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- Withdrawn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 |
|---|---|---|---|---|
| EP2038272B8 (en) * | 2006-06-30 | 2013-10-23 | 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 |
| US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
| US9029408B2 (en) | 2008-06-16 | 2015-05-12 | Gtx, Inc. | Compounds for treatment of cancer |
| US8822513B2 (en) | 2010-03-01 | 2014-09-02 | Gtx, Inc. | Compounds for treatment of cancer |
| MX2010014066A (es) | 2008-06-16 | 2011-06-01 | Univ Tennessee Res Foundation | Compuestos para el tratamiento del cancer. |
| JP5879273B2 (ja) | 2010-03-01 | 2016-03-08 | ジーティーエックス・インコーポレイテッド | 癌を処置するための化合物 |
| 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 |
| PL2797888T3 (pl) * | 2011-12-31 | 2016-12-30 | Połączone związki tricykliczne jako inhibitory kinazy raf | |
| WO2013138617A1 (en) | 2012-03-16 | 2013-09-19 | Axikin Pharmaceuticals, Inc. | 3,5-diaminopyrazole kinase inhibitors |
| NZ631142A (en) | 2013-09-18 | 2016-03-31 | Axikin Pharmaceuticals Inc | Pharmaceutically acceptable salts of 3,5-diaminopyrazole kinase inhibitors |
| TWI703133B (zh) | 2014-12-23 | 2020-09-01 | 美商艾克斯基製藥公司 | ３,５-二胺基吡唑激酶抑制劑 |
| CN113307805A (zh) | 2015-04-15 | 2021-08-27 | 百济神州有限公司 | B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途 |
| 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 |
| WO2018146253A1 (en) | 2017-02-10 | 2018-08-16 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway |
| WO2019133810A1 (en) | 2017-12-28 | 2019-07-04 | Tract Pharmaceuticals, Inc. | Stem cell culture systems for columnar epithelial stem cells, and uses related thereto |
| CA3121202A1 (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 |
| EP1206446B1 (de) * | 1999-08-07 | 2004-05-26 | Boehringer Ingelheim Pharma GmbH & Co.KG | Carbonsäureamide, deren herstellung und deren verwendung als arzneimittel |
| US6982348B2 (en) * | 2001-01-26 | 2006-01-03 | Takeda Pharmaceutical Company Limited | 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 |
| US7601868B2 (en) * | 2003-02-12 | 2009-10-13 | Takeda Pharmaceutical Company Limited | Amine derivative |
| 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. |
| EP1663978B1 (en) * | 2003-07-23 | 2007-11-28 | Bayer Pharmaceuticals Corporation | Fluoro substituted omega-carboxyaryl diphenyl urea for the treatment and prevention of diseases and conditions |
| JP4829506B2 (ja) * | 2004-02-17 | 2011-12-07 | 石原産業株式会社 | チオ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 US US11/899,361 patent/US20080064729A1/en not_active Abandoned
- 2007-09-05 WO PCT/US2007/019325 patent/WO2008030448A1/en not_active Ceased
- 2007-09-05 JP JP2009527385A patent/JP2010502706A/ja not_active Withdrawn
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