HRP20151430T1 - Derivati piridina i pirazina za lijeäśenje cistiäśne fibroze - Google Patents
Derivati piridina i pirazina za lijeäśenje cistiäśne fibroze Download PDFInfo
- Publication number
- HRP20151430T1 HRP20151430T1 HRP20151430TT HRP20151430T HRP20151430T1 HR P20151430 T1 HRP20151430 T1 HR P20151430T1 HR P20151430T T HRP20151430T T HR P20151430TT HR P20151430 T HRP20151430 T HR P20151430T HR P20151430 T1 HRP20151430 T1 HR P20151430T1
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- optionally substituted
- trifluoromethyl
- amino
- amide
- Prior art date
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- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 title 2
- 150000003216 pyrazines Chemical class 0.000 title 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 52
- 125000005843 halogen group Chemical group 0.000 claims 34
- 125000000217 alkyl group Chemical group 0.000 claims 27
- 125000005842 heteroatom Chemical group 0.000 claims 23
- 229910052760 oxygen Inorganic materials 0.000 claims 23
- 229910052717 sulfur Inorganic materials 0.000 claims 23
- 125000001424 substituent group Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 18
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 17
- 150000002367 halogens Chemical group 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 8
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 7
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 125000004043 oxo group Chemical group O=* 0.000 claims 5
- -1 R 14 Chemical compound 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims 3
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 3
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- UWWNIBQLEBYWJZ-UHFFFAOYSA-N 3-amino-5,6-bis(trifluoromethyl)pyridine-2-carboxylic acid Chemical compound NC1=CC(C(F)(F)F)=C(C(F)(F)F)N=C1C(O)=O UWWNIBQLEBYWJZ-UHFFFAOYSA-N 0.000 claims 2
- TZBFDPNSDFVMAL-UHFFFAOYSA-N 3-amino-6-(4-fluorophenyl)-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(O)(C)C(F)(F)F)=NC(C=2C=CC(F)=CC=2)=C1C(F)(F)F TZBFDPNSDFVMAL-UHFFFAOYSA-N 0.000 claims 2
- HZEFBJDLLZEVBS-UHFFFAOYSA-N 3-amino-6-(6-methylpyridin-3-yl)-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=NC(C)=CC=C1C1=NC(C(=O)NCC(C)(O)C(F)(F)F)=C(N)C=C1C(F)(F)F HZEFBJDLLZEVBS-UHFFFAOYSA-N 0.000 claims 2
- USHQRIKZLHNPQR-SNVBAGLBSA-N 3-amino-6-methoxy-n-[(2r)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NC[C@@](C)(O)C(F)(F)F)=C(N)C=C1C(F)(F)F USHQRIKZLHNPQR-SNVBAGLBSA-N 0.000 claims 2
- USHQRIKZLHNPQR-JTQLQIEISA-N 3-amino-6-methoxy-n-[(2s)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NC[C@](C)(O)C(F)(F)F)=C(N)C=C1C(F)(F)F USHQRIKZLHNPQR-JTQLQIEISA-N 0.000 claims 2
- 125000005915 C6-C14 aryl group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 230000036571 hydration Effects 0.000 claims 2
- 238000006703 hydration reaction Methods 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 230000000414 obstructive effect Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 210000002345 respiratory system Anatomy 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- WHFKKQOPYKKTRR-UHFFFAOYSA-N 3-amino-6-(1,3-oxazol-2-yl)-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(O)(C)C(F)(F)F)=NC(C=2OC=CN=2)=C1C(F)(F)F WHFKKQOPYKKTRR-UHFFFAOYSA-N 0.000 claims 1
- UFCJPGYFNTWEJU-UHFFFAOYSA-N 3-amino-6-(1-methylpyrazol-4-yl)-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=NN(C)C=C1C1=NC(C(=O)NCC(C)(O)C(F)(F)F)=C(N)C=C1C(F)(F)F UFCJPGYFNTWEJU-UHFFFAOYSA-N 0.000 claims 1
- KGUOYCPINMKTEY-UHFFFAOYSA-N 3-amino-6-(2,4-dichlorophenyl)-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(O)(C)C(F)(F)F)=NC(C=2C(=CC(Cl)=CC=2)Cl)=C1C(F)(F)F KGUOYCPINMKTEY-UHFFFAOYSA-N 0.000 claims 1
- QSUKHXHXEOGZBK-GFCCVEGCSA-N 3-amino-6-(4-chloro-2-methylphenyl)-n-[(2r)-3,3,3-trifluoro-2-hydroxypropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound CC1=CC(Cl)=CC=C1C1=NC(C(=O)NC[C@@H](O)C(F)(F)F)=C(N)C=C1C(F)(F)F QSUKHXHXEOGZBK-GFCCVEGCSA-N 0.000 claims 1
- GJQPKGWZJDQMIQ-UHFFFAOYSA-N 3-amino-6-(4-fluorophenyl)-n-(2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(C)(O)C)=NC(C=2C=CC(F)=CC=2)=C1C(F)(F)F GJQPKGWZJDQMIQ-UHFFFAOYSA-N 0.000 claims 1
- TZBFDPNSDFVMAL-OAHLLOKOSA-N 3-amino-6-(4-fluorophenyl)-n-[(2r)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NC[C@](O)(C)C(F)(F)F)=NC(C=2C=CC(F)=CC=2)=C1C(F)(F)F TZBFDPNSDFVMAL-OAHLLOKOSA-N 0.000 claims 1
- TZBFDPNSDFVMAL-HNNXBMFYSA-N 3-amino-6-(4-fluorophenyl)-n-[(2s)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NC[C@@](O)(C)C(F)(F)F)=NC(C=2C=CC(F)=CC=2)=C1C(F)(F)F TZBFDPNSDFVMAL-HNNXBMFYSA-N 0.000 claims 1
- SFKNCCQBPWDVKN-UHFFFAOYSA-N 3-amino-6-bromo-n-(1,3-dioxolan-2-ylmethyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NCC1OCCO1 SFKNCCQBPWDVKN-UHFFFAOYSA-N 0.000 claims 1
- GVRZCDPWQYZXNS-UHFFFAOYSA-N 3-amino-6-bromo-n-(2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound CC(C)(O)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N GVRZCDPWQYZXNS-UHFFFAOYSA-N 0.000 claims 1
- OPLNZGRSQIIIAO-UHFFFAOYSA-N 3-amino-6-bromo-n-(2-hydroxypropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound CC(O)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N OPLNZGRSQIIIAO-UHFFFAOYSA-N 0.000 claims 1
- ZYWMZMYAYYWCDE-UHFFFAOYSA-N 3-amino-6-bromo-n-(2-methoxyethyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COCCNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N ZYWMZMYAYYWCDE-UHFFFAOYSA-N 0.000 claims 1
- RIMPMQYAYQSIRX-UHFFFAOYSA-N 3-amino-6-bromo-n-(2-methyl-2-piperidin-1-ylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1CCCCN1C(C)(C)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N RIMPMQYAYQSIRX-UHFFFAOYSA-N 0.000 claims 1
- PRICOGDBMOXKKB-UHFFFAOYSA-N 3-amino-6-bromo-n-(2-morpholin-4-yl-2-phenylethyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NCC(C=1C=CC=CC=1)N1CCOCC1 PRICOGDBMOXKKB-UHFFFAOYSA-N 0.000 claims 1
- FKVGABLCWNRNCT-UHFFFAOYSA-N 3-amino-6-bromo-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound FC(F)(F)C(O)(C)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N FKVGABLCWNRNCT-UHFFFAOYSA-N 0.000 claims 1
- HMTZYEHOLZSQKH-UHFFFAOYSA-N 3-amino-6-bromo-n-(3,3,3-trifluoro-2-hydroxypropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NCC(O)C(F)(F)F HMTZYEHOLZSQKH-UHFFFAOYSA-N 0.000 claims 1
- IZNGGIWWUGSTJK-UHFFFAOYSA-N 3-amino-6-bromo-n-(3,3,3-trifluoro-2-methoxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC(C)(C(F)(F)F)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N IZNGGIWWUGSTJK-UHFFFAOYSA-N 0.000 claims 1
- FBKLGQNLLLOCOC-UHFFFAOYSA-N 3-amino-6-bromo-n-(3-methyl-2-oxobutyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound CC(C)C(=O)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N FBKLGQNLLLOCOC-UHFFFAOYSA-N 0.000 claims 1
- IXGCWTUELRQRAE-UHFFFAOYSA-N 3-amino-6-bromo-n-(oxolan-2-ylmethyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NCC1OCCC1 IXGCWTUELRQRAE-UHFFFAOYSA-N 0.000 claims 1
- VJSZJLMTQKHBKQ-UHFFFAOYSA-N 3-amino-6-bromo-n-[(2-methyloxolan-2-yl)methyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound N=1C(Br)=C(C(F)(F)F)C=C(N)C=1C(=O)NCC1(C)CCCO1 VJSZJLMTQKHBKQ-UHFFFAOYSA-N 0.000 claims 1
- FKVGABLCWNRNCT-SECBINFHSA-N 3-amino-6-bromo-n-[(2r)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound FC(F)(F)[C@@](O)(C)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N FKVGABLCWNRNCT-SECBINFHSA-N 0.000 claims 1
- FKVGABLCWNRNCT-VIFPVBQESA-N 3-amino-6-bromo-n-[(2s)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound FC(F)(F)[C@](O)(C)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N FKVGABLCWNRNCT-VIFPVBQESA-N 0.000 claims 1
- HMTZYEHOLZSQKH-YFKPBYRVSA-N 3-amino-6-bromo-n-[(2s)-3,3,3-trifluoro-2-hydroxypropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NC[C@H](O)C(F)(F)F HMTZYEHOLZSQKH-YFKPBYRVSA-N 0.000 claims 1
- KABJGLMCDHJSJB-UHFFFAOYSA-N 3-amino-6-bromo-n-[2-(4-fluorophenyl)-2-morpholin-4-ylethyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NCC(C=1C=CC(F)=CC=1)N1CCOCC1 KABJGLMCDHJSJB-UHFFFAOYSA-N 0.000 claims 1
- RZHBHISYYNDQRR-UHFFFAOYSA-N 3-amino-6-bromo-n-[2-(dimethylamino)-2-phenylethyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C=1C=CC=CC=1C(N(C)C)CNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N RZHBHISYYNDQRR-UHFFFAOYSA-N 0.000 claims 1
- CJMBGYUOORNPLR-UHFFFAOYSA-N 3-amino-6-bromo-n-[3,3,3-trifluoro-2-hydroxy-2-(trifluoromethyl)propyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NCC(O)(C(F)(F)F)C(F)(F)F CJMBGYUOORNPLR-UHFFFAOYSA-N 0.000 claims 1
- IXGCWTUELRQRAE-ZCFIWIBFSA-N 3-amino-6-bromo-n-[[(2r)-oxolan-2-yl]methyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NC[C@@H]1OCCC1 IXGCWTUELRQRAE-ZCFIWIBFSA-N 0.000 claims 1
- IXGCWTUELRQRAE-LURJTMIESA-N 3-amino-6-bromo-n-[[(2s)-oxolan-2-yl]methyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound NC1=CC(C(F)(F)F)=C(Br)N=C1C(=O)NC[C@H]1OCCC1 IXGCWTUELRQRAE-LURJTMIESA-N 0.000 claims 1
- JUKULCRENGDXKQ-UHFFFAOYSA-N 3-amino-6-cyclopropyl-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(O)(C)C(F)(F)F)=NC(C2CC2)=C1C(F)(F)F JUKULCRENGDXKQ-UHFFFAOYSA-N 0.000 claims 1
- QOLIZSVOBMCSPJ-NSHDSACASA-N 3-amino-6-ethoxy-n-[(2s)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound CCOC1=NC(C(=O)NC[C@](C)(O)C(F)(F)F)=C(N)C=C1C(F)(F)F QOLIZSVOBMCSPJ-NSHDSACASA-N 0.000 claims 1
- USHQRIKZLHNPQR-UHFFFAOYSA-N 3-amino-6-methoxy-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NCC(C)(O)C(F)(F)F)=C(N)C=C1C(F)(F)F USHQRIKZLHNPQR-UHFFFAOYSA-N 0.000 claims 1
- SGMQDTWKBCOQTJ-UHFFFAOYSA-N 3-amino-6-methoxy-n-(3,3,3-trifluoro-2-hydroxypropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NCC(O)C(F)(F)F)=C(N)C=C1C(F)(F)F SGMQDTWKBCOQTJ-UHFFFAOYSA-N 0.000 claims 1
- JLZLMMKWPPNUJJ-UHFFFAOYSA-N 3-amino-6-methoxy-n-[3,3,3-trifluoro-2-[(4-methoxyphenyl)methylamino]-2-methylpropyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=CC(OC)=CC=C1CNC(C)(C(F)(F)F)CNC(=O)C1=NC(OC)=C(C(F)(F)F)C=C1N JLZLMMKWPPNUJJ-UHFFFAOYSA-N 0.000 claims 1
- IGGKDUGORVNOGN-UHFFFAOYSA-N 3-amino-6-methoxy-n-[3,3,3-trifluoro-2-hydroxy-2-(trifluoromethyl)propyl]-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NCC(O)(C(F)(F)F)C(F)(F)F)=C(N)C=C1C(F)(F)F IGGKDUGORVNOGN-UHFFFAOYSA-N 0.000 claims 1
- HQGQMJKYAPMBRQ-UHFFFAOYSA-N 3-amino-6-pyridin-4-yl-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(O)(C)C(F)(F)F)=NC(C=2C=CN=CC=2)=C1C(F)(F)F HQGQMJKYAPMBRQ-UHFFFAOYSA-N 0.000 claims 1
- NMXSTLHGFBNGMD-UHFFFAOYSA-N 3-amino-6-pyrrolidin-1-yl-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound C1=C(N)C(C(=O)NCC(O)(C)C(F)(F)F)=NC(N2CCCC2)=C1C(F)(F)F NMXSTLHGFBNGMD-UHFFFAOYSA-N 0.000 claims 1
- VJOIAFQFVKJERR-UHFFFAOYSA-N 3-amino-n-(2-amino-3,3,3-trifluoro-2-methylpropyl)-6-methoxy-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NCC(C)(N)C(F)(F)F)=C(N)C=C1C(F)(F)F VJOIAFQFVKJERR-UHFFFAOYSA-N 0.000 claims 1
- POGTUVIIGKHISG-UHFFFAOYSA-N 3-amino-n-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound FC(F)(F)C(O)(C)CNC(=O)C1=NC=C(C(F)(F)F)C=C1N POGTUVIIGKHISG-UHFFFAOYSA-N 0.000 claims 1
- DOVVSHMLCFFGGB-SECBINFHSA-N 3-amino-n-[(2r)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5,6-bis(trifluoromethyl)pyridine-2-carboxamide Chemical compound FC(F)(F)[C@@](O)(C)CNC(=O)C1=NC(C(F)(F)F)=C(C(F)(F)F)C=C1N DOVVSHMLCFFGGB-SECBINFHSA-N 0.000 claims 1
- DOVVSHMLCFFGGB-VIFPVBQESA-N 3-amino-n-[(2s)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]-5,6-bis(trifluoromethyl)pyridine-2-carboxamide Chemical compound FC(F)(F)[C@](O)(C)CNC(=O)C1=NC(C(F)(F)F)=C(C(F)(F)F)C=C1N DOVVSHMLCFFGGB-VIFPVBQESA-N 0.000 claims 1
- CMFXZGDPYQFXMK-UHFFFAOYSA-N 3-amino-n-[2-hydroxy-3-methyl-2-(trifluoromethyl)butyl]-6-methoxy-5-(trifluoromethyl)pyridine-2-carboxamide Chemical compound COC1=NC(C(=O)NCC(O)(C(C)C)C(F)(F)F)=C(N)C=C1C(F)(F)F CMFXZGDPYQFXMK-UHFFFAOYSA-N 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940088710 antibiotic agent Drugs 0.000 claims 1
- 229940125715 antihistaminic agent Drugs 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 239000003434 antitussive agent Substances 0.000 claims 1
- 229940124584 antitussives Drugs 0.000 claims 1
- 229940124630 bronchodilator Drugs 0.000 claims 1
- 239000000168 bronchodilator agent Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000002713 epithelial sodium channel blocking agent Substances 0.000 claims 1
- DUZCWGDFTIWAOZ-UHFFFAOYSA-N methyl 3-[[3-amino-6-bromo-5-(trifluoromethyl)pyridine-2-carbonyl]amino]propanoate Chemical compound COC(=O)CCNC(=O)C1=NC(Br)=C(C(F)(F)F)C=C1N DUZCWGDFTIWAOZ-UHFFFAOYSA-N 0.000 claims 1
- 239000002357 osmotic agent Substances 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- 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
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Claims (18)
1. Spoj, naznačen time, da ima formulu I:
[image]
ili njegove farmaceutski prihvatljive soli, u kojoj:
A je N ili CR4a;
R1 je H; C1-C8 alkil opcijski supstituiran s jednim ili više atoma halogena; C2-C8 alkenil; C2-C8 alkinil; C3-C10 cikloalkil; C5-C10 cikloalkenil; -C1-C4 alkil-C3-C8 cikloalkil; C1-C8 alkoksi opcijski supstituiran s jednim ili više atoma halogena; halogen; SO2NR8R9; SO2R10; S-C1-C8 alkil opcijski supstituiran s jednim ili više atoma halogena; S-C6-C14 aril; CN; NR11R12; C(O)NR13R14; NR13SO2R15; NR13C(O)R15, CrO2R15, -(C0-C4 alkil)-C6-C14 aril; ili
-(C0-C4 alkil)- 3- do 14-člana heterociklička skupina, pri čemu se heterociklička skupina sastoji od najmanje jednog heteroatoma odabranog od N,O i S;
gdje je svaka od cikloalkilne, cikloalkenilne, arilne i heterocikličke skupine opcijski supstituirana s jednim ili više Z supstituenata;
R2 je C1-C4 haloalkil;
svaki od R3 i R4a je neovisno H ili C1-C8 alkil opcijski supstituiran s jednim ili više atoma halogena;
R4 je H, ili C1-C8 alkil opcijski supstituiran s jednim ili više halogena;
R5 je -(CH2)m-NR17R18, -(CH2)m-OR; C1-C8 alkoksi opcijski supstituiran s jednim ili više atoma halogena; -(C0-C4 alkil)-CO2R15-(C0-C4 alkil)-C6-C14 aril ili -3- do 14-člana heterociklička skupina, dok heterociklička skupina ima najmanje jedan heteroatom odabran od N, O i S; gdje su skupine -(C0-C4 alkil)-C6-C14 aril i -(C0-C4 alkil)-3- do 14-člana heterociklička skupina, svaka opcijski supstituirana s jednim ili više Z supstituenata;
R6 je C1-C8 alkil opcijski supstituiran s jednim ili više atoma halogena; C3-C10 cikloalkil; -C1-C4 alkil-C3-C8 cikloalkil; C1-C8 alkoksi opcijski supstituiran s jednim ili više atoma halogena; OH; CN; halogen; -(C0-C4 alkil)-C6-C14 aril; ili -(C0-C4 alkil)-3- do 14-člana heterociklička skupina, pri čemu heterociklička skupina sadrži najmanje jedan heteroatom odabran od N, O i S; gdje su skupine cikloalkilna, cikloalkenilna, -(C0-C4 alkil)-C6-C14 arilna i -(C0-C4 alkil)-3- do 14-člana heterociklička skupina, svaka opcijski supstituirana s jednim ili više Z supstituenata; ili R6 je H, i R5 je -(CH2)m-NR17R18, -(CH2)m-OR, C1-C8 alkoksi opcijski supstituiran s jednim ili više atoma halogena; -(C0-C4 alkil)-C6-C14 aril; -(C0-C4alkil)- 3- do 14-člana heterociklička skupina, dok heterociklička skupina sadrži najmanje jedan heteroatom odabran od N, O i S; ili -(C0-C4 alkil)-CO2R15, gdje su -(C0-C4 alkil)-C6-C14 aril i -(C0-C4 alkil)-3- do 14-člana heterociklička skupina,skupine koje su opcijski supstituirane s jednim ili više Z supstituenata; ili
R4 i R6 zajedno s atomima ugljika za koje su vezani, tvore 3- do 8-člani karbociklički sustav prstena; ili
R4 i R5 zajedno tvore okso skupinu (C=O) i R6 je C1-C4 alkil opcijski supstituiran s jednim ili više atoma halogena; C1-C4 alkoksi opcijski supstituiran s jednim ili više atoma halogena; -(C0-C4 alkil)-C6-C14 aril; ili -(C0-C4 alkil)-3- do 14-člana heterociklička skupina, dok heterociklička skupina sadrži najmanje jedan heteroatom odabran od N, O i S, pri čemu su svaka od arilne i heterocikličke skupine opcijski supstituirane s jednim ili više Z supstituenata; ili
R5 i R6 zajedno s atomima ugljika na koje su vezani, tvore 5- do 8-člani heterociklički sustav prstena koji sadrži jedan ili više heteroatoma odabranih od N, O i S, dok je sustav prstena opcijski supstituiran s jednim ili više Z supstituenata; ili
R4 i R5 i R6 zajedno s atomima ugljika na koje su vezani, tvore 5- do 8-člani heterociklički sustav prstena, koji sadrži jedan ili više heteroatoma odabranih od N, O i S, pri čemu je sustav prstena opcijski supstituiran s jednim ili više Z supstituenata;
R je H, ili C1-C8 alkil opcijski supstituiran s jednim ili više halogena;
m je 0, 1, 2 ili 3;
R8, R11, R13 i R17 su svaki neovisno H, C1-C8 alkil opcijski supstituiran s jednim ili više atoma halogena, C3-C10 cikloalkil ili -(C1-C4 alkil)-C3-C8 cikloalkil;
R9, R10, R12, R14, R15 i R18 su svaki neovisno H; C1-C8 alkil opcijski supstituiran s jednim ili više atoma halogena; C2-C8 alkenil; C2-C8 alkinil; C3-C10 cikloalkil; C5-C10 cikloalkenil; -C1-C4 alkil-C3-C8 cikloalkil; -(C0-C4 alkil)-C6-C14 aril; ili -(C0-C4 alkil)- 3- do 14-člana heterociklička skupina, pri čemu heterociklička skupina sadrži najmanje jedan heteroatom odabran od N, O i S, dok je svaka od cikloalkilne, cikloalkenilne, arilne i heterocikličke skupine opcijski supstituirana s jednim ili više Z supstituenata; ili
R8 i R9, R11 i R12, R13 i R14, te R17 i R18 zajedno s atomom dušika na kojega su priključeni, mogu tvoriti 4- do 14-članu heterocikličku skupinu opcijski supstituiranu s jednim ili više Z supstituenata;
Z je neovisno OH, aril, O-aril, benzil, O-benzil, C1-C6 alkil opcijski supstituiran s jednom ili više OH-skupina ili NH2-skupina, C1-C6 alkil opcijski supstituiran s jednim ili više atoma halogena, C1-C6 alkoksi opcijski supstituiran s jednom ili više OH-skupina ili C1-C4 alkoksi, NR18(SO2)R21, (SO2)NR19R21, (SO2)R21NR18C(O)R21, C(O)NR19R21, NR18C(O)NR19R21, NR18C(O)OR19, NR19R21, C(O)OR19, C(O)R19, SR19, OR19, okso, CN, NO2, halogen ili 3- do 14-člana heterociklička skupina, dok heterociklička skupina sadrži jedan ili više heteroatoma odabranih od N, O i S;
R19 i R21 su svaki neovisno H; C1-C8 alkil; C3-C8 cikloalkil; C1-C4 alkoksi-C1-C4 alkil; (C0-C4 alkil)-aril opcijski supstituiran s jednom ili više skupina odabranih od sljedećih: C1-C6 alkil, C1-C6 alkoksi i halogen; (C0-C4 alkil)-3- do 14-člana heterociklička skupina, heterociklička skupina uključujući jedan ili više heteroatoma odabranih od N, O i S, opcijski supstituiran s jednom ili više skupina odabranih od sljedećih: halogen, okso, C1-C6 alkil i C(O)C1-C6 alkil; (C0-C4 alkil)-O-aril opcijski supstituiran s jednom ili više skupina odabranih od sljedećih: C1-C6 alkil, C1-C6 alkoksi i halogen; i (C0-C4 alkil)-O- 3- do 14-člana heterociklička skupina, dok heterociklička skupina uključuje jedan ili više heteroatoma odabranih od N, O i S, opcijski supstituirana s jednom ili više skupina odabranih od sljedećih: halogen, C1-C6 alkil ili C(O)C1-C6 alkil; gdje su alkil-skupine opcijski supstituirane s jednim ili više atoma halogena, C1-C4 alkoksi, C(O)NH2, C(O)NHC1-C6 alkil ili C(O)N(C1-C6 alkil)2; ili
R19 i R21 zajedno s atomom dušika na kojega su priključeni, tvore 5- do 10-članu heterocikličku skupinu, dok heterociklička skupina uključuje jedan ili više dodatnih heteroatoma odabranih od N, O i S, gdje je heterociklička skupina opcijski supstituirana s jednim ili više supstituenata odabranih od sljedećih: OH; halogen; aril; 5- do 10-člana heterociklička skupina uključuje jedan ili više heteroatoma odabranih od N, O i S; S(O)2-aril; S(O)2-C1-C6 alkil; C1-C6 alkil opcijski supstituiran s jednim ili više atoma halogena; C1-C6 alkoksi opcijski supstituiran s jednom ili više OH-skupina ili C1-C4 alkoksi; i C(O)OC1-C6 alkil, dok su arilna i heterociklička skupina, supstituentske skupine koje su i same opcijski supstituirane sa sljedećima: C1-C6 alkil, C1-C6 haloalkil ili C1-C6 alkoksi.
2. Spoj prema zahtjevu 1, naznačen time, da A je CR4a.
3. Spoj prema zahtjevu 1 ili zahtjevu 2, naznačen time, da
R1 je C1-C8 alkil opcijski supstituiran s jednim ili više atoma halogena;
C1-C8 alkoksi opcijski supstituiran s jednim ili više atoma halogena; halogen; NR11R12, C6-C14 aril; ili -(C0-C4 alkil)-5- do 6-člana heterociklička skupina, gdje heterociklička skupina sadrži najmanje jedan heteroatom odabran od N, O i S, pri čemu je svaka od arilne i heterocikličke skupine opcijski supstituirana s jednim ili više Z supstituenata.
4. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da
R4 je H ili C1-C4 alkil opcijski supstituiran s jednim ili više atoma halogena;
R5 jeC1-C4 alkoksi opcijski supstituiran s jednim ili više atoma halogena; -(CH2)m-NR17R18, -(CH2)m-OR; ili -(C0-C4 alkil)-3- do 14-člana heterociklička skupina, dok heterociklička skupina sadrži najmanje jedan heteroatom odabran od N, O i S, pri čemu su heterocikličke skupine opcijski supstituirane s jednim ili više Z supstituenata; R6 je C1-C4 alkil opcijski supstituiran s jednim ili više atoma halogena; C1-C4 alkoksi opcijski supstituiran s jednim ili više atoma halogena; ili -(C0-C4 alkil)-C6-C14 aril, dok je aril opcijski supstituiran s jednim ili više Z supstituenata; ili
R4 i R6 zajedno s atomima ugljika na koje su vezani, tvore 3- do 6-člani karbociklički sustav prstena; ili
R5 i R6 zajedno s atomima ugljika na koje su vezani, tvore 5- do 8-člani heterociklički sustav prstena koji sadrži jedan ili više heteroatoma odabranih od N, O i S, gdje je sustav prstena opcijski supstituiran s jednim ili više Z supstituenata; m je 0 ili 1;
R17 i R18 su svaki neovisno H;
C1-C8 alkil opcijski supstituiran s jednim ili više atoma halogena.
5. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da A je CR4a;
R1 je C1-C4 alkil opcijski supstituiran s jednim ili više atoma halogena; ili C1-C4 alkoksi opcijski supstituiran s jednim ili više atoma halogena;
R2 je CF3;
R3 je H, CH3 ili CF3;
R4 je H ili Me;
R4a je H;
R5 je -NR17R18 ili OH, i
R6 je C1-C4 alkil opcijski supstituiran s jednim ili više atoma halogena.
6. Spoj, naznačen time, da je predstavljen formulom II,
[image]
ili njegova farmaceutski prihvatljiva sol, u kojoj
A je N ili CR4a;
R4a je H ili C1-C4 alkil;
R1 je C1-C8 alkil opcijski supstituiran s jednim ili više atoma halogena; C1-C8 alkoksi opcijski supstituiran s jednim ili više atoma halogena; halogen; NR11R12, C6-C14 aril;
ili -(C0-C4 alkil)- 5- do 6-člana heterociklička skupina, pri čemu heterociklička skupina sadrži najmanje jedan heteroatom odabran od N, O i S, dok je arilna i heterociklička skupina svaka opcijski supstituirana s jednim ili više Z supstituenata;
R3 je H ili CH3;
R101 je:
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R11 je H, C1-C8 alkil opcijski supstituiran s jednim ili više atoma halogena, C3-C10 cikloalkil ili -(C1-C4 alkil)-C3-C8 cikloalkil;
R12 i R18 su svaki neovisno H; C1-C8 alkil opcijski supstituiran s jednim ili više atoma halogena; C2-C8 alkenil; C2-C8 alkinil; C3-C10 cikloalkil; C5-C10 cikloalkenil; -C1-C4 alkil-C3-C8 cikloalkil; -(C0-C4 alkil)-C6-C14 aril; ili -(C0-C4 alkil)- 3- do 14-člana heterociklička skupina, dok heterociklička skupina sadrži najmanje jedan heteroatom odabran od N, O i S, gdje je svaka od cikloalkilne, cikloalkenilne, arilne i heterocikličke skupine opcijski supstituirana s jednim ili više Z supstituenata; ili
R11 i R12 zajedno s atomom dušika na kojega su priključeni, mogu tvoriti 4- do 14-članu heterocikličku skupinu opcijski supstituiranu s jednim ili više Z supstituenata;
Z je neovisno OH, aril, O-aril, benzil, O-benzil, C1-C6 alkil opcijski supstituiran s jednom ili više OH-skupina ili NH2-skupina, C1-C6 alkil opcijski supstituiran s jednim ili više atoma halogena, C1-C6 alkoksi opcijski supstituiran s jednom ili više OH-skupina ili C1-C4 alkoksi, NR18(SO2)R21, (SO2)NR19R21, (SO2)R21NR18C(O)R21, C(O)NR19R21, NR18C(O)NR19R21, NR18C(O)OR19, NR19R21, C(O)OR19, C(O)R19, SR19, OR19, okso, CN, NO2, halogen ili 3- do 14-člana heterociklička skupina, gdje heterociklička skupina sadrži najmanje jedan heteroatom odabran od N, O i S;
R19 i R21 su svaki neovisno H; C1-C8 alkil; C3-C8 cikloalkil; C1-C4 alkoksi-C1-C4 alkil; (C0-C4 alkil)-aril opcijski supstituiran s jednom ili više skupina odabranih od sljedećih: C1-C6 alkil, alkoksi i halogen; (C0-C4 alkil)-3- do 14-člana heterociklička skupina, gdje heterociklička skupina uključuje jedan ili više heteroatoma odabranih od N, O i S, opcijski supstituirana s jednom ili više skupina odabranih od sljedećih: halogen, okso, C1-C6 alkil i C(O)C1-C6 alkil; (C0-C4 alkil)-O-aril opcijski supstituiran s jednom ili više skupina odabranih od sljedećih: C1-C6 alkil, C1-C6 alkoksi i halogen; i (C0-C4 alkil)-O-3- do 14-člana heterociklička skupina, dok heterociklička skupina uključuje jedan ili više heteroatoma odabranih od N, O i S, opcijski supstituirana s jednom ili više skupina odabranih od sljedećih: halogen, C1-C6 alkil ili C(O)C1-C6 alkil;
pri čemu su alkilne skupine opcijski supstituirane s jednim ili više atoma halogena, C1-C4 alkoksi, C(O)NH2, C(O)NHC1-C6 alkil ili C(O)N(C1-C6 alkil)2; ili
R19 i R21 zajedno s atomom dušika na kojega su priključeni, tvore 5- do 10-članu heterocikličku skupinu, gdje heterociklička skupina uključuje jedan ili više dodatnih heteroatoma odabranih od N, O i S, dok je heterociklička skupina opcijski supstituirana s jednim ili više supstituenata odabranih od OH; halogen; aril; 5- do 10-člana heterociklička skupina koja uključuje jedan ili više heteroatoma odabranih od N, O i S; S(O)2-aril; S(O)2-C1-C6 alkil; C1-C6 alkil opcijski supstituiran s jednim ili više atoma halogena; C1-C6 alkoksi opcijski supstituiran s jednom ili više OH-skupina ili s C1-C4 alkoksi; i C(O)OC1-C6 alkil, gdje su arilna i heterociklička supstituenska skupina i same opcijski supstituirane sa sljedećima: C1-C6 alkil, C1-C6 haloalkil ili C1-C6 alkoksi.
7. Spoj prema zahtjevu 1, naznačen time, da je odabran od sljedećih:
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-(3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-(3,3,3-trifluoro-2-hidroksi-propil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-((S)-3,3,3- trifluoro-2-hidroksi-propil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-[(R)-1-(tetrahidro-furan-2-il)metil]-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-([1,3]dioksolan-2-ilmetil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-[(S)-1-(tetrahidrofuran-2-il)metil]-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-(tetrahidro-furan-2-ilmetil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-(2-metil-2-piperidin-1-il-propil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-(2-hidroksi-propil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-(2-hidroksi-2-metil-propil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-(2-metil-tetrahidrofuran-2-il-metil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-(2-metoksi-etil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-[2-(4-fluoro-fenil)-2-morfolin-4-il-etil]-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-(2-morfolin-4-il-2-fenil-etil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-(2-dimetilamino-2-fenil-etil)-amid;
3-amino-6-(4-fluoro-fenil)-5-trifluorometil-piridin-2-karboksilna kiselina-(3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-5-trifluorometil-piridin-2-karboksilna kiselina-(3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-6-(4-kloro-2-metiI-fenil)-5-trifluorometil-piridin-2-karboksilna kiselina-((R)-3,3,3-trifluoro-2-hidroksi-propil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-(3,3,3-trifluoro-2-hidroksi-2-trifluorometil-propil)-amid;
5-amino-6'-metil-3-trifluorometil-[2,3']bipiridinil-6-karboksilna kiselina-(3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-((R)-3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-((S)-3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-6-metoksi-5-trifluorometil-piridin-2-karboksilna kiselina-(3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-6-(4-fluoro-fenil)-5-trifluorometil-piridin-2-kaxboksilna kiselina-((S)-3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-6-(4-fluoro-feniI)-5-trifluorometil-piridin-2-karboksilna kiselina-((R)-3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-6-(2,4-dikloro-fenil)-5-trifluorometiI-piridin-2-karboksilna kiselina-(3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-6-(4-fluoro-fenil)-5-trifluorometil-piridin-2-karboksilna kiselina-(2-hidroksi-2-metil-propil)-amid;
3-amino-6-metoksi-5-trifluorometil-piridin-2-karboksilna kiselina-(3,3,3-trifluoro-2-hidroksi-propil)-amid;
S-amino-6'-metil-3-trifluorometil-[2,3']bipiridinil-6-karboksilna kiselina-(3,3,3-trifluoro-2-hidroksi-2-trifluorometil-propil)-amid;
5-amino-6'-metil-3-trifluorometil-[2,3']bipiridinil-6-karboksilna kiselina-(3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-5,6-bis-trifluorometil-piridin-2-karboksilna kiselina-((S)-3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-5,6-bis-trifluorometil-piridin-2-karboksilna kiselina-((R)-3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-6-metoksi-5-trifluorometil-piridin-2-karboksilna kiselina-((S)-3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
3-amino-6-metoksi-5-trifluorometil-piridin-2-karboksilna kiselina-((R)-3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid;
metil 3-(3-amino-6-bromo-5-(trifluorometil)pikolinamido)propanoat;
3-amino-6-(oksazol-2-il)-N-(3,3,3-trifluoro-2-hidroksi-2-metilpropil)-5-(trifluorometil)pikolinamid;
3-amino-6-bromo-N-(3,3,3-trifluoro-2-metoksi-2-metilpropil)-5-(trifluorometil)pikolinamid;
3-amino-N-(2-hidroksi-3-metil-2-(trifluorometil)butil)-6-metoksi-5-(trifluorometil)pikolinamid;
3-amino-6-ciklopropil-N-(3,3,3-trifluoro-2-hidroksi-2-metilpropil)-5-(trifluorometil)pikolinamid;
3-amino-6-metoksi-N-(3,3,3-trifluoro-2-hidroksi-2-(trifluorometil)propil)-5-(trifluorometil)pikolinamid;
5-amino-N-(3,3,3-trifluoro-2-hidroksi-2-metilpropil)-3-(trifluorometil)-2,4'-bipiridin-6-karboksamid;
3-amino-6-bromo-5-trifluorometil-piridin-2-karboksilna kiselina-(3-metil-2-okso-butil)-amid;
3-amino-6-(1-metil-1H-pirazol-4-il)-N-(3,3,3-trifluoro-2-hidroksi-2-metilpropil)-5-(trifluorometil)pikolinamid;
(S)-3-amino-6-etoksi-N-(3,3,3-trifluoro-2-hidroksi-2-metilpropil)-5-(trifluorometil)pikolinamid;
3-amino-6-(pirolidin-1-il)-N-(3,3,3-trifluoro-2-hidroksi-2-metilpropil)-5-(trifluorometil)pikolinamid;
3-amino-N-(2-amino-3,3,3-trifluoro-2-metilpropil)-6-metoksi-5-(trifluorometil)pikolinamid; i
3-amino-6-metoksi-N-(3,3,3-trifluoro-2-(4-metoksibenzilamino)-2-metilpropil)-5-(trifluorometil)pikolinamid;
ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema zahtjevu 7, naznačen time, da je to:
3-amino-6-metoksi-5-trifluorometil-piridin-2-karboksilna kiselina-((S)-3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid,
ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema zahtjevu 7, naznačen time, da je to:
3-amino-6-metoksi-5-trifluorometil-piridin-2-karboksilna kiselina-((R)-3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid,
ili njegova farmaceutski prihvatljiva sol.
10. Spoj prema zahtjevu 7, naznačen time, da je to:
3-amino-6-(4-fluoro-fenil)-5-trifluorometil-piridin-2-karboksilna kiselina-(3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid,
ili njegova farmaceutski prihvatljiva sol.
11. Spoj prema zahtjevu 7, naznačen time, da je to:
3-amino-5,6-bis-trifluorometil-piridin-2-karboksilna kiselina-((S)-(3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid,
ili njegova farmaceutski prihvatljiva sol.
12. Spoj prema zahtjevu 7, naznačen time, da je to:
3-amino-5,6-bis-trifluorometil-piridin-2-karboksilna kiselina-((R)-(3,3,3-trifluoro-2-hidroksi-2-metil-propil)-amid,
ili njegova farmaceutski prihvatljiva sol.
13. Spoj ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od zahtjeva 1 do 12, naznačen/a time, da se upotrebljava kao farmaceutsko sredstvo.
14. Spoj ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od zahtjeva 1 do 12, naznačena time, da se upotrebljava u liječenju upalne ili opstrukcijske bolesti dišnih puteva ili stanja kojima pogoduje mukozna hidratacija.
15. Spoj ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od zahtjeva 1 do 12, naznačen/a time, da se upotrebljava u liječenju cistične fibroze.
16. Uporaba spoja ili njegove farmaceutski prihvatljive soli, prema bilo kojem od zahtjeva 1 do 12, naznačena time, da je za proizvodnju lijeka koji se upotrebljava u liječenju upalne ili opstrukcijske bolesti dišnih puteva ili stanja kojima pogoduje mukozna hidratacija.
17. Farmaceutski sastav, naznačen time, da obuhvaća spoj ili njegovu farmaceutski prihvatljivu sol, prema bilo kojem od zahtjeva 1 do 12, i jedno ili više farmaceutski prihvatljivih pomoćnih sredstava.
18. Farmaceutska kombinacija, naznačena time, da obuhvaća:
prvi djelatni sastojak koji sadrži spoj ili njegovu farmaceutski prihvatljivu sol, prema bilo kojem od zahtjeva 1 do 12, i
drugi djelatni sastojak odabran od sljedećih: osmotska sredstva, ENaC-blokatori, protuupalna sredstva, bronhodilatorna sredstva, antihistaminska sredstva, antitusivna sredstva, antibiotici i ljekovite DNase-supstance, pri čemu prvi i drugi djelatni sastojci mogu biti u istom ili u drugačijem farmaceutskom sastavu.
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