ME02373B - Biciklična heterociklična jedinjenja kao inhibitori protein tirozin kinaze - Google Patents
Biciklična heterociklična jedinjenja kao inhibitori protein tirozin kinazeInfo
- Publication number
- ME02373B ME02373B MEP-2016-3A MEP316A ME02373B ME 02373 B ME02373 B ME 02373B ME P316 A MEP316 A ME P316A ME 02373 B ME02373 B ME 02373B
- Authority
- ME
- Montenegro
- Prior art keywords
- alkyl
- heterocyclyl
- compound according
- groups
- independently represent
- Prior art date
Links
- 125000002618 bicyclic heterocycle group Chemical group 0.000 title 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 14
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000006553 (C3-C8) cycloalkenyl group Chemical group 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004674 methylcarbonyl group Chemical group CC(=O)* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 238000011282 treatment Methods 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (14)
1.Jedinjenje formule (I): pri čemu predstavlja jednostruku ili dvostruku vezu, tako da je najmanje jedna veza u 5-članom prstenastom sistemu dvostruka veza; prsten A može biti opciono supstituisan sa 1, 2 ili 3 Ra grupe; R4 i R5 nezavisno predstavljaju vodonik, alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, C1-6 alkanol, haloC1-6 alkil, -(CH2)n-NRxRy, -(CH2)S-COORz, -(CH2)n-0-(CH2)m-0H, -(CH2)n-aril, -(CH2)n-0-aril, -(CH2)n-heterociklil ili - (CH2)n-0-heterociklil, pri čemu pomenute alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, aril i heterociklil grupe mogu biti opciono supstituisane sa 1, 2 ili 3 Ra grupe; Rx, Ry i Rz nezavisno predstavljaju vodonik, alkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkanol, -COOC1-6 alkil, hidroksi, C1-6 alkoksi, haloC1-6 alkil, -CO-(CH2)n-C1-6 alkoksi, alkilamino, C3-8 cikloalkil ili C3-8 cikloalkenil; R2 predstavlja -CONR7R8 ili -CORx grupu; R7 i R8 nezavisno predstavljaju vodonik, alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, aril, heterociklil ili R7 i R8 zajedno sa atomom azota za koji su pričvršćeni mogu obrazovati heterociklil prsten koji sadrži azot, pri čemu pomenuti C1-6 alkil, aril i heterociklil može biti opciono supstituisan sa 1, 2 ili 3 Rb grupe; Ra predstavlja halogen, alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, -ORx, -0-(CH2)n-0Rx, haloC1-6 alkil, haloC1-6 alkoksi, alkanol, =0, =S, nitro, Si(Rx)4, -(CH2)S-CN, -S-Rx, -SORx, -S02-Rx, -CORx, -(CRxRy)s-COORz, - (CH2)s-CONRxRy, -(CH2)s-NRxRy, -(CH2)s-NRxCORy, -(CH2)S-NRxS02-Ry, -(CH2)s-NH-S02-NRxRy, -OCONRxRy, -(CH2)s-NRxC02Ry, -O-(CH2)s-CRxRy-(CH2)rORz ili -(CH2)s-S02NRxRy grupe; Rb predstavlja Ra grupu ili -Y-karbocikličnu ili -Z-heterociklil grupu, pri čemu pomenute karbociklične i heterociklil grupe mogu biti opciono supstituisane sa 1, 2 ili 3 Ra grupe; Y i Z nezavisno predstavljaju vezu, -CO-(CH2)s-, -COO-, -(CH2)n-, -NRX-(CH2)S-, -(CH2)s-NRx-, -CONRx-, -NRxCO-, -S02NRx-, -NRxS02-, -NRxCONRy-, -NRxCSNRy-, - 0-(CH2)s-, -(CH2)s-0-, -S-, -SO- ili -(CH2)s-S02-; m i n nezavisno predstavljaju ceo broj od 1-4; s i t nezavisno predstavljaju ceo broj od 0-4; ili njegova farmaceutski prihvatljiva so ili solvat.
2.Jedinjenje prema zahtjevu 1, pri čemu R1 i R5 nezavisno predstavljaju vodonik, alkil, alkanol, -(CH2)n-NRxRy, -(CH2)n-aril ili haloC1-6 alkil; Rx, Ry i Rz nezavisno predstavljaju vodonik, alkil, alkanol, hidroksi, alkoksi, haloC1-6 alkil ili -CO-(CH2)n-C1-6 alkoksi; Ra predstavlja halogen, alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, -0RX, -0-(CH2)n-0Rx, haloC1-6 alkil, haloC1-6 alkoksi, C1-6 alkanol, =0, =S, nitro, -(CH2)s-CN, -S-Rx, -SO-Rx, -S02-Rx, -CORx, -(CRxRy)s-COORz, -(CH2)S-CONRxRy, -(CH2)s-NRxRv, -(CH2)s-NRxCORy, -(CH2)s-NRxS02-Ry, -OCONRxRy, -(CH2)s-NRxC02Ry, -0-(CH2)s-CRxRy-(CH2), -0Rz ili -(CH2)s-S02NRxRy grupe; Rb predstavlja -Y-karbocikličnu ili -Z-heterociklil grupu, pri čemu pomenute karbociklične i heterociklil grupe mogu biti opciono supstituisane sa 1, 2 ili 3 Ra grupe; Y i Z nezavisno predstavljaju vezu, CO, -(CH2)n-, -NRx-(CH2)n-, -O- ili -0-(CH2)s-.
3. Jedinjenje prema zahtjevu 1 pri čemu je jedan od R4 i R5 vodonik, a drugi je -CH2CF3 ili -CH2CH3.
4. Jedinjenje prema bilo kom od prethodnih zahtjeva, pri čemu R2 predstavlja -CONR7R8 grupu.
5. Jedinjenje prema zahtjevu 4, pri čemu i R7 i R8 predstavljaju vodonik ili C1-6 alkil; ili jedan od R7 i R8 predstavlja vodonik, a drugi predstavlja: C1-6 alkil opciono supstituisan sa -ORx grupom ili -Z-heterociklil grupu opciono supstituisanu sa Ra grupom; C3-8 cikloalkil; ili heterociklil opciono supstituisan sa Ra grupom.
6. Jedinjenje prema zahtjevu 4, pri čemu R7 i R8 zajedno sa atomom azota za koji su pričvršćeni obrazuju heterociklil prsten koji sadrži azot i opciono je supstituisan sa 1, 2 ili 3 Rb grupama.
7. Jedinjenje prema bilo kom od zahtjeva 1 do 3, pri čemu R2 predstavlja - COOH.
8. Jedinjenje prema bilo kom od zahtjeva 1 do 3, pri čemu R2 predstavlja - CORx grupu.
9. Jedinjenje prema zahtjevu 8, pri čemu R2 predstavlja -COMe.
10. Jedinjenje prema bilo kom od prethodnih zahtjeva, pri čemu Y i Z nezavisno predstavljaju vezu, CO, -CH2-, -(CH2)2, -(CH2)3 ili -0-.
11. Jedinjenje prema bilo kom od prethodnih zahtjeva koje ima sledeći prstenasti sistem:
12. Farmaceutska kompozicija koja sadrži jedinjenje formule (I) prema bilo kom od zahtjeva 1 do 11.
13. Jedinjenje prema bilo kom od zahtjeva 1 do 11 za primjenu u terapiji.
14. Jedinjenje prema bilo kom od zahtjeva 1 do 11 za primenu u profilaksi ili liječenju kancera.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97955507P | 2007-10-12 | 2007-10-12 | |
| GBGB0720041.3A GB0720041D0 (en) | 2007-10-12 | 2007-10-12 | New Compounds |
| US6117808P | 2008-06-13 | 2008-06-13 | |
| EP08806556.0A EP2197880B1 (en) | 2007-10-12 | 2008-10-10 | Bicyclic heterocyclic compounds as protein tyrosine kinase inhibitors |
| PCT/GB2008/003418 WO2009047506A1 (en) | 2007-10-12 | 2008-10-10 | Bicyclic heterocyclic compounds as protein tyrosine kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02373B true ME02373B (me) | 2016-06-20 |
Family
ID=38788133
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2016-3A ME02373B (me) | 2007-10-12 | 2008-10-10 | Biciklična heterociklična jedinjenja kao inhibitori protein tirozin kinaze |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US8076354B2 (me) |
| EP (1) | EP2197880B1 (me) |
| JP (1) | JP5497648B2 (me) |
| AU (1) | AU2008309418B2 (me) |
| CA (1) | CA2701865C (me) |
| CY (1) | CY1117139T1 (me) |
| DK (1) | DK2197880T3 (me) |
| ES (1) | ES2559685T3 (me) |
| GB (1) | GB0720041D0 (me) |
| HR (1) | HRP20160002T1 (me) |
| HU (1) | HUE026275T2 (me) |
| ME (1) | ME02373B (me) |
| PL (1) | PL2197880T3 (me) |
| PT (1) | PT2197880E (me) |
| RS (1) | RS54518B1 (me) |
| SI (1) | SI2197880T1 (me) |
| WO (1) | WO2009047506A1 (me) |
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| GB0720041D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
| GB0810902D0 (en) | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906470D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
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-
2007
- 2007-10-12 GB GBGB0720041.3A patent/GB0720041D0/en not_active Ceased
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2008
- 2008-10-10 US US12/682,508 patent/US8076354B2/en active Active
- 2008-10-10 SI SI200831563T patent/SI2197880T1/sl unknown
- 2008-10-10 RS RS20160029A patent/RS54518B1/sr unknown
- 2008-10-10 PL PL08806556T patent/PL2197880T3/pl unknown
- 2008-10-10 WO PCT/GB2008/003418 patent/WO2009047506A1/en not_active Ceased
- 2008-10-10 AU AU2008309418A patent/AU2008309418B2/en not_active Ceased
- 2008-10-10 PT PT88065560T patent/PT2197880E/pt unknown
- 2008-10-10 ME MEP-2016-3A patent/ME02373B/me unknown
- 2008-10-10 DK DK08806556.0T patent/DK2197880T3/en active
- 2008-10-10 ES ES08806556.0T patent/ES2559685T3/es active Active
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- 2008-10-10 HR HRP20160002TT patent/HRP20160002T1/hr unknown
- 2008-10-10 CA CA2701865A patent/CA2701865C/en active Active
- 2008-10-10 HU HUE08806556A patent/HUE026275T2/en unknown
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Also Published As
| Publication number | Publication date |
|---|---|
| HUE026275T2 (en) | 2016-06-28 |
| HK1145495A1 (zh) | 2011-04-21 |
| AU2008309418A1 (en) | 2009-04-16 |
| JP2011500544A (ja) | 2011-01-06 |
| US20100331296A1 (en) | 2010-12-30 |
| GB0720041D0 (en) | 2007-11-21 |
| US20120035153A1 (en) | 2012-02-09 |
| CY1117139T1 (el) | 2017-04-05 |
| CA2701865C (en) | 2016-01-26 |
| CA2701865A1 (en) | 2009-04-16 |
| US8859583B2 (en) | 2014-10-14 |
| HRP20160002T1 (hr) | 2016-03-11 |
| US8076354B2 (en) | 2011-12-13 |
| AU2008309418B2 (en) | 2014-04-17 |
| PL2197880T3 (pl) | 2016-07-29 |
| RS54518B1 (sr) | 2016-06-30 |
| ES2559685T3 (es) | 2016-02-15 |
| EP2197880A1 (en) | 2010-06-23 |
| WO2009047506A1 (en) | 2009-04-16 |
| DK2197880T3 (en) | 2016-01-25 |
| SI2197880T1 (sl) | 2016-04-29 |
| PT2197880E (pt) | 2016-02-23 |
| EP2197880B1 (en) | 2015-12-23 |
| JP5497648B2 (ja) | 2014-05-21 |
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