JP2013505245A5 - - Google Patents
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- JP2013505245A5 JP2013505245A5 JP2012529871A JP2012529871A JP2013505245A5 JP 2013505245 A5 JP2013505245 A5 JP 2013505245A5 JP 2012529871 A JP2012529871 A JP 2012529871A JP 2012529871 A JP2012529871 A JP 2012529871A JP 2013505245 A5 JP2013505245 A5 JP 2013505245A5
- Authority
- JP
- Japan
- Prior art keywords
- independently
- halogen
- hydrogen
- saturated
- oxo
- 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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- 229910052736 halogen Inorganic materials 0.000 claims 141
- 150000002367 halogens Chemical class 0.000 claims 140
- 229910052739 hydrogen Inorganic materials 0.000 claims 140
- 239000001257 hydrogen Substances 0.000 claims 140
- 150000002431 hydrogen Chemical group 0.000 claims 109
- 229920006395 saturated elastomer Polymers 0.000 claims 99
- 125000001931 aliphatic group Chemical group 0.000 claims 88
- 229910052757 nitrogen Inorganic materials 0.000 claims 72
- 125000003118 aryl group Chemical group 0.000 claims 65
- 125000000217 alkyl group Chemical group 0.000 claims 62
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 60
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 57
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 53
- 229910052717 sulfur Inorganic materials 0.000 claims 52
- 229910052760 oxygen Inorganic materials 0.000 claims 51
- 125000005842 heteroatom Chemical group 0.000 claims 48
- 125000001188 haloalkyl group Chemical group 0.000 claims 46
- 125000000753 cycloalkyl group Chemical group 0.000 claims 45
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 44
- 239000011593 sulfur Substances 0.000 claims 44
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 43
- 125000002619 bicyclic group Chemical group 0.000 claims 43
- 239000001301 oxygen Substances 0.000 claims 43
- 125000002950 monocyclic group Chemical group 0.000 claims 41
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 33
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 29
- 125000004980 cyclopropylene group Chemical group 0.000 claims 25
- 150000002825 nitriles Chemical group 0.000 claims 23
- 125000004043 oxo group Chemical group O=* 0.000 claims 22
- 150000003839 salts Chemical class 0.000 claims 22
- 108091000080 Phosphotransferase Proteins 0.000 claims 20
- 102000020233 phosphotransferase Human genes 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000003275 alpha amino acid group Chemical group 0.000 claims 8
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 7
- 101100115718 Arabidopsis thaliana CYS5 gene Proteins 0.000 claims 6
- 108010064266 CYS7 Proteins 0.000 claims 6
- 102000001253 Protein Kinase Human genes 0.000 claims 6
- 101100498074 Schizosaccharomyces pombe (strain 972 / ATCC 24843) cys11 gene Proteins 0.000 claims 6
- 230000033115 angiogenesis Effects 0.000 claims 6
- 125000004122 cyclic group Chemical group 0.000 claims 6
- 108060006633 protein kinase Proteins 0.000 claims 6
- 101150012469 CYS2 gene Proteins 0.000 claims 5
- 102100025802 Cystin-1 Human genes 0.000 claims 5
- 101000855767 Homo sapiens Cystin-1 Proteins 0.000 claims 5
- 101100222745 Schizosaccharomyces pombe (strain 972 / ATCC 24843) met17 gene Proteins 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000003107 substituted aryl group Chemical group 0.000 claims 5
- 101100115720 Arabidopsis thaliana CYS6 gene Proteins 0.000 claims 4
- -1 CYS8 Proteins 0.000 claims 4
- 101100330293 Schizosaccharomyces pombe (strain 972 / ATCC 24843) cys12 gene Proteins 0.000 claims 4
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 102100037813 Focal adhesion kinase 1 Human genes 0.000 claims 3
- 101000878536 Homo sapiens Focal adhesion kinase 1 Proteins 0.000 claims 3
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 3
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims 3
- 101100426732 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) cys-9 gene Proteins 0.000 claims 3
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 3
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims 3
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 claims 3
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 101150067142 CYS3 gene Proteins 0.000 claims 2
- 101150006642 CYS4 gene Proteins 0.000 claims 2
- ZEOWTGPWHLSLOG-UHFFFAOYSA-N Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F Chemical compound Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F ZEOWTGPWHLSLOG-UHFFFAOYSA-N 0.000 claims 2
- 102100023593 Fibroblast growth factor receptor 1 Human genes 0.000 claims 2
- 101710182386 Fibroblast growth factor receptor 1 Proteins 0.000 claims 2
- 102100023600 Fibroblast growth factor receptor 2 Human genes 0.000 claims 2
- 101710182389 Fibroblast growth factor receptor 2 Proteins 0.000 claims 2
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 claims 2
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 claims 2
- 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 claims 2
- 101000917134 Homo sapiens Fibroblast growth factor receptor 4 Proteins 0.000 claims 2
- 101001106413 Homo sapiens Macrophage-stimulating protein receptor Proteins 0.000 claims 2
- 101000950695 Homo sapiens Mitogen-activated protein kinase 8 Proteins 0.000 claims 2
- 101000912503 Homo sapiens Tyrosine-protein kinase Fgr Proteins 0.000 claims 2
- 101000818543 Homo sapiens Tyrosine-protein kinase ZAP-70 Proteins 0.000 claims 2
- 102100037808 Mitogen-activated protein kinase 8 Human genes 0.000 claims 2
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims 2
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims 2
- 102000018471 Proto-Oncogene Proteins B-raf Human genes 0.000 claims 2
- 108010091528 Proto-Oncogene Proteins B-raf Proteins 0.000 claims 2
- 102000001332 SRC Human genes 0.000 claims 2
- 108060006706 SRC Proteins 0.000 claims 2
- 102100026150 Tyrosine-protein kinase Fgr Human genes 0.000 claims 2
- 102100021125 Tyrosine-protein kinase ZAP-70 Human genes 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 239000013038 irreversible inhibitor Substances 0.000 claims 2
- 229940037201 oris Drugs 0.000 claims 2
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims 1
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 1
- 102100034111 Activin receptor type-1 Human genes 0.000 claims 1
- 102100025422 Bone morphogenetic protein receptor type-2 Human genes 0.000 claims 1
- 102100023060 Casein kinase I isoform gamma-2 Human genes 0.000 claims 1
- 102100025567 Citron Rho-interacting kinase Human genes 0.000 claims 1
- 101710087170 Citron rho-interacting kinase Proteins 0.000 claims 1
- 102100038113 Cyclin-dependent kinase 14 Human genes 0.000 claims 1
- 102100031679 Cyclin-dependent kinase-like 1 Human genes 0.000 claims 1
- 102100031683 Cyclin-dependent kinase-like 4 Human genes 0.000 claims 1
- 102100031480 Dual specificity mitogen-activated protein kinase kinase 1 Human genes 0.000 claims 1
- 101710146526 Dual specificity mitogen-activated protein kinase kinase 1 Proteins 0.000 claims 1
- 102000050554 Eph Family Receptors Human genes 0.000 claims 1
- 108091008815 Eph receptors Proteins 0.000 claims 1
- 108091008794 FGF receptors Proteins 0.000 claims 1
- 102100034051 Heat shock protein HSP 90-alpha Human genes 0.000 claims 1
- 101000799140 Homo sapiens Activin receptor type-1 Proteins 0.000 claims 1
- 101000934635 Homo sapiens Bone morphogenetic protein receptor type-2 Proteins 0.000 claims 1
- 101001049881 Homo sapiens Casein kinase I isoform gamma-2 Proteins 0.000 claims 1
- 101000884374 Homo sapiens Cyclin-dependent kinase 14 Proteins 0.000 claims 1
- 101000777728 Homo sapiens Cyclin-dependent kinase-like 1 Proteins 0.000 claims 1
- 101000777775 Homo sapiens Cyclin-dependent kinase-like 4 Proteins 0.000 claims 1
- 101001016865 Homo sapiens Heat shock protein HSP 90-alpha Proteins 0.000 claims 1
- 101001103039 Homo sapiens Inactive tyrosine-protein kinase transmembrane receptor ROR1 Proteins 0.000 claims 1
- 101001005128 Homo sapiens LIM domain kinase 1 Proteins 0.000 claims 1
- 101000916644 Homo sapiens Macrophage colony-stimulating factor 1 receptor Proteins 0.000 claims 1
- 101000628949 Homo sapiens Mitogen-activated protein kinase 10 Proteins 0.000 claims 1
- 101000950710 Homo sapiens Mitogen-activated protein kinase 6 Proteins 0.000 claims 1
- 101000950669 Homo sapiens Mitogen-activated protein kinase 9 Proteins 0.000 claims 1
- 101000663003 Homo sapiens Non-receptor tyrosine-protein kinase TNK1 Proteins 0.000 claims 1
- 101001103036 Homo sapiens Nuclear receptor ROR-alpha Proteins 0.000 claims 1
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 claims 1
- 101000878540 Homo sapiens Protein-tyrosine kinase 2-beta Proteins 0.000 claims 1
- 101001026790 Homo sapiens Tyrosine-protein kinase Fes/Fps Proteins 0.000 claims 1
- 101000851018 Homo sapiens Vascular endothelial growth factor receptor 1 Proteins 0.000 claims 1
- 102100039615 Inactive tyrosine-protein kinase transmembrane receptor ROR1 Human genes 0.000 claims 1
- 102100026023 LIM domain kinase 1 Human genes 0.000 claims 1
- 229940124647 MEK inhibitor Drugs 0.000 claims 1
- 102100024299 Maternal embryonic leucine zipper kinase Human genes 0.000 claims 1
- 101710154611 Maternal embryonic leucine zipper kinase Proteins 0.000 claims 1
- 102000004232 Mitogen-Activated Protein Kinase Kinases Human genes 0.000 claims 1
- 108090000744 Mitogen-Activated Protein Kinase Kinases Proteins 0.000 claims 1
- 102100026931 Mitogen-activated protein kinase 10 Human genes 0.000 claims 1
- 102100037801 Mitogen-activated protein kinase 6 Human genes 0.000 claims 1
- 102100037809 Mitogen-activated protein kinase 9 Human genes 0.000 claims 1
- 101100490437 Mus musculus Acvrl1 gene Proteins 0.000 claims 1
- 102100037669 Non-receptor tyrosine-protein kinase TNK1 Human genes 0.000 claims 1
- 108091007960 PI3Ks Proteins 0.000 claims 1
- 102000038030 PI3Ks Human genes 0.000 claims 1
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 claims 1
- 102100037787 Protein-tyrosine kinase 2-beta Human genes 0.000 claims 1
- 102100031463 Serine/threonine-protein kinase PLK1 Human genes 0.000 claims 1
- 102100024537 Tyrosine-protein kinase Fer Human genes 0.000 claims 1
- 102100037333 Tyrosine-protein kinase Fes/Fps Human genes 0.000 claims 1
- 108091008605 VEGF receptors Proteins 0.000 claims 1
- 108010053100 Vascular Endothelial Growth Factor Receptor-3 Proteins 0.000 claims 1
- 102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 claims 1
- 102100033178 Vascular endothelial growth factor receptor 1 Human genes 0.000 claims 1
- 102100033179 Vascular endothelial growth factor receptor 3 Human genes 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000005605 benzo group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 claims 1
- 229930182817 methionine Natural products 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000003607 modifier Substances 0.000 claims 1
- 108010056274 polo-like kinase 1 Proteins 0.000 claims 1
- 108010067366 proto-oncogene protein c-fes-fps Proteins 0.000 claims 1
- 230000003381 solubilizing effect Effects 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000002653 sulfanylmethyl group Chemical group [H]SC([H])([H])[*] 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 0 C[C@@]1(*)C(NC(N*=CC=C(C=*C)Oc2ccnc(*)c2)=O)=CC=C(*)C(*)=C1 Chemical compound C[C@@]1(*)C(NC(N*=CC=C(C=*C)Oc2ccnc(*)c2)=O)=CC=C(*)C(*)=C1 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24298809P | 2009-09-16 | 2009-09-16 | |
| US61/242,988 | 2009-09-16 | ||
| PCT/US2010/048916 WO2011034907A2 (en) | 2009-09-16 | 2010-09-15 | Protein kinase conjugates and inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015174949A Division JP6397389B2 (ja) | 2009-09-16 | 2015-09-04 | プロテインキナーゼコンジュゲート及びインヒビター |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013505245A JP2013505245A (ja) | 2013-02-14 |
| JP2013505245A5 true JP2013505245A5 (https=) | 2013-11-07 |
| JP5806670B2 JP5806670B2 (ja) | 2015-11-10 |
Family
ID=43759252
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012529871A Active JP5806670B2 (ja) | 2009-09-16 | 2010-09-15 | プロテインキナーゼコンジュゲート及びインヒビター |
| JP2015174949A Ceased JP6397389B2 (ja) | 2009-09-16 | 2015-09-04 | プロテインキナーゼコンジュゲート及びインヒビター |
| JP2018163436A Expired - Fee Related JP6889689B2 (ja) | 2009-09-16 | 2018-08-31 | プロテインキナーゼコンジュゲート及びインヒビター |
| JP2021086337A Pending JP2021121219A (ja) | 2009-09-16 | 2021-05-21 | プロテインキナーゼコンジュゲート及びインヒビター |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015174949A Ceased JP6397389B2 (ja) | 2009-09-16 | 2015-09-04 | プロテインキナーゼコンジュゲート及びインヒビター |
| JP2018163436A Expired - Fee Related JP6889689B2 (ja) | 2009-09-16 | 2018-08-31 | プロテインキナーゼコンジュゲート及びインヒビター |
| JP2021086337A Pending JP2021121219A (ja) | 2009-09-16 | 2021-05-21 | プロテインキナーゼコンジュゲート及びインヒビター |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US9556426B2 (https=) |
| EP (1) | EP2478361A4 (https=) |
| JP (4) | JP5806670B2 (https=) |
| KR (1) | KR20120093220A (https=) |
| CN (2) | CN102713618B (https=) |
| AU (2) | AU2010295690B2 (https=) |
| BR (1) | BR112012005962A8 (https=) |
| CA (1) | CA2773985A1 (https=) |
| IL (1) | IL218678A0 (https=) |
| IN (1) | IN2012DN02534A (https=) |
| MX (1) | MX339811B (https=) |
| NZ (2) | NZ620174A (https=) |
| RU (1) | RU2012114902A (https=) |
| SG (1) | SG179172A1 (https=) |
| WO (1) | WO2011034907A2 (https=) |
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| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| ES2660418T3 (es) | 2008-07-16 | 2018-03-22 | Pharmacyclics Llc | Inhibidores de la tirosina quinasa de Bruton para el tratamiento de tumores sólidos |
| JP2012501654A (ja) * | 2008-09-05 | 2012-01-26 | アビラ セラピューティクス， インコーポレイテッド | 不可逆的インヒビターの設計のためのアルゴリズム |
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- 2010-09-15 IN IN2534DEN2012 patent/IN2012DN02534A/en unknown
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- 2010-09-15 WO PCT/US2010/048916 patent/WO2011034907A2/en not_active Ceased
- 2010-09-15 JP JP2012529871A patent/JP5806670B2/ja active Active
- 2010-09-15 AU AU2010295690A patent/AU2010295690B2/en not_active Ceased
- 2010-09-15 EP EP10817748.6A patent/EP2478361A4/en not_active Withdrawn
- 2010-09-15 CA CA2773985A patent/CA2773985A1/en not_active Abandoned
- 2010-09-15 KR KR1020127009760A patent/KR20120093220A/ko not_active Ceased
- 2010-09-15 CN CN201510330338.8A patent/CN105063001A/zh active Pending
- 2010-09-15 MX MX2012003332A patent/MX339811B/es active IP Right Grant
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