HRP20100072T1 - Derivati benzokinazolina i njihova uporaba u liječenju bolesti kosti - Google Patents

Derivati benzokinazolina i njihova uporaba u liječenju bolesti kosti Download PDF

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HRP20100072T1
HRP20100072T1 HR20100072T HRP20100072T HRP20100072T1 HR P20100072 T1 HRP20100072 T1 HR P20100072T1 HR 20100072 T HR20100072 T HR 20100072T HR P20100072 T HRP20100072 T HR P20100072T HR P20100072 T1 HRP20100072 T1 HR P20100072T1
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phenyl
isopropyl
ynyloxy
prop
quinazoline
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Ammon Sandra
Beerli Ren�
Widler Leo
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Novartis Ag
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Abstract

Spoj, naznačen time, da je formule (I) ili njegova farmaceutski prihvatljiva sol ili njegov ester prolijeka: gdje: Q je CH ili N; R2 je C1-C4 alkil; Y je R5-O-;gdje R5 je etinil ili propinil; X je izabran iz skupine koju čine aril, heteroaril, C1-C10 alkil, C1-C10 alkiloksi, cikloalkil, heterocikloalkil, aril C1-C4 alkil, heteroaril C1-C4 alkil, cikloalkil C1-C4 alkil, heterocikloalkil C1-C4 alkil, arilamino, heteroarilamino, aril C1-C4 alkilamino, heteroaril C1-C4 alkilamino, C1-C6 alkilamino, C1-C6 dialkilamino, ariloksi, heteroariloksi, aril C1-C4 alkiloksi, heteroaril C1-C4 alkiloksi, cikloalkil C1-C4 alkilamino, heterocikloalkil C1-C4 alkilamino, cikloalkil C1-C4 alkiloksi ili heterocikloalkil C1-C4 alkiloksi od kojih je svaki po izboru supstituiran jedanput ili više, pri čemu izborni supstituend ili supstituendi na X su neovisno izabrani iz skupine koju čine halo, cijano, trifluorometil, nitro, hidroksi i po izboru supstituiran (C1-C4 alkil, C1-C4 alkiloksi, amino, sulfanil, sulfonil, oksikarbonil, hidroksil, sulfinil, aminosulfonil, sulfonilamino, karbonil, karboniloksi, karbonil amino, karboksil, acil, acilamino ili karbamoil), izborni supstituend ili supstituendi su izabrani iz skupine koju čine C1-C6 alkil, C1-C6 alkiloksi, karboksil, hidroksil, hidroksi C1-C4 alkil; od kojih svaki zauzvrat može po izboru biti supstituiran s C1-C6 alkiloksi, C1-C6 alkil, C1-C3 fluoriranim alkil, C1-C6 alkiloksi, karboksil, hidroksil, hidroksi C1-C4 alkil, halo, cijano, nitro; teR3 i R4 svaki predstavljaju jedan ili više supstituenada neovisno izabranih između: H, halo, C1-C4 alkil, C1-C4 alkiloksi i CF3,izborni supstituend ili supstituendi na R3 ili R4 su neovisno izabrani iz skupine koju čine C1-C4 alkil, halo, C1-C4 alkiloksi, cijano, sulfanil, sulfonil, amino, oksikarbonil i hidroksil, koji mogu zauzvrat biti po izboru supstituirani jedanput ili više s C1-C4 alkil, halo, C1-C4 alkiloksi, cijano, sulfanil, sulfonil, amino, oksikarbonil ili hidroksil. Patent sadrži još 11 patentnih zahtjeva.

Claims (12)

1. Spoj, naznačen time, da je formule (I) ili njegova farmaceutski prihvatljiva sol ili njegov ester prolijeka: [image] gdje: Q je CH ili N; R2 je C1-C4 alkil; Y je R5-O-; gdje R5 je etinil ili propinil; X je izabran iz skupine koju čine aril, heteroaril, C1-C10 alkil, C1-C10 alkiloksi, cikloalkil, heterocikloalkil, aril C1-C4 alkil, heteroaril C1-C4 alkil, cikloalkil C1-C4 alkil, heterocikloalkil C1-C4 alkil, arilamino, heteroarilamino, aril C1-C4 alkilamino, heteroaril C1-C4 alkilamino, C1-C6 alkilamino, C1-C6 dialkilamino, ariloksi, heteroariloksi, aril C1-C4 alkiloksi, heteroaril C1-C4 alkiloksi, cikloalkil C1-C4 alkilamino, heterocikloalkil C1-C4 alkilamino, cikloalkil C1-C4 alkiloksi ili heterocikloalkil C1-C4 alkiloksi od kojih je svaki po izboru supstituiran jedanput ili više, pri čemu izborni supstituend ili supstituendi na X su neovisno izabrani iz skupine koju čine halo, cijano, trifluorometil, nitro, hidroksi i po izboru supstituiran (C1-C4 alkil, C1-C4 alkiloksi, amino, sulfanil, sulfonil, oksikarbonil, hidroksil, sulfinil, aminosulfonil, sulfonilamino, karbonil, karboniloksi, karbonil amino, karboksil, acil, acilamino ili karbamoil), izborni supstituend ili supstituendi su izabrani iz skupine koju čine C1-C6 alkil, C1-C6 alkiloksi, karboksil, hidroksil, hidroksi C1-C4 alkil; od kojih svaki zauzvrat može po izboru biti supstituiran s C1-C6 alkiloksi, C1-C6 alkil, C1-C3 fluoriranim alkil, C1-C6 alkiloksi, karboksil, hidroksil, hidroksi C1-C4 alkil, halo, cijano, nitro; te R3 i R4 svaki predstavljaju jedan ili više supstituenada neovisno izabranih između: H, halo, C1-C4 alkil, C1-C4 alkiloksi i CF3, izborni supstituend ili supstituendi na R3 ili R4 su neovisno izabrani iz skupine koju čine C1-C4 alkil, halo, C1-C4 alkiloksi, cijano, sulfanil, sulfonil, amino, oksikarbonil i hidroksil, koji mogu zauzvrat biti po izboru supstituirani jedanput ili više s C1-C4 alkil, halo, C1-C4 alkiloksi, cijano, sulfanil, sulfonil, amino, oksikarbonil ili hidroksil.
2. Spoj u skladu sa zahtjevom 1, naznačen time, da je formule (I') ili njegova farmaceutski prihvatljiva sol ili njegov ester prolijeka: [image] gdje: Q je CH ili N; R2 je C1-C4 alkil; Y je R5-O-; gdje R5 je etinil ili propargil; X je izabran iz skupine koju čine aril, heteroaril, C1-C6 alkil, cikloalkil, heterocikloalkil, aril C1-C4 alkil, heteroaril C1-C4 alkil, arilamino, aril C1-C4 alkilamino, heteroaril C1-C4 alkilamino, C1-C6 alkilamino, C1-C6 dialkilamino amino, ariloksi, heteroariloksi, aril C1-C4 alkiloksi ili heteroaril C1-C4 alkiloksi, od kojih je svaki po izboru supstituiran jedanput ili više, pri čemu izborni supstituend ili supstituendi na X su neovisno izabrani iz skupine koju čine C1-C4 alkil, halo, C1-C4 alkiloksi, cijano, trifluorometil, hidroksi, amino, nitro i C1-C4 alkil supstituiran (sulfanil, sulfonil, amino, oksikarbonil, hidroksil, sulfinil, karbonil, karboksil ili karbamoil); te R3 i R4 svaki predstavljaju jedan ili više supstituenada neovisno izabranih između H, halo, po izboru supstituiranog C1-C4 alkil i po izboru supstituiranog C1-C4 alkiloksi, izborni supstituend ili supstituendi na R3 ili R4 su neovisno izabrani iz skupine koju čine C1-C4 alkil, halo, C1-C4 alkiloksi, cijano, sulfanil, sulfonil, amino, oksikarbonil i hidroksil.
3. Spoj u skladu sa zahtjevom 1, naznačen time, da je formule (II) ili njegova farmaceutski prihvatljiva sol ili njegov ester prolijeka: [image] gdje X' je izabran iz skupine koju čine aril, heteroaril, cikloalkil, heterocikloalkil, -C1-C4 alkilaril, -C1-C4 alkilheteroaril, arilamino, heteroarilamino, aril C1-C4 alkilamino, heteroaril C1-C4 alkilamino, ariloksi, heteroariloksi, aril C1-C4 alkiloksi, heteroaril C1-C4 alkiloksi, aril C1-C4 alkil, heteroaril C1-C4 alkil, C1-C6 alkil, -C1-C4 alkilamino ili amino, od kojih je svaki po izboru supstituiran jedanput ili više, pri čemu izborni supstituend ili supstituendi na X' su neovisno izabrani iz skupine koju čine halo, cijano, trifluorometil, nitro, hidroksi i po izboru supstituirani (C1-C4 alkil, C1-C4 alkoksi, amino, sulfanil, sulfonil, amino, oksikarbonil, hidroksil, sulfinil, karbonil, karboksil, acil, acilamino ili karbamoil); izborni supstituend ili supstituendi su izabrani između C1-C6 alkil, C1-C6 alkiloksi, karboksil, hidroksil i hidroksi C1-C4 alkil; od kojih svaki zauzvrat može biti po izboru supstituiran s C1-C6 alkiloksi, C1-C6 alkil, C1-C6 alkiloksi, karboksil, hidroksil, hidroksi C1-C4 alkil, halo, cijano, nitro, te R2' je C1-C4 alkil.
4. Spoj u skladu sa zahtjevom 3, naznačen time, da R2' je izopropil.
5. Spoj u skladu sa zahtjevom 2 ili 3, naznačen time, da X' je po izboru supstituiran (aril, heteroaril, heterocikloalkil, arilamino, heteroarilamino, aril C1-C4 alkilamino, heteroaril C1-C4 alkilamino, ariloksi, heteroariloksi, C1-C6 alkiloksi, aril C1-C4 alkiloksi, heteroaril C1-C4 alkiloksi), gdje su supstituendi kao što su definirani u zahtjevu 2 ili zahtjevu 3.
6. Spoj u skladu s bilo kojim od ranijih zahtjeva, naznačen time, da je izabran iz slijedeće skupine: (4-terc.-butil-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon [4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-fenil-metanon (2-metoksi-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (3-metoksi-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-metoksi-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-fluoro-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (3-fluoro-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (3-kloro-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-kloro-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-fluoro-fenil)-[4-(4-terc.-butil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (3-fluoro-fenil)-[4-(4-terc.-butil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (3-bromo-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-bromo-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-metil-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-izopropil-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-etil-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-propil-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-cijano-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-metiltio-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-metansulfonil-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-dimetilamino-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-etoksi-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon metil ester 4-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-karbonil]-benzojeve kiseline (4-dimetilamino-fenil)-[4-(4-terc.-butil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon etil ester 4-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-karbonil]-benzojeve kiseline (4-metoksi-fenil)-[4-(4-terc.-butil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (3-etoksi-4-metoksi-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-terc.-butiloksi-fenil)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-hidroksi)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (4-butiloksi)-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon furan-2-il-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon furan-3-il-[4-(4-terc.-butil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon furan-3-il-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon tiofen-2-il-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (3-metil-tiofen-2-il-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon benz[b]tiofen-2-il-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon tiofen-3-il-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon (1-metil-1H-pirol)-2-il-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon etil ester 4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-karboksilne kiseline [4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-piridin-3-il-metanon [4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-naftalen-1-il-metanon [4-(4-izopropil-fenil)-6-propargiloksi-naftalen-2-il]-metanon benzotiazol-2-il-[4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon [4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-tiazol-5-il-metanon [4-(4-izopropil-fenil)-6-propargiloksi-kinazolin-2-il]-piperidin-1-il-metanon (3-kloro-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3-metoksi-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3-metilsulfanil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-3,4-dihidro-kinazolin-2-karboksilne kiseline (3-metansulfonil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-3,4-dihidro-kinazolin-2-karboksilne kiseline (3-trifluorometilsulfanil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3-sulfamoil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-3,4-dihidro-kinazolin-2-karboksilne kiseline [3-(2-hidroksi-etansulfonil)-fenil]-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-3,4-dihidro-kinazolin-2-karboksilne kiseline (5-etansulfonil-2-hidroksi-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-3,4-dihidro-kinazolin-2-karboksilne kiseline (3-nitro-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3-cijano-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline metil ester 3-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-benzojeve kiseline etil ester 3-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-benzojeve kiseline izopropil ester 3-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-benzojeve kiseline terc.-butil ester 3-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-benzojeve kiseline (3-karbamoil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3-acetil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline metil ester 3-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-5-metoksibenzojeve kiseline (3-metilkarbamoilfenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3-terc.-butilkarbamoilfenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3-dimetilkarbamoil-5-trifluorometil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline metil ester 3-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-5-trifluorometilbenzojeve kiseline izopropil ester 3-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-5-trifluorometilbenzojeve kiseline metil ester 2-fluoro-5-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-benzojeve kiseline izopropil ester 2-fluoro-5-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-benzojeve kiseline metil ester 2-kloro-5-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-benzojeve kiseline metil ester 2,5-dikloro-3-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-benzojeve kiseline izopropil ester 2,5-dikloro-3-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-benzojeve kiseline (3-cijano-5-fluorofenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3,4-dicijano-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (4-cijano-3-trifluorometil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3-trifluorometilfenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (4-acetilamino-3-trifluorometil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3-metoksi-5-trifluorometil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3,5-bis-trifluorometil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3-fluoro-5-trifluorometil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (4-fluoro-3-trifluorometil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline metil ester 3-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-2-metil-benzojeve kiseline metil ester 3-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-4-metil-benzojeve kiseline metil ester 3-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-4-metoksibenzojeve kiseline dimetil ester 5-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-izoftalne kiseline dimetil ester 4-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-ftalne kiseline (3,5-dikloro-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3,4-dikloro-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3-kloro-4-fluorofenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (4-kloro-3-trifluorometil-fenil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline metil ester 5-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-piridin-2-karboksilne kiseline metil ester 5-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-nikotinske kiseline izopropil ester 5-{[4-(4-izopropil-fenil)-5-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-nikotinske kiseline [4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-il]-pirol-1-il-metanon (5-metil-1H-pirazol-3-il)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline etil ester (2-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-tiazol-4-il)-octene kiseline naftalen-1-ilamid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline izokinolin-8-ilamid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline ftalazin-5-ilamid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline kinolin-5-ilamid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline kinolin-8-ilamid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline izokinolin-4-ilamid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (5-acetil-kinolin-8-il)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (3-bromo-6-metoksi-kinolin-8-il)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline kinolin-2-ilamid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline kinolin-6-ilamid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (2-metil-kinolin-6-il)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline etil ester (6-{[4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karbonil]-amino}-kinolin-8-iloksi)-octene kiseline (1H-benzoimidazol-4-il)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline benzotiazol-2-ilamid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (benzo[1,3]dioksol-5-ilmetil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline (tiofen-2-ilmetil)-amid 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline 3-metoksi-fenil ester 4-(4-izopropil-fenil)-6-prop-2-iniloksi-kinazolin-2-karboksilne kiseline etil ester 1-(4-izopropil-fenil)-7-prop-2-iniloksi-izokinolin-3-karboksilne kiseline 1,2-dimetil-propil ester 1-(4-izopropil-fenil)-7-prop-2-iniloksi-izokinolin-3-karboksilne kiseline izobutil ester 1-(4-izopropil-fenil)-7-prop-2-iniloksi-izokinolin-3-karboksilne kiseline ciklopropilmetil ester 1-(4-izopropil-fenil)-7-prop-2-iniloksi-izokinolin-3-karboksilne kiseline benzil ester 1-(4-izopropil-fenil)-7-prop-2-iniloksi-izokinolin-3-karboksilne kiseline 2-metoksi-benzil ester 1-(4-izopropil-fenil)-7-prop-2-iniloksi-izokinolin-3-karboksilne kiseline 3-metoksi-benzil ester 1-(4-izopropil-fenil)-7-prop-2-iniloksi-izokinolin-3-karboksilne kiseline 4-metoksikarbonilbenzil ester 1-(4-izopropil-fenil)-7-prop-2-iniloksi-izokinolin-3-karboksilne kiseline fenetil ester 1-(4-izopropil-fenil)-7-prop-2-iniloksi-izokinolin-3-karboksilne kiseline 1-fenil-etil ester 1-(4-izopropil-fenil)-7-prop-2-iniloksi-izokinolin-3-karboksilne kiseline [3-(2-hidroksi-etansulfonil)-fenil]-amid 1-(4-izopropil-fenil)-7-prop-2-iniloksi-izokinolin-3-karboksilne kiseline [1-(4-izopropil-fenil)-7-prop-2-iniloksi-izokinolin-3-il]-(3-metoksi-fenil)-metanon [1-(4-izopropil-fenil)-7-prop-2-iniloksi-izokinolin-3-il]-(4-metoksi-fenil)-metanon.
7. Spoj, naznačen time, da je izabran iz skupine koju čine: (4-dimetilamino-fenil)-[4-(4-ciklopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon i (4-etoksi-fenil)-[4-(4-ciklopropil-fenil)-6-propargiloksi-kinazolin-2-il]-metanon.
8. Farmaceutski pripravak, naznačen time, da sadrži spoj formule (I) zajedno s farmaceutski prihvatljivom pomoćnom tvari, sredstvom za razrijeđivanje ili podlogom.
9. Spoj formule (I), naznačen time, da potiče oslobađanja paratireoidnog hormona.
10. Postupak priprave spoja formule (I) u skladu sa zahtjevom 1 ili zahtjevom 7 u slobodnom obliku ili u obliku soli, naznačen time, da sadrži slijedeće korake: (i) za slučajeve kada Q je N, reakciju spoja formule (III) sa spojem formule (IV) i amonijevom soli u prisutnosti prikladnog otapala: [image] ili (ii) reakciju spoja formule V [image] gdje LG predstavlja prikladnu odlazeću skupinu; s organometalnim reagensom formule VI: X-Met VI pod prikladnim anhidridnim uvjetima; ili (iii) reakciju spoja formule Va [image] s organometalnim reagensom formule VI: X-Met VI pod prikladnim anhidridnim uvjetima neposredno nakon čega slijedi oksidacija do karbonil spoja pomoću odgovarajućeg oksidacijskog sredstva; ili (iv) reakciju spoja formule VII [image] sa spojem X-H gdje H čini dio amino ili hidroksi skupine, a reakcija se provodi u prisutnosti kupirajućeg reagensa; ili (v) reakciju spoja formule VIII [image] gdje Hal je halogen ili odlazeća skupina sa spojem X-H gdje H čini dio amino ili hidroksi skupine, a reakcija se provodi u prisutnosti kupirajućeg reagensa.
11. Uporaba spoja formule (I) u skladu sa zahtjevom 1 ili 7, naznačena time, da se koristi izradi lijeka za prevenciju ili liječenje stanja kosti koja su povezana s povećanim osiromašivanjem kalcijem ili povećanom resorpcijom ili sa stanjima u kojima je poželjna stimulacija formiranja kosti ili je poželjno fiksiranje kalcija u kosti.
12. Kombinacija, naznačena time, da sadrži terapeutski učinkovitu količinu spoja u skladu s bilo kojim zahtjevom od 1 do 7 i drugu ljekovitu supstanciju izabranu iz skupine koju čine: kalcij, kalcitonin ili njegov analog ili derivat, steroidni hormon, djelomični agonist estrogena ili kombinacija estrogen-gestagen, SERM (Selective Estrogen Receptor Modulator), RANKL antitijelo, inhibitor katepsina K, vitamin D ili njegov analog ili PTH, PTH fragment ili derivat PTH za istovremeno, odijeljeno ili uzastopno liječenje.
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