HRP20150868T1 - Derivati kinolina i kinoksalina kao inhibitori kinaze - Google Patents
Derivati kinolina i kinoksalina kao inhibitori kinaze Download PDFInfo
- Publication number
- HRP20150868T1 HRP20150868T1 HRP20150868TT HRP20150868T HRP20150868T1 HR P20150868 T1 HRP20150868 T1 HR P20150868T1 HR P20150868T T HRP20150868T T HR P20150868TT HR P20150868 T HRP20150868 T HR P20150868T HR P20150868 T1 HRP20150868 T1 HR P20150868T1
- Authority
- HR
- Croatia
- Prior art keywords
- pyrido
- trifluoroethyl
- quinolin
- pyrimidin
- compound according
- Prior art date
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- 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 14
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 10
- 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
- 150000003839 salts Chemical class 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 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
- OYRRZWATULMEPF-UHFFFAOYSA-N pyrimidin-4-amine Chemical compound NC1=CC=NC=N1 OYRRZWATULMEPF-UHFFFAOYSA-N 0.000 claims 6
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 5
- 125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000004739 (C1-C6) alkylsulfonyl 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
- 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
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 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
- 238000004519 manufacturing process Methods 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
- 230000003040 nociceptive 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
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 125000004171 alkoxy aryl group Chemical group 0.000 claims 1
- 125000000217 alkyl 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
- 229940079593 drug Drugs 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
- MTQFXNKSAGBBOZ-HXUWFJFHSA-N n-[(1r)-1-(8-chloro-2-pyrazin-2-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=CN=CC=N1 MTQFXNKSAGBBOZ-HXUWFJFHSA-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
- 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
- VZKOSMBWTLLPTL-NRFANRHFSA-N n-[(1s)-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-NRFANRHFSA-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
-
- 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
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Quinoline Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (38)
1. Spoj formule (I) ili njegov N-oksid, ili njegova farmaceutski prihvatljiva sol ili solvat:
[image]
pri čemu
U predstavlja -CF3, -CHF2 ili -CH2F;
Q predstavlja kisik, sumpor, N-R4 ili kovalentnu vezu;
Z predstavlja opcionalno supstituiranu bicikličnu heteroarilnu skupinu koja se sastoji od dva spojena šestočlana aromatična prstena, heteroarilna skupina Z sadrži najmanje jedan atom dušika te je za ostatak molekule vezana preko atoma ugljika;
M predstavlja arilnu ili heteroarilnu skupinu, od kojih svaka može biti opcionalno supstituirana s jednim ili više supstituenata;
W predstavlja C-R5 ili N;
R1, R2 i R3 neovisno predstavljaju vodik, 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 vodik ili C1-6 alkil; i
R5 predstavlja vodik, halogen, C1-6 alkil ili C1-6 alkoksi.
2. N-oksid derivat spoja formule (I) kako je definirano u patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol ili solvat.
3. Spoj prema patentnom zahtjevu 1 ili zahtjevu 2 naznačen time da U predstavlja -CF3.
4. Spoj prema zahtjevu 3 naznačen time da atom ugljika, za koji su –Q-Z i -CF3 skupine izravno vezane, ima (R) konfiguraciju.
5. Spoj prema bilo kojem od prethodnih patentnih zahtjeva naznačen time da Q predstavlja N-R4.
6. Spoj prema patentnom zahtjevu 5 naznačen time da R4 predstavlja vodik ili metil.
7. Spoj prema bilo kojem od prethodnih zahtjeva naznačen time da Z predstavlja kinolinil, izokinolinil, cinolinil, kinazolinil, kinoksalinil, ftalazinil, naftiridinil, pirido-pirimidinil ili pteridinil skupine koje su sve vezane za ostatak molekula preko atoma ugljika i od kojih svaka skupina može biti opcionalno supstituirana s jednim ili više supstituenata nezavisno izabranih od halogena, cijano, nitro, C1-6 alkila, trifluorometila, hidroksi, okso, C1-6 alkoksi, difluorometoksi, trifluorometoksi, C1-6 alkiltio , C1-6 alkilsulfinila, C1-6 alkilsulfonila, amino, C1-6 alkilamino, di(C1-6) alkilamino, arilamino, C1-6 alkoksiaril(C1-6)alkilamino, C2-6 alkilkarbonilamino, C2-6 alkoksikarbonilamino, C1-6 alkilsulfonilamino, formila, C2-6 alkilkarbonila, C3-6 cikloalkilkarbonila, C3-6 heterocikloalkilkarbonila, (C1-6)alkil-(C3-6) heterocikloalkilkarbonila, karboksi, C2-6 alkoksikarbonila, aminokarbonila, C1-6 alkilaminokarbonila, di(C1-6) alkilaminokarbonila, aminosulfonila, C1-6 alkilaminosulfonila i di(C1-6)alkilaminosulfonila.
8. Spoj prema patentnom zahtjevu 7 naznačen time da Z predstavlja pirido[3,2-d]-pirimidin-4-il.
9. Spoj prema bilo kojem od prethodnih patentnih zahtjeva naznačen time da 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 skupina može biti opcionalno supstituirana s jednim ili više supstituenata izabranih od halogena, cijano, nitro, C1-6 alkila, trifluorometila, hidroksi, C1-6 alkoksi, difluorometoksi, trifluorometoksi, C1-6 alkiltio, C1-6 alkilsulfinila, C1-6 alkilsulfonila, amino, C1-6 alkilamino, di(C1-6)alkilamino, C2-6 alkilkarbonilamino, C2-6 alkoksikarbonilamino, C1-6 alkilsulfonilamino, formila, C2-6 alkilkarbonila, karboksi, C2-6 alkoksikarbonila, aminokarbonila, C1-6 alkilaminokarbonila, di(C1-6)alkilaminokarbonila, aminosulfonila, C1-6 alkilaminosulfonila, di(C1-6)alkilamino sulfonila, C3-7cikloalkila, C3-6 heterocikloalkila, (C1-6)alkil(C3-6)heterocikloalkila, monocikličnog arila i monocikličnog heteroarila.
10. Spoj prema patentnom zahtjevu 9 naznačen time da M predstavlja fenil, piridinil ili pirazinil, od kojih svaka skupina može biti opcionalno supstituirana s jednim ili više supstituenata koji su nezavisno izabrani od halogena, C1-6 alkila i C1-6 alkoksi.
11. Spoj prema patentnom zahtjevu 10 naznačen time da M predstavlja piridinil.
12. Spoj prema patentnom zahtjevu 10 naznačen time da M predstavlja metilpiridinil.
13. Spoj prema bilo kojem od prethodnih zahtjeva naznačen time da W predstavlja C-R5.
14. Spoj prema patentnom zahtjevu 13 naznačen time da R5 predstavlja vodik.
15. Spoj prema bilo kojem od prethodnih patentnih zahtjeva naznačen time da R3 predstavlja vodik.
16. Spoj prema patentnom zahtjevu 1 predstavljen formulom (IIA); ili njegova farmaceutski prihvatljiva sol ili solvat:
[image]
pri čemu su R1 i R2 kako su definirani u zahtjevu 1;
X predstavlja N ili CH;
R16 i R17 neovisno predstavljaju vodik, halogen, cijano, C1-6 alkil, trifluorometil, amino, C1-6 alkilamino ili di(C1-6)alkilamino; i
R18 i R19 neovisno predstavljaju vodik, halogen, cijano, C1-6 alkil, trifluorometil ili aminokarbonil.
17. Spoj prema patentnom zahtjevu 16 naznačen time da R19 predstavlja vodik.
18. Spoj prema patentnom zahtjevu 17 predstavljen formulom (IIB) ili njegova farmaceutski prihvatljiva sol ili solvat:
[image]
Pri čemu su R1 i R2 kako su definirani u patentnom zahtjevu 1; i
X, R16, R17 i R18 su kako su definirani u patentnom zahtjevu 16.
19. Spoj prema bilo kojem od patentnih zahtjeva 16 do 18 naznačen time da X predstavlja N.
20. Spoj prema bilo kojem od patentnih zahtjeva 16 do 19 naznačen time da R16 predstavlja vodik.
21. Spoj prema bilo kojem od patentnih zahtjeva 16 do 20 naznačen time da R17 predstavlja vodik.
22. Spoj prema bilo kojem od patentnih zahtjeva 16 do 21 naznačen time da R18 predstavlja vodik ili C1-6 alkil.
23. Spoj prema patentnom zahtjevu 22 naznačen time da R18 predstavlja vodik.
24. Spoj prema patentnom zahtjevu 22 naznačen time da R18 predstavlja metil.
25. Spoj prema bilo kojem od prethodnih zahtjeva naznačen time da R1 predstavlja vodik, halogen, C1-6 alkil, trifluorometil ili C1-6 alkilsulfonil.
26. Spoj prema patentnom zahtjevu 25 naznačen time da R1 predstavlja kloro.
27. Spoj prema patentnom zahtjevu 25 naznačen time da R1 predstavlja trifluorometil.
28. Spoj prema bilo kojem od prethodnih patentnih zahtjeva naznačen time da R2 predstavlja vodik, halogen ili C1-6 alkil.
29. Spoj prema patentnom zahtjevu 28 naznačen time da R2 predstavlja vodik.
30. Spoj prema patentnom zahtjevu 1 izabran od sljedećeg:
N-{(R)-1-[8-kloro-2-(piridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin;
N-{(R)-1-[8-kloro-2-(1-oksipiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin;
N-[(R)-1-(8-kloro-2-fenilkinolin-3-il) -2,2,2-trifluoroetil] pirido[3,2-d] pirimidin-4-ilamin;
N-{(R)-1-[8-kloro-2-(4-metilpiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin;
N-{(R)-1-[8-kloro-2-(4-metil-1-oksipiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin;
N-{(R)-1-[8-kloro-2-(2-metilpiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin;
N-{(R)-1-[8-kloro-2-(2-metil-1-oksipiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin;
N-{(R)-1-[8-kloro-2-(5-metilpiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin;
N-{(R)-1-[8-kloro-2-(5-metil-1-oksipiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin;
N-{(R)-1-[8-kloro-2-(pirazin-2-il)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin;
N-{(R)-1-[8-kloro-2-(6-metoksipirazin-2-il)kinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin;
N-{(R)-1-[8-kloro-2-(6-metilpiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin;
N-{(R)-1-[8-kloro-2-(6-metil-1-oksipiridin-3-il)kinolin-3-y]]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin;
N-{(R)-1-[8-metil-2-(piridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-amin;
N-{(R)-1-[8-metil-2-(1-oksipiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin;
N-{(R)-1-[7-fluoro-8-metil-2-(piridin-3-il)kinolin-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)kinolin-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)kinolin-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)kinolin-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)kinolin-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)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin;
N-{(R)-1-[2-(piridin-3-il)-8-(trifluorometil)kinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin;
N-{(R)-1-[2-(1-oksipiridin-3-il)-8-(trifluorometil)kinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin;
N-{(R)-1-[2-(6-metilpiridin-3-il)-5,6,8-trifluorokinolin-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-trifluorokinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin;
N-{(R)-1-[8-kloro-2-(piridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}-N-metil-pirido[3,2-d]pirimidin-4-ilamin;
N-{(R)-1-[8-kloro-2-(piridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}-N-(1-oksipirido-[3,2-d]pirimidin-4-il)amin;
N-{(R)-1-[8-kloro-2-(1-oksipiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}-N-(1-oksi-pirido[3,2-d]pirimidin-4-il)amin;
N-{(S)-1-[8-kloro-2-(piridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin;
N-{(S)-1-[8-kloro-2-(1-oksipiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin;
N-{(R)-1-[2-(piridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin;
N-{(R)-1-[2-(1-oksipiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-amin ;
N-{(R)-1-[8-kloro-2-(6-kloropiridin-3-il)kinolin-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)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin;
N-{(R)-1-[8-(metansulfonil)-2-(2-metilpiridin-3-il)kinolin-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)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin; i
N-{(R)-1-[8-(metansulfonil)-2-(piridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin.
31. Spoj formule (I) kako je definirano u zahtjevu 1 ili njegov N-oksid ili njegova farmaceutski prihvatljiva sol ili solvat, za upotrebu u terapiji.
32. Spoj formule (I) kako je definirano u zahtjevu 1 ili njegov N-oksid ili njegova farmaceutski prihvatljiva sol ili solvat, za upotrebu u liječenju i/ili prevenciji poremećaja za koje je indicirana primjena selektivnog PI3K inhibitora.
33. Farmaceutski sastav koji sadrži spoj formule (I) kako je definirano u zahtjevu 1 ili njegov N-oksid ili njegova farmaceutski prihvatljiva sol ili solvat, zajedno s farmaceutski prihvatljivim nosačem.
34. Uporaba spoja formule (I) kako je definirano u zahtjevu 1 ili njegovog N-oksida ili njegove farmaceutski prihvatljive soli ili solvata, za proizvodnju lijeka za liječenje i/ili prevenciju poremećaja za koje je indicirana primjena selektivnog PI3K inhibitora.
35. N-{(R)-1-[8-Kloro-2-(1-oksipiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin prema patentnom zahtjevu 1.
36. N-{(R)-1-[8-Kloro-2-(1-oksipiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin prema zahtjevu 1, za upotrebu u liječenju i/ili prevenciji upalnih, autoimunih, kardiovaskularnih, neurodegenerativnih, metaboličkih, onkoloških, nociceptivnih ili oftalmičkih stanja.
37. Farmaceutski sastav prema patentnom zahtjevu 33 koji sadrži N-{(R)-1-[8-kloro-2-(1-oksipiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin zajedno s farmaceutski prihvatljivim nosačem.
38. Upotreba N-{(R)-1-[8-kloro-2-(1-oksipiridin-3-il)kinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamina za proizvodnju lijeka za liječenje i/ili prevenciju upalnih, autoimunih, kardiovaskularnih, neurodegenerativnih, metaboličkih, onkoloških, nociceptivnih ili oftalmičkih stanja.
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| GBGB1014963.1A GB201014963D0 (en) | 2010-09-08 | 2010-09-08 | Therapeutic agents |
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| EP20110755423 EP2614061B1 (en) | 2010-09-08 | 2011-09-02 | Quinoline and quinoxaline derivatives as kinase inhibitors |
| PCT/GB2011/051647 WO2012032334A1 (en) | 2010-09-08 | 2011-09-02 | Quinoline and quinoxaline derivatives as kinase inhibitors |
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| EP2427195B1 (en) | 2009-05-07 | 2019-05-01 | Intellikine, LLC | Heterocyclic compounds and uses thereof |
| ES2593256T3 (es) | 2010-05-21 | 2016-12-07 | Infinity Pharmaceuticals, Inc. | Compuestos químicos, composiciones y métodos para las modulaciones de cinasas |
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| UA115767C2 (uk) | 2011-01-10 | 2017-12-26 | Інфініті Фармасьютікалз, Інк. | Способи отримання ізохінолінонів і тверді форми ізохінолінонів |
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| ME03300B (me) | 2012-06-13 | 2019-07-20 | Incyte Holdings Corp | Supsтituisana triciklična jedinjenja као inhibiтori fgfr |
| US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
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| WO2008118454A2 (en) | 2007-03-23 | 2008-10-02 | Amgen Inc. | Derivatives of quinoline or benzopyrazine and their uses for the treatment of (inter alia) inflammatory diseases, autoimmune diseases or various kinds of cancer |
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| EP2499129B1 (en) | 2009-11-12 | 2014-07-30 | UCB Pharma, S.A. | Quinoline and quinoxaline derivatives as kinase inhibitors |
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