HRP20121023T1 - Inhibitori za iap - Google Patents

Inhibitori za iap Download PDF

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HRP20121023T1
HRP20121023T1 HRP20121023TT HRP20121023T HRP20121023T1 HR P20121023 T1 HRP20121023 T1 HR P20121023T1 HR P20121023T T HRP20121023T T HR P20121023TT HR P20121023 T HRP20121023 T HR P20121023T HR P20121023 T1 HRP20121023 T1 HR P20121023T1
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compounds
formula
inhibitors
image
phenyl
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HRP20121023TT
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Mark G. Palermo
Sushil Kumar Sharma
Christopher Sean Straub
Rung-Ming David Wang
Leigh Zawel
Yanlin Zhang
Zhuoliang Chen
Yaping Wang
Fan Yang
Wojciech Wrona
Gang Liu
Mark G. Charest
Feng He
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Novartis Ag
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Publication of HRP20121023T1 publication Critical patent/HRP20121023T1/hr

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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D207/06—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
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    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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Claims (18)

1. Spojevi, naznačeni time, da imaju formulu (IV) [image] gdje U je: [image] i gdje (a) R1 i R3 su metil ili etil; R2 je H, metil, etil, klorometil, diklorometil ili trifluorometil; R4 je C1-C4alkil; C3-C7 cikloalkil; C3-C7 cikloalkil-C1-C7alkil; fenil-C1-C7alkil ili aril, R5 je H; U ima strukturu formule II gdje X je N; R6, R’6, R7 i R’7 su H; ili R6 je -C(O)-C1-C4alkil-fenil i R’6, R7 i R’7 su H; n je 0, tako da oba (Ra)n i (Rb)n označavaju vezu; Rc je H; Rd je Ar1-D-Ar2, pri čemu su Ar1 i Ar2 supstituirani ili nesupstituirani fenil ili het: i D je N(Rh), gdje Rh je H, Me, -CHO, -SO2, -C(O), -CHOH, -CF3 ili -SO2CH3; ili gdje (b) R1 i R3 su metil ili etil; R2 je H, metil, etil, klorometil, diklorometil ili trifluorometil; R4 je C1-C4alkil; C3-C7cikloalkil; C3-C7cikloalkil- C1-C7alkil; fenil-C1-C7alkil ili aril; R5 je H; U ima strukturu formule II gdje X je N; R6, R’6, R7 i R’7 su H; n je 0, tako da oba (Ra)n i (Rb)n označavaju vezu; Rc je H; Rd je Ar1-D-Ar2, gdje su Ar1 i Ar2 supstituirani ili nesupstituirani fenil ili het; i D je -O-; ili gdje (c) R1 i R3 su metil ili etil; R2 je H, metil, etil, klorometil, diklorometil ili trifluorometil; R4 je C1-C4alkil ili C3-C7cikloalkil; R5 je H; U ima strukturu formule II gdje X je N; R6, R’6, R7 i R’7 su H; n je 0, tako da oba (Ra)n i (Rb)n označavaju vezu; Rc je H; Rd je Ar1-D-Ar2; Ar1 i Ar2 su supstituirani ili nesupstituirani fenil ili het; i D je C(O); pri čemu je "het" 5-7-člani heterociklički prsten koji sadrži 1-4 heteroatoma odabrana od N, O i S, ili 8-12-člani kondenzirani sustav prstena uključujući najmanje jedan 5-7-člani heterociklički prsten koji sadrži 1, 2 ili 3 heteroatoma odabrana od N, O i S, gdje je spomenuti heterociklički prsten ili kondenzirani sustav prstena nesupstituiran ili supstituiran na atomu ugljika ili dušika; ili njihove farmaceutski prihvatljive soli.
2. Spojevi formule (IV) prema zahtjevu 1, naznačeni time, da D je N(Rh), a R4 je metil, etil, butil, izopropil, t-butil, cikloheksil, -CH2-ciklopentil, -CH2-cikloheksil, -CH2-ciklopropil, fenil ili -CH2-fenil.
3. Spojevi formule (IV) prema zahtjevu 1 ili 2, naznačeni time, da D je N(Rh), a Ar1 i Ar2 su supstituiran ili nesupstituiran fenil ili het, gdje je spomenuti het supstituiran ili nesupstituiran triazin, pirimidin, piridin, oksazol, 2,4-difluorofenil, Cl-fenil ili fluorofenil.
4. Spojevi formule (IV) prema zahtjevu 1, naznačeni time, da D je -O- i R4 je metil, etil, butil, izopropil, t-butil, cikloheksil, -CH2-ciklopentil, -CH2-cikloheksil, -CH2-ciklopropil, fenil ili -CH2-fenil.
5. Spojevi formule (IV) prema zahtjevu 1 ili 4, naznačeni time, da D je -O-, a Ar1 i Ar2 su supstituiran ili nesupstituiran fenil ili het, gdje je spomenuti het supstituiran ili nesupstituiran pirimidin, piridin, oksazol ili 2-metiloksazol.
6. Spojevi formule (IV) prema zahtjevu 1, naznačeni time, da D je C(O), a R4 je izopropil, t-butil, ciklopentil ili cikloheksil.
7. Spojevi formule (IV) prema zahtjevu 1 ili 6, naznačeni time, da D je C(O), a Ar1 i Ar2 su supstituiran ili nesupstituiran fenil ili het, gdje je spomenuti het supstituiran ili nesupstituiran oksazol, tiazol ili oksadiazol.
8. Spojevi formule (IV) prema zahtjevu 1, naznačeni time, da su odabrani od sljedećih: Primjer 6 [image] [image] [image] [image] [image] [image] [image] [image] [image] i Primjer 195 [image] ili njihove farmaceutski prihvatljive soli.
9. Farmaceutski sastav, naznačen time, da obuhvaća farmaceutski prihvatljiv nosač i terapeutski učinkovitu količinu spoja formule (IV) prema bilo kojem od zahtjeva 1 do 8.
10. Spojevi formule (IV) prema bilo kojem od zahtjeva 1 do 8, naznačeni time, da se upotrebljavaju u medicini.
11. Uporaba spoja formule (IV) prema bilo kojem od zahtjeva 1 do 8, naznačena time, da je za proizvodnju lijeka za liječenje proliferativne bolesti.
12. Uporaba prema zahtjevu 11, naznačena time, da proliferativna bolest je tumor.
13. Uporaba prema zahtjevu 11 ili 12, naznačena time, da je proliferativna bolest odabrana od sljedećih: rak dojke, urogenitalni rak, rak pluća, gastrointestinalni rak, epidermalni rak, melanom, rak jajnika, rak gušterače, neuroblastom, rak glave i/ili vrata, rak mjehura, renalni ili gastrički rak, rak mozga, tumor usta, plućni tumor, kolorektalni tumor, tumor prostate i multipli mijelom.
14. Kombinacija, naznačena time, da obuhvaća spoj formule (IV) prema bilo kojem od zahtjeva 1 do 8 i neko drugo antiproliferativno sredstvo.
15. Kombinacija prema zahtjevu 14, naznačena time, da je drugo antiproliferativno sredstvo odabrano od sljedećih: inhibitori aromataze; antiestrogeni, inhibitori topoizomeraze I; inhibitori topoizomeraze II; mikrotubulna aktivna sredstva; alkilacijska sredstva; inhibitori histonske deacetilaze; spojevi koji induciraju stanične diferencijacijske procese, inhibitori ciklooksigenaze; MMP-inhibitori; mTOR-inhibitori; antineoplastični antimetaboliti; platinski spojevi; spojevi koji ciljaju na aktivnost kinaze proteina ili lipida, na primjer da je smanjuju i drugi antiangiogenski spojevi; spojevi koji ciljaju na aktivnost fosfataze proteina ili lipida, na primjer da je smanjuju ili inhibiraju; gonadorelinski agonisti; antiandrogeni; inhibitori aminopeptidaze metionina; bisfosfonati; tvari koje modificiraju biološku reakciju; antiproliferativna protutijela; inhibitori heparanaze; inbitori onkogenskih Ras-izoforma; inhibitori telomeraze; inhibitori proteazoma; sredstva koja se koriste u liječenju hematoloških maligniteta; spojevi koji ciljaju na aktivnost Flt-3, na primjer da je smanjuju ili inhibiraju; Hsp90-inhibitori; temozolomid (TEMODAL®) i leukovorin.
16. Kombinacija prema zahtjevu 15, naznačena time, da drugo antiproliferativno sredstvo je mikrotubulno aktivno sredstvo.
17. Kombinacija prema zahtjevu 16, naznačena time, da mikrotubulno aktivno sredstvo je paklitaksel ili docetaksel.
18. Spojevi formule (IV) prema bilo kojem od zahtjeva 1 do 8, naznačeni time, da se upotrebljavaju za liječenje bilo koje indikacije opisane u bilo kojem od zahtjeva 11, 12 ili 13.
HRP20121023TT 2004-04-07 2012-12-12 Inhibitori za iap HRP20121023T1 (hr)

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US (4) US20080242658A1 (hr)
EP (3) EP2253614B1 (hr)
JP (3) JP4691549B2 (hr)
KR (2) KR20080083220A (hr)
CN (1) CN1964970B (hr)
AR (1) AR048927A1 (hr)
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