JP2008523099A5 - - Google Patents
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- JP2008523099A5 JP2008523099A5 JP2007545694A JP2007545694A JP2008523099A5 JP 2008523099 A5 JP2008523099 A5 JP 2008523099A5 JP 2007545694 A JP2007545694 A JP 2007545694A JP 2007545694 A JP2007545694 A JP 2007545694A JP 2008523099 A5 JP2008523099 A5 JP 2008523099A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- heteroaryl
- compound
- heteroalkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 125000003118 aryl group Chemical group 0.000 claims 132
- 125000000217 alkyl group Chemical group 0.000 claims 131
- 125000001072 heteroaryl group Chemical group 0.000 claims 125
- 150000001875 compounds Chemical class 0.000 claims 91
- 229910052739 hydrogen Inorganic materials 0.000 claims 63
- 239000001257 hydrogen Substances 0.000 claims 63
- 125000004404 heteroalkyl group Chemical group 0.000 claims 58
- 150000002431 hydrogen Chemical group 0.000 claims 58
- 125000002252 acyl group Chemical group 0.000 claims 40
- 125000000623 heterocyclic group Chemical group 0.000 claims 35
- 229910052736 halogen Inorganic materials 0.000 claims 26
- 150000002367 halogens Chemical group 0.000 claims 26
- 229910052757 nitrogen Inorganic materials 0.000 claims 21
- 239000003814 drug Substances 0.000 claims 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims 15
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 14
- 125000006590 (C2-C6) alkenylene group Chemical group 0.000 claims 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims 14
- 229940079593 drug Drugs 0.000 claims 13
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 13
- -1 heteroaliphatic Chemical group 0.000 claims 11
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 10
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 7
- 125000002723 alicyclic group Chemical group 0.000 claims 6
- 125000001931 aliphatic group Chemical group 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 239000003795 chemical substances by application Substances 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 229910052799 carbon Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 208000020084 Bone disease Diseases 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 2
- 208000019838 Blood disease Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 108010025020 Nerve Growth Factor Proteins 0.000 claims 2
- 102000007072 Nerve Growth Factors Human genes 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 2
- 230000001028 anti-proliverative effect Effects 0.000 claims 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 230000001066 destructive effect Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 208000014951 hematologic disease Diseases 0.000 claims 2
- 208000018706 hematopoietic system disease Diseases 0.000 claims 2
- 239000002955 immunomodulating agent Substances 0.000 claims 2
- 229940121354 immunomodulator Drugs 0.000 claims 2
- 229960003444 immunosuppressant agent Drugs 0.000 claims 2
- 239000003018 immunosuppressive agent Substances 0.000 claims 2
- 208000033065 inborn errors of immunity Diseases 0.000 claims 2
- 208000019423 liver disease Diseases 0.000 claims 2
- UHOVQNZJYSORNB-UHFFFAOYSA-N monobenzene Natural products C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 2
- 239000003900 neurotrophic factor Substances 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 208000028529 primary immunodeficiency disease Diseases 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 208000020446 Cardiac disease Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010023825 Laryngeal cancer Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 102100025093 Zinc fingers and homeoboxes protein 2 Human genes 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000000840 anti-viral effect Effects 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 229940044683 chemotherapy drug Drugs 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000019622 heart disease Diseases 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 206010023841 laryngeal neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 230000001926 lymphatic effect Effects 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 210000004798 organs belonging to the digestive system Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 102000009929 raf Kinases Human genes 0.000 claims 1
- 108010077182 raf Kinases Proteins 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
- 0 CC(*)CCC(C)N=C(C)CCC*CC(C)CN Chemical compound CC(*)CCC(C)N=C(C)CCC*CC(C)CN 0.000 description 13
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 | ||
| US11/301,311 | 2005-12-12 | ||
| 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 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 true JP2008523099A5 (cg-RX-API-DMAC7.html) | 2009-02-26 |
| JP5111113B2 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 (cg-RX-API-DMAC7.html) |
| EP (1) | EP1828186A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP5111113B2 (cg-RX-API-DMAC7.html) |
| AU (1) | AU2005316668B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2590294A1 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2006065703A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (111)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY29439A1 (es) * | 2005-03-25 | 2006-10-02 | Glaxo Group Ltd | Nuevos compuestos |
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| US8247408B2 (en) | 2005-10-07 | 2012-08-21 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of PI3Kα for the treatment of cancer |
| CN101365682A (zh) | 2005-12-08 | 2009-02-11 | 千禧药品公司 | 具有激酶抑制活性的双环化合物 |
| MY146420A (en) | 2006-09-15 | 2012-08-15 | Pfizer Prod Inc | Pyrido (2, 3-d) pyrimidinone compounds and their use as pi3 inhibitors |
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| 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 |
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| CL2008001933A1 (es) | 2007-06-29 | 2009-09-25 | Millennium Pharm Inc | Compuestos derivados de pirimidina, inhibidores de la raf quinasa; compuestos intermediarios; procedimiento de preparacion; composicion farmaceutica; y su uso para tratar trastornos proliferativos, cardiacos, neurodegenerativos, inflamatorios, oseos, inmunologicos enfermedad viral, entre otros. |
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| JP5581390B2 (ja) * | 2009-10-23 | 2014-08-27 | イーライ リリー アンド カンパニー | Akt阻害剤 |
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| CN103596926B (zh) | 2011-12-31 | 2015-11-25 | 百济神州有限公司 | 作为raf激酶抑制剂的稠合三环化合物 |
| TWI615143B (zh) | 2012-02-24 | 2018-02-21 | 標誌製藥公司 | 使用tor激酶抑制劑組合療法以治療癌症之方法 |
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| BR112015023399A8 (pt) | 2013-03-15 | 2019-12-03 | Biomarin Pharm Inc | inibidores de hdac, seu uso e composição farmacêutica |
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| EA036160B1 (ru) | 2013-03-15 | 2020-10-08 | Селджен Кар Ллс | Гетероарильные соединения и их применение |
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| CN105377260B (zh) | 2013-04-17 | 2020-06-12 | 西格诺药品有限公司 | 二氢吡嗪并-吡嗪类化合物在制备治疗癌症的药物中的应用 |
| BR112015026021A2 (pt) | 2013-04-17 | 2017-07-25 | Signal Pharm Llc | terapia de combinação compreendendo um inibidor de tor quinase e n-(3-(5-flúor-2-(4-(2-met-oxietoxi)fenilamino)pirimidin-4-ilamino)fenil)acrilamida para o tratamento de câncer |
| KR102240356B1 (ko) | 2013-04-17 | 2021-04-14 | 시그날 파마소티칼 엘엘씨 | Tor 키나제 억제제와 5-치환된 퀴나졸리논 화합물을 포함하는 암 치료용 조합 요법 |
| KR102271344B1 (ko) | 2013-04-17 | 2021-07-01 | 시그날 파마소티칼 엘엘씨 | 디하이드로피라지노-피라진을 사용한 암의 치료 |
| JP6382947B2 (ja) | 2013-04-17 | 2018-08-29 | シグナル ファーマシューティカルズ,エルエルシー | 前立腺癌を治療するためのジヒドロピラジノ−ピラジン化合物及びアンドロゲン受容体アンタゴニストを含む組合せ療法 |
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2005
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2010
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