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HRP20160852T1 - Biciklični heterociklični spojevi kao inhibitori protein tirozin kinaze - Google Patents

Biciklični heterociklični spojevi kao inhibitori protein tirozin kinaze Download PDF

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HRP20160852T1
HRP20160852T1 HRP20160852TT HRP20160852T HRP20160852T1 HR P20160852 T1 HRP20160852 T1 HR P20160852T1 HR P20160852T T HRP20160852T T HR P20160852TT HR P20160852 T HRP20160852 T HR P20160852T HR P20160852 T1 HRP20160852 T1 HR P20160852T1
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compound according
heterocyclyl
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Gordon Saxty
Valerio Berdini
Christopher William Murray
Charlotte Mary Griffiths-Jones
Emma Vickerstaffe
Gilbert Ebai Besong
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Astex Therapeutics Limited
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    • 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
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Claims (12)

1. Spoj formule (I): [image] pri čemu • predstavlja jednostruku ili dvostruku vezu, tako da je najmanje jedna veza u 5 članom prstenastom sustavu dvostruka veza; prsten A može biti opcionalno supstituiran s 1, 2 ili 3 Ra grupe; B predstavlja –heterociklil grupu gdje navedena heterociklil grupa može biti opcionalno supstituiran s 1, 2 ili 3 Ra grupe; Ra predstavlja halogen, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, -ORx, -O-(CH2)n-ORx, haloC1-6 alkil, haloC1-6 alkoksi, C1-6 alkanol, =O, =S, nitro, Si(Rx)4- (CH2)s-CN, -S-Rx, -SO-Rx, -SO2-Rx, -CORx, -(CRxRy)s-COORz, -(CH2)s-CONRxRy, - (CH2)s-NRxRy, -(CH2)s-NRxCORy, -(CH2)s-NRxSO2-Ry, - (CH2)s-NH-SO2-NRxRy,- OCONRxRy, - (CH2)s-NRxCO2Ry,-O-(CH2)sCRxRy-(CH2)t-ORz ili -(CH2)s-SO2NRxRy grupe; Rx, Ry i Rz neovisno predstavljaju vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkanol, hidroksi, C1-6 alkoksi, haloC1-6 alkil, -CO-(CH2)n-C1-6 alkoksi, C3-8 cikloalkil ili C3-8 cikloalkenil; R7 i R8 neovisno predstavljaju vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, aril, heterociklil ili R7 i R8 zajedno s atomom dušika za koji su pričvršćeni mogu obrazovati heterociklil prsten koji sadrži dušik, pri čemu spomenuti C1-6 alkil, aril i heterociklil može biti opcionalno supstituiran s 1, 2 ili 3 Rb grupe; R1 i Rb neovisno predstavlja Ra grupu ili -Y-karbocikličnu ili -Z-heterociklil grupu, pri čemu spomenute karbociklične i heterociklil grupe mogu biti opcionalno supstituirane s 1, 2 ili 3 Ra grupe; Y i Z neovisno predstavljaju vezu, -CO-(CH2)s-, -COO-, -(CH2)n-, -NRx-(CH2)s-, -(CH2)s-NRx-, -CONRx-, -NRxCO-, -SO2NRx-, -NRxSO2-, -NRxCONRy-, -NRxCSNRy-, - O-(CH2)s-, -(CH2)s-O-, -S-, -SO- ili -(CH2)s-SO2-; n predstavljaju cijeli broj od 1-4; s i t neovisno predstavljaju cijeli broj od 0-4; q neovisno predstavljaju cijeli broj od 0-2; ili njegova farmaceutski prihvatljiva sol ili solvat.
2. Spoj prema zahtjevu 1, pri čemu B predstavlja aromatičnu ili nearomatičnu heterociklil grupu; Ra predstavlja halogen, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, -ORx, -O-(CH2)n-ORx, haloC1-6 alkil, haloC1-6 alkoksi, C1-6 alkanol, =O, =S, nitro, -(CH2)s-CN, -S-Rx, -SO-Rx, -SO2-Rx, -CORx, -(CRxRy)s-COORz, -(CH2)s-CONRxRy, -(CH2)s-NRxRy, -(CH2)s-NRxCORy, -(CH2)s-NRxSO2-Ry, -OCON-RxRy, - (CH2)s-NRxCO2Ry, -O-(CH2)s-CRxRy-(CH2)t-ORz ili -(CH2)s-SO2NRxRy grupe; Y i Z neovisno predstavljaju vezu, -CO-, CH2-, -(CH2)2-, -CH2)3-, - O-(CH2)s ili NH-(CH2)n-.
3. Spoj prema zahtjevu 2 pri čemu heterociklil grupa je 5 ili 6 člana monociklična heterociklil grupa.
4. Spoj prema zahtjevu 3 pri čemu heterociklil grupa je piridil, pirazinil, triazinol, oksadiazolil, imidazolil ili tiadiazolil.
5. Spoj prema zahtjevu 4 pri čemu heterociklil grupa je tiadiazolil.
6. Spoj prema bilo kojem od predhodnih zahtjeva pri čemu q predstavlja 0.
7. Spoj prema bilo kojem od predhodnih zahtjeva pri čemu R7 i R8 zajedno predstavljaju vodik ili C1-6 alkil; ili jedan od R7 i R8 predstavlja vodik i drugi predstavlja C1-6 alkil (opcionalno supstituiran s -ORx grupom), C3-8 cikloalkil ili heterociklil.
8. Spoj prema bilo kojem od predhodnih zahtjeva 1 - 6, pri čemu R7 i R8 zajedno s atomom dušika za koji su pričvršćeni obrazuju heterociklil prsten opcionalno supstituiran s 1,2 ili 3 Rb grupama.
9. Spoj prema bilo kojem od prethodnih zahtjeva koje ima slijedeći prstenasti sustav: [image]
10. Farmaceutska kompozicija koja sadrži spoj formule (I) prema bilo kojem od zahtjeva 1 do 9.
11. Spoj prema bilo kojem od zahtjeva 1 do 9 za primjenu u terapiji.
12. Spoj prema bilo kojem od zahtjeva 1 do 9 za primjenu u profilaksi ili liječenju raka.
HRP20160852TT 2007-10-12 2016-07-13 Biciklični heterociklični spojevi kao inhibitori protein tirozin kinaze HRP20160852T1 (hr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US97958907P 2007-10-12 2007-10-12
GBGB0720038.9A GB0720038D0 (en) 2007-10-12 2007-10-12 New compounds
US6117208P 2008-06-13 2008-06-13
PCT/GB2008/003439 WO2009047522A1 (en) 2007-10-12 2008-10-10 Bicyclic heterocyclic compounds as protein tyrosine kinase inhibitors
EP08806575.0A EP2203449B1 (en) 2007-10-12 2008-10-10 Bicyclic heterocyclic compounds as protein tyrosine kinase inhibitors

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US (2) US8071614B2 (hr)
EP (1) EP2203449B1 (hr)
JP (1) JP5562858B2 (hr)
AU (1) AU2008309342C1 (hr)
CA (1) CA2701868C (hr)
CY (1) CY1117820T1 (hr)
ES (1) ES2585352T3 (hr)
GB (1) GB0720038D0 (hr)
HK (1) HK1145496A1 (hr)
HR (1) HRP20160852T1 (hr)
HU (1) HUE028999T2 (hr)
ME (1) ME02815B (hr)
PL (1) PL2203449T3 (hr)
PT (1) PT2203449T (hr)
RS (1) RS55045B1 (hr)
SI (1) SI2203449T1 (hr)
WO (1) WO2009047522A1 (hr)

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