JP2010538094A5 - - Google Patents
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- JP2010538094A5 JP2010538094A5 JP2010524200A JP2010524200A JP2010538094A5 JP 2010538094 A5 JP2010538094 A5 JP 2010538094A5 JP 2010524200 A JP2010524200 A JP 2010524200A JP 2010524200 A JP2010524200 A JP 2010524200A JP 2010538094 A5 JP2010538094 A5 JP 2010538094A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- aryl
- heteroaryl
- ring
- 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- Withdrawn
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- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims description 169
- 150000001875 compounds Chemical class 0.000 claims description 135
- 125000000217 alkyl group Chemical group 0.000 claims description 127
- 125000003118 aryl group Chemical group 0.000 claims description 70
- 125000001072 heteroaryl group Chemical group 0.000 claims description 69
- 125000000623 heterocyclic group Chemical group 0.000 claims description 58
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims description 45
- 229910052801 chlorine Inorganic materials 0.000 claims description 35
- 229910052731 fluorine Inorganic materials 0.000 claims description 34
- 229910052794 bromium Inorganic materials 0.000 claims description 33
- 229910005965 SO 2 Inorganic materials 0.000 claims description 32
- 125000003342 alkenyl group Chemical group 0.000 claims description 31
- 125000000304 alkynyl group Chemical group 0.000 claims description 31
- 229910052739 hydrogen Inorganic materials 0.000 claims description 30
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 29
- 229910052799 carbon Inorganic materials 0.000 claims description 28
- 125000005842 heteroatom Chemical group 0.000 claims description 28
- 229910052740 iodine Inorganic materials 0.000 claims description 28
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 25
- 125000004429 atom Chemical group 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 17
- 229920006395 saturated elastomer Polymers 0.000 claims description 17
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 14
- 239000003795 chemical substances by application Substances 0.000 claims description 12
- 229910052717 sulfur Inorganic materials 0.000 claims description 12
- 125000005843 halogen group Chemical group 0.000 claims description 11
- 201000010099 disease Diseases 0.000 claims description 10
- 229910052760 oxygen Inorganic materials 0.000 claims description 10
- -1 carbocycle Chemical group 0.000 claims description 9
- 229910052736 halogen Inorganic materials 0.000 claims description 9
- 239000000203 mixture Substances 0.000 claims description 9
- 229910052757 nitrogen Inorganic materials 0.000 claims description 8
- 125000006413 ring segment Chemical group 0.000 claims description 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 7
- 208000035475 disorder Diseases 0.000 claims description 7
- 241000124008 Mammalia Species 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- 230000002401 inhibitory effect Effects 0.000 claims description 6
- 125000002950 monocyclic group Chemical group 0.000 claims description 6
- 208000024891 symptom Diseases 0.000 claims description 6
- 108091000080 Phosphotransferase Proteins 0.000 claims description 5
- 230000003463 hyperproliferative effect Effects 0.000 claims description 5
- 102000020233 phosphotransferase Human genes 0.000 claims description 5
- 102000027426 receptor tyrosine kinases Human genes 0.000 claims description 5
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims description 5
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 4
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 208000029462 Immunodeficiency disease Diseases 0.000 claims description 4
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 4
- 206010012601 diabetes mellitus Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 208000019423 liver disease Diseases 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000002837 carbocyclic group Chemical group 0.000 claims description 3
- 150000002367 halogens Chemical class 0.000 claims description 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 3
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 2
- 208000020084 Bone disease Diseases 0.000 claims description 2
- 208000035473 Communicable disease Diseases 0.000 claims description 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 2
- 206010061218 Inflammation Diseases 0.000 claims description 2
- 108010025020 Nerve Growth Factor Proteins 0.000 claims description 2
- 102000007072 Nerve Growth Factors Human genes 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 208000006011 Stroke Diseases 0.000 claims description 2
- 108090000190 Thrombin Proteins 0.000 claims description 2
- 230000000172 allergic effect Effects 0.000 claims description 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 2
- 230000001028 anti-proliverative effect Effects 0.000 claims description 2
- 239000003443 antiviral agent Substances 0.000 claims description 2
- 208000010668 atopic eczema Diseases 0.000 claims description 2
- 125000002619 bicyclic group Chemical group 0.000 claims description 2
- 230000020411 cell activation Effects 0.000 claims description 2
- 230000030833 cell death Effects 0.000 claims description 2
- 208000015114 central nervous system disease Diseases 0.000 claims description 2
- 230000001066 destructive effect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 208000014951 hematologic disease Diseases 0.000 claims description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 2
- 239000005556 hormone Substances 0.000 claims description 2
- 229940088597 hormone Drugs 0.000 claims description 2
- 239000002955 immunomodulating agent Substances 0.000 claims description 2
- 229940121354 immunomodulator Drugs 0.000 claims description 2
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims description 2
- 125000002757 morpholinyl group Chemical group 0.000 claims description 2
- 201000001119 neuropathy Diseases 0.000 claims description 2
- 230000007823 neuropathy Effects 0.000 claims description 2
- 239000003900 neurotrophic factor Substances 0.000 claims description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
- 210000000056 organ Anatomy 0.000 claims description 2
- 230000001575 pathological effect Effects 0.000 claims description 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 125000004193 piperazinyl group Chemical group 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 208000037803 restenosis Diseases 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 208000010110 spontaneous platelet aggregation Diseases 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 229960004072 thrombin Drugs 0.000 claims description 2
- 238000002054 transplantation Methods 0.000 claims description 2
- 230000003612 virological effect Effects 0.000 claims description 2
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 17
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 17
- 230000001105 regulatory effect Effects 0.000 claims 2
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 2
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 150000001717 carbocyclic compounds Chemical class 0.000 claims 1
- 0 CC(C)CN(*)C(C(*)(*)C(N(*)*=C)=*)=* Chemical compound CC(C)CN(*)C(C(*)(*)C(N(*)*=C)=*)=* 0.000 description 9
- 238000000034 method Methods 0.000 description 5
- 125000003709 fluoroalkyl group Chemical group 0.000 description 3
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 description 1
- RMMFFMJLIHITAH-UHFFFAOYSA-N CC(C)c1c[n](C)nc1 Chemical compound CC(C)c1c[n](C)nc1 RMMFFMJLIHITAH-UHFFFAOYSA-N 0.000 description 1
- MFEIKQPHQINPRI-UHFFFAOYSA-N CCc1cnccc1 Chemical compound CCc1cnccc1 MFEIKQPHQINPRI-UHFFFAOYSA-N 0.000 description 1
- RIKMMFOAQPJVMX-UHFFFAOYSA-N Cc1c[nH]nc1 Chemical compound Cc1c[nH]nc1 RIKMMFOAQPJVMX-UHFFFAOYSA-N 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97047207P | 2007-09-06 | 2007-09-06 | |
| PCT/US2008/075477 WO2009033084A1 (en) | 2007-09-06 | 2008-09-05 | Pyrazolo-pyridines as tyrosine kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010538094A JP2010538094A (ja) | 2010-12-09 |
| JP2010538094A5 true JP2010538094A5 (OSRAM) | 2012-09-27 |
Family
ID=39876737
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010524200A Withdrawn JP2010538094A (ja) | 2007-09-06 | 2008-09-05 | チロシンキナーゼ阻害剤としてのピラゾロピリジン類 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20110130406A1 (OSRAM) |
| EP (1) | EP2193130A1 (OSRAM) |
| JP (1) | JP2010538094A (OSRAM) |
| CN (1) | CN101918403A (OSRAM) |
| CA (1) | CA2698753A1 (OSRAM) |
| WO (1) | WO2009033084A1 (OSRAM) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2032538A2 (en) * | 2006-06-08 | 2009-03-11 | Array Biopharma, Inc. | Quinoline compounds and methods of use |
| AU2009221808A1 (en) * | 2008-03-06 | 2009-09-11 | Genentech, Inc. | Combination therapy with c-met and EGFR antagonists |
| US8293897B2 (en) | 2008-10-14 | 2012-10-23 | Ning Xi | Compounds comprising a spiro-ring and methods of use |
| CA2752421C (en) | 2009-03-21 | 2013-08-06 | Ning Xi | Amino ester derivatives, salts thereof and methods of use |
| WO2011139891A1 (en) | 2010-04-29 | 2011-11-10 | Deciphera Pharmaceuticals, Llc | Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activites |
| EP2563362B1 (en) | 2010-04-29 | 2014-03-12 | Deciphera Pharmaceuticals, LLC | Cyclopropyl dicarboxamides and analogs exhibiting anti-cancer and anti-proliferative activites |
| WO2012003338A1 (en) | 2010-07-01 | 2012-01-05 | Takeda Pharmaceutical Company Limited | COMBINATION OF A cMET INHIBITOR AND AN ANTIBODY TO HGF AND/OR cMET |
| TW201247631A (en) | 2011-04-28 | 2012-12-01 | Du Pont | Herbicidal pyrazinones |
| CN104230922B (zh) * | 2013-06-19 | 2016-12-28 | 中国科学院上海药物研究所 | 一类五元杂环并吡啶类化合物及其制备方法和用途 |
| CN107002119A (zh) | 2014-03-24 | 2017-08-01 | 豪夫迈·罗氏有限公司 | 使用c‑met拮抗剂的癌症治疗及前者与hgf表达的关联 |
| AR101106A1 (es) | 2014-07-02 | 2016-11-23 | Pharmacyclics Llc | Inhibidores de tirosina quinasa de bruton |
| US10398774B2 (en) | 2014-12-09 | 2019-09-03 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Human monoclonal antibodies against AXL |
| WO2016135041A1 (en) | 2015-02-26 | 2016-09-01 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Fusion proteins and antibodies comprising thereof for promoting apoptosis |
| MY197742A (en) | 2015-03-17 | 2023-07-12 | Univ Tsukuba | Morphinan derivative |
| HUE057838T2 (hu) | 2016-06-07 | 2022-06-28 | Jacobio Pharmaceuticals Co Ltd | SHP2 inhibitorokként hasznos új heterociklusos származékok |
| US10246462B2 (en) | 2016-09-09 | 2019-04-02 | Flx Bio, Inc. | Chemokine receptor modulators and uses thereof |
| CN117122598A (zh) | 2016-09-16 | 2023-11-28 | 日本化学药品株式会社 | 吗啡喃衍生物的在阿片δ受体激动剂相关疾病的治疗中的应用 |
| TWI664175B (zh) | 2017-03-23 | 2019-07-01 | 大陸商北京加科思新藥研發有限公司 | 用於作為shp2抑制劑之新穎雜環衍生物 |
| CN112839935A (zh) | 2018-09-26 | 2021-05-25 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1773826A4 (en) * | 2004-07-02 | 2009-06-03 | Exelixis Inc | MODULATORS OF C-MET AND THEIR METHOD OF USE |
| US7547782B2 (en) * | 2005-09-30 | 2009-06-16 | Bristol-Myers Squibb Company | Met kinase inhibitors |
-
2008
- 2008-09-05 US US12/676,790 patent/US20110130406A1/en not_active Abandoned
- 2008-09-05 WO PCT/US2008/075477 patent/WO2009033084A1/en not_active Ceased
- 2008-09-05 EP EP08799257A patent/EP2193130A1/en not_active Withdrawn
- 2008-09-05 CA CA2698753A patent/CA2698753A1/en not_active Abandoned
- 2008-09-05 JP JP2010524200A patent/JP2010538094A/ja not_active Withdrawn
- 2008-09-05 CN CN2008801150441A patent/CN101918403A/zh active Pending
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