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Claims for Patent: 7,893,074

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Claims for Patent: 7,893,074

Title:2, 4-pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders
Abstract: Novel pyrimidine derivatives of formula I ##STR00001## to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
Inventor(s): Garcia-Echeverria; Carlos (Basel, CH), Kanazawa; Takanori (Tsukuba, JP), Kawahara; Eiji (Tsukuba, JP), Masuya; Keiichi (Tsukuba, JP), Matsuura; Naoko (Tsukuba, JP), Miyake; Takahiro (Tsukuba, JP), Ohmori; Osamu (Tsukuba, JP), Umemura; Ichiro (Tsukuba, JP), Steensma; Ruo (La Jolla, CA), Chopiuk; Greg (San Diego, CA), Jiang; Jiqing (San Diego, CA), Wan; Yongqin (Irvine, CA), Ding; Qiang (San Diego, CA), Zhang; Qiong (San Diego, CA), Gray; Nathanael Schiander (San Diego, CA), Karanewsky; Donald (Escondido, CA)
Assignee: Novartis AG (Basel, CH) IRM LLC (Hamilton, BM)
Application Number:10/568,367
Patent Claims: 1. A compound of formula I ##STR01007## wherein each of R.sup.0, R.sup.1, and R.sup.2 independently is hydrogen, --S(O).sub.0-2NR.sub.12R.sub.13, --S(O).sub.0-2R.sub.13, --NR.sub.12S(O).sub.0-2R.sub.13 or --C(O)NR.sub.12R.sub.13; R.sup.3 is --S(O).sub.0-2R.sub.13 or --C(O)NR.sub.12R.sub.13; wherein R.sub.12 is selected from hydrogen and C.sub.1-6alkyl; and R.sub.13 is selected from hydrogen, C.sub.1-6alkyl and C.sub.3-12cycloalkyl; R.sup.4 is hydrogen; each of R.sup.5 and R.sup.6 independently is hydrogen or halogen; and each of R.sup.7, R.sup.8, R.sup.9, and R.sup.10 independently is ethoxy, ethyl, propyl, t-butyl, trifluoromethyl, nitrile, cyclobutyloxy, 2,2,2-trifluoroethoxy, isobutyloxy, t-butyloxy, isopropyloxy, methyl-amino-carbonyl, cyclopropyl-methoxy, dimethylamino-propyl-amino, methoxy-ethoxy, --XR.sub.11, --C(O)R.sub.11 or --OXR.sub.11; wherein X is a bond, methylene or ethylene; R.sub.11 is selected from piperazinyl, piperidinyl, pyrrolidinyl, morpholino, azepanyl and 1,4-dioxa-8-aza-spiro[4.5]dec-8-yl; wherein R.sub.11 is optionally substituted by 1 to 3 radicals independently selected from methyl, isopropyl, acetyl, acetyl-methyl-amino, 3-dimethylamino-2,2-dimethyl-propylamino, ethyl-methyl-amino-ethoxy, diethyl-amino-ethoxy, amino-carbonyl, ethyl, 2-oxo-pyrrolidin-1-yl, pyrrolidinyl, pyrrolidinyl-methyl, piperidinyl optionally substituted with methyl or ethyl, morpholino, dimethylamino, dimethylamino-propyl-amino, methyl-amino and ethyl-amino; wherein one of R.sup.7, R.sup.8 and R.sup.9 independently of each other can also be hydrogen; A is C; or salts thereof.

2. A compound of formula I according to claim 1, wherein each of R.sup.0 or R.sup.2 independently is hydrogen; R.sup.1 is hydrogen; and R.sup.3 is selected from propyl-sulfonyl, ethyl-amino-carbonyl, cyclohexyl-sulfonyl, and isopropyl-sulfonyl.

3. A pharmaceutical composition comprising a compound according to claim 1, as active ingredient together with one or more pharmaceutically acceptable diluents or carriers.

4. A combination comprising a therapeutically effective amount of a compound according to claim 1 and one or more further known drug substances, said further drug substance being useful in the treatment of neoplastic diseases or immune system disorders.

5. A method for the treatment of breast tumor in a subject in need thereof which comprises administering an effective amount of a compound according to claim 1.

6. A compound of Formula I' ##STR01008## in which: n' is selected from 1 and 2; R'.sub.1 is selected from phenyl, pyridinyl, pyrazolyl and pyrimidinyl; wherein the phenyl, pyridinyl, pyrazolyl and pyrmidinyl of R'.sub.1 is substituted by 2 to 3 radicals independently selected from ethoxy, ethyl, propyl, methyl, t-butyl, trifluoromethyl, nitrile, cyclobutyloxy, 2,2,2-trifluoroethoxy, isobutyloxy, t-butyloxy, isopropyloxy, methyl-amino-carbonyl, cyclopropyl-methoxy, dimethylamino-propyl-amino, methoxy-ethoxy, --X'R'.sub.4, --C(O)R'.sub.4 and --OX'R'.sub.4; wherein X' is a bond, methylene or ethylene; R'.sub.4 is selected from piperazinyl, piperidinyl, pyrrolidinyl, morpholino, azepanyl and 1,4-dioxa-8-aza-spiro[4.5]dec-8-yl; wherein R'.sub.4 is optionally substituted by 1 to 3 radicals independently selected from methyl, isopropyl, acetyl, acetyl-methyl-amino, 3-dimethylamino-2,2-dimethyl-propylamino, ethyl-methyl-amino-ethoxy, diethyl-amino-ethoxy, amino-carbonyl, ethyl, 2-oxo-pyrrolidin-1-yl, pyrrolidinyl, pyrrolidinyl-methyl, piperidinyl optionally substituted with methyl or ethyl, morpholino, dimethylamino, dimethylamino-propyl-amino, methyl-amino and ethyl-amino R'.sub.2 is selected from hydrogen and halo; R'.sub.3 is selected from propyl-sulfonyl, ethyl-amino-carbonyl, cyclohexyl-sulfonyl, and isopropyl-sulfonyl; or the pharmaceutically acceptable salts thereof; with the proviso that the compound of Formula I' is not ##STR01009## wherein Rx is ##STR01010##

7. A pharmaceutical composition comprising a compound according to claim 6, as active ingredient together with one or more pharmaceutically acceptable diluents or carriers.

8. A combination comprising a therapeutically effective amount of a compound according to claim 6 and one or more further known drug substances, said further drug substance being useful in the treatment of neoplastic diseases or immune system disorders.

9. A method for the treatment of breast tumor in a subject in need thereof which comprises administering an effective amount of a compound according to claim 6.
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