BRPI0815715A8 - Compostos 5-(-4-(haloalcóxi)fenil)pirimidina-2-amina e composições como inibidores de quinases. - Google Patents
Compostos 5-(-4-(haloalcóxi)fenil)pirimidina-2-amina e composições como inibidores de quinases.Info
- Publication number
- BRPI0815715A8 BRPI0815715A8 BRPI0815715A BRPI0815715A BRPI0815715A8 BR PI0815715 A8 BRPI0815715 A8 BR PI0815715A8 BR PI0815715 A BRPI0815715 A BR PI0815715A BR PI0815715 A BRPI0815715 A BR PI0815715A BR PI0815715 A8 BRPI0815715 A8 BR PI0815715A8
- Authority
- BR
- Brazil
- Prior art keywords
- compounds
- beta
- raf
- haloalkoxy
- pyrimidine
- Prior art date
Links
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 title abstract 2
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 230000002159 abnormal effect Effects 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- -1 p70S6K Proteins 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 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 abstract 1
- 101150053778 CSF1R gene Proteins 0.000 abstract 1
- 102100023274 Dual specificity mitogen-activated protein kinase kinase 4 Human genes 0.000 abstract 1
- 102100023401 Dual specificity mitogen-activated protein kinase kinase 6 Human genes 0.000 abstract 1
- 101100127166 Escherichia coli (strain K12) kefB gene Proteins 0.000 abstract 1
- 101150036586 FES gene Proteins 0.000 abstract 1
- 101001115395 Homo sapiens Dual specificity mitogen-activated protein kinase kinase 4 Proteins 0.000 abstract 1
- 101000624426 Homo sapiens Dual specificity mitogen-activated protein kinase kinase 6 Proteins 0.000 abstract 1
- 101100457333 Homo sapiens MAPK11 gene Proteins 0.000 abstract 1
- 101000916644 Homo sapiens Macrophage colony-stimulating factor 1 receptor Proteins 0.000 abstract 1
- 101000950695 Homo sapiens Mitogen-activated protein kinase 8 Proteins 0.000 abstract 1
- 101000950669 Homo sapiens Mitogen-activated protein kinase 9 Proteins 0.000 abstract 1
- 101000606502 Homo sapiens Protein-tyrosine kinase 6 Proteins 0.000 abstract 1
- 101000922131 Homo sapiens Tyrosine-protein kinase CSK Proteins 0.000 abstract 1
- 101150028321 Lck gene Proteins 0.000 abstract 1
- 102100028198 Macrophage colony-stimulating factor 1 receptor Human genes 0.000 abstract 1
- 108700036166 Mitogen-Activated Protein Kinase 11 Proteins 0.000 abstract 1
- 102100026929 Mitogen-activated protein kinase 11 Human genes 0.000 abstract 1
- 102100023482 Mitogen-activated protein kinase 14 Human genes 0.000 abstract 1
- 102100037808 Mitogen-activated protein kinase 8 Human genes 0.000 abstract 1
- 102100037809 Mitogen-activated protein kinase 9 Human genes 0.000 abstract 1
- 101150038994 PDGFRA gene Proteins 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 102000018471 Proto-Oncogene Proteins B-raf Human genes 0.000 abstract 1
- 108010091528 Proto-Oncogene Proteins B-raf Proteins 0.000 abstract 1
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 abstract 1
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 abstract 1
- 102000001788 Proto-Oncogene Proteins c-raf Human genes 0.000 abstract 1
- 108010029869 Proto-Oncogene Proteins c-raf Proteins 0.000 abstract 1
- 101150046814 SAPK2 gene Proteins 0.000 abstract 1
- 108060006706 SRC Proteins 0.000 abstract 1
- 101001045447 Synechocystis sp. (strain PCC 6803 / Kazusa) Sensor histidine kinase Hik2 Proteins 0.000 abstract 1
- 102100031167 Tyrosine-protein kinase CSK Human genes 0.000 abstract 1
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 abstract 1
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 abstract 1
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 abstract 1
- 101150060629 def gene Proteins 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000003828 downregulation Effects 0.000 abstract 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 abstract 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 abstract 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 abstract 1
- 108010068338 p38 Mitogen-Activated Protein Kinases Proteins 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 239000003909 protein kinase inhibitor Substances 0.000 abstract 1
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- 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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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract
COMPOSTO 5-(4-(HALOALCÓXI)FENIL) PIRIMIDINA-2-AMINA, SEU USO E COMPOSIÇÃO FARMACÉUTICA COMPREENDENDO O MESMO. A presente invenção refere-se a compostos de fórmula (I), e a composições farmacêuticas dos mesmos, que são úteis como inibidores de proteínas quinase, assim como métodos para usar tais compostos para tratar, melhorar ou prevenir uma condição associada à atividade anormal ou desregulada de quinases. Em algumas modalidades, a invenção oferece métodos para usar tais compostos para tratar, melhorar ou prevenir doenças ou distúrbios que envolvem a atividade anormal de c-kit, PDGFRa(Alfa) PDGFRP (Beta), CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGF (Beta), SRC, EGFR, trkB, FGFRS3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2(Beta), BRK, Fms, KDR, c-raf ou b-raf quinases.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US95726007P | 2007-08-22 | 2007-08-22 | |
| PCT/US2008/073573 WO2009026276A1 (en) | 2007-08-22 | 2008-08-19 | 5- (4- (haloalkoxy) phenyl) pyrimidine-2-amine compounds and compositions as kinase inhibitors |
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| BRPI0815715A2 BRPI0815715A2 (pt) | 2017-06-13 |
| BRPI0815715A8 true BRPI0815715A8 (pt) | 2017-07-04 |
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| WO2009026276A1 (en) * | 2007-08-22 | 2009-02-26 | Irm Llc | 5- (4- (haloalkoxy) phenyl) pyrimidine-2-amine compounds and compositions as kinase inhibitors |
| US9469637B2 (en) | 2012-04-25 | 2016-10-18 | Takeda Pharmaceutical Company Limited | Nitrogenated heterocyclic compound |
| US9416111B2 (en) | 2012-06-22 | 2016-08-16 | Merck Sharp & Dohme Corp. | Substituted diazine and triazine spleen tyrosine kinease (Syk) inhibitors |
| WO2013192098A1 (en) * | 2012-06-22 | 2013-12-27 | Merck Sharp & Dohme Corp. | SUBSTITUTED PYRIDINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| JP6205356B2 (ja) | 2012-07-13 | 2017-09-27 | 武田薬品工業株式会社 | 複素環化合物 |
| WO2014031438A2 (en) * | 2012-08-20 | 2014-02-27 | Merck Sharp & Dohme Corp. | SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| AU2014205483B2 (en) | 2013-01-10 | 2017-11-30 | Gilead Sciences, Inc. | Non-selective kinase inhibitors |
| WO2014142255A1 (ja) | 2013-03-14 | 2014-09-18 | 武田薬品工業株式会社 | 複素環化合物 |
| EP3018123B1 (en) | 2013-07-03 | 2023-05-10 | Takeda Pharmaceutical Company Limited | Amide compound |
| EP3018126A4 (en) | 2013-07-03 | 2016-12-07 | Takeda Pharmaceuticals Co | HETEROCYCLIC CONNECTION |
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| CN104458674A (zh) * | 2013-09-12 | 2015-03-25 | 中国药科大学 | 一种筛选血管内皮生长因子1激酶抑制剂高通量筛选方法 |
| CN104458675A (zh) * | 2013-09-12 | 2015-03-25 | 中国药科大学 | 一种筛选干细胞因子受体激酶抑制剂高通量筛选方法 |
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| KR101694753B1 (ko) | 2015-08-28 | 2017-01-11 | 주식회사 온코크로스 | 크로몰린 또는 이의 약학적으로 허용가능한 염을 유효성분으로 함유하는 간질환 예방 및 치료용 약학적 조성물 |
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| KR101974145B1 (ko) * | 2017-12-22 | 2019-04-30 | 한국생명공학연구원 | 보풀 추출물을 유효성분으로 함유하는 아토피 피부염의 예방, 개선 또는 치료용 조성물 |
| TWI893032B (zh) | 2019-12-13 | 2025-08-11 | 日商日本新藥股份有限公司 | 作為pdgf受體激酶抑制劑之化合物及組合物 |
| US20240351996A1 (en) * | 2021-07-09 | 2024-10-24 | Cz Biohub Sf, Llc | Cdk19-selective inhibitors, and methods of use thereof |
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| KR20120049397A (ko) | 2006-11-03 | 2012-05-16 | 노파르티스 아게 | 단백질 키나제 억제제로서의 화합물 및 조성물 |
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| US8268850B2 (en) | 2007-05-04 | 2012-09-18 | Irm Llc | Pyrimidine derivatives and compositions as C-kit and PDGFR kinase inhibitors |
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| MA31704B1 (fr) | 2010-09-01 |
| ZA201001513B (en) | 2010-10-27 |
| AR068014A1 (es) | 2009-10-28 |
| PT2190825E (pt) | 2014-07-16 |
| CN101784530A (zh) | 2010-07-21 |
| TW200914023A (en) | 2009-04-01 |
| BRPI0815715A2 (pt) | 2017-06-13 |
| WO2009026276A1 (en) | 2009-02-26 |
| RU2010110640A (ru) | 2011-09-27 |
| KR20100043288A (ko) | 2010-04-28 |
| CR11264A (es) | 2010-04-19 |
| AU2008289037B2 (en) | 2012-03-01 |
| JP5599312B2 (ja) | 2014-10-01 |
| JP2014177486A (ja) | 2014-09-25 |
| CO6260074A2 (es) | 2011-03-22 |
| CA2697081C (en) | 2013-04-23 |
| PE20090992A1 (es) | 2009-08-14 |
| TN2010000087A1 (en) | 2011-09-26 |
| EP2190825B1 (en) | 2014-04-09 |
| CL2008002478A1 (es) | 2009-05-15 |
| CA2697081A1 (en) | 2009-02-26 |
| KR101218926B1 (ko) | 2013-01-04 |
| EP2190825A1 (en) | 2010-06-02 |
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| RU2455288C2 (ru) | 2012-07-10 |
| US8293757B2 (en) | 2012-10-23 |
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