ME02203B - Hinolin i hinoksalin derivati kao inhibitori kinaza - Google Patents
Hinolin i hinoksalin derivati kao inhibitori kinazaInfo
- Publication number
- ME02203B ME02203B MEP-2015-120A MEP12015A ME02203B ME 02203 B ME02203 B ME 02203B ME P12015 A MEP12015 A ME P12015A ME 02203 B ME02203 B ME 02203B
- Authority
- ME
- Montenegro
- Prior art keywords
- pyrido
- trifluoroethyl
- quinolin
- pyrimidin
- compound according
- Prior art date
Links
- 125000001567 quinoxalinyl group Chemical class N1=C(C=NC2=CC=CC=C12)* 0.000 title claims 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 title 2
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 34
- 125000004548 quinolin-3-yl group Chemical group N1=CC(=CC2=CC=CC=C12)* 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 12
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 10
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 9
- OYRRZWATULMEPF-UHFFFAOYSA-N pyrimidin-4-amine Chemical compound NC1=CC=NC=N1 OYRRZWATULMEPF-UHFFFAOYSA-N 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 claims 6
- 150000001204 N-oxides Chemical class 0.000 claims 6
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 4
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 4
- -1 cinolinyl Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 claims 3
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 claims 3
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 3
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 3
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 3
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 3
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 150000001721 carbon Chemical group 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 3
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- 239000012828 PI3K inhibitor Substances 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 230000001363 autoimmune Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 230000002503 metabolic effect Effects 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 230000000626 neurodegenerative effect Effects 0.000 claims 2
- 230000000771 oncological effect Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 125000004171 alkoxy aryl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000001769 aryl amino group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- BYPOIZPQBUYOET-JOCHJYFZSA-N n-[(1r)-1-(8-chloro-2-phenylquinolin-3-yl)-2,2,2-trifluoroethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound C1([C@@H](NC=2C3=NC=CC=C3N=CN=2)C(F)(F)F)=CC2=CC=CC(Cl)=C2N=C1C1=CC=CC=C1 BYPOIZPQBUYOET-JOCHJYFZSA-N 0.000 claims 1
- IXIRZQBQJSZCOZ-JOCHJYFZSA-N n-[(1r)-1-(8-chloro-2-pyridin-3-ylquinolin-3-yl)-2,2,2-trifluoroethyl]-n-methylpyrido[3,2-d]pyrimidin-4-amine Chemical compound C1([C@@H](N(C)C=2C3=NC=CC=C3N=CN=2)C(F)(F)F)=CC2=CC=CC(Cl)=C2N=C1C1=CC=CN=C1 IXIRZQBQJSZCOZ-JOCHJYFZSA-N 0.000 claims 1
- VZKOSMBWTLLPTL-OAQYLSRUSA-N n-[(1r)-1-(8-chloro-2-pyridin-3-ylquinolin-3-yl)-2,2,2-trifluoroethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound C1([C@@H](NC=2C3=NC=CC=C3N=CN=2)C(F)(F)F)=CC2=CC=CC(Cl)=C2N=C1C1=CC=CN=C1 VZKOSMBWTLLPTL-OAQYLSRUSA-N 0.000 claims 1
- FZDKVHZRNGOTFF-JOCHJYFZSA-N n-[(1r)-1-[8-chloro-2-(2-methylpyridin-3-yl)quinolin-3-yl]-2,2,2-trifluoroethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound CC1=NC=CC=C1C1=NC2=C(Cl)C=CC=C2C=C1[C@H](C(F)(F)F)NC1=NC=NC2=CC=CN=C12 FZDKVHZRNGOTFF-JOCHJYFZSA-N 0.000 claims 1
- QTJPGBSSOQOAIE-JOCHJYFZSA-N n-[(1r)-1-[8-chloro-2-(4-methylpyridin-3-yl)quinolin-3-yl]-2,2,2-trifluoroethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound CC1=CC=NC=C1C1=NC2=C(Cl)C=CC=C2C=C1[C@H](C(F)(F)F)NC1=NC=NC2=CC=CN=C12 QTJPGBSSOQOAIE-JOCHJYFZSA-N 0.000 claims 1
- QKAZCOHRTUWMJE-JOCHJYFZSA-N n-[(1r)-1-[8-chloro-2-(5-methylpyridin-3-yl)quinolin-3-yl]-2,2,2-trifluoroethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound CC1=CN=CC(C=2C(=CC3=CC=CC(Cl)=C3N=2)[C@@H](NC=2C3=NC=CC=C3N=CN=2)C(F)(F)F)=C1 QKAZCOHRTUWMJE-JOCHJYFZSA-N 0.000 claims 1
- XYIFFGRMYFDNFK-OAQYLSRUSA-N n-[(1r)-1-[8-chloro-2-(6-chloropyridin-3-yl)quinolin-3-yl]-2,2,2-trifluoroethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound C1([C@@H](NC=2C3=NC=CC=C3N=CN=2)C(F)(F)F)=CC2=CC=CC(Cl)=C2N=C1C1=CC=C(Cl)N=C1 XYIFFGRMYFDNFK-OAQYLSRUSA-N 0.000 claims 1
- KGKWBHVBYQAASO-OAQYLSRUSA-N n-[(1r)-1-[8-chloro-2-(6-methoxypyrazin-2-yl)quinolin-3-yl]-2,2,2-trifluoroethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound COC1=CN=CC(C=2C(=CC3=CC=CC(Cl)=C3N=2)[C@@H](NC=2C3=NC=CC=C3N=CN=2)C(F)(F)F)=N1 KGKWBHVBYQAASO-OAQYLSRUSA-N 0.000 claims 1
- JJUXOACOOMIQPY-JOCHJYFZSA-N n-[(1r)-1-[8-chloro-2-(6-methylpyridin-3-yl)quinolin-3-yl]-2,2,2-trifluoroethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound C1=NC(C)=CC=C1C1=NC2=C(Cl)C=CC=C2C=C1[C@H](C(F)(F)F)NC1=NC=NC2=CC=CN=C12 JJUXOACOOMIQPY-JOCHJYFZSA-N 0.000 claims 1
- AVWZKDRUBYNBKS-OAQYLSRUSA-N n-[(1r)-2,2,2-trifluoro-1-(2-pyridin-3-ylquinolin-3-yl)ethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound C1([C@@H](NC=2C3=NC=CC=C3N=CN=2)C(F)(F)F)=CC2=CC=CC=C2N=C1C1=CC=CN=C1 AVWZKDRUBYNBKS-OAQYLSRUSA-N 0.000 claims 1
- KQDYBAFPEOMBNS-JOCHJYFZSA-N n-[(1r)-2,2,2-trifluoro-1-(7-fluoro-8-methyl-2-pyridin-3-ylquinolin-3-yl)ethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound N1=C2C(C)=C(F)C=CC2=CC([C@@H](NC=2C3=NC=CC=C3N=CN=2)C(F)(F)F)=C1C1=CC=CN=C1 KQDYBAFPEOMBNS-JOCHJYFZSA-N 0.000 claims 1
- GTAQXRQPCMCMER-JOCHJYFZSA-N n-[(1r)-2,2,2-trifluoro-1-(8-methyl-2-pyridin-3-ylquinolin-3-yl)ethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound N1=C2C(C)=CC=CC2=CC([C@@H](NC=2C3=NC=CC=C3N=CN=2)C(F)(F)F)=C1C1=CC=CN=C1 GTAQXRQPCMCMER-JOCHJYFZSA-N 0.000 claims 1
- ICIBONXBUUDLGI-JOCHJYFZSA-N n-[(1r)-2,2,2-trifluoro-1-(8-methylsulfonyl-2-pyridin-3-ylquinolin-3-yl)ethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound N1=C2C(S(=O)(=O)C)=CC=CC2=CC([C@@H](NC=2C3=NC=CC=C3N=CN=2)C(F)(F)F)=C1C1=CC=CN=C1 ICIBONXBUUDLGI-JOCHJYFZSA-N 0.000 claims 1
- OTXAAXUOFSGBPE-HSZRJFAPSA-N n-[(1r)-2,2,2-trifluoro-1-[2-(2-methylpyridin-3-yl)-8-methylsulfonylquinolin-3-yl]ethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound CC1=NC=CC=C1C1=NC2=C(S(C)(=O)=O)C=CC=C2C=C1[C@H](C(F)(F)F)NC1=NC=NC2=CC=CN=C12 OTXAAXUOFSGBPE-HSZRJFAPSA-N 0.000 claims 1
- IYSBCARDBXJRJP-OAQYLSRUSA-N n-[(1r)-2,2,2-trifluoro-1-[2-pyridin-3-yl-8-(trifluoromethyl)quinolin-3-yl]ethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound C1([C@@H](NC=2C3=NC=CC=C3N=CN=2)C(F)(F)F)=CC2=CC=CC(C(F)(F)F)=C2N=C1C1=CC=CN=C1 IYSBCARDBXJRJP-OAQYLSRUSA-N 0.000 claims 1
- LGHGTUQRWBOTFE-JOCHJYFZSA-N n-[(1r)-2,2,2-trifluoro-1-[5,6,8-trifluoro-2-(6-methylpyridin-3-yl)quinolin-3-yl]ethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound C1=NC(C)=CC=C1C1=NC2=C(F)C=C(F)C(F)=C2C=C1[C@H](C(F)(F)F)NC1=NC=NC2=CC=CN=C12 LGHGTUQRWBOTFE-JOCHJYFZSA-N 0.000 claims 1
- BIHZIJXESDDRSI-HSZRJFAPSA-N n-[(1r)-2,2,2-trifluoro-1-[7-fluoro-8-methyl-2-(2-methylpyridin-3-yl)quinolin-3-yl]ethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound CC1=NC=CC=C1C1=NC2=C(C)C(F)=CC=C2C=C1[C@H](C(F)(F)F)NC1=NC=NC2=CC=CN=C12 BIHZIJXESDDRSI-HSZRJFAPSA-N 0.000 claims 1
- ITBBAGFFVBMGPH-HSZRJFAPSA-N n-[(1r)-2,2,2-trifluoro-1-[7-fluoro-8-methyl-2-(5-methylpyridin-3-yl)quinolin-3-yl]ethyl]pyrido[3,2-d]pyrimidin-4-amine Chemical compound CC1=CN=CC(C=2C(=CC3=CC=C(F)C(C)=C3N=2)[C@@H](NC=2C3=NC=CC=C3N=CN=2)C(F)(F)F)=C1 ITBBAGFFVBMGPH-HSZRJFAPSA-N 0.000 claims 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000011593 sulfur Chemical group 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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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
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Ophthalmology & Optometry (AREA)
- Physical Education & Sports Medicine (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Quinoline Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (38)
1. Jedinjenje formule (I) ili njegov N-oksid, ili njegova farmaceutski prihvatljiva so ili solvat:gdeU predstavlja -CF3, -CHF2 ili -CH2F;Q predstavlja kiseonik, sumpor, N-R4 ili kovalentnu vezu;Z predstavlja opciono supstituisanu bicikličnu heteroaril grupu koja se sastoji od dva kuplovana šesto-člana aromatična prstena, heteroaril grupa Z sadrži najmanje jedan atom azota koji je za ostatak molekula vezan preko atoma ugljenika;M predstavlja aril ili heteroaril grupu, od kojih svaka može biti opciono supstituisana sa jednim ili više supstituenata;W predstavlja C-R5 ili N;R1, R2 i R3 nezavisno predstavljaju vodonik, halogen, cijano, nitro, C1-6 alkil, trifluorometil, C3-7 cikloalkil(C1-6)alkil, C3-7heterocikloalkil(C1-6)alkil, aril(C1-6)-alkil, heteroaril(C1-6)alkil, hidroksi, C1-6 alkoksi, difluorometoksi, trifluorometoksi, C1-6 alkiltio, C1-6 alkilsulfinil, C1-6 alkilsulfonil, amino, C1-6 alkilamino, di(C1-6)alkilamino, C2-6 alkilkarbonilamino, C2-6 alkoksikarbonilamino, C1-6 alkilsulfonilamino, formil, C2-6 alkilkarbonil, karboksi, C2-6 alkoksikarbonil, aminokarbonil, C1-6 alkilaminokarbonil, di(C1-6) alkilaminokarbonil, aminosulfonil, C1- 6 alkilaminosulfonil ili di(C1-6) alkilaminosulfonil;R4 predstavlja vodonik ili C1-6 alkil; iR5 predstavlja vodonik, halogen, C1-6 alkil ili C1-6 alkoksi.
2. N-oksid derivat jedinjenja formule (I) kako je definisano u patentnom zahtevu 1, ili njegova farmaceutski prihvatljiva so ili solvat.
3. Jedinjenje prema patentnom zahtevu 1 ili zahtevu 2, naznačeno time što U predstavlja -CF3.
4. Jedinjenje prema zahtevu 3, naznačeno time što atom ugljenika za koji su -KZ i -CF3 grupe direktno vezane, ima (R) konfiguraciju.
5. Jedinjenje prema bilo kojem od prethodnih patentnih zahteva naznačeno time što Q predstavlja N-R4.
6. Jedinjenje prema patentnom zahtevu 5 naznačeno time što R4 predstavlja vodonik ili metil.
7. Jedinjenje prema bilo kom od prethodnih zahteva naznačeno time što Z predstavlja hinolinil, izohinolinil, cinolinil, hinazolinil, hinoksalinil, ftalazinil, naftiridinil, pirido-pirimidinil ili pteridinil grupe koje su sve vezane za ostatak molekula preko atoma ugljenika, i od kojih svaka grupa može biti opciono supstituisana sa jednim ili više supstituenata nezavisno izabranih između: halogen, cijano, nitro, C1-6 alkil, trifluorometil, hidroksi, okso, C1-6 alkoksi, difluorometoksi, trifluorometoksi, C1-6 alkiltio , C1-6 alkilsulfinil, C1-6 alkilsulfonil, amino, C1-6 alkilamino, di(C1-6) alkilamino, arilamino, C1-6 alkoksiaril(C1-6)alkilamino, C2-6 alkilkarbonilamino, C2-6 alkoksi karbonilamino, C1-6 alkilsulfonilamino, formil, C2-6 alkilkarbonil, C3-6 cikloalkilkarbonil, C3-6 heterocikloalkilkarbonil, (C1-6)alkil-(C3-6) heterocikloalkilkarbonil, karboksi, C2-6 alkoksikarbonil, aminokarbonil, C1-6 alkilaminokarbonil, di(C1-6) alkilaminokarbonil, aminosulfonil, C1-6 alkilaminosulfonil i di(C1-6)alkilaminosulfonil.
8. Jedinjenje prema patentnom zahtevu 7, naznačeno time što Z predstavlja pirido[3,2-d]-pirimidin-4-il.
9. Jedinjenje prema bilo kojem od prethodnih patentnih zahteva naznačeno time što M predstavlja fenil, pirolil, furil, tienil, imidazolil, oksazolil, izoksazolil, tiazolil, izotiazolil, pirazolil, triazolil, oksadiazolil, tiadiazolil, piridinil, pirimidinil, piridazinil, pirazinil, tetrazolil ili triazinil, od kojih svaka grupa može biti opciono supstituisana sa jednim ili više supstituenata izabranih od: halogena, cijano, nitro, C1-6 alkil, trifluorometil, hidroksi, C1-6 alkoksi, difluorometoksi, trifluorometoksi, C1-6 alkiltio, C1-6 alkilsulfinil, C1-6 alkilsulfonil, amino, C1-6 alkilamino, di(C1-6)alkilamino, C2-6 alkilkarbonilamino, C2-6 alkoksikarbonilamino, C1-6 alkilsulfonilamino, formil, C2 -6 alkilkarbonil, karboksi, C2-6 alkoksikarbonil, aminokarbonil, C1-6 alkilaminokarbonil, di(C1-6)alkilaminokarbonil, aminosulfonil, C1-6 alkilaminosulfonil, di(C1-6)alkilamino sulfonil, C3-7cikloalkil, C3-6 heterocikloalkil, (C1-6)alkil(C3-6) heterocikloalkil, monociklični aril i monociklični heteroaril.
10. Jedinjenje prema patentnom zahtevu 9, naznačeno time što M predstavlja fenil, piridinil ili pirazinil, od kojih svaka grupa može biti opciono supstituisana sa jednim ili više supstituenata koji su nezavisno izabrani od: halogena, C1-6 alkil i C1-6 alkoksi.
11. Jedinjenje prema patentnom zahtevu 10 naznačeno time što M predstavlja piridinil.
12. Jedinjenje prema patentnom zahtevu 10 naznačeno time što M predstavlja metilpiridinil.
13. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time što W predstavlja C-R5.
14. Jedinjenje prema patentnom zahtevu 13, naznačeno time što R5 predstavlja vodonik.
15. Jedinjenje prema bilo kojem od prethodnih patentnih zahteva naznačeno time što R3 predstavlja vodonik.
16. Jedinjenje prema patentnom zahtevu 1 predstavljeno formulom (IIA); ili njegova farmaceutski prihvatljiva so ili solvat: gde su R1 i R2 kao što je definisano u zahtevu 1; X predstavlja N ili CH; R16 i R17 nezavisno predstavljaju vodonik, halogen, cijano, C1-6 alkil, trifluorometil, amino, C1-6 alkilamino ili di(C1-6)alkilamino; i R18 i R19 nezavisno predstavljaju vodonik, halogen, cijano, C1-6 alkil, trifluorometil ili aminokarbonil.
17. Jedinjenje prema patentnom zahtevu 16 naznačeno time što R19 predstavlja vodonik.
18. Jedinjenje prema patentnom zahtevu 17 predstavljeno formulom (IIb), ili njegova farmaceutski prihvatljiva so ili solvat gde su R1 i R2 kao što je definisano u patentnom zahtevu 1; i X, R16, R17 i R18 su kao što je definisano u patentnom zahtevu 16.
19. Jedinjenje prema bilo kojem od patentnih zahteva 16 do 18 naznačeno time što X predstavlja N.
20. Jedinjenje prema bilo kojem od patentnih zahteva 16 do 19 naznačeno time što R16 predstavlja vodonik.
21. Jedinjenje prema bilo kojem od patentnih zahteva 16 do 20 naznačeno time što R17 predstavlja vodonik.
22. Jedinjenje prema bilo kojem od patentnih zahteva 16 do 21 naznačeno time što R18 predstavlja vodonik ili C1-6 alkil.
23. Jedinjenje prema patentnom zahtevu 22, naznačeno time što R18 predstavlja vodonik.
24. Jedinjenje prema patentnom zahtevu 22, naznačeno time što R18 predstavlja metil.
25. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time što R1 predstavlja vodonik, halogen, C1-6 alkil, trifluorometil ili C1-6 alkilsulfonil.
26. Jedinjenje prema patentnom zahtevu 25, naznačeno time što R1 predstavlja hloro.
27. Jedinjenje prema patentnom zahtevu 25, naznačeno time što R1 predstavlja trifluorometil.
28. Jedinjenje prema bilo kojem od prethodnih patentnih zahteva naznačeno time što R2 predstavlja vodonik, halogen ili C1-6 alkil.
29. Jedinjenje prema patentnom zahtevu 28, naznačeno time što R2 predstavlja vodonik.
30. Jedinjenje prema patentnom zahtevu 1 izabrano od sledećeg: N-{(R)-1-[8-hloro-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-[(R)-1-(8-hloro-2-fenilhinolin-3-il) -2,2,2-trifluoroetil] pirido [3,2-d] pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(4-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(4-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(2-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(2-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(5-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(5-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(pyrazin-2-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(6-metoksipirazin-2-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(6-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[8-hloro-2-(6-metil-1-oksipiridin-3-il)hinolin-3-y]]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[8-metil-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-amin; N-{(R)-1-[8-metil-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(2-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(2-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(5-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(5-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; N-{(R)-1-[2-(piridin-3-il)-8-(trifluorometil)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[2-(1-oksipiridin-3-il)-8-(trifluorometil)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[2-(6-metilpiridin-3-il)-5,6,8-trifluorohinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[2-(6-metil-1-oksipiridin-3-il)-5,6,8-trifluorohinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; N-{(R)-1-[8-hloro-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-N-metil-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-N-(1-oksipirido-[3,2-d]pirimidin-4-il) amin; N-{(R)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-N-(1-oksi-pirido[3,2-d]pirimidin-4-il)amin; N-{(S)-1-[8-hloro-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-{(S)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-{(R)-1-[2-(piridin-3-il) hinolin-3-il]-2,2,2-trifluoroetil} pirido [3,2-d] pirimidin-4-amin; N-{(R)-1-[2-(1-oksipiridin-3-il) hinolin-3-il] -2,2,2-trifluoroetil} pirido [3,2-d] -pirimidin-4-amin ; N-{(R)-1-[8-hloro-2-(6-hloropiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[2-(2-metil-1-oksipiridin-3-il)-8-(trifluorometil)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; N-{(R)-1-[8-(Metansulfonil)-2-(2-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin -4-amin; N-{(R)-1-[8-(metansulfonil)-2-(2-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; i N-{(R)-1-[8-(metansulfonil)-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin.
31. Jedinjenje formule (I) kako je definisano u zahtevu 1 ili njegov N-oksid, ili njegova farmaceutski prihvatljiva so ili solvat, za upotrebu u terapiji.
32. Jedinjenje formule (I) kako je definisano u zahtevu 1 ili njegov N-oksid, ili njegova farmaceutski prihvatljiva so ili solvat, za upotrebu u lečenju i/ili prevenciji poremećaja za koje je indikovna administracija selektivnog PI3K inhibitora.
33. Farmaceutska kompozicija koja sadrži jedinjenje formule (I) kako je definisano u zahtevu 1 ili njegov N-oksid, ili njegovu farmaceutski prihvatljivu so ili solvat, zajedno sa farmaceutski prihvatljivim nosačem.
34. Upotreba jedinjenja formule (I) kako je definisano u zahtevu 1 ili njegovog N-oksida, ili njegove farmaceutski prihvatljive soli ili solvata, za proizvodnju medikamenta za lečenje i/ili prevenciju poremećaja za koje je indikovana administracija selektivnog PI3K inhibitora.
35. N-{(R)-1-[8-Hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-il amin prema patentnom zahtevu 1.
36. N-{(R)-1-[8-Hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin prema zahtevu 1, za upotrebu u lečenju i/ili prevenciji zapaljenskih, autoimunih, kardiovaskularnih, neurodegenerativnih, metaboličkih, onkoloških, noiceptivnih ili oftalmičkih stanja.
37. Farmaceutska kompozicija prema patentnom zahtevu 33, koja sadrži N-{(R)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin zajedno sa farmaceutski prihvatljivim nosačem.
38. Upotreba N-{(R)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-ilamina za proizvodnju medikamenta za lečenje i/ili prevenciju inflamatornih, autoimunih, kardiovaskularnih, neurodegenerativnih, metaboličkih, onkoloških, noiceptivnih ili oftalmičkih stanja. 2
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| HRP20160350T1 (hr) * | 2007-03-23 | 2016-05-06 | Amgen Inc. | Heterociklički spojevi i njihove uporabe |
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