonylphenyl)-N4-(3-chloro-4-methoxyphenyl)-5-trimethylsilylethynyl-2,4-pyrimidinediamine;
VI-29 N2-(3-aminosulfonyl-4-methoxyphenyl)-N4-(3-chloro-4-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-30 N2-(3-aminosulfonyl-4-methoxy-5-were)-N4-(3-chloro-4-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-32 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(4-Cryptor-methoxyphenyl)-2,4-pyrimidinediamine;
VI-33 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(4-triptoreline-phenyl)-2,4-pyrimidinediamine;
VI-34 N2-(3-aminosulfonyl-4-methoxy-5-methylp the Nile)-5-fluoro-N4-(4-triptoreline)-2,4-pyrimidinediamine;
VI-35 N2-(3-aminosulphonylphenyl)-N4-(4-tert-butylphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-36 N2-(3-aminosulfonyl-4-were)-N4-(4-tert-butylphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-37 N2-(3-aminosulfonyl-4-methoxy-5-were)-N4-(4-tert-butylphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-38 N2-(3-aminosulphonylphenyl)-N4-(4-chloro-3-trifluoromethyl-phenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-39 N2-(3-aminosulfonyl-4-were)-N4-(4-chloro-3-Cryptor-were)-5-fluoro-2,4-pyrimidinediamine;
VI-40 N2-(3-aminosulfonyl-4-methoxy-5-were)-N4-(4-chloro-3-trifluoromethyl-phenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-41 N2-(3-aminosulfonyl-4-chlorophenyl)-5-fluoro-N4-(4-Cryptor-phenyl)-2,4-pyrimidinediamine;
VI-42 N2-(3-aminosulfonyl-4-chlorophenyl)-5-fluoro-N4-(4-Cryptor-methoxyphenyl)-2,4-pyrimidinediamine;
VI-43 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(4-tert-butylphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-44 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(3-chloro-4-Cryptor-methyl-phenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-45 N2-(3-aminosulfonyl-4-ISO-propylphenyl)-N4-(3-chloro-4-methoxy-phenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-46 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(4-Cryptor-methylethylenediamine)-2,4-pyrimidinediamine;
VI-47 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(4-trifluoromethyl-methylenedioxyphenyl)-2,4-pyrimidinediamine;
VI-48 N2-(3-aminosulfonyl-4-chlorophenyl)-5-fluoro-N4-(4-Cryptor-methylethylenediamine)-2,4-pyrimidinediamine;
VI-49 N2-(3-aminosulfonyl-4-meth is fenil)-5-fluoro-N4-[3-(methylenedioxymethyl)phenyl]-2,4-pyrimidinediamine;
VI-50 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(4-Cryptor-were)-2,4-pyrimidinediamine;
VI-51 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(4-Cryptor-were)-2,4-pyrimidinediamine;
VI-52 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(4-hydroxy-were)-2,4-pyrimidinediamine;
VI-54 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(4-vinyl-phenyl)-2,4-pyrimidinediamine;
VI-55 N2-(3-aminosulfonyl-4-chlorophenyl)-5-fluoro-N4-[4-(prop-2-ynyloxy)phenyl]-2,4-pyrimidinediamine;
VI-57 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-(prop-2-ynyloxy)phenyl]-2,4-pyrimidinediamine;
VI-58 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-methyl-4-(prop-2-ynyloxy)phenyl]-2,4-pyrimidinediamine;
VI-59 N2-(3-aminosulfonyl-4-were)-N4-[3-chloro-4-(prop-2-ynyloxy)phenyl]-5-fluoro-2,4-pyrimidinediamine;
VI-60 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-fluoro-4-(prop-2-ynyloxy)phenyl]-2,4-pyrimidinediamine;
VI-61 N2-(3-aminosulfonyl-4-were)-N4-[4-(but-2-ynyloxy)phenyl]-5-fluoro-2,4-pyrimidinediamine;
VI-62 N2-[3-propiomelanocortin-4-were]-5-fluoro-N4-[4-(prop-2-ynyloxy)phenyl]-2,4-pyrimidinediamine;
VI-63 N2-[3-aminosulfonyl-4-(2-propyl)phenyl]-5-fluoro-N4-[4-(prop-2-ynyloxy)phenyl]2,4-pyrimidinediamine;
VI-64 N4-{4-[2-(dimethylaminoethoxy)ethyl]phenyl}-5-fluoro-N2-(3-propionylthiocholine)-2,4-pyrimidinediamine;
VI-65 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(prop-2-ynylamine)phenyl]-2,4-pyrimidinediamine;
VI-66 N4-{4-[2-(who dimetilaminokhalkona)ethyl]phenyl}-5-fluoro-N2-(3-propionylthiocholine)-2,4-]pyrimidinediamine sodium salt;
VI-67 N2-(3-aminosulfonyl-4-were)-N4-{4-[bis(prop-2-inyl)amino]phenyl}-5-fluoro-2,4-pyrimidinediamine;
VI-68 5-fluoro-N2-(4-methyl-3-methylaminoethanol)-N4-[4-(prop-2-ynyloxy)phenyl]-2,4-pyrimidinediamine;
VI-69 5-fluoro-N2-{[4-methyl-3-((1-methylpiperidin-4-yl)aminosulfonyl)]phenyl}-N4-[4-(prop-2-ynyloxy)phenyl]-2,4-pyrimidinediamine;
VI-70 N2-[3-aminosulfonyl-4-(1-methylpiperazin-4-yl)phenyl]-5-fluoro-N4-[4-(prop-2-ynyloxy)phenyl]-2,4-pyrimidinediamine;
VI-71 N4-{4-[2-(aminocarbonyl)ethyl]phenyl}-N2-(3-aminosulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
VI-72 N4-{4-[2-(aminocarbonyl)ethyl]phenyl}-N2-(3-aminosulphonylphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-73 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-{4-[(prop-2-ynyloxy)carbonylmethyl]phenyl}-2,4-pyrimidinediamine;
VI-74 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-{4-[(prop-2-ynyloxy)carbonylmethyl]phenyl}-2,4-pyrimidinediamine;
VI-75 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(prop-2-inyl-aminosulfonyl)phenyl]-2,4-pyrimidinediamine;
VI-76 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(prop-2-ineliminability)phenyl]-2,4-pyrimidinediamine;
VI-78 5-fluoro-N2-[3-(prop-2-ineliminability)phenyl]-N4-[4-(prop-2-ynyloxy)phenyl]-2,4-pyrimidinediamine;
VI-79 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-(prop-2-ineliminability)phenyl]-2,4-pyrimidinediamine;
VI-81 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[3-(prop-2-ineliminability)phenyl]-2,4-pyrimidinedione is a;
VI-83 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(3-fluoro-propyl)phenyl]-2,4-pyrimidinediamine;
VI-84 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(3-forproper)phenyl]-2,4-pyrimidinediamine;
VI-86 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(3-hydroxypropyl)phenyl]-2,4-pyrimidinediamine;
VI-87 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(3-hydroxypropyl)phenyl]-2,4-pyrimidinediamine;
VI-89 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-hydroxybutyl)phenyl]-2,4-pyrimidinediamine;
VI-90 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(4-hydroxybutyl)phenyl]-2,4-pyrimidinediamine;
VI-92 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-terbutyl)-phenyl]-2,4-pyrimidinediamine;
VI-93 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(4-terbutyl)phenyl]-2,4-pyrimidinediamine;
VI-95 N2-(3-aminosulfonyl-4-methyl)phenyl-5-fluoro-N4-(4-thio-methylcarbamyl)phenyl-2,4-pyrimidinediamine;
VI-96 N2-(3-butylaminoethyl)-N4-(3-cyano-4-methyl-phenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-97 N2-(3-butylaminoethyl)-N4-(3-chloro-4-forfinal)-5-fluoro-2,4-pyrimidinediamine;
VI-98 N2-(3-aminosulphonylphenyl)-N4-(3-cyano-4-forfinal)-5-fluoro-2,4-pyrimidinediamine;
VI-99 N2-(3-aminosulphonylphenyl)-N4-(3-cyano-4-were)-5-fluoro-2,4-pyrimidinediamine;
VI-100 N2-(3-aminosulfonyl-4-forfinal)-5-fluoro-N4-(4-hydroxy-phenyl)-2,4-pyrimidinediamine;
VI-101 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(4-hydroxyphenyl)-2,4-pyrimidinediamine;
VI-102 N2-(3-aminosulfonyl-4-were)5-fluoro-N4-[4-hydroxy-phenyl]-2,4-pyrimidinediamine;
VI-103 N4-[4(2-cyanoethyl)-3-were]-5-fluoro-N2-(4-methyl-3-propionylthiocholine)-2,4-pyrimidinediamine;
VI-104 N4-[4-(2-cyanoethyl)-3-were]-5-fluoro-N2-(4-methyl-3-propionylthiocholine)-2,4-pyrimidinediamine sodium salt;
VI-105 N4-(3,4-dichlorophenyl)-N4-methyl-5-fluoro-N2-[3-(N,N-diethyl)-aminosulfonyl-4-methoxyphenyl]-2,4-pyrimidinediamine;
VI-107 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(4-methoxy-3-chlorophenyl]-2,4-pyrimidinediamine;
VI-108 N4-(3-chloro-4-methoxyphenyl)-N2-(3-N,N-diethylamino-sulfonyl-4-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-110 N2-(3-aminosulphonylphenyl)-N4-(3,4-dichlorophenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-111 N2-(3-aminosulfonyl-4-chlorophenyl)-5-fluoro-N4-[4-(2-methoxy-ethylenoxy)phenyl]-2,4-pyrimidinediamine;
VI-112 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(2-methoxyethoxy)phenyl]-2,4-pyrimidinediamine;
VI-113 N2,N4-bis(3-aminosulphonylphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-114 N2,N4-bis(3-aminosulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
VI-115 N2,N4-bis(3-aminosulfonyl-4-chlorophenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-116 N2-[3-aminosulfonyl-4-(4-methylpiperazin-1-yl)phenyl]-N4-(3-chloro-4-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
VII-1 N2-(3-aminosulfonyl-4-were)-N4-[(2S,4R)-1-(2-cyanoacetyl)-2-ethoxycarbonylpyrimidine-4-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-2 N2-(3-aminosulfonyl-4-were)-N4-[(2S,4S)-1-(2-cyanoacetyl)-2-ethoxycarbonylpyrimidine-4-yl]-5-fluoro-2,4-is pirimidinami;
VII-3 racemic N2-(3-aminosulfonyl-4-were)-N4-(1-benzyl-4-methyl-piperidine-3-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-4 racemic N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(4-methyl-piperidine-3-yl)-2,4-pyrimidinediamine;
VII-5 racemic N2-(3-aminosulfonyl-4-were)-N4-(1-cyanomethylene-carbonyl-4-methylpiperidin-3-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-6 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(2-methoxyphenyl-5-yl)-2,4-pyrimidinediamine;
VII-7 N2-(3-aminosulphonylphenyl)-N4-(2-amino-3-methoxyphenyl-6-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-8 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(2-amino-3-methoxyphenyl-6-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-9 N2-(3-aminosulfonyl-4-were)-N4-[2-amino-3-methoxy-pyrid-6-yl]-5-fluoro-2,4-pyrimidinediamine (66);
VII-10 N4-(2-amino-3-methoxyphenyl-6-yl)-N2-[3-(ethoxycarbonylmethylene)-aminosulphonylphenyl)-5-fluoro-2,4-pyrimidinediamine;
VII-11 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(2,2,4-trimethyl-l,1,3-trioxo-benzo[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
VII-14 N2-(3-aminosulfonyl)phenyl-N4-[(N-ethylsulfonyl)-1,2,3,4-tetrahydroisoquinoline-6-yl]-5-fluoro-2,4-pyrimidinediamine;
VII-15 N2-(3-aminosulfonyl-4-methyl)phenyl-N4-[(N-ethylsulfonyl)-1,2,3,4-tetrahydroisoquinoline-6-yl]-5-fluoro-2,4-pyrimidinediamine;
VII-16 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(1,2,3,4-tetrahydrothieno-7-yl)-2,4-pyrimidinediamine;
VII-17 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[2-(methylaminomethyl)-1,2,3,4-those who reginasocial-7-yl]-2,4-pyrimidinediamine;
VII-18 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[2-(dimethylaminoethyl)-1,2,3,4-tetrahydrothieno-7-yl]-2,4-pyrimidinediamine;
VII-19 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[1-(methylaminomethyl)-1,2,3,4-tetrahydroxy-6-yl]-2,4-pyrimidinediamine;
VII-20 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[1-(methylaminomethyl)-1,2,3,4-tetrahydroxy-6-yl]-2,4-pyrimidinediamine;
VII-21 N2-(3-aminosulfonyl-4-were)-N4-[3,4-dihydro-(1H)-quinoline-2-one-6-yl]-5-fluoro-2,4-pyrimidinediamine
VII-22 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[1-(3-methoxy-propyl)indazolin-5-yl]-2,4-pyrimidinediamine;
VII-23 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[1-(2-methoxy-ethyl)indazolin-5-yl]-2,4-pyrimidinediamine;
VII-26 racemic N2-(3-aminosulfonyl-4-were)-N4-[2-(N,N-dimethyl-aminocarbonyl)-2,3-dihydrobenzofuran-5-yl]-5-fluoro-2,4-pyrimidinediamine;
VII-27 racemic N2-(3-aminosulfonyl-4-chlorophenyl)-N4-[2-(N,N-dimethyl-aminocarbonyl)-2,3-dihydrobenzofuran-5-yl]-5-fluoro-2,4-pyrimidinediamine;
VII-28 N2-(3-aminosulphonylphenyl)-N4-(chroman-4-amine-6-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-30 N2-(3-aminosulfonyl-4-were)-5-methyl-N4-(3-oxo-benzo[1,4]oxazin-6-yl)-2,4-pyrimidinediamine;
VII-32 N2-(3-aminosulphonylphenyl)-5-methyl-N4-(3-oxo-benzo[1,4]-oxazin-6-yl)-2,4-pyrimidinediamine;
VII-33 N2-(3-Aminosulfonyl-4-were)-5-methyl-N4-(4-methyl-3-oxo-benzo[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
VII-35 N2-(3-aminosulphonylphenyl)-5-methyl-N4-(4-methyl-3-oxo-b is the site, located between[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
VII-36 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(3-oxo-4-cyanomethyl-benzo[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
VII-38 N2-(3-aminosulfonyl-4-methoxy-5-were)-N4-(2,2-debtor-4H-benzo[1,4]oxazin-3-one-6-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-39 5-amino-N2-(3-aminosulphonylphenyl)-N4-(2,2-dimethyl-3-oxo-4H-benzo[1,4]oxazin-6-yl)-2,4-pyrimidinediamine;
VII-41 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(4-methyl-3-oxo-benzo[1,4]oxazin-6-yl)-2,4-pyrimidinediamine;
VII-42 N2-(3-aminosulphonylphenyl)-N4-[2,2,4-trimethyl-3-oxo-5-pyrid[1,4]oxazin-7-yl]-5-fluoro-2,4-pyrimidinediamine;
VII-44 N2-(3-aminosulfonyl-4-methyl-phenyl)-5-fluoro-N4-(3-oxo-4H-benzo[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
VII-45 N2-(3-Aminosulfonyl-4-methyl-phenyl)-5-fluoro-N4-(3-oxo-4H-benzo[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
VII-46 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-(2,2,4-trimethyl-1,1,3-trioxo-benzo[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
VII-49 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(4-methyl-3-oxo-benzo[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
VII-51 N2-(3-aminosulphonylphenyl)-N4-[2,2-dimethyl-3-oxo-4H-5-pyrid[1,4]oxazin-7-yl]-5-fluoro-2,4-pyrimidinediamine;
VII-53 N2-(3-aminosulfonyl-4-were)-N4-(2-lanamento-furan-5-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-54 N2-(3-aminosulphonylphenyl)-N4-(2-aminocarbonylmethyl-furan-5-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-55 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(3-pyridinyl-methyl)benzo[1,4]oxazin-7-yl]-2,4-pyrimidinediamine;
VII-56 N2-(3-aminosulphonylphenyl)-5-the top-N4-[4-(3-pyridinyl-methyl)benzo[1,4]oxazin-7-yl]-2,4-pyrimidinediamine;
VII-57 N2-(3-aminosulfonyl-4-were)-N4-(benzothiophen-5-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-58 N2-(3-aminosulphonylphenyl)-N4-(benzothiophen-5-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-64 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(quinoline-2-yl)-2,4-pyrimidinediamine;
VII-65 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(quinoline-3-yl)-2,4-pyrimidinediamine;
VII-66 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(quinoline-3-yl)-2,4-pyrimidinediamine;
VII-67 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(quinoline-5-yl)-2,4-pyrimidinediamine;
VII-68 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(quinoline-5-yl)-2,4-pyrimidinediamine;
VII-69 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(quinoline-6-yl)-2,4-pyrimidinediamine;
VII-70 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(quinoline-6-yl)-2,4-pyrimidinediamine;
VII-71 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(2-methyl-quinoline-6-yl)-2,4-pyrimidinediamine;
VII-72 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(2-methylinosine-6-yl)-2,4-pyrimidinediamine;
VII-73 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(2-hydroxy-4-methylinosine-6-yl)-2,4-pyrimidinediamine;
VII-74 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(2-hydroxy-4-methyl-quinoline-6-yl)-2,4-pyrimidinediamine;
VII-75 N2-(3-aminosulfonyl-4-were)-N4-(2-N,N'-dimethylamine-quinoline-6-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-76 N2-(3-aminosulphonylphenyl)-N4-(2-N,N'-dimethylamine-quinoline-6-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-77 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(quinoline-8-yl)-2,4-Piri is inindiana;
VII-78 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(quinoline-8-yl)-2,4-pyrimidinediamine;
VII-79 N2-(3-aminosulfonyl-4-forfinal)-5-fluoro-N4-(quinoline-8-yl)-2,4-pyrimidinediamine;
VII-80 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(2-methyl-quinoline-8-yl)-2,4-pyrimidinediamine;
VII-81 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(2-methylinosine-8-yl)-2,4-pyrimidinediamine;
VII-82 (1R,2R,3S,4S)N4-(3-aminocarbonylmethyl[2.2.1]hept-5-EN-2-yl)-N2-(3-aminosulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
VII-83 (1R,2R,3S,4S)N2-(3-aminosulfonyl-4-methoxy-5-methyl-phenyl)-N4-(3-aminocarbonylmethyl[2.2.1]hept-5-EN-2-yl)-5-fluoro-2,4-pyrimidinediamine; and
VIII-3 N4-(3-chloro-4-methoxyphenyl)-5-fluoro-N2-(5-methyl-2H-1,1-dioxo-1,2,4-benzothiadiazin-7-yl)-2,4-pyrimidinediamine.

10. Compounds selected from the group consisting of:
IX-21 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(2-cyanobenzoyl-5-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-22 N2-(3-aminosulfonyl-4-ISO-propylphenyl)-N4-(2-lanamento-furan-5-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-23 N4-[4-(1-acetyl-4-piperidinyl)carbonitril]-N2-(3-amino-sulfanilyl)-5-fluoro-2,4-pyrimidinediamine;
IX-24 N4-[4-(1-acetyl-4-piperidinyl)carbonitril]-N2-(3-amino-sulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
IX-25 N4-[4-(1-acetyl-4-piperidinyl)carbonitril]-5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-2,4-pyrimidinediamine;
IX-27 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(4-methylpiperazin-1-ylcarbonyl)phenyl]-2,4-pyrimi is Indiamen;
IX-28 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-methyl-piperazine-1-ylcarbonyl)phenyl]-2,4-pyrimidinediamine;
IX-29 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(1-methanesulfonyl-4-piperidinyl)carbonitril]-2,4-pyrimidinediamine;
IX-30 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(1-methanesulfonyl-4-piperidinyl)carbonitril]-2,4-pyrimidinediamine;
IX-31 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-5-fluoro-N4-[4-(1-methanesulfonyl-4-piperidinyl)carbonitril]-2,4-pyrimidinediamine;
IX-33 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-5-fluoro-N4-[4-(4-thiomorpholine)carbonitril]-2,4-pyrimidinediamine;
IX-34 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-thiomorpholine)carbonitril]-2,4-pyrimidinediamine;
IX-35 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(4-thiomorpholine)carbonitril]-2,4-pyrimidinediamine;
IX-37 N2-(3-aminosulphonylphenyl)-N4-[4-(1,1-dioxo-4-thio-morpholinyl)carbonitril]-5-fluoro-2,4-pyrimidinediamine;
IX-38 N2-(3-aminosulfonyl-4-were)-N4-[4-(1,1-dioxo-4-thiomorpholine)carbonitril]-5-fluoro-2,4-pyrimidinediamine;
IX-39 N4-[4-(1,1-dioxo-4-thiomorpholine)carbonitril]-5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-2,4-pyrimidinediamine;
IX-42 N4-(4-acetyldeoxynivalenol)-N2-(3-amino-sulfanilyl)-5-fluoro-2,4-pyrimidinediamine;
IX-43 N4-(4-acetyldeoxynivalenol)-N2-(3-aminosulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
IX-45 N2-(3-aminosulfonyl-4-methylphen is)-N4-[(4R)-1-(2-cyanoacetyl)-pyrrolidin-4-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-46 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-(5-methoxy-carbonyl-thiophene-2-yl)-2,4-pyrimidinediamine;
IX-47 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(5-methoxy-carbonyl-thiophene-2-yl)-2,4-pyrimidinediamine;
IX-48 N2-(3-aminosulfonyl-4-forfinal)-5-fluoro-N4-(5-methoxy-carbonyl-thiophene-2-yl)-2,4-pyrimidinediamine;
IX-54 5-fluoro-N2-[3-N-(methyl)aminosulfonyl-4-were]-N4-[4-(2-pyridinyl)-3-chloromethyloxirane]-2,4-pyrimidinediamine.

11. Compounds selected from the group including
I-1 N2-(4-aminosulphonylphenyl)-N4-(3-cyanoethoxy-4,5-dimethoxy-phenyl)-5-fluoro-2,4-pyrimidinediamine;
I-3 N2-(4-aminosulfonyl)phenyl-N4-(3-cyanoethoxy)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-6 N4-(3-cyanoethoxy)phenyl-5-fluoro-N2-[4-(4-methylpiperazin-1-yl)sulfonyl]phenyl-2,4-pyrimidinediamine;
I-7 N2-(4-aminosulfonyl-3-methoxy)phenyl-N4-(3-cyanoethoxy)-phenyl-5-fluoro-2,4-pyrimidinediamine;
I-16 N2-(4-aminosulfonyl)phenyl-N4-(4-cyanoethoxy)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-18 N4-(4-cyanoethoxy)phenyl-5-fluoro-N2-[4-(4-methylpiperazin-1-yl)-sulfonyl]phenyl-2,4-pyrimidinediamine;
I-22 N2-(4-aminosulfonyl)phenyl-N4-(4-cyanoethoxy-3-methyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-25 N2-(4-aminosulfonyl)phenyl-N4-(4-cyanoethoxy-3,5-dimethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-28 N2-(4-aminosulfonyl-3-methoxyphenyl)-N4-(4-cyano-methoxy)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-29 N2-(4-aminosulfonyl-3-methoxy)phenyl-N4-(4-cyanoethoxy-3-IU who yl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-32 N2-(4-aminosulfonyl-3-methoxy)phenyl-N4-(4-cyanoethoxy-3,5-dimethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-40 N4-(4-cyanoethoxy-3, 5dimethylphenyl)-5-fluoro-N2-[4-(4-methylpiperazin-1-yl)sulfanilyl]-2,4-pyrimidinediamine;
I-41 N2-(4-aminosulphonylphenyl)-N4-(3-chloro-4-cinematographer)-5-fluoro-2,4-pyrimidinediamine;
I-44 N2-(4-aminosulphonylphenyl)-N4-(4-cyanoethoxy-3-forfinal)-5-fluoro-2,4-pyrimidinediamine:
I-45 N2-(4-aminosulphonylphenyl)-N4-(4-cyanoethoxy-3-methoxy-phenyl)-5-fluoro-2,4-pyrimidinediamine;
I-52 N2-(4-aminosulphonylphenyl)-N4-[4-cyanoethoxy-3-(1-cyano-methylpyrazole-3-yl)phenyl]-5-fluoro-2,4-pyrimidinediamine;
I-55 N2-(3-aminosulfonyl-4-yl)-N4-(4-cinematographer)-5-fluoro-2,4-pyrimidinediamine;
I-57 N2-(4-aminosulphonylphenyl)-N4-(4-cinematographer-5)-methyl-2,4-pyrimidinediamine;
I-60 racemic N2-(4-aminosulfonyl)phenyl-N4-[4-(1-cyano)-ethoxy-3-were-5-fluoro-2,4-pyrimidinediamine;
I-63 racemic N2-(4-aminosulfonyl)phenyl-N4-[4-(1-cyano)-ethoxy-3,5-dimethyl]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-64 racemic N2-(4-aminosulfonyl-3-methoxy)phenyl-N4-[4-(1-cyano)ethoxy-3-methyl]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-66 racemic N2-(4-aminosulfonyl)phenyl-N4-[4-(1-cyano)-ethoxy]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-70 racemic N2-(4-aminosulfonyl-3-methoxy)phenyl-N4-[4-(1-cyano)ethoxy]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-75 N2-(4-aminosulfonyl)phenyl-N4-[4-(1-cyano-1-m is Teal)ethoxy]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-77 N2-(4-aminosulfonyl-3-methoxy)phenyl-N4-[4-(1-cyano-1-methyl)ethoxy]phenyl-5-fluoro-2,4-pyrimidinediamine;
I-91 N4-(3-aminocarbonylmethyl)phenyl-N2-(4-aminosulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-97 N4-(4-aminocarbonylmethyl-3-chlorophenyl)-N2-(4-amino-sulfanilyl)-5-fluoro-2,4-pyrimidinediamine;
I-100 N4-(4-aminocarbonylmethyl-3-forfinal)-N2-(4-amino-sulfanilyl)-5-fluoro-2,4-pyrimidinediamine;
I-103 N4-(4-aminocarbonylmethyl-3-methoxyphenyl)-N2-(4-amino-sulfanilyl)-5-fluoro-2,4-pyrimidinediamine;
I-108 N4-(4-aminocarbonylmethyl)-N2-(4-amino-sulfanilyl)-5-methyl-2,4-pyrimidinediamine;
I-113 N4-(4-aminocarbonylmethyl-3-methyl)phenyl-N2-(4-amino-sulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-114 N4-(4-aminocarbonylmethyl-3,5-dimethyl)phenyl-N2-(4-amino-sulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-115 N4-(4-aminocarbonylmethyl)phenyl-N2-(4-amino-sulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-116 racemic N4-[4-(1-aminocarbonyl)ethoxy]phenyl-N2-(4-aminosulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-119 racemic N4-[4-(1-aminocarbonyl)ethoxy-3-methyl]phenyl-N2-(4-aminosulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-122 racemic N4-[4-(1-aminocarbonyl)ethoxy-3,5-dimethyl]phenyl-N2-(4-aminosulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-125 N4-[4-(1-aminocarbonyl-1-methyl)ethoxy]phenyl-N2-(4-aminosulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
I-128 N2-(4-aminosweet ylphenyl)-N4-(4-dimethylaminobenzoyl-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
I-131 N2-(4-aminosulphonylphenyl)-N4-(3-chloro-4-dimethylamino-carbonylmethyl)-5-fluoro-2,4-pyrimidinediamine;
I-134 N2-(4-aminosulphonylphenyl)-N4-(3-chloro-4-dimethylamino-carbonylmethyl)-5-methyl-2,4-pyrimidinediamine;
I-137 N2-(4-aminosulphonylphenyl)-N4-(4-dimethyl-aminocarbonylmethyl-3-forfinal)-5-methyl-2,4-pyrimidinediamine;
I-143 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-(4-methylamino-carbonylmethyl)-2,4-pyrimidinediamine;
I-146 N2-(4-aminosulphonylphenyl)-N4-(3-chloro-4-methylamino-carbonylmethyl)-5-fluoro-2,4-pyrimidinediamine;
I-149 N2-(4-aminosulphonylphenyl)-N4-(3-chloro-4-methylenedioxybenzyl)-5-methyl-2,4-pyrimidinediamine;
I-154 N2-(4-aminosulphonylphenyl)-N4-(3-fluoro-4-methylamino-carbonylmethyl)-5-methyl-2,4-pyrimidinediamine;
I-157 N4-(4-allylaminogeldanamycin)-N2-(4-amino-sulfanilyl)-5-fluoro-2,4-pyrimidinediamine;
I-163 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-pyridinyl)-methylenediphenyl]-2,4-pyrimidinediamine;
I-164 N2-(3-aminosulfonyl-4-yl)-5-fluoro-N4-[4-(2-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-165 N2-[4-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[4-(2-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-175 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-pyridinyl)-3-chloromethyloxirane]-2,4-pyrimidinediamine;
I-176 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-pyridinyl)-3-methylethylenediamine]-2,4-pyrimidinediamine;
I-177 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-pyridinyl)-3-permitidentifier]-2,4-pyrimidinediamine;
I-181 N2-(4-aminosulphonylphenyl)-5-methyl-N4-[4-(2-pyridinyl)-methylenediphenyl]-2,4-pyrimidinediamine;
I-185 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[3-(3-pyridinyl)-methylenediphenyl]-2,4-pyrimidinediamine;
I-186 N2-[4-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[3-(3-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-191 N2-[4-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[4-(3-pyridinyl)methylenediphenyl]-2,4-pyrimidinediamine;
I-205 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-morpholino-ethyloxy)phenyl)-2,4-pyrimidinediamine;
I-209 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-methyl-3-(2-morpholinosydnonimine)phenyl]-2,4-pyrimidinediamine;
I-210 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-morpholine-4-yl-2-oxo-ethoxy)phenyl]-2,4-pyrimidinediamine;
I-231 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-240 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[3-methyl-4-(5-methyl-isoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-245 N2-[4-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[3-methyl-4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-246 N2-[4-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[4-(5-methylisoxazol-3-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-253 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[3-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-256 N2-[4-(2-N,N-diethylaminoethyl)amino shall wltnylfj)-5-fluoro-N4-[3-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-263 N2-[4-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[4-(3-methyl-1,2,4-oxadiazol-5-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-268 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-(4-[3-methyl-1,2,4-oxadiazol-5-yl]methylenedioxyphenyl)-2,4-pyrimidinediamine;
I-269 5-fluoro-N2-(4-N-methylaminomethyl)-3-methoxyphenyl-N4-(4-triptoreline-3-chlorophenyl)-2,4-pyrimidinediamine;
I-270 5-fluoro-N4-(3-hydroxyphenyl)-N2-(4-N-methylaminomethyl)-3-methoxyphenyl]-2,4-pyrimidinediamine;
I-272 5-fluoro-N4-(4-[3-methyl-1,2,4-oxadiazol-5-yl]methylenedioxyphenyl)-N2-(5-piperidinecarbonitrile)-2,4-pyrimidinediamine;
I-275 N2-(4-aminosulfonyl)phenyl-5-fluoro-N4-[4-(5-methyl-1,2,4-oxadiazol-3-yl)methoxy]phenyl-2,4-pyrimidinediamine;
I-284 N2-[4-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[4-(2-methylthiazole-4-yl)methylenediphenyl]-2,4-pyrimidinediamine;
I-285 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-methylthiazole-4-yl)methylenediphenyl]-2,4-pyrimidinediamine;
II-14 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(3-pyridyloxy)-phenyl]-2,4-pyrimidinediamine;
II-15 N2-[3,5-bis(aminosulfonyl)phenyl)-5-fluoro-N4-[4-(3-pyridyloxy)phenyl]-2,4-pyrimidinediamine;
III-2 N2-[4-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-(4-cyanomethylene)-2,4-pyrimidinediamine;
III-3 N2-(4-aminosulfonyl)phenyl-N4-(4-cyanomethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-6 N4-(4-cyanomethyl)phenyl-5-fluoro-N2-[4-(4-methylpiperazin-1-yl)sulfonyl]phenyl-2,4-pyrimidinediamine;
III-9 N2-(-aminosulfonyl-3-methoxy)phenyl-N4-(4-cyanomethyl)-phenyl-5-fluoro-2,4-pyrimidinediamine;
III-27 N2-(4-aminosulphonylphenyl)-N4-(4-cyanoethylidene)-5-methyl-2,4-pyrimidinediamine and his proletarienne form;
III-32 N4-(4-aminocarbonylmethyl)-N2-(4-amino-sulfanilyl)-5-fluoro-2,4-pyrimidinediamine;
III-35 N2-(4-aminosulfonyl)phenyl-N4-(4-ethylcarboxyl-aminomethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-38 N2-(4-aminosulfonyl)phenyl-N4-(3-cyclopropanecarbonyl-aminomethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-41 N2-(4-aminosulfonyl)phenyl-N4-(4-cyclopropanecarbonyl-aminomethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-44 N4-(4-acrylamidoethyl)-N2-(4-aminosulphonylphenyl)-5-fluoro-2,4-pyrimidinediamine;
III-49 N4-[4-(2-aminocarboxylate)phenyl]-N2-(4-amino-sulfanilyl)-5-fluoro-2,4-pyrimidinediamine
III-67 N2-[4-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[4-(4-pyridinylmethyl)phenyl]-2,4-pyrimidinediamine;
III-71 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-pyridinyl-methyl)phenyl]-2,4-pyrimidinediamine;
III-72 N2-[4-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[4-(4-pyridinylmethyl)phenyl]-2,4-pyrimidinediamine;
III-79 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-pyridinyl)-phenethyl]-2,4-pyrimidinediamine;
III-84 N2-[4-(2-N,N-diethylaminoethyl)aminosulphonylphenyl)-5-fluoro-N4-[4-(1-imidazolidinyl)phenyl]-2,4-pyrimidinediamine;
III-90 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(1-imidazolyl)-phenethyl]-2,4-pyrimidinediamine;
III-92 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(2-methyl-1-imidazolyl the Teal)phenyl]-2,4-pyrimidinediamine;
III-96 N2-4-aminosulphonylphenyl)-5-fluoro-N4-(4-[1-(1,2,3-triazolyl)methyl]phenyl}-2,4-pyrimidinediamine;
III-99 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-{4-[1-(1,2,4-triazolyl)methyl]phenyl}-2,4-pyrimidinediamine;
III-113 N4-(3-aminocarbonylmethyl)phenyl-N2-(4-amino-sulfonyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-116 N2-(4-aminosulfonyl)phenyl-N4-(3-ethylaminomethyl-aminomethyl)phenyl-5-fluoro-2,4-pyrimidinediamine;
III-119 N2-(4-aminosulphonylphenyl)-N4-(4-ethylaminomethyl-aminomethylphenol]-5-fluoro-2,4-pyrimidinediamine;
III-122 N2-(4-aminosulfonyl)phenyl-N4-[4-(2-ethylaminomethyl-amino)ethyl]phenyl-5-fluoro-2,4-pyrimidinediamine;
III-125 N2-(4-aminosulfonyl)phenyl-[N4-[4-(N-carbarnoyl-N-propyl)aminomethyl]phenyl-5-fluoro-2,4-pyrimidinediamine;
IV-3 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[3-(1,3-oxazol-5-yl)phenyl]-2,4-pyrimidinediamine;
IV-8 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(1,3-oxazol-5-yl)phenyl]-2,4-pyrimidinediamine;
V-3 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[3-oxo-4-(2-pyridylmethyl)-benzo[1,4]oxazin-6-yl]-2,4-pyrimidinediamine;
V-4 racemic N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[2-methyl-3-oxo-4-(4-methoxybenzyl)-benzo[1,4]oxazin-6-yl]-2,4-pyrimidinediamine;
V-6 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-(3-oxo-4-cyanomethyl-benzo[1,4]oxazin-6-yl)-2,4-pyrimidinediamine;
V-10 (R/S)-N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[2-methyl-3-oxo-4-(4-methoxybenzyl)-benzo[1,4]thiazin-6-yl]-2,4-pyrimidinediamine;
V-11 N2-(4-aminosulphonylphenyl)-5-the top-N4-(3-oxo-4-cyanomethyl-benzo[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
VI-1 5-fluoro-N4-(3-hydroxyphenyl)-N2-[4-(N-methyl)aminosulfonyl-3-methoxyphenyl]-2,4-pyrimidinediamine;
VI-31 N2-(3-aminosulfonyl-4-yl)-N4-(3-chloro-4-methoxyphenyl)-5-fluoro-2,4-pyrimidinediamine;
VI-53 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(prop-2-ynyloxy)phenyl]-2,4-pyrimidinediamine;
VI-56 5-fluoro-N2-(4-methyl-3-propionylthiocholine)-N4-[4-(prop-2-ynyloxy)phenyl]-2,4-pyrimidinediamine;
VI-77 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(prop-2-ineliminability)phenyl]-2,4-pyrimidinediamine;
VI-80 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[3-(prop-2-inyl-aminosulfonyl)phenyl]-2,4-pyrimidinediamine;
VI-82 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(3-forproper)-phenyl]-2,4-pyrimidinediamine;
VI-85 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(3-hydroxypropyl)phenyl]-2,4-pyrimidinediamine;
VI-88 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-hydroxybutyl)phenyl]-2,4-pyrimidinediamine;
VI-91 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-terbutyl)-phenyl]-2,4-pyrimidinediamine;
VI-94 N2-(4-aminosulfonyl)phenyl-5-fluoro-N4-(4-thiomethyl-carbonyl)phenyl-2,4-pyrimidinediamine;
VI-106 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-(4-methoxy-3-chlorophenyl]-2,4-pyrimidinediamine;
VI-109 N2-(4-aminosulphonylphenyl)-N4-(3,4-dichlorophenyl)-5-fluoro-2,4-pyrimidinediamine;
VII-12 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-(2,2,4-trimethyl-1,1,3-trioxo-benzo[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
VII-13 N2-(4-aminosulfonyl)phenyl-N4-[(N-ethylsulfonyl)-1,2,3,4-tetrahydrothieno the Lin-6-yl]-5-fluoro-2,4-pyrimidinediamine;
VII-24 N4-(3,4-atlanticcity)-5-fluoro-N2-[4-(pyrrolidin-1-ylsulphonyl)phenyl]-2,4-pyrimidinediamine;
VII-25 N4-(3,4-atlanticcity)-5-fluoro-N2-[4-(N-methyl)amino-sulfonyl-3-methoxyphenyl]-2,4-pyrimidinediamine;
VII-29 N2-(4-aminosulphonylphenyl)-N4-(chroman-4-amine-6-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-31 N2-(4-aminosulphonylphenyl)-5-methyl-N4-(3-oxo-benzo[1,4]-oxazin-6-yl)-2,4-pyrimidinediamine;
VII-34 N2-(4-aminosulphonylphenyl)-5-methyl-N4-(4-methyl-3-oxo-benzo[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
VII-37 N4-(2,2-dimethyl-3-oxo-4H-benzo[1,4]oxazin-6-yl)-5-fluoro-N2-[4-(N-methyl)aminosulfonyl-3-methoxyphenyl]-2,4-pyrimidinediamine;
VII-40 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-(4-methyl-3-oxo-benzo[1,4]oxazin-6-yl)-2,4-pyrimidinediamine;
VII-43 N2-(4-aminosulphonylphenyl)-N4-[2,2,4-trimethyl-3-oxo-5-pyrid[1,4]oxazin-5-yl]-5-fluoro-2,4-pyrimidinediamine;
VII-47 N2-(4-aminosulphonylphenyl)-N4-cyanomethyl-5-fluoro-N4-[3-oxo-4-methyl-benzo[1,4]thiazin-6-yl]-2,4-pyrimidinediamine;
VII-48 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-(4-methyl-3-oxo-benzo[1,4]thiazin-6-yl)-2,4-pyrimidinediamine;
VII-50 5-fluoro-N4-(4-methyl-3-oxo-benzo[1,4]thiazin-6-yl)-N2-(3-piperidinecarbonitrile)-2,4-pyrimidinediamine;
VII-52 N2-(4-aminosulphonylphenyl)-N4-[2,2-dimethyl-3-oxo-4H-5-pyrid[1,4]oxazin-7-yl]-5-fluoro-2,4-pyrimidinediamine;
VII-59 N2-(4-aminosulphonylphenyl)-N4-(4-N-tert-butoxycarbonyl-amino-3,4-dihydro-2H-1-benzopyran-6-yl)-5-fluoro-2,4-pyrimidinediamine;
VII-60 N2-(3-aminosulphonylphenyl is)-5-fluoro-N4-[4-(1-methyl-sulfonyl)indolin-5-yl]-2,4-pyrimidinediamine;
VII-61 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[4-(1-methyl-sulfonyl)indolin-5-yl]-2,4-pyrimidinediamine;
VII-62 5-fluoro-N2-[3-(N-methylaminomethyl)-4-were]-N4-[4-(1-methylsulphonyl)indolin-5-yl]-2,4-pyrimidinediamine;
VII-63 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(1-methyl-sulfonyl)indolin-5-yl]-2,4-pyrimidinediamine;
IX-1 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[1-(propyne-3-yl)indol-5-yl]-2,4-pyrimidinediamine;
IX-2 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[1-(propyne-3-yl)indol-5-yl]-2,4-pyrimidinediamine;
IX-3 N2-(3-aminosulfonyl-4-were)-5-fluoro-N4-[1-(propyne-3-yl)indol-6-yl]-2,4-pyrimidinediamine;
IX-4 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-[1-(propyne-3-yl)indol-6-yl]-2,4-pyrimidinediamine;
IX-5 N2-(3-aminosulphonylphenyl)-N4-(1-cyanomethylene-5-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-6 N2-(4-aminosulphonylphenyl)-N4-(1-cyanomethylene-5-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-7 N2-(3-aminosulfonyl-4-chlorophenyl)-N4-(1-cyanomethylene-5-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-8 N2-(3-aminosulfonyl-4-were)-N4-(1-cyanomethylene-5-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-9 N4-[3-(aminocarbonyl)-1H-indol-6-yl]-N2-(3-aminosulfonyl-4-were)-5-fluoro-2,4-pyrimidinediamine;
IX-10 N4-[3-(aminocarbonyl)-1H-indol-6-yl]-N2-(3-aminosulfonyl-4-chlorophenyl)-5-fluoro-2,4-pyrimidinediamine;
IX-11 N2-(3-aminosulfonyl-4-were)-N4-(3-cyanomethyl-1H-indol-6-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-12 N2-(3-aminosulphonylphenyl)-N4-(3-what manometer-1H-indol-6-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-13 N2-(3-aminosulphonylphenyl)-N4-(3-cyanomethyl-1H-indol-5-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-14 N2-(3-aminosulfonyl-4-were)-N4-(3-cyanomethyl-1H-indol-5-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-15 N2-(3-aminosulphonylphenyl)-N4-(3-cyanomethyl-1H-indol-7-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-16 N2-(3-aminosulfonyl-4-were)-N4-(3-cyanomethyl-1H-indol-7-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-17 N2-[3-aminosulfonyl-4-(4-methylpiperazin-1-yl)phenyl]-N4-(3-cyanomethyl-1H-indol-6-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-18 N2-[3-aminosulfonyl-4-(4-methylpiperazin-1-yl)phenyl]-N4-(3-cyanomethyl-1H-indol-7-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-19 N4-(3-cyanomethyl-1H-indol-5-yl)-5-fluoro-N2-[3-(1-methyl-4-aminopiperidin)sulfonyl-4-were]-2,4-pyrimidinediamine;
IX-20 N2-(3-aminosulfonyl-4-were)-N4-(3-cyanomethyl-1-methyl-indol-5-yl)-5-fluoro-2,4-pyrimidinediamine;
IX-26 N4-[4-(1-acetyl-4-piperidinyl)carbonitril]-N2-(4-aminosulphonylphenyl)-5-fluoro-2,4-pyrimidinediamine;
IX-32 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(1-methanesulfonyl-4-piperazinil)carbonitril]-2,4-pyrimidinediamine;
IX-36 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-[4-(4-thio-morpholinyl)carbonitril]-2,4-pyrimidinediamine;
IX-40 N2-(4-aminosulphonylphenyl)-N4-[4-(1,1-dioxo-4-thiomorpholine)carbonitril]-5-fluoro-2,4-pyrimidinediamine;
IX-41 N4-(4-acetyldeoxynivalenol)-N2-(4-aminosulphonylphenyl)-5-fluoro-2,4-pyrimidinediamine;
IX-44 N2-[2-(4-aminosulphonylphenyl is)-N4-[3,5-dimethyl-4-(4-methylpiperazin-1-yl]phenyl)-5-fluoro-2,4-pyrimidinediamine;
IX-49 N2-(4-aminosulphonylphenyl)-5-fluoro-N4-(5-methoxycarbonyl-thiophene-2-yl)-2,4-pyrimidinediamine;
IX-50 N4-(3,4-acid)-5-fluoro-N2-[4-(N-methyl)amino-sulfonyl-3-methoxyphenyl]-2,4-pyrimidinediamine;
IX-51 N4-(3,5-acid)-5-fluoro-N2-[4-(N-methyl)amino-sulfonyl-3-methoxyphenyl]-2,4-pyrimidinediamine;
IX-52 N4-(4-chloro-3-triptoreline)-5-fluoro-N2-[4-(N-methyl)-aminosulfonyl-3-methoxyphenyl]-2,4-pyrimidinediamine;
IX-53 N4-(3-chloro-4-trifloromethyl)-5-fluoro-N2-[4-(N-methyl)-aminosulfonyl-3-methoxyphenyl]-2,4-pyrimidinediamine;
X-1 6-carbonyloxy-N4-(3,4-dichlorophenyl)-N2-(3-N,N-diethylaminomethyl-6-methoxyphenyl)-2,4-pyrimidinediamine;
X-2 6-carbonyloxy-(3-N,N-diethylaminomethyl-6-methoxyphenyl)-N4-[3-oxo-benzo[1,4]oxazin-6-yl]-2,4-pyrimidinediamine;
X-3 N2-(3-aminosulphonylphenyl)-5-fluoro-N4-(2-methylindol-6-ylmethylene)-2,4-pyrimidinediamine.

12. Pharmaceutical composition for inhibiting the way JAK and inhibition of JAK-kinase, comprising a therapeutically effective amount of a compound according to any one of claims 1 to 11, and at least one pharmaceutically acceptable excipient, diluent, preservative, or stabilizer or a mixture thereof.

13. The composition according to item 12, in which the compound is a compound according to claim 1.

14. The composition according to item 12, in which the compound is a compound according to claim 5.

15. The composition according to item 12, in which the connection is the first connection according to claim 6.

16. A method of inhibiting the activity of a JAK kinase, in which the contacting in vitro JAK kinase with a compound according to any one of claims 1 to 11, in an amount effective for inhibiting the activity of the JAK kinase.

17. The method of inhibition of the cascade of signal transduction involving, JAK3 kinase, in which the contacting in vitro a cell expressing a receptor involved in this cascade of signal transmission, with the compound according to any one of claims 1 to 11.

18. The use of compounds according to any one of claims 1 to 11 in the manufacture of medicinal products for the treatment mediated T-cell autoimmune disease, for treating or preventing allograft rejection in transplant recipient, for the treatment or prevention of hypersensitivity reactions type IV, including the manufacture of the above medicines containing compound according to any one of claims 1 to 11, in an amount effective for the treatment of autoimmune diseases or rejection of the allograft or hypersensitivity reactions type IV.

19. Use p in which the specified rejection is an acute rejection.

20. Use p in which the specified rejection is a chronic rejection.

21. Use p, wherein said allograft is selected from the group consisting of transpla the tat kidney, heart, liver and lung.

22. Use p in which the specified connection used in combination or in addition to another immunosuppressant selected from the group comprising tacrolimus and sirolimus.

23. Use p, in which the introduction of a compound according to any one of claims 1 to 11 in the preventive purposes.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to organic chemistry, namely to new 1,2-dihydroquinoline derivatives of general formula , or to a pharmaceutically acceptable salt thereof, wherein R1 represents a lower alkyl group; R2 represents a hydrogen atom; each of R3 and R4 represents a lower alkyl group; R5 represents a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group; X represents -CO-, -C(O)NR8 - or -S(O)2-; each of R7 and/or R8 may be identical or different, and represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower cycloalkyl group, a phenyl or naphthyl group, a saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, a lower alkoxy group, a phenoxy group; provided R7 and/or R8 represent a lower alkyl group, a lower alkoxy group, the mentioned lower alkyl group and lower alkoxy group may contain one or three groups specified in a halogen atom, a phenyl group, an unsubstituted monocyclic 6-member heterocyclyl with one heteroatom specified in a nitrogen atom, and 5 carbon atoms in a cycle, a lower alkoxy group, and -NRaRb as a substitute (substitutes); provided R7 and/or R8 represent a phenyl group, a saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, a phenoxy group, the mentioned phenyl group, saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, phenoxy group may contain one or two groups specified in a halogen atom, a lower alkyl group, a halogen-substituted lower alkyl group, a phenyl group, a hydroxyl group, a lower alkoxy group, a halogen-substituted lower alkoxy group, a lower alkylthio group, a lower alkylcarbonyl group, a lower alkoxycarbonyl group, a lower alkylcarbonyloxy group, -NRaRb, a nitro group and a cyano group as a substitute (substitutes); Ra and Rb may be identical or different, and each of them represents a hydrogen atom, a lower alkyl group, a lower alkoxycarbonyl group; Y represents a lower alkylene group; Z represents an oxygen atom; p is equal to 2, provided p is equal to 2, R6 may be identical or different. The invention also relates to a pharmaceutical composition and a glucocorticoid receptor modulator of the compound of formula (1).

EFFECT: there are produced new 1,2-dihydroquinoline derivatives possessing glucocorticoid receptor binding activity.

7 cl, 1 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pyrrol derivatives of formula (1): or a pharmaceutically acceptable salt thereof wherein the values A, R1-R3, n are specified in clause 1 of the patent claim.

EFFECT: compounds (1) inhibit activity against the interleukin IL-6 production that allows using them both in pharmaceutical compositions, and in a prophylactic drug for ocular inflammatory disease.

23 cl, 2 tbl, 22 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing substituted pyrimidin-5-yl carboxylic acids of formula I and can be used in organic chemistry. The method is realised by reacting N-substituted guanidines and hetarylamidines with ethoxymethylene derivatives of 1,3-ketoesters according to a scheme given below (where the substitutes are as defined in the claim).

EFFECT: improved method of producing substituted pyrimidin-5-yl carboxylic acids of formula I.

2 tbl, 14 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to organic chemistry and specifically to a method of producing M-(1,5,3-dithiazepan-3-yl)amides of general formula (1) where R = p-C5H4N (a), (CH3)3CO (b), o-CH3OC6H4 (c), which involves reaction of N1,N1,N6,N6-tetramethyl-2,5-dithiahexane-1,6-diamine with a hydrazide of general formula RC(O)NHNH2 [R is as described above] in the presence of a samarium nitrate crystalline hydrate Sm(NO3)3·6H2O catalyst with molar ratio N1,N1,N6,N6-tetramethyl-2,5-dithiahexane-1,6-diamine:RC(O)NHNH2:Sm(NO3)3·6H2O=10:10:(0.3-0.7) at temperature of 65-75°C and atmospheric pressure in the mixture of solvents - ethyl alcohol and chloroform for 20-28 hours.

EFFECT: method of producing N-(1,5,3-dithiazepan-3-yl)amides with high selectivity and output, which can be used as biologically active compounds, selective sorbents and extractants of noble and precious metals.

1 cl, 1 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds for treating cell-proliferative disorders having formula (II): wherein the values R1,R2, X, A, B, R6, R7, R9 are specified in cl. 1 of the patent claim with the exception of the compound of formula: .

EFFECT: there are presented compounds possessing anticancer activity.

95 cl, 27 dwg, 11 tbl, 9 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to organic chemistry and specifically to a method of producing N-(1,5,3-dithiazepinan-3-yl)amides of general formula (1): where R = p-C5H4N (a), (CH3)3CO (b), o-CH3OC6H4 (c) which involves reaction of t-butyl-1,5,3-dithiazepinane with a hydrazide of general formula RC(O)NHNH2 [R is as described above] in the presence of an iron chloride crystalline hydrate catalyst FeCl3-6H2O in molar ratio t-butyl-1,5,3-dithiazepinane:RC(O)NHNH2:FeCl3-6H2O=10:10:(0.3-0.7) at temperature of 65-75°C and atmospheric pressure of a mixture of solvents - ethyl alcohol-chloroform for 40-48 hours.

EFFECT: novel method of producing N-(1,5,3-dithiazepinan-3-yl)amides with high selectivity and output, which can be used as biologically active compounds, selective sorbents and extractants of noble and precious metals.

1 cl, 1 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of general formula (I), wherein A represents a pyrrole group or a pyrazole group, and X represents a carbon atom or a nitrogen atom; R1 represents a carboxy group; R2 independently represents a group specified in a substitute group α; R3 independently represents phenyl(C1-C6alkyl)group substituted by, phenyl(C1-C6alkyl)group (wherein the substitute(s) represents (represent) 1-4 groups independently specified in the substitute group α); m is equal to 0, 1, 2 or 3, n is equal to 0 or 1; each of R4, R5, R6 and R7 independently represents a hydrogen atom, C1-C6alkyl group or a halogen atom; B represents a substituted naphthyl group (wherein the substitute(s) represents (represent) 1-4 groups independently specified in the substitute group α), or the group represented by formula (II), wherein B1, B2 and α are those as specified in the patent claim. Also, the invention refers to a pharmaceutical composition possessing lipolysis inhibiting activity, to the use of the compounds of formula (I) in preparing a drug preparation for treating hyperlipidemia, dislipidemia, abnormal lipid metabolism, arteriosclerosis or type II diabetes mellitus and to a method of treating or preventing the mentioned diseases.

EFFECT: preparing the compounds of formula (I) possessing lipolysis inhibiting activity.

36 cl, 1 dwg, 1 tbl, 69 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound selected from a group consisting of: 4-[(2-{[(2S)-2-fluoropropyl](pyridin-2-ylsulfonyl)amino}-4,5-dimethylphenoxy)methyl]benzoic acid, 4-[(2-{[(2R)-2-fluoropropyl](pyridin-2-ylsulfonyl)amino}-4,5-dimethylphenoxy)methyl]benzoic acid, 4-{[(6-{[(2R)-2-fluoropropyl](pyridin-2-ylsulfonyl)amino}-2,3-dihydro-1H-inden-5-yl)oxy)methyl} benzoic acid, 4-[(5-chlor-2-{[(2S)-2-fluoropropyl](pyridin-2-ylsulfonyl)amino}-4-methylphenoxy)methyl]benzoic acid, 4-[(5-chlor-2-{[(2R)-2-fluoropropyl](pyridin-2-ylsulfonyl)amino}-4-methylphenoxy)methyl]benzoic acid, 4-[(2-{[(2R)-3-fluor-2- methylpropyl](pyridin-2-ylsulfonyl)amino}-4,5-dimethylphenoxy)methyl]benzoic acid, 4-[(2-{[(2S)-3-fluor-2- methylpropyl](pyridin-2-ylsulfonyl)amino}-4,5-dimethylphenoxy)methyl]benzoic acid, 4-{[(6-{[(2R)-2-fluorobutyl](pyridin-2-ylsulfonyl)amino}-2,3-dihydro-1H-inden-5-yl)oxy)methyl} benzoic acid, 4-{[(6-{[(2S)-2-fluorobutyl](pyridin-2-ylsulfonyl)amino}-2,3-dihydro-1H-inden-5-yl)oxy)methyl}benzoic acid, 4-[(5-chlor-2-{[(2R)-2-fluoropropyl] (pyridin-3-ylsulfonyl)amino}-4-methylphenoxy)methyl]benzoic acid, 4-[(5-chlor- 2-{[(2S)-2-fluoropropyl](pyridin-3-ylsulfonyl)amino}-4-methylphenoxy)methyl] benzoic acid, 4-[(2-{[(2S)-2-fluoropropyl](pyridin-3-ylsulfonyl)amino}-4,5-dimethylphenoxy)methyl]benzoic acid, 4-[(2-{[(2R)-2-fluoropropyl](pyridin-3-ylsulfonyl)amino}-4,5-dimethylphenoxy)methyl] benzoic acid, 4-{[(6-{[(2S)-2-fluoropropyl](pyridin-3-ylsulfonyl)amino}-2,3-dihydro-1H-inden-5-yl)oxy)methyl} benzoic acid and 4-{[(6-{[(2R)-2-fluoropropyl](pyridin-3-ylsulfonyl)amino}-2,3-dihydro-1H-inden-5-yl)oxy)methyl}benzoic acid, or a pharmaceutically acceptable salt thereof. These compounds have an EP1 receptor antagonist effect and may be used for treating the dysfunction pollakiuria.

EFFECT: preparing the sulfonamide compounds with a strong EP1 receptor antagonist effect.

23 cl, 24 tbl, 31 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new pyrimidine derivatives and their pharmaceutically acceptable salts possessing the properties of a HIV replication inhibitor. In formula (I'): , R1 means a hydrogen atom; R7 means a hydrogen atom; C1-6alkyl; R8 means a hydrogen atom; C1-6alkyl; R4 means cyano; R9 means -CH=CH-CN; R5 means C3-7cycloalkyl; C1-6alkyloxy; aryl; Het; C1-6alkyl substituted by a radical specified in hydroxy, C1-6alkyloxy, cyano, amino, mono- and di-C1-6alkylamino, C1-6alkylcarbonylamino, aryl, Het, dioxoalanine optionally substituted by one or two C1-6alkyl radicals, tetrahydrofuranyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl optionally substituted by C1-6alkyl or C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, aryl C1-6alkyloxycarbonyl and C3-7cycloalkyl; or R5 means C1-6alkyl substituted by two C1-6alkyloxy radicals; R6 means a hydrogen atom or C1-6alkyl; X means -NR1- or -O; the values of Het are presented in the patent claim. The invention also refers to a pharmaceutical composition containing said compounds.

EFFECT: preparing the pharmaceutically acceptable salts possessing the properties of a HIV replication inhibitor.

9 cl, 2 tbl, 7 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing 2,2'-dibenzthiazolyl-disulphide via electrochemical oxidation of an alkaline solution of 2-mercaptobenzthiazole at temperature of 70°C and current density of 1 A/cm2, wherein the process is carried out on alternating current with frequency of 55…575 Hz, preferably 100…120 Hz and more preferably 105…115 Hz. The highest current output is achieved using alternating current with frequency of 110 Hz.

EFFECT: high efficiency of the electrolysis cell, reduced electric power consumption, avoiding use of toxic and expensive reagents.

2 cl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to organic chemistry, namely to new 1,2-dihydroquinoline derivatives of general formula , or to a pharmaceutically acceptable salt thereof, wherein R1 represents a lower alkyl group; R2 represents a hydrogen atom; each of R3 and R4 represents a lower alkyl group; R5 represents a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group; X represents -CO-, -C(O)NR8 - or -S(O)2-; each of R7 and/or R8 may be identical or different, and represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower cycloalkyl group, a phenyl or naphthyl group, a saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, a lower alkoxy group, a phenoxy group; provided R7 and/or R8 represent a lower alkyl group, a lower alkoxy group, the mentioned lower alkyl group and lower alkoxy group may contain one or three groups specified in a halogen atom, a phenyl group, an unsubstituted monocyclic 6-member heterocyclyl with one heteroatom specified in a nitrogen atom, and 5 carbon atoms in a cycle, a lower alkoxy group, and -NRaRb as a substitute (substitutes); provided R7 and/or R8 represent a phenyl group, a saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, a phenoxy group, the mentioned phenyl group, saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, phenoxy group may contain one or two groups specified in a halogen atom, a lower alkyl group, a halogen-substituted lower alkyl group, a phenyl group, a hydroxyl group, a lower alkoxy group, a halogen-substituted lower alkoxy group, a lower alkylthio group, a lower alkylcarbonyl group, a lower alkoxycarbonyl group, a lower alkylcarbonyloxy group, -NRaRb, a nitro group and a cyano group as a substitute (substitutes); Ra and Rb may be identical or different, and each of them represents a hydrogen atom, a lower alkyl group, a lower alkoxycarbonyl group; Y represents a lower alkylene group; Z represents an oxygen atom; p is equal to 2, provided p is equal to 2, R6 may be identical or different. The invention also relates to a pharmaceutical composition and a glucocorticoid receptor modulator of the compound of formula (1).

EFFECT: there are produced new 1,2-dihydroquinoline derivatives possessing glucocorticoid receptor binding activity.

7 cl, 1 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pyrrol derivatives of formula (1): or a pharmaceutically acceptable salt thereof wherein the values A, R1-R3, n are specified in clause 1 of the patent claim.

EFFECT: compounds (1) inhibit activity against the interleukin IL-6 production that allows using them both in pharmaceutical compositions, and in a prophylactic drug for ocular inflammatory disease.

23 cl, 2 tbl, 22 ex

FIELD: chemistry.

SUBSTANCE: invention relates to N-hydroxylsulphonamide derivatives of formula or , where R1 is H; R2 is H; n is 0; b is an integer in the range of 1-4; R3, R4, R5, R6 and R7 are independently selected from H, halogen, carboxyl, carboxyl ester selected from a group including -C(O)O-morpholino, -C(O)O-C1-C8alkyl and -C(O)O-substituted C1-C8alkyl, where the substitute is morpholino; acylamino, which is a -C(O)NRaRb group, where Ra and Rb are independently C1-C8alkyl, or Ra and Rb together with a nitrogen atom to which they are bonded form morpholino; and sulphonylamino, which is a SO2NR2 group, where two groups R, together with a nitrogen atom to which they are bonded, form morpholino; R8 is selected from halogen and carbonylamino, selected from a -CONH-substituted C1-C8alkyl, where the substitute is morpholino; and -CONR2, where two groups R, together with a nitrogen atom to which they are bonded, form morpholino; C is a heteroaromatic ring which contains cyclic fragments Q9, Q10, Q11, Q12, Q13 and Q14, which are independently selected from C, CH and S, under the condition that at least one of the fragments Q9, Q10, Q11, Q12, Q13 and Q14 is S. The invention also relates to a method of modulating nitroxyl levels, a method of treating diseases which respond to treatment with nitroxyl, a treatment set and a pharmaceutical composition containing compounds of formula (I) or (III).

EFFECT: compounds of formula (I) or (III) for treating diseases which respond to treatment with nitroxyl.

20 cl, 5 ex, 4 tbl, 7 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing substituted pyrimidin-5-yl carboxylic acids of formula I and can be used in organic chemistry. The method is realised by reacting N-substituted guanidines and hetarylamidines with ethoxymethylene derivatives of 1,3-ketoesters according to a scheme given below (where the substitutes are as defined in the claim).

EFFECT: improved method of producing substituted pyrimidin-5-yl carboxylic acids of formula I.

2 tbl, 14 ex

FIELD: chemistry.

SUBSTANCE: invention relates to isoxazole-pyridine derivatives of formula , where X; R1; R2, R3, R4, R5 and R6 are as described in claim 1 of the invention and a pharmaceutically acceptable salt thereof. The invention also relates to a medicinal agent for treating diseases associated with the binding site of the GABA A α5 receptor based on compounds of formula I and use of said compounds in preparing a medicinal agent.

EFFECT: novel compounds are active towards the binding site of said receptor and are useful in treating cognitive disorders such as Alzheimer's disease.

22 cl, 372 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of general formula (I), wherein A represents a pyrrole group or a pyrazole group, and X represents a carbon atom or a nitrogen atom; R1 represents a carboxy group; R2 independently represents a group specified in a substitute group α; R3 independently represents phenyl(C1-C6alkyl)group substituted by, phenyl(C1-C6alkyl)group (wherein the substitute(s) represents (represent) 1-4 groups independently specified in the substitute group α); m is equal to 0, 1, 2 or 3, n is equal to 0 or 1; each of R4, R5, R6 and R7 independently represents a hydrogen atom, C1-C6alkyl group or a halogen atom; B represents a substituted naphthyl group (wherein the substitute(s) represents (represent) 1-4 groups independently specified in the substitute group α), or the group represented by formula (II), wherein B1, B2 and α are those as specified in the patent claim. Also, the invention refers to a pharmaceutical composition possessing lipolysis inhibiting activity, to the use of the compounds of formula (I) in preparing a drug preparation for treating hyperlipidemia, dislipidemia, abnormal lipid metabolism, arteriosclerosis or type II diabetes mellitus and to a method of treating or preventing the mentioned diseases.

EFFECT: preparing the compounds of formula (I) possessing lipolysis inhibiting activity.

36 cl, 1 dwg, 1 tbl, 69 ex

FIELD: chemistry.

SUBSTANCE: invention relates to pyrazinone derivatives of formula (I):

, where R1, R2, R3, R4, R5, R and R7 are as defined in claim 1 of the invention. The invention also describes a crystalline form, compounds of formula I, use of the compound of formula I in producing a medicinal agent for treating chronic obstructive pulmonary disease. A pharmaceutical composition and a pharmaceutical product are also described. Methods of obtaining compounds of formula I are also described.

EFFECT: novel compounds which can be used in therapy are obtained and described.

20 cl, 334 ex, 15 tbl, 12 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of general formula (1) and pharmaceutically acceptable salts thereof, which exhibit inhibitory activity on phospholipase A2 enzyme and therefore have prostaglandin and/or leucotriene production suppressing action. In formula X is a halogen atom, cyano group, C1-C3 alkyl group, which can be substituted with halogen atoms, C1-C3 alkoxy group or hydroxy group, C2-C4 alkenyl group, C1-C3 alkoxy group or hydroxy group; Y is a hydrogen atom or C1-C3 alkyl group; Z is C1-C3 alkyl group; G is selected from formulae and , where in formulae (G2) and (G5) R4 is a hydrogen atom or C1-C6 alkyl group which can be substituted with halogen atoms; D is -NR10C(O)-, -C(O)NR10-, -S(O)2NR10- or -N(R11)-; R10 is a hydrogen atom; R11 is a hydrogen atom or C1-C3 alkyl group; A is a single bond, C1-C6 alkylene, which can be substituted with a phenyl group, or C2-C4 alkenylene; Q is a phenyl group or a 5-6-member aromatic heterocyclic group containing 1-3 heteroatoms selected from N, O, S, optionally substituted with a benzene ring; R5, R6 and R7 all or independently denote a hydrogen atom, a halogen atom, C1-C6 alkyl group which can be substituted with halogen atoms, C1-C6 alkoxy group which can be substituted with halogen atoms, phenyloxy group, phenyl group or a 5-6-member aromatic heterocyclic group containing 1-3 heteroatoms selected from N, O, where said phenyl group and 5-6-member aromatic heterocyclic group can be substituted with a C1-C3 alkyl group which can be substituted with halogen atoms or a C1-C3 alkoxy group. The invention also relates to specific compounds, a medicinal agent, a pharmaceutical composition, a phospholipase A2 enzyme activity inhibitor and a treatment method.

EFFECT: improved method.

21 cl, 56 tbl, 561 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to novel tetrahydroisoquinolin-1-one derivatives of general formula or pharmaceutically acceptable salts thereof, where R1 is: lower alkylene-OH, lower alkylene-N(R0)(R6), lower alkylene-CO2R0, C5-6cycloalkyl, C6-10cycloalkenyl, aryl, heterocyclic group, -(lower alkylen, substituted OR0)-aryl or lower alkylene-heterocyclic group, where the lower alkylene in R1 can be substituted with 1-2 groups G1; cycloalkyl, cycloalkenyl and heterocyclic group in R1 can be substituted with 1-2 groups G2; aryl can be substituted with 1-2 groups G3; R0: identical or different from each other, each denotes H or a lower alkyl; R6: R0, or -S(O)2-lower alkyl, R2 is: lower alkyl, lower alkylene-OR0, lower alkylene-aryl, lower alkylene-O-lower alkylene-aryl, -CO2R0, -C(O)N(R0)2, -C(O)N(R0)-aryl, -C(O)N(R0)-lower alkylene-aryl, aryl or heterocyclic group, where the aryl in R2 can be substituted with 1-3 groups G4; R3 is: H or lower alkyl, or R2 and R3 can be combined to form C5-alkylene; R4 is: -N(R7)(R8), -N(R10)-OR7, -N(R0)-N(R0)(R7), -N(R0)-S(O)2-aryl or -N(R0)-S(O)2-R7, R7 is: lower alkyl, halogen-lower alkyl, lower alkylene-CN, lower alkylene-OR0, lower alkylene-CO2R0, lower alkylene-C(O)N(R0)2, lower alkylene-C(O)N(R0)N(R0)2, lower alkylene-C(=NOH)NH2, heteroaryl, lower alkylene-X-aryl or lower alkylene-X-heterocyclic group, where the lower alkylene in R7 can be substituted with 1-2 groups G1; aryl, heteroaryl and heterocyclic group in R7 can be substituted with 1-2 groups G6; X is: a single bond, -O-, -C(O)-, -N(R0)-, -S(O)p- or *-C(O)N(R0)-, where * in X has a value ranging from a bond to a lower alkylene, m is: an integer from 0 to 1, p is: is 2, R8 is: H, or R7 and R6 can be combined to form a lower alkylene-N(R9)-lower alkylene group, R9 is: aryl, R10 is: H, R5 is: lower alkyl, halogen, nitro, -OR0, -N(R0)2, or -O-lower alkylene-aryl, where the group G1 is: -OR0, N(R0)(R6) and aryl; group G2 is: lower alkyl, lower alkylene-OR0, -OR0, -N(R0)2, -N(R0)-lower alkylene-OR0, -N(R0)C(O)OR0, -N(R0)C(O)-lower alkylene-OR0, -N(R0)C(O)N(R0)2, -N(R0)C(=NR0)-lower alkyl, -N(R0)S(O)2-lower alkyl, -N(lower alkylene-CO2R0)-S(O)2-lower alkyl, -N(R0)S(O)2-aryl, -N(R0)S(O)2N(R0)2, -S(O)2-lower alkyl, -CO2R0, -CO2-lower alkylene-Si(lower alkyl)3, -C(O)N(R0)2, -C(O)N(R0)-lower alkylene-OR0, -C(O)N(R0)-lower alkylene-N(R0)2, -C(O)N(R0)-lower alkylene-CO2R0, -C(O)N(R0)-O-lower alkylene-heterocyclic group, -C(O)R0, -C(O)-lower alkylene-OR0, C(O)-heterocyclic group and oxo; under the condition that "aryl" in group G2 can be substituted with one lower alkyl; group G3 is: -OR0; group G4 is: halogen, CN, nitro, lower alkyl, -OR0, -N(R0)2) -CO2R0; group G5 is: halogen, -OR0, -N(R0)2 and aryl; group G6 is: halogen, lower alkyl which can be substituted with -OR0, halogen-lower alkyl which is substituted with -OR0, -OR0, -CN, -N(R0)2, -CO2R0, -C(O)N(R0)2, lower alkylene-OC(O)R0, lower alkylene-OC(O)-aryl, lower alkylene-CO2R0, halogen-lower alkylene-CO2R0, lower alkylene-C(O)]N(R0)2, halogen-lower alkylene-C(O)N(R0)2, -O-lower alkylene-CO2R0, -O-lower alkylene-CO2-lower alkylene-aryl, -C(O)N(R0)S(O)2-lower alkyl, lower alkylene-C(O)N(R0)S(O)2-lower alkyl, -S(O)2-lower alkyl, -S(O)2N(R0)2, heterocyclic group, -C(-NH)=NO-C(O)O-C1-10-alkyl, -C(=NOH)NH2, C(O)N=C(N(R0)2)2, -N(R0)C(O)R0, -N(R0)C(O)-lower alkylene-OR0, -N(R0)C(O)OR0, -C(aryl)3 and oxo; under the condition that the "heterocyclic group" in group G6 is substituted with 1 group selected from a group consisting of -OR0, oxo and thioxo (=S); where the "cycloalkenyl" relates to C5-10 cycloalkenyl, including a cyclic group which is condensed with a benzene ring at the site of the double bond; the "aryl" relates to an aromatic monocyclic C6-hydrocarbon group; the "heterocyclic group" denotes a cyclic group consisting of i) a monocyclic 5-6-member heterocycle having 1-4 heteroatoms selected from O, S and N, or ii) a bicyclic 8-9-member heterocycle having 1-3 heteroatoms selected from O, S and N, obtained via condensation of the monocyclic heterocycle and one ring selected from a group consisting of a monocyclic heterocycle, a benzene ring, wherein the N ring atom can be oxidised to form an oxide; the "heteroaryl" denotes pyridyl or benzimidazolyl; provided that existing compounds given in claim 1 of the invention are excluded. The invention also relates to a pharmaceutical composition based on the compound of formula (I), use of the compound of formula (I) and a method of treatment using the compound of formula (I).

EFFECT: obtaining novel tetrahydroisoquinolin-1-one derivatives which are useful as a BB2 receptor antagonist.

11 cl, 302 tbl, 59 ex

FIELD: chemistry.

SUBSTANCE: invention relates to substituted N-phenylpyrrolidinyl methylpyrrolidine amides of formula , where R, R1, R2 and R3 are identical or different and independently denote H, (C1-C4)alkyl, CF3; R4 denotes phenyl, cyclohexyl, pyridinyl, furanyl, isoxazolyl, quinolinyl, naphthyridinyl, indolyl, benzoimidazolyl, benzofuranyl, chromanyl, 4-oxo-4H-chromenyl, 2,3-dihydrobenzofuranyl, benzo[1,3]dioxolyl and 2,5-dioxo-2,3,4,5-tetrahydro-1H-benzo[e]][1,4]diazepinyl; where said R4 is optionally substituted one to more times with a substitute selected from halogen, hydroxy, (C1-C4) alkyl, (C1-C4) alkoxy, CF3, hydroxymethyl, 2-hydroxyethylamino, methoxyethylamide, benzyloxymethyl, piperidinyl, N-acetylpiperidinyl, pyrrolyl, imidazolyl, 5-oxo-4,5-dihydropyrazolyl; or pharmaceutically acceptable salt thereof or enantiomer or diastereomer thereof.

EFFECT: compounds have modulating activity on histamine H3 receptor, which enables use thereof to prepare a pharmaceutical composition.

10 cl, 3 dwg, 29 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds for treating cell-proliferative disorders having formula (II): wherein the values R1,R2, X, A, B, R6, R7, R9 are specified in cl. 1 of the patent claim with the exception of the compound of formula: .

EFFECT: there are presented compounds possessing anticancer activity.

95 cl, 27 dwg, 11 tbl, 9 ex

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