JP2010502706A5 - - Google Patents
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- Publication number
- JP2010502706A5 JP2010502706A5 JP2009527385A JP2009527385A JP2010502706A5 JP 2010502706 A5 JP2010502706 A5 JP 2010502706A5 JP 2009527385 A JP2009527385 A JP 2009527385A JP 2009527385 A JP2009527385 A JP 2009527385A JP 2010502706 A5 JP2010502706 A5 JP 2010502706A5
- Authority
- JP
- Japan
- Prior art keywords
- ring
- aliphatic
- optionally substituted
- alkyl
- independently
- 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.)
- Withdrawn
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- 125000000217 alkyl group Chemical group 0.000 claims description 222
- 125000001931 aliphatic group Chemical group 0.000 claims description 217
- 125000003118 aryl group Chemical group 0.000 claims description 128
- 229910052739 hydrogen Inorganic materials 0.000 claims description 99
- 239000001257 hydrogen Substances 0.000 claims description 98
- 125000000623 heterocyclic group Chemical group 0.000 claims description 92
- 150000002431 hydrogen Chemical class 0.000 claims description 90
- 125000001072 heteroaryl group Chemical group 0.000 claims description 88
- 229910052757 nitrogen Inorganic materials 0.000 claims description 87
- 125000005843 halogen group Chemical group 0.000 claims description 84
- 150000001875 compounds Chemical class 0.000 claims description 74
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 70
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 68
- 229910052799 carbon Inorganic materials 0.000 claims description 57
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 44
- 125000001153 fluoro group Chemical group F* 0.000 claims description 40
- -1 2-oxazolyl Chemical group 0.000 claims description 34
- 125000001424 substituent group Chemical group 0.000 claims description 33
- 125000005842 heteroatom Chemical group 0.000 claims description 28
- 229910052717 sulfur Inorganic materials 0.000 claims description 27
- 125000002947 alkylene group Chemical group 0.000 claims description 25
- 125000004432 carbon atom Chemical group C* 0.000 claims description 25
- 229910052760 oxygen Inorganic materials 0.000 claims description 23
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 18
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 17
- 125000002723 alicyclic group Chemical group 0.000 claims description 16
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 16
- 125000006413 ring segment Chemical group 0.000 claims description 16
- 125000003107 substituted aryl group Chemical group 0.000 claims description 16
- 125000002883 imidazolyl group Chemical group 0.000 claims description 14
- 125000002757 morpholinyl group Chemical group 0.000 claims description 14
- 125000004193 piperazinyl group Chemical group 0.000 claims description 14
- 125000003386 piperidinyl group Chemical group 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 14
- 125000004076 pyridyl group Chemical group 0.000 claims description 12
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 10
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 10
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 10
- 125000002971 oxazolyl group Chemical group 0.000 claims description 10
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims description 10
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 10
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 10
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 10
- 125000000335 thiazolyl group Chemical group 0.000 claims description 10
- 125000001425 triazolyl group Chemical group 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 8
- 125000002632 imidazolidinyl group Chemical group 0.000 claims description 8
- 125000002636 imidazolinyl group Chemical group 0.000 claims description 8
- 125000002755 pyrazolinyl group Chemical group 0.000 claims description 8
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 8
- 125000001422 pyrrolinyl group Chemical group 0.000 claims description 8
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 8
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 7
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 6
- 239000001301 oxygen Substances 0.000 claims description 6
- 229920006395 saturated elastomer Polymers 0.000 claims description 6
- 239000011593 sulfur Substances 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 238000011282 treatment Methods 0.000 claims description 5
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 125000006574 non-aromatic ring group Chemical group 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 125000004434 sulfur atom Chemical group 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 3
- 102000009929 raf Kinases Human genes 0.000 claims description 3
- 108010077182 raf Kinases Proteins 0.000 claims description 3
- 125000000389 2-pyrrolyl group Chemical group [H]N1C([*])=C([H])C([H])=C1[H] 0.000 claims description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 2
- 125000001397 3-pyrrolyl group Chemical group [H]N1C([H])=C([*])C([H])=C1[H] 0.000 claims description 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 2
- KDDQRKBRJSGMQE-UHFFFAOYSA-N 4-thiazolyl Chemical group [C]1=CSC=N1 KDDQRKBRJSGMQE-UHFFFAOYSA-N 0.000 claims description 2
- CWDWFSXUQODZGW-UHFFFAOYSA-N 5-thiazolyl Chemical group [C]1=CN=CS1 CWDWFSXUQODZGW-UHFFFAOYSA-N 0.000 claims description 2
- 125000002393 azetidinyl group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000002541 furyl group Chemical group 0.000 claims description 2
- 125000001475 halogen functional group Chemical group 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 125000004940 pyridazin-4-yl group Chemical group N1=NC=C(C=C1)* 0.000 claims description 2
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims description 2
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 125000004306 triazinyl group Chemical group 0.000 claims description 2
- 150000001721 carbon Chemical group 0.000 claims 19
- 125000004429 atom Chemical group 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 5
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 125000005313 fatty acid group Chemical group 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 0 C*C1=NC(*)(*)C(*)(*)N1 Chemical compound C*C1=NC(*)(*)C(*)(*)N1 0.000 description 11
- 238000000034 method Methods 0.000 description 3
- SNHMUERNLJLMHN-UHFFFAOYSA-N Ic1ccccc1 Chemical compound Ic1ccccc1 SNHMUERNLJLMHN-UHFFFAOYSA-N 0.000 description 1
- GBODIBRLMJJUNK-UHFFFAOYSA-N O=C(C1CCCC1)NI Chemical compound O=C(C1CCCC1)NI GBODIBRLMJJUNK-UHFFFAOYSA-N 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US84293106P | 2006-09-07 | 2006-09-07 | |
| PCT/US2007/019325 WO2008030448A1 (en) | 2006-09-07 | 2007-09-05 | Phenethylamide derivatives with kinase inhibitory activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010502706A JP2010502706A (ja) | 2010-01-28 |
| JP2010502706A5 true JP2010502706A5 (https=) | 2011-10-20 |
Family
ID=39015981
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009527385A Withdrawn JP2010502706A (ja) | 2006-09-07 | 2007-09-05 | キナーゼ阻害活性を有するフェネチルアミド誘導体 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20080064729A1 (https=) |
| EP (1) | EP2061761A1 (https=) |
| JP (1) | JP2010502706A (https=) |
| WO (1) | WO2008030448A1 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8778977B2 (en) * | 2006-06-30 | 2014-07-15 | Sunesis Pharmaceuticals, Inc. | Pyridinonyl PDK1 inhibitors |
| JP5693239B2 (ja) | 2008-01-23 | 2015-04-01 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | ４−ピリジノン化合物および癌についてのその使用 |
| US9029408B2 (en) | 2008-06-16 | 2015-05-12 | Gtx, Inc. | Compounds for treatment of cancer |
| AU2009330686B2 (en) | 2008-06-16 | 2014-07-03 | The Ohio State University Research Foundation | Compounds for the treatment of cancer |
| US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
| US8822513B2 (en) | 2010-03-01 | 2014-09-02 | Gtx, Inc. | Compounds for treatment of cancer |
| MX2012010115A (es) | 2010-03-01 | 2013-02-26 | Gtx Inc | Compuestos para el tratamiento de cancer. |
| CN102010367B (zh) * | 2010-12-17 | 2012-10-10 | 山东金城医药化工股份有限公司 | 一种高纯度4-氯-2-吡啶甲酸甲酯盐酸盐的制备工艺 |
| CN102532123B (zh) * | 2010-12-29 | 2016-03-09 | 中国医学科学院药物研究所 | 噻唑-5-甲酰胺化合物、及其制法和药物组合物与用途 |
| US9408885B2 (en) | 2011-12-01 | 2016-08-09 | Vib Vzw | Combinations of therapeutic agents for treating melanoma |
| US9273046B2 (en) * | 2011-12-31 | 2016-03-01 | Beigene, Ltd. | Fused tricyclic compounds as Raf kinase inhibitors |
| KR20140138293A (ko) | 2012-03-16 | 2014-12-03 | 액시킨 파마수티컬스 인코포레이티드 | 3,5-다이아미노피라졸 키나아제 억제제 |
| NZ631142A (en) | 2013-09-18 | 2016-03-31 | Axikin Pharmaceuticals Inc | Pharmaceutically acceptable salts of 3,5-diaminopyrazole kinase inhibitors |
| US9546163B2 (en) | 2014-12-23 | 2017-01-17 | Axikin Pharmaceuticals, Inc. | 3,5-diaminopyrazole kinase inhibitors |
| NZ735715A (en) | 2015-04-15 | 2022-09-30 | Beigene Ltd | Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore |
| CN105218436B (zh) * | 2015-10-21 | 2019-02-05 | 济南诚汇双达化工有限公司 | 一种制备4-氯-2-吡啶甲酸甲酯的方法 |
| JP6175519B2 (ja) * | 2016-01-04 | 2017-08-09 | ベイジーン リミテッド | Ｒａｆキナーゼ阻害剤としての縮合三環式化合物 |
| US10864203B2 (en) | 2016-07-05 | 2020-12-15 | Beigene, Ltd. | Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer |
| JP7341060B2 (ja) | 2017-02-10 | 2023-09-08 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | Ｍａｐｋ経路の活性化に関連付けられる癌の処置のための方法及び医薬組成物 |
| EP3732285A1 (en) | 2017-12-28 | 2020-11-04 | Tract Pharmaceuticals, Inc. | Stem cell culture systems for columnar epithelial stem cells, and uses related thereto |
| WO2020113094A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| CN110407824B (zh) * | 2019-08-08 | 2021-07-02 | 安徽医科大学 | 芳基甲酰胺类化合物及其制备方法、药物组合物及用途 |
| WO2025019600A2 (en) * | 2023-07-18 | 2025-01-23 | The General Hospital Corporation | Modulators of neurodegeneration |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE730884A (https=) * | 1968-04-01 | |||
| US4478853A (en) * | 1982-05-17 | 1984-10-23 | S. C. Johnson & Son, Inc. | Skin conditioning composition |
| US4500710A (en) * | 1983-06-16 | 1985-02-19 | Mitsubishi Chemical Industries, Limited | Quinophthalone dyes for cellulose-containing fibers |
| GB9107043D0 (en) * | 1991-04-04 | 1991-05-22 | Pfizer Ltd | Therapeutic agents |
| DE4220983A1 (de) * | 1992-06-26 | 1994-01-05 | Bayer Ag | Imidazolyl-substituierte Phenylpropion- und -zimtsäurederivate |
| US5506245A (en) * | 1992-10-12 | 1996-04-09 | Adir Et Compagnie | Thiazolidinedione compounds |
| WO2001010823A1 (de) * | 1999-08-07 | 2001-02-15 | Boehringer Ingelheim Pharma Kg | Carbonsäureamide, deren herstellung und deren verwendung als arzneimittel |
| EP1362846A4 (en) * | 2001-01-26 | 2006-10-04 | Takeda Pharmaceutical | AMINOETHANOL DERIVATIVES |
| US6831193B2 (en) * | 2001-05-18 | 2004-12-14 | Abbott Laboratories | Trisubstituted-N-[(1S)-1,2,3,4-Tetrahydro-1-naphthalenyl]benzamides which inhibit P2X3 and P2X2/3 containing receptors |
| WO2004072018A1 (ja) * | 2003-02-12 | 2004-08-26 | Takeda Pharmaceutical Company Limited | アミン誘導体 |
| FR2856065B1 (fr) * | 2003-06-13 | 2005-08-19 | Servier Lab | Nouveaux derives de benzothiazine et benzothiadiazine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| EA010485B1 (ru) * | 2003-07-23 | 2008-10-30 | Байер Фамэсьютиклс Копэрейшн | Производное n,n'-дифенилмочевины, фармацевтическая композиция (варианты) и способ лечения и предупреждения заболеваний и состояний с его использованием (варианты) |
| JP2005263787A (ja) * | 2004-02-17 | 2005-09-29 | Ishihara Sangyo Kaisha Ltd | アミド系化合物又はその塩、並びにそれらを含有するサイトカイン産生抑制剤 |
| TW200616974A (en) * | 2004-07-01 | 2006-06-01 | Astrazeneca Ab | Chemical compounds |
| AU2006204724A1 (en) * | 2005-01-14 | 2006-07-20 | Millennium Pharmaceuticals, Inc. | Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity |
-
2007
- 2007-09-05 EP EP07837722A patent/EP2061761A1/en not_active Withdrawn
- 2007-09-05 WO PCT/US2007/019325 patent/WO2008030448A1/en not_active Ceased
- 2007-09-05 US US11/899,361 patent/US20080064729A1/en not_active Abandoned
- 2007-09-05 JP JP2009527385A patent/JP2010502706A/ja not_active Withdrawn
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