DK3194376T3 - Pyridin-2(1h)-on quinolinon-derivater som mutant-isocitratdehydrogenase inhibitorer - Google Patents
Pyridin-2(1h)-on quinolinon-derivater som mutant-isocitratdehydrogenase inhibitorer Download PDFInfo
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- DK3194376T3 DK3194376T3 DK15778433.1T DK15778433T DK3194376T3 DK 3194376 T3 DK3194376 T3 DK 3194376T3 DK 15778433 T DK15778433 T DK 15778433T DK 3194376 T3 DK3194376 T3 DK 3194376T3
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
- A61K31/47—Quinolines; Isoquinolines
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Claims (18)
1. Forbindelse med formlen I:
eller farmaceutisk salt, enantiomer, hydrat, solvat, eller tautomer deraf, hvor: hver Wi og W2 er uafhængigt CH, CF eller N; W3 er uafhængigt, CR2 eller N; U er N eller CFte; A er valgt fra gruppen bestående af H, D, halogen, CN, -CHO, -COOH, -COOR, -C(O)NH2, -C(O)NHR, R'S(O)2-, -O(CH2)nC(O)R', R'S(O)-, heteroaryl, -SOMe, -SO2Me,
hvor X og Y er uafhængig i hver forekomst af C, N, NR', S, og O, forudsat at ringen indeholdende X og Y ikke kan have flere end 4 N- eller NH-atomer eller flere end et S- eller O-atom, og hvor S og O ikke er sammenhængende; R og R' ved hver forekomst er uafhængigt valgt fra gruppen bestående af H, OH, CN, -CH2CN, halogen, -NRyRs, CHCF2, CFs, Ci-Ce-alkyl, R7S(O)2-, C-i-Ce-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, Cs-Cs-cycloalkyl, C3-C8-cycloalkylalkyl, 3- til 8-leddet heterocyclyl, aryl, og heteroaryl, hvor hver R eventuelt er substitueret med en eller flere substituenter valgt fra gruppen
bestående af OH, halogen, C-i-Cs-alkoxy, NH2, R7S(O)2-, CN, C3-C8-cycloalkyl, 3- til 8-leddet heterocyclyl, aryl, heteroaryl, og R7S(O)-; Ri er uafhængigt OH, CN, halogen, CHCF2, CF3, Ci-Ce-alkyl, C-i-Cs-alkoxy, C2-C6-alkenyl, C2-C6-alkenyl, Cs-Cs-cycloalkyl, 3- til 8-leddet heterocyclyl, aryl, eller heteroaryl, hvor hver Ci-Ce-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, Cs-Cs-cycloalkyl, 3- til 8-leddet heterocyclyl, aryl, eller heteroaryl eventuelt er substitueret en eller flere gange med substituenter valgt fra gruppen bestående af halogen, OH, NH2, CN, Ci-Ce-alkyl, og C-i-Cs-alkoxy; hver R2 er uafhængigt H, OH, CN, halogen, CF3, CHF2, benzyl, Ci-Ce-alkyl, Ci-Ce-alkoxy, NH2, -O(CH2)nR', -O(CH2)nC(O)NHR', -O(CH2)nC(O)R', NHRy, -N(R7)(R8), NHC(O)Ry, NHS(O)R7, NHS(O)2R7, NHC(O)OR7, NHC(O)NHR7, -S(O)2NHR7, NHC(O)N(Rs)R7, OCH2R7, CHRR' eller OCHR'R7, hvor C1 -Ce-alkyl, Ci-Ce-alkoxy eventuelt er substitueret med en eller flere substituenter valgt fra gruppen bestående af C1 -Ce-alkyl, Ci-Cs-alkoxy, C2-Ce-alkenyl, C2-Ce-alkynyl, Cs-Cs-cycloalkyl, Cs-Cs-cycloalkyl substitueret med et eller flere af halogen, 3- til 8-leddet heterocyclyl, aryl, -heteroaryl-C(0)NH2, og heteroaryl; eller Ri og R2 kan indgå kemisk forbindelse med en C4-C6 cycloalkyl eller en 3- til 8- leddet heterocyclyl indeholdende mindst et atom valgt fra gruppen bestående af N, O, og S; R3 er H, Ci-Ce-alkyl, eller -OH; R4 og R5 er uafhængigt H, halogen, CH2OH, Ci-C3-alkyl, eller Ci-C3-alkyl substitueret med halogen, eller R4 og Rs når de indgår kemisk forbindelse med en Cs-Ce-cycloalkyl eller Cs-Ce-heterocyclyl; hver Rs er H, halogen, Ci-Cs-alkyl, Ci-Cs-alkyl substitueret med halogen, Ci-Ce-alkoxy, Ci-Ce-alkoxy substitueret med et eller flere af halogen, C2-C6-alkenyl, C2-Ce-alkynyl, Cs-Cs-cycloalkyl, 3- til 8-leddet heterocyclyl, aryl, eller heteroaryl; R7 og Rs er uafhængigt H, Ci-Cs-alkyl, Ci-Ce-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, C3-Cs-cycloalkyl, 3- til 8-leddet heterocyclyl, aryl, og heteroaryl; eller når R7 og Rs indgår en kemisk forbindelse kan de danne en 3- til 8-leddet heterocyclyl- eller heteroaryl ring; Rg er uafhængigt H, D, CD3, CF3, Ci-Cs-alkyl, C2-s-alkenyl, C3-s-alkynyl, C3-Cs-cycloalkyl, hvor alkyl, alkenyl, alkynyl, og cycloalkyl eventuelt er substitueret med amino, OH, halo, eller alkoxy; n er 0, 1, eller 2; og r er 0, 1, eller 2; med det forbehold at når A er H, så er Ri ikke Ci-Cs-alkyl eller Ci-Ce-alkoxy og Ri og R2 kan ikke indgå en kemisk forbindelse med en 3- til 8-leddet heterocyclyl.
2. Forbindelse ifølge krav 1, hvor A er CN, H eller F.
3. Forbindelse ifølge krav 2, hvor A er CN og U er N.
4. Forbindelse ifølge krav 1, hvor A er CN og R9 er H, Ci-C6-alkyl eller C3-C6- cycloalkyl.
5. Forbindelse ifølge krav 4, hvor R9 er methyl.
6. Forbindelse ifølge krav 1, hvor R3 er H, methyl eller ethyl.
7. Forbindelse ifølge krav 1, hvor: a) R4 og Rs er H; eller b) R4 er H og Rs er methyl; eller c) R4 og Rs er halogen; eller d) FU er F og Rs er methyl; eller e) R4 og Rs kan indgå en kemisk forbindelse med en C3-C5 cycloalkyl.
8. Forbindelse ifølge krav 1, hvor R4 er H og Rs er (S)-methyl
9. Forbindelse ifølge krav 1, hvor W1, W2, og W3 er CH, eller CF
10. Forbindelse ifølge krav 1, hvor W1 eller W3 er N.
11. Forbindelse ifølge krav 1, hvor Ri er halogen.
12. Forbindelse ifølge krav 11, hvor Ri er chlor.
13. Forbindelse ifølge krav 1, hvor: a) R2 er H, halogen, eller Ci-Ce alkoxy; eller b) R2 er Ci-Ce alkoxy substitueret med heteroaryl eller 3- til 8-leddet heterocyclyl.
14. Forbindelse ifølge krav 1 valgt fra gruppen bestående af: 5- {[(6-chlor-2-oxo-1,2-dihydroquinolin-3-yl)methyl]amino}-1-methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 6- chlor-3-{[( 1 -ethyl-2-oxo-1,2-dihydropyridin-3-yl)amino]methyl}-1,2-dihydroquinolin-2-on; 6-chlor-3-{[( 1 -methyl-2-oxo-1,2-dihydropyridin-3-yl)amino]methyl}-1,2-dihydroquinolin-2-on; 5-{[(6-chlor-2-oxo-1,2-dihydroquinolin-3-yl)methyl]amino}-6-oxo-1,6-dihydropyridin-2-carbonitril; 6-chlor-3-{[( 1 -cyclopropyl-2-oxo-1,2-dihydropyridin-3-yl)amino]methyl}-1,2-dihydroquinolin-2-on; 6-chlor-3-{[(1,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)amino]methyl}-1,2-dihydroquinolin-2-on; 3-{[(6-brom-2-oxo-1,2-dihydropyridin-3-yl)amino]methyl}-6-chlor-1,2-dihydroquinolin-2-on; 6-chlor-3-({[2-oxo-6-(trifluormethyl)-1,2-dihydropyridin-3-yl]amino}methyl)-1,2-dihydroquinolin-2-on; 6-chlor-3-({[1-methyl-2-oxo-6-(trifluoromethyl)-1,2-dihydropyridin-3-yl]amino}methyl)-1,2-dihydroquinolin-2-on; 6-chlor-7-methoxy-3-{[(1 -methyl-2-oxo-1,2-di hydropy ridi n-3- yl)amino]methyl}-1,2-dihydroquinolin-2-on; 6-chlor-3-{[(1-methyl-2-oxo-1,2-dihydropyridin-3-yl)amino]methyl}-7-(pyridin-2-ylmethoxy)-1,2-dihydroquinolin-2-on; 5-{[(1 S)-1 -(6-chlor-2-oxo-1,2-di hydroqui noli n-3-yl)ethyl]ami no}-1 -methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -(6-chlor-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino}-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-{[(1 R)-1 -(6-chlor-2-oxo-1,2-di hydroqu i nol i n-3-yl)ethyl]am i no}-1 -methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -(6-chlor-7-fluor-2-oxo-1,2-di hydroqu i nol i n-3-yl)ethyl]am i no}-1 -methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -(6-chlor-2-oxo-1,2-di hydroqui noli n-3-yl)ethyl]ami no}-1 -methyl-6-oxo-1,6-dihydropyrazin-2-carbonitril; 5-{[(1 R)-1 -(6-chlor-7-fluor-2-oxo-1,2-di hydroqu i nol i n-3-yl)ethyl]am i no}-1 -methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5- {[1 -(6-chlor-7-fluor-2-oxo-1,2-di hyd roqui noli n-3-yl)ethyl]ami no}-1 -methyl-
6- OXO-1,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -(6-chlor-7-methoxy-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino}-1 -methyl-6-oxo-1,6-di hydropyridi n-2-carbonitril; 5-{[(1 R)-1 -(6-chlor-7-methoxy-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino}-1 -methyl-6-oxo-1,6-di hydropyridi n-2-carbonitril; 5-{[1 -(6-chlor-7-methoxy-2-oxo-1,2-di hydroqu i nol i n-3-yl)ethyl]am i no}-1 -methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -[6-chlor-2-oxo-7-(pyridin-2-ylmethoxy)-1,2-dihydroquinolin-3-yl]ethyl]amino}-1-methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-{[(1 R)-1 -[6-chlor-2-oxo-7-(pyridin-2-ylmethoxy)-1,2-dihydroquinolin-3-yl]ethyl]amino}-1-methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-({1-[6-chlor-2-oxo-7-(pyridin-2-ylmethoxy)-1,2-dihydroquinolin-3-yl]ethyl}amino)-1-methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -{6-chlor-2-oxo-7-[(1 R)-1 - (py ridi n-2-yl)ethoxy]-1,2-dihydroqunolin-3-yl}ethyl]amino}-1-methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-[(1 S)-1 -[6-chlor-7-(cyclopropylmethoxy)-2-oxo-1,2-dihydroquinolin-3-yl]ethyl]amino}-1-methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -[6-chlor-2-oxo-7-(propan-2-yloxy)-1,2-dihydroquinolin-3-yl]ethyl]amino}-1-methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -(6-chlor-8-fluor-2-oxo-1,2-di hydroqu i nol i n-3-yl)ethyl]am i no}-1 -methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -(6-chlor-2-oxo-1,2-dihydro-1,8-naphthyridi n-3-yl)ethyl]ami no}-1 -methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5- {[(1 R)-1 -(7-chlor-3-oxo-3,4-dihydroquinoxalin-2-yl)ethyl]amino}-1 -methyl-
6- OXO-1,6-dihydropyridin-2-carbonitril; 5- {[(1 S)-1 -(7-chlor-3-oxo-3,4-dihydroquinoxalin-2-yl)ethyl]amino}-1 -methyl-
6- OXO-1,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -(6-chlor-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino}-6-oxo-1 -(trifluormethyl)-l ,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -[6-chlor-7-(2-hydroxypropan-2-yl)-2-oxo-1,2-dihydroquinolin-3-yl]ethyl]amino}-1-methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -(6-chlor-7-cyclopropyl-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl)ethyl]amino}-1-methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -{6-chlor-7-[(2-hydroxy-2-methylpropyl)amino]-2-oxo-1,2-dihydroquinolin-3-yl}ethyl]amino}-1-methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5-{[(1 S)-1 -[7-(azetidin-1 -yl)-6-chlor-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl]ethyl]amino}-1-methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 5- {[(1 S)-1 -[7-(azetidin-1 -yl)-6-chlor-2-oxo-1,2-dihydroquinolin-3-yl]ethyl]amino}-1-methyl-6-oxo-1,6-dihydropyridin-2-carbonitril; 6- chlor-3-[( 1 S)-1 -{[1 -methyl-2-oxo-6-(1 H-1,2,3,4-tetrazol-1 -yl)-1,2-dihydropyridin-3-yl]amino}ethyl]-1,2-dihydroquinolin-2-on; og 5-{[(1 S)-1 -(6-chlor-2-oxo-1,2-dihydroqunolin-3-yl)ethyl]amino}-1 -methyl-6-oxo-1,6-dihydropyridin-2-carboxamid.
15. Forbindelse ifølge krav 1, hvor forbindelsen er 5-{[(1S)-1-(6-chlor-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino}-1-methyl-6-oxo-1,6-dihydropyridin-2-carbonitril.
16. Forbindelse ifølge krav 1 med: a) formlen la:
eller b) formlen la-2:
eller c) formlen Ib:
17. Forbindelse ifølge krav 16 med: a) formlen la-1:
b) formlen lb-1:
18. Farmaceutisk sammensætning omfattende forbindelsen ifølge et hvilket som helst af kravene 1-17 og farmaceutisk acceptabel bærer.
Applications Claiming Priority (4)
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US201462053006P | 2014-09-19 | 2014-09-19 | |
US201562128089P | 2015-03-04 | 2015-03-04 | |
US201562150812P | 2015-04-21 | 2015-04-21 | |
PCT/US2015/051055 WO2016044789A1 (en) | 2014-09-19 | 2015-09-18 | Pyridin-2(1h)-one quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
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DK18198969.0T DK3447050T3 (da) | 2014-09-19 | 2015-09-18 | Pyridin-2(1h)-on-quinolinderivater som mutant-isocitrat dehydrogenaseinhibitorer |
DK15778433.1T DK3194376T3 (da) | 2014-09-19 | 2015-09-18 | Pyridin-2(1h)-on quinolinon-derivater som mutant-isocitratdehydrogenase inhibitorer |
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ES2768694T3 (es) | 2014-09-19 | 2020-06-23 | Forma Therapeutics Inc | Composiciones de quinolinona pirimidinas como inhibidores de isocitrato dehidrogenasa mutante |
CU20170029A7 (es) | 2014-09-19 | 2017-08-08 | Bayer Pharma AG | Indazoles sustituidos con bencilo en calidad de inhibidores de bub1, útiles para el tratamiento o profilaxis de una enfermedad hiperproliferativa y/o un trastorno que responde a la inducción de la muerte celular, un procedimiento para la preparación de estos compuestos, y compuestos intermediarios |
BR112017005238B1 (pt) | 2014-09-19 | 2023-01-17 | Forma Therapeutics, Inc | Derivados de piridin-2(1h)-ona quinolinona, seu uso e composição farmacêutica |
EP3201185B1 (en) | 2014-09-19 | 2018-11-21 | Forma Therapeutics, Inc. | Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
JP6820836B2 (ja) | 2014-09-19 | 2021-01-27 | フォーマ セラピューティクス,インコーポレイテッド | 変異イソクエン酸デヒドロゲナーゼ阻害剤としてのフェニルキノリノン誘導体 |
CA2971872C (en) | 2014-12-22 | 2023-10-10 | The United States Of America As Represented By The Secretary, Department Of Health And Human Services | Mutant idh1 inhibitors useful for treating cancer |
US10407419B2 (en) | 2015-04-21 | 2019-09-10 | Forma Therapeutics, Inc. | Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors |
WO2016171755A1 (en) | 2015-04-21 | 2016-10-27 | Forma Therapeutics, Inc. | Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
EP3619196B1 (de) | 2017-05-04 | 2022-03-30 | Bayer CropScience Aktiengesellschaft | 2-{[2-(phenyloxymethyl)pyridin-5-yl]oxy}-ethanamin-derivate und verwandte verbindungen als schädlingsbekämpfungsmittel z.b. für den pflanzenschutz |
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