JP6117208B2 - ｃ−ｋｉｔキナーゼインヒビターとしての化合物及び組成物 - Google Patents
ｃ−ｋｉｔキナーゼインヒビターとしての化合物及び組成物 Download PDFInfo
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- JP6117208B2 JP6117208B2 JP2014528513A JP2014528513A JP6117208B2 JP 6117208 B2 JP6117208 B2 JP 6117208B2 JP 2014528513 A JP2014528513 A JP 2014528513A JP 2014528513 A JP2014528513 A JP 2014528513A JP 6117208 B2 JP6117208 B2 JP 6117208B2
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- Prior art keywords
- oxadiazol
- pyridine
- imidazo
- carboxamide
- methylphenyl
- Prior art date
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- 229940043355 kinase inhibitor Drugs 0.000 title description 3
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- -1 C 1 -C 6 alkyl Chemical group 0.000 claims description 312
- 125000005842 heteroatom Chemical group 0.000 claims description 230
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 190
- 229910052760 oxygen Inorganic materials 0.000 claims description 126
- 201000010099 disease Diseases 0.000 claims description 118
- 229910052717 sulfur Inorganic materials 0.000 claims description 115
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 107
- 150000003839 salts Chemical class 0.000 claims description 104
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 93
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- 239000008194 pharmaceutical composition Substances 0.000 claims description 71
- 125000001424 substituent group Chemical group 0.000 claims description 70
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 67
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 66
- 208000035475 disorder Diseases 0.000 claims description 63
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- ZMBYQTGAXZOMOO-UHFFFAOYSA-N imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=CC=CN2C(C(=O)N)=CN=C21 ZMBYQTGAXZOMOO-UHFFFAOYSA-N 0.000 claims description 40
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 39
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- DFPAKSUCGFBDDF-UHFFFAOYSA-N Nicotinamide Chemical compound NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 claims description 36
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- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 33
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- 229910052799 carbon Inorganic materials 0.000 claims description 30
- SHQSVMDWKBRBGB-UHFFFAOYSA-N cyclobutanone Chemical compound O=C1CCC1 SHQSVMDWKBRBGB-UHFFFAOYSA-N 0.000 claims description 30
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 28
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims description 26
- 125000003118 aryl group Chemical group 0.000 claims description 25
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 24
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical compound O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 claims description 24
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- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims description 19
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- 125000000753 cycloalkyl group Chemical group 0.000 claims description 18
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- KTHXBEHDVMTNOH-UHFFFAOYSA-N cyclobutanol Chemical compound OC1CCC1 KTHXBEHDVMTNOH-UHFFFAOYSA-N 0.000 claims description 14
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- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims description 13
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- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 12
- 208000030159 metabolic disease Diseases 0.000 claims description 12
- WQGWDDDVZFFDIG-UHFFFAOYSA-N pyrogallol Chemical compound OC1=CC=CC(O)=C1O WQGWDDDVZFFDIG-UHFFFAOYSA-N 0.000 claims description 12
- AHHWIHXENZJRFG-UHFFFAOYSA-N oxetane Chemical compound C1COC1 AHHWIHXENZJRFG-UHFFFAOYSA-N 0.000 claims description 11
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- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 9
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- 125000003545 alkoxy group Chemical group 0.000 claims description 7
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 7
- 125000002757 morpholinyl group Chemical group 0.000 claims description 7
- VBSCTWFMHAWPSW-UHFFFAOYSA-N n-[5-[5-(3-hydroxy-3-methylcyclobutyl)-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C1CC(C)(O)C1 VBSCTWFMHAWPSW-UHFFFAOYSA-N 0.000 claims description 7
- 125000004193 piperazinyl group Chemical group 0.000 claims description 7
- 125000004793 2,2,2-trifluoroethoxy group Chemical group FC(CO*)(F)F 0.000 claims description 6
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims description 6
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 6
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims description 6
- 125000003386 piperidinyl group Chemical group 0.000 claims description 6
- 208000002815 pulmonary hypertension Diseases 0.000 claims description 6
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 6
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 6
- 125000001425 triazolyl group Chemical group 0.000 claims description 6
- 206010002198 Anaphylactic reaction Diseases 0.000 claims description 5
- 230000036783 anaphylactic response Effects 0.000 claims description 5
- 208000003455 anaphylaxis Diseases 0.000 claims description 5
- 239000003937 drug carrier Substances 0.000 claims description 5
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 5
- 125000004574 piperidin-2-yl group Chemical group N1C(CCCC1)* 0.000 claims description 5
- 125000004483 piperidin-3-yl group Chemical group N1CC(CCC1)* 0.000 claims description 5
- 125000001359 1,2,3-triazol-4-yl group Chemical group [H]N1N=NC([*])=C1[H] 0.000 claims description 4
- 125000006432 1-methyl cyclopropyl group Chemical group [H]C([H])([H])C1(*)C([H])([H])C1([H])[H] 0.000 claims description 4
- 206010007559 Cardiac failure congestive Diseases 0.000 claims description 4
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims description 4
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims description 4
- HAJVNPLYVSZWRG-CYBMUJFWSA-N n-[5-[5-[(1r)-2,2-difluorocyclopropyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1[C@H]1CC1(F)F HAJVNPLYVSZWRG-CYBMUJFWSA-N 0.000 claims description 4
- RHNJOZCVGSBEAG-KBPBESRZSA-N n-[5-[5-[(1r,2s)-2-fluorocyclopropyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1[C@H]1C[C@@H]1F RHNJOZCVGSBEAG-KBPBESRZSA-N 0.000 claims description 4
- HAJVNPLYVSZWRG-ZDUSSCGKSA-N n-[5-[5-[(1s)-2,2-difluorocyclopropyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1[C@@H]1CC1(F)F HAJVNPLYVSZWRG-ZDUSSCGKSA-N 0.000 claims description 4
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 4
- 125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 claims description 4
- 125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 claims description 4
- 125000004496 thiazol-5-yl group Chemical group S1C=NC=C1* 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- HVLLSFSZBNWGEY-UHFFFAOYSA-N 7-cyano-n-[5-[5-(3,3-difluorocyclobutyl)-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC(=CC3=NC=2)C#N)C(C)=CC=C1C(N=1)=NOC=1C1CC(F)(F)C1 HVLLSFSZBNWGEY-UHFFFAOYSA-N 0.000 claims description 3
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 3
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 3
- RHJXTZUDRRZZBR-UHFFFAOYSA-N n-[2-methyl-5-[5-(3-oxocyclobutyl)-1,2,4-oxadiazol-3-yl]phenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C1CC(=O)C1 RHJXTZUDRRZZBR-UHFFFAOYSA-N 0.000 claims description 3
- XCRIYMJWHVQZPI-UHFFFAOYSA-N n-[5-[5-(3,3-difluorocyclobutyl)-1,2,4-oxadiazol-3-yl]-2-fluorophenyl]-6-(5-methyl-1h-1,2,4-triazol-3-yl)imidazo[1,2-a]pyridine-3-carboxamide Chemical compound N1C(C)=NN=C1C1=CN2C(C(=O)NC=3C(=CC=C(C=3)C=3N=C(ON=3)C3CC(F)(F)C3)F)=CN=C2C=C1 XCRIYMJWHVQZPI-UHFFFAOYSA-N 0.000 claims description 3
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- RHNJOZCVGSBEAG-ZIAGYGMSSA-N n-[5-[5-[(1s,2r)-2-fluorocyclopropyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1[C@@H]1C[C@H]1F RHNJOZCVGSBEAG-ZIAGYGMSSA-N 0.000 claims description 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 3
- 125000005869 (methoxyethoxy)methanyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])* 0.000 claims description 2
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims description 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 2
- ZFFHSMSEOODFLB-UHFFFAOYSA-N 6-cyano-n-[5-[5-(3,3-difluorocyclobutyl)-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=C(C=CC3=NC=2)C#N)C(C)=CC=C1C(N=1)=NOC=1C1CC(F)(F)C1 ZFFHSMSEOODFLB-UHFFFAOYSA-N 0.000 claims description 2
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- GYBSZVNBXDIORM-UHFFFAOYSA-N 6-fluoro-n-[5-[5-(3-hydroxycyclobutyl)-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=C(F)C=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C1CC(O)C1 GYBSZVNBXDIORM-UHFFFAOYSA-N 0.000 claims description 2
- DXOREGNPVAKXRD-UHFFFAOYSA-N 6-fluoro-n-[5-[5-[1-(methoxymethyl)cyclobutyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound N=1C(C=2C=C(NC(=O)C=3N4C=C(F)C=CC4=NC=3)C(C)=CC=2)=NOC=1C1(COC)CCC1 DXOREGNPVAKXRD-UHFFFAOYSA-N 0.000 claims description 2
- RFSJBIGRJQSQJP-UHFFFAOYSA-N 7-fluoro-n-[5-[5-[3-hydroxy-3-(trifluoromethyl)cyclobutyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC(F)=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C1CC(O)(C(F)(F)F)C1 RFSJBIGRJQSQJP-UHFFFAOYSA-N 0.000 claims description 2
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- STTCYAFMCPPVTG-UHFFFAOYSA-N n-[2-fluoro-5-[5-(3-methylidenecyclobutyl)-1,2,4-oxadiazol-3-yl]phenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(F)=CC=C1C(N=1)=NOC=1C1CC(=C)C1 STTCYAFMCPPVTG-UHFFFAOYSA-N 0.000 claims description 2
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- TUZSVQWAIOHMAN-UHFFFAOYSA-N n-[2-methyl-5-[5-(5-oxaspiro[3.4]octan-2-yl)-1,2,4-oxadiazol-3-yl]phenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C(C1)CC21CCCO2 TUZSVQWAIOHMAN-UHFFFAOYSA-N 0.000 claims description 2
- BFENDVJZXZZBMZ-HAQQTFLXSA-N n-[2-methyl-5-[5-[(7r)-7-methyl-5,8-dioxaspiro[3.4]octan-2-yl]-1,2,4-oxadiazol-3-yl]phenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound O1[C@H](C)COC11CC(C=2ON=C(N=2)C=2C=C(NC(=O)C=3N4C=CC=CC4=NC=3)C(C)=CC=2)C1 BFENDVJZXZZBMZ-HAQQTFLXSA-N 0.000 claims description 2
- ZTSBMHAPDJMGKM-UHFFFAOYSA-N n-[2-methyl-5-[5-[1-(trifluoromethyl)cyclopropyl]-1,2,4-oxadiazol-3-yl]phenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C1(C(F)(F)F)CC1 ZTSBMHAPDJMGKM-UHFFFAOYSA-N 0.000 claims description 2
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- XBZQIWZQXUSRKJ-UHFFFAOYSA-N n-[5-(5-cyclobutyl-1,2,4-oxadiazol-3-yl)-2-fluorophenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(F)=CC=C1C(N=1)=NOC=1C1CCC1 XBZQIWZQXUSRKJ-UHFFFAOYSA-N 0.000 claims description 2
- LAAFMNKBPFCIJU-UHFFFAOYSA-N n-[5-(5-cyclobutyl-1,2,4-oxadiazol-3-yl)-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C1CCC1 LAAFMNKBPFCIJU-UHFFFAOYSA-N 0.000 claims description 2
- ZGOBVKLRYAOXSK-UHFFFAOYSA-N n-[5-(5-cyclopentyl-1,2,4-oxadiazol-3-yl)-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C1CCCC1 ZGOBVKLRYAOXSK-UHFFFAOYSA-N 0.000 claims description 2
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- CXAIUYZBLYTVTR-UHFFFAOYSA-N n-[5-[5-(2-hydroxyspiro[3.3]heptan-6-yl)-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C(C1)CC21CC(O)C2 CXAIUYZBLYTVTR-UHFFFAOYSA-N 0.000 claims description 2
- QVVZVIMTCBNZEO-UHFFFAOYSA-N n-[5-[5-(3,3-difluorocyclobutyl)-1,2,4-oxadiazol-3-yl]-2,4-dimethylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC(C)=C1C(N=1)=NOC=1C1CC(F)(F)C1 QVVZVIMTCBNZEO-UHFFFAOYSA-N 0.000 claims description 2
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- RMXVIPAFTSRMND-UHFFFAOYSA-N n-[5-[5-(3,3-difluorocyclobutyl)-1,2,4-oxadiazol-3-yl]-2-methylphenyl]-6-(1h-pyrazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide Chemical compound CC1=CC=C(C=2N=C(ON=2)C2CC(F)(F)C2)C=C1NC(=O)C(N1C=2)=CN=C1C=CC=2C=1C=NNC=1 RMXVIPAFTSRMND-UHFFFAOYSA-N 0.000 claims description 2
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- YIDCEVNXBMMFHY-UHFFFAOYSA-N n-[5-[5-(3,3-difluorocyclobutyl)-1,2,4-oxadiazol-3-yl]-2-methylphenyl]-7-[1-(2-hydroxyethyl)triazol-4-yl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound CC1=CC=C(C=2N=C(ON=2)C2CC(F)(F)C2)C=C1NC(=O)C(N1C=C2)=CN=C1C=C2C1=CN(CCO)N=N1 YIDCEVNXBMMFHY-UHFFFAOYSA-N 0.000 claims description 2
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- KXHHTSTVKBSBSY-UHFFFAOYSA-N n-[5-[5-(5,9-dioxaspiro[3.5]nonan-2-yl)-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C(C1)CC21OCCCO2 KXHHTSTVKBSBSY-UHFFFAOYSA-N 0.000 claims description 2
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- KIRYEJRGNGQAGY-HUUCEWRRSA-N n-[5-[5-[(1s,2r)-2-fluorocyclopropyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]-7-methylimidazo[1,2-a]pyridine-3-carboxamide Chemical compound C=1N=C2C=C(C)C=CN2C=1C(=O)NC(C(=CC=1)C)=CC=1C(N=1)=NOC=1[C@@H]1C[C@H]1F KIRYEJRGNGQAGY-HUUCEWRRSA-N 0.000 claims description 2
- RHNJOZCVGSBEAG-KGLIPLIRSA-N n-[5-[5-[(1s,2s)-2-fluorocyclopropyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1[C@@H]1C[C@@H]1F RHNJOZCVGSBEAG-KGLIPLIRSA-N 0.000 claims description 2
- TTXRVIZQMULATC-UHFFFAOYSA-N n-[5-[5-[1-(dimethylamino)cyclopropyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound N=1C(C=2C=C(NC(=O)C=3N4C=CC=CC4=NC=3)C(C)=CC=2)=NOC=1C1(N(C)C)CC1 TTXRVIZQMULATC-UHFFFAOYSA-N 0.000 claims description 2
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- AUBYKKLQGKVMBE-UHFFFAOYSA-N n-[5-[5-[1-(methanesulfonamido)cyclobutyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C1(NS(C)(=O)=O)CCC1 AUBYKKLQGKVMBE-UHFFFAOYSA-N 0.000 claims description 2
- LSYNSQSFZORUPT-UHFFFAOYSA-N n-[5-[5-[1-(methanesulfonamido)cyclopropyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C1(NS(C)(=O)=O)CC1 LSYNSQSFZORUPT-UHFFFAOYSA-N 0.000 claims description 2
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- KKVSEJYYZYNJTP-UHFFFAOYSA-N n-[5-[5-[2-(1-hydroxycyclopropyl)ethyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1CCC1(O)CC1 KKVSEJYYZYNJTP-UHFFFAOYSA-N 0.000 claims description 2
- WKGLUTLJDPODRX-UHFFFAOYSA-N n-[5-[5-[3-(2-methoxyethoxy)cyclobutyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1C(OCCOC)CC1C1=NC(C=2C=C(NC(=O)C=3N4C=CC=CC4=NC=3)C(C)=CC=2)=NO1 WKGLUTLJDPODRX-UHFFFAOYSA-N 0.000 claims description 2
- BWCMRRLLHHZFMK-UHFFFAOYSA-N n-[5-[5-[3-(3-hydroxypropylidene)cyclobutyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C1CC(=CCCO)C1 BWCMRRLLHHZFMK-UHFFFAOYSA-N 0.000 claims description 2
- SJOBZOWGSQODEZ-UHFFFAOYSA-N n-[5-[5-[3-(cyclopropylmethoxyimino)cyclobutyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1C(C1)CC1=NOCC1CC1 SJOBZOWGSQODEZ-UHFFFAOYSA-N 0.000 claims description 2
- VLIRSVBOVAFGHU-UHFFFAOYSA-N n-[5-[5-[3-methoxy-3-(trifluoromethyl)cyclobutyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]-n-methylimidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1C(OC)(C(F)(F)F)CC1C1=NC(C=2C=C(C(C)=CC=2)N(C)C(=O)C=2N3C=CC=CC3=NC=2)=NO1 VLIRSVBOVAFGHU-UHFFFAOYSA-N 0.000 claims description 2
- VWCUNZJDOSTKOT-UHFFFAOYSA-N n-[5-[5-[[(3,3-difluorocyclobutyl)amino]methyl]-1,2,4-oxadiazol-3-yl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide Chemical compound C1=C(NC(=O)C=2N3C=CC=CC3=NC=2)C(C)=CC=C1C(N=1)=NOC=1CNC1CC(F)(F)C1 VWCUNZJDOSTKOT-UHFFFAOYSA-N 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- WMOGDCLNSOMBFC-UHFFFAOYSA-N 2-[4-[3-[[5-[5-(3,3-difluorocyclobutyl)-1,2,4-oxadiazol-3-yl]-2-methylphenyl]carbamoyl]imidazo[1,2-a]pyridin-6-yl]pyrazol-1-yl]acetic acid Chemical compound CC1=CC=C(C=2N=C(ON=2)C2CC(F)(F)C2)C=C1NC(=O)C(N1C=2)=CN=C1C=CC=2C=1C=NN(CC(O)=O)C=1 WMOGDCLNSOMBFC-UHFFFAOYSA-N 0.000 claims 1
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- YNDXUCZADRHECN-JNQJZLCISA-N triamcinolone acetonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O YNDXUCZADRHECN-JNQJZLCISA-N 0.000 description 1
- 229960002117 triamcinolone acetonide Drugs 0.000 description 1
- 125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
- FEZBIKUBAYAZIU-UHFFFAOYSA-N trimethobenzamide Chemical compound COC1=C(OC)C(OC)=CC(C(=O)NCC=2C=CC(OCCN(C)C)=CC=2)=C1 FEZBIKUBAYAZIU-UHFFFAOYSA-N 0.000 description 1
- 229960004161 trimethobenzamide Drugs 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
- 208000006961 tropical spastic paraparesis Diseases 0.000 description 1
- ZNRGQMMCGHDTEI-ITGUQSILSA-N tropisetron Chemical compound C1=CC=C2C(C(=O)O[C@H]3C[C@H]4CC[C@@H](C3)N4C)=CNC2=C1 ZNRGQMMCGHDTEI-ITGUQSILSA-N 0.000 description 1
- 229960003688 tropisetron Drugs 0.000 description 1
- 201000008827 tuberculosis Diseases 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000005951 type IV hypersensitivity Effects 0.000 description 1
- 208000027930 type IV hypersensitivity disease Diseases 0.000 description 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 description 1
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 description 1
- 241000701161 unidentified adenovirus Species 0.000 description 1
- 230000003827 upregulation Effects 0.000 description 1
- 210000003932 urinary bladder Anatomy 0.000 description 1
- 230000002227 vasoactive effect Effects 0.000 description 1
- 208000001319 vasomotor rhinitis Diseases 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
- 239000008136 water-miscible vehicle Substances 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 229960005332 zileuton Drugs 0.000 description 1
- MWLSOWXNZPKENC-SSDOTTSWSA-N zileuton Chemical compound C1=CC=C2SC([C@H](N(O)C(N)=O)C)=CC2=C1 MWLSOWXNZPKENC-SSDOTTSWSA-N 0.000 description 1
- 150000003751 zinc Chemical class 0.000 description 1
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A61P11/04—Drugs for disorders of the respiratory system for throat disorders
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- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- A—HUMAN NECESSITIES
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Bioinformatics & Cheminformatics (AREA)
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- Public Health (AREA)
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- Immunology (AREA)
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- Hematology (AREA)
- Obesity (AREA)
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- Emergency Medicine (AREA)
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- Transplantation (AREA)
- Biomedical Technology (AREA)
- Child & Adolescent Psychology (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161530028P | 2011-09-01 | 2011-09-01 | |
| US61/530,028 | 2011-09-01 | ||
| PCT/US2012/052621 WO2013033070A1 (en) | 2011-09-01 | 2012-08-28 | COMPOUNDS AND COMPOSITIONS AS c-KIT KINASE INHIBITORS |
Publications (3)
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| JP2014525444A JP2014525444A (ja) | 2014-09-29 |
| JP2014525444A5 JP2014525444A5 (enExample) | 2015-10-29 |
| JP6117208B2 true JP6117208B2 (ja) | 2017-04-19 |
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| UY34305A (es) | 2011-09-01 | 2013-04-30 | Novartis Ag | Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar |
| BR112014004560A2 (pt) | 2011-09-01 | 2017-04-04 | Irm Llc | compostos e composições como inibidores de c-kit quinase |
| ES2689429T3 (es) * | 2012-07-13 | 2018-11-14 | Ucb Biopharma Sprl | Derivados de imidazopiridina como moduladores de actividad de TNF |
| WO2014110200A1 (en) | 2013-01-10 | 2014-07-17 | Zisman Lawrence S | Non-selective kinase inhibitors |
| US9073921B2 (en) | 2013-03-01 | 2015-07-07 | Novartis Ag | Salt forms of bicyclic heterocyclic derivatives |
| ES2959419T3 (es) | 2013-10-11 | 2024-02-26 | Pulmokine Inc | Formulaciones secas por aspersión |
| EP3077394A1 (de) * | 2013-12-05 | 2016-10-12 | Bayer Pharma Aktiengesellschaft | Aryl- und hetaryl-substituierte imidazo[1,2-a]pyridin-3-carboxamide und ihre verwendung |
| CN103965190A (zh) * | 2014-05-20 | 2014-08-06 | 定陶县友帮化工有限公司 | 一种咪唑并[1,2-a]吡啶-3-甲酸的合成方法 |
| PL3316969T3 (pl) | 2015-07-02 | 2022-06-20 | Janssen Sciences Ireland Unlimited Company | Związki przeciwbakteryjne |
| US10059708B2 (en) * | 2016-04-26 | 2018-08-28 | Northwestern University | Therapeutic targeting of the interleukin 1 receptor-associated kinase 4 (IRAK4) in leukemias characterized by rearrangements in the mixed lineage leukemia gene (MLL-r) |
| BR112018076126A2 (pt) | 2016-06-16 | 2019-03-26 | Janssen Sciences Ireland Unlimited Company | compostos heterocíclicos como antibacterianos |
| CN109415349A (zh) | 2016-06-16 | 2019-03-01 | 爱尔兰詹森科学公司 | 杂环化合物作为抗细菌剂 |
| MX389551B (es) | 2016-10-27 | 2025-03-20 | Pulmokine Inc | Politerapia para tratar hipertension pulmonar. |
| EP4417262A3 (en) | 2017-03-01 | 2024-11-27 | Janssen Sciences Ireland Unlimited Company | Combination therapy |
| CN111039946A (zh) * | 2018-10-15 | 2020-04-21 | 上海轶诺药业有限公司 | 一类咪唑并芳环类化合物的制备和应用 |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| CA3139552A1 (en) * | 2019-05-13 | 2020-11-19 | Novartis Ag | Crystalline forms of n-(5-(5-((1r,2s)-2-fluorocyclopropyl)-1, 2,4-oxadiazol-3-yl)-2-methylphenyl)imidazo[1,2-a]pyridine-3-carboxamide |
| ES2978573T3 (es) | 2019-09-13 | 2024-09-16 | Janssen Sciences Ireland Unlimited Co | Compuestos antibacterianos |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| FI4122923T3 (fi) * | 2020-03-17 | 2025-11-12 | Sumitomo Pharma Co Ltd | Oksadiatsolijohdannainen |
| JP2023534963A (ja) * | 2020-07-15 | 2023-08-15 | サード ハーモニック バイオ， インコーポレイテッド | 選択的ｃ－ｋｉｔキナーゼ阻害剤の結晶質形態 |
| TW202237096A (zh) | 2020-11-19 | 2022-10-01 | 瑞士商諾華公司 | 選擇性ｃ－ｋｉｔ激酶抑制劑之醫藥組合物及其製造及使用方法 |
| TW202237097A (zh) | 2020-11-19 | 2022-10-01 | 美商第三諧波生物公司 | 選擇性ｃ－ｋｉｔ激酶抑制劑之醫藥組合物及其製造及使用方法 |
| WO2022182982A1 (en) * | 2021-02-26 | 2022-09-01 | Third Harmonic Bio, Inc. | Methods for treating c-kit kinase mediated diseases and disorders using a selective c-kit kinase inhibitor |
| AU2022237769A1 (en) | 2021-03-16 | 2023-11-02 | Janssen Sciences Ireland Unlimited Company | Antibacterial compounds |
| MX2023010948A (es) | 2021-03-17 | 2023-11-28 | Janssen Sciences Ireland Unlimited Co | Compuestos antibacterianos. |
| CN117440958A (zh) * | 2021-03-17 | 2024-01-23 | 爱尔兰詹森科学公司 | 抗菌化合物 |
| JP2024540052A (ja) | 2021-10-28 | 2024-10-31 | ヤンセン・サイエンシズ・アイルランド・アンリミテッド・カンパニー | 細菌感染の治療に使用するためのイミダゾピリジンアミド及び関連化合物 |
| WO2024089170A1 (en) | 2022-10-27 | 2024-05-02 | Janssen Sciences Ireland Unlimited Company | Antibacterial compounds |
| EP4626884A1 (en) | 2022-11-30 | 2025-10-08 | Blueprint Medicines Corporation | N-phenyl-pyrazolo[1,5-a]pyridine-3-carboxamide derivatives as wild type c-kit kinase inhibitors for the treatment of urticaria |
| EP4630424A1 (en) * | 2022-12-07 | 2025-10-15 | Third Harmonic Bio, Inc. | Compounds and compositions as c-kit kinase inhibitors |
| WO2024123966A1 (en) * | 2022-12-07 | 2024-06-13 | Third Harmonic Bio, Inc. | Compounds and compositions as c-kit kinase inhibitors |
| WO2024223859A1 (en) | 2023-04-26 | 2024-10-31 | Janssen Pharmaceutica Nv | Antibacterial compounds |
| US20250042898A1 (en) * | 2023-07-25 | 2025-02-06 | Enanta Pharmaceuticals, Inc. | Pharmaceutical Compounds And Compositions As c-Kit Kinase Inhibitors |
| WO2025096979A1 (en) | 2023-11-02 | 2025-05-08 | Arcus Biosciences, Inc. | Thiazole compounds as kit inhibitors and methods of use thereof |
| WO2025146196A1 (zh) * | 2024-01-04 | 2025-07-10 | 上海翰森生物医药科技有限公司 | 多环类衍生物抑制剂、其制备方法和应用 |
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| GB9518993D0 (en) * | 1995-09-16 | 1995-11-15 | Agrevo Uk Ltd | Fungicides |
| US20070072861A1 (en) * | 2000-03-27 | 2007-03-29 | Barbara Roniker | Method of using cyclooxygenase-2 inhibitors in the prevention of cardiovascular disorders |
| AU2003251561A1 (en) | 2002-06-20 | 2004-01-06 | Beacon Looms, Inc. | Knitted electrical conductor fabric |
| JP2007524596A (ja) | 2003-02-28 | 2007-08-30 | トランスフォーム・ファーマシューティカルズ・インコーポレイテッド | 共結晶医薬組成物 |
| US7754717B2 (en) | 2005-08-15 | 2010-07-13 | Amgen Inc. | Bis-aryl amide compounds and methods of use |
| CN101622244A (zh) * | 2006-11-03 | 2010-01-06 | Irm责任有限公司 | 作为蛋白激酶抑制剂的化合物和组合物 |
| UY33726A (es) * | 2010-11-15 | 2012-06-29 | Abbott Lab | Inhibidores de nampt y rock |
| AU2012302080A1 (en) * | 2011-09-01 | 2014-04-17 | Irm Llc | Compounds and compositions as c-kit kinase inhibitors |
| BR112014004560A2 (pt) * | 2011-09-01 | 2017-04-04 | Irm Llc | compostos e composições como inibidores de c-kit quinase |
| EA201490537A1 (ru) * | 2011-09-01 | 2014-07-30 | АйАрЭм ЭлЭлСи | СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗЫ C-Kit |
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