DK2262807T3 - Hidtil ukendte tyrosinkinasehæmmere - Google Patents
Hidtil ukendte tyrosinkinasehæmmere Download PDFInfo
- Publication number
- DK2262807T3 DK2262807T3 DK09721981.0T DK09721981T DK2262807T3 DK 2262807 T3 DK2262807 T3 DK 2262807T3 DK 09721981 T DK09721981 T DK 09721981T DK 2262807 T3 DK2262807 T3 DK 2262807T3
- Authority
- DK
- Denmark
- Prior art keywords
- alkyl
- oxo
- mmol
- dihydropyridin
- ethyl
- Prior art date
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Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
- A61K31/435—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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Claims (18)
- HIDTIL UKENDTE TYROSINKINASEHÆMMERE Patentkrav1. Forbindelse med formel (I) eller en stereoisomer, en tautomer, et salt eller et hydrat deraf:hvor: R2 og R3 hver for sig er hydrogen, Cl-C6-alkyl, Cl-C6-alkoxy, halogen, cyano, Cl-C6-alkylamino eller di-(Cl-C6-alkyl)amino; W er O, S eller NRe, hvor Re er udvalgt blandt hydrogen eller Cl-C6-alkyl; eller W er binding af to hydrogenatomer til et carbonatom til frembringelse af en eventuelt substitueret methylengruppe:hvor Rf er udvalgt blandt hydrogen eller Cl-C6-alkyl; R4 erhvor Ra er eventuelt substitueret aryl eller heteroaryl; Rb er Cl-C6-alkyl, trifluormethyl, hydroxymethyl, methoxymethyl, aminomethyl, di-(Cl-C6-alkyl)aminomethyl eller heterocyclylaminomethyl; Rc er udvalgt blandt hydrogen, hydroxy, Cl-C6-alkoxy eller Cl-C6-alkyl; Rd er udvalgt blandt hydrogen eller Cl-C6-alkyl; og R1 er udvalgt uafhængigt blandt eventuelt substitueret heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl, heterocyclyloxyalkyl, heteroalkyl, heterocyclylaminoalkyl, aminoalkyl, Cl-C6-alkylaminoalkyl, di-(Cl-C6-alkyl)-aminoalkyl, aminocycloalkyl, alkylaminocycloalkyl, di-(Cl-C6-alkyl)-aminocycloalkyl, di-(Cl-C6-alkyl)-aminocycloalkylalkyl, hvor substituenterne er udvalgt blandt hydrogen, Cl-C6-alkyl, hydroxy, Cl-C6-alkoxy, amino, amidino, carboxamido, sulfonamido, hydroxy, cyano, primær, sekundær eller tertiær amino, halo, azido, Cl-C6-alkoxyalkyl, cyanoalkyl, azidoalkyl, haloalkyl, hydroxyalkyl, methansulfonylalkyl, primær, sekundær eller tertiær aminoalkyl, eventuelt substitueret aryl, heteroaryl, heteroalkyl, heterocyclyl, cycloalkyl, alkenyl og alkynyl.
- 2. Forbindelse ifølge krav 1, hvor R og R er hydrogen eller methyl.
- 3. Forbindelse ifølge krav 1, hvor W er binding af to hydrogenatomer til et carbonatom til frembringelse af methylen.
- 4. Forbindelse ifølge krav 1, hvor Ra er eventuelt substitueret thienyl eller phenyl, hvor de eventuelle substituenter er alkyl, alkoxy eller halo.
- 5. Forbindelse ifølge krav 1, hvor Ra er eventuelt substitueret thienyl eller phenyl, hvor de eventuelle substituenter er methyl, methoxy eller fluor.
- 6. Forbindelse ifølge krav 1, hvor Ra er 2-thienyl, phenyl, 3-methyl-2-thienyl, 2-methylphenyl, 5-fluor-2-methylphenyl, 5-fluor-2-methoxyphenyl, 2,3,5-trifluorphenyl eller 2,3,5,6-tetrafluorphenyl.
- 7. Forbindelse ifølge krav 1, hvor Rc og Rd er hydrogen eller hydroxy.
- 8. Forbindelse ifølge krav 1, hvor Rb er alkyl.
- 9. Forbindelse ifølge krav 1, hvor Rb er methyl.
- 10. Forbindelse ifølge krav 1, hvor R1 er udvalgt fra gruppen, der består af:hvor: R13 er udvalgt blandt hydrogen, Cl-C6-alkyl, heteroalkyl, heterocyclyl, cycloalkyl og heterocycloalkyl; R14 er udvalgt blandt hydrogen, hydroxy, Cl-C6-alkoxy, di-(Cl-C6-alkyl)amino, Cl-C6-alkyl, heteroalkyl, heterocyclyl, cycloalkyl, heterocycloalkyl, C1-C6-alkoxyalkyl, cyanoalkyl, azidoalkyl, nitroalkyl, ketoalkyl, methansulfonylalkyl, aminoalkyl, Cl-C6-alkylaminoalkyl, di-(Cl-C6-alkyl)aminoalkyl, eventuelt substitueret aryl, heteroaryl, arylalkyl og heteroarylalkyl; R15 er udvalgt blandt hydrogen, amino, Cl-C6-alkylamino, di-(Cl-C6-alkyl)amino, hydroxy, Cl-C6-alkoxy, heteroalkyl, Cl-C6-alkoxyalkyl, aminoalkyl, Cl-C6-alkylaminoalkyl og di-(Cl-C6-alkyl)aminoalkyl; a er et heltal fra 0 til 4; og t, u, v er uafhængige heltal fra 0 til 5.
- 11. Forbindelse ifølge krav 1, hvor R1 er udvalgt fra gruppen, der består af:
- 12. Forbindelse ifølge krav 1, hvor R'-methylenkæden mellem forbindelsen og heteroatomet eventuelt er substitueret med en eller flere hydrogen, Cl-C6-alkyl, hydroxy, hydroxy-Cl-C6-alkyl, Cl-C6-alkoxy, carboxamido eller sulfonamido.
- 13. Forbindelse ifølge krav 1, hvor R'-methylengrupperne eventuelt er substitueret med et heteroatom, der er udvalgt blandt O og S, NR***, S=0 eller S(=0)2, hvor R*** er udvalgt blandt hydrogen, hydroxy, Cl-C6-alkyl, C1-C6-alkoxy, heteroalkyl, hydroxyalkyl, aminoalkyl, Cl-C6-alkylaminoalkyl og di-(Cl-C6-alkyl)aminoalkyl.
- 14. Forbindelse ifølge krav 1, hvor R'-ringen eventuelt er substitueret med en Cl-C6-alkyl- eller heteroalkylgruppe.
- 15. Forbindelse ifølge krav 1 medfølgende formel (la):
- 16. Forbindelse ifølge krav 1, hvor forbindelsen er udvalgt fra gruppen, der består af:(lS,)-6-(l-methylpiperidin-4-yl)-2-(2-oxo-4-(l-(thiophen-2-yl)propan-2-ylamino)- l,2-dihydropyridin-3-yl)-6,7-dihydroimidazo[4,5-f]isoindol-5(3//)-on,2- (4-((\R,2S)-1 -hydroxy-1 -phenylpropan-2-ylamino)-2-oxo-1,2-dihydropyridin- 3- yl)-6-(3-(pyrrolidin-l-yl)propyl)-6,7-dihydroimidazo[4,5-f]isoindol-5(3//)-on,(3,)-2-(4-(l-(3-methylthiophen-2-yl)propan-2-ylamino)-2-oxo-l,2- dihydropyridin-3-yl)-6-(2-(pyrrolidin-l-yl)ethyl)-6,7-dihydroimidazo[4,5- /]isoindol-5(l//)-on,6-(2-((i?)-2-methylpyrrolidin-l-yl)ethyl)-2-(4-((lS,)-l-(3-methylthiophen-2- yl)propan-2-ylamino)-2-oxo-l,2-dihydropyridin-3-yl)-6,7-dihydroimidazo[4,5- /]isoindol-5(l//)-on,(5)-6-(2-(methyl(2-(methylsulfonyl)ethyl)amino)eth yl)-2-(4-( 1-(3- methylthiophen-2-yl)propan-2-ylamino)-2-oxo-l,2-dihydropyridin-3-yl)-6,7- dihydroimidazo[4,5-/]isoindol-5(3//)-on,(5)-2-(2-oxo-4-(l-otolylpropan-2-ylamino)-l,2-dihydropyridin-3-yl)-6-(2- (pyrrolidin-l-yl)ethyl)-6,7-dihydroimidazo[4,5-/]isoindol-5(l//)-on,(5)-6-(2-(dimethylamino)ethyl)-2-(4-(l-(5-fhior-2-methylphenyl)propan-2- ylamino)-2-oxo-l,2-dihydropyridin-3-yl)-6,7-dihydroimidazo[4,5-/]isoindol- 5(l//)-on,(5)-2-(4-( l-(5-fhior-2-methoxyphenyl)propan-2-ylamino)-2-oxo-1,2- dihydropyridin-3-yl)-6-(2-(pyrrolidin-l-yl)ethyl)-6,7-dihydroimidazo[4,5- /]isoindol-5(li7)-on,(5)-6-(2-(dimethylamino)ethyl)-2-(4-(l-(5-fhior-2-methoxyphenyl)propan-2- ylamino)-2-oxo-l,2-dihydropyridin-3-yl)-6,7-dihydroimidazo[4,5-/]isoindol- 5(li7)-on,(5)-2-(4-( l-(5-fhior-2-methylphenyl)propan-2-ylamino)-2-oxo-1,2- dihydropyridin-3-yl)-4-methyl-6-(2-(pyrrolidin-l-yl)ethyl)-6,7- dihydroimidazo[4,5-/]isoindol-5(l//)-on,(5)-6-(2-(dimethylamino)ethyl)-2-(2-oxo-4-(l-(2,3,5-trifhiorphenyl)propan-2- ylamino)-l,2-dihydropyridin-3-yl)-6,7-dihydroimidazo[4,5-/]isoindol-5(l//)-on,(S)-2-(2-oxo-4-(l-(2,3,5-trifhiorphenyl)propan-2-ylamino)-l,2-dihydropyridin-3- yl)-6-(2-(pyrrolidin-l-yl)ethyl)-6,7-dihydroimidazo[4,5-/]isoindol-5(l//)-on,2-(4-((S)-1 -(5-fhior-2-methylphenyl)propan-2-ylamino)-2-oxo-1,2- dihydropyridin-3-yl)-6-(2-((^)-2-methylpyrrolidin-l-yl)ethyl)-6,7- dihydroimidazo[4,5-/]isoindol-5(l//)-on,6-(2-((Æ)-2-methylpyrrolidin-l-yl)ethyl)-2-(2-oxo-4-((S)-l-(2,3,5- trifhiorphenyl)propan-2-ylamino)-l,2-dihydropyridin-3-yl)-6,7- dihydroimidazo[4,5-/]isoindol-5(li7)-on,(5)-2-(2-oxo-4-(l-(2,3,5,6-tetrafhiorphenyl)propan-2-ylamino)-l,2- dihydropyridin-3-yl)-6-(2-(pyrrolidin-l-yl)ethyl)-6,7-dihydroimidazo[4,5- /]isoindol-5(l//)-on og(5)-2-(4-( l-(5-fhior-2-methylphenyl)propan-2-ylamino)-2-oxo-1,2-dihydropyridin-3-yl)-6-(2-(methylamino)ethyl)-6,7-dihydroimidazo[4,5- /]isoindol-5(l//)-on.
- 17. Farmaceutisk præparat, der omfatter en forbindelse ifølge et hvilket som helst af kravene 1-16 og et eller flere farmaceutisk acceptable fortyndingsmidler, excipienser eller bærematerialer.
- 18. Forbindelse ifølge et hvilket som helst af kravene 1-16 til anvendelse til behandling eller forebyggelse af en tilstand eller forstyrrelse, der er forbundet med tyrosinkinaseaktivitet, hvor tilstanden eller forstyrrelsen er udvalgt fra gruppen, der består af ALK-positivt anaplastisk storcellet lymfom, en inflammatorisk myofibroblastisk tumor, diffust storcellet B-celle-non-Hodgkin-lymfom, ikke-småcellet lungecancer, øsofaguskarcinom, brystcancer, neuroblastom og glioblastom.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US3803208P | 2008-03-19 | 2008-03-19 | |
PCT/US2009/001691 WO2009117097A1 (en) | 2008-03-19 | 2009-03-18 | Novel tyrosine kinase inhibitors |
Publications (1)
Publication Number | Publication Date |
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DK2262807T3 true DK2262807T3 (da) | 2015-11-30 |
Family
ID=40814009
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK09721981.0T DK2262807T3 (da) | 2008-03-19 | 2009-03-18 | Hidtil ukendte tyrosinkinasehæmmere |
Country Status (9)
Country | Link |
---|---|
US (1) | US8815906B2 (da) |
EP (2) | EP2262807B1 (da) |
JP (2) | JP5628145B2 (da) |
CN (1) | CN102036990B (da) |
AU (1) | AU2009226153B2 (da) |
CA (1) | CA2718872C (da) |
DK (1) | DK2262807T3 (da) |
MX (1) | MX2010010272A (da) |
WO (1) | WO2009117097A1 (da) |
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-
2009
- 2009-03-18 AU AU2009226153A patent/AU2009226153B2/en not_active Ceased
- 2009-03-18 EP EP09721981.0A patent/EP2262807B1/en not_active Not-in-force
- 2009-03-18 WO PCT/US2009/001691 patent/WO2009117097A1/en active Application Filing
- 2009-03-18 CA CA2718872A patent/CA2718872C/en not_active Expired - Fee Related
- 2009-03-18 US US12/922,891 patent/US8815906B2/en not_active Expired - Fee Related
- 2009-03-18 DK DK09721981.0T patent/DK2262807T3/da active
- 2009-03-18 MX MX2010010272A patent/MX2010010272A/es active IP Right Grant
- 2009-03-18 CN CN200980118256.XA patent/CN102036990B/zh not_active Expired - Fee Related
- 2009-03-18 JP JP2011500801A patent/JP5628145B2/ja not_active Expired - Fee Related
- 2009-03-18 EP EP15177176.3A patent/EP2966076A1/en not_active Withdrawn
-
2013
- 2013-01-18 JP JP2013006922A patent/JP2013082744A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
US8815906B2 (en) | 2014-08-26 |
CA2718872A1 (en) | 2009-09-24 |
JP2013082744A (ja) | 2013-05-09 |
CN102036990A (zh) | 2011-04-27 |
JP5628145B2 (ja) | 2014-11-19 |
MX2010010272A (es) | 2011-05-25 |
US20130053376A1 (en) | 2013-02-28 |
CA2718872C (en) | 2016-09-13 |
AU2009226153A1 (en) | 2009-09-24 |
WO2009117097A1 (en) | 2009-09-24 |
EP2262807A1 (en) | 2010-12-22 |
EP2966076A1 (en) | 2016-01-13 |
EP2262807B1 (en) | 2015-08-12 |
AU2009226153B2 (en) | 2014-02-20 |
JP2011515397A (ja) | 2011-05-19 |
CN102036990B (zh) | 2015-09-30 |
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