HRP20161714T1 - Inhibitori kinaze - Google Patents
Inhibitori kinaze Download PDFInfo
- Publication number
- HRP20161714T1 HRP20161714T1 HRP20161714TT HRP20161714T HRP20161714T1 HR P20161714 T1 HRP20161714 T1 HR P20161714T1 HR P20161714T T HRP20161714T T HR P20161714TT HR P20161714 T HRP20161714 T HR P20161714T HR P20161714 T1 HRP20161714 T1 HR P20161714T1
- Authority
- HR
- Croatia
- Prior art keywords
- triazolo
- yloxy
- urea
- pyridin
- tert
- Prior art date
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- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 239000004202 carbamide Substances 0.000 claims 66
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 45
- 229910052736 halogen Inorganic materials 0.000 claims 28
- 150000002367 halogens Chemical class 0.000 claims 28
- 125000004093 cyano group Chemical group *C#N 0.000 claims 21
- 229910052757 nitrogen Inorganic materials 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 13
- -1 C3–C7cycloalkyl Chemical group 0.000 claims 11
- 229910052799 carbon Inorganic materials 0.000 claims 11
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 7
- 125000002950 monocyclic group Chemical group 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 150000001721 carbon Chemical group 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 4
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 4
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 4
- 101001132698 Homo sapiens Retinoic acid receptor beta Proteins 0.000 claims 4
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 4
- 102100033909 Retinoic acid receptor beta Human genes 0.000 claims 4
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 4
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 4
- 125000002993 cycloalkylene group Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 4
- 239000001301 oxygen Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 230000005764 inhibitory process Effects 0.000 claims 3
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 claims 3
- 108010068338 p38 Mitogen-Activated Protein Kinases Proteins 0.000 claims 3
- 150000003254 radicals Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- HXZRXOOGYAZGKZ-RVVSJWLRSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(3s)-3-hydroxypyrrolidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5C[C@@H](O)CC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 HXZRXOOGYAZGKZ-RVVSJWLRSA-N 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 208000016300 Idiopathic chronic eosinophilic pneumonia Diseases 0.000 claims 2
- 230000001668 ameliorated effect Effects 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 201000009323 chronic eosinophilic pneumonia Diseases 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 230000005713 exacerbation Effects 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 208000013403 hyperactivity Diseases 0.000 claims 2
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 2
- 125000004092 methylthiomethyl group Chemical group [H]C([H])([H])SC([H])([H])* 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 208000002815 pulmonary hypertension Diseases 0.000 claims 2
- 208000023504 respiratory system disease Diseases 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- IMVFOYQUPDYTOQ-WDJPJFJCSA-N 1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC3=NOC(=C3)C(C)(C)C)CC1)C=C2 IMVFOYQUPDYTOQ-WDJPJFJCSA-N 0.000 claims 1
- HATYBQODHDOCSQ-LOSJGSFVSA-N 1-[(1s,4r)-4-[(3-amino-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]-3-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 HATYBQODHDOCSQ-LOSJGSFVSA-N 0.000 claims 1
- BEVPYSDORKGQPB-MPQUPPDSSA-N 1-[(1s,4r)-4-[[3-(4-azaspiro[2.5]octan-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]-3-[5-tert-butyl-2-[3-(2-morpholin-4-ylethoxy)phenyl]pyrazol-3-yl]urea Chemical compound O([C@@H]1CC[C@@H](C2=CC=CC=C21)NC(=O)NC1=CC(=NN1C=1C=C(OCCN2CCOCC2)C=CC=1)C(C)(C)C)C(=CN12)C=CC1=NN=C2N1CCCCC11CC1 BEVPYSDORKGQPB-MPQUPPDSSA-N 0.000 claims 1
- RCNSFOCYKMRYKM-RWYWNGKESA-N 1-[(1s,4r)-4-[[3-(8-azabicyclo[3.2.1]octan-8-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]-3-[5-tert-butyl-2-[3-[2-(dimethylamino)ethoxy]phenyl]pyrazol-3-yl]urea Chemical compound CN(C)CCOC1=CC=CC(N2C(=CC(=N2)C(C)(C)C)NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5C6CCC5CCC6)=NN=C4C=C3)CC2)=C1 RCNSFOCYKMRYKM-RWYWNGKESA-N 0.000 claims 1
- FMKRMNOGZRJSPU-IOWSJCHKSA-N 1-[(1s,4r)-4-[[3-(azepan-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]-3-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCCCCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 FMKRMNOGZRJSPU-IOWSJCHKSA-N 0.000 claims 1
- KPFFZUJXFIPZQF-AJMMQEIQSA-N 1-[(1s,4r)-4-[[3-[(2r,6s)-2,6-dimethylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]-3-(3-fluoro-5-morpholin-4-ylphenyl)urea Chemical compound C[C@H]1CCC[C@@H](C)N1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3C=C(C=C(F)C=3)N3CCOCC3)CC1)C=C2 KPFFZUJXFIPZQF-AJMMQEIQSA-N 0.000 claims 1
- YYMCMGFUYWRXOB-XZWHSSHBSA-N 1-[5-(1-hydroxy-2-methylpropan-2-yl)-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCCCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)CO)=N1 YYMCMGFUYWRXOB-XZWHSSHBSA-N 0.000 claims 1
- LIFNQHPANZMKRV-HXABMTEBSA-N 1-[5-tert-butyl-2-(2-hydroxyethyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s,6r)-2,6-dimethylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCC[C@@H](C)N1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)CCO)CC1)C=C2 LIFNQHPANZMKRV-HXABMTEBSA-N 0.000 claims 1
- CPKWBPPYOUWLCZ-CHHQVBBHSA-N 1-[5-tert-butyl-2-(2-methyl-3-morpholin-4-ylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-1-methylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN1CCC[C@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C(=C(N4CCOCC4)C=CC=3)C)CC1)C=C2 CPKWBPPYOUWLCZ-CHHQVBBHSA-N 0.000 claims 1
- PPFGEEDXASGMPQ-JPHFWNGBSA-N 1-[5-tert-butyl-2-(2-morpholin-4-ylethyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)CCN3CCOCC3)CC1)C=C2 PPFGEEDXASGMPQ-JPHFWNGBSA-N 0.000 claims 1
- IQHWSWARBZUBRZ-KNWZFJHESA-N 1-[5-tert-butyl-2-(2-morpholin-4-ylethyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s,6r)-2,6-dimethylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCC[C@@H](C)N1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)CCN3CCOCC3)CC1)C=C2 IQHWSWARBZUBRZ-KNWZFJHESA-N 0.000 claims 1
- LAHMSWSHHXPIDI-HOSFBAFGSA-N 1-[5-tert-butyl-2-(2-piperidin-1-ylethyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)CCN3CCCCC3)CC1)C=C2 LAHMSWSHHXPIDI-HOSFBAFGSA-N 0.000 claims 1
- ZGXPERDRDOTNOJ-XZWHSSHBSA-N 1-[5-tert-butyl-2-(4-cyanophenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound O([C@@H]1CC[C@@H](C2=CC=CC=C21)NC(=O)NC1=CC(=NN1C=1C=CC(=CC=1)C#N)C(C)(C)C)C(=CN12)C=CC1=NN=C2N1CCCCC1 ZGXPERDRDOTNOJ-XZWHSSHBSA-N 0.000 claims 1
- LFOHYZPXUYIYHE-URLMMPGGSA-N 1-[5-tert-butyl-2-(4-hydroxyphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound O([C@@H]1CC[C@@H](C2=CC=CC=C21)NC(=O)NC1=CC(=NN1C=1C=CC(O)=CC=1)C(C)(C)C)C(=CN12)C=CC1=NN=C2N1CCCCC1 LFOHYZPXUYIYHE-URLMMPGGSA-N 0.000 claims 1
- NCMGDIVPZOYKKB-URLMMPGGSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[(3-pyrrolidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 NCMGDIVPZOYKKB-URLMMPGGSA-N 0.000 claims 1
- HXTSJZZEGDYJLM-XZWHSSHBSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-(1,4-oxazepan-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCOCCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 HXTSJZZEGDYJLM-XZWHSSHBSA-N 0.000 claims 1
- XNSIGYCUYYNVGK-IOWSJCHKSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-(2-pyrrolidin-1-ylethyl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(CCN5CCCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 XNSIGYCUYYNVGK-IOWSJCHKSA-N 0.000 claims 1
- MLIPRTUGIVHFOC-XZWHSSHBSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-(4-hydroxy-4-methylpiperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCC(C)(O)CC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 MLIPRTUGIVHFOC-XZWHSSHBSA-N 0.000 claims 1
- WYUFXWNYNNZXKN-XZWHSSHBSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-(4-hydroxypiperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCC(O)CC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 WYUFXWNYNNZXKN-XZWHSSHBSA-N 0.000 claims 1
- SYOGEJFFMOMZQL-IOWSJCHKSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-(4-methyl-1,4-diazepan-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1CN(C)CCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 SYOGEJFFMOMZQL-IOWSJCHKSA-N 0.000 claims 1
- QJAYFHLAFHHZCA-XZWHSSHBSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-(4-methylpiperazin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1CN(C)CCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 QJAYFHLAFHHZCA-XZWHSSHBSA-N 0.000 claims 1
- RHWDYVVRBVVSNZ-RRPNLBNLSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-(dimethylamino)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound N([C@H]1CC[C@H](C2=CC=CC=C21)OC=1C=CC2=NN=C(N2C=1)N(C)C)C(=O)NC1=CC(C(C)(C)C)=NN1C1=CC=C(C)C=C1 RHWDYVVRBVVSNZ-RRPNLBNLSA-N 0.000 claims 1
- FCDBOHMWPXGTLH-XZWHSSHBSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-(morpholin-4-ylmethyl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(CN5CCOCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 FCDBOHMWPXGTLH-XZWHSSHBSA-N 0.000 claims 1
- RTLMCLAYNTXJRR-XZWHSSHBSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-(piperazin-1-ylmethyl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(CN5CCNCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 RTLMCLAYNTXJRR-XZWHSSHBSA-N 0.000 claims 1
- IOQMXSYGKHLIIY-WUFINQPMSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-(propan-2-ylamino)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound N([C@H]1CC[C@H](C2=CC=CC=C21)OC=1C=CC2=NN=C(N2C=1)NC(C)C)C(=O)NC1=CC(C(C)(C)C)=NN1C1=CC=C(C)C=C1 IOQMXSYGKHLIIY-WUFINQPMSA-N 0.000 claims 1
- HMHPIWRDKBSONS-XZWHSSHBSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-(pyrrolidin-1-ylmethyl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(CN5CCCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 HMHPIWRDKBSONS-XZWHSSHBSA-N 0.000 claims 1
- QUFKNDLYIZSFKS-AJQTZOPKSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(1-methylpiperidin-4-yl)methyl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1CN(C)CCC1CC1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 QUFKNDLYIZSFKS-AJQTZOPKSA-N 0.000 claims 1
- KJJSQQVDYZTFBX-FRXPANAUSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2r)-1-methylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN1CCC[C@@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 KJJSQQVDYZTFBX-FRXPANAUSA-N 0.000 claims 1
- PMORFOXRERGOFV-TZFWCWEWSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2r)-2-(hydroxymethyl)pyrrolidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5[C@H](CCC5)CO)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 PMORFOXRERGOFV-TZFWCWEWSA-N 0.000 claims 1
- HVVCDRRULYCSDO-SDDUWZMOSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2r)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 HVVCDRRULYCSDO-SDDUWZMOSA-N 0.000 claims 1
- TYPGJWBJSAAYEL-ZGIBFIJWSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2r)-pyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C([C@@H]5NCCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 TYPGJWBJSAAYEL-ZGIBFIJWSA-N 0.000 claims 1
- YWWCAKJSNDQKLU-UKXUPQFXSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-1,2-dimethylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN1CCC[C@@]1(C)C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 YWWCAKJSNDQKLU-UKXUPQFXSA-N 0.000 claims 1
- OTQIIULRWJNZQZ-RWSKJCERSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-1,4,4-trimethylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN1CC(C)(C)C[C@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 OTQIIULRWJNZQZ-RWSKJCERSA-N 0.000 claims 1
- ONKKBCDDIASQCO-OWHBQTKESA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-1-(3-hydroxypropyl)pyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C([C@H]5N(CCC5)CCCO)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 ONKKBCDDIASQCO-OWHBQTKESA-N 0.000 claims 1
- QKKCHOZHCWILMV-RWSKJCERSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-1-ethylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CCN1CCC[C@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 QKKCHOZHCWILMV-RWSKJCERSA-N 0.000 claims 1
- NFMBVJPJNQMKMF-RWSKJCERSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-1-methylpiperidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN1CCCC[C@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 NFMBVJPJNQMKMF-RWSKJCERSA-N 0.000 claims 1
- KJJSQQVDYZTFBX-OIFRRMEBSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-1-methylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN1CCC[C@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 KJJSQQVDYZTFBX-OIFRRMEBSA-N 0.000 claims 1
- QKNKVZDNCWFQBN-OWHBQTKESA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-1-propan-2-ylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CC(C)N1CCC[C@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 QKNKVZDNCWFQBN-OWHBQTKESA-N 0.000 claims 1
- LWSLDXIIUWGCDR-NPYCNQADSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-(hydroxymethyl)-1-methylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN1CCC[C@@]1(CO)C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 LWSLDXIIUWGCDR-NPYCNQADSA-N 0.000 claims 1
- HVVCDRRULYCSDO-LGXAAPQCSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 HVVCDRRULYCSDO-LGXAAPQCSA-N 0.000 claims 1
- TYPGJWBJSAAYEL-YTCPBCGMSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-pyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C([C@H]5NCCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 TYPGJWBJSAAYEL-YTCPBCGMSA-N 0.000 claims 1
- KLWJHTNOZPQBAL-UJLGHMMASA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s,4r)-4-fluoro-1-methylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN1C[C@H](F)C[C@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 KLWJHTNOZPQBAL-UJLGHMMASA-N 0.000 claims 1
- GIROLIMCTRSIKP-MAOWDPDTSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s,6r)-2,6-dimethylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCC[C@@H](C)N1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 GIROLIMCTRSIKP-MAOWDPDTSA-N 0.000 claims 1
- MDILDVZLIKQNRN-SDDUWZMOSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(3r)-1-methylpiperidin-3-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1N(C)CCC[C@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 MDILDVZLIKQNRN-SDDUWZMOSA-N 0.000 claims 1
- CTZMGCYOCWKVLR-NRSKXHDUSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(3r)-1-methylpyrrolidin-3-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1N(C)CC[C@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 CTZMGCYOCWKVLR-NRSKXHDUSA-N 0.000 claims 1
- GRPSKPDBBGEMBU-SDDUWZMOSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(3r)-3-(hydroxymethyl)piperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5C[C@H](CO)CCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 GRPSKPDBBGEMBU-SDDUWZMOSA-N 0.000 claims 1
- ZQJBWYAHZHMBEF-NRSKXHDUSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(3r)-3-(hydroxymethyl)pyrrolidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5C[C@H](CO)CC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 ZQJBWYAHZHMBEF-NRSKXHDUSA-N 0.000 claims 1
- QQIVIPXZDZRORN-TZFWCWEWSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(3r)-3-hydroxypiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5C[C@H](O)CCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 QQIVIPXZDZRORN-TZFWCWEWSA-N 0.000 claims 1
- HXZRXOOGYAZGKZ-OFQAEJFBSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(3r)-3-hydroxypyrrolidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5C[C@H](O)CC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 HXZRXOOGYAZGKZ-OFQAEJFBSA-N 0.000 claims 1
- MDILDVZLIKQNRN-LGXAAPQCSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(3s)-1-methylpiperidin-3-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1N(C)CCC[C@@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 MDILDVZLIKQNRN-LGXAAPQCSA-N 0.000 claims 1
- GRPSKPDBBGEMBU-LGXAAPQCSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(3s)-3-(hydroxymethyl)piperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5C[C@@H](CO)CCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 GRPSKPDBBGEMBU-LGXAAPQCSA-N 0.000 claims 1
- ZQJBWYAHZHMBEF-QZFRTWIZSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(3s)-3-(hydroxymethyl)pyrrolidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5C[C@@H](CO)CC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 ZQJBWYAHZHMBEF-QZFRTWIZSA-N 0.000 claims 1
- WPISUZSSSFYYRT-FRXPANAUSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(3s)-4-methylmorpholin-3-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN1CCOC[C@@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 WPISUZSSSFYYRT-FRXPANAUSA-N 0.000 claims 1
- KOGHOSPWYAJOSM-IOWSJCHKSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(4-methylpiperazin-1-yl)methyl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1CN(C)CCN1CC1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 KOGHOSPWYAJOSM-IOWSJCHKSA-N 0.000 claims 1
- GEYPGDJAMZBVBK-IOWSJCHKSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[1-(dimethylamino)cyclopentyl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound N=1N=C2C=CC(O[C@H]3C4=CC=CC=C4[C@@H](NC(=O)NC=4N(N=C(C=4)C(C)(C)C)C=4C=CC(C)=CC=4)CC3)=CN2C=1C1(N(C)C)CCCC1 GEYPGDJAMZBVBK-IOWSJCHKSA-N 0.000 claims 1
- BAIRDDIIZWYRHL-AJQTZOPKSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[2-(4-methylpiperazin-1-yl)ethyl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1CN(C)CCN1CCC1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 BAIRDDIIZWYRHL-AJQTZOPKSA-N 0.000 claims 1
- SBRHELUWHYVPLK-XZWHSSHBSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[2-(dimethylamino)ethyl-methylamino]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound N([C@H]1CC[C@H](C2=CC=CC=C21)OC=1C=CC2=NN=C(N2C=1)N(C)CCN(C)C)C(=O)NC1=CC(C(C)(C)C)=NN1C1=CC=C(C)C=C1 SBRHELUWHYVPLK-XZWHSSHBSA-N 0.000 claims 1
- RUHHSWHOTHUJES-URLMMPGGSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[2-(dimethylamino)propan-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound N([C@H]1CC[C@H](C2=CC=CC=C21)OC=1C=CC2=NN=C(N2C=1)C(C)(C)N(C)C)C(=O)NC1=CC(C(C)(C)C)=NN1C1=CC=C(C)C=C1 RUHHSWHOTHUJES-URLMMPGGSA-N 0.000 claims 1
- RTJLBAKEGIITKV-MPQUPPDSSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[2-(morpholin-4-ylmethyl)phenyl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(C=5C(=CC=CC=5)CN5CCOCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 RTJLBAKEGIITKV-MPQUPPDSSA-N 0.000 claims 1
- XJLMWFJIJNUMBD-MPQUPPDSSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[3-(morpholin-4-ylmethyl)phenyl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(C=5C=C(CN6CCOCC6)C=CC=5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 XJLMWFJIJNUMBD-MPQUPPDSSA-N 0.000 claims 1
- CDJAJHGSVPTKHD-IOWSJCHKSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[4-(2-hydroxyethyl)piperazin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCN(CCO)CC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 CDJAJHGSVPTKHD-IOWSJCHKSA-N 0.000 claims 1
- YZBDWSPVFZAOBU-AJQTZOPKSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[4-(2-hydroxyethyl)piperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCC(CCO)CC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 YZBDWSPVFZAOBU-AJQTZOPKSA-N 0.000 claims 1
- IYMSNHSJVBSIAN-AJQTZOPKSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[4-(2-hydroxypropan-2-yl)piperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCC(CC5)C(C)(C)O)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 IYMSNHSJVBSIAN-AJQTZOPKSA-N 0.000 claims 1
- JUCVIQPUESHERW-IOWSJCHKSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[4-(hydroxymethyl)piperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCC(CO)CC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 JUCVIQPUESHERW-IOWSJCHKSA-N 0.000 claims 1
- ICTCPIYVRNOFKT-AJQTZOPKSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[[1-(2,2-difluoroethyl)piperidin-4-yl]methyl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(CC5CCN(CC(F)F)CC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 ICTCPIYVRNOFKT-AJQTZOPKSA-N 0.000 claims 1
- ASVZASHTYMGAOY-AJQTZOPKSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[methyl(2-morpholin-4-ylethyl)amino]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound N=1N=C2C=CC(O[C@H]3C4=CC=CC=C4[C@@H](NC(=O)NC=4N(N=C(C=4)C(C)(C)C)C=4C=CC(C)=CC=4)CC3)=CN2C=1N(C)CCN1CCOCC1 ASVZASHTYMGAOY-AJQTZOPKSA-N 0.000 claims 1
- XGYITCMBPCGUIA-RWSKJCERSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4r)-4-[[8-methyl-3-[(2s)-1-methylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN1CCC[C@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2C XGYITCMBPCGUIA-RWSKJCERSA-N 0.000 claims 1
- FNZGHWSBOGBXEO-KYJUHHDHSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4s)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=CC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@@H](OC3=CN4C(N5CCCCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 FNZGHWSBOGBXEO-KYJUHHDHSA-N 0.000 claims 1
- KJJSQQVDYZTFBX-DTXPUJKBSA-N 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[(1s,4s)-4-[[3-[(2s)-1-methylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN1CCC[C@H]1C1=NN=C2N1C=C(O[C@@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)CC1)C=C2 KJJSQQVDYZTFBX-DTXPUJKBSA-N 0.000 claims 1
- FVZPBIRMGJRVHZ-URLMMPGGSA-N 1-[5-tert-butyl-2-(6-methylpyridin-3-yl)pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=NC(C)=CC=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCCCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 FVZPBIRMGJRVHZ-URLMMPGGSA-N 0.000 claims 1
- DYYFUFQEMFYRBN-AJQTZOPKSA-N 1-[5-tert-butyl-2-[1-(2-morpholin-4-ylethyl)pyrazol-4-yl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound O([C@@H]1CC[C@@H](C2=CC=CC=C21)NC(=O)NC1=CC(=NN1C1=CN(CCN2CCOCC2)N=C1)C(C)(C)C)C(=CN12)C=CC1=NN=C2N1CCCCC1 DYYFUFQEMFYRBN-AJQTZOPKSA-N 0.000 claims 1
- MSSHWENRKDIVFA-ZIINUWHCSA-N 1-[5-tert-butyl-2-[1-(2-morpholin-4-ylethyl)pyrazol-4-yl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C3=CN(CCN4CCOCC4)N=C3)CC1)C=C2 MSSHWENRKDIVFA-ZIINUWHCSA-N 0.000 claims 1
- YSKOKHOVMCOKCY-JHOUSYSJSA-N 1-[5-tert-butyl-2-[1-(3-morpholin-4-ylpropyl)pyrazol-4-yl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound O([C@@H]1CC[C@@H](C2=CC=CC=C21)NC(=O)NC1=CC(=NN1C1=CN(CCCN2CCOCC2)N=C1)C(C)(C)C)C(=CN12)C=CC1=NN=C2N1CCCCC1 YSKOKHOVMCOKCY-JHOUSYSJSA-N 0.000 claims 1
- OOGBVDJIMLFJAA-URLMMPGGSA-N 1-[5-tert-butyl-2-[1-[2-(dimethylamino)ethyl]imidazol-4-yl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN(C)CCN1C=NC(N2C(=CC(=N2)C(C)(C)C)NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCCCC5)=NN=C4C=C3)CC2)=C1 OOGBVDJIMLFJAA-URLMMPGGSA-N 0.000 claims 1
- ZCGLQYCDXXXUOQ-XZWHSSHBSA-N 1-[5-tert-butyl-2-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=NN(CCN(C)C)C=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCCCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 ZCGLQYCDXXXUOQ-XZWHSSHBSA-N 0.000 claims 1
- NEOFBONIFALDKM-MAOWDPDTSA-N 1-[5-tert-butyl-2-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2r,6s)-2,6-dimethylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCC[C@@H](C)N1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C3=CN(CCN(C)C)N=C3)CC1)C=C2 NEOFBONIFALDKM-MAOWDPDTSA-N 0.000 claims 1
- PPZSTJQLZOPKBO-LGXAAPQCSA-N 1-[5-tert-butyl-2-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C3=CN(CCN(C)C)N=C3)CC1)C=C2 PPZSTJQLZOPKBO-LGXAAPQCSA-N 0.000 claims 1
- NBHSAIVAOKTXJV-IOWSJCHKSA-N 1-[5-tert-butyl-2-[1-[3-(dimethylamino)propyl]pyrazol-4-yl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=NN(CCCN(C)C)C=C1N1C(NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCCCC5)=NN=C4C=C3)CC2)=CC(C(C)(C)C)=N1 NBHSAIVAOKTXJV-IOWSJCHKSA-N 0.000 claims 1
- WFIZTUSHTIAVTC-HOSFBAFGSA-N 1-[5-tert-butyl-2-[2-(4-methylpiperazin-1-yl)ethyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)CCN3CCN(C)CC3)CC1)C=C2 WFIZTUSHTIAVTC-HOSFBAFGSA-N 0.000 claims 1
- BRIBDOAFGLMLHM-HOSFBAFGSA-N 1-[5-tert-butyl-2-[2-[2-(dimethylamino)ethyl-methylamino]pyrimidin-4-yl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3N=C(N=CC=3)N(C)CCN(C)C)CC1)C=C2 BRIBDOAFGLMLHM-HOSFBAFGSA-N 0.000 claims 1
- FVYNMBIROAFACG-IOWSJCHKSA-N 1-[5-tert-butyl-2-[3-(2-hydroxyethoxy)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound O([C@@H]1CC[C@@H](C2=CC=CC=C21)NC(=O)NC1=CC(=NN1C=1C=C(OCCO)C=CC=1)C(C)(C)C)C(=CN12)C=CC1=NN=C2N1CCCCC1 FVYNMBIROAFACG-IOWSJCHKSA-N 0.000 claims 1
- BVCPALJEBTYVCE-AJQTZOPKSA-N 1-[5-tert-butyl-2-[3-(2-hydroxyethoxymethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound O([C@@H]1CC[C@@H](C2=CC=CC=C21)NC(=O)NC1=CC(=NN1C=1C=C(COCCO)C=CC=1)C(C)(C)C)C(=CN12)C=CC1=NN=C2N1CCCCC1 BVCPALJEBTYVCE-AJQTZOPKSA-N 0.000 claims 1
- LSFQNNFTVPSQBZ-IOWSJCHKSA-N 1-[5-tert-butyl-2-[3-(2-hydroxyethylsulfanyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound O([C@@H]1CC[C@@H](C2=CC=CC=C21)NC(=O)NC1=CC(=NN1C=1C=C(SCCO)C=CC=1)C(C)(C)C)C(=CN12)C=CC1=NN=C2N1CCCCC1 LSFQNNFTVPSQBZ-IOWSJCHKSA-N 0.000 claims 1
- LFIUFKYQMBSQKY-NGWURLOXSA-N 1-[5-tert-butyl-2-[3-(2-morpholin-4-ylethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=C(CCN4CCOCC4)C=CC=3)CC1)C=C2 LFIUFKYQMBSQKY-NGWURLOXSA-N 0.000 claims 1
- DSDZXDXKVVLUDJ-TVIAEEBLSA-N 1-[5-tert-butyl-2-[3-(2-piperidin-1-ylethoxy)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=C(OCCN4CCCCC4)C=CC=3)CC1)C=C2 DSDZXDXKVVLUDJ-TVIAEEBLSA-N 0.000 claims 1
- AVAQDIXVBBBQGA-TVIAEEBLSA-N 1-[5-tert-butyl-2-[3-(2-piperidin-1-ylethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=C(CCN4CCCCC4)C=CC=3)CC1)C=C2 AVAQDIXVBBBQGA-TVIAEEBLSA-N 0.000 claims 1
- BZPISJIATYKGTG-MYYHXLQYSA-N 1-[5-tert-butyl-2-[3-(2-pyrrolidin-1-ylethoxy)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2r,6s)-2,6-dimethylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCC[C@@H](C)N1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=C(OCCN4CCCC4)C=CC=3)CC1)C=C2 BZPISJIATYKGTG-MYYHXLQYSA-N 0.000 claims 1
- MCLKXOSHMUGFGI-NGWURLOXSA-N 1-[5-tert-butyl-2-[3-(2-pyrrolidin-1-ylethoxy)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=C(OCCN4CCCC4)C=CC=3)CC1)C=C2 MCLKXOSHMUGFGI-NGWURLOXSA-N 0.000 claims 1
- HTJIQZAYUHTHGN-NGWURLOXSA-N 1-[5-tert-butyl-2-[3-(2-pyrrolidin-1-ylethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=C(CCN4CCCC4)C=CC=3)CC1)C=C2 HTJIQZAYUHTHGN-NGWURLOXSA-N 0.000 claims 1
- CYWAUYOYRABYEA-XZWHSSHBSA-N 1-[5-tert-butyl-2-[3-(hydroxymethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound O([C@@H]1CC[C@@H](C2=CC=CC=C21)NC(=O)NC1=CC(=NN1C=1C=C(CO)C=CC=1)C(C)(C)C)C(=CN12)C=CC1=NN=C2N1CCCCC1 CYWAUYOYRABYEA-XZWHSSHBSA-N 0.000 claims 1
- FBWPYWOWCXQISI-JCXRYELGSA-N 1-[5-tert-butyl-2-[3-(morpholin-4-ylmethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=C(CN4CCOCC4)C=CC=3)CC1)C=C2 FBWPYWOWCXQISI-JCXRYELGSA-N 0.000 claims 1
- GJLRZDZTDUUGIK-OIDHKYIRSA-N 1-[5-tert-butyl-2-[3-(piperidin-1-ylmethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound O([C@@H]1CC[C@@H](C2=CC=CC=C21)NC(=O)NC1=CC(=NN1C=1C=C(CN2CCCCC2)C=CC=1)C(C)(C)C)C(=CN12)C=CC1=NN=C2N1CCCCC1 GJLRZDZTDUUGIK-OIDHKYIRSA-N 0.000 claims 1
- DMKWGCKWBCMPGC-NGWURLOXSA-N 1-[5-tert-butyl-2-[3-(piperidin-1-ylmethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=C(CN4CCCCC4)C=CC=3)CC1)C=C2 DMKWGCKWBCMPGC-NGWURLOXSA-N 0.000 claims 1
- WTZJZACQMVDSQY-JCXRYELGSA-N 1-[5-tert-butyl-2-[3-(pyrrolidin-1-ylmethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=C(CN4CCCC4)C=CC=3)CC1)C=C2 WTZJZACQMVDSQY-JCXRYELGSA-N 0.000 claims 1
- FOMWVCKACWAEAY-OIDHKYIRSA-N 1-[5-tert-butyl-2-[3-[(4-hydroxypiperidin-1-yl)methyl]phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound O([C@@H]1CC[C@@H](C2=CC=CC=C21)NC(=O)NC1=CC(=NN1C=1C=C(CN2CCC(O)CC2)C=CC=1)C(C)(C)C)C(=CN12)C=CC1=NN=C2N1CCCCC1 FOMWVCKACWAEAY-OIDHKYIRSA-N 0.000 claims 1
- FJFBFJWNPMYCTO-OIDHKYIRSA-N 1-[5-tert-butyl-2-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1CN(C)CCN1CC1=CC=CC(N2C(=CC(=N2)C(C)(C)C)NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCCCC5)=NN=C4C=C3)CC2)=C1 FJFBFJWNPMYCTO-OIDHKYIRSA-N 0.000 claims 1
- WYLSALUKYRKZPB-FRJUPVQCSA-N 1-[5-tert-butyl-2-[3-[(dimethylamino)methyl]phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=C(CN(C)C)C=CC=3)CC1)C=C2 WYLSALUKYRKZPB-FRJUPVQCSA-N 0.000 claims 1
- BMMJCYVJTXZEFD-CHLVBXGZSA-N 1-[5-tert-butyl-2-[3-[2-(4-methylpiperazin-1-yl)ethoxy]phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s,6r)-2,6-dimethylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCC[C@@H](C)N1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=C(OCCN4CCN(C)CC4)C=CC=3)CC1)C=C2 BMMJCYVJTXZEFD-CHLVBXGZSA-N 0.000 claims 1
- DIPURTWBAPAIJP-JHOUSYSJSA-N 1-[5-tert-butyl-2-[3-[2-(dimethylamino)ethoxy]phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN(C)CCOC1=CC=CC(N2C(=CC(=N2)C(C)(C)C)NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCCCC5)=NN=C4C=C3)CC2)=C1 DIPURTWBAPAIJP-JHOUSYSJSA-N 0.000 claims 1
- UICAWNXPOFRERT-SZAHLOSFSA-N 1-[5-tert-butyl-2-[3-[2-(dimethylamino)ethoxy]phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[di(propan-2-yl)amino]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound N([C@H]1CC[C@H](C2=CC=CC=C21)OC=1C=CC2=NN=C(N2C=1)N(C(C)C)C(C)C)C(=O)NC1=CC(C(C)(C)C)=NN1C1=CC=CC(OCCN(C)C)=C1 UICAWNXPOFRERT-SZAHLOSFSA-N 0.000 claims 1
- SKSUDAWXICVVEY-HPFIMXAPSA-N 1-[5-tert-butyl-2-[3-[2-(dimethylamino)ethoxy]phenyl]pyrazol-3-yl]-3-[(1s,4s)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=C(OCCN(C)C)C=CC=3)CC1)C=C2 SKSUDAWXICVVEY-HPFIMXAPSA-N 0.000 claims 1
- HJWOJGSDYYJNGA-XZWHSSHBSA-N 1-[5-tert-butyl-2-[4-(hydroxymethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound O([C@@H]1CC[C@@H](C2=CC=CC=C21)NC(=O)NC1=CC(=NN1C=1C=CC(CO)=CC=1)C(C)(C)C)C(=CN12)C=CC1=NN=C2N1CCCCC1 HJWOJGSDYYJNGA-XZWHSSHBSA-N 0.000 claims 1
- VLIFFKUVZXPQOC-XZWHSSHBSA-N 1-[5-tert-butyl-2-[4-(hydroxymethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-(4-hydroxypiperidin-1-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound O([C@@H]1CC[C@@H](C2=CC=CC=C21)NC(=O)NC1=CC(=NN1C=1C=CC(CO)=CC=1)C(C)(C)C)C(=CN12)C=CC1=NN=C2N1CCC(O)CC1 VLIFFKUVZXPQOC-XZWHSSHBSA-N 0.000 claims 1
- HGULZGGYSUYMMV-RWSKJCERSA-N 1-[5-tert-butyl-2-[4-(hydroxymethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-1-methylpiperidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN1CCCC[C@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(CO)=CC=3)CC1)C=C2 HGULZGGYSUYMMV-RWSKJCERSA-N 0.000 claims 1
- WMFFZSCASIJTKB-OIFRRMEBSA-N 1-[5-tert-butyl-2-[4-(hydroxymethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-1-methylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound CN1CCC[C@H]1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(CO)=CC=3)CC1)C=C2 WMFFZSCASIJTKB-OIFRRMEBSA-N 0.000 claims 1
- PCBVMJFEKHHTNX-JCXRYELGSA-N 1-[5-tert-butyl-2-[4-(morpholin-4-ylmethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(CN4CCOCC4)=CC=3)CC1)C=C2 PCBVMJFEKHHTNX-JCXRYELGSA-N 0.000 claims 1
- UWIDFVDXNMJMFN-NGWURLOXSA-N 1-[5-tert-butyl-2-[4-(piperidin-1-ylmethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(CN4CCCCC4)=CC=3)CC1)C=C2 UWIDFVDXNMJMFN-NGWURLOXSA-N 0.000 claims 1
- WVMVXFQXQBEXKE-JCXRYELGSA-N 1-[5-tert-butyl-2-[4-(pyrrolidin-1-ylmethyl)phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[[3-[(2s)-2-methylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCCCN1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(CN4CCCC4)=CC=3)CC1)C=C2 WVMVXFQXQBEXKE-JCXRYELGSA-N 0.000 claims 1
- ZVXYBSOXXHRGQE-OIDHKYIRSA-N 1-[5-tert-butyl-2-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]pyrazol-3-yl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1CN(C)CCN1CC1=CC=C(N2C(=CC(=N2)C(C)(C)C)NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C(N5CCCCC5)=NN=C4C=C3)CC2)C=C1 ZVXYBSOXXHRGQE-OIDHKYIRSA-N 0.000 claims 1
- LJHPYMQOGRXVHY-LITSAYRRSA-N 1-[5-tert-butyl-3-(methanesulfonamido)-2-methoxyphenyl]-3-[(1s,4r)-4-[(3-piperidin-1-yl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=C(C(C)(C)C)C=C(NS(C)(=O)=O)C(OC)=C1NC(=O)N[C@@H]1C2=CC=CC=C2[C@H](OC2=CN3C(N4CCCCC4)=NN=C3C=C2)CC1 LJHPYMQOGRXVHY-LITSAYRRSA-N 0.000 claims 1
- JRZOIEWLSODTDS-OWPQXHQJSA-N 1-[5-tert-butyl-3-(methanesulfonamido)-2-methoxyphenyl]-3-[(1s,4r)-4-[[3-[(2s)-1-methylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C1=C(C(C)(C)C)C=C(NS(C)(=O)=O)C(OC)=C1NC(=O)N[C@@H]1C2=CC=CC=C2[C@H](OC2=CN3C([C@H]4N(CCC4)C)=NN=C3C=C2)CC1 JRZOIEWLSODTDS-OWPQXHQJSA-N 0.000 claims 1
- HFCQVVYZAFRJGW-GXKKKHDSSA-N 1-cyclopropyl-3-[(1s,4r)-4-[[3-[(2r,6s)-2,6-dimethylpiperidin-1-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]urea Chemical compound C[C@H]1CCC[C@@H](C)N1C1=NN=C2N1C=C(O[C@H]1C3=CC=CC=C3[C@@H](NC(=O)NC3CC3)CC1)C=C2 HFCQVVYZAFRJGW-GXKKKHDSSA-N 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- HTAJQCXADBTAST-RWSKJCERSA-N ethyl 3-[3-tert-butyl-5-[[(1s,4r)-4-[[3-[(2s)-1-methylpyrrolidin-2-yl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]oxy]-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoylamino]pyrazol-1-yl]benzoate Chemical compound CCOC(=O)C1=CC=CC(N2C(=CC(=N2)C(C)(C)C)NC(=O)N[C@@H]2C3=CC=CC=C3[C@H](OC3=CN4C([C@H]5N(CCC5)C)=NN=C4C=C3)CC2)=C1 HTAJQCXADBTAST-RWSKJCERSA-N 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000006340 pentafluoro ethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
Classifications
-
- 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
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
- C07C53/02—Formic acid
- C07C53/06—Salts thereof
-
- 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
- C07D231/40—Acylated on said nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
Claims (12)
1. Spoj formule (I) ili odgovarajuća farmaceutski prihvatljiva sol:
[image]
(I)
naznačen time da
W je NH,
Y je O,
R1 je skupina odabrana od (IIa) - (IIc):
[image]
(IIa) (IIb) (IIc)
R8 i R9 svaki neovisno jesu vodik ili C1–C6alkil, ili R8 i R9 mogu zajedno s dušikovim atomom za koji su vezani tvoriti 5-11-člani zasićeni monociklički ili fuzinirani ili spiro-biciklički sustav prstenova koji mogu dalje sadržavati heteroatom koji je kisik ili dušik, a rečeni dušikov atom može biti supstituiran s C1–C6alkilom, pri čemu takve C1–C6alkilne skupine mogu biti supstituirane skupinama C1–C6alkil, C3–C6cikloalkil, hidroksil ili halogen;
X1, X2, X3, X4 i X5 svaki neovisno jest ugljikov atom, dušikov atom, skupina –(CH)– ili skupina –NH–, a takva da svaka njihova kombinacija tvori aromatski sustav prstena,
R10 je izabran iz sljedeće skupine: vodik, –CN, –NRARB, –N(RC)(C2–C6alkilen)–NRARB, –N(RC)(C3–C7cikloalkilen)–NRARB, –(C1–C6alkilen)–NRARB, –(C3–C7cikloalkilen)–NRARB,–O–(C2–C6alkilen)–NRARB,–O–(C3–C7cikloalkilen)–NRARB, –S–(C2–C6alkilen)–NRARB, –S–(C3–C7cikloalkilen)–NRARB, –N(RC)C(O)–(C1–C6alkilen)–NRARB, –N(RC)C(O)–(C3–C7cikloalkilen)–NRARB, –C(O)N(RC)–(C2–C6alkilen)–NRARB, –C(O)N(RC)–(C3–C7cikloalkilen)–NRARB, –C(O)N(RC)–(C2–C6alkilen)–ORD, –C(O)N(RC)–(C3–C7cikloalkilen)–ORD, –N(RC)C(O)NRARB, –C(O)NRARB, –N(RC)C(O)N(RC)–(C2–C6alkilen)–NRARB, –N(RC)C(O)N(RC)–(C3–C7cikloalkilen)–NRARB, –(C2–C6alkilen)–ORD, –(C3–C7cikloalkilen)–ORD, –O–(C2–C6alkilen)–ORD, –O–(C3–C7cikloalkilen)–ORD, –S–(C2–C6alkilen)–ORD, –S–(C3–C7cikloalkilen)–ORD, –N(RC) S(O)2– (C1–C6alkilen)–NRARB, –N(RC)S(O)2–(C3–C7cikloalkilen)–NRARB, –S(O)2N(RC)–(C2–C6alkilen)–NRARB, –S(O)2N(RC)–(C3–C7cikloalkilen)–NRARB, –S(O)2N(RC)–(C2–C6alkilen)–ORD, –S(O)2N(RC)–(C3–C7cikloalkilen)–ORD, –N(RC)S(O)2–(C2–C6alkilen)–ORD, –N(RC) S(O)2–(C3–C7cikloalkilen)–ORD,–S(O)2N(RARB), –N(RC)S(O)2RD, –N(RC)C(O)RC, –ORC, –SRC, –(C3–C7heterocikloalkil), (C5–C7heterocikloalkil)–(C1–C6alkil), (C5–C7heterocikloalkil)(C3–C6cikloalkil)– te C3–C7 heterocikloalkilkarbonil; gdje bilo koji takav C1–C6alkilni, C3–C6cikloalkilni, –(C1–C6alkilenski)–, –(C2–C6alkilenski)–, –(C3–C7cikloalkilenski)–, –(C3–C7heterocikloalkilni), (C5–C7heterocikloalkilni)–(C1–C6 alkilni), (C5–C7 heterocikloalkilni)–(C3–C6 cikloalkilni) te (C3–C7heterocikloalkilni)karbonilni dio gore navedenih skupina može biti supstituiran skupinama C1–C6 alkil, C3–C7cikloalkil, hidroksil ili halogen;
R11 je vezan za X4 i odabran je iz sljedeće skupine:
vodik; –CN; C1–C6alkil koji je supstituiran sa skupinom odabranom od sljedećih: –CN, –ORC, –SRC, halogen; C3–C6cikloalkil koji je supstituiran skupinom odabranom od sljedećih: C1–C4alkil, –CN, –ORC, –SRD, halogen; –NRARB, –N(RC)(C2–C6alkilen)–NRARB, –N(RC)(C3–C7cikloalkilen)–NRARB, –(C1–C6alkilen)–NRARB, –(C3–C7cikloalkilen)–NRARB, –O–(C2–C6alkilen)–NRARB, –O–(C3–C7cikloalkilen)–NRARB, –S–(C2–C6alkilen)–NRARB, –S–(C3–C7cikloalkilen)–NRARB, –N(RC)C(O)–(C1–C6alkilen)–NRARB, –N(RC)C(O)–(C3–C7cikloalkilen)–NRARB, –C(O)N(RC)–(C2–C6alkilen)–NRARB, –C(O)N(RC)–(C3–C7cikloalkilen)–NRARB, –C(O)N(RC)–(C2–C6alkilen)–ORD, –C(O)N(RC)–(C3–C7cikloalkilen)–ORD, –N(RC)C(O)N(RARB), –C(O)N(RARB), –N(RC)C(O)N(RC)–(C2–C6alkilen)–NRARB, –N(RC)C(O)N(RC)–(C3–C7cikloalkilen)–NRARB, –O–(C2–C6alkilen)–ORD, –O–(C3–C7cikloalkilen)–ORD, –S–(C2–C6alkilen)–ORD, –S–(C3–C7cikloalkilen)–ORD, –N(RC)S(O)2–(C1–C6alkilen)–NRARB, –N(RC)S(O)2–(C3–C7cikloalkilen)–NRARB, –S(O)2N(RC)–(C2–C6alkilen)–NRARB, –S(O)2N(RC)–(C3–C7cikloalkilen)–NRARB, –S(O)2N(RC)–(C2–C6alkilen)–ORD, –S(O)2N(RC)–(C3–C7cikloalkilen)–ORD, –N(RC)S(O)2–(C2–C6alkilen)–ORD, –N(RC)S(O)2(C3–C7cikloalkilen)–ORD, –S(O)2N(RARB), –N(RC)S(O)2RD, –N(RC)C(O)RC, ORC, SRC, –(C3–C7heterocikloalkil), (C5–C7heterocikloalkil)–(C1–C6alkil), (C5–C7heterocikloalkil)(C3–C6cikloalkil) te (C3–C7 heterocikloalkil) karbonil, gdje bilo koji takav C1–C6alkilni, C3–C6cikloalkilni, – (C1–C6alkilenski)–, –(C2–C6alkilenski)–, –(C3–C7cikloalkilenski)–, –(C3–C7heterocikloalkilni), (C5–C7heterocikloalkilni)–(C1–C6alkilni), (C5–C7 heterocikloalkilni)–(C3–C6 cikloalkilni) te (C3–C7heterocikloalkilni)karbonilni dio gore navedenih skupina može biti supstiutiran s jednom, dvjema ili trima skupinama R25 koji su neovisno odabrani iz sljedeće skupine: C1–C6alkil, (C1–C3) halogenalkil, (C1–C4)hidroksialkil, C3–C7cikloalkil, hidroksil te halogen; ili
R11 je vezan za X4 te jest fenil ili 5- ili 6-člani monociklički heteroaril, pri čemu je takav fenil ili 5- ili 6-člani monociklički heteroaril supstituiran skupinom odabranom od sljedećih: C1–C6alkil koji je supstituiran skupinom –CN; C3–C6cikloalkil koji je supstituiran skupinom odabranom od sljedećih: –CN, –ORC, –SRC ili halogen; –N(RC)(C2–C6alkilen)–NRARB, –N(RC)(C3–C7cikloalkilen)–NRARB, –(C1–C6alkilen)–NRARB, –(C3–C7cikloalkilen )–NRARB, –O–(C3–C7cikloalkilen)–NRARB, –S–(C2–C6alkilen)–NRARB, –S–(C3–C7cikloalkilen)–NRARB, –N(RC)C(O)–(C1–C6alkilen)–NRARB, –N(RC)C(O)–(C3–C7cikloalkilen)–NRARB, –C(O)N(RC)–(C2–C6alkilen)–NRARB, –C(O)N(RC)–(C3–C7cikloalkilen)–NRARB, –C(O)N(RC)–(C2–C6alkilen)–ORD, –C(O)N(RC)–(C3–C7cikloalkilen)–ORD, –N(RC)C(O)N(RC)–(C2–C6alkilen)–NRARB, –N(RC)C(O)N(RC)–(C3–C7cikloalkilen)–NRARB, –O–(C3–C7cikloalkilen)–ORD, –S–(C3–C7cikloalkilen)–ORD, –N(RC)S(O)2–(C1–C6alkilen)–NRARB, –N(RC)S(O)2–(C3–C7cikloalkilen)–NRARB, –S(O)2N(RC)–(C2–C6alkilen)–NRARB, –S(O)2N(RC)–(C3–C7cikloalkilen)–NRARB, –S(O)2N(RC)–(C2–C6alkilen)–ORD, –S(O)2N(RC)–(C3–C7cikloalkilen)–ORD, –N(RC)S(O)2–(C2–C6alkilen)–ORD, –N(RC)S(O)2–(C3–C7cikloalkilen)–ORD, – N(RC)S(O)2RD, –(C3–C7heterocikloalkil), (C5–C7heterocikloalkil)–(C1–C6alkil), (C5–C7heterocikloalkil)(C3–C6cikloalkil) te (C3–C7heterocikloalkil)karbonil, pri čemu bilo koji takav C1–C6alkilni, C3–C6cikloalkilni, –(C1–C6alkilenski)––(C2–C6alkilenski)–, –(C3–C7cikloalkilenski)–, –(C3–C7heterocikloalkilni), (C5–C7heterocikloalkilni)–(C1–C6alkilni), (C5–C7heterocikloalkilni)–(C3–C6 cikloalkilni te (C3–C7heterocikloalkilni)karbonilni dio gore navedenih skupina može biti supstiutiran s jednom, dvjema ili trima skupinama R25 koje su neovisno odabrane iz sljedeće skupine: C1–C6alkil, (C1–C3) haloalkil, (C1–C4)hidroksialkil, C3–C7cikloalkil, hidroksil te halogen;
RA i RB su svakom prilikom neovisno vodik, C1–C6alkil ili C3–C7 cikloalkil, a takav C1–C6alkil i C3–C7cikloalkil može biti supstituiran sljedećim skupinama: C1–C3alkil, C3–C7cikloalkil, –ORD, –CN ili halogen; alternativno, RA i RB mogu zajedno s atomom dušika za koji su vezani tvoriti 5-11-člani zasićeni heterociklički monociklički ili biciklički sustav prstenova koji može biti supstituiran jednom ili više sljedećih skupina –ORD, –CN, halogen, C1–C6alkil ili C3–C7 cikloalkil, a takav C1–C6alkil i C3–C7cikloalkil može biti supstituiran sljedećim skupinama: C1–C3 alkil, C3–C7 cikloalkil, –ORD, –CN ili halogen; a koji 5-11-člani zasićeni heterociklički monociklički ili biciklički prsten može sadržavati daljnji heteroatom koji je kisik ili dušik, a rečeni dušikov atom može biti supstituiran s C1–C6alkilom ili C3–C6cikloalkilom, gdje bilo koji takav C1–C6alkil ili C3–C6cikloalkil može biti supstituiran skupinom C1–C6alkil, C3–C7cikloalkil, –ORD, –CN, ili halogen; i/ili RA i RB mogu biti vezani za jedan ugljikov atom –(C1–C6alkilenskog)–, –(C2–C6alkilenskog)– ili –(C3–C7cikloalkilenskog)– dijela skupine vezane za dušik za koji su vezani tvoreći zasićeni prsten koji sadržava do 6 atoma u prstenu;
RC je svakom prilikom neovisno vodik, C1–C6alkil ili C3–C6 cikloalkil, a takav C1–C6alkil i C3–C6cikloalkil mogu biti supstituirani sljedećim skupinama: C1–C3alkil, –ORD, –CN ili halogen;
RD je svakom prilikom neovisno vodik, –CH3 ili –C2H5;
R12 i R13 neovisno jesu vodik, C1–C6alkil, ili halogen;
A je divaletni cikloalkilenski radikal koji ima 5 ili 6 atoma u prstenu, a rečeni cikloalkilenski prsten vezan je za W i Y i fuzioniran je s fenilnim prstenom, a takav fenilni prsten može biti supstituiran jednom ili dvjema skupinama R24, a pri čemu rečeni divalentni cikloalkilenski radikal, ima sljedeću formulu:
[image]
R24 je svakom prilikom neovisno odabran iz sljedeće skupine: C1–C6alkil, halogen te cijano;
R2 je radikal formule (IIIa), (IIIb), (IIIc) ili (IIId):
[image]
(IIIa) (IIIb) (IIIc) (IIId)
pri čemu
R14 je odabran iz sljedeće skupine : –F, –CH3, –C2H5, –CH2OH, –CH2OMe, –CF2CF3–, CH2SCH3, –SCH3 te –SC2H5;
R15 i R16 neovisno jesu –CH3 ili –C2H5;
R17 je odabran iz sljedeće skupine: nevezni elektrosnki par, vodik, –CF3, –NRERF, –(C3–C7cikloalkil), –(C3–C7heterocikloalkil), aril ili heteroaril gdje takav –(C3–C7cikloalkil), –(C3–C7heterocikloalkil), aril ili heteroaril mogu biti supstituirani sljedećim skupinama: C1–C6alkil, C3–C7cikloalkil ili halogen; ili
R17 jest skupina opće formule (IV)
[image]
(IV)
u kojoj
R20 jest odabran iz sljedeće skupine : –F, –CH3, –C2H5, –CH2OH, –CH2OMe, ––CF2CF3–, CH2SCH3, –SCH3 te –SC2H5;
R21 je –CH3 ili –C2H5;
ili
R20 i R21 kao što je gore definirano mogu zajedno s ugljikovim atomom za koji su vezani tvoriti zasićeni 3-7 člani monociklički prsten;
RE i RF svaki neovinso jest C1–C6alkil, koji može biti supstituiran skupinom C1–C3alkil, –ORG, –CN ili halogen; alternativno, RE i RF mogu zajedno s dušikovim atomom za koji su vezani tvoriti zasićeni 5–11-člani monociklički ili biciklički heterociklički sustav prstena koji može biti supstituiran sljedećim skupinama: –ORG, –CN, halogen, C1–C6alkil ili C3–C7 cikloalkil, a takav C1–C6alkil i C3–C7cikloalkil može biti supstituiran sljedećom skupinom: C1–C3alkil, C3–C7cikloalkil, –ORG, –CN ili halogen; a koji 5–11–člani zasićeni monociklički ili biciklički heterociklički prsten može sadržavati daljnji heteroatom koji je kisik ili dušik, a rečeni dušikov atom može biti supstituiran C1–C6alkilom ili C3–C6cikloalkilom, pri čemu bilo koji takav C1–C6alkil ili C3–C6cikloalkil može biti supstituiran skupinom C1–C6alkil ili C3–C7cikloalkil;
RG is vodik, –CH3 ili –C2H5;
R18 je odabran iz sljedeće skupine: nevenzi elektronski par, vodik, aril, heteroaril, –(C1–C6alkil), –(C3–C7cikloalkil), –(C3–C7heterocikloalkil), (C5–C7heterocikloalkil)–(C1–C6alkil) te (C5–C7heterocikloalkil)–(C3–C6cikloalkil), gdje bilo koji takav aril, heteroaril, –(C1–C6alkil), –(C3–C7cikloalkil), –(C3–C7heterocikloalkil), (C5–C7heterocikloalkil)–(C1–C6alkil) te (C5–C7heterocikloalkil)–(C3–C6 cikloalkil) može biti supstituiran skupinom –CN, –OH, halogen, –COORM, C1–C6alkil, C3–C6cikloalkil, –O–(C1–C6alkil), –O–(C3–C6cikloalkil), –S–(C1–C6alkil), –S–(C3–C6cikloalkil), –NRHRJ, –N(RL)(C2–C6alkilen)–NRHRJ, –N(RL)(C3–C7cikloalkilen)–NRHRJ, –(C1–C6alkilen)–NRHRJ, –(C3–C7cikloalkilen)–NRHRJ, –O–(C2–C6alkilen)–NRHRJ, –O–(C3–C7cikloalkilen)–NRHRJ, –S–(C2–C6alkilen)–NRHRJ, –S–(C3–C7cikloalkilen)–NRHRJ, –N(RL)C(O)–(C1–C6alkilen)–NRHRJ, –N(RL)C(O)–(C3–C7cikloalkilen)–NRHRJ, –C(O)N(RL)–(C2–C6alkilen)–NRHRJ, –C(O)N(RL)–(C3–C7cikloalkilen)–NRHRJ, –C(O)N(RL)–(C2–C6alkilen)–ORM, –C(O)N(RL)–(C3–C7cikloalkilen )–ORM, –N(RL)C(O)N(RHRJ), –C(O)N(RHRJ), –N(RL)C(O)N(RL)–(C2–C6alkilen)–NRHRJ, –N(RL)C(O)N(RL)–(C3–C7cikloalkilen)–NRHRJ, –O–(C2–C6alkilen)–ORM, –O–(C3–C7cikloalkilen)–ORM, –S–(C2–C6alkilen)–ORM, –S–(C3–C7cikloalkilen)–ORM, –N(RL)S(O)2–(C1–C6alkilen)–NRHRJ, –N(RL) S(O)2–(C3–C7cikloalkilen)–NRHRJ, – S(O)2N(RL)–(C2–C6alkilen)–NRHRJ, – S(O)2N(RL)–(C3–C7cikloalkilen)–NRHRJ, – S(O)2N(RL)–(C2–C6alkilen)–ORM, –S(O)2N(RL)–(C3–C7cikloalkilen)–ORM, –N(RL) S(O)2–(C2–C6alkilen)–ORM, –N(RL) S(O)2–(C3–C7cikloalkilen)–ORM, – S(O)2N(RHRJ), –N(RL) S(O)2 RL, –N(RL)C(O) RL, O RL, S RL, –(C3–C7heterocikloalkil), (C5–C7heterocikloalkil)–(C1–C6alkil) te (C5–C7 heterocikloalkil)–(C3–C6cikloalkil), gdje je bilo koji takav C1–C6alkilni, C3–C6cikloalkilni, –(C1–C6alkilenski)–, –(C2–C6alkilenski)–, –(C3–C7cikloalkilenski)–, –(C3–C7heterocikloalkilni), (C5–C7heterocikloalkilni)–(C1–C6 alkilni) te (C5–C7heterocikloalkilni)–(C3–C6 cikloalkilni) dio gore navedenih skupina može biti supstituiran skupinom C1–C6alkil, C3–C7 cikloalkil, –O RL ili halogen;
RH i RJ, su u svakoj prilici neovisno vodik, C1–C6alkil ili C3–C6cikloalkil, a takav C1–C6 alkil ili C3–C6cikloalkil može biti supstituiran skupinom C1–C3alkil, –ORM, CN ili halogen; alternativno, RH i RJ mogu i zajedno s dušikovim atomom za koji su vezani tvoriti 5-11–člani zasićeni monociklički ili biciklički heterociklički sustav prstenova koji može biti supstituiran s jednom ili više sljedećih skupina: –ORM, –CN, halogen, C1–C6alkil ili C3–C7 cikloalkil, a takav C1–C6alkil i C3–C7cikloalkil može biti supstituiran skupinom C1–C3alkil, C3–C7cikloalkil, –ORM, CN ili halogen; te koji 5-11–člani zasićeni monociklički ili biciklički heterociklički prsten može dalje sadržavati heteroatom koji je kisik ili dušik, a rečeni dušikov atom može biti supstituiran s C1–C6alkilom ili C3–C6cikloalkilom, gdje bilo koji takav C1–C6alkil ili C3–C6cikloalkil može biti supstituiran skupinom C1–C6alkil, C3–C7 cikloalkil, –ORM, CN, ili halogen;
i/ili RH i RJ mogu biti vezani za jedan ugljikov atom –(C1–C6alkilenskog)–, –(C2–C6alkilenskog)– ili –(C3–C7cikloalkilenskog)– dijela skupine vezane za dušik za koji su vezani tvoreći zasićeni prsten koji sadržava do 6 atoma u prstenu:
RL je svakom prilikom neovisno vodik, C1–C6alkil ili C3–C6cikloalkil, a takav C1–C6alkil ili C3–C6cikloalkil može biti supstituiran skupinom C1–C3alkil, –ORM, –CN ili halogen;
RM je svakom prilikom neovisno vodik, C1–C6alkil ili C3–C6cikloalkil, a takav C1–C6alkil ili C3–C6cikloalkil može biti supstituiran skupinom hidroksil, –CN ili halogen;
z1, z2, z3 i z4 su neovisno odabrani iz sljedeće skupine: C, N, S, O, skupina –CH– te skupina –NH–, u takvoj kombinaciji da nastali tvoreni prsten jest aromatski sustav;
R19 je odabran iz sljedeće skupine: vodik, –CF3, –NRERF, –(C3–C7cikloalkil), –(C3–C7heterocikloalkil), aril ili heteroaril gdje bilo koji ovaj –(C3–C7cikloalkil), –(C3–C7heterocikloalkil), aril ili heteroaril može biti supstituiran skupinom C1–C6alkil, C3–C7cikloalkil, ili halogen; ili
R19 jest skupina opće formule (V)
[image]
(V)
u kojoj R20, R21, RE i RF jesu kao što su gore definirani;
T je –N= ili –CR23=;
R23 je H, halogen, –CH3, ili –CN;
R22 je H, halogen, –CH3, ili –CN;
q je 0, 1, 2 ili 3.
2. Spoj formule (I) prema patentnom zahtjevu 1 koji jest spoj formule (Ia), naznačen time da je stereogeni ugljikov centar cikloalkilenskog dijela prstena A koji je vezan za skupinu W i naznačen niže brojem (1) ima sljedeću apsolutnu konfiguraciju niže predstavljenu kao:
[image]
(Ia)
ili odgovarajuća farmaceutski prihvatljiva sol.
3. Spoj formule (I) prema patentnom zahtjevu 1 ili 2 koji jest spoj formule (Ib), naznačen time da su stereogeni ugljikovi centri cikloalkilenskog dijela prstena A koji su vezani za skupinu W i Y i naznačeni niže brojevima (1) i (2), ima sljedeću apsolutnu konfiguraciju niže predstavljenu kao:
[image]
(Ib)
ili odgovarajuća farmaceutski prihvatljiva sol.
4. Spoj formule (I) prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time da
R1 jest skupina formule (IIc):
[image]
(IIc)
Ili odgovarajuća farmaceutski prihvatljiva sol.
5. Spoj formule (I) prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time da
R1 jest skupina formule (IIca) kao što je gore definirano, koja je spojena za skupinu Y preko ugljika koji je u susjedstvu X2
[image]
(IIca)
te gdje X4 jest ugljikov atom, X5 je dušikov atom, X3 je dušikov atom te X2 je skupina –CH–, te R13jest vodik;
gdje je R11 sljedeća skupina:
[image]
u kojoj može biti prisutan R25 i predstavlja jedan, dva ili tri supstituenta koji su neovinso odabrani od sljedećih: C1–C6alkil, (C1–C3) halogenalkil, (C1–C4)hidroksialkil, C3–C7cikloalkil, hidroksil i halogen; te gdje zvjezdica prestavlja mjesto vezanja skupine R11 za ostatak molekule preko X4;
gdje R2 jest radikal formule (IIIb):
[image]
(IIIb)
u kojoj z1 = –CH–, z2= C, z3 i z4 jesu N te R17 jest skupina opće formule (IV)
[image]
(IV)
te gdje R20 jest –CH3 ili –CH2OH, R21 je –CH3 te R18 je kao što je definirano u patetnom zahtjevu 1.
6. Spoj formule (I) prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time da
R1 jest skupina formule (IIca) kao što je gore definirano, koja je spojena za skupinu Y preko ugljika koji je u susjedstvu X2
[image]
(IIca)
te gdje X4 jest ugljikov atom, X5 je dušikov atom, X3 je dušikov atom te X2 je skupina –CH– i R13jest vodik;
gdje je R11 sljedeća skupina:
[image]
u kojoj može biti prisutan R25 i predstavlja jedan, dva ili tri supstituenta koji su neovinso odabrani od sljedeće skupine: C1–C6alkil, (C1–C3) halogenalkil, (C1–C4)hidroksialkil, C3–C7cikloalkil, hidroksil i halogen; te gdje zvjezdica prestavlja mjesto vezanja skupine R11 na ostatak molekule preko X4;
gdje R2 jest radikal formule (IIIb):
[image]
(IIIb)
u kojoj z1 = –CH–, z2= C, z3 i z4 jesu N te R17 jest skupina opće formule (IV)
[image]
(IV)
te gdje R20 jest –CH3 ili –CH2OH, R21 je –CH3 te R18 je kao što je definirano u patetnom zahtjevu 1.
7. Spoj prema patentnom zahtjevu 1 odabran od sljedećih:
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(2-pirolidin-1-il-etil)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-((1S,4R)-4-{3-[2-(4-metil-piperazin-1-il)-etil]-[1,2,4]triazolo[4,3-a]piridin-6-iloksi}-1,2,3,4-tetrahidro-naftalen-1-il)-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4R)-4-(3-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4R)-4-(3-piperidin-4-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4R)-4-[3-((S)-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4R)-4-((S)-3-pirolidin-2-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4R)-4-(3-piperazin-1-ilmetil-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4R)-4-(3-izopropilamino-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4R)-4-((R)-3-pirolidin-2-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(4-metil-piperazin-1-ilmetil)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4R)-4-(3-morfolin-4-ilmetil-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4R)-4-(3-pirolidin-1-ilmetil-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(4-morfolin-4-ilmetil-fenil)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(3-morfolin-4-ilmetil-fenil)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(2-morfolin-4-ilmetil-fenil)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(1-metil-piperidin-4-ilmetil)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-((1S,4R)-4-{3-[1-(2,2-difluoro-etil)-piperidin-4-ilmetil]-[1,2,4]triazolo[4,3-a]piridin-6-iloksi}-1,2,3,4-tetrahidro-naftalen-1-il)-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4R)-4-[3-(4-hidroksipiperidin-1-il)-[1,2,4]triazolo[4,3-a]piridine-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(lS,4R)-4-{3-[(2-hidroksi-etil)-metil-amino]-[1,2,4]triazolo[4,3-a]piridine-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-3-hidroksi-pirolidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-3-hidroksi-pirolidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((R)-2-hidroksimetil-pirolidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-hidroksimetil-pirolidin-1-il)-[1,2,4]triazololo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(3-hidroksimetil-fenil)-2H-pirazol-3-il]-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
3-[3-tert-butil-5-(3-{(1S,4R)-4-[3-((S)-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-ureido)-pirazol-1-il]-benzojeva kiselina etil-ester;
1-[5-tert-butil-2-(3-hidroksimetil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(4-hidroksimetil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}urea;
1-[5-tert-butil-2-(4-hidroksimetil-fenil)-2H-pirazol-3-il]-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-{5-tert-butil-2-[3-(2-hidroksi-etilsulfanil)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-(2-Hidroksi-1,1-dimetil-etil)-2-p-tolil-2H-pirazol-3-il]-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-[5-tert-butil-2-(4-hidroksimetil-fenil)-2H-pirazol-3-il]-3-{(1S,3S)-3-[3-((S)-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-indan-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((R)-3-hidroksi-pirolidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-hidroksi-etoksi)-fenil]-2H-pirazol-3-il}-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-{5-tert-butil-2-[3-(2-dimetilamino-etoksi)-fenil]-2H-pirazol-3-il}-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-{5-tert-butil-2-[3-(4-metil-piperazin-1-ilmetil)-fenil]-2H-pirazol-3-il}-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-{5-tert-butil-2-[3-(2-hidroksi-etoksi)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-1-metil-pirolidin-2-i)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-((1S,4R)-4-{3-[(2-dimetilamino-etil)-metil-amino]-[1,2,4]triazolo[4,3-a]piridin-6-iloksi}-1,2,3,4-tetrahidro-naftalen-1-il)-urea;
1-[5-tert-butil-2-(3-piperidin-1-ilmetil-fenil)-2H-pirazol-3-il]-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-((1S,4R)-4-{3-[metil-(2-morfolin-4-il-etil)-amino]-[1,2,4]triazolo[4,3-a]piridin-6-iloksi}-1,2,3,4-tetrahidro-naftalen-1-il)-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((R)-1-morfolin-4-il-etil)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-1-morfolin-4-il-etil)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-1,2-dimetil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-hidroksi-etoksimetil)-fenil]-2H-pirazol-3-il}-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4R)-4-(3-[1,4]oksazepan-4-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-{3-[4-(2-hidroksi-etil)-piperazin-1-ilmetil]-fenil}-2H-pirazol-3-il)-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-{5-tert-butil-2-[3-(4-hidroksi-piperidin-1-ilmetil)-fenil]-2H-pirazol-3-il}-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-{5-tert-butil-2-[3-(2-hidroksi-etilsulfanil)-fenil]-2H-pirazol-3-il}-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(4-hidroksimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4S)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(3-hidroksimetil-4-metil-piperazin-1-ilmetil)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(4-hidroksimetil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-(4-hidroksi-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-1-izopropil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4R)-4-(3-dimetilamino-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((R)-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-1-etil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-1-metil-piperidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-3-hidroksi-piperidin-1-il)-[14,2,4]triazolo[4,3-
a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((R)-3-hidroksi-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(4-hidroksimetil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-1-metil-piperidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(4-hidroksietil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[(1S,4R)-4-(3-Azepan-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-3-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(4-metil-piperazine-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(4-metil-[1,4]diazepan-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}urea;
1-[5-tert-butil-2-(4-hidroksi-fenil)-2H-pirazol-3-il]-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-[5-tert-butil-2-(4-cijano-fenil)-2H-pirazol-3-il]-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4S)-4-[3-((S)-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(4-hidroksi-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-((1S,4R)-4-{3-[4-(1-hidroksi-1-metil-etil)-piperidin-1-il]-[1,2,4]triazolo[4,3-a]piridin-6-iloksi}-1,2,3,4-tetrahidro-naftalen-1-il)-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-[(1S,4R)-4-(3-pirolidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(1-dimetilamino-1-metil-etil)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((R)-3-hidroksimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-3-hidroksimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(4-hidroksi-4-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(1-metil-1-pirolidin-1-il-etil)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((R)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-4-metil-morfolin-3-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-((1S,4R)-4-{3-[(S)-1-(3-hidroksi-propil)-pirolidin-2-il]-[1,2,4]triazolo[4,3-a]piridin-6-iloksi}-1,2,3,4-tetrahidro-naftalen-1-il)-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-hidroksimetil-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(1,4-dimetil-piperazin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-1,4,4-trimetil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-1-metil-piperidin-3-il)-[1,2,4]triazolo [4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((R)-1-metil-piperidin-3-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((R)-1-metil-pirolidin-3-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((2S,4R)-4-fluoro-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-3-hidroksimetil-pirolidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((R)-3-hidroksimetil-pirolidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-((1S,4R)-4-{3-[4-(2-hidroksi-etil)-piperazin-1-il]-[1,2,4]triazolo[4,3-a]piridin-6-iloksi}-1,2,3,4-tetrahidro-naftalen-1-il)-urea;
1-{5-tert-butil-2-[3-(2-dimetilamino-etoksi)-fenil]-2H-pirazol-3-il-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidronaftalen-1-il]-urea;
1-{5-tert-butil-2-[3-(2-dimetilamino-etoksi)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-(cis-2,6-dimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(3-morfolin-4-ilmetil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(4-metil-piperazin-1-ilmetil)-fenil]-2H-pirazol-3-il}-3-{1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-(1-dimetilamino-ciklopentil)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[(1S,4R)-4-(3-amino-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-3-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-urea;
1-[5-tert-butil-2-(6-metil-piridin-3-il)-2H-pirazol-3-il]-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-{5-tert-butil-2-[3-(2-dimetilamino-etoksi)-fenil]-2H-pirazol-3-il}-3-[(1S,4R)-4-(3-diizopropilamino-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
N-(5-tert-butil-2-metoksi-3-{3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-ureido}-fenil)-metansulfonamid;
1-(5-tert-butil-2-p-tolil-2H-pirazol-3-il)-3-{(1S,4R)-4-[8-metil-3-((S)-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[4-(4-metil-piperazin-1-ilmetil)-fenil]-2H-pirazol-3-il}-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-(3-tert-butil-1’-metil-1’H-[1,4’]bipirazolil-5-il)-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-[3-tert-butil-1’-(2-dimetilamino-etil)-1’H-[1,4’]bipirazolil-5-il]-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
N-[5-tert-butil-2-metoksi-3-(3-{(lS,4R)-4-[3-((S)-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-ureido)-fenil]-metansulfonamid;
1-[5-tert-butil-2-(2-hidroksi-etil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-izoksazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[3-tert-butil-1’-(2-morfolin-4-il-etil)-1’H-[1,4’]bipirazolil-5-il]-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-[3-tert-butil-1’-(3-dimetilamino-propil)-1’H-[1,4’]bipirazolil-5-il]-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-[3-tert-butil-1’-(3-morfolin-4-il-propil)-1’H-[1,4’]bipirazolil-5-il]-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-{(1S,4R)-4-[3-((2S,6R)-2,6-dimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidronaftalen-1-il}-3-(3-fluor-5-morfolin-4-il-fenil)-urea;
1-[5-tert-butil-2-(2-morfolin-4-il-etil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-ciklopropil-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(2-hidroksi-etil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[-(2-dimetilamino-etil)-1H-imidazol-4-il]-2H-pirazol-3-il}-3-[(1S,4R)-4-(3-piperidin-1-il-[1,2,4]triazolo[4,3-a]piridin-6-iloksi)-1,2,3,4-tetrahidro-naftalen-1-il]-urea;
1-[5-tert-butil-2-(2-hidroksi-etil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-1-metil-piperidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(2-morfolin-4-il-etil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{(1S,4R)-4-[3-(8-aza-biciklo[3.2.1]okt-8-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-3-{5-tert-butil-2-[3-(2-dimetilamino-etoksi)-fenil]-2H-pirazol-3-il}-urea;
1-{5-tert-butil-2-[3-(2-dimetilamino-etoksi)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((R)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[3-tert-butil-1’-(2-morfolin-4-il-etil)-1’H-[1,4’]bipirazolil-5-il]-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[3-tert-butil-1’-(2-dimetilamino-etil)-1’H-[1,4’]bipirazolil-5-il]-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-metil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidronaftalen-1-il]-urea;
1-[5-tert-butil-2-(2-dimetilamino-etil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(2-piperidin-1-il-etil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[2-(4-metil-piperazin-1-il)-etil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(3-morfolin-4-ilmetil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-morfolin-4-il-etil)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-pirolidin-1-il-etil)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-{3-[2-(etil-metil-amino)-etil]-fenil}-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-dimetilamino-etil)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-piperidin-1-il-etil)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-{3-[2-(4-metil-piperazin-1-il)-etil]-fenil}-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metilpiperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-[1,4]oksazepan-4-il-etil)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-{3-[2-(4-metil-[1,4]diazepan-1-il)-etil]-fenil}-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(2-hidroksi-etil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-3-metil-morfolin-4-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-{2-[(2-dimetilamino-etil)-metil-amino]-pirimidin-4-il}-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-dimetilamino-etoksi)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-3-metil-morfolin-4-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(2-morfolin-4-il-etil)-2H-pirazol-3-il]-3-{1S,4R)-4-[3-((S)-3-metil-morfolin-4-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(4-metil-piperazin-1-ilmetil)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(3-pirolidin-1-ilmetil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-pirolidin-1-il-etoksi)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimetilpiperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-{3-[2-(4-metil-piperazin-1-il)-etoksi]-fenil}-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-{3-[2-(etil-metil-amino)-etoksi]-fenil}-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((2S,6R)-2,6-dimetil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{(1S,4R)-4-[3-(4-aza-spiro[2.5]okt-4-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-3-{5-tert-butil-2-[3-(2-dimetilamino-etoksi)-fenil]-2H-pirazol-3-il}-urea;
1-[5-tert-butil-2-(3-morfolin-4-il-metil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-1-metil-pirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidronaftalen-1-il}-urea;
1-(5-tert-butil-2-{3-[(2-dimetilamino-etil)-metil-amino]-fenil}-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-((R)-2-dimetilamino-1-metil-etoksi)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-((S)-2-dimetilamino-1-metil-etoksi)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[2-[3-(2-dimetilamino-etoksi)-fenil]-5-(2-hidroksi-1,1-dimetil-etil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-pirolidin-1-il-etoksi)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-dietilamino-etoksi)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-morfolin-4-il-etoksi)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-piperidin-1-il-etoksi)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-{3-[2-(4-metil-piperazin-1-il)-etoksi]-fenil}-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-{3-[2-(4-fluoropiperidin-1-il)-etoksi]-fenil}-2H-pirazol-3-il}-3-{1S,4R)-4-[3-((S)-2-metilpiperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-{3-[2-(4-metil-[1,4]-diazepan-1-il)-etoksi]-fenil}-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-[1,4]oksazepan-4-il-etoksi)-fenil]-2H-pirazol-3-il}-3-{1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(2-{3-[2-(8-aza-biciklo[3.2.1]okt-8-il)-etoksi]-fenil}-5-tert-butil-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-{3-[2-(etil-metil-amino)-etoksi]-fenil}-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metilpiperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-(3-{2-[(2-metoksi-etil)-metil-amino]-etoksi}-fenil}-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-{3-[2-(4-metoksi-piperidin-1-il-etoksi]-fenil}-2H-pirazol-3-il)-3-(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-{3-[2-(3-oksa-8-aza-biciklo[3.2.1]okt-8-il)-etoksi]-fenil}-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(4-metoksi-piperidin-1-ilmetil)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metilpiperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(3-{[(2-metoksi-etil)-metil-amino]-metil}-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(4-fluor-piperidin-1-ilmetil)-fenil]-2H-pirazol-3-il}-3-{1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(3-dimetilaminometil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(3-pirolidin-1-ilmetil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{(1S,4R)-4-[3-(4-aza-spiro[2.5]okt-4-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-3-{5-tert-butil-2-[3-(2-morfolin-4-il-etoksi)-fenil]-2H-pirazol-3-il}-urea;
1-[5-tert-butil-2-(3-piperidin-1-ilmetil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(4-metil-[1,4]diazepan-1-ilmetil)-fenil]-2H-pirazol-3-il}-3-{1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-((1S,4S)-5-metil-2,5-diaza-biciklo[2.2.1]hept-2-ilmetil)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(4-morfolin-4-ilmetil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(4-dimetilaminometil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-15-tert-butil-2-[4-(4-metil-piperazin-1-ilmetil)-fenil]-2H-pirazol-3-il}-3-{1S,4R)-4-[3-((S)-2-metilpiperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[4-(4-metil-[1,4]diazepan-1-ilmetil)-fenil]-2H-pirazol-3-il}-3-{1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[4-(4-metoksi-piperidin-1-ilmetil)-fenil]-2H-pirazol-3-il}-3-{1S,4R)-4-[3-((S)-2-metilpiperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(4-pirolidin-1-ilmetil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(4-piperidin-1-ilmetil-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[4-(4-fluoro-piperidin-1-ilmetil)-fenil]-2H-pirazol-3-il}-3-{1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-(5-tert-butil-2-{4-[(etil-metil-amino)-metil]-fenil}-2H-pirazol-3-il)-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[5-tert-butil-2-(4-{[(2-metoksi-etil)-metil-amino]-metil}-fenil)-2H-pirazol-3-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(2-dimetilamino-etoksi)-fenil]-2H-pirazol-3-il-3-{(1S,4S)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidronaftalen-1-il]-urea;
1-[3-tert-butil-1’-(2-dimetilamino-etil)-1’H-[1,4’]bipirazolil-5-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-[3-tert-butil-1’-(2-morfolin-4-il-etil)-1’H-[1,4’]bipirazolil-5-il]-3-{(1S,4R)-4-[3-((S)-2-metil-piperidin-1-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
1-{5-tert-butil-2-[3-(4-metil-piperazin-1-ilmetil)-fenil]-2H-pirazol-3-il}-3-{(1S,4R)-4-[3-((S)-1-metilpirolidin-2-il)-[1,2,4]triazolo[4,3-a]piridin-6-iloksi]-1,2,3,4-tetrahidro-naftalen-1-il}-urea;
i odgovarajuće farmaceutski prihvatljive soli.
8. Farmaceutski pripravak koji sadržava spoj kao što je prijavljen u bilo kojem od prethodnih patentnih zahtjeva 1 do 7, zajedno s jednim ili više farmaceutski prihvatljivih nosača.
9. Spoj kao što je prijavljen u bilo kojem od patentnih zahtjeva 1 do 7 za upotrebu u liječenju bolesti i stanja koja se poboljšavaju inhibicijom aktivnosti p38 MAP kinaze.
10. Spojevi prema bilo kojem od patetnih zahtjeva 1 do 7 za upotrebu u liječenju bolesti ili stanja koja se poboljšavaju inhibicijom aktivnosti p38 MAP kinaze prema patentnom zahtjevu 9, naznačeno time da bolesti ili stanja jesu sljedeći: kronična eozinofilna upala pluća, astma, COPD, respiratorni distresni sindrom odraslih (ARDS), pogoršanje hiperaktivnosti dišnih puteva kao posljedica terapije s drugim lijekovima ili bolest dišnih puteva povezana s plućnom hipertenzijom.
11. Upotreba spoja kao što je prijavljen u bilo kojem od patentnih zahtjeva 1 do 7 u proizvodnji lijeka za liječenje bolesti ili stanja koja se poboljšavaju inhibicijom aktivnosti p38 MAP kinaze.
12. Upotreba prema patentnom zahtjevu 11, naznačeno time da bolest ili stanje jesu sljedeći: kronična eozinofilna upala pluća, astma, COPD, respiratorni distresni sindrom odraslih (ARDS), pogoršanje hiperaktivnosti dišnih puteva kao posljedica terapije s drugim lijekovima ili bolest dišnih puteva povezana s plućnom hipertenzijom.
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GB201214750D0 (en) | 2012-08-17 | 2012-10-03 | Respivert Ltd | Compounds |
WO2014033446A1 (en) | 2012-08-29 | 2014-03-06 | Respivert Limited | Kinase inhibitors |
WO2014033449A1 (en) | 2012-08-29 | 2014-03-06 | Respivert Limited | Kinase inhibitors |
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MX363950B (es) | 2013-04-02 | 2019-04-08 | Topivert Pharma Ltd | Derivados de urea utiles como inhibidores de quinasa. |
EP2981534B1 (en) | 2013-04-02 | 2017-07-19 | Topivert Pharma Limited | Kinase inhibitors based upon n-alkyl pyrazoles |
BR112015029504A2 (pt) * | 2013-06-06 | 2017-07-25 | Chiesi Farm Spa | inibidores quinase |
KR20160015221A (ko) * | 2013-06-06 | 2016-02-12 | 키에시 파르마슈티시 엣스. 피. 에이. | 키나아제 억제제 |
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