RU2012114902A - Конъюгаты и ингибиторы протеинкиназы - Google Patents
Конъюгаты и ингибиторы протеинкиназы Download PDFInfo
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- RU2012114902A RU2012114902A RU2012114902/04A RU2012114902A RU2012114902A RU 2012114902 A RU2012114902 A RU 2012114902A RU 2012114902/04 A RU2012114902/04 A RU 2012114902/04A RU 2012114902 A RU2012114902 A RU 2012114902A RU 2012114902 A RU2012114902 A RU 2012114902A
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- Prior art keywords
- halogen
- saturated
- oxo
- independently
- represents hydrogen
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- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 title 1
- 239000003909 protein kinase inhibitor Substances 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 146
- 239000001257 hydrogen Substances 0.000 claims abstract 146
- 229910052736 halogen Inorganic materials 0.000 claims abstract 144
- 150000002367 halogens Chemical class 0.000 claims abstract 144
- 229920006395 saturated elastomer Polymers 0.000 claims abstract 101
- 125000003118 aryl group Chemical group 0.000 claims abstract 70
- 125000000217 alkyl group Chemical group 0.000 claims abstract 62
- 125000001183 hydrocarbyl group Chemical group 0.000 claims abstract 61
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims abstract 58
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 54
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract 53
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 52
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 51
- 125000005842 heteroatom Chemical group 0.000 claims abstract 49
- 125000001188 haloalkyl group Chemical group 0.000 claims abstract 47
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 46
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims abstract 44
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims abstract 44
- 125000002950 monocyclic group Chemical group 0.000 claims abstract 44
- 239000001301 oxygen Chemical group 0.000 claims abstract 44
- 239000011593 sulfur Chemical group 0.000 claims abstract 44
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims abstract 35
- 125000004980 cyclopropylene group Chemical group 0.000 claims abstract 26
- 150000002825 nitriles Chemical class 0.000 claims abstract 24
- 102000001253 Protein Kinase Human genes 0.000 claims abstract 17
- 108060006633 protein kinase Proteins 0.000 claims abstract 17
- 101100115718 Arabidopsis thaliana CYS5 gene Proteins 0.000 claims abstract 7
- 108010064266 CYS7 Proteins 0.000 claims abstract 7
- 102100025802 Cystin-1 Human genes 0.000 claims abstract 7
- 101000855767 Homo sapiens Cystin-1 Proteins 0.000 claims abstract 7
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims abstract 6
- 101100115720 Arabidopsis thaliana CYS6 gene Proteins 0.000 claims abstract 5
- -1 CYS8 Proteins 0.000 claims abstract 5
- 101100330292 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) cys-12 gene Proteins 0.000 claims abstract 4
- 101100426732 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) cys-9 gene Proteins 0.000 claims abstract 4
- 239000012634 fragment Substances 0.000 claims abstract 3
- 239000003607 modifier Substances 0.000 claims abstract 3
- 125000004434 sulfur atom Chemical group 0.000 claims abstract 3
- 101100022915 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) cys-11 gene Proteins 0.000 claims abstract 2
- 108020001775 protein parts Proteins 0.000 claims abstract 2
- 239000000126 substance Substances 0.000 claims abstract 2
- 150000002431 hydrogen Chemical class 0.000 claims 116
- 125000001931 aliphatic group Chemical group 0.000 claims 90
- 125000002619 bicyclic group Chemical group 0.000 claims 43
- 150000001875 compounds Chemical class 0.000 claims 34
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 28
- 150000003839 salts Chemical class 0.000 claims 22
- 108091000080 Phosphotransferase Proteins 0.000 claims 20
- 102000020233 phosphotransferase Human genes 0.000 claims 20
- 125000003275 alpha amino acid group Chemical group 0.000 claims 8
- 101150012469 CYS2 gene Proteins 0.000 claims 6
- 101100222745 Schizosaccharomyces pombe (strain 972 / ATCC 24843) met17 gene Proteins 0.000 claims 6
- 101100498074 Schizosaccharomyces pombe (strain 972 / ATCC 24843) cys11 gene Proteins 0.000 claims 5
- 230000033115 angiogenesis Effects 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000003107 substituted aryl group Chemical group 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 4
- 102100037813 Focal adhesion kinase 1 Human genes 0.000 claims 3
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 3
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 3
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims 3
- 238000000034 method Methods 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
- 101000878536 Homo sapiens Focal adhesion kinase 1 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
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 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
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims 2
- 102100021125 Tyrosine-protein kinase ZAP-70 Human genes 0.000 claims 2
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 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
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- NCGVZTZWMFOVHN-VKHMYHEASA-N (2r)-2-(methylideneamino)-3-sulfanylpropanoic acid Chemical compound OC(=O)[C@H](CS)N=C NCGVZTZWMFOVHN-VKHMYHEASA-N 0.000 claims 1
- 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
- 108010093488 His-His-His-His-His-His Proteins 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
- 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
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 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
- 101100330293 Schizosaccharomyces pombe (strain 972 / ATCC 24843) cys12 gene Proteins 0.000 claims 1
- 102100031463 Serine/threonine-protein kinase PLK1 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
- 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
- 239000003112 inhibitor Substances 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 230000002427 irreversible effect Effects 0.000 claims 1
- 239000013038 irreversible inhibitor Substances 0.000 claims 1
- 229930182817 methionine Natural products 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 108010056274 polo-like kinase 1 Proteins 0.000 claims 1
- 230000003381 solubilizing effect Effects 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 0 C*c1c[o]nc1[Re] Chemical compound C*c1c[o]nc1[Re] 0.000 description 6
- YPIINMAYDTYYSQ-UHFFFAOYSA-N C=Cc1n[nH]cc1 Chemical compound C=Cc1n[nH]cc1 YPIINMAYDTYYSQ-UHFFFAOYSA-N 0.000 description 1
- IPBXLJFBVNLKFE-ZCFIWIBFSA-N CCC[C@@H](C)NC Chemical compound CCC[C@@H](C)NC IPBXLJFBVNLKFE-ZCFIWIBFSA-N 0.000 description 1
- UCSNLIFJJLTPGO-UHFFFAOYSA-N CCSCCc1ncc(C)[s]1 Chemical compound CCSCCc1ncc(C)[s]1 UCSNLIFJJLTPGO-UHFFFAOYSA-N 0.000 description 1
- VRRVIHSULZWANF-SOFGYWHQSA-N CCc1nc(/C=C/SCC)ncc1 Chemical compound CCc1nc(/C=C/SCC)ncc1 VRRVIHSULZWANF-SOFGYWHQSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/10—Transferases (2.)
- C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
- C12N9/1205—Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/96—Stabilising an enzyme by forming an adduct or a composition; Forming enzyme conjugates
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
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- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2661197C2 (ru) * | 2011-11-29 | 2018-07-13 | Дженентек, Инк. | Производные 2-фениламинопиримидина в качестве модуляторов богатой лейцином повторной киназы 2 (lrrk2) для лечения болезни паркинсона |
| RU2704112C2 (ru) * | 2013-10-25 | 2019-10-24 | Блюпринт Медсинс Корпорейшн | Ингибиторы рецептора фактора роста фибробластов |
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| ES2616789T3 (es) | 2006-09-22 | 2017-06-14 | Pharmacyclics, Inc. | Inhibidores de tirosina cinasa de Bruton |
| US8809273B2 (en) | 2007-03-28 | 2014-08-19 | Pharmacyclics, Inc. | Inhibitors of Bruton's tyrosine kinase |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| PL2300013T5 (pl) | 2008-05-21 | 2025-04-28 | Takeda Pharmaceutical Company Limited | Pochodne fosforu jako inhibitor kinazy |
| CN102159214A (zh) | 2008-07-16 | 2011-08-17 | 药品循环公司 | 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂 |
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| IN2012DN02534A (OSRAM) | 2009-09-16 | 2015-08-28 | Avila Therapeutics Inc | |
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| MX342405B (es) | 2010-06-03 | 2016-09-28 | Pharmacyclics Inc | El uso de inhibidores de la tirosina quinasa de bruton (btk). |
| CA2797947C (en) * | 2010-06-04 | 2019-07-09 | Charles Baker-Glenn | Aminopyrimidine derivatives as lrrk2 modulators |
| AU2011328139A1 (en) | 2010-11-10 | 2013-04-04 | F. Hoffmann-La Roche Ag | Pyrazole aminopyrimidine derivatives as LRRK2 modulators |
| AU2012250517B2 (en) | 2011-05-04 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
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| WO2013074986A1 (en) | 2011-11-17 | 2013-05-23 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| PL2840080T3 (pl) * | 2012-04-17 | 2018-06-29 | Fujifilm Corporation | Zawierający azot związek heterocykliczny lub jego sól |
| JP6469567B2 (ja) | 2012-05-05 | 2019-02-13 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Egfr発動性がんの細胞増殖阻害用化合物 |
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| BR112015001690A2 (pt) | 2012-07-24 | 2017-11-07 | Pharmacyclics Inc | mutações associadas com a resistência a inibidores da tirosina quinase de bruton (btk) |
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| DK2970205T3 (da) | 2013-03-14 | 2019-07-29 | Tolero Pharmaceuticals Inc | JAK2- og ALK2-inhibitorer og fremgangsmåder til anvendelse deraf |
| NZ711376A (en) | 2013-03-15 | 2020-01-31 | Sanofi Sa | Heteroaryl compounds and uses thereof |
| EA036160B1 (ru) * | 2013-03-15 | 2020-10-08 | Селджен Кар Ллс | Гетероарильные соединения и их применение |
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- 2010-09-15 CA CA2773985A patent/CA2773985A1/en not_active Abandoned
- 2010-09-15 MX MX2012003332A patent/MX339811B/es active IP Right Grant
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- 2010-09-15 CN CN201510330338.8A patent/CN105063001A/zh active Pending
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- 2010-09-15 NZ NZ620174A patent/NZ620174A/en not_active IP Right Cessation
- 2010-09-15 SG SG2012018545A patent/SG179172A1/en unknown
- 2010-09-15 AU AU2010295690A patent/AU2010295690B2/en not_active Ceased
- 2010-09-15 JP JP2012529871A patent/JP5806670B2/ja active Active
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2012
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2661197C2 (ru) * | 2011-11-29 | 2018-07-13 | Дженентек, Инк. | Производные 2-фениламинопиримидина в качестве модуляторов богатой лейцином повторной киназы 2 (lrrk2) для лечения болезни паркинсона |
| RU2704112C2 (ru) * | 2013-10-25 | 2019-10-24 | Блюпринт Медсинс Корпорейшн | Ингибиторы рецептора фактора роста фибробластов |
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