JP5111113B2 - Rafキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン - Google Patents
Rafキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン Download PDFInfo
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- JP5111113B2 JP5111113B2 JP2007545694A JP2007545694A JP5111113B2 JP 5111113 B2 JP5111113 B2 JP 5111113B2 JP 2007545694 A JP2007545694 A JP 2007545694A JP 2007545694 A JP2007545694 A JP 2007545694A JP 5111113 B2 JP5111113 B2 JP 5111113B2
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- pharmaceutically acceptable
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- 0 C*Ic1n[o]c(C)c1* Chemical compound C*Ic1n[o]c(C)c1* 0.000 description 67
- OXUSZWNVXYYBPP-UHFFFAOYSA-N COC(c(ncnc1N2Cc(c(OC)cc(OC)c3)c3OC)c1N=CC2=O)=O Chemical compound COC(c(ncnc1N2Cc(c(OC)cc(OC)c3)c3OC)c1N=CC2=O)=O OXUSZWNVXYYBPP-UHFFFAOYSA-N 0.000 description 2
- HACRFKOAAJJPJG-UHFFFAOYSA-N CC(C)NC(c(ncnc1N2Cc(c(OC)cc(OC)c3)c3OC)c1NCC2=O)=O Chemical compound CC(C)NC(c(ncnc1N2Cc(c(OC)cc(OC)c3)c3OC)c1NCC2=O)=O HACRFKOAAJJPJG-UHFFFAOYSA-N 0.000 description 1
- FPKOAGZCCJPQBF-UHFFFAOYSA-N CC(C)NC(c1ncnc(N2)c1NCC2=O)=O Chemical compound CC(C)NC(c1ncnc(N2)c1NCC2=O)=O FPKOAGZCCJPQBF-UHFFFAOYSA-N 0.000 description 1
- XESTXJCTINZREH-MRVPVSSYSA-N CCOC(c1n[nH]c([C@@H](C)NC(OC(C)(C)C)=O)c1)=O Chemical compound CCOC(c1n[nH]c([C@@H](C)NC(OC(C)(C)C)=O)c1)=O XESTXJCTINZREH-MRVPVSSYSA-N 0.000 description 1
- IREJNGCJJQWZMA-UHFFFAOYSA-N CN(C=C)/N=C\N Chemical compound CN(C=C)/N=C\N IREJNGCJJQWZMA-UHFFFAOYSA-N 0.000 description 1
- SJRJJKPEHAURKC-UHFFFAOYSA-N CN1CCOCC1 Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 description 1
- RXAVWULUIVOHHA-UHFFFAOYSA-N CNC(CCCC1)=C1N Chemical compound CNC(CCCC1)=C1N RXAVWULUIVOHHA-UHFFFAOYSA-N 0.000 description 1
- CGAWAWMACGGOPF-UHFFFAOYSA-N CNC(CCCCC1)=C1N Chemical compound CNC(CCCCC1)=C1N CGAWAWMACGGOPF-UHFFFAOYSA-N 0.000 description 1
- DFXIYUSZRPCFFA-SNVBAGLBSA-N C[C@H](c1cc(-c([nH]2)nc3c2nc(C(C)(C)C)nc3)n[o]1)NC(c1c(CCC(N2)=O)c2ncn1)=O Chemical compound C[C@H](c1cc(-c([nH]2)nc3c2nc(C(C)(C)C)nc3)n[o]1)NC(c1c(CCC(N2)=O)c2ncn1)=O DFXIYUSZRPCFFA-SNVBAGLBSA-N 0.000 description 1
- OXHNLMTVIGZXSG-UHFFFAOYSA-N C[n]1cccc1 Chemical compound C[n]1cccc1 OXHNLMTVIGZXSG-UHFFFAOYSA-N 0.000 description 1
- UQNVNVPGTLKLPS-UHFFFAOYSA-N IN1C=NNC1 Chemical compound IN1C=NNC1 UQNVNVPGTLKLPS-UHFFFAOYSA-N 0.000 description 1
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
- C07D475/06—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- Health & Medical Sciences (AREA)
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- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Vascular Medicine (AREA)
- Communicable Diseases (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Virology (AREA)
- Oncology (AREA)
- Emergency Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Transplantation (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63564404P | 2004-12-13 | 2004-12-13 | |
| US60/635,644 | 2004-12-13 | ||
| US63674004P | 2004-12-16 | 2004-12-16 | |
| US60/636,740 | 2004-12-16 | ||
| PCT/US2005/044804 WO2006065703A1 (en) | 2004-12-13 | 2005-12-12 | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors |
| US11/301,311 | 2005-12-12 | ||
| US11/301,311 US7767687B2 (en) | 2004-12-13 | 2005-12-12 | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008523099A JP2008523099A (ja) | 2008-07-03 |
| JP2008523099A5 JP2008523099A5 (OSRAM) | 2009-02-26 |
| JP5111113B2 true JP5111113B2 (ja) | 2012-12-26 |
Family
ID=36097240
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007545694A Expired - Fee Related JP5111113B2 (ja) | 2004-12-13 | 2005-12-12 | Rafキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US7767687B2 (OSRAM) |
| EP (1) | EP1828186A1 (OSRAM) |
| JP (1) | JP5111113B2 (OSRAM) |
| AU (1) | AU2005316668B2 (OSRAM) |
| CA (1) | CA2590294A1 (OSRAM) |
| WO (1) | WO2006065703A1 (OSRAM) |
Families Citing this family (111)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR053450A1 (es) * | 2005-03-25 | 2007-05-09 | Glaxo Group Ltd | Derivados de 3,4-dihidro-pirimido(4,5-d)pirimidin-2-(1h)-ona 1,5,7 trisustituidos como inhibidores de la quinasa p38 |
| EP1926735A1 (en) | 2005-09-22 | 2008-06-04 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
| EP1931670B1 (en) | 2005-10-07 | 2012-09-12 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of pi3k |
| JP5461012B2 (ja) | 2005-10-07 | 2014-04-02 | エクセリクシス, インク. | PI3Kαのピリドピリミジノン型阻害剤 |
| KR20080074220A (ko) | 2005-12-08 | 2008-08-12 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 키나아제 억제 활성을 갖는 비시클릭 화합물 |
| ATE514695T1 (de) | 2006-09-15 | 2011-07-15 | Pfizer Prod Inc | Pyrido(2,3-d)pyrimidinonverbindungen und ihre verwendung als pi3-inhibitoren |
| KR101504669B1 (ko) | 2006-10-19 | 2015-03-20 | 시그날 파마소티칼 엘엘씨 | 헤테로아릴 화합물, 이들의 조성물 그리고 단백질 키나아제 억제제로서의 이들의 용도 |
| TW200835497A (en) * | 2007-01-11 | 2008-09-01 | Astrazeneca Ab | Chemical compounds 636 |
| ATE487720T1 (de) * | 2007-02-01 | 2010-11-15 | Astrazeneca Ab | 5,6,7,8-tetrahydropteridin-derivate als hsp90- hemmer |
| JP5238172B2 (ja) * | 2007-03-22 | 2013-07-17 | 公益財団法人相模中央化学研究所 | パーフルオロアルキル基を有する含窒素六員環化合物およびその製造方法 |
| CA2694284A1 (en) * | 2007-06-29 | 2009-01-08 | Jennifer Cossrow | Heterocyclic compounds useful as raf kinase inhibitors |
| TWI444379B (zh) * | 2007-06-29 | 2014-07-11 | Sunesis Pharmaceuticals Inc | 有用於作為Raf激酶抑制劑之化合物 |
| CA2735593C (en) | 2008-09-03 | 2017-08-15 | Repligen Corporation | Compositions including 6-aminohexanoic acid derivatives as hdac inhibitors |
| EP2350070A1 (en) | 2008-09-30 | 2011-08-03 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of pi3k and mtor |
| US8110578B2 (en) | 2008-10-27 | 2012-02-07 | Signal Pharmaceuticals, Llc | Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway |
| AU2009334997A1 (en) * | 2008-12-30 | 2011-08-04 | Millennium Pharmaceuticals, Inc. | Heteroaryl compounds useful as Raf kinase inhibitors |
| EA020151B1 (ru) * | 2009-10-23 | 2014-09-30 | Эли Лилли Энд Компани | Ингибиторы akt и фармацевтические составы, их содержащие |
| NZ599549A (en) | 2009-10-26 | 2013-11-29 | Signal Pharm Llc | Methods of synthesis and purification of heteroaryl compounds |
| ES2670659T3 (es) * | 2010-02-03 | 2018-05-31 | Signal Pharmaceuticals, Llc | Identificación de mutación en LKB1 como un biomarcador predictivo para la sensibilidad a inhibidores de la quinasa TOR |
| AR080151A1 (es) | 2010-02-09 | 2012-03-14 | Exelixis Inc | Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| EP2680694B1 (en) | 2011-02-28 | 2019-01-02 | BioMarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| US10059723B2 (en) | 2011-02-28 | 2018-08-28 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| US8957066B2 (en) | 2011-02-28 | 2015-02-17 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| AU2012315988A1 (en) * | 2011-09-30 | 2014-04-10 | Kineta, Inc. | Anti-viral compounds |
| SG10201505102WA (en) | 2011-10-19 | 2015-07-30 | Signal Pharm Llc | Treatment Of Cancer With TOR Kinase Inhibitors |
| CN104093398B (zh) | 2011-12-02 | 2017-03-15 | 西格诺药品有限公司 | 7‑(6‑(2‑羟基丙烷‑2‑基)吡啶‑3‑基)‑1‑((反式)‑4‑甲氧基环己基)‑3,4‑二氢吡嗪并[2,3‑b]吡嗪‑2(1h)‑酮、其固体形式的药物组合物及其使用方法 |
| DK2797888T3 (en) * | 2011-12-31 | 2016-09-19 | Beigene Ltd | Fused tricyclic compounds as RAF kinase inhibitors |
| KR102064626B1 (ko) | 2012-02-24 | 2020-01-09 | 시그날 파마소티칼 엘엘씨 | Tor 키나제 억제자 복합 치료법을 사용한 비소세포 폐암의 치료 방법 |
| SI2861595T1 (sl) | 2012-06-13 | 2017-04-26 | Incyte Holdings Corporation | Substituirane triciklične spojine kot inhibitorji fgfr |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| CN105188704B (zh) | 2013-01-16 | 2017-09-19 | 西格诺药品有限公司 | 被取代的吡咯并嘧啶化合物、其组合物和使用其的治疗方法 |
| TWI647220B (zh) | 2013-03-15 | 2019-01-11 | 美商西建卡爾有限責任公司 | 雜芳基化合物及其用途 |
| MX370142B (es) | 2013-03-15 | 2019-12-03 | Biomarin Pharm Inc | Inhibidores de hdac. |
| US9663524B2 (en) | 2013-03-15 | 2017-05-30 | Celgene Car Llc | Substituted pyrido[2,3-d]pyrimidines as protein kinase inhibitors |
| UA120248C2 (uk) | 2013-03-15 | 2019-11-11 | Селджен Кар Ллс | Гетероарильні сполуки та їх застосування |
| NZ631082A (en) | 2013-04-17 | 2017-06-30 | Signal Pharm Llc | Methods for treating cancer using tor kinase inhibitor combination therapy |
| WO2014172436A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer |
| US9358232B2 (en) | 2013-04-17 | 2016-06-07 | Signal Pharmaceuticals, Llc | Methods for treating cancer using TOR kinase inhibitor combination therapy |
| KR102221029B1 (ko) | 2013-04-17 | 2021-02-26 | 시그날 파마소티칼 엘엘씨 | 디하이드로피라지노-피라진을 사용한 암의 치료 |
| EA037683B1 (ru) | 2013-04-17 | 2021-04-29 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Фармацевтические составы, способы, твердые формы и способы применения, относящиеся к 1-этил-7-(2-метил-6-(1h-1,2,4-триазол-3-ил)пиридин-3-ил)-3,4-дигидропиразино[2,3-b] пиразин-2(1h)-ону |
| UA115805C2 (uk) | 2013-04-17 | 2017-12-26 | Сігнал Фармасьютікалз, Елелсі | Комбінована терапія, яка включає сполуку дигідропіразинопіразину й антагоніст рецептора андрогену, для лікування раку простати |
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| US7767687B2 (en) | 2010-08-03 |
| US20110059976A1 (en) | 2011-03-10 |
| AU2005316668A1 (en) | 2006-06-22 |
| WO2006065703A1 (en) | 2006-06-22 |
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