DK2344474T3 - Picolinamidderivater som kinaseinhibitorer - Google Patents
Picolinamidderivater som kinaseinhibitorer Download PDFInfo
- Publication number
- DK2344474T3 DK2344474T3 DK09782396.7T DK09782396T DK2344474T3 DK 2344474 T3 DK2344474 T3 DK 2344474T3 DK 09782396 T DK09782396 T DK 09782396T DK 2344474 T3 DK2344474 T3 DK 2344474T3
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- DK
- Denmark
- Prior art keywords
- equiv
- added
- tert
- synthesis
- solution
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
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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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
-
- 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
- C07D401/02—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
-
- 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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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (15)
1. Forbindelse med formlen II eller en stereoisomer, en tautomer eller et farmaceutisk acceptabelt salt deraf, r5 Y H R“ X O Ri 5 II hvori Y er cyclohexyl, substitueret med en til tre substituenter, idet disse substituenter er valgt blandt hydroxyl, amino, Ci-4alkyl eller Ci-4halogenalkyl; Ri er hydrogen, NH2 eller halogen; 10 R12 indbyrdes uafhængigt er hydrogen eller halogen; og Rs er cyclohexyl, phenyl eller pyridyl, hvori cyclohexyl-, phenyl- og pyridylgrupperne indbyrdes uafhængigt er substitueret med op til tre substituenter valgt blandt halogen, hydroxyl, Ci-4alkyl og Ci^alkoxy.
2. Forbindelse med formlen II ifølge krav 1 valgt blandt yx Chiral > i CH j| ;; ; j*W r'r^F )6-(2,6-difluorphenyl)-5-fluor^N-(4-((1R,3S,5S)-3-hydroxy-5-I h N iTF ^methylcyclohexyl)pyridin-3-yl)picolinamid I rVv^ i I [ V c| ; OH Chiral ί i oh ,νη2Τ )N-(4-((1R,3R,4R,5S)-3-amino-4-hydroxy-5- F jX )methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluor-4- y h nF )hydroxyphenyl)-5-fluorpicolinamid iV °| i ^^^OHChiral : | HjC,, )N-(4-((1R,3R,4R,5S)-3-amino-4-hydroxy-5- i 3 F TF )methylcyclohexyl)pyridin-3-yl)-5-fluor-6-(2-fluor-5- å n XT )hydroxyphenyl)picolinamid ]_________O °_____________________________j______________________________________________________________________________________________________________________________________________________________i
i_____V ό 1 ............
___.................................................................i β-1
5- I 3- i )-1 )- i 6- I 3- I )-1
i h
i h i h K |c k i c c C k k k k
lid i
j Η
j( |ε C |li j h : F I F j F j F i f I F j F j F
I- ϊ
3. Forbindelse med formlen II ifølge krav 1, som er 3-amino-N-(4-((1 R,3S)-3-amino-cyclohexyl)pyridin-3-yl)-6-(2,6-difluorphenyl)-5-fluorpicolinamid med formlen i- i 1A
eller et farmaceutisk acceptabelt salt deraf.
4. Forbindelse med formlen II ifølge krav 1, som er N-(4-((1R,3R,4R,5S)-3-amino-4-
hydroxy-5-methylcyclohexyl' ~~ ' iyl)-5-fluorpicolinamid med formlen eller et farmaceutisk acceptabelt salt deraf.
5. Forbindelse med formlen II ifølge krav 1, som er N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorphenyl)-5-fluorpicolinamid med formen
eller et farmaceutisk acceptabelt salt deraf.
6. Forbindelse med formlen II ifølge krav 1, som er N-(4-((1R,3S)-3-aminocyclohexyl)-pyridin-3-yl)-6-(2,6-difluorphenyl)-5-fluorpicolinamid med formlen
eller et farmaceutisk acceptabelt salt deraf.
7. Forbindelse med formlen II ifølge krav 1, som er N-(4-((1R,3R,4S,5S)-3-amino-4-fluor-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorphenyl)-5-fluorpicolinamid med formlen
eller et farmaceutisk acceptabelt salt deraf.
8. Farmaceutisk sammensætning omfattende en forbindelse ifølge et hvilket som helst af kravene 1 til 7.
9. Farmaceutisk sammensætning omfattende en forbindelse ifølge et hvilket som helst af kravene 1 til 7, hvori den farmaceutiske sammensætning omfatter et yderligere middel til behandling af cancer.
10. Farmaceutisk sammensætning ifølge krav 9, hvori det yderligere middel er valgt blandt irinotecan, topotecan, gemcitabin, 5-fluoruracil, leucovorin, carboplatin, cisplatin, taxaner, tezacitabin, cyclophosphamid, vincaalkaloider, imatinib (Gleevec), anthra-cycliner, rituximab og trastuzumab.
11. Anvendelse af en forbindelse ifølge et hvilket som helst af kravene 1 til 7 til fremstilling af et medikament til behandling af en tilstand ved modulation af provirus-integration af Maloney-kinase-aktivitet (PIM-kinase aktivitet).
12. Anvendelse ifølge krav 11, ved hvilken tilstanden er en cancer valgt blandt carcinomer i lungerne, bugspytkirtlen, skjoldbruskkirtlen, ovarierne, blæren, brystet, prostata eller tyktarmen, melanomer, myeloid leukæmi, multipelt myelom og erythro-eukæmi, villøst colonadenom og osteosarcom.
13. Forbindelse ifølge et hvilket som helst af kravene 1 til 7 til anvendelse ved behandling af en tilstand ved modulation af provirus-integration af Maloney-kinase-aktivitet (PI M-kinase-aktivitet).
14. Forbindelse ifølge krav 13, hvor tilstanden er en cancer valgt blandt carcinomer i ungerne, bugspytkirtlen, skjoldbruskkirtlen, ovarierne, blæren, brystet, prostata eller tyktarmen, melanomer, myeloid leukæmi, multipelt myelom og erythroleukæmi, villøst colonadenom og osteosarcom.
15. Forbindelse ifølge et hvilket som helst af kravene 1 til 7 til anvendelse ved behandling af PIM-beslægtede lidelser i kombination med mindst et yderligere middel til behandling af cancer.
16. Terapeutisk sammensætning omfattende mindst en forbindelse ifølge et hvilket som helst af kravene 1 til 7 i kombination med ét eller flere yderligere midler til behandling af cancer.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US9366608P | 2008-09-02 | 2008-09-02 | |
US22566009P | 2009-07-15 | 2009-07-15 | |
PCT/EP2009/061205 WO2010026124A1 (en) | 2008-09-02 | 2009-08-31 | Picolinamide derivatives as kinase inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
DK2344474T3 true DK2344474T3 (da) | 2015-12-14 |
Family
ID=41228825
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK09782396.7T DK2344474T3 (da) | 2008-09-02 | 2009-08-31 | Picolinamidderivater som kinaseinhibitorer |
Country Status (39)
Country | Link |
---|---|
US (4) | US8329732B2 (da) |
EP (1) | EP2344474B1 (da) |
JP (2) | JP5412519B2 (da) |
KR (1) | KR101345920B1 (da) |
CN (3) | CN103333157A (da) |
AU (1) | AU2009289319C1 (da) |
BR (1) | BRPI0918268B1 (da) |
CA (1) | CA2734415C (da) |
CL (1) | CL2011000454A1 (da) |
CO (1) | CO6351725A2 (da) |
CR (1) | CR20110114A (da) |
DK (1) | DK2344474T3 (da) |
DO (1) | DOP2011000067A (da) |
EA (1) | EA020136B1 (da) |
EC (1) | ECSP11010859A (da) |
ES (1) | ES2551900T3 (da) |
GE (1) | GEP20135849B (da) |
HK (2) | HK1156627A1 (da) |
HN (1) | HN2011000629A (da) |
HR (1) | HRP20151410T1 (da) |
HU (1) | HUE026381T2 (da) |
IL (1) | IL211291A (da) |
MA (1) | MA32684B1 (da) |
ME (1) | ME01291A (da) |
MX (1) | MX2011002365A (da) |
MY (1) | MY150136A (da) |
NI (1) | NI201100052A (da) |
NZ (1) | NZ591449A (da) |
PE (1) | PE20110298A1 (da) |
PL (1) | PL2344474T3 (da) |
PT (1) | PT2344474E (da) |
RS (1) | RS54506B1 (da) |
SI (1) | SI2344474T1 (da) |
SM (1) | SMT201600005B (da) |
SV (1) | SV2011003849A (da) |
TW (1) | TWI434843B (da) |
UY (1) | UY32085A (da) |
WO (1) | WO2010026124A1 (da) |
ZA (1) | ZA201101118B (da) |
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