DE1041982T1 - HEMMUNG DER p38 KINASE AKTIVITÄT DURCH SUBSTITUIERTEN HETEROCYCLISCHEN HARNSTOFFEN - Google Patents
HEMMUNG DER p38 KINASE AKTIVITÄT DURCH SUBSTITUIERTEN HETEROCYCLISCHEN HARNSTOFFENInfo
- Publication number
- DE1041982T1 DE1041982T1 DE1041982T DE98964709T DE1041982T1 DE 1041982 T1 DE1041982 T1 DE 1041982T1 DE 1041982 T DE1041982 T DE 1041982T DE 98964709 T DE98964709 T DE 98964709T DE 1041982 T1 DE1041982 T1 DE 1041982T1
- Authority
- DE
- Germany
- Prior art keywords
- butyl
- urea
- tert
- substituted
- pyridinyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 230000000694 effects Effects 0.000 title claims 2
- 230000005764 inhibitory process Effects 0.000 title 1
- 150000003672 ureas Chemical class 0.000 title 1
- -1 aryl ureas Chemical class 0.000 claims abstract 19
- 201000010099 disease Diseases 0.000 claims abstract 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 9
- 230000001404 mediated effect Effects 0.000 claims abstract 4
- 102000004127 Cytokines Human genes 0.000 claims abstract 3
- 108090000695 Cytokines Proteins 0.000 claims abstract 3
- 206010028980 Neoplasm Diseases 0.000 claims abstract 3
- 108091005804 Peptidases Proteins 0.000 claims abstract 3
- 201000011510 cancer Diseases 0.000 claims abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 2
- 238000000034 method Methods 0.000 claims 39
- 150000001875 compounds Chemical class 0.000 claims 21
- 229910052736 halogen Inorganic materials 0.000 claims 19
- 150000002367 halogens Chemical group 0.000 claims 19
- 239000004202 carbamide Substances 0.000 claims 18
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 17
- 125000003118 aryl group Chemical group 0.000 claims 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 14
- 238000006467 substitution reaction Methods 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 11
- 125000004076 pyridyl group Chemical group 0.000 claims 11
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 11
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 8
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 125000002877 alkyl aryl group Chemical group 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 4
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 239000011593 sulfur Substances 0.000 claims 3
- PEZPHMOCGURMEM-UHFFFAOYSA-N (2,3-dichlorophenyl)urea Chemical compound NC(=O)NC1=CC=CC(Cl)=C1Cl PEZPHMOCGURMEM-UHFFFAOYSA-N 0.000 claims 2
- QYYQTVPREWFJTR-UHFFFAOYSA-N (4-pyridin-4-yloxyphenyl)urea Chemical compound C1=CC(NC(=O)N)=CC=C1OC1=CC=NC=C1 QYYQTVPREWFJTR-UHFFFAOYSA-N 0.000 claims 2
- YAXXWOLZFGHUMQ-UHFFFAOYSA-N 1-(5-tert-butyl-2-methylpyrazol-3-yl)-1-(3-pyridin-4-ylsulfanylphenyl)urea Chemical compound CN1N=C(C(C)(C)C)C=C1N(C(N)=O)C1=CC=CC(SC=2C=CN=CC=2)=C1 YAXXWOLZFGHUMQ-UHFFFAOYSA-N 0.000 claims 2
- HGGBXDNWWLQKFO-UHFFFAOYSA-N 1-(5-tert-butyl-2-methylpyrazol-3-yl)-3-[4-pyridin-4-ylsulfanyl-3-(trifluoromethyl)phenyl]urea Chemical compound CN1N=C(C(C)(C)C)C=C1NC(=O)NC(C=C1C(F)(F)F)=CC=C1SC1=CC=NC=C1 HGGBXDNWWLQKFO-UHFFFAOYSA-N 0.000 claims 2
- SCTUFFRENWOJON-UHFFFAOYSA-N C(C)(C)(C)C1=CC(=CS1)N(C(=O)N)C1=CC=C(C=C1)SC1=CC=NC=C1 Chemical compound C(C)(C)(C)C1=CC(=CS1)N(C(=O)N)C1=CC=C(C=C1)SC1=CC=NC=C1 SCTUFFRENWOJON-UHFFFAOYSA-N 0.000 claims 2
- 239000004365 Protease Substances 0.000 claims 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 2
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims 2
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- JVKPSHHYGNWFFP-UHFFFAOYSA-N (3-pyridin-4-ylsulfanylphenyl)urea Chemical compound NC(=O)NC1=CC=CC(SC=2C=CN=CC=2)=C1 JVKPSHHYGNWFFP-UHFFFAOYSA-N 0.000 claims 1
- ORLPLMYCUFHCTN-UHFFFAOYSA-N 1-(2-bromo-5-tert-butylthiophen-3-yl)-3-(4-methylphenyl)urea Chemical compound C1=CC(C)=CC=C1NC(=O)NC1=C(Br)SC(C(C)(C)C)=C1 ORLPLMYCUFHCTN-UHFFFAOYSA-N 0.000 claims 1
- ORIFMUAUSBIDGC-UHFFFAOYSA-N 1-(3-tert-butyl-1,2-oxazol-5-yl)-3-(4-pyridin-4-yloxyphenyl)urea Chemical compound O1N=C(C(C)(C)C)C=C1NC(=O)NC(C=C1)=CC=C1OC1=CC=NC=C1 ORIFMUAUSBIDGC-UHFFFAOYSA-N 0.000 claims 1
- YSOLQZIGFKVUPX-UHFFFAOYSA-N 1-(3-tert-butyl-1,2-oxazol-5-yl)-3-(4-pyridin-4-ylsulfanylphenyl)urea Chemical compound O1N=C(C(C)(C)C)C=C1NC(=O)NC(C=C1)=CC=C1SC1=CC=NC=C1 YSOLQZIGFKVUPX-UHFFFAOYSA-N 0.000 claims 1
- NJHHSVCMQSVKLK-UHFFFAOYSA-N 1-(3-tert-butyl-1,2-oxazol-5-yl)-3-[4-(4-methoxyanilino)phenyl]urea Chemical compound C1=CC(OC)=CC=C1NC(C=C1)=CC=C1NC(=O)NC1=CC(C(C)(C)C)=NO1 NJHHSVCMQSVKLK-UHFFFAOYSA-N 0.000 claims 1
- OWVOVWYDNHUGBF-UHFFFAOYSA-N 1-(5-tert-butyl-1,2-oxazol-3-yl)-1-(4-pyridin-4-yloxyphenyl)urea Chemical compound C(C)(C)(C)C1=CC(=NO1)N(C(N)=O)C1=CC=C(C=C1)OC1=CC=NC=C1 OWVOVWYDNHUGBF-UHFFFAOYSA-N 0.000 claims 1
- GYJWQQJEAAHIIW-UHFFFAOYSA-N 1-(5-tert-butyl-1,2-oxazol-3-yl)-1-(4-pyridin-4-ylsulfanylphenyl)urea Chemical compound O1C(C(C)(C)C)=CC(N(C(N)=O)C=2C=CC(SC=3C=CN=CC=3)=CC=2)=N1 GYJWQQJEAAHIIW-UHFFFAOYSA-N 0.000 claims 1
- BUEAHSOXZBKYRU-UHFFFAOYSA-N 1-(5-tert-butyl-1,2-oxazol-3-yl)-1-[4-(pyridin-4-ylmethyl)phenyl]urea Chemical compound C(C)(C)(C)C1=CC(=NO1)N(C(N)=O)C1=CC=C(C=C1)CC1=CC=NC=C1 BUEAHSOXZBKYRU-UHFFFAOYSA-N 0.000 claims 1
- BWYIEKUXLAWWDO-UHFFFAOYSA-N 1-(5-tert-butyl-1,2-oxazol-3-yl)-3-(3-pyridin-4-ylsulfanylphenyl)urea Chemical compound O1C(C(C)(C)C)=CC(NC(=O)NC=2C=C(SC=3C=CN=CC=3)C=CC=2)=N1 BWYIEKUXLAWWDO-UHFFFAOYSA-N 0.000 claims 1
- OCVLLNOZMGLZMR-UHFFFAOYSA-N 1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[3-(3-methylpyridin-4-yl)oxyphenyl]urea Chemical compound CC1=CN=CC=C1OC1=CC=CC(NC(=O)NC2=NOC(=C2)C(C)(C)C)=C1 OCVLLNOZMGLZMR-UHFFFAOYSA-N 0.000 claims 1
- IWCPQASLCDOVME-UHFFFAOYSA-N 1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[3-[fluoro(pyridin-4-yl)methyl]phenyl]urea Chemical compound O1C(C(C)(C)C)=CC(NC(=O)NC=2C=C(C=CC=2)C(F)C=2C=CN=CC=2)=N1 IWCPQASLCDOVME-UHFFFAOYSA-N 0.000 claims 1
- DMQFIGFOGVTSFP-UHFFFAOYSA-N 1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[4-(4-hydroxyphenoxy)phenyl]urea Chemical compound O1C(C(C)(C)C)=CC(NC(=O)NC=2C=CC(OC=3C=CC(O)=CC=3)=CC=2)=N1 DMQFIGFOGVTSFP-UHFFFAOYSA-N 0.000 claims 1
- UPTPHBBPQWSUFJ-UHFFFAOYSA-N 1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[4-pyridin-4-ylsulfanyl-3-(trifluoromethyl)phenyl]urea Chemical compound O1C(C(C)(C)C)=CC(NC(=O)NC=2C=C(C(SC=3C=CN=CC=3)=CC=2)C(F)(F)F)=N1 UPTPHBBPQWSUFJ-UHFFFAOYSA-N 0.000 claims 1
- HFDKZSDVVYXDMY-UHFFFAOYSA-N 1-(5-tert-butyl-1H-pyrazol-3-yl)-1-(4-pyridin-4-yloxyphenyl)urea Chemical compound N1C(C(C)(C)C)=CC(N(C(N)=O)C=2C=CC(OC=3C=CN=CC=3)=CC=2)=N1 HFDKZSDVVYXDMY-UHFFFAOYSA-N 0.000 claims 1
- YOUFVBDDKCYRBT-UHFFFAOYSA-N 1-(5-tert-butyl-1H-pyrazol-3-yl)-1-[4-(pyridin-4-ylmethyl)phenyl]urea Chemical compound N1C(C(C)(C)C)=CC(N(C(N)=O)C=2C=CC(CC=3C=CN=CC=3)=CC=2)=N1 YOUFVBDDKCYRBT-UHFFFAOYSA-N 0.000 claims 1
- PXMZWZHOSUYALM-UHFFFAOYSA-N 1-(5-tert-butyl-1h-pyrazol-3-yl)-3-(3-pyridin-4-yloxyphenyl)urea Chemical compound N1N=C(C(C)(C)C)C=C1NC(=O)NC1=CC=CC(OC=2C=CN=CC=2)=C1 PXMZWZHOSUYALM-UHFFFAOYSA-N 0.000 claims 1
- NISMKTLRQBAMPS-UHFFFAOYSA-N 1-(5-tert-butyl-1h-pyrazol-3-yl)-3-(4-pyridin-4-ylsulfanylphenyl)urea Chemical compound N1C(C(C)(C)C)=CC(NC(=O)NC=2C=CC(SC=3C=CN=CC=3)=CC=2)=N1 NISMKTLRQBAMPS-UHFFFAOYSA-N 0.000 claims 1
- VWBAHTCOVBWTMX-UHFFFAOYSA-N 1-(5-tert-butyl-1h-pyrazol-3-yl)-3-[4-(pyridin-4-ylmethyl)phenyl]urea Chemical compound N1N=C(C(C)(C)C)C=C1NC(=O)NC(C=C1)=CC=C1CC1=CC=NC=C1 VWBAHTCOVBWTMX-UHFFFAOYSA-N 0.000 claims 1
- LVXHHBZKFYKYEL-UHFFFAOYSA-N 1-(5-tert-butyl-2-methylpyrazol-3-yl)-3-(2,3-dichlorophenyl)urea Chemical compound CN1N=C(C(C)(C)C)C=C1NC(=O)NC1=CC=CC(Cl)=C1Cl LVXHHBZKFYKYEL-UHFFFAOYSA-N 0.000 claims 1
- FNCGBIQSBMRFGO-UHFFFAOYSA-N 1-(5-tert-butylthiophen-3-yl)-1-(2,3-dichlorophenyl)urea Chemical compound S1C(C(C)(C)C)=CC(N(C(N)=O)C=2C(=C(Cl)C=CC=2)Cl)=C1 FNCGBIQSBMRFGO-UHFFFAOYSA-N 0.000 claims 1
- DFVUEUQJPMPJMY-UHFFFAOYSA-N 1-(5-tert-butylthiophen-3-yl)-1-(4-pyridin-4-yloxyphenyl)urea Chemical compound S1C(C(C)(C)C)=CC(N(C(N)=O)C=2C=CC(OC=3C=CN=CC=3)=CC=2)=C1 DFVUEUQJPMPJMY-UHFFFAOYSA-N 0.000 claims 1
- QGNZBPXTRYLNDP-UHFFFAOYSA-N 1-(5-tert-butylthiophen-3-yl)-1-[4-(4-ethoxyphenoxy)phenyl]urea Chemical compound C1=CC(OCC)=CC=C1OC1=CC=C(N(C(N)=O)C=2C=C(SC=2)C(C)(C)C)C=C1 QGNZBPXTRYLNDP-UHFFFAOYSA-N 0.000 claims 1
- IYQMYSWZQMEBTC-UHFFFAOYSA-N 1-(5-tert-butylthiophen-3-yl)-1-[4-(4-hydroxyphenoxy)phenyl]urea Chemical compound S1C(C(C)(C)C)=CC(N(C(N)=O)C=2C=CC(OC=3C=CC(O)=CC=3)=CC=2)=C1 IYQMYSWZQMEBTC-UHFFFAOYSA-N 0.000 claims 1
- ZQLOKBHUXHHXNG-UHFFFAOYSA-N 1-(5-tert-butylthiophen-3-yl)-1-[4-(pyridin-4-ylmethyl)phenyl]urea Chemical compound S1C(C(C)(C)C)=CC(N(C(N)=O)C=2C=CC(CC=3C=CN=CC=3)=CC=2)=C1 ZQLOKBHUXHHXNG-UHFFFAOYSA-N 0.000 claims 1
- WKYHBIQUWHYHAF-UHFFFAOYSA-N 1-(5-tert-butylthiophen-3-yl)-3-[4-(4-ethoxyphenoxy)phenyl]urea Chemical compound C1=CC(OCC)=CC=C1OC(C=C1)=CC=C1NC(=O)NC1=CSC(C(C)(C)C)=C1 WKYHBIQUWHYHAF-UHFFFAOYSA-N 0.000 claims 1
- OPTYENRVSZMHPJ-UHFFFAOYSA-N 1-(5-tert-butylthiophen-3-yl)-3-[4-(4-propan-2-yloxyphenoxy)phenyl]urea Chemical compound C1=CC(OC(C)C)=CC=C1OC(C=C1)=CC=C1NC(=O)NC1=CSC(C(C)(C)C)=C1 OPTYENRVSZMHPJ-UHFFFAOYSA-N 0.000 claims 1
- RMNIXRMFHYBQQB-UHFFFAOYSA-N 1-[3-(2-methylbutan-2-yl)-1,2-oxazol-5-yl]-3-(3-pyridin-4-ylsulfanylphenyl)urea Chemical compound O1N=C(C(C)(C)CC)C=C1NC(=O)NC1=CC=CC(SC=2C=CN=CC=2)=C1 RMNIXRMFHYBQQB-UHFFFAOYSA-N 0.000 claims 1
- PRUKAVRSMUKMPZ-UHFFFAOYSA-N 1-[3-(3-methylpentan-3-yl)-1,2-oxazol-5-yl]-1-(4-pyridin-4-yloxyphenyl)urea Chemical compound O1N=C(C(C)(CC)CC)C=C1N(C(N)=O)C(C=C1)=CC=C1OC1=CC=NC=C1 PRUKAVRSMUKMPZ-UHFFFAOYSA-N 0.000 claims 1
- AVGDYMIXTWFURX-UHFFFAOYSA-N 1-[3-(3-methylpentan-3-yl)-1,2-oxazol-5-yl]-3-[4-(pyridin-4-ylmethyl)phenyl]urea Chemical compound O1N=C(C(C)(CC)CC)C=C1NC(=O)NC(C=C1)=CC=C1CC1=CC=NC=C1 AVGDYMIXTWFURX-UHFFFAOYSA-N 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- HKQBXLJMQGQRDF-UHFFFAOYSA-N C(C)(C)(C)C1=CC(=CS1)N(C(=O)N)C1=CC=C(C=C1)OC1=CC=C(C=C1)OC Chemical compound C(C)(C)(C)C1=CC(=CS1)N(C(=O)N)C1=CC=C(C=C1)OC1=CC=C(C=C1)OC HKQBXLJMQGQRDF-UHFFFAOYSA-N 0.000 claims 1
- VARNKUIXNDPMRS-UHFFFAOYSA-N C(C)(C)(C)C1=CC(=NO1)N(C(=O)N)C1=CC(=CC=C1)SC1=C(C=NC=C1)C Chemical compound C(C)(C)(C)C1=CC(=NO1)N(C(=O)N)C1=CC(=CC=C1)SC1=C(C=NC=C1)C VARNKUIXNDPMRS-UHFFFAOYSA-N 0.000 claims 1
- NCWIXQOCLSDUPO-UHFFFAOYSA-N C(C)(C)(C)C1=NOC(=C1)N(C(=O)N)C1=CC=C(C=C1)CC1=CC=NC=C1 Chemical compound C(C)(C)(C)C1=NOC(=C1)N(C(=O)N)C1=CC=C(C=C1)CC1=CC=NC=C1 NCWIXQOCLSDUPO-UHFFFAOYSA-N 0.000 claims 1
- VVSDYIZJNRURTB-UHFFFAOYSA-N CN1N=C(C=C1N(C(=O)N)C1=CC=C(C=C1)SC1=CC=NC=C1)C(C)(C)C Chemical compound CN1N=C(C=C1N(C(=O)N)C1=CC=C(C=C1)SC1=CC=NC=C1)C(C)(C)C VVSDYIZJNRURTB-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 108090001005 Interleukin-6 Proteins 0.000 claims 1
- 108090001007 Interleukin-8 Proteins 0.000 claims 1
- 101001013152 Mycobacterium avium Major membrane protein 1 Proteins 0.000 claims 1
- 101001013151 Mycobacterium leprae (strain TN) Major membrane protein I Proteins 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- CKKFAPLZDWYTHG-UHFFFAOYSA-N [3-(4-methylphenoxy)phenyl]urea Chemical compound C1=CC(C)=CC=C1OC1=CC=CC(NC(N)=O)=C1 CKKFAPLZDWYTHG-UHFFFAOYSA-N 0.000 claims 1
- AIOQDSPVQFKKQO-UHFFFAOYSA-N [4-(4-hydroxyphenoxy)phenyl]urea Chemical compound C1=CC(NC(=O)N)=CC=C1OC1=CC=C(O)C=C1 AIOQDSPVQFKKQO-UHFFFAOYSA-N 0.000 claims 1
- WANKHXKMUWCUTK-UHFFFAOYSA-N [4-(4-methoxyphenoxy)phenyl]urea Chemical compound C1=CC(OC)=CC=C1OC1=CC=C(NC(N)=O)C=C1 WANKHXKMUWCUTK-UHFFFAOYSA-N 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 244000309464 bull Species 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000002519 immonomodulatory effect Effects 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 238000000021 kinase assay Methods 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 125000003944 tolyl group Chemical group 0.000 claims 1
- 102000035195 Peptidases Human genes 0.000 abstract 1
- 230000003157 cancerolytic effect Effects 0.000 abstract 1
- 235000013877 carbamide Nutrition 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
-
- 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
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- 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
- A61P37/02—Immunomodulators
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/38—Nitrogen atoms
- C07D231/42—Benzene-sulfonamido pyrazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D261/14—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/44—Acylated amino or imino radicals
- C07D277/48—Acylated amino or imino radicals by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof, e.g. carbonylguanidines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/30—Hetero atoms other than halogen
- C07D333/36—Nitrogen atoms
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Tropical Medicine & Parasitology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Communicable Diseases (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Urology & Nephrology (AREA)
- Transplantation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US99575097A | 1997-12-22 | 1997-12-22 | |
| PCT/US1998/026080 WO1999032111A1 (en) | 1997-12-22 | 1998-12-22 | INHIBITION OF p38 KINASE ACTIVITY USING SUBSTITUTED HETEROCYCLIC UREAS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DE1041982T1 true DE1041982T1 (de) | 2001-06-07 |
Family
ID=25542167
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE1041982T Pending DE1041982T1 (de) | 1997-12-22 | 1998-12-22 | HEMMUNG DER p38 KINASE AKTIVITÄT DURCH SUBSTITUIERTEN HETEROCYCLISCHEN HARNSTOFFEN |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP1041982B1 (enExample) |
| JP (1) | JP4403482B2 (enExample) |
| AT (1) | ATE529109T1 (enExample) |
| AU (1) | AU739642B2 (enExample) |
| CA (1) | CA2315720A1 (enExample) |
| DE (1) | DE1041982T1 (enExample) |
| ES (1) | ES2154253T3 (enExample) |
| IL (3) | IL136738A0 (enExample) |
| MX (1) | MXPA00006233A (enExample) |
| WO (1) | WO1999032111A1 (enExample) |
Families Citing this family (147)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1019040T1 (de) * | 1997-05-23 | 2001-02-08 | Bayer Corp., West Haven | Hemmung von p38 kinase aktivität durch arylharnstoff |
| EP1473292A1 (en) * | 1997-11-03 | 2004-11-03 | Boehringer Ingelheim Pharmaceuticals, Inc. | Aromatic heterocyclic compounds as anti-inflammatory agents |
| AU2006201959B2 (en) * | 1997-12-22 | 2008-09-04 | Bayer Healthcare Llc | Inhibition of Raf Kinase using Substituted Heterocyclic Ureas |
| PL205321B1 (pl) * | 1997-12-22 | 2010-04-30 | Bayer Corp | Zastosowanie podstawionych heterocyklicznych moczników do wytwarzania leku do hamowania kinazy raf, podstawione heterocykliczne moczniki oraz kompozycja farmaceutyczna je zawierająca |
| US7329670B1 (en) | 1997-12-22 | 2008-02-12 | Bayer Pharmaceuticals Corporation | Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas |
| US7517880B2 (en) | 1997-12-22 | 2009-04-14 | Bayer Pharmaceuticals Corporation | Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas |
| SI1690853T1 (sl) * | 1999-01-13 | 2010-07-30 | Bayer Healthcare Llc | Uporaba omega-karboksiarilno substituiranih difenilsečnin kot inhibitorjev raf-kinaze |
| ATE556713T1 (de) * | 1999-01-13 | 2012-05-15 | Bayer Healthcare Llc | Omega-carboxyarylsubstituierte-diphenyl- harnstoffe als p38-kinasehemmer |
| EP1140840B1 (en) | 1999-01-13 | 2006-03-22 | Bayer Pharmaceuticals Corp. | -g(v)-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| US20020065296A1 (en) * | 1999-01-13 | 2002-05-30 | Bayer Corporation | Heteroaryl ureas containing nitrogen hetero-atoms as p38 kinase inhibitors |
| US7351834B1 (en) | 1999-01-13 | 2008-04-01 | Bayer Pharmaceuticals Corporation | ω-Carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| US8124630B2 (en) | 1999-01-13 | 2012-02-28 | Bayer Healthcare Llc | ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| UA73492C2 (en) * | 1999-01-19 | 2005-08-15 | Aromatic heterocyclic compounds as antiinflammatory agents | |
| CA2360934A1 (en) | 1999-02-22 | 2000-08-31 | Lin-Hua Zhang | Polycyclo heterocyclic derivatives as antiinflammatory agents |
| EP1163236B1 (en) | 1999-03-12 | 2005-11-09 | Boehringer Ingelheim Pharmaceuticals Inc. | Aromatic heterocyclic compounds as anti-inflammatory agents |
| EE04799B1 (et) | 1999-03-12 | 2007-04-16 | Boehringer Ingelheim Pharmaceuticals, Inc. | Ühendid, mis on kasulikud põletikuvastaste vahenditena, nende ühendite valmistamise meetodid ja neid sisaldavad farmatseutilised kompositsioonid |
| DE60024830T2 (de) | 1999-07-09 | 2006-06-14 | Boehringer Ingelheim Pharma | Verfahren zur herstellung heteroarylsubstituierter ureaverbindungen |
| US6387900B1 (en) | 1999-08-12 | 2002-05-14 | Pharmacia & Upjohn S.P.A. | 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents |
| HUP0203542A3 (en) | 1999-08-12 | 2003-07-28 | Upjohn Co | 3(5)-amino-pyrazole derivatives, process for their preparation, their use and pharmaceutical compositions containing the same |
| EP1232150B1 (en) | 1999-11-16 | 2007-10-10 | Boehringer Ingelheim Pharmaceuticals Inc. | Urea derivatives as anti-inflammatory agents |
| SE9904177D0 (sv) * | 1999-11-18 | 1999-11-18 | Astra Ab | Novel compounds |
| US6525046B1 (en) | 2000-01-18 | 2003-02-25 | Boehringer Ingelheim Pharmaceuticals, Inc. | Aromatic heterocyclic compounds as antiinflammatory agents |
| US6608052B2 (en) | 2000-02-16 | 2003-08-19 | Boehringer Ingelheim Pharmaceuticals, Inc. | Compounds useful as anti-inflammatory agents |
| GB0010757D0 (en) | 2000-05-05 | 2000-06-28 | Astrazeneca Ab | Chemical compounds |
| GB0016787D0 (en) | 2000-07-07 | 2000-08-30 | Pfizer Ltd | Compounds useful in therapy |
| FR2812633A1 (fr) * | 2000-08-04 | 2002-02-08 | Aventis Cropscience Sa | Derives de phenyl(thio)urees et phenyl(thio)carbamates fongicides |
| US6645990B2 (en) | 2000-08-15 | 2003-11-11 | Amgen Inc. | Thiazolyl urea compounds and methods of uses |
| FR2815030A1 (fr) * | 2000-10-05 | 2002-04-12 | Lipha | Derives nitroso de la diphenylamine, compositions pharmaceutiques les contenant et leur utilisation pour la preparation de medicaments |
| HU230302B1 (hu) | 2000-10-20 | 2015-12-28 | Eisai R&D Management Co., Ltd. | Nitrogéntartalmú aromás származékok és ezeket tartalmazó gyógyászati készítmények |
| JP2004517080A (ja) | 2000-11-29 | 2004-06-10 | グラクソ グループ リミテッド | Tie−2および/またはvegfr−2の阻害剤として有用なベンゾイミダゾール誘導体 |
| CA2432809C (en) * | 2000-12-21 | 2010-11-30 | Schering Corporation | Heteroaryl urea neuropeptide y y5 receptor antagonists |
| US6946476B2 (en) | 2000-12-21 | 2005-09-20 | Schering Corporation | Heteroaryl urea neuropeptide Y Y5 receptor antagonists |
| US7235576B1 (en) | 2001-01-12 | 2007-06-26 | Bayer Pharmaceuticals Corporation | Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| US7371763B2 (en) | 2001-04-20 | 2008-05-13 | Bayer Pharmaceuticals Corporation | Inhibition of raf kinase using quinolyl, isoquinolyl or pyridyl ureas |
| TWI324154B (enExample) * | 2001-04-27 | 2010-05-01 | Kyowa Hakko Kirin Co Ltd | |
| MXPA03010487A (es) | 2001-05-16 | 2004-03-09 | Boehringer Ingelheim Pharma | Derivados de diarilurea utiles como agentes antiinflamatorios. |
| EP1395561A1 (en) | 2001-05-25 | 2004-03-10 | Boehringer Ingelheim Pharmaceuticals Inc. | Carbamate and oxamide compounds as inhibitors of cytokine production |
| ES2269709T3 (es) | 2001-06-05 | 2007-04-01 | Boehringer Ingelheim Pharmaceuticals Inc. | Compuestos de cicloalquil-urea, fusionada con grupos benzo y 1,4-disustituida. |
| EP1408950B1 (en) | 2001-07-11 | 2007-04-25 | Boehringer Ingelheim Pharmaceuticals Inc. | Methods of treating cytokine mediated diseases |
| JP4825375B2 (ja) * | 2001-08-28 | 2011-11-30 | 株式会社 資生堂 | ジチアゾール化合物及びマトリックスメタロプロテアーゼ活性阻害剤、皮膚外用剤 |
| GB0121941D0 (en) | 2001-09-11 | 2001-10-31 | Astrazeneca Ab | Chemical compounds |
| ATE495741T1 (de) | 2001-09-26 | 2011-02-15 | Pfizer Italia Srl | Aminoindazolderivate mit kinaseinhibierender wirkung, verfahren zu deren herstellung und diese enthaltende pharmazeutische zusammensetzungen |
| EP1438048A1 (en) | 2001-10-18 | 2004-07-21 | Boehringer Ingelheim Pharmaceuticals Inc. | 1,4-disubstituted benzo-fused urea compounds as cytokine inhibitors |
| AU2003209116A1 (en) | 2002-02-11 | 2003-09-04 | Bayer Pharmaceuticals Corporation | Aryl ureas with angiogenesis inhibiting activity |
| WO2003068223A1 (en) * | 2002-02-11 | 2003-08-21 | Bayer Corporation | Aryl ureas with raf kinase and angiogenesis inhibiting activity |
| US10653684B2 (en) | 2002-02-11 | 2020-05-19 | Bayer Healthcare Llc | Aryl ureas with angiogenisis inhibiting activity |
| EP1474393A1 (en) * | 2002-02-11 | 2004-11-10 | Bayer Pharmaceuticals Corporation | Aryl ureas as kinase inhibitors |
| ES2299689T3 (es) | 2002-02-25 | 2008-06-01 | Boehringer Ingelheim Pharmaceuticals Inc. | Compuestos de cicloalquil-uera fusionada con benzo 1,4-disustituido, utiles para el tratamiento de enfermedades por citoquinas. |
| WO2003097610A1 (en) * | 2002-05-17 | 2003-11-27 | Pharmacia Italia S.P.A. | Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| KR101124245B1 (ko) | 2002-06-27 | 2012-07-02 | 노보 노르디스크 에이/에스 | 치료제로서 아릴 카르보닐 유도체 |
| WO2004002481A1 (en) | 2002-06-27 | 2004-01-08 | Novo Nordisk A/S | Aryl carbonyl derivatives as therapeutic agents |
| JP2005538066A (ja) | 2002-07-09 | 2005-12-15 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | 新規な抗コリン作用薬及びp38キナーゼ阻害剤を用いた新規な医薬組成物 |
| MXPA05002493A (es) * | 2002-09-05 | 2005-05-27 | Neurosearch As | Derivados de diarilurea y su uso como bloqueadores del canal del cloro. |
| 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 |
| WO2004064730A2 (en) * | 2003-01-14 | 2004-08-05 | Cytokinetics, Inc. | Compounds, compositions and methods |
| MXPA05009102A (es) * | 2003-02-28 | 2006-05-31 | Bayer Pharmaceuticals Corp | Derivados de piridina sustituida utiles en el tratamiento del cancer y otros trastornos. |
| EP1608639A2 (en) | 2003-02-28 | 2005-12-28 | Bayer Pharmaceuticals Corporation | Novel bicyclic urea derivatives useful in the treatment of cancer and other disorders |
| JP2006521345A (ja) * | 2003-03-28 | 2006-09-21 | ファルマシア・アンド・アップジョン・カンパニー・エルエルシー | ニコチン性アセチルコリン受容体の正のアロステリック調節剤 |
| PT1636585E (pt) | 2003-05-20 | 2008-03-27 | Bayer Pharmaceuticals Corp | Diarilureias com actividade inibidora de cinase |
| NZ544920A (en) | 2003-07-23 | 2009-11-27 | Bayer Healthcare Llc | 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide and metabolites for the treatment and prevention of diseases and conditions |
| CN100450998C (zh) | 2003-11-11 | 2009-01-14 | 卫材R&D管理有限公司 | 脲衍生物的制备方法 |
| US20050171172A1 (en) | 2003-11-13 | 2005-08-04 | Ambit Biosciences Corporation | Amide derivatives as PDGFR modulators |
| GB0330042D0 (en) | 2003-12-24 | 2004-01-28 | Pharmacia Italia Spa | Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions them |
| GB0330043D0 (en) | 2003-12-24 | 2004-01-28 | Pharmacia Italia Spa | Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions comprising them |
| MXPA06007667A (es) | 2004-01-06 | 2006-09-01 | Novo Nordisk As | Heteroaril-ureas y su uso como activadores de glucocinasa. |
| KR20060132882A (ko) * | 2004-01-30 | 2006-12-22 | 메르크 파텐트 게엠베하 | 비스아릴우레아 유도체 |
| TW200530236A (en) | 2004-02-23 | 2005-09-16 | Chugai Pharmaceutical Co Ltd | Heteroaryl phenylurea |
| US20060211752A1 (en) | 2004-03-16 | 2006-09-21 | Kohn Leonard D | Use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune/inflammatory diseases associated with toll-like receptor overexpression |
| CA2564325A1 (en) | 2004-04-30 | 2005-11-24 | Bayer Pharmaceuticals Corporation | Substituted pyrazolyl urea derivatives useful in the treatment of cancer |
| US7507735B2 (en) | 2004-06-17 | 2009-03-24 | Cytokinetics, Inc. | Compounds, compositions and methods |
| EP1609789A1 (en) * | 2004-06-23 | 2005-12-28 | Eli Lilly And Company | Ureido-pyrazole derivatives and their use as kinase inhibitors |
| US20060035893A1 (en) | 2004-08-07 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders |
| EP1797881B1 (en) | 2004-09-17 | 2009-04-15 | Eisai R&D Management Co., Ltd. | Medicinal composition with improved stability and reduced gelation properties |
| US7741479B2 (en) | 2004-12-07 | 2010-06-22 | Locus Pharmaceuticals, Inc. | Urea inhibitors of MAP kinases |
| US7612200B2 (en) | 2004-12-07 | 2009-11-03 | Locus Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| PE20060777A1 (es) | 2004-12-24 | 2006-10-06 | Boehringer Ingelheim Int | Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas |
| NZ561178A (en) | 2005-03-07 | 2010-11-26 | Bayer Schering Pharma Ag | Pharmaceutical composition comprising an omega-carboxyaryl substituted diphenyl urea for the treatment of cancer |
| DE102005015253A1 (de) | 2005-04-04 | 2006-10-05 | Merck Patent Gmbh | Pyrazolderivate |
| EP2281901B1 (en) | 2005-08-02 | 2013-11-27 | Eisai R&D Management Co., Ltd. | Anti-tumour pharmaceutical composition with angiogenesis inhibitors |
| US7538223B2 (en) | 2005-08-04 | 2009-05-26 | Cytokinetics, Inc. | Compounds, compositions and methods |
| DE102005037499A1 (de) | 2005-08-09 | 2007-02-15 | Merck Patent Gmbh | Pyrazolderivate |
| EP1790342A1 (de) | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
| CA2628039A1 (en) | 2005-11-11 | 2007-05-18 | Aeterna Zentaris Gmbh | Novel pyridopyrazines and their use as modulators of kinases |
| US8217042B2 (en) | 2005-11-11 | 2012-07-10 | Zentaris Gmbh | Pyridopyrazines and their use as modulators of kinases |
| AR058347A1 (es) | 2005-12-15 | 2008-01-30 | Cytokinetics Inc | Entidades quimias composiciones y metodos |
| US7825120B2 (en) | 2005-12-15 | 2010-11-02 | Cytokinetics, Inc. | Certain substituted ((piperazin-1-ylmethyl)benzyl)ureas |
| EP1959962A2 (en) | 2005-12-16 | 2008-08-27 | Cytokinetics, Inc. | Certain chemical entities, compositions, and methods |
| EP1962852B1 (en) | 2005-12-19 | 2017-01-25 | Cytokinetics, Inc. | Compounds, compositions and methods |
| WO2007075650A2 (en) * | 2005-12-21 | 2007-07-05 | Bayer Healthcare Ag | Substituted pyrimidine derivatives useful in the treatment of cancer and other disorders |
| WO2007076460A2 (en) * | 2005-12-23 | 2007-07-05 | Kalypsys, Inc. | Substituted thiazole ureas useful as inhibitors of protein kinases |
| EP2036557B1 (en) | 2006-05-18 | 2015-10-21 | Eisai R&D Management Co., Ltd. | Antitumor agent for thyroid cancer |
| EP2338488A1 (en) | 2006-05-26 | 2011-06-29 | Bayer HealthCare, LLC | Drug combinations with substituted diaryl ureas for the treatment of cancer |
| DE102006029795A1 (de) * | 2006-06-27 | 2008-01-03 | Schebo Biotech Ag | Neue Harnstoff-Derivate und deren Verwendungen |
| CN101511793B (zh) | 2006-08-28 | 2011-08-03 | 卫材R&D管理有限公司 | 针对未分化型胃癌的抗肿瘤剂 |
| US7897762B2 (en) | 2006-09-14 | 2011-03-01 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of proliferative diseases |
| WO2008079972A2 (en) | 2006-12-20 | 2008-07-03 | Bayer Healthcare Llc | 4-{4- [ ({3-tert-butyl-1- [3- (hydroxymethyl) phenyl] - 1h- pyrazol- 5 -yl } carbamoyl) -amin o] -3-chlorophenoxy} -n-methylpyridine-2-carboxamide as an inhibitor of the vegfr kinase for the treatment of cancer |
| AU2008211952B2 (en) | 2007-01-29 | 2012-07-19 | Eisai R & D Management Co., Ltd. | Composition for treatment of undifferentiated-type of gastric cancer |
| WO2008125014A1 (fr) * | 2007-04-13 | 2008-10-23 | Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. | Composés d'urée, leurs procédés de préparation et leurs utilisations pharmaceutiques |
| CA2684950A1 (en) | 2007-04-20 | 2008-10-30 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases |
| EP1992344A1 (en) | 2007-05-18 | 2008-11-19 | Institut Curie | P38 alpha as a therapeutic target in pathologies linked to FGFR3 mutation |
| JP5638244B2 (ja) | 2007-11-09 | 2014-12-10 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 血管新生阻害物質と抗腫瘍性白金錯体との併用 |
| BRPI0920707A2 (pt) | 2008-10-02 | 2015-12-29 | Respivert Ltd | compostos |
| GB0818033D0 (en) | 2008-10-02 | 2008-11-05 | Respivert Ltd | Novel compound |
| AU2009326148B2 (en) * | 2008-12-11 | 2014-05-08 | Respivert Limited | p38 MAP kinase inhibitors |
| GB0905955D0 (en) | 2009-04-06 | 2009-05-20 | Respivert Ltd | Novel compounds |
| KR20120059558A (ko) * | 2009-08-19 | 2012-06-08 | 암비트 바이오사이언시즈 코포레이션 | 바이아릴 화합물 및 이의 사용 방법 |
| MX2012014776A (es) | 2010-06-25 | 2013-01-29 | Eisai R&D Man Co Ltd | Agente antitumoral que emplea compuestos con efecto inhibidor de cinasas combinados. |
| JP2013531067A (ja) | 2010-07-19 | 2013-08-01 | バイエル ヘルスケア リミティド ライアビリティ カンパニー | 疾病及び状態の処置及び予防のためのフルオロ置換オメガ−カルボキシアリールジフェニル尿素を用いた組み合わせ薬 |
| EP2508184A1 (en) | 2011-04-06 | 2012-10-10 | Æterna Zentaris GmbH | Pyridopyrazine derivatives and their use |
| MX2013009931A (es) | 2011-04-18 | 2013-10-01 | Eisai R&D Man Co Ltd | Agentes terapeuticos contra tumores. |
| US9945862B2 (en) | 2011-06-03 | 2018-04-17 | Eisai R&D Management Co., Ltd. | Biomarkers for predicting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds |
| CN103172648B (zh) * | 2011-12-20 | 2016-05-25 | 上海迪诺医药科技有限公司 | 三杂环衍生物、制备方法及应用 |
| ES2917222T3 (es) | 2011-12-28 | 2022-07-07 | Kyoto Prefectural Public Univ Corp | Normalización del cultivo de células endoteliales de la córnea |
| 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 |
| US20150225373A1 (en) | 2012-08-29 | 2015-08-13 | Respivert Limited | Kinase inhibitors |
| RU2664541C2 (ru) | 2012-11-13 | 2018-08-20 | Эррэй Биофарма Инк. | Бициклические соединения мочевины, тиомочевины, гуанидина и цианогуанидина, пригодные для лечения боли |
| MX365733B (es) | 2012-11-13 | 2019-06-12 | Array Biopharma Inc | Compuestos de n-pirrolidinil, n' -pirazolil-urea, tiourea, guanidina y cianoguanidina como inhibidores de trka cinasa. |
| US9334239B2 (en) | 2012-12-21 | 2016-05-10 | Eisai R&D Management Co., Ltd. | Amorphous form of quinoline derivative, and method for producing same |
| BR122017003181A2 (pt) * | 2013-02-19 | 2019-09-10 | Ono Pharmaceutical Co | composto inibidor de trk, composição farmacêutica e medicamento compreendendo dito composto e seu uso para profilaxia e/ou terapia de doença relacionada à trk e/ou para inibir trk |
| US10517861B2 (en) | 2013-05-14 | 2019-12-31 | Eisai R&D Management Co., Ltd. | Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds |
| US9750723B2 (en) | 2013-10-31 | 2017-09-05 | Ohio University | Prevention and treatment of non-alcoholic fatty liver disease |
| EP3069732B1 (en) | 2013-11-14 | 2023-07-12 | The Doshisha | Drug for treating corneal endothelium by promoting cell proliferation or inhibiting cell damage |
| HUE045340T2 (hu) | 2014-05-15 | 2019-12-30 | Array Biopharma Inc | 1-((3S,4R)-4-(3-fluorfenil)-1-(2-metoxietil)pirrolidin-3-il)-3-(4-metil-3-(2- metilpirimidin-5-il)-1-fenil-1H-pirazol-5-il)karbamid mint TrkA kináz inhibitor |
| CN106659714B (zh) | 2014-07-18 | 2021-06-08 | 俄亥俄大学 | 用于改变生物信号传导的咪唑和噻唑组合物 |
| AU2015301891B2 (en) | 2014-08-11 | 2019-12-05 | Angion Biomedica Corporation | Cytochrome P450 inhibitors and uses thereof |
| CN106660964B (zh) | 2014-08-28 | 2021-09-03 | 卫材R&D管理有限公司 | 高纯度喹啉衍生物及其生产方法 |
| CR20170093A (es) | 2014-09-10 | 2017-07-17 | Glaxosmithkline Ip Dev Ltd | Nuevos compuestos como inhibidores de ret (reorganizado durante la transfección) |
| ES2819871T3 (es) | 2014-09-10 | 2021-04-19 | Glaxosmithkline Ip Dev Ltd | Compuestos utilizados como inhibidores de la quinasa reordenada durante la transfección (RET) |
| US9638690B2 (en) | 2014-11-07 | 2017-05-02 | The University Of British Columbia | Compounds and compositions for use as alkylating agent sensors and methods of use thereof |
| EP3240778A4 (en) | 2014-12-31 | 2018-07-11 | Angion Biomedica Corp. | Methods and agents for treating disease |
| PL3263106T3 (pl) | 2015-02-25 | 2024-04-02 | Eisai R&D Management Co., Ltd. | Sposób tłumienia goryczy pochodnej chinoliny |
| KR102662228B1 (ko) | 2015-03-04 | 2024-05-02 | 머크 샤프 앤드 돔 코포레이션 | 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합 |
| ES2886107T3 (es) | 2015-06-16 | 2021-12-16 | Prism Biolab Co Ltd | Antineoplásico |
| AU2016309356B2 (en) | 2015-08-20 | 2021-06-24 | Eisai R&D Management Co., Ltd. | Tumor therapeutic agent |
| MX380144B (es) | 2017-02-08 | 2025-03-12 | Eisai R&D Man Co Ltd | Composicion farmaceutica de tratamiento de tumores. |
| CA3061888A1 (en) | 2017-05-16 | 2018-11-22 | Eisai R&D Management Co., Ltd. | Treatment of hepatocellular carcinoma |
| CN111818915B (zh) | 2018-01-31 | 2024-05-24 | 德西费拉制药有限责任公司 | 治疗胃肠道间质瘤的组合疗法 |
| AU2019216351B2 (en) | 2018-01-31 | 2024-07-25 | Deciphera Pharmaceuticals, Llc | Combination therapy for the treatment of mastocytosis |
| EP4487909A3 (en) | 2018-06-12 | 2025-03-19 | vTv Therapeutics LLC | Therapeutic uses of glucokinase activators in combination with insulin or insulin analogs |
| NZ784949A (en) | 2019-08-12 | 2025-09-26 | Deciphera Pharmaceuticals Llc | Ripretinib for treating gastrointestinal stromal tumors |
| TWI878335B (zh) | 2019-08-12 | 2025-04-01 | 美商迪賽孚爾製藥有限公司 | 治療胃腸道基質瘤方法 |
| AU2020419197B2 (en) | 2019-12-30 | 2023-08-31 | Deciphera Pharmaceuticals, Llc | Amorphous kinase inhibitor formulations and methods of use thereof |
| KR20250057151A (ko) | 2019-12-30 | 2025-04-28 | 데시페라 파마슈티칼스, 엘엘씨 | 1-(4-브로모-5-(1-에틸-7-(메틸아미노)-2-옥소-1,2-디히드로-1,6-나프티리딘-3-일)-2-플루오로페닐)-3-페닐우레아의조성물 |
| US12391658B2 (en) | 2020-02-18 | 2025-08-19 | Vtv Therapeutics Llc | Sulfoxide and sulfone glucokinase activators and methods of use thereof |
| CN116102522A (zh) * | 2021-11-09 | 2023-05-12 | 河南省化工研究所有限责任公司 | 一种阳离子蓝染料中间体的制备方法 |
| US11779572B1 (en) | 2022-09-02 | 2023-10-10 | Deciphera Pharmaceuticals, Llc | Methods of treating gastrointestinal stromal tumors |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3646059A (en) * | 1969-05-05 | 1972-02-29 | Du Pont | Plant growth regulatory ureidopyrazoles |
| KR0133550B1 (ko) * | 1991-01-21 | 1998-04-23 | 요시또시 가즈오 | 3-벤질리덴-1-카르바모일-2-피롤리돈 유사체 |
| US5162360A (en) * | 1991-06-24 | 1992-11-10 | Warner-Lambert Company | 2-heteroatom containing urea and thiourea ACAT inhibitors |
| DE4227989A1 (de) | 1992-08-21 | 1994-06-09 | Schering Ag | Mittel zur transdermalen Applikation enthaltend 3-Keto-desogestrel |
| CA2171982C (en) * | 1993-09-17 | 2000-02-01 | John Cheung-Lun Lee | Drug binding protein |
| US5559137A (en) * | 1994-05-16 | 1996-09-24 | Smithkline Beecham Corp. | Compounds |
| CA2288787A1 (en) * | 1997-05-22 | 1998-11-26 | G.D. Searle And Co. | Pyrazole derivatives as p38 kinase inhibitors |
| EP0983260A2 (en) * | 1997-05-22 | 2000-03-08 | G.D. Searle & Co. | 3(5)-HETEROARYL SUBSTITUTED PYRAZOLES AS p38 KINASE INHIBITORS |
| DE1019040T1 (de) * | 1997-05-23 | 2001-02-08 | Bayer Corp., West Haven | Hemmung von p38 kinase aktivität durch arylharnstoff |
| WO1998056377A1 (en) * | 1997-06-13 | 1998-12-17 | Smithkline Beecham Corporation | Novel pyrazole and pyrazoline substituted compounds |
| US6080763A (en) * | 1997-11-03 | 2000-06-27 | Boehringer Ingelheim Pharmaceuticals, Inc. | Aromatic heterocyclic compounds and their use as anti-inflammatory agents |
| DE69836563T2 (de) * | 1997-12-22 | 2007-05-16 | Bayer Pharmaceuticals Corp., West Haven | INHIBIERUNG DER p38 KINASE-AKTIVITÄT DURCH DIE VERWENDUNG VON ARYL- UND HETEROARYL-SUBSTITUIERTEN HARNSTOFFEN |
| TR200002617T2 (tr) * | 1997-12-22 | 2000-11-21 | Bayer Corporation | Aril ve heteroaril sübstitüentli heterosiklik üreler kullanılarak RAF kinazın inhibe edilmesi |
| PL205321B1 (pl) * | 1997-12-22 | 2010-04-30 | Bayer Corp | Zastosowanie podstawionych heterocyklicznych moczników do wytwarzania leku do hamowania kinazy raf, podstawione heterocykliczne moczniki oraz kompozycja farmaceutyczna je zawierająca |
-
1998
- 1998-12-22 EP EP98964709A patent/EP1041982B1/en not_active Expired - Lifetime
- 1998-12-22 JP JP2000525102A patent/JP4403482B2/ja not_active Expired - Fee Related
- 1998-12-22 MX MXPA00006233A patent/MXPA00006233A/es not_active Application Discontinuation
- 1998-12-22 ES ES98964709T patent/ES2154253T3/es not_active Expired - Lifetime
- 1998-12-22 AT AT98964709T patent/ATE529109T1/de not_active IP Right Cessation
- 1998-12-22 DE DE1041982T patent/DE1041982T1/de active Pending
- 1998-12-22 WO PCT/US1998/026080 patent/WO1999032111A1/en not_active Ceased
- 1998-12-22 AU AU19971/99A patent/AU739642B2/en not_active Ceased
- 1998-12-22 CA CA002315720A patent/CA2315720A1/en not_active Abandoned
- 1998-12-22 IL IL13673898A patent/IL136738A0/xx active IP Right Grant
-
2000
- 2000-06-12 IL IL136738A patent/IL136738A/en not_active IP Right Cessation
-
2005
- 2005-08-10 IL IL170201A patent/IL170201A/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| MXPA00006233A (es) | 2002-09-18 |
| EP1041982A4 (en) | 2006-06-14 |
| JP4403482B2 (ja) | 2010-01-27 |
| AU739642B2 (en) | 2001-10-18 |
| ATE529109T1 (de) | 2011-11-15 |
| ES2154253T3 (es) | 2012-01-27 |
| CA2315720A1 (en) | 1999-07-01 |
| EP1041982B1 (en) | 2011-10-19 |
| AU1997199A (en) | 1999-07-12 |
| ES2154253T1 (es) | 2001-04-01 |
| WO1999032111A1 (en) | 1999-07-01 |
| IL170201A (en) | 2006-12-31 |
| JP2001526223A (ja) | 2001-12-18 |
| IL136738A (en) | 2007-06-17 |
| IL136738A0 (en) | 2001-06-14 |
| EP1041982A1 (en) | 2000-10-11 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| DE1041982T1 (de) | HEMMUNG DER p38 KINASE AKTIVITÄT DURCH SUBSTITUIERTEN HETEROCYCLISCHEN HARNSTOFFEN | |
| DE1056725T1 (de) | Hemmung von raf-kinase unter verwendung von aryl- und heteroarylsubstituierten heterocyclischen harnstoffen | |
| DE1043995T1 (de) | INHIBIERUNG DER p38 KINASE-AKTIVITÄT DURCH DIE VERWENDUNG VON ARYL- UND HETEROARYLSUBSTITUIERTEN HARNSTOFFEN | |
| DE1047418T1 (de) | Inhibierung der raf-kinase durch substituierte heterocyclische harnstoffverbindungen | |
| DE2117571A1 (de) | Unsymmetrische 1,4-Dihydropyridincarbonsäureester, Verfahren zu ihrer Herstellung sowie ihre Verwendung als Arzneimittel I. Arfm: Farbenfabriken Bayer AG, 5090 Leverkusen | |
| KR870001196A (ko) | 피리딘 화합물과 그의 제법 및 그를 함유하는 약학조성물 | |
| FR2741621B1 (fr) | Nouveaux derives de pyrazole, procede pour leur preparation et compositions pharmaceutiques en contenant | |
| JP2001526223A5 (enExample) | ||
| DE1042305T1 (de) | HEMMUNG DER p38 KINASE UNTER VERWENDUNG VON SYMMETRISCHEN UND ASYMMETRISCHEN DIPHENYLHARNSTOFFEN | |
| DE69807660T2 (de) | Verfahren zur herstellung von pyrazolderivaten | |
| DE73328T1 (de) | Pyrimidin und s-triazin-derivate mit antilipidemischer wirkung. | |
| EP0060223A3 (de) | Mikrobizide Mittel | |
| RU98117621A (ru) | Новые производные пиперазина и пиперидина, способ их получения, фармкомпозиция на их основе, способ лечения, промежуточный продукт | |
| DE59202241D1 (de) | Neue Pyridylderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung. | |
| AT394194B (de) | Verfahren zur herstellung neuer 5-pyrimidincarboxamide und -thiocarboxamide | |
| DE69720515T2 (de) | Isoquinolinamin und phtalazinamin derivate, die reagieren mit crf rezeptoren | |
| DE2228377A1 (de) | Dihydropyridin-carbonsaeureamide, verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel | |
| DE2837477A1 (de) | Sila-substituierte 1,4-dihydropyridin- derivate | |
| DE10237883A1 (de) | Substituierte Isoxazolderivate und ihre Verwendung in der Pharmazie | |
| EP0031801A3 (en) | 6-substituted 4-(2',3'-dichlorophenyl)-2-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid diesters having hypotensive properties as well as process for their preparation and pharmaceutical preparations containing same | |
| EP0129764A3 (de) | Substituierte Phenylsulfonylguanidin-Derivate | |
| DE2614189A1 (de) | Therapeutisch wirksame ureido- und semicarbazido-derivate des tiazols und verfahren zu ihrer herstellung | |
| ATE282595T1 (de) | Pyridin- und piperidinderivate zur behandlung von neurodegenerativen erkrankungen | |
| EP0093252A2 (de) | Thiomethylpyridin-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel | |
| DE2340571A1 (de) | Verfahren zur herstellung von heterocyclischen verbindungen |