ECSP10010044A - Compuestos de 5-(4-(halo-alcoxi)-fenil)-pirimidin-2-amina y composiciones como inhibidores de cinasa - Google Patents
Compuestos de 5-(4-(halo-alcoxi)-fenil)-pirimidin-2-amina y composiciones como inhibidores de cinasaInfo
- Publication number
- ECSP10010044A ECSP10010044A EC2010010044A ECSP10010044A ECSP10010044A EC SP10010044 A ECSP10010044 A EC SP10010044A EC 2010010044 A EC2010010044 A EC 2010010044A EC SP10010044 A ECSP10010044 A EC SP10010044A EC SP10010044 A ECSP10010044 A EC SP10010044A
- Authority
- EC
- Ecuador
- Prior art keywords
- compounds
- raf
- kinase inhibitors
- pirimidin
- alcoxi
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 230000002159 abnormal effect Effects 0.000 abstract 2
- 230000003247 decreasing effect Effects 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- -1 p70S6K Proteins 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
- 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
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 abstract 1
- 101710182396 Fibroblast growth factor receptor 3 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
- 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
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta 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
- 102100037808 Mitogen-activated protein kinase 8 Human genes 0.000 abstract 1
- 102100037809 Mitogen-activated protein kinase 9 Human genes 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 abstract 1
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 abstract 1
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 abstract 1
- 108010029869 Proto-Oncogene Proteins c-raf Proteins 0.000 abstract 1
- 102100033479 RAF proto-oncogene serine/threonine-protein kinase Human genes 0.000 abstract 1
- 102000001332 SRC Human genes 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
- 108090001012 Transforming Growth Factor beta Proteins 0.000 abstract 1
- 102000004887 Transforming Growth Factor beta Human genes 0.000 abstract 1
- 102100031167 Tyrosine-protein kinase CSK Human genes 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 abstract 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 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
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 abstract 1
- 108010068338 p38 Mitogen-Activated Protein Kinases Proteins 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 239000003909 protein kinase inhibitor Substances 0.000 abstract 1
- 230000001105 regulatory effect Effects 0.000 abstract 1
Classifications
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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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- A61K31/495—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
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- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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Abstract
La invención proporciona compuestos de la fórmula (1), y composiciones farmacéuticas de los mismos, los cuales son útiles como inhibidores de cinasa de proteína, así como métodos para utilizar tales compuestos con el fin de tratar, disminuir, o prevenir una condición asociada con una actividad de cinasa anormal o mal regulada. En algunas modalidades, la invención proporciona métodos para utilizar tales compuestos con el fin de tratar, disminuir, o prevenir enfermedades o trastornos que involucren una activación anormal de las cinasas c-kit, PDGFR?, PDGFRß, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGFß, SRC, EGFR, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2ß, BRK, Fms, KDR, c-raf o b-raf.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US95726007P | 2007-08-22 | 2007-08-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP10010044A true ECSP10010044A (es) | 2010-04-30 |
Family
ID=39929716
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2010010044A ECSP10010044A (es) | 2007-08-22 | 2010-03-19 | Compuestos de 5-(4-(halo-alcoxi)-fenil)-pirimidin-2-amina y composiciones como inhibidores de cinasa |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US8293757B2 (es) |
| EP (1) | EP2190825B1 (es) |
| JP (2) | JP5599312B2 (es) |
| KR (2) | KR20120107538A (es) |
| CN (1) | CN101784530A (es) |
| AR (1) | AR068014A1 (es) |
| AU (1) | AU2008289037B2 (es) |
| BR (1) | BRPI0815715A8 (es) |
| CA (1) | CA2697081C (es) |
| CL (1) | CL2008002478A1 (es) |
| CO (1) | CO6260074A2 (es) |
| CR (1) | CR11264A (es) |
| EC (1) | ECSP10010044A (es) |
| ES (1) | ES2477878T3 (es) |
| MA (1) | MA31704B1 (es) |
| MX (1) | MX2010002004A (es) |
| PE (1) | PE20090992A1 (es) |
| PL (1) | PL2190825T3 (es) |
| PT (1) | PT2190825E (es) |
| RU (1) | RU2455288C2 (es) |
| TN (1) | TN2010000087A1 (es) |
| TW (1) | TW200914023A (es) |
| WO (1) | WO2009026276A1 (es) |
| ZA (1) | ZA201001513B (es) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2008289037B2 (en) * | 2007-08-22 | 2012-03-01 | Novartis Ag | 5- (4- (haloalkoxy) phenyl) pyrimidine-2-amine compounds and compositions as kinase inhibitors |
| JP5303557B2 (ja) | 2007-08-22 | 2013-10-02 | アイアールエム・リミテッド・ライアビリティ・カンパニー | キナーゼ阻害剤である2−ヘテロアリールアミノ−ピリミジン誘導体 |
| PE20142258A1 (es) | 2012-04-25 | 2015-01-15 | Takeda Pharmaceutical | Compuesto heterociclico nitrogenado |
| EP2863916B1 (en) | 2012-06-22 | 2018-07-18 | Merck Sharp & Dohme Corp. | Substituted pyridine spleen tyrosine kinase (syk) inhibitors |
| WO2013192088A1 (en) * | 2012-06-22 | 2013-12-27 | Merck Sharp & Dohme Corp. | SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| EP2873669A4 (en) | 2012-07-13 | 2015-11-25 | Takeda Pharmaceutical | HETEROCYCLIC CONNECTION |
| WO2014031438A2 (en) * | 2012-08-20 | 2014-02-27 | Merck Sharp & Dohme Corp. | SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| EP3007689B1 (en) | 2013-01-10 | 2018-03-07 | Pulmokine, Inc. | Non-selective kinase inhibitors |
| US9834520B2 (en) | 2013-03-14 | 2017-12-05 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| JP6411342B2 (ja) | 2013-07-03 | 2018-10-24 | 武田薬品工業株式会社 | アミド化合物 |
| WO2015002231A1 (ja) | 2013-07-03 | 2015-01-08 | 武田薬品工業株式会社 | 複素環化合物 |
| US20160159808A1 (en) | 2013-07-24 | 2016-06-09 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| 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 |
| EP3054937B1 (en) | 2013-10-11 | 2023-07-26 | Pulmokine, Inc. | Spray dry formulations |
| US9403810B2 (en) | 2014-05-14 | 2016-08-02 | Novartis Ag | Carboxamide derivatives |
| KR101694753B1 (ko) * | 2015-08-28 | 2017-01-11 | 주식회사 온코크로스 | 크로몰린 또는 이의 약학적으로 허용가능한 염을 유효성분으로 함유하는 간질환 예방 및 치료용 약학적 조성물 |
| KR20230093341A (ko) | 2016-10-27 | 2023-06-27 | 풀모킨 인코포레이티드 | 폐고혈압을 치료하기 위한 병용 요법 |
| KR101974145B1 (ko) * | 2017-12-22 | 2019-04-30 | 한국생명공학연구원 | 보풀 추출물을 유효성분으로 함유하는 아토피 피부염의 예방, 개선 또는 치료용 조성물 |
| CN115315421B (zh) | 2019-12-13 | 2024-12-03 | 日本新药株式会社 | 作为pdgf受体激酶抑制剂的化合物和组合物 |
| WO2023283488A2 (en) * | 2021-07-09 | 2023-01-12 | Chan Zuckerberg Biohub, Inc. | Cdk19-selective inhibitors, and methods of use thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0164204A1 (en) * | 1984-05-12 | 1985-12-11 | FISONS plc | Novel pharmaceutically useful pyrimidines |
| US5516775A (en) | 1992-08-31 | 1996-05-14 | Ciba-Geigy Corporation | Further use of pyrimidine derivatives |
| EP0672035A1 (en) | 1993-10-01 | 1995-09-20 | Novartis AG | Pyrimidineamine derivatives and processes for the preparation thereof |
| TW440563B (en) * | 1996-05-23 | 2001-06-16 | Hoffmann La Roche | Aryl pyrimidine derivatives and a pharmaceutical composition thereof |
| EP1052238A4 (en) | 1998-01-28 | 2007-05-02 | Shionogi & Co | NEW TRICYCLIC CONNECTION |
| DK1282607T3 (en) | 2000-05-08 | 2016-02-01 | Janssen Pharmaceutica Nv | Prodrugs of HIV replication inhibiting pyrimidines |
| GB0022438D0 (en) * | 2000-09-13 | 2000-11-01 | Novartis Ag | Organic Compounds |
| US7429599B2 (en) | 2000-12-06 | 2008-09-30 | Signal Pharmaceuticals, Llc | Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK |
| US7129242B2 (en) | 2000-12-06 | 2006-10-31 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto |
| US7122544B2 (en) | 2000-12-06 | 2006-10-17 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto |
| DE60212836T2 (de) | 2001-05-16 | 2007-01-25 | Gpc Biotech Ag | Pyridylpyrimidin-derivate als wirksame verbindungen gegen prionen-krankheiten |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| GB0222514D0 (en) | 2002-09-27 | 2002-11-06 | Novartis Ag | Organic compounds |
| US20050014753A1 (en) | 2003-04-04 | 2005-01-20 | Irm Llc | Novel compounds and compositions as protein kinase inhibitors |
| EP1628666B1 (en) | 2003-05-14 | 2015-09-23 | NeuroGenetic Pharmaceuticals, Inc. | Compouds and uses thereof in modulating amyloid beta |
| CA2536954C (en) | 2003-08-29 | 2012-11-27 | Exelixis, Inc. | C-kit modulators and methods of use |
| ES2229928B1 (es) | 2003-10-02 | 2006-07-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de pirimidin-2-amina. |
| WO2005040135A1 (ja) | 2003-10-24 | 2005-05-06 | Ono Pharmaceutical Co., Ltd. | 抗ストレス薬およびその医薬用途 |
| ES2390227T3 (es) | 2004-09-09 | 2012-11-07 | Natco Pharma Limited | Nuevos derivados de fenilaminopirimidina como inhibidores de la BCR-ABL kinasa |
| KR20070084067A (ko) | 2004-10-13 | 2007-08-24 | 와이어쓰 | N-벤젠설포닐 치환 아닐리노-피리미딘 동족체 |
| CA2585490A1 (en) | 2004-11-12 | 2006-05-18 | Galapagos Nv | Nitrogen heteroaromatic compounds which bind to the active site of protein kinase enzymes |
| WO2006081034A2 (en) | 2004-12-23 | 2006-08-03 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
| EA015890B1 (ru) | 2005-06-14 | 2011-12-30 | Тайджен Байотекнолоджи Ко. Лтд. | Производные пиримидина |
| BRPI0616575A2 (pt) * | 2005-09-27 | 2011-06-21 | Irm Llc | compostos e composições contendo diarilamina, seu uso como moduladores de receptores de c-kit bem como método para sua produção |
| BRPI0618135A2 (pt) | 2005-11-03 | 2011-08-16 | Irm Llc | compostos e composições como inibidores da proteìna quinase |
| CA2668190A1 (en) | 2006-11-03 | 2008-05-15 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| ATE544761T1 (de) | 2007-05-04 | 2012-02-15 | Irm Llc | Pyrimidinderivate und zusammensetzungen als c-kit-und pdgfr-kinasehemmer |
| EA019524B1 (ru) | 2007-05-04 | 2014-04-30 | Айрм Ллк | СОЕДИНЕНИЯ И КОМПОЗИЦИИ КАК ИНГИБИТОРЫ КИНАЗЫ с-kit И PDGFR |
| AU2008289037B2 (en) * | 2007-08-22 | 2012-03-01 | Novartis Ag | 5- (4- (haloalkoxy) phenyl) pyrimidine-2-amine compounds and compositions as kinase inhibitors |
| JP5303557B2 (ja) | 2007-08-22 | 2013-10-02 | アイアールエム・リミテッド・ライアビリティ・カンパニー | キナーゼ阻害剤である2−ヘテロアリールアミノ−ピリミジン誘導体 |
-
2008
- 2008-08-19 AU AU2008289037A patent/AU2008289037B2/en not_active Ceased
- 2008-08-19 US US12/674,416 patent/US8293757B2/en not_active Expired - Fee Related
- 2008-08-19 WO PCT/US2008/073573 patent/WO2009026276A1/en not_active Ceased
- 2008-08-19 KR KR1020127024444A patent/KR20120107538A/ko not_active Withdrawn
- 2008-08-19 EP EP08798168.4A patent/EP2190825B1/en active Active
- 2008-08-19 CN CN200880103897A patent/CN101784530A/zh active Pending
- 2008-08-19 PT PT87981684T patent/PT2190825E/pt unknown
- 2008-08-19 CA CA2697081A patent/CA2697081C/en not_active Expired - Fee Related
- 2008-08-19 JP JP2010521974A patent/JP5599312B2/ja not_active Expired - Fee Related
- 2008-08-19 KR KR1020107006090A patent/KR101218926B1/ko not_active Expired - Fee Related
- 2008-08-19 PL PL08798168T patent/PL2190825T3/pl unknown
- 2008-08-19 RU RU2010110640/04A patent/RU2455288C2/ru not_active IP Right Cessation
- 2008-08-19 MX MX2010002004A patent/MX2010002004A/es active IP Right Grant
- 2008-08-19 BR BRPI0815715A patent/BRPI0815715A8/pt not_active IP Right Cessation
- 2008-08-19 ES ES08798168.4T patent/ES2477878T3/es active Active
- 2008-08-22 AR ARP080103671A patent/AR068014A1/es unknown
- 2008-08-22 CL CL2008002478A patent/CL2008002478A1/es unknown
- 2008-08-22 PE PE2008001428A patent/PE20090992A1/es not_active Application Discontinuation
- 2008-08-22 TW TW097132234A patent/TW200914023A/zh unknown
-
2010
- 2010-02-11 CR CR11264A patent/CR11264A/es not_active Application Discontinuation
- 2010-02-19 TN TNP2010000087A patent/TN2010000087A1/fr unknown
- 2010-03-02 ZA ZA201001513A patent/ZA201001513B/xx unknown
- 2010-03-12 MA MA32694A patent/MA31704B1/fr unknown
- 2010-03-19 EC EC2010010044A patent/ECSP10010044A/es unknown
- 2010-03-23 CO CO10033947A patent/CO6260074A2/es not_active Application Discontinuation
-
2014
- 2014-05-28 JP JP2014110269A patent/JP2014177486A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| KR20100043288A (ko) | 2010-04-28 |
| AR068014A1 (es) | 2009-10-28 |
| CO6260074A2 (es) | 2011-03-22 |
| TW200914023A (en) | 2009-04-01 |
| ES2477878T3 (es) | 2014-07-18 |
| KR101218926B1 (ko) | 2013-01-04 |
| BRPI0815715A2 (pt) | 2017-06-13 |
| JP2010536867A (ja) | 2010-12-02 |
| KR20120107538A (ko) | 2012-10-02 |
| MX2010002004A (es) | 2010-03-11 |
| CL2008002478A1 (es) | 2009-05-15 |
| US8293757B2 (en) | 2012-10-23 |
| CA2697081A1 (en) | 2009-02-26 |
| CR11264A (es) | 2010-04-19 |
| EP2190825A1 (en) | 2010-06-02 |
| CA2697081C (en) | 2013-04-23 |
| JP2014177486A (ja) | 2014-09-25 |
| US20110301175A1 (en) | 2011-12-08 |
| ZA201001513B (en) | 2010-10-27 |
| BRPI0815715A8 (pt) | 2017-07-04 |
| RU2010110640A (ru) | 2011-09-27 |
| CN101784530A (zh) | 2010-07-21 |
| EP2190825B1 (en) | 2014-04-09 |
| PT2190825E (pt) | 2014-07-16 |
| RU2455288C2 (ru) | 2012-07-10 |
| JP5599312B2 (ja) | 2014-10-01 |
| AU2008289037B2 (en) | 2012-03-01 |
| PL2190825T3 (pl) | 2014-09-30 |
| MA31704B1 (fr) | 2010-09-01 |
| WO2009026276A1 (en) | 2009-02-26 |
| PE20090992A1 (es) | 2009-08-14 |
| TN2010000087A1 (en) | 2011-09-26 |
| AU2008289037A1 (en) | 2009-02-26 |
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