RU2008121974A - Соединения и композиции в качестве ингибиторов протеинкиназ - Google Patents
Соединения и композиции в качестве ингибиторов протеинкиназ Download PDFInfo
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- RU2008121974A RU2008121974A RU2008121974/04A RU2008121974A RU2008121974A RU 2008121974 A RU2008121974 A RU 2008121974A RU 2008121974/04 A RU2008121974/04 A RU 2008121974/04A RU 2008121974 A RU2008121974 A RU 2008121974A RU 2008121974 A RU2008121974 A RU 2008121974A
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- Prior art keywords
- pyrimidin
- phenyl
- ylamino
- halogen
- amide
- Prior art date
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- 150000001875 compounds Chemical class 0.000 title claims abstract 12
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 239000003909 protein kinase inhibitor Substances 0.000 title 1
- -1 —NHC (O) R3 Chemical class 0.000 claims abstract 26
- 125000004178 (C1-C4) alkyl group Chemical class 0.000 claims abstract 14
- 125000000229 (C1-C4)alkoxy group Chemical class 0.000 claims abstract 12
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims abstract 8
- 229910052736 halogen Inorganic materials 0.000 claims abstract 8
- 150000002367 halogens Chemical class 0.000 claims abstract 8
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 8
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 8
- 239000001301 oxygen Substances 0.000 claims abstract 8
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims abstract 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims abstract 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 4
- XTHBFKDDURQBLJ-UHFFFAOYSA-N 4-n,6-n-bis[3-(trifluoromethyl)phenyl]pyrimidine-4,6-diamine Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(C=CC=3)C(F)(F)F)C=2)=C1 XTHBFKDDURQBLJ-UHFFFAOYSA-N 0.000 claims abstract 2
- 150000004677 hydrates Chemical class 0.000 claims abstract 2
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 239000012453 solvate Substances 0.000 claims abstract 2
- 238000000034 method Methods 0.000 claims 3
- WEVYNIUIFUYDGI-UHFFFAOYSA-N 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide Chemical compound NC(=O)C1=CC=CC(C=2N=CN=C(NC=3C=CC(OC(F)(F)F)=CC=3)C=2)=C1 WEVYNIUIFUYDGI-UHFFFAOYSA-N 0.000 claims 2
- 208000031295 Animal disease Diseases 0.000 claims 2
- 101100123850 Caenorhabditis elegans her-1 gene Proteins 0.000 claims 2
- 102000002427 Cyclin B Human genes 0.000 claims 2
- 108010068150 Cyclin B Proteins 0.000 claims 2
- 102100032857 Cyclin-dependent kinase 1 Human genes 0.000 claims 2
- 101710106279 Cyclin-dependent kinase 1 Proteins 0.000 claims 2
- 101100481408 Danio rerio tie2 gene Proteins 0.000 claims 2
- 108700012928 MAPK14 Proteins 0.000 claims 2
- 102000054819 Mitogen-activated protein kinase 14 Human genes 0.000 claims 2
- 101100335081 Mus musculus Flt3 gene Proteins 0.000 claims 2
- 101100481410 Mus musculus Tek gene Proteins 0.000 claims 2
- 101150056950 Ntrk2 gene Proteins 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 101150071831 RPS6KA1 gene Proteins 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 230000007170 pathology Effects 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- OMJPKBHPEZBRLI-UHFFFAOYSA-N 2-n,4-n-bis[3-(trifluoromethyl)phenyl]pyridine-2,4-diamine Chemical compound FC(F)(F)C1=CC=CC(NC=2C=C(NC=3C=C(C=CC=3)C(F)(F)F)N=CC=2)=C1 OMJPKBHPEZBRLI-UHFFFAOYSA-N 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- YMGUBTXCNDTFJI-UHFFFAOYSA-N cyclopropanecarboxylic acid Chemical compound OC(=O)C1CC1 YMGUBTXCNDTFJI-UHFFFAOYSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
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- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract
1. Соединение формулы I ! ! в котором n выбран из 1, 2 и 3, ! m выбран из 1, 2 и 3, ! X1 выбран из связи, кислорода, NH и N(СН3), ! Х2 выбран из кислорода и NH, ! Y выбран из азота и СН, ! R1 выбран из галоидзамещенного (С1-С4)алкила, галоидзамещенной (С1-С4)алкоксигруппы, (С1-С4)алкила, галоида и (С1-С4)алкоксигруппы, ! R2 выбран из галоидзамещенного (С1-С4)алкила, галоидзамещенной (С1-С4)алкоксигруппы, (С1-С4)алкила, галоида, (С1-С4)алкоксигруппы и -NHC(O)R3, где R3 является (С3-С12) циклоалкилом, ! а также его фармацевтически приемлемые соли, гидраты, сольваты и изомеры. ! 2. Соединение согласно п.1, в котором ! n выбран из 1 и 2, ! m выбран из 1 и 2, ! X1 выбран из связи, кислорода, NH и N(CH3), ! Х2 выбран из кислорода и NH, ! Y выбран из азота и СН, ! R1 выбран из галоидзамещенного (С1-С4)алкила, (С1-С4)алкила, галоида и (С1-С4)алкоксигруппы, ! R2 выбран из галоидзамещенного (С1-С4)алкила, -NHC(O)R3 и (С1-С4)алкоксигруппы, где R3 является (С3-С12) циклоалкилом. ! 3. Соединение согласно п.2, в котором R1 выбран из циклопропилкарбониламиногруппы, циклогексилкарбониламиногруппы, трифторметила и метоксигруппы, а R2 выбран из трифторметила, метила, галоида и метоксигруппы. ! 4. Соединение согласно п.1, выбранное из {3-[6-(3-трифторметилфениламино)пиримидин-4-иламино]фенил}амида циклопропанкарбоновой кислоты, N,N'-бис(3-трифторметилфенил)пиримидин-4,6-диамина, {2-метокси-5-[6-(3-трифторметилфениламино)пиримидин-4-иламино]фенил}амида циклопропанкарбоновой кислоты, {2-метокси-5-[6-(3-трифторметилфениламино)пиримидин-4-иламино]фенил}амида циклогексанкарбоновой кислоты, [3-(6-о-толиламинопиримидин-4-иламино)фенил]амида циклопропанкарбоновой кислоты, {3-[6-(2-хлорфениламино)пиримидин-4-иламино]фенил}амида циклопропанкарбоновой кислоты, (3-{6-
Claims (8)
1. Соединение формулы I
в котором n выбран из 1, 2 и 3,
m выбран из 1, 2 и 3,
X1 выбран из связи, кислорода, NH и N(СН3),
Х2 выбран из кислорода и NH,
Y выбран из азота и СН,
R1 выбран из галоидзамещенного (С1-С4)алкила, галоидзамещенной (С1-С4)алкоксигруппы, (С1-С4)алкила, галоида и (С1-С4)алкоксигруппы,
R2 выбран из галоидзамещенного (С1-С4)алкила, галоидзамещенной (С1-С4)алкоксигруппы, (С1-С4)алкила, галоида, (С1-С4)алкоксигруппы и -NHC(O)R3, где R3 является (С3-С12) циклоалкилом,
а также его фармацевтически приемлемые соли, гидраты, сольваты и изомеры.
2. Соединение согласно п.1, в котором
n выбран из 1 и 2,
m выбран из 1 и 2,
X1 выбран из связи, кислорода, NH и N(CH3),
Х2 выбран из кислорода и NH,
Y выбран из азота и СН,
R1 выбран из галоидзамещенного (С1-С4)алкила, (С1-С4)алкила, галоида и (С1-С4)алкоксигруппы,
R2 выбран из галоидзамещенного (С1-С4)алкила, -NHC(O)R3 и (С1-С4)алкоксигруппы, где R3 является (С3-С12) циклоалкилом.
3. Соединение согласно п.2, в котором R1 выбран из циклопропилкарбониламиногруппы, циклогексилкарбониламиногруппы, трифторметила и метоксигруппы, а R2 выбран из трифторметила, метила, галоида и метоксигруппы.
4. Соединение согласно п.1, выбранное из {3-[6-(3-трифторметилфениламино)пиримидин-4-иламино]фенил}амида циклопропанкарбоновой кислоты, N,N'-бис(3-трифторметилфенил)пиримидин-4,6-диамина, {2-метокси-5-[6-(3-трифторметилфениламино)пиримидин-4-иламино]фенил}амида циклопропанкарбоновой кислоты, {2-метокси-5-[6-(3-трифторметилфениламино)пиримидин-4-иламино]фенил}амида циклогексанкарбоновой кислоты, [3-(6-о-толиламинопиримидин-4-иламино)фенил]амида циклопропанкарбоновой кислоты, {3-[6-(2-хлорфениламино)пиримидин-4-иламино]фенил}амида циклопропанкарбоновой кислоты, (3-{6-[метил(3-трифторметилфенил)амино]пиримидин-4-иламино}фенил)амида циклопропанкарбоновой кислоты, {3-[6-(3-трифторметилфенокси)пиримидин-4-иламино]фенил}амида циклопропанкарбоновой кислоты, {2-метокси-5-[6-(3-трифторметилфениламино)пиримидин-4-иламино]фенил}амида циклопропанкарбоновой кислоты, {3-[6-(2,5-диметоксифенил)пиримидин-4-иламино]фенил}амида циклопропанкарбоновой кислоты, {3-[6-(5-хлор-2-метоксифенил)пиримидин-4-иламино]фенил}амида циклопропанкарбоновой кислоты, (3-{метил[6-(3-трифторметилфениламино)пиримидин-4-ил]амино}фенил)амида циклопропанкарбоновой кислоты, {3-[2-(3-трифторметилфениламино)пиримидин-4-иламино]фенил}амида циклопропанкарбоновой кислоты, {3-[4-(3-трифторметилфениламино)пиримидин-2-иламино]фенил}амида циклопропанкарбоновой кислоты, 4,6-бис(3-рифторметилфенокси)пиримидина и N,N'-биc(3-тpифтopмeтилфeнил)пиpидин-2,4-диaминa.
5. Фармацевтическая композиция, включающая терапевтически эффективное количество соединения согласно п.1 в сочетании с фармацевтически приемлемым наполнителем.
6. Способ лечения заболевания животного, при котором ингибирование киназной активности может предотвратить, ингибировать или облегчить патологию и/или симптоматику заболевания, каковой способ включает введение животному терапевтически эффективного количества соединения согласно п.1.
7. Способ согласно п.6, в котором киназа выбрана из Lck, IR, IGF-1R, JNK1α, Flt3, Fes, EFGR (Her-1, erbB-1), cSRC, CDK1/циклин B, c-RAF, ВТК, Bmx, Axl, Aurora-A, Abl, BCR-Abl, TrkB, Tie2, Syk, SGK, SAPK2a, Rsk1 и Met.
8. Применение соединения согласно п.1 в изготовлении лекарственного средства для лечения заболевания животного, при котором активность киназ Lck, IR, IGF-1R, JNK1α, Flt3, Fes, EFGR (Her-1, erbB-1), cSRC, CDK1/циклин В, c-RAF, ВТК, Bmx, Axl, Aurora-А, Abl, BCR-Abl, TrkB, Tie2, Syk, SGK, SAPK2a, Rsk1 и/или Met вносит вклад в патологию и/или симптоматику заболевания.
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| WO2007056151A3 (en) | 2007-08-02 |
| CA2626479A1 (en) | 2007-05-18 |
| EP1943233A2 (en) | 2008-07-16 |
| WO2007056151A2 (en) | 2007-05-18 |
| AU2006311910A1 (en) | 2007-05-18 |
| US20090181991A1 (en) | 2009-07-16 |
| KR20080053954A (ko) | 2008-06-16 |
| JP2009514876A (ja) | 2009-04-09 |
| CN101300234A (zh) | 2008-11-05 |
| BRPI0618135A2 (pt) | 2011-08-16 |
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