ZA200201898B - Tyrosine kinase inhibitors. - Google Patents
Tyrosine kinase inhibitors. Download PDFInfo
- Publication number
- ZA200201898B ZA200201898B ZA200201898A ZA200201898A ZA200201898B ZA 200201898 B ZA200201898 B ZA 200201898B ZA 200201898 A ZA200201898 A ZA 200201898A ZA 200201898 A ZA200201898 A ZA 200201898A ZA 200201898 B ZA200201898 B ZA 200201898B
- Authority
- ZA
- South Africa
- Prior art keywords
- alkyl
- cycloalkyl
- optionally substituted
- substituents selected
- aryl
- Prior art date
Links
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 title claims description 3
- 239000005483 tyrosine kinase inhibitor Substances 0.000 title claims description 3
- 125000000217 alkyl group Chemical group 0.000 claims description 93
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 92
- 125000001424 substituent group Chemical group 0.000 claims description 87
- 125000003118 aryl group Chemical group 0.000 claims description 62
- 150000001875 compounds Chemical class 0.000 claims description 52
- 125000000623 heterocyclic group Chemical group 0.000 claims description 51
- 229910052736 halogen Inorganic materials 0.000 claims description 43
- 150000002367 halogens Chemical class 0.000 claims description 43
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 30
- 206010028980 Neoplasm Diseases 0.000 claims description 27
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims description 24
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims description 24
- 125000003545 alkoxy group Chemical group 0.000 claims description 24
- 229910052757 nitrogen Inorganic materials 0.000 claims description 24
- 125000000304 alkynyl group Chemical group 0.000 claims description 23
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims description 21
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims description 21
- 125000003342 alkenyl group Chemical group 0.000 claims description 20
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 20
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 20
- 125000002950 monocyclic group Chemical group 0.000 claims description 20
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims description 20
- 125000006664 (C1-C3) perfluoroalkyl group Chemical group 0.000 claims description 18
- 229910052717 sulfur Inorganic materials 0.000 claims description 15
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims description 13
- 230000033115 angiogenesis Effects 0.000 claims description 12
- 201000011510 cancer Diseases 0.000 claims description 12
- 229910003827 NRaRb Inorganic materials 0.000 claims description 11
- 229910052760 oxygen Inorganic materials 0.000 claims description 11
- 125000005275 alkylenearyl group Chemical group 0.000 claims description 10
- 125000005843 halogen group Chemical group 0.000 claims description 10
- 125000005842 heteroatom Chemical group 0.000 claims description 10
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 7
- 229910052799 carbon Inorganic materials 0.000 claims description 6
- 239000003102 growth factor Substances 0.000 claims description 5
- 239000003112 inhibitor Substances 0.000 claims description 5
- 206010012689 Diabetic retinopathy Diseases 0.000 claims description 4
- 230000001419 dependent effect Effects 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 229910052739 hydrogen Inorganic materials 0.000 claims description 3
- 208000027866 inflammatory disease Diseases 0.000 claims description 3
- 238000000034 method Methods 0.000 claims description 3
- -1 2-(4-morpholin-4-ylmethyl-pyridin-2-ylamino)-thiazole-S-carbonitrile Chemical compound 0.000 claims description 2
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims description 2
- 241000124008 Mammalia Species 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims description 2
- 206010064930 age-related macular degeneration Diseases 0.000 claims description 2
- 210000004556 brain Anatomy 0.000 claims description 2
- 201000008275 breast carcinoma Diseases 0.000 claims description 2
- 210000000867 larynx Anatomy 0.000 claims description 2
- 210000004072 lung Anatomy 0.000 claims description 2
- 201000005249 lung adenocarcinoma Diseases 0.000 claims description 2
- 210000004324 lymphatic system Anatomy 0.000 claims description 2
- 208000002780 macular degeneration Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 230000007170 pathology Effects 0.000 claims description 2
- 201000006845 reticulosarcoma Diseases 0.000 claims description 2
- 208000029922 reticulum cell sarcoma Diseases 0.000 claims description 2
- 230000004276 retinal vascularization Effects 0.000 claims description 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 2
- 210000002784 stomach Anatomy 0.000 claims description 2
- 239000002834 estrogen receptor modulator Substances 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- VEEGZPWAAPPXRB-BJMVGYQFSA-N (3e)-3-(1h-imidazol-5-ylmethylidene)-1h-indol-2-one Chemical compound O=C1NC2=CC=CC=C2\C1=C/C1=CN=CN1 VEEGZPWAAPPXRB-BJMVGYQFSA-N 0.000 claims 3
- 229940122440 HIV protease inhibitor Drugs 0.000 claims 3
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 3
- 229940123468 Transferase inhibitor Drugs 0.000 claims 3
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 3
- 229940121369 angiogenesis inhibitor Drugs 0.000 claims 3
- 230000001028 anti-proliverative effect Effects 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 239000002254 cytotoxic agent Substances 0.000 claims 3
- 229940127089 cytotoxic agent Drugs 0.000 claims 3
- 231100000599 cytotoxic agent Toxicity 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 239000004030 hiv protease inhibitor Substances 0.000 claims 3
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 3
- 229940075993 receptor modulator Drugs 0.000 claims 3
- 102000027483 retinoid hormone receptors Human genes 0.000 claims 3
- 108091008679 retinoid hormone receptors Proteins 0.000 claims 3
- 239000003558 transferase inhibitor Substances 0.000 claims 3
- 102100025306 Integrin alpha-IIb Human genes 0.000 claims 2
- 101710149643 Integrin alpha-IIb Proteins 0.000 claims 2
- 150000001204 N-oxides Chemical class 0.000 claims 2
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims 2
- 239000005557 antagonist Substances 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 238000001959 radiotherapy Methods 0.000 claims 2
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims 2
- 239000000849 selective androgen receptor modulator Substances 0.000 claims 2
- FQJJCPJSVFSADI-UHFFFAOYSA-N 1-[4-[[2-[(5-phenyl-1,3-thiazol-2-yl)amino]pyridin-4-yl]methyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1CC1=CC=NC(NC=2SC(=CN=2)C=2C=CC=CC=2)=C1 FQJJCPJSVFSADI-UHFFFAOYSA-N 0.000 claims 1
- NVJDZCZMQHCHHE-UHFFFAOYSA-N 1-[[2-[(5-phenyl-1,3-thiazol-2-yl)amino]pyridin-4-yl]methyl]piperidine-3-carboxylic acid Chemical compound C1C(C(=O)O)CCCN1CC1=CC=NC(NC=2SC(=CN=2)C=2C=CC=CC=2)=C1 NVJDZCZMQHCHHE-UHFFFAOYSA-N 0.000 claims 1
- AKSUYZOAHTYTCG-UHFFFAOYSA-N 1-ethyl-4-[[2-[(5-phenyl-1,3-thiazol-2-yl)amino]pyridin-4-yl]methyl]piperazine-2,3-dione Chemical compound O=C1C(=O)N(CC)CCN1CC1=CC=NC(NC=2SC(=CN=2)C=2C=CC=CC=2)=C1 AKSUYZOAHTYTCG-UHFFFAOYSA-N 0.000 claims 1
- JIEUMKHQJAYXEW-UHFFFAOYSA-N 1-methyl-4-[[2-[(5-phenyl-1,3-thiazol-2-yl)amino]pyridin-4-yl]methyl]piperazin-2-one Chemical compound C1C(=O)N(C)CCN1CC1=CC=NC(NC=2SC(=CN=2)C=2C=CC=CC=2)=C1 JIEUMKHQJAYXEW-UHFFFAOYSA-N 0.000 claims 1
- UEJJHQNACJXSKW-UHFFFAOYSA-N 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1C1CCC(=O)NC1=O UEJJHQNACJXSKW-UHFFFAOYSA-N 0.000 claims 1
- LJXLOEHKZRKIIO-UHFFFAOYSA-N 2-[[4-(piperazin-1-ylmethyl)pyridin-2-yl]amino]-1,3-thiazole-5-carbonitrile Chemical compound S1C(C#N)=CN=C1NC1=CC(CN2CCNCC2)=CC=N1 LJXLOEHKZRKIIO-UHFFFAOYSA-N 0.000 claims 1
- XDYCIZMIODKDCK-UHFFFAOYSA-N 2-[[4-[(4-acetylpiperazin-1-yl)methyl]pyridin-2-yl]amino]-1,3-thiazole-5-carbonitrile Chemical compound C1CN(C(=O)C)CCN1CC1=CC=NC(NC=2SC(=CN=2)C#N)=C1 XDYCIZMIODKDCK-UHFFFAOYSA-N 0.000 claims 1
- UMQOALQQFLEVNG-UHFFFAOYSA-N 2-[[4-[(4-methylsulfonylpiperazin-1-yl)methyl]pyridin-2-yl]amino]-1,3-thiazole-5-carbonitrile Chemical compound C1CN(S(=O)(=O)C)CCN1CC1=CC=NC(NC=2SC(=CN=2)C#N)=C1 UMQOALQQFLEVNG-UHFFFAOYSA-N 0.000 claims 1
- PYEWLRYVZITCIE-UHFFFAOYSA-N 2-[[4-[(piperidin-4-ylmethylamino)methyl]pyridin-2-yl]amino]-1,3-thiazole-5-carbonitrile Chemical compound S1C(C#N)=CN=C1NC1=CC(CNCC2CCNCC2)=CC=N1 PYEWLRYVZITCIE-UHFFFAOYSA-N 0.000 claims 1
- WUAWDHDGRGQQSS-UHFFFAOYSA-N 2-[[4-[[4-(2-hydroxyacetyl)piperazin-1-yl]methyl]pyridin-2-yl]amino]-1,3-thiazole-5-carbonitrile Chemical compound C1CN(C(=O)CO)CCN1CC1=CC=NC(NC=2SC(=CN=2)C#N)=C1 WUAWDHDGRGQQSS-UHFFFAOYSA-N 0.000 claims 1
- APCZORVVDYPETN-UHFFFAOYSA-N 4-[[2-[(5-cyano-1,3-thiazol-2-yl)amino]pyridin-4-yl]methyl]-n,n-dimethylpiperazine-1-carboxamide Chemical compound C1CN(C(=O)N(C)C)CCN1CC1=CC=NC(NC=2SC(=CN=2)C#N)=C1 APCZORVVDYPETN-UHFFFAOYSA-N 0.000 claims 1
- 102000012936 Angiostatins Human genes 0.000 claims 1
- 108010079709 Angiostatins Proteins 0.000 claims 1
- 229910014585 C2-Ce Inorganic materials 0.000 claims 1
- HVXBOLULGPECHP-WAYWQWQTSA-N Combretastatin A4 Chemical compound C1=C(O)C(OC)=CC=C1\C=C/C1=CC(OC)=C(OC)C(OC)=C1 HVXBOLULGPECHP-WAYWQWQTSA-N 0.000 claims 1
- 229940122204 Cyclooxygenase inhibitor Drugs 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 102000015696 Interleukins Human genes 0.000 claims 1
- 108010063738 Interleukins Proteins 0.000 claims 1
- 229940124761 MMP inhibitor Drugs 0.000 claims 1
- 208000022873 Ocular disease Diseases 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 102000010780 Platelet-Derived Growth Factor Human genes 0.000 claims 1
- 108010038512 Platelet-Derived Growth Factor Proteins 0.000 claims 1
- UIRKNQLZZXALBI-MSVGPLKSSA-N Squalamine Chemical compound C([C@@H]1C[C@H]2O)[C@@H](NCCCNCCCCN)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@H](C)CC[C@H](C(C)C)OS(O)(=O)=O)[C@@]2(C)CC1 UIRKNQLZZXALBI-MSVGPLKSSA-N 0.000 claims 1
- UIRKNQLZZXALBI-UHFFFAOYSA-N Squalamine Natural products OC1CC2CC(NCCCNCCCCN)CCC2(C)C2C1C1CCC(C(C)CCC(C(C)C)OS(O)(=O)=O)C1(C)CC2 UIRKNQLZZXALBI-UHFFFAOYSA-N 0.000 claims 1
- 239000003098 androgen Substances 0.000 claims 1
- FZCSTZYAHCUGEM-UHFFFAOYSA-N aspergillomarasmine B Natural products OC(=O)CNC(C(O)=O)CNC(C(O)=O)CC(O)=O FZCSTZYAHCUGEM-UHFFFAOYSA-N 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- WNRZHQBJSXRYJK-UHFFFAOYSA-N carboxyamidotriazole Chemical compound NC1=C(C(=O)N)N=NN1CC(C=C1Cl)=CC(Cl)=C1C(=O)C1=CC=C(Cl)C=C1 WNRZHQBJSXRYJK-UHFFFAOYSA-N 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 claims 1
- 229960005537 combretastatin A-4 Drugs 0.000 claims 1
- HVXBOLULGPECHP-UHFFFAOYSA-N combretastatin A4 Natural products C1=C(O)C(OC)=CC=C1C=CC1=CC(OC)=C(OC)C(OC)=C1 HVXBOLULGPECHP-UHFFFAOYSA-N 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 210000002950 fibroblast Anatomy 0.000 claims 1
- 102000006495 integrins Human genes 0.000 claims 1
- 108010044426 integrins Proteins 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- YNGAAYRYZIAUJL-UHFFFAOYSA-N n-[1-[[2-[(5-cyano-1,3-thiazol-2-yl)amino]pyridin-4-yl]methyl]pyrrolidin-3-yl]methanesulfonamide Chemical compound C1C(NS(=O)(=O)C)CCN1CC1=CC=NC(NC=2SC(=CN=2)C#N)=C1 YNGAAYRYZIAUJL-UHFFFAOYSA-N 0.000 claims 1
- YFVAGXCBQNGTOV-UHFFFAOYSA-N n-[4-[(4-methylsulfonylpiperazin-1-yl)methyl]pyridin-2-yl]-5-phenyl-1,3-thiazol-2-amine Chemical compound C1CN(S(=O)(=O)C)CCN1CC1=CC=NC(NC=2SC(=CN=2)C=2C=CC=CC=2)=C1 YFVAGXCBQNGTOV-UHFFFAOYSA-N 0.000 claims 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 239000002599 prostaglandin synthase inhibitor Substances 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 208000007442 rickets Diseases 0.000 claims 1
- 229950001248 squalamine Drugs 0.000 claims 1
- 229960001603 tamoxifen Drugs 0.000 claims 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 1
- 229960003433 thalidomide Drugs 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- COKMIXFXJJXBQG-NRFANRHFSA-N tirofiban Chemical group C1=CC(C[C@H](NS(=O)(=O)CCCC)C(O)=O)=CC=C1OCCCCC1CCNCC1 COKMIXFXJJXBQG-NRFANRHFSA-N 0.000 claims 1
- 229960003425 tirofiban Drugs 0.000 claims 1
- 230000000451 tissue damage Effects 0.000 claims 1
- 231100000827 tissue damage Toxicity 0.000 claims 1
- 229960000575 trastuzumab Drugs 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 208000027930 type IV hypersensitivity disease Diseases 0.000 claims 1
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 claims 1
- 108010073929 Vascular Endothelial Growth Factor A Proteins 0.000 description 20
- 102000005962 receptors Human genes 0.000 description 17
- 108020003175 receptors Proteins 0.000 description 17
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 description 7
- 102000016549 Vascular Endothelial Growth Factor Receptor-2 Human genes 0.000 description 7
- 102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 description 5
- 230000012010 growth Effects 0.000 description 5
- 230000019491 signal transduction Effects 0.000 description 5
- 101100381481 Caenorhabditis elegans baz-2 gene Proteins 0.000 description 4
- 108700020796 Oncogene Proteins 0.000 description 4
- 101100372762 Rattus norvegicus Flt1 gene Proteins 0.000 description 4
- 230000004614 tumor growth Effects 0.000 description 4
- 102000004190 Enzymes Human genes 0.000 description 3
- 108090000790 Enzymes Proteins 0.000 description 3
- 241000699670 Mus sp. Species 0.000 description 3
- 108091000080 Phosphotransferase Proteins 0.000 description 3
- 108091008605 VEGF receptors Proteins 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 230000006870 function Effects 0.000 description 3
- 230000014509 gene expression Effects 0.000 description 3
- 230000005764 inhibitory process Effects 0.000 description 3
- 230000002297 mitogenic effect Effects 0.000 description 3
- 102000020233 phosphotransferase Human genes 0.000 description 3
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 description 2
- 208000005623 Carcinogenesis Diseases 0.000 description 2
- 241000699660 Mus musculus Species 0.000 description 2
- 206010029113 Neovascularisation Diseases 0.000 description 2
- 102000043276 Oncogene Human genes 0.000 description 2
- 241000288906 Primates Species 0.000 description 2
- 108010034265 Vascular Endothelial Growth Factor Receptors Proteins 0.000 description 2
- 230000002491 angiogenic effect Effects 0.000 description 2
- 210000004204 blood vessel Anatomy 0.000 description 2
- 230000036952 cancer formation Effects 0.000 description 2
- 231100000504 carcinogenesis Toxicity 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 2
- 230000003834 intracellular effect Effects 0.000 description 2
- 239000003446 ligand Substances 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- 238000011580 nude mouse model Methods 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 210000001525 retina Anatomy 0.000 description 2
- 239000000758 substrate Substances 0.000 description 2
- 210000003556 vascular endothelial cell Anatomy 0.000 description 2
- BJHCYTJNPVGSBZ-YXSASFKJSA-N 1-[4-[6-amino-5-[(Z)-methoxyiminomethyl]pyrimidin-4-yl]oxy-2-chlorophenyl]-3-ethylurea Chemical compound CCNC(=O)Nc1ccc(Oc2ncnc(N)c2\C=N/OC)cc1Cl BJHCYTJNPVGSBZ-YXSASFKJSA-N 0.000 description 1
- ZKHQWZAMYRWXGA-KQYNXXCUSA-J ATP(4-) Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP([O-])(=O)OP([O-])(=O)OP([O-])([O-])=O)[C@@H](O)[C@H]1O ZKHQWZAMYRWXGA-KQYNXXCUSA-J 0.000 description 1
- ZKHQWZAMYRWXGA-UHFFFAOYSA-N Adenosine triphosphate Natural products C1=NC=2C(N)=NC=NC=2N1C1OC(COP(O)(=O)OP(O)(=O)OP(O)(O)=O)C(O)C1O ZKHQWZAMYRWXGA-UHFFFAOYSA-N 0.000 description 1
- 108700028369 Alleles Proteins 0.000 description 1
- 102000007299 Amphiregulin Human genes 0.000 description 1
- 108010033760 Amphiregulin Proteins 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 102000056058 Betacellulin Human genes 0.000 description 1
- 101800001382 Betacellulin Proteins 0.000 description 1
- 201000004569 Blindness Diseases 0.000 description 1
- 102100025064 Cellular tumor antigen p53 Human genes 0.000 description 1
- 108090000695 Cytokines Proteins 0.000 description 1
- 102000004127 Cytokines Human genes 0.000 description 1
- 101000827763 Drosophila melanogaster Fibroblast growth factor receptor homolog 1 Proteins 0.000 description 1
- 101710113436 GTPase KRas Proteins 0.000 description 1
- 102000018710 Heparin-binding EGF-like Growth Factor Human genes 0.000 description 1
- 101800001649 Heparin-binding EGF-like growth factor Proteins 0.000 description 1
- 101001005128 Homo sapiens LIM domain kinase 1 Proteins 0.000 description 1
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 description 1
- 206010021143 Hypoxia Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 102100023915 Insulin Human genes 0.000 description 1
- 108090001061 Insulin Proteins 0.000 description 1
- 102100026023 LIM domain kinase 1 Human genes 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241001529936 Murinae Species 0.000 description 1
- 101100372766 Mus musculus Kdr gene Proteins 0.000 description 1
- 101100268066 Mus musculus Zap70 gene Proteins 0.000 description 1
- 102400000058 Neuregulin-1 Human genes 0.000 description 1
- 108090000556 Neuregulin-1 Proteins 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 208000034038 Pathologic Neovascularization Diseases 0.000 description 1
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 description 1
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 description 1
- 101000852966 Rattus norvegicus Interleukin-1 receptor-like 1 Proteins 0.000 description 1
- 102000004278 Receptor Protein-Tyrosine Kinases Human genes 0.000 description 1
- 108090000873 Receptor Protein-Tyrosine Kinases Proteins 0.000 description 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 description 1
- 102100029986 Receptor tyrosine-protein kinase erbB-3 Human genes 0.000 description 1
- 101710100969 Receptor tyrosine-protein kinase erbB-3 Proteins 0.000 description 1
- 102100029981 Receptor tyrosine-protein kinase erbB-4 Human genes 0.000 description 1
- 101710100963 Receptor tyrosine-protein kinase erbB-4 Proteins 0.000 description 1
- 108010053096 Vascular Endothelial Growth Factor Receptor-1 Proteins 0.000 description 1
- 102100033178 Vascular endothelial growth factor receptor 1 Human genes 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 230000001772 anti-angiogenic effect Effects 0.000 description 1
- 230000003305 autocrine Effects 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 230000024245 cell differentiation Effects 0.000 description 1
- 230000003915 cell function Effects 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 230000005754 cellular signaling Effects 0.000 description 1
- 230000003399 chemotactic effect Effects 0.000 description 1
- 208000029742 colonic neoplasm Diseases 0.000 description 1
- 230000001086 cytosolic effect Effects 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 210000001671 embryonic stem cell Anatomy 0.000 description 1
- 210000002889 endothelial cell Anatomy 0.000 description 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 description 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 description 1
- 208000021045 exocrine pancreatic carcinoma Diseases 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000001605 fetal effect Effects 0.000 description 1
- 108091071773 flk family Proteins 0.000 description 1
- 238000003209 gene knockout Methods 0.000 description 1
- 208000005017 glioblastoma Diseases 0.000 description 1
- 239000000833 heterodimer Substances 0.000 description 1
- 230000000521 hyperimmunizing effect Effects 0.000 description 1
- 230000001146 hypoxic effect Effects 0.000 description 1
- 230000006698 induction Effects 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 229940125396 insulin Drugs 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 108020004999 messenger RNA Proteins 0.000 description 1
- 239000003226 mitogen Substances 0.000 description 1
- 230000000394 mitotic effect Effects 0.000 description 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 description 1
- 230000017074 necrotic cell death Effects 0.000 description 1
- 230000000263 nonmitogenic effect Effects 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 230000003076 paracrine Effects 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 description 1
- 230000026731 phosphorylation Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 238000011809 primate model Methods 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 108010014186 ras Proteins Proteins 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 208000004644 retinal vein occlusion Diseases 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 238000011808 rodent model Methods 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 108091008578 transmembrane receptors Proteins 0.000 description 1
- 102000027257 transmembrane receptors Human genes 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 125000001493 tyrosinyl group Chemical group [H]OC1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 description 1
- 230000006444 vascular growth Effects 0.000 description 1
- 230000004862 vasculogenesis Effects 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
Classifications
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
- 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
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15334899P | 1999-09-10 | 1999-09-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200201898B true ZA200201898B (en) | 2003-05-28 |
Family
ID=22546828
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200201898A ZA200201898B (en) | 1999-09-10 | 2002-03-07 | Tyrosine kinase inhibitors. |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US6586423B2 (no) |
| EP (1) | EP1218376B1 (no) |
| JP (2) | JP3892296B2 (no) |
| KR (1) | KR20020027635A (no) |
| CN (1) | CN1390215A (no) |
| AT (1) | ATE309241T1 (no) |
| AU (1) | AU779908B2 (no) |
| BG (1) | BG106465A (no) |
| BR (1) | BR0013899A (no) |
| CA (1) | CA2384101A1 (no) |
| CZ (1) | CZ2002861A3 (no) |
| DE (1) | DE60023926T2 (no) |
| EA (1) | EA200200351A1 (no) |
| EE (1) | EE200200123A (no) |
| ES (1) | ES2250186T3 (no) |
| HU (1) | HUP0202682A3 (no) |
| IL (1) | IL148385A0 (no) |
| MX (1) | MXPA02002559A (no) |
| NO (1) | NO20021166L (no) |
| PL (1) | PL355639A1 (no) |
| SK (1) | SK4772002A3 (no) |
| WO (1) | WO2001017995A1 (no) |
| ZA (1) | ZA200201898B (no) |
Families Citing this family (175)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2308833A3 (en) | 1999-04-15 | 2011-09-28 | Bristol-Myers Squibb Company | Cyclic protein tyrosine kinase inhibitors |
| PT1347971E (pt) | 2000-12-21 | 2006-06-30 | Bristol Myers Squibb Co | Inibidores tiazolilicos de tirosina-cinases da familia tec |
| ATE430742T1 (de) | 2000-12-21 | 2009-05-15 | Smithkline Beecham Corp | Pyrimidinamine als angiogenesemodulatoren |
| EP1671969A3 (en) * | 2000-12-21 | 2006-07-26 | Bristol-Myers Squibb Company | Thiazolyl inhibitors of tec family tyrosine kinases |
| CA2436487A1 (en) * | 2001-01-30 | 2002-08-08 | Cytopia Pty Ltd. | Methods of inhibiting kinases |
| US7081454B2 (en) | 2001-03-28 | 2006-07-25 | Bristol-Myers Squibb Co. | Tyrosine kinase inhibitors |
| JP2004536057A (ja) | 2001-05-11 | 2004-12-02 | バーテックス ファーマシューティカルズ インコーポレイテッド | ｐ３８インヒビターとして使用する２，５−二置換ピリジン、ピリミジン、ピリダジンおよび１，２，４−トリアジンの誘導体 |
| CA2450934A1 (en) | 2001-06-19 | 2002-12-27 | Marco Dodier | Pyrimidine inhibitors of phosphodiesterase (pde) 7 |
| WO2003000687A1 (en) * | 2001-06-22 | 2003-01-03 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| DE10133665A1 (de) * | 2001-07-11 | 2003-01-30 | Boehringer Ingelheim Pharma | Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Herstellung |
| WO2003015778A1 (en) | 2001-08-17 | 2003-02-27 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| ES2429132T3 (es) | 2001-08-31 | 2013-11-13 | The Rockefeller University | Atividad de fosfodiesterasa y regulación de la señalización mediada por fosfodiesterasa 1-B en el cerebro |
| AU2002329000A1 (en) * | 2001-09-24 | 2003-04-07 | University Of Aarhus | Methods for diagnosis and treatment of diseases associated with altered expression of pik3r1 |
| WO2003062215A1 (en) * | 2002-01-25 | 2003-07-31 | Kylix Pharmaceuticals B.V. | 4(hetero-) aryl substituted (thia-/oxa-/pyra) zoles for inhibition of tie-2 |
| US20040014744A1 (en) * | 2002-04-05 | 2004-01-22 | Fortuna Haviv | Substituted pyridines having antiangiogenic activity |
| JP2005530745A (ja) | 2002-05-02 | 2005-10-13 | メルク エンド カムパニー インコーポレーテッド | チロシンキナーゼ阻害剤 |
| DE60317198T2 (de) * | 2002-05-23 | 2008-12-04 | Cytopia Research Pty. Ltd., Richmond | Proteinkinaseinhibitoren |
| US6872724B2 (en) | 2002-07-24 | 2005-03-29 | Merck & Co., Inc. | Polymorphs with tyrosine kinase activity |
| US20040023981A1 (en) * | 2002-07-24 | 2004-02-05 | Yu Ren | Salt forms with tyrosine kinase activity |
| US20040023978A1 (en) * | 2002-07-24 | 2004-02-05 | Yu Ren | Active salt forms with tyrosine kinase activity |
| AR043057A1 (es) * | 2002-10-30 | 2005-07-13 | Vertex Pharma | Compuestos derivados de piridintiazoles como inhibidores de la quinasa rock y otras proteinas quinasa |
| AU2002953255A0 (en) * | 2002-12-11 | 2003-01-02 | Cytopia Research Pty Ltd | Protein kinase inhibitors |
| GB0305152D0 (en) | 2003-03-06 | 2003-04-09 | Novartis Ag | Organic compounds |
| GB2400101A (en) * | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
| AR044519A1 (es) * | 2003-05-02 | 2005-09-14 | Novartis Ag | Derivados de piridin-tiazol amina y de pirimidin-tiazol amina |
| WO2005000208A2 (en) * | 2003-05-30 | 2005-01-06 | Combinatorx, Inc. | Combination therapy for the treatment of neoplasms |
| EP1644365A2 (en) * | 2003-07-02 | 2006-04-12 | Biofocus Discovery Ltd | Pyrazine and pyridine derivatives as rho kinase inhibitors |
| US7312215B2 (en) | 2003-07-29 | 2007-12-25 | Bristol-Myers Squibb Company | Benzimidazole C-2 heterocycles as kinase inhibitors |
| US20050107350A1 (en) * | 2003-08-22 | 2005-05-19 | Pharmacia Corporation | Method for the treatment or prevention of bone disorders with a cyclooxygenase-2 inhibitor alone and in combination with a bone disorder treatment agent and compositions therewith |
| GB0320197D0 (en) | 2003-08-28 | 2003-10-01 | Novartis Ag | Organic compounds |
| US7572799B2 (en) | 2003-11-24 | 2009-08-11 | Pfizer Inc | Pyrazolo[4,3-d]pyrimidines as Phosphodiesterase Inhibitors |
| SI1689715T1 (sl) | 2003-12-03 | 2011-07-29 | Ym Biosciences Australia Pty | Inhibitorji tubulina |
| US7294640B2 (en) | 2004-02-06 | 2007-11-13 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| WO2006008874A1 (ja) * | 2004-05-21 | 2006-01-26 | Banyu Pharmaceutical Co., Ltd. | アミノチアゾール骨格を有するＣｄｋ４，６選択的阻害剤 |
| CA2568451A1 (en) * | 2004-06-04 | 2005-12-22 | Arena Pharmaceuticals, Inc. | Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
| EP1828165B1 (en) * | 2004-10-29 | 2013-03-20 | Msd K.K. | Novel aminopyridine derivatives having aurora a selective inhibitory action |
| US7491720B2 (en) | 2004-10-29 | 2009-02-17 | Banyu Pharmaceutical Co., Ltd. | Aminopyridine derivatives having Aurora A selective inhibitory action |
| CA2585490A1 (en) * | 2004-11-12 | 2006-05-18 | Galapagos Nv | Nitrogen heteroaromatic compounds which bind to the active site of protein kinase enzymes |
| GB0428082D0 (en) * | 2004-12-22 | 2005-01-26 | Welcome Trust The Ltd | Therapeutic compounds |
| EP1846394B1 (en) | 2005-02-04 | 2011-10-26 | AstraZeneca AB | Pyrazolylaminopyridine derivatives useful as kinase inhibitors |
| DE602006001515D1 (de) | 2005-02-16 | 2008-07-31 | Astrazeneca Ab | Chemische verbindungen |
| US20080287437A1 (en) | 2005-05-16 | 2008-11-20 | Astrazeneca Ab | Pyrazolylaminopyrimidine Derivatives Useful as Tyrosine Kinase Inhibitors |
| WO2006125803A1 (en) | 2005-05-24 | 2006-11-30 | Laboratoires Serono S.A. | Thiazole derivatives and use thereof |
| WO2006129842A1 (ja) * | 2005-06-01 | 2006-12-07 | Banyu Pharmaceutical Co., Ltd. | オーロラa選択的阻害作用を有する新規アミノピリジン誘導体 |
| CN101248050B (zh) | 2005-06-06 | 2013-07-17 | 武田药品工业株式会社 | 有机化合物 |
| US20090233896A1 (en) * | 2005-06-09 | 2009-09-17 | Arrington Kenneth L | Inhibitors of checkpoint kinases |
| CN101273023A (zh) * | 2005-08-02 | 2008-09-24 | Irm责任有限公司 | 作为蛋白激酶抑制剂的5-取代的噻唑-2-基氨基化合物和组合物 |
| EP1919287A4 (en) * | 2005-08-23 | 2010-04-28 | Intra Cellular Therapies Inc | ORGANIC COMPOUNDS FOR TREATING A REDUCED DOPAMINE RECEPTOR SIGNALING ACTIVITY |
| US20080287475A1 (en) | 2005-10-28 | 2008-11-20 | Astrazeneca Ab | 4-(3-Aminopyrazole) Pyrimidine Derivatives for Use as Tyrosine Kinase Inhibitors in the Treatment of Cancer |
| WO2007053345A1 (en) * | 2005-11-01 | 2007-05-10 | Array Biopharma Inc. | Glucokinase activators |
| US20070130203A1 (en) * | 2005-12-07 | 2007-06-07 | Ask Jeeves, Inc. | Method and system to provide targeted advertising with search results |
| KR100728221B1 (ko) * | 2005-12-08 | 2007-06-13 | 한국전자통신연구원 | 터보부호 ｏｆｄｍ 시스템용 반복적 잔류 주파수 위상 보정장치 및 그 방법 |
| US7572809B2 (en) * | 2005-12-19 | 2009-08-11 | Hoffmann-La Roche Inc. | Isoquinoline aminopyrazole derivatives |
| JP5236499B2 (ja) * | 2006-01-27 | 2013-07-17 | アレイ バイオファーマ、インコーポレイテッド | グルコキナーゼ活性化剤 |
| WO2007097839A2 (en) * | 2006-02-16 | 2007-08-30 | Massachusetts Eye And Ear Infirmary | Ansamycin analogs or heat shock 90 inhibitors in combination with pdt treatin conditions of the eye |
| CA2647208C (en) | 2006-03-24 | 2014-05-13 | Array Biopharma Inc. | Glucokinase activators |
| WO2007125405A2 (en) * | 2006-05-01 | 2007-11-08 | Pfizer Products Inc. | Substituted 2-amino-fused heterocyclic compounds |
| US8246966B2 (en) * | 2006-08-07 | 2012-08-21 | University Of Georgia Research Foundation, Inc. | Trypanosome microsome system and uses thereof |
| JP2008081492A (ja) * | 2006-08-31 | 2008-04-10 | Banyu Pharmaceut Co Ltd | オーロラａ選択的阻害作用を有する新規アミノピリジン誘導体 |
| ES2411604T3 (es) | 2006-11-13 | 2013-07-05 | Intra-Cellular Therapies, Inc. | Compuestos orgánicos |
| US8338433B2 (en) * | 2006-11-22 | 2012-12-25 | University Of Georgia Research Foundation, Inc. | Tyrosine kinase inhibitors as anti-kinetoplastid agents |
| EP2089034A4 (en) | 2006-12-05 | 2010-07-28 | Intra Cellular Therapies Inc | NEW USES |
| MX2009006543A (es) | 2006-12-20 | 2009-06-26 | Amgen Inc | Compuestos heterociclicos y su uso en el tratamiento de la inflamacion, angiogenesis y cancer. |
| MX2009008665A (es) * | 2007-02-13 | 2009-08-21 | Ab Science | Procedimiento para la sintesis de compuestos de 2-aminotiazol como inhibidores de quinasa. |
| CA2680122A1 (en) | 2007-03-05 | 2008-09-18 | Kyowa Hakko Kirin Co., Ltd. | Pharmaceutical composition |
| UA99459C2 (en) | 2007-05-04 | 2012-08-27 | Астразенека Аб | 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer |
| ES2569734T3 (es) * | 2007-09-21 | 2016-05-12 | Array Biopharma, Inc. | Derivados de piridin-2-il-tiourea y de piridin-2-il-amina como intermedios para la preparación de piridin-2-il-amino-1,2,4-tiadiazoles activadores de la glucocinasa |
| NZ585236A (en) | 2007-10-09 | 2012-03-30 | Merck Patent Gmbh | Pyridine derivatives useful as glucokinase activators |
| CN101952282A (zh) | 2007-12-20 | 2011-01-19 | 诺瓦提斯公司 | 用作pi 3激酶抑制剂的噻唑衍生物 |
| JPWO2009130900A1 (ja) * | 2008-04-24 | 2011-08-11 | 日本曹達株式会社 | オキシム誘導体、中間体化合物および植物病害防除剤 |
| UA104147C2 (uk) | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
| US11464781B2 (en) | 2009-02-25 | 2022-10-11 | Intra-Cellular Therapies, Inc. | PDE1 inhibitors for ophthalmic disorders |
| JP2012526810A (ja) | 2009-05-13 | 2012-11-01 | イントラ−セルラー・セラピーズ・インコーポレイテッド | 有機化合物 |
| US8293753B2 (en) * | 2009-07-02 | 2012-10-23 | Novartis Ag | Substituted 2-carboxamide cycloamino ureas |
| EP2947098B1 (en) | 2009-07-20 | 2019-11-20 | Bristol-Myers Squibb Company | Combination of anti-ctla4 antibody with gemcitabine for the synergistic treatment of proliferative diseases |
| SG10201507362TA (en) | 2009-08-05 | 2015-10-29 | Intra Cellular Therapies Inc | Novel Regulatory Proteins And Inhibitors |
| JP5513620B2 (ja) | 2009-08-31 | 2014-06-04 | ポステック・アカデミー‐インダストリー・ファウンデーション | 血管内皮細胞成長因子受容体の阻害によるＴｈ１７炎症疾患治療方法およびこのための薬学的組成物 |
| AU2010310746B2 (en) | 2009-10-20 | 2015-07-23 | Nestec S.A. | Proximity-mediated assays for detecting oncogenic fusion proteins |
| KR100953511B1 (ko) * | 2009-12-28 | 2010-04-21 | (주)지노믹트리 | 건선 진단용 키트 및 칩 |
| EP2519517B1 (en) | 2009-12-29 | 2015-03-25 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
| CA2816957A1 (en) | 2010-11-07 | 2012-05-10 | Targegen, Inc. | Compositions and methods for treating myelofibrosis |
| MX2013006101A (es) | 2010-12-17 | 2013-07-02 | Hoffmann La Roche | Compuestos heterociclicos nitrogenados sustituidos fusionados en posicion 6,6 y usos de los mismos. |
| CN103501832B (zh) | 2011-02-17 | 2016-10-19 | 雀巢产品技术援助有限公司 | 通过过滤分离白细胞和肿瘤细胞的装置和方法 |
| UA112539C2 (uk) | 2011-03-03 | 2016-09-26 | Новартіс Аг | Спосіб одержання похідних 2-карбоксамідциклоаміносечовини |
| US9255072B2 (en) * | 2011-03-04 | 2016-02-09 | National Health Rsearch Institutes | Pyrazole compounds and thiazole compounds as protein kinases inhibitors |
| RU2011122942A (ru) * | 2011-06-08 | 2012-12-20 | Общество С Ограниченной Ответственностью "Асинэкс Медхим" | Новые ингибиторы киназ |
| US8912224B2 (en) | 2011-09-12 | 2014-12-16 | Sanofi | Substituted 2-(chroman-6-yloxy)-thiazoles and their use as pharmaceuticals |
| PT2567958E (pt) | 2011-09-12 | 2015-01-14 | Sanofi Sa | 2-(croman-6-iloxi)-tiazoles substituídos e sua utilização como produtos farmacêuticos |
| AU2011376746B2 (en) | 2011-09-12 | 2017-06-15 | Sanofi | Substituted 2-(chroman-6-yloxy)-thiazoles and their use as pharmaceuticals |
| PL2844282T3 (pl) | 2012-05-04 | 2019-11-29 | Pfizer | Antygeny związane z gruczołem krokowym i schematy immunoterapii oparte na szczepionce |
| CN104470918A (zh) * | 2012-05-30 | 2015-03-25 | 日本新药株式会社 | 芳香族杂环衍生物及医药 |
| JP6549040B2 (ja) | 2013-02-17 | 2019-07-24 | イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． | 新規使用 |
| TWI659032B (zh) | 2013-03-15 | 2019-05-11 | 美商內胞醫療公司 | 有機化合物及其用途 |
| JP2016518343A (ja) | 2013-03-15 | 2016-06-23 | イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． | 新規使用 |
| CN103254184B (zh) * | 2013-05-27 | 2015-03-18 | 湖南科技大学 | 5-取代-3-[5-羟基-4-吡喃酮-2-基-甲硫基]-4-氨基-1,2,4-三唑类化合物及其用途 |
| CN103319467B (zh) * | 2013-06-15 | 2015-10-14 | 湖南科技大学 | 一种4-[5-羟基-4-吡喃酮-2-基亚甲氨基]-3-巯基-1,2,4-三唑化合物及用途 |
| TWI623551B (zh) | 2013-08-02 | 2018-05-11 | 輝瑞大藥廠 | 抗ｃｘｃｒ４抗體及抗體－藥物結合物 |
| PL226024B1 (pl) | 2013-10-23 | 2017-06-30 | Wrocławskie Centrum Badań Eit + Spółka Z Ograniczoną | Zastosowanie N-[2-[4-(4-metoksyfenylo)-1,3-tiazol-2-ilo]etylo]- -2-okso-2,5,6,7-tetrahydrocyklopenta[b] pirydyno-3-karboksyamidu |
| US9884872B2 (en) | 2014-06-20 | 2018-02-06 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US10285992B2 (en) | 2014-08-07 | 2019-05-14 | Intra-Cellular Therapies, Inc. | Combinations of PDE1 inhibitors and NEP inhibitors and associated methods |
| US10131671B2 (en) | 2014-08-07 | 2018-11-20 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US10059702B2 (en) * | 2014-09-08 | 2018-08-28 | The Johns Hopkins University | Inhibitors of LC3/ATG3 interaction and their use in the treatment of cancer |
| AU2015317527B2 (en) | 2014-09-17 | 2020-08-20 | Intra-Cellular Therapies, Inc. | Compounds and methods |
| US10704104B2 (en) | 2014-10-20 | 2020-07-07 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods for screening a subject for a cancer |
| WO2016091891A1 (en) | 2014-12-09 | 2016-06-16 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Human monoclonal antibodies against axl |
| WO2016135041A1 (en) | 2015-02-26 | 2016-09-01 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Fusion proteins and antibodies comprising thereof for promoting apoptosis |
| JP6861166B2 (ja) | 2015-03-27 | 2021-04-21 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | サイクリン依存性キナーゼの阻害剤 |
| EP3300500B9 (en) | 2015-05-20 | 2021-01-13 | Amgen Inc. | Triazole agonists of the apj receptor |
| JP2018521021A (ja) * | 2015-06-11 | 2018-08-02 | バジリア・ファルマスーチカ・インターナショナル・アーゲーＢａｓｉｌｅａ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｉｎｔｅｒｎａｔｉｏｎａｌ Ａｇ | 排出ポンプ阻害剤及びその治療的使用 |
| JP2018525029A (ja) | 2015-07-07 | 2018-09-06 | インセルム（インスティチュート ナショナル デ ラ サンテ エ デ ラ リシェルシェ メディカル） | ミオシン１８ａに対する特異性を有する抗体およびその使用 |
| JP6791951B2 (ja) | 2015-08-27 | 2020-11-25 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 肺ガンを患っている患者の生存時間を予測するための方法 |
| EP3347018B1 (en) | 2015-09-09 | 2021-09-01 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| WO2017055322A1 (en) | 2015-09-29 | 2017-04-06 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for quantifying the population of neutrophils in a tissue sample |
| WO2017055327A1 (en) | 2015-09-29 | 2017-04-06 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for quantifying the population of endothelial cells in a tissue sample |
| WO2017055326A1 (en) | 2015-09-29 | 2017-04-06 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for quantifying the population of myeloid dendritic cells in a tissue sample |
| WO2017055324A1 (en) | 2015-09-29 | 2017-04-06 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for quantifying the population of cells of monocytic origin in a tissue sample |
| BR112018067525A2 (pt) | 2016-02-26 | 2019-02-05 | Centre Nat Rech Scient | anticorpos tendo especificidade para o btla e seus usos |
| US10682354B2 (en) | 2016-03-28 | 2020-06-16 | Intra-Cellular Therapies, Inc. | Compositions and methods |
| EP3452466B1 (en) | 2016-05-03 | 2020-08-12 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the apj receptor |
| RU2741786C2 (ru) | 2016-05-25 | 2021-01-28 | Энсэрм (Энститю Насьональ Де Ла Санте Э Де Ла Решерш Медикаль) | Способы и композиции для лечения опухолей |
| WO2018011166A2 (en) | 2016-07-12 | 2018-01-18 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for quantifying the population of myeloid dendritic cells in a tissue sample |
| JP7219207B2 (ja) | 2016-07-29 | 2023-02-07 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 腫瘍関連マクロファージを標的化する抗体及びその使用 |
| WO2018049417A1 (en) | 2016-09-12 | 2018-03-15 | Intra-Cellular Therapies, Inc. | Novel uses |
| MD3529262T2 (ro) | 2016-10-21 | 2022-01-31 | Inst Nat Sante Rech Med | Metode pentru promovarea răspunsului celulelor T |
| US20190345500A1 (en) | 2016-11-14 | 2019-11-14 | |Nserm (Institut National De La Santé Et De La Recherche Médicale) | Methods and pharmaceutical compositions for modulating stem cells proliferation or differentiation |
| WO2018093576A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Alkyl substituted triazole compounds as agonists of the apj receptor |
| EP3541792B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole furan compounds as agonists of the apj receptor |
| WO2018093577A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Cycloalkyl substituted triazole compounds as agonists of the apj receptor |
| WO2018097945A1 (en) | 2016-11-16 | 2018-05-31 | Amgen Inc. | Heteroaryl-substituted triazoles as apj receptor agonists |
| WO2018093580A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Triazole pyridyl compounds as agonists of the apj receptor |
| US10906890B2 (en) | 2016-11-16 | 2021-02-02 | Amgen Inc. | Triazole phenyl compounds as agonists of the APJ receptor |
| JP2020510432A (ja) | 2017-03-02 | 2020-04-09 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | Ｎｅｃｔｉｎ−４への特異性を有する抗体及びその使用 |
| WO2018185516A1 (en) | 2017-04-05 | 2018-10-11 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for treating cardiovascular toxicity induced by anti-cancer therapy |
| WO2018189403A1 (en) | 2017-04-14 | 2018-10-18 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of cancer |
| CN110769855A (zh) * | 2017-04-21 | 2020-02-07 | 史蒂文·霍夫曼 | 用于治疗视网膜病变的组合物和方法 |
| US11389434B2 (en) | 2017-05-18 | 2022-07-19 | Inserm | Methods and pharmaceutical compositions for the treatment of mast cell diseases |
| WO2019072885A1 (en) | 2017-10-11 | 2019-04-18 | INSERM (Institut National de la Santé et de la Recherche Médicale) | MAGNETIC NANOPARTICLES FOR THE TREATMENT OF CANCER |
| WO2019072888A1 (en) | 2017-10-11 | 2019-04-18 | INSERM (Institut National de la Santé et de la Recherche Médicale) | METHODS OF PREDICTING THE THERAPEUTIC RESPONSE IN HEPATOCELLULAR CANCER |
| EP3704122B1 (en) | 2017-11-03 | 2021-09-01 | Amgen Inc. | Fused triazole agonists of the apj receptor |
| JP7408036B2 (ja) | 2017-11-24 | 2024-01-05 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | ガンを処置するための方法及び組成物 |
| US11814686B2 (en) | 2017-12-07 | 2023-11-14 | Institut National de la Santéde la Recherche Médicale | Method for screening and treating a subject for a cancer |
| CN107868040A (zh) * | 2017-12-21 | 2018-04-03 | 苏州艾缇克药物化学有限公司 | 一种2‑氨基吡啶‑4‑甲酸甲酯的合成方法 |
| US11839614B2 (en) | 2018-01-31 | 2023-12-12 | Intra-Cellular Therapies, Inc. | Methods for treating or mitigating cardiotoxicity characterized by inhibition of adenosine A2 signaling and/or adenosine A2 receptor expression |
| US20210047696A1 (en) | 2018-03-28 | 2021-02-18 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for treating cancer |
| KR102245670B1 (ko) * | 2018-04-03 | 2021-04-29 | 영남대학교 산학협력단 | 신규한 6-헤테로아릴아미노-2,4,5-트라이메틸피리딘-3-올 화합물, 또는 이를 포함하는 염증성 장질환 및 자가면역 질환의 예방 또는 치료용 약학 조성물 |
| US20210164984A1 (en) | 2018-04-13 | 2021-06-03 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for predicting outcome and treatment of patients suffering from prostate cancer or breast cancer |
| US11807624B2 (en) | 2018-05-01 | 2023-11-07 | Amgen Inc. | Substituted pyrimidinones as agonists of the APJ receptor |
| WO2019211370A1 (en) | 2018-05-03 | 2019-11-07 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for treating cancer |
| WO2019211369A1 (en) | 2018-05-03 | 2019-11-07 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for treating cancer |
| US20210213020A1 (en) | 2018-05-30 | 2021-07-15 | Inserm (Institut National De La Santé Et De La Rechirche Médicale) | Methods and pharmaceutical compositions for treating cancer |
| WO2019234221A1 (en) | 2018-06-08 | 2019-12-12 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for stratification and treatment of a patient suffering from chronic lymphocytic leukemia |
| WO2020030634A1 (en) | 2018-08-06 | 2020-02-13 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and compositions for treating cancers |
| KR102328682B1 (ko) * | 2018-08-27 | 2021-11-18 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| WO2020053122A1 (en) | 2018-09-10 | 2020-03-19 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Combination of her2/neu antibody with heme for treating cancer |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| EP3924520A1 (en) | 2019-02-13 | 2021-12-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and compositions for selecting a cancer treatment in a subject suffering from cancer |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| WO2020180959A1 (en) | 2019-03-05 | 2020-09-10 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| WO2020178400A1 (en) | 2019-03-06 | 2020-09-10 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Method to diagnose a cmmrd |
| US11919904B2 (en) | 2019-03-29 | 2024-03-05 | Incyte Corporation | Sulfonylamide compounds as CDK2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| WO2020223558A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | Tricyclic amine compounds as cdk2 inhibitors |
| JP2022538733A (ja) | 2019-05-20 | 2022-09-06 | インセルム（インスティチュート ナショナル デ ラ サンテ エ デ ラ リシェルシェ メディカル） | 新規抗ｃｄ２５抗体 |
| US20220290244A1 (en) | 2019-08-02 | 2022-09-15 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Method for screening a subject for a cancer |
| PE20221010A1 (es) | 2019-08-14 | 2022-06-15 | Incyte Corp | Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2 |
| EP3800201A1 (en) | 2019-10-01 | 2021-04-07 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Cd28h stimulation enhances nk cell killing activities |
| JP2022551668A (ja) | 2019-10-11 | 2022-12-12 | インサイト・コーポレイション | Ｃｄｋ２阻害剤としての二環式アミン |
| WO2021116119A1 (en) | 2019-12-09 | 2021-06-17 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Antibodies having specificity to her4 and uses thereof |
| WO2021228956A1 (en) | 2020-05-12 | 2021-11-18 | INSERM (Institut National de la Santé et de la Recherche Médicale) | New method to treat cutaneous t-cell lymphomas and tfh derived lymphomas |
| WO2022101463A1 (en) | 2020-11-16 | 2022-05-19 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of the last c-terminal residues m31/41 of zikv m ectodomain for triggering apoptotic cell death |
| KR20230165202A (ko) | 2021-01-29 | 2023-12-05 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | Msi 암을 진단하는 방법 |
| US20220389104A1 (en) | 2021-05-28 | 2022-12-08 | Ose Immunotherapeutics | Method for Treating CD127-Positive Cancers by Administering an Anti-CD127 Agent |
| CN114230514A (zh) * | 2021-11-26 | 2022-03-25 | 渭南瑞联制药有限责任公司 | 一种合成3-氟-2-氨基异烟腈的方法 |
| WO2024052503A1 (en) | 2022-09-08 | 2024-03-14 | Institut National de la Santé et de la Recherche Médicale | Antibodies having specificity to ltbp2 and uses thereof |
| WO2024061930A1 (en) | 2022-09-22 | 2024-03-28 | Institut National de la Santé et de la Recherche Médicale | New method to treat and diagnose peripheral t-cell lymphoma (ptcl) |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8302591D0 (en) * | 1983-01-31 | 1983-03-02 | Fujisawa Pharmaceutical Co | Thiazole derivatives |
| FR2581063B1 (fr) * | 1985-04-30 | 1987-07-17 | Chauvin Blache Lab | Amino-2 thiazoles n-substitues, leur procede de preparation et leur application en therapeutique |
| US4788195A (en) | 1986-01-13 | 1988-11-29 | American Cyanamid Company | 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines |
| US4876252A (en) | 1986-01-13 | 1989-10-24 | American Cyanamid Company | 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines |
| JPH0753666B2 (ja) * | 1987-09-14 | 1995-06-07 | 久光製薬株式会社 | 置換ジフェニルチアゾール誘導体からなる抗炎症剤 |
| DE3905763A1 (de) * | 1989-02-24 | 1990-09-06 | Bayer Ag | Sulfonylierte azinyliminoheteroazole, verfahren und zwischenprodukte zu ihrer herstellung und ihre verwendung als herbizide |
| DE4124942A1 (de) | 1991-07-27 | 1993-01-28 | Thomae Gmbh Dr K | 5-gliedrige heterocyclen, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| TW225528B (no) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| WO1994001423A1 (en) | 1992-07-07 | 1994-01-20 | Nippon Soda Co., Ltd. | Thiazole derivative |
| US5516775A (en) | 1992-08-31 | 1996-05-14 | Ciba-Geigy Corporation | Further use of pyrimidine derivatives |
| GB9314884D0 (en) * | 1993-07-19 | 1993-09-01 | Zeneca Ltd | Tricyclic derivatives |
| US5543520A (en) | 1993-10-01 | 1996-08-06 | Ciba-Geigy Corporation | Pyrimidine derivatives |
| AU693475B2 (en) | 1993-10-01 | 1998-07-02 | Novartis Ag | Pyrimidineamine derivatives and processes for the preparation thereof |
| JPH07149745A (ja) * | 1993-11-30 | 1995-06-13 | Hisamitsu Pharmaceut Co Inc | 新規な２−アミノチアゾール誘導体 |
| US5530000A (en) * | 1993-12-22 | 1996-06-25 | Ortho Pharmaceutical Corporation | Substituted pyrimidinylaminothiazole derivatives useful as platelet aggreggation inhibitors |
| WO1995035275A1 (en) | 1994-06-22 | 1995-12-28 | British Biotech Pharmaceuticals Limited | Metalloproteinase inhibitors |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| US5958934A (en) | 1996-05-23 | 1999-09-28 | Syntex (U.S.A.) Inc. | Aryl pyrimidine derivatives and uses thereof |
| US5952331A (en) | 1996-05-23 | 1999-09-14 | Syntex (Usa) Inc. | Aryl pyrimidine derivatives |
| TW440563B (en) | 1996-05-23 | 2001-06-16 | Hoffmann La Roche | Aryl pyrimidine derivatives and a pharmaceutical composition thereof |
| DE19824175A1 (de) | 1998-05-29 | 1999-12-02 | Novartis Ag | Amino-azol-Verbindungen |
| WO1999064418A1 (en) | 1998-06-05 | 1999-12-16 | Novartis Ag | Aryl pyridinyl thiazoles |
| AU768751B2 (en) * | 1998-06-18 | 2004-01-08 | Bristol-Myers Squibb Company | Carbon substituted aminothiazole inhibitors of cyclin dependent kinases |
| ES2342240T3 (es) | 1998-08-11 | 2010-07-02 | Novartis Ag | Derivados de isoquinolina con actividad que inhibe la angiogenia. |
| US6184226B1 (en) | 1998-08-28 | 2001-02-06 | Scios Inc. | Quinazoline derivatives as inhibitors of P-38 α |
| AUPP873799A0 (en) * | 1999-02-17 | 1999-03-11 | Fujisawa Pharmaceutical Co., Ltd. | Pyridine compounds |
| EP2308833A3 (en) | 1999-04-15 | 2011-09-28 | Bristol-Myers Squibb Company | Cyclic protein tyrosine kinase inhibitors |
-
2000
- 2000-09-06 EE EEP200200123A patent/EE200200123A/xx unknown
- 2000-09-06 CZ CZ2002861A patent/CZ2002861A3/cs unknown
- 2000-09-06 WO PCT/US2000/024432 patent/WO2001017995A1/en active IP Right Grant
- 2000-09-06 MX MXPA02002559A patent/MXPA02002559A/es unknown
- 2000-09-06 SK SK477-2002A patent/SK4772002A3/sk unknown
- 2000-09-06 BR BR0013899-1A patent/BR0013899A/pt not_active Application Discontinuation
- 2000-09-06 AT AT00961583T patent/ATE309241T1/de not_active IP Right Cessation
- 2000-09-06 CA CA002384101A patent/CA2384101A1/en not_active Abandoned
- 2000-09-06 JP JP2001522218A patent/JP3892296B2/ja not_active Expired - Fee Related
- 2000-09-06 AU AU73517/00A patent/AU779908B2/en not_active Ceased
- 2000-09-06 ES ES00961583T patent/ES2250186T3/es not_active Expired - Lifetime
- 2000-09-06 HU HU0202682A patent/HUP0202682A3/hu unknown
- 2000-09-06 CN CN00815561A patent/CN1390215A/zh active Pending
- 2000-09-06 EA EA200200351A patent/EA200200351A1/ru unknown
- 2000-09-06 EP EP00961583A patent/EP1218376B1/en not_active Expired - Lifetime
- 2000-09-06 IL IL14838500A patent/IL148385A0/xx unknown
- 2000-09-06 KR KR1020027003134A patent/KR20020027635A/ko not_active Application Discontinuation
- 2000-09-06 PL PL00355639A patent/PL355639A1/xx not_active Application Discontinuation
- 2000-09-06 DE DE60023926T patent/DE60023926T2/de not_active Expired - Lifetime
-
2002
- 2002-02-01 US US10/061,817 patent/US6586423B2/en not_active Expired - Fee Related
- 2002-02-01 US US10/062,351 patent/US6586424B2/en not_active Expired - Fee Related
- 2002-02-28 BG BG106465A patent/BG106465A/xx unknown
- 2002-03-07 ZA ZA200201898A patent/ZA200201898B/en unknown
- 2002-03-08 NO NO20021166A patent/NO20021166L/no not_active Application Discontinuation
-
2006
- 2006-09-27 JP JP2006262211A patent/JP2007045835A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| EA200200351A1 (ru) | 2002-10-31 |
| HUP0202682A3 (en) | 2003-03-28 |
| EP1218376B1 (en) | 2005-11-09 |
| DE60023926T2 (de) | 2006-07-20 |
| US6586423B2 (en) | 2003-07-01 |
| PL355639A1 (en) | 2004-05-04 |
| ATE309241T1 (de) | 2005-11-15 |
| US20030064996A1 (en) | 2003-04-03 |
| KR20020027635A (ko) | 2002-04-13 |
| ES2250186T3 (es) | 2006-04-16 |
| EP1218376A1 (en) | 2002-07-03 |
| US20020147203A1 (en) | 2002-10-10 |
| EE200200123A (et) | 2003-08-15 |
| BR0013899A (pt) | 2003-07-08 |
| JP2003509342A (ja) | 2003-03-11 |
| AU7351700A (en) | 2001-04-10 |
| EP1218376A4 (en) | 2002-11-20 |
| JP2007045835A (ja) | 2007-02-22 |
| IL148385A0 (en) | 2002-09-12 |
| NO20021166L (no) | 2002-04-25 |
| CN1390215A (zh) | 2003-01-08 |
| US6586424B2 (en) | 2003-07-01 |
| CZ2002861A3 (cs) | 2002-06-12 |
| DE60023926D1 (de) | 2005-12-15 |
| WO2001017995A1 (en) | 2001-03-15 |
| MXPA02002559A (es) | 2002-07-30 |
| HUP0202682A2 (hu) | 2003-02-28 |
| NO20021166D0 (no) | 2002-03-08 |
| AU779908B2 (en) | 2005-02-17 |
| JP3892296B2 (ja) | 2007-03-14 |
| SK4772002A3 (en) | 2002-11-06 |
| CA2384101A1 (en) | 2001-03-15 |
| BG106465A (en) | 2002-12-29 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ZA200201898B (en) | Tyrosine kinase inhibitors. | |
| JP5261383B2 (ja) | ヒトプロテインチロシンホスファターゼ阻害剤および使用法 | |
| JP2009542659A5 (no) | ||
| KR101157844B1 (ko) | 인간 단백질 티로신 포스파타제 억제제 및 사용 방법 | |
| CN101415422B (zh) | 抗癌药用组合物 | |
| RU2009121564A (ru) | Азаадамантановые производные и способы применения | |
| US7309787B2 (en) | Kinase inhibitors | |
| CN106604920B (zh) | 具有四氢吡喃基甲基的吡啶酮衍生物 | |
| TW200534853A (en) | Synergistic methods and compositions for treating cancer | |
| ZA200604148B (en) | Benzimidazolyl derivatives | |
| CN1409708A (zh) | 酪氨酸激酶抑制剂 | |
| CA2915566C (en) | 2,3-dihydrobenzofuran-5-yl compounds as dyrk kinase inhibitors | |
| JP2006507302A5 (no) | ||
| CA2614746A1 (en) | Heteroaryl benzamide derivatives for use as glk activators in the treatment of diabetes | |
| JP2009535386A (ja) | チアゾール誘導体および抗腫瘍剤としてのその使用 | |
| JP4324791B2 (ja) | ２−アシルアミノチアゾール誘導体又はその塩 | |
| US20130165458A1 (en) | Quinazoline compounds as kinase inhibitors | |
| JP4774995B2 (ja) | アシルアミノチアゾール誘導体を有効成分とする医薬組成物 | |
| US9321762B2 (en) | Quinazoline compounds, method for preparing the same and use thereof | |
| CN101160308B (zh) | 具有改进药物特性的喹啉酮类化合物的药学上可接受的盐 | |
| AU2015290176B2 (en) | Quinoxaline compounds, method for preparing the same and use thereof | |
| Wang et al. | Recent advances of anti-angiogenic inhibitors targeting VEGF/VEGFR axis | |
| ES2292329A1 (es) | Inhibidores de quinasa para el tratamiento de enfermedades. | |
| TW201722937A (zh) | 苯基咪唑化合物 | |
| JP2011225582A (ja) | 疾患の治療のためのキナーゼ阻害剤 |