RU2009142851A - Ингибиторы киназы, пригодные для лечения миелопролиферативных заболеваний и других пролиферативных заболеваний - Google Patents
Ингибиторы киназы, пригодные для лечения миелопролиферативных заболеваний и других пролиферативных заболеваний Download PDFInfo
- Publication number
- RU2009142851A RU2009142851A RU2009142851/15A RU2009142851A RU2009142851A RU 2009142851 A RU2009142851 A RU 2009142851A RU 2009142851/15 A RU2009142851/15 A RU 2009142851/15A RU 2009142851 A RU2009142851 A RU 2009142851A RU 2009142851 A RU2009142851 A RU 2009142851A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- group
- fluoro
- pyrazol
- substituted
- Prior art date
Links
- 201000010099 disease Diseases 0.000 title claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims 6
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 230000002071 myeloproliferative effect Effects 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 230000002062 proliferating effect Effects 0.000 title 1
- -1 tetrazinyl triazinyl Chemical group 0.000 claims abstract 35
- 150000001875 compounds Chemical class 0.000 claims abstract 25
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 5
- 125000003226 pyrazolyl group Chemical group 0.000 claims abstract 5
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims abstract 4
- 229910052799 carbon Inorganic materials 0.000 claims abstract 4
- 125000004076 pyridyl group Chemical group 0.000 claims abstract 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims abstract 4
- 125000002883 imidazolyl group Chemical group 0.000 claims abstract 3
- AMFYRKOUWBAGHV-UHFFFAOYSA-N 1h-pyrazolo[4,3-b]pyridine Chemical compound C1=CN=C2C=NNC2=C1 AMFYRKOUWBAGHV-UHFFFAOYSA-N 0.000 claims abstract 2
- YEDUAINPPJYDJZ-UHFFFAOYSA-N 2-hydroxybenzothiazole Chemical compound C1=CC=C2SC(O)=NC2=C1 YEDUAINPPJYDJZ-UHFFFAOYSA-N 0.000 claims abstract 2
- GAMYYCRTACQSBR-UHFFFAOYSA-N 4-azabenzimidazole Chemical compound C1=CC=C2NC=NC2=N1 GAMYYCRTACQSBR-UHFFFAOYSA-N 0.000 claims abstract 2
- MYONAGGJKCJOBT-UHFFFAOYSA-N benzimidazol-2-one Chemical compound C1=CC=CC2=NC(=O)N=C21 MYONAGGJKCJOBT-UHFFFAOYSA-N 0.000 claims abstract 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims abstract 2
- 125000004604 benzisothiazolyl group Chemical group S1N=C(C2=C1C=CC=C2)* 0.000 claims abstract 2
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims abstract 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims abstract 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims abstract 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims abstract 2
- QRUDEWIWKLJBPS-UHFFFAOYSA-N benzotriazole Chemical compound C1=CC=C2N[N][N]C2=C1 QRUDEWIWKLJBPS-UHFFFAOYSA-N 0.000 claims abstract 2
- 239000012964 benzotriazole Substances 0.000 claims abstract 2
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims abstract 2
- 125000004122 cyclic group Chemical group 0.000 claims abstract 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims abstract 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims abstract 2
- 125000002541 furyl group Chemical group 0.000 claims abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims abstract 2
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims abstract 2
- 125000001041 indolyl group Chemical group 0.000 claims abstract 2
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims abstract 2
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims abstract 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims abstract 2
- 125000004498 isoxazol-4-yl group Chemical group O1N=CC(=C1)* 0.000 claims abstract 2
- 125000004499 isoxazol-5-yl group Chemical group O1N=CC=C1* 0.000 claims abstract 2
- 125000001624 naphthyl group Chemical group 0.000 claims abstract 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims abstract 2
- 125000002971 oxazolyl group Chemical group 0.000 claims abstract 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims abstract 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims abstract 2
- 125000005247 tetrazinyl group Chemical group N1=NN=NC(=C1)* 0.000 claims abstract 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims abstract 2
- 125000000335 thiazolyl group Chemical group 0.000 claims abstract 2
- 125000001544 thienyl group Chemical group 0.000 claims abstract 2
- 150000003852 triazoles Chemical class 0.000 claims abstract 2
- 125000001425 triazolyl group Chemical group 0.000 claims abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 43
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 10
- 108060006633 protein kinase Proteins 0.000 claims 9
- 102000001253 Protein Kinase Human genes 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 3
- KDCGOANMDULRCW-UHFFFAOYSA-N 7H-purine Chemical compound N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- MZAGXDHQGXUDDX-JSRXJHBZSA-N (e,2z)-4-ethyl-2-hydroxyimino-5-nitrohex-3-enamide Chemical compound [O-][N+](=O)C(C)C(/CC)=C/C(=N/O)/C(N)=O MZAGXDHQGXUDDX-JSRXJHBZSA-N 0.000 claims 2
- VHIIRLFZGKOCAT-UHFFFAOYSA-N 1-(1-tert-butyl-5-oxopyrrolidin-3-yl)-3-[2-fluoro-4-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxyphenyl]urea Chemical compound C1=NN(C)C=C1C1=CC(OC=2C=C(F)C(NC(=O)NC3CC(=O)N(C3)C(C)(C)C)=CC=2)=CC=N1 VHIIRLFZGKOCAT-UHFFFAOYSA-N 0.000 claims 2
- MNRVBWUOBIGJGN-UHFFFAOYSA-N 1-(5-tert-butyl-2-methylpyrazol-3-yl)-3-[2-fluoro-4-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxyphenyl]urea Chemical compound C1=NN(C)C=C1C1=CC(OC=2C=C(F)C(NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C)=CC=2)=CC=N1 MNRVBWUOBIGJGN-UHFFFAOYSA-N 0.000 claims 2
- QSGWEIPTQPDIHO-UHFFFAOYSA-N 1-[2-fluoro-4-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxyphenyl]-3-(5-fluoropyridin-3-yl)urea Chemical compound C1=NN(C)C=C1C1=CC(OC=2C=C(F)C(NC(=O)NC=3C=C(F)C=NC=3)=CC=2)=CC=N1 QSGWEIPTQPDIHO-UHFFFAOYSA-N 0.000 claims 2
- WXSZBMMGPZMAKP-UHFFFAOYSA-N 1-[2-fluoro-4-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxyphenyl]-3-(5-methylpyridin-3-yl)urea Chemical compound CC1=CN=CC(NC(=O)NC=2C(=CC(OC=3C=C(N=CC=3)C3=CN(C)N=C3)=CC=2)F)=C1 WXSZBMMGPZMAKP-UHFFFAOYSA-N 0.000 claims 2
- WEVYNIUIFUYDGI-UHFFFAOYSA-N 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide Chemical compound NC(=O)C1=CC=CC(C=2N=CN=C(NC=3C=CC(OC(F)(F)F)=CC=3)C=2)=C1 WEVYNIUIFUYDGI-UHFFFAOYSA-N 0.000 claims 2
- 108010011042 Envoplakin Proteins 0.000 claims 2
- 102100027253 Envoplakin Human genes 0.000 claims 2
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 2
- 230000001594 aberrant effect Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000004202 carbamide Substances 0.000 claims 2
- OGEBRHQLRGFBNV-RZDIXWSQSA-N chembl2036808 Chemical compound C12=NC(NCCCC)=NC=C2C(C=2C=CC(F)=CC=2)=NN1C[C@H]1CC[C@H](N)CC1 OGEBRHQLRGFBNV-RZDIXWSQSA-N 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 231100000590 oncogenic Toxicity 0.000 claims 2
- 230000002246 oncogenic effect Effects 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000006593 (C2-C3) alkynyl group Chemical class 0.000 claims 1
- 125000006529 (C3-C6) alkyl group Chemical group 0.000 claims 1
- ZCXLTWVZYXBHJS-UHFFFAOYSA-N 1,2-benzoxazepine Chemical compound O1N=CC=CC2=CC=CC=C12 ZCXLTWVZYXBHJS-UHFFFAOYSA-N 0.000 claims 1
- OKANEFWFFOQCOY-UHFFFAOYSA-N 1-(1-tert-butylpyrazol-4-yl)-3-[2-fluoro-4-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxyphenyl]urea Chemical compound C1=NN(C)C=C1C1=CC(OC=2C=C(F)C(NC(=O)NC3=CN(N=C3)C(C)(C)C)=CC=2)=CC=N1 OKANEFWFFOQCOY-UHFFFAOYSA-N 0.000 claims 1
- RZQSHGDKNQMMEF-UHFFFAOYSA-N 1-(3-tert-butyl-1,2-oxazol-5-yl)-3-[2-fluoro-4-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxyphenyl]urea Chemical compound C1=NN(C)C=C1C1=CC(OC=2C=C(F)C(NC(=O)NC=3ON=C(C=3)C(C)(C)C)=CC=2)=CC=N1 RZQSHGDKNQMMEF-UHFFFAOYSA-N 0.000 claims 1
- BHEYRAWNMWGPIN-UHFFFAOYSA-N 1-[2-fluoro-3-methyl-4-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxyphenyl]-3-(3-propan-2-yl-1,2-oxazol-5-yl)urea Chemical compound O1N=C(C(C)C)C=C1NC(=O)NC(C(=C1C)F)=CC=C1OC1=CC=NC(C2=CN(C)N=C2)=C1 BHEYRAWNMWGPIN-UHFFFAOYSA-N 0.000 claims 1
- PLMLRBKZJBGMQM-UHFFFAOYSA-N 1-[2-fluoro-4-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxyphenyl]-3-(1-propan-2-ylimidazol-4-yl)urea Chemical compound CC(C)N1C=NC(NC(=O)NC=2C(=CC(OC=3C=C(N=CC=3)C3=CN(C)N=C3)=CC=2)F)=C1 PLMLRBKZJBGMQM-UHFFFAOYSA-N 0.000 claims 1
- RDPJTBRKUFEHIT-UHFFFAOYSA-N 1-[2-fluoro-4-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxyphenyl]-3-(1-propan-2-ylpyrazol-4-yl)urea Chemical compound C1=NN(C(C)C)C=C1NC(=O)NC(C(=C1)F)=CC=C1OC1=CC=NC(C2=CN(C)N=C2)=C1 RDPJTBRKUFEHIT-UHFFFAOYSA-N 0.000 claims 1
- DQFQCHIDRBIESA-UHFFFAOYSA-N 1-benzazepine Chemical compound N1C=CC=CC2=CC=CC=C12 DQFQCHIDRBIESA-UHFFFAOYSA-N 0.000 claims 1
- NZZXMWABAWENRC-UHFFFAOYSA-N 1-cyclohexyl-3-[2,3-difluoro-4-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxyphenyl]urea Chemical compound C1=NN(C)C=C1C1=CC(OC=2C(=C(F)C(NC(=O)NC3CCCCC3)=CC=2)F)=CC=N1 NZZXMWABAWENRC-UHFFFAOYSA-N 0.000 claims 1
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 claims 1
- CAAMSDWKXXPUJR-UHFFFAOYSA-N 3,5-dihydro-4H-imidazol-4-one Chemical compound O=C1CNC=N1 CAAMSDWKXXPUJR-UHFFFAOYSA-N 0.000 claims 1
- KDOPAZIWBAHVJB-UHFFFAOYSA-N 5h-pyrrolo[3,2-d]pyrimidine Chemical compound C1=NC=C2NC=CC2=N1 KDOPAZIWBAHVJB-UHFFFAOYSA-N 0.000 claims 1
- 201000004569 Blindness Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 101100123850 Caenorhabditis elegans her-1 gene Proteins 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 108091008794 FGF receptors Proteins 0.000 claims 1
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims 1
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 208000035268 Mast Cell Activation disease Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 102100030485 Platelet-derived growth factor receptor alpha Human genes 0.000 claims 1
- 101710148465 Platelet-derived growth factor receptor alpha Proteins 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims 1
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 claims 1
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000002785 azepinyl group Chemical group 0.000 claims 1
- 229940049706 benzodiazepine Drugs 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 208000019065 cervical carcinoma Diseases 0.000 claims 1
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 125000002576 diazepinyl group Chemical group N1N=C(C=CC=C1)* 0.000 claims 1
- 125000005044 dihydroquinolinyl group Chemical group N1(CC=CC2=CC=CC=C12)* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 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
- 102000037865 fusion proteins Human genes 0.000 claims 1
- 108020001507 fusion proteins Proteins 0.000 claims 1
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 230000003463 hyperproliferative effect Effects 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000000516 mast-cell leukemia Diseases 0.000 claims 1
- 208000008585 mastocytosis Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 208000025113 myeloid leukemia Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 125000000160 oxazolidinyl group Chemical group 0.000 claims 1
- 125000005968 oxazolinyl group Chemical group 0.000 claims 1
- 125000003585 oxepinyl group Chemical group 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 1
- 125000005545 phthalimidyl group Chemical group 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 239000010802 sludge Substances 0.000 claims 1
- 239000003381 stabilizer Substances 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims 1
- YWBFPKPWMSWWEA-UHFFFAOYSA-O triazolopyrimidine Chemical compound BrC1=CC=CC(C=2N=C3N=CN[N+]3=C(NCC=3C=CN=CC=3)C=2)=C1 YWBFPKPWMSWWEA-UHFFFAOYSA-O 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 0 **1N=CC(c2ccccn2)=C1 Chemical compound **1N=CC(c2ccccn2)=C1 0.000 description 1
- IELZFJBBJXHQIN-UHFFFAOYSA-N C[n]1ncc(-c2ccccn2)c1 Chemical compound C[n]1ncc(-c2ccccn2)c1 IELZFJBBJXHQIN-UHFFFAOYSA-N 0.000 description 1
- UOACMFNQMPEHLE-UHFFFAOYSA-N O=C(Nc1cccnc1)Nc(cccc1)c1F Chemical compound O=C(Nc1cccnc1)Nc(cccc1)c1F UOACMFNQMPEHLE-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Ophthalmology & Optometry (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91321607P | 2007-04-20 | 2007-04-20 | |
| US60/913,216 | 2007-04-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2009142851A true RU2009142851A (ru) | 2011-05-27 |
Family
ID=39872877
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2009142851/15A RU2009142851A (ru) | 2007-04-20 | 2008-04-18 | Ингибиторы киназы, пригодные для лечения миелопролиферативных заболеваний и других пролиферативных заболеваний |
Country Status (14)
| Country | Link |
|---|---|
| US (4) | US20080269267A1 (enExample) |
| EP (5) | EP2481736A1 (enExample) |
| JP (2) | JP2010524974A (enExample) |
| KR (2) | KR20100014811A (enExample) |
| CN (2) | CN101878031A (enExample) |
| AU (4) | AU2008242720A1 (enExample) |
| BR (2) | BRPI0807717A2 (enExample) |
| CA (4) | CA2684950A1 (enExample) |
| EA (1) | EA200970700A1 (enExample) |
| IL (1) | IL201650A0 (enExample) |
| MX (2) | MX2009011343A (enExample) |
| RU (1) | RU2009142851A (enExample) |
| SG (1) | SG183054A1 (enExample) |
| WO (4) | WO2008131276A1 (enExample) |
Families Citing this family (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110189167A1 (en) * | 2007-04-20 | 2011-08-04 | Flynn Daniel L | Methods and Compositions for the Treatment of Myeloproliferative Diseases and other Proliferative Diseases |
| BRPI0807717A2 (pt) | 2007-04-20 | 2014-05-20 | Deciphera Pharmaceuticals Llc | Inibidores de quinase úteis para o tratamento de doenças mieloproliferativas e outras doenças proliferativas. |
| KR20110099687A (ko) * | 2008-10-29 | 2011-09-08 | 데시페라 파마슈티칼스, 엘엘씨. | 항-암과 항-증식성 활성을 나타내는 시클로프로판 아미드와 유사체 |
| AU2010289353B2 (en) * | 2009-09-03 | 2016-12-08 | Allergan, Inc. | Compounds as tyrosine kinase modulators |
| WO2011062955A2 (en) * | 2009-11-18 | 2011-05-26 | University Of Massachusetts | Compounds for modulating tlr2 |
| PL2509961T3 (pl) | 2009-12-11 | 2016-09-30 | Pochodne imidazolidynodionu | |
| US8912184B1 (en) | 2010-03-01 | 2014-12-16 | Alzheimer's Institute Of America, Inc. | Therapeutic and diagnostic methods |
| EP2594566A4 (en) * | 2010-07-16 | 2014-10-01 | Kyowa Hakko Kirin Co Ltd | AROMATIC HETEROCYCLIC NITROGEN CYCLE DERIVATIVE |
| CN103080109A (zh) * | 2010-09-01 | 2013-05-01 | 苏州爱斯鹏药物研发有限责任公司 | 氘代杂环化合物激酶抑制剂 |
| CN102408408A (zh) * | 2010-09-20 | 2012-04-11 | 北大方正集团有限公司 | 具有抗肿瘤作用的芳基脲衍生物 |
| CN102432592A (zh) * | 2010-09-29 | 2012-05-02 | 北大方正集团有限公司 | 具有抗肿瘤作用的芳基脲衍生物及其制备方法 |
| US9346790B2 (en) | 2010-12-06 | 2016-05-24 | Autifony Therapeutics Limited | Hydantoin derivatives useful as Kv3 inhibitors |
| US8563558B2 (en) * | 2010-12-06 | 2013-10-22 | Confluence Life Sciences, Inc. | Substituted pyridine urea compounds |
| CN102558144A (zh) * | 2010-12-22 | 2012-07-11 | 北大方正集团有限公司 | 一种芳基脲衍生物 |
| CN102532113B (zh) * | 2010-12-22 | 2014-09-10 | 北大方正集团有限公司 | 芳基脲衍生物 |
| KR20120100027A (ko) * | 2011-03-02 | 2012-09-12 | 한국생명공학연구원 | 엔도사이토시스 모티프 및 단백질 도입 도메인을 포함하는 암 예방 또는 치료용 약학적 조성물 |
| UA114711C2 (uk) | 2011-05-13 | 2017-07-25 | Еррей Біофарма Інк. | Сполуки піролідинілсечовини й піролідинілтіосечовини як інгібітори кінази trka |
| JP6008953B2 (ja) | 2011-06-07 | 2016-10-19 | アウトイフオンイ トヘラペウトイクス リミテッド | Ｋｖ３阻害剤としてのヒダントイン誘導体 |
| WO2013036232A2 (en) * | 2011-09-08 | 2013-03-14 | Deciphera Pharmaceuticals, Llc | Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases |
| WO2013161919A1 (ja) | 2012-04-26 | 2013-10-31 | 小野薬品工業株式会社 | Ｔｒｋ阻害化合物 |
| BR112014028718A2 (pt) | 2012-05-22 | 2017-06-27 | Autifony Therapeutics Ltd | derivados de hidantoína como inibidores de kv3 |
| US9422252B2 (en) | 2012-05-22 | 2016-08-23 | Autifony Therapeutics Limited | Triazoles as Kv3 inhibitors |
| US8461179B1 (en) | 2012-06-07 | 2013-06-11 | Deciphera Pharmaceuticals, Llc | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| EP2875014B1 (en) * | 2012-07-17 | 2017-11-29 | Washington University | Anti-mucus drugs and uses therefor |
| WO2014078328A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9790178B2 (en) | 2012-11-13 | 2017-10-17 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| US9981959B2 (en) | 2012-11-13 | 2018-05-29 | Array Biopharma Inc. | Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| WO2014078378A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9809578B2 (en) | 2012-11-13 | 2017-11-07 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors |
| EP2922844B1 (en) | 2012-11-13 | 2018-01-10 | Array Biopharma, Inc. | N-pyrrolidinyl, n'-pyrazolyl- urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9822118B2 (en) | 2012-11-13 | 2017-11-21 | Array Biopharma Inc. | Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| WO2014078331A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9790210B2 (en) | 2012-11-13 | 2017-10-17 | Array Biopharma Inc. | N-(monocyclic aryl),N'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| HRP20161613T1 (hr) | 2012-11-13 | 2017-01-13 | Array Biopharma, Inc. | Tvari bicikličke ureje, tioureje, gvanidina i cijanogvanidina korisne za liječenje boli |
| EP2960234B1 (en) | 2013-02-19 | 2018-12-19 | ONO Pharmaceutical Co., Ltd. | Trk-inhibiting compound |
| CA2903081A1 (en) | 2013-03-14 | 2014-09-25 | Quanticel Pharmaceuticals, Inc. | Histone demethylase inhibitors |
| WO2014172639A1 (en) * | 2013-04-19 | 2014-10-23 | Ruga Corporation | Raf kinase inhibitors |
| ITMI20132201A1 (it) * | 2013-12-23 | 2015-06-24 | Isagro Spa | Processo per la sintesi regioselettiva di pirazoli |
| CN104974132B (zh) * | 2014-04-08 | 2017-05-17 | 北大方正集团有限公司 | 多取代的吡啶化合物、制备方法、用途及药物组合物 |
| RU2719489C2 (ru) | 2014-05-15 | 2020-04-17 | Эррэй Биофарма Инк. | 1-((3S,4R)-4-(3-ФТОРФЕНИЛ)-1-(2-МЕТОКСИЭТИЛ)ПИРРОЛИДИН-3-ИЛ)-3-(4-МЕТИЛ-3-(2-МЕТИЛПИРИМИДИН-5-ИЛ)-1-ФЕНИЛ-1Н-ПИРАЗОЛ-5-ИЛ)МОЧЕВИНА В КАЧЕСТВЕ ИНГИБИТОРА TrkA КИНАЗЫ |
| PE20181539A1 (es) * | 2016-02-02 | 2018-09-26 | Basf Se | Proceso de hidrogenacion catalitico para preparar pirazoles |
| CN105646448B (zh) * | 2016-02-03 | 2019-03-01 | 沈阳药科大学 | 吡啶类化合物及其用途 |
| CN108341813B (zh) * | 2017-01-24 | 2020-11-17 | 四川大学 | 取代的1-(异恶唑-3-基)-3-(3-氟-4-苯基)脲衍生物及其制备方法和用途 |
| AU2018392816B2 (en) | 2017-12-22 | 2023-04-20 | HiberCell Inc. | Chromenopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors |
| BR112020015581A2 (pt) | 2018-01-31 | 2021-02-02 | Deciphera Pharmaceuticals, Llc | terapia de combinação para o tratamento de tumores estromais gastrointestinais |
| EP3746060A1 (en) | 2018-01-31 | 2020-12-09 | Deciphera Pharmaceuticals, LLC | Combination therapy for the treatment of mastocytosis |
| CA3121202A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| BR112021012812A2 (pt) | 2018-12-28 | 2021-12-07 | Deciphera Pharmaceuticals Llc | Csf1r inhibitors para uso e tratamento de câncer |
| EP3934763A4 (en) * | 2019-03-06 | 2023-03-15 | University Of Maryland, Baltimore | SCAFFOLDS OF TETRAMERIC PROTEINS USED AS NANO-CARRIERS OF THERAPEUTIC PEPTIDES FOR THE TREATMENT OF CANCER AND OTHER DISEASES |
| CN118878519A (zh) | 2019-05-10 | 2024-11-01 | 德西费拉制药有限责任公司 | 苯基氨基嘧啶酰胺自噬抑制剂及其使用方法 |
| IL287795B2 (en) | 2019-05-10 | 2025-05-01 | Deciphera Pharmaceuticals Llc | Heteroarylaminopyrimidine amides as autophagy inhibitors and methods of using them |
| WO2020257180A1 (en) | 2019-06-17 | 2020-12-24 | Deciphera Pharmaceuticals, Llc | Aminopyrimidine amide autophagy inhibitors and methods of use thereof |
| WO2021013712A1 (en) | 2019-07-19 | 2021-01-28 | Anagenesis Biotechnologies S.A.S. | Polyaromatic urea derivatives and their use in the treatment of muscle diseases |
| WO2021030405A1 (en) | 2019-08-12 | 2021-02-18 | Deciphera Pharmaceuticals, Llc | Ripretinib for treating gastrointestinal stromal tumors |
| KR20220045189A (ko) | 2019-08-12 | 2022-04-12 | 데시페라 파마슈티칼스, 엘엘씨. | 위장관 기질 종양을 치료하는 방법 |
| CN118948773A (zh) | 2019-12-30 | 2024-11-15 | 德西费拉制药有限责任公司 | 1-(4溴-5-(1乙基-7-(甲氨基)-2侧氧基-1,2-二氢-1,6-萘啶-3基)-2氟苯基)-3-苯基脲的组合物 |
| SMT202300467T1 (it) | 2019-12-30 | 2024-01-10 | Deciphera Pharmaceuticals Llc | Formulazioni di inibitori di chinasi amorfi e loro procedimenti d’uso |
| MX2022014021A (es) * | 2020-05-08 | 2023-02-16 | Georgiamune Llc | Moduladores de akt3. |
| EP4247795A1 (en) | 2020-11-18 | 2023-09-27 | Deciphera Pharmaceuticals, LLC | Gcn2 and perk kinase inhibitors and methods of use thereof |
| CN112830936B (zh) * | 2021-01-08 | 2022-01-28 | 广西师范大学 | 核黄素化合物、其制备方法及应用 |
| EP4029501A1 (en) | 2021-01-19 | 2022-07-20 | Anagenesis Biotechnologies | Combination of polyaromatic urea derivatives and glucocorticoid or hdac inhibitor for the treatment of diseases or conditions associated with muscle cells and/or satellite cells |
| CN115772167B (zh) * | 2021-09-08 | 2025-07-29 | 暨南大学 | 含脲结构的化合物及其应用 |
| MX2024007042A (es) | 2021-12-09 | 2024-09-04 | Deciphera Pharmaceuticals Llc | Inhibidores de raf quinasa y metodos de uso de los mismos. |
| US11779572B1 (en) | 2022-09-02 | 2023-10-10 | Deciphera Pharmaceuticals, Llc | Methods of treating gastrointestinal stromal tumors |
| WO2025122952A1 (en) | 2023-12-08 | 2025-06-12 | Deciphera Pharmaceuticals, Llc | Formulations of vimseltinib |
Family Cites Families (99)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1115350B (de) | 1959-04-17 | 1961-10-19 | Siemens Ag | Selbstschalter, insbesondere Leitungsschutz-schalter, mit einem aus einem Kniegelenk bestehenden Antriebsmechanismus fuer das Schaltorgan |
| GB971307A (en) | 1961-03-02 | 1964-09-30 | Wellcome Found | 5-anilinopyrimidines |
| GB1127875A (en) * | 1967-03-23 | 1968-09-18 | Parke Davis & Co | 4-(5-nitro-2-furyl) thiazolyl hydantoins and hydrouracils |
| US3949002A (en) * | 1970-11-13 | 1976-04-06 | Imperial Chemical Industries Limited | Process for producing sulfone containing thiophenols |
| US3818024A (en) * | 1972-02-16 | 1974-06-18 | Velsicol Chemical Corp | Benzothiazol substituted thiadiazolidines |
| CH565887A5 (enExample) | 1972-08-22 | 1975-08-29 | Ciba Geigy Ag | |
| US3939122A (en) * | 1973-04-11 | 1976-02-17 | Bayer Aktiengesellschaft | Process for the preparation of compounds which contain hydantoin rings |
| FR2337554A1 (fr) | 1976-01-08 | 1977-08-05 | Buzas Andre | Nouveaux derives de la pyrazolidinedione |
| US4093624A (en) * | 1977-01-31 | 1978-06-06 | Icn Pharmaceuticals, Inc. | 1,2,4-Thiadiazolidine-3,5-dione |
| FR2396549A2 (fr) | 1977-07-06 | 1979-02-02 | Buzas Andre | Nouveaux derives de la pyrazolidinedione |
| US4256758A (en) | 1979-06-11 | 1981-03-17 | Merck & Co., Inc. | 4-Substituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase |
| US4298743A (en) | 1979-09-11 | 1981-11-03 | Merck & Co., Inc. | 4-(Substituted phenyl thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones |
| US4296237A (en) * | 1979-09-11 | 1981-10-20 | Merck & Co., Inc. | 4-(Pyridyl, piperazinyl and thiazolyl substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones |
| US4432992A (en) * | 1979-11-05 | 1984-02-21 | Merck & Co., Inc. | 4-[5(and 4)-Substituted-2-thienyl]-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase |
| US4366189A (en) * | 1979-12-21 | 1982-12-28 | Ciba-Geigy Corporation | 4-Heterocyclyl-4'-vinylstilbenes |
| JPS5915247A (ja) | 1982-07-16 | 1984-01-26 | Mitsubishi Paper Mills Ltd | 画像形成方法 |
| JPS59177557A (ja) * | 1983-03-28 | 1984-10-08 | Fuji Photo Film Co Ltd | ハロゲン化銀カラ−写真感光材料 |
| DE3406329A1 (de) | 1984-02-22 | 1985-08-22 | Merck Patent Gmbh, 6100 Darmstadt | Pyridone |
| US4816454A (en) * | 1984-09-21 | 1989-03-28 | Cassella Aktiengesellschaft | 4,5-dihydro-3(2H)-pyridazinones and their pharmacological use |
| US5103014A (en) * | 1987-09-30 | 1992-04-07 | American Home Products Corporation | Certain 3,3'-[[[(2-phenyl-4-thiazolyl)methoxy]phenyl]methylene]dithiobis-propanoic acid derivatives |
| AU606808B2 (en) | 1988-06-29 | 1991-02-14 | Otsuka Pharmaceutical Factory, Inc. | Arylcarboxamide substituted by alkylphosphonates, process for preparing the same and a pharmaceutical composition containing the same |
| GB9012936D0 (en) | 1990-06-11 | 1990-08-01 | Fujisawa Pharmaceutical Co | Thiophene derivatives,processes for preparation thereof and pharmaceutical composition comprising the same |
| US5254715A (en) | 1990-11-07 | 1993-10-19 | Warner-Lambert Company | Aminosulfonyl carbamates |
| EP0525197B1 (en) * | 1991-01-21 | 1997-08-27 | Shionogi Seiyaku Kabushiki Kaisha | 3-benzylidene-1-carbamoyl-2-pyrrolidone analogs |
| US5162360A (en) * | 1991-06-24 | 1992-11-10 | Warner-Lambert Company | 2-heteroatom containing urea and thiourea ACAT inhibitors |
| DE4302702A1 (de) | 1993-02-01 | 1994-08-04 | Bayer Ag | Arylaminosulfonylharnstoffe |
| WO1994021617A1 (en) | 1993-03-19 | 1994-09-29 | Dowelanco | A process for preparing halogenated isothiazoles |
| EP0692483A1 (en) | 1993-03-30 | 1996-01-17 | Yoshitomi Pharmaceutical Industries, Ltd. | Cell adhesion inhibitor and thienotriazolodiazepine compound |
| WO1994024095A1 (en) | 1993-04-16 | 1994-10-27 | Abbott Laboratories | Immunosuppressive agents |
| CA2123728A1 (en) * | 1993-05-21 | 1994-11-22 | Noriyoshi Sueda | Urea derivatives and their use as acat inhibitors |
| DE4337847A1 (de) | 1993-11-05 | 1995-05-11 | Bayer Ag | Substituierte Phenylaminosulfonylharnstoffe |
| EP0733048A1 (en) | 1993-12-07 | 1996-09-25 | Smithkline Beecham Plc | Heterocyclic biphenylylamides useful as 5ht1d antagonists |
| DE4343831A1 (de) | 1993-12-22 | 1995-06-29 | Magyar Tudomanyos Akademia | Substituierte Sulfonylharnstoffe |
| FR2715155B1 (fr) * | 1994-01-19 | 1996-07-26 | Mayoly Spindler | Inhibiteurs de la monoamine oxydase B et leurs procédés de préparation. |
| DE4414840A1 (de) | 1994-04-28 | 1995-11-02 | Bayer Ag | Substituierte Phenylaminosulfonylharnstoffe |
| CN100384825C (zh) | 1994-06-15 | 2008-04-30 | 大塚制药株式会社 | 苯并杂环衍生物 |
| DK0793656T3 (da) | 1994-11-24 | 2003-07-21 | Basilea Pharmaceutica Ag | Hidtil ukendte benzyl-pyrimidiner |
| US5494925A (en) * | 1994-12-02 | 1996-02-27 | Sterling Winthrop Inc. | 2-heterocyclyloxymethyl and 2-heterocyclylthiomethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof |
| US5972951A (en) | 1994-12-22 | 1999-10-26 | Smithkline Beecham Plc | Tetracyclic spiro compounds, process for their preparation and their use as 5HT1D receptor antagonists |
| EP0739884B1 (en) | 1995-04-24 | 2003-08-13 | Semiconductor Energy Laboratory Co., Ltd. | Liquid crystal compound and liquid crystal composition containing the same |
| JPH09221476A (ja) | 1995-12-15 | 1997-08-26 | Otsuka Pharmaceut Co Ltd | 医薬組成物 |
| GB9605945D0 (en) | 1996-03-21 | 1996-05-22 | Smithkline Beecham Plc | Novel compounds |
| PL192628B1 (pl) * | 1996-04-23 | 2006-11-30 | Vertex Pharma | Pochodne mocznika, kompozycje farmaceutyczne i zastosowanie związku i kompozycji |
| JPH107804A (ja) | 1996-06-25 | 1998-01-13 | Japan Synthetic Rubber Co Ltd | 熱硬化性樹脂組成物 |
| GB9623833D0 (en) | 1996-11-16 | 1997-01-08 | Zeneca Ltd | Chemical compound |
| US6020357A (en) * | 1996-12-23 | 2000-02-01 | Dupont Pharmaceuticals Company | Nitrogen containing heteroaromatics as factor Xa inhibitors |
| ATE230742T1 (de) | 1997-03-27 | 2003-01-15 | Great Lakes Chemical Europ | 2-(2'-hydroxphenyl)-benzotriazole und ihre verwendung als lichtschutzmittel für organische polymere |
| DE69826695T2 (de) | 1997-05-23 | 2006-02-02 | Bayer Pharmaceuticals Corp., West Haven | Arylharnstoffderivate zur behandlung von inflammatorischen oder immunomodulatorischen erkrankungen |
| US6235786B1 (en) * | 1997-08-06 | 2001-05-22 | Abbott Laboratories | Reverse hydroxamate inhibitors of matrix metalloproteinases |
| US6294573B1 (en) * | 1997-08-06 | 2001-09-25 | Abbott Laboratories | Reverse hydroxamate inhibitors of matrix metalloproteinases |
| CN1271279A (zh) | 1997-09-23 | 2000-10-25 | 普尼卡有限公司 | 用于治疗细胞因子介导性疾病的酰胺类衍生物 |
| IT1295933B1 (it) | 1997-10-30 | 1999-05-28 | Great Lakes Chemical Italia | 2-(2'-idrossifenil)benzotriazoli e procedimento per la loro preparazione |
| JP2001521934A (ja) * | 1997-11-03 | 2001-11-13 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | 抗炎症薬としての芳香族ヘテロ環式化合物 |
| CA2315720A1 (en) | 1997-12-22 | 1999-07-01 | Bayer Corporation | Inhibition of p38 kinase activity using substituted heterocyclic ureas |
| DK1043995T3 (da) | 1997-12-22 | 2007-03-05 | Bayer Pharmaceuticals Corp | Inhibering af p38 kinaseaktivitet ved anvendelse af aryl- og heteroaryl-substituerede, heterocykliske urinstoffer |
| RU2265597C2 (ru) | 1997-12-22 | 2005-12-10 | Байер Копэрейшн | Арил- и гетероарилзамещенные гетероциклические производные мочевины, способ ингибирования киназы raf и фармацевтическая композиция |
| DK1047418T3 (da) | 1997-12-22 | 2005-11-21 | Bayer Pharmaceuticals Corp | Inhibering af raf-kinase ved hjælp af substituerede heterocykliske urinstoffer |
| NZ333399A (en) | 1997-12-24 | 2000-05-26 | Sankyo Co | Cyclooxygenase-2 inhibitors (COX-2) for the prevention and treatment of tumors, cachexia and tumor-metastasis |
| EP0928790B1 (en) * | 1998-01-02 | 2003-03-05 | F. Hoffmann-La Roche Ag | Thiazole derivatives |
| EP0956855B1 (en) | 1998-04-24 | 2003-03-12 | K.U. Leuven Research & Development | Immunosuppressive effects of 8 substituted xanthine derivatives |
| US6197599B1 (en) * | 1998-07-30 | 2001-03-06 | Guorong Chin | Method to detect proteins |
| GB9823873D0 (en) * | 1998-10-30 | 1998-12-30 | Pharmacia & Upjohn Spa | 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents |
| UA73492C2 (en) * | 1999-01-19 | 2005-08-15 | Aromatic heterocyclic compounds as antiinflammatory agents | |
| JP2000275886A (ja) | 1999-03-23 | 2000-10-06 | Konica Corp | 電子写真感光体、それを用いたプロセスカートリッジ及び画像形成装置 |
| US6410254B1 (en) * | 1999-05-18 | 2002-06-25 | Cytokinetics | Compositions and assays utilizing ADP or phosphate for detecting protein modulators |
| US6525046B1 (en) * | 2000-01-18 | 2003-02-25 | Boehringer Ingelheim Pharmaceuticals, Inc. | Aromatic heterocyclic compounds as antiinflammatory agents |
| US6500628B1 (en) * | 2000-05-25 | 2002-12-31 | Millennium Pharmaceuticals, Inc. | Nucleic acid molecules encoding human kinase and phosphatase homologues and uses therefor |
| US6645990B2 (en) * | 2000-08-15 | 2003-11-11 | Amgen Inc. | Thiazolyl urea compounds and methods of uses |
| EP1506962B1 (en) * | 2000-10-20 | 2008-07-02 | Eisai R&D Management Co., Ltd. | Nitrogen-containing aromatic heterocycles |
| WO2002066442A1 (en) * | 2001-02-15 | 2002-08-29 | Boehringer Ingelheim Pharmaceuticals, Inc. | Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents |
| WO2002070662A2 (en) * | 2001-03-02 | 2002-09-12 | Gpc Biotech Ag | Three hybrid assay system |
| ATE338758T1 (de) * | 2001-03-23 | 2006-09-15 | Merck Sharp & Dohme | Imidazopyrimidin-derivate als liganden für gaba- rezeptoren |
| EP1281399A3 (en) | 2001-08-01 | 2004-02-11 | Warner-Lambert Company | Dual inhibitors of wax ester and cholesteryl ester synthesis for inhibiting sebum production |
| EP1427412A1 (en) * | 2001-09-13 | 2004-06-16 | Boehringer Ingelheim Pharmaceuticals Inc. | Methods of treating cytokine mediated diseases |
| US20040023961A1 (en) | 2002-02-11 | 2004-02-05 | Bayer Corporation | Aryl ureas with raf kinase and angiogenisis inhibiting activity |
| SI1478358T1 (sl) * | 2002-02-11 | 2013-09-30 | Bayer Healthcare Llc | Sorafenib tozilat za zdravljenje bolezni, značilnih po abnormalni angiogenezi |
| WO2003072569A1 (en) * | 2002-02-25 | 2003-09-04 | Boehringer Ingelheim Pharmaceuticals, Inc. | 1,4-disubstituted benzofused cycloalkyl urea compounds useful in treating cytokine mediated diseases |
| AR037647A1 (es) | 2002-05-29 | 2004-12-01 | Novartis Ag | Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina |
| AU2003246927A1 (en) | 2002-07-03 | 2004-01-23 | Astex Technology Limited | 3-`(hetero) arylmethoxy ! pyridines and their analogues as p38 map kinase inhibitors |
| US20040138216A1 (en) | 2002-12-23 | 2004-07-15 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Process for the preparation of an essentially pure polymorph of an n-pyrazolyl-n'-naphthyl-urea |
| US20080045706A1 (en) * | 2002-12-31 | 2008-02-21 | Flynn Daniel L | Anti-inflammatory medicaments |
| US7202257B2 (en) * | 2003-12-24 | 2007-04-10 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
| US7144911B2 (en) * | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| US20040171075A1 (en) * | 2002-12-31 | 2004-09-02 | Flynn Daniel L | Modulation of protein functionalities |
| EP1603879A2 (en) * | 2003-02-28 | 2005-12-14 | Bayer Pharmaceuticals Corporation | Substituted pyridine derivatives useful in the treatment of cancer and other disorders |
| US7557129B2 (en) * | 2003-02-28 | 2009-07-07 | Bayer Healthcare Llc | Cyanopyridine derivatives useful in the treatment of cancer and other disorders |
| WO2004113352A1 (en) | 2003-06-19 | 2004-12-29 | Amedis Pharmaceuticals Ltd. | Silylated heterocyclylurea derivatives as cytokine-inhibitors |
| WO2005002673A1 (en) | 2003-07-03 | 2005-01-13 | Astex Therapeutics Limited | Raf kinase inhibitors |
| EP1684762A4 (en) * | 2003-11-13 | 2009-06-17 | Ambit Biosciences Corp | UREA DERIVATIVES AS MODULATORS OF KINASE |
| US20070191336A1 (en) * | 2003-12-24 | 2007-08-16 | Flynn Daniel L | Anti-inflammatory medicaments |
| US20080220497A1 (en) * | 2003-12-24 | 2008-09-11 | Flynn Daniel L | Modulation of protein functionalities |
| AU2005321946B2 (en) * | 2004-12-23 | 2012-08-16 | Deciphera Pharmaceuticals, Llc | Enzyme modulators and treatments |
| US20090312349A1 (en) * | 2004-12-23 | 2009-12-17 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
| US7622583B2 (en) * | 2005-01-14 | 2009-11-24 | Chemocentryx, Inc. | Heteroaryl sulfonamides and CCR2 |
| TW200804349A (en) | 2005-12-23 | 2008-01-16 | Kalypsys Inc | Novel substituted pyrimidinyloxy ureas as inhibitors of protein kinases |
| US7790756B2 (en) * | 2006-10-11 | 2010-09-07 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases |
| US20080248487A1 (en) * | 2007-04-09 | 2008-10-09 | Flynn Daniel L | Modulation of protein functionalities |
| US20080248548A1 (en) * | 2007-04-09 | 2008-10-09 | Flynn Daniel L | Modulation of protein functionalities |
| BRPI0807717A2 (pt) | 2007-04-20 | 2014-05-20 | Deciphera Pharmaceuticals Llc | Inibidores de quinase úteis para o tratamento de doenças mieloproliferativas e outras doenças proliferativas. |
-
2008
- 2008-04-18 BR BRPI0807717-7A2A patent/BRPI0807717A2/pt not_active IP Right Cessation
- 2008-04-18 RU RU2009142851/15A patent/RU2009142851A/ru not_active Application Discontinuation
- 2008-04-18 MX MX2009011343A patent/MX2009011343A/es not_active Application Discontinuation
- 2008-04-18 AU AU2008242720A patent/AU2008242720A1/en not_active Abandoned
- 2008-04-18 EP EP12153098A patent/EP2481736A1/en not_active Withdrawn
- 2008-04-18 EP EP08746306A patent/EP2146718A4/en not_active Withdrawn
- 2008-04-18 EP EP08746279A patent/EP2146716A4/en not_active Withdrawn
- 2008-04-18 KR KR1020097017379A patent/KR20100014811A/ko not_active Withdrawn
- 2008-04-18 CA CA002684950A patent/CA2684950A1/en active Pending
- 2008-04-18 CN CN2008800085252A patent/CN101878031A/zh active Pending
- 2008-04-18 EP EP08746294A patent/EP2146717A4/en not_active Withdrawn
- 2008-04-18 CA CA002684666A patent/CA2684666A1/en not_active Abandoned
- 2008-04-18 JP JP2010504293A patent/JP2010524974A/ja active Pending
- 2008-04-18 SG SG2012053559A patent/SG183054A1/en unknown
- 2008-04-18 EP EP08746333A patent/EP2148677A4/en not_active Withdrawn
- 2008-04-18 KR KR1020097024209A patent/KR20100017184A/ko not_active Withdrawn
- 2008-04-18 WO PCT/US2008/060896 patent/WO2008131276A1/en not_active Ceased
- 2008-04-18 WO PCT/US2008/060867 patent/WO2008131253A1/en not_active Ceased
- 2008-04-18 US US12/105,302 patent/US20080269267A1/en not_active Abandoned
- 2008-04-18 US US12/105,408 patent/US8143293B2/en not_active Expired - Fee Related
- 2008-04-18 AU AU2008242767A patent/AU2008242767A1/en not_active Abandoned
- 2008-04-18 WO PCT/US2008/060833 patent/WO2008131227A1/en not_active Ceased
- 2008-04-18 US US12/105,350 patent/US20080269254A1/en not_active Abandoned
- 2008-04-18 AU AU2008242697A patent/AU2008242697A1/en not_active Abandoned
- 2008-04-18 CA CA002684949A patent/CA2684949A1/en not_active Abandoned
- 2008-04-18 WO PCT/US2008/060855 patent/WO2008140895A1/en not_active Ceased
- 2008-04-18 BR BRPI0810094-2A2A patent/BRPI0810094A2/pt not_active IP Right Cessation
- 2008-04-18 MX MX2009009066A patent/MX2009009066A/es not_active Application Discontinuation
- 2008-04-18 AU AU2008251723A patent/AU2008251723A1/en not_active Abandoned
- 2008-04-18 EA EA200970700A patent/EA200970700A1/ru unknown
- 2008-04-18 CN CN200880020714A patent/CN101801383A/zh active Pending
- 2008-04-18 JP JP2010504274A patent/JP2010524970A/ja active Pending
- 2008-04-18 US US12/105,376 patent/US20080261961A1/en not_active Abandoned
- 2008-04-18 CA CA002678639A patent/CA2678639A1/en not_active Abandoned
-
2009
- 2009-10-20 IL IL201650A patent/IL201650A0/en unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2009142851A (ru) | Ингибиторы киназы, пригодные для лечения миелопролиферативных заболеваний и других пролиферативных заболеваний | |
| JP2010524970A5 (enExample) | ||
| RU2009117615A (ru) | Ингибиторы киназ, применимые для лечения миелопролиферативных заболеваний и других пролиферативных заболеваний | |
| JP2010506850A5 (enExample) | ||
| US8129394B2 (en) | Heteroaryl-substituted imidazole compounds and uses thereof | |
| EP3601259A1 (en) | Isoquinolines as inhibitors of hpk1 | |
| US8865732B2 (en) | Heterocyclic compounds and uses thereof | |
| RU2017138100A (ru) | Имидазолонилхинолины и их применение в качестве ингибиторов киназы атм | |
| JP2016516791A5 (enExample) | ||
| CN114846005A (zh) | Shp2抑制剂及其应用 | |
| JP2010524974A5 (enExample) | ||
| JP2021501145A5 (enExample) | ||
| RU2014119250A (ru) | Производные 8-карбамоил-2-(2,3-дизамещенного пирид-6-ил)-1,2,3,4-тетрагидроизохинолина в качестве индуцирующих апоптоз средств для лечения рака и иммунных и аутоиммунных заболеваний | |
| RU2012131124A (ru) | Птеридиноны как ингибиторы polo-подобных киназ | |
| JP2013539777A5 (enExample) | ||
| JPWO2020201991A5 (enExample) | ||
| AU2022201717B2 (en) | Treatment of cancer | |
| JP2025535046A (ja) | Ｋｒａｓ ｇ１２ｃ変異タンパク質の複素環阻害剤及びその使用 | |
| WO2024006726A2 (en) | Compounds as inhibitors of axl | |
| RU2019116251A (ru) | Пиразоло[3,4-b]пиридины и имидазо[1,5-b]пиридазины в качестве ингибиторов pde1 | |
| TWI824010B (zh) | 治療血癌之組合療法 | |
| IL302543A (en) | ΡΡΑRγ MODULATORS AND METHODS OF USE | |
| WO2024229317A1 (en) | Spiro-heterocyclic inhibitors of kras g12c mutant proteins and uses thereof | |
| WO2015114452A2 (en) | Antibacterial compounds | |
| TWI753229B (zh) | 用於治療癌症之組合療法 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20130218 |