HRP20100715T1 - Triazoli korisni kao inhibitori protein kinaza - Google Patents

Triazoli korisni kao inhibitori protein kinaza Download PDF

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HRP20100715T1
HRP20100715T1 HR20100715T HRP20100715T HRP20100715T1 HR P20100715 T1 HRP20100715 T1 HR P20100715T1 HR 20100715 T HR20100715 T HR 20100715T HR P20100715 T HRP20100715 T HR P20100715T HR P20100715 T1 HRP20100715 T1 HR P20100715T1
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aliphatic
agent
treatment
diseases
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J. Davies Robert
J. Forster Cornelia
J. Arnost Michael
Wang Jian
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Vertex Pharmaceuticals Incorporated
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Abstract

Spoj formule (II): pri čemuX je N; Y je NR°, ili O; n je 0; m je 0; p je 0; R1 je -N(H)R2;R2 je vodik; R3 je 2-piridil; R5 je vodik, ili -CN; naznačen time, da je svaki pojedini neovisni slučaj R° odabran iz vodika, opcionalno supstituiranog C1-6 alifatskog, nesupstituiranog 5-6-ero članog heteroarila ili heterocikličkog prstena (pod uvjetom da je dušikov atom u heterocikličkom prstenu opcijski supstituiran sa -R+ ili -C(O)R+, pri čemu R+ je (C1-6alkil), bolje (C1-4alkil), fenil, -O(Ph), ili -CH2(Ph), ili, bez obzira na gornju definiciju, dva neovisna slučaja R°, na istom supstituentu ili različitim supstituentima, uzeta zajedno sa atomom(ima) u kojima je pojedina R° grupa vezana, formira 5-8-ero člani heterociklil, aril, ili heteroarilni prsten ili 3-8-ero člani cikloalkilni prsten koji ima 0-3 heteroatoma nezavisno odabrana iz dušika, kisika, ili sumpora; pri čemu svaki nezavisni slučaj R° je odabran iz vodika, opcijski supstituiranog C1-6alifatskog, nesupstituiranog 5-6-ero članog heteroarila ili heterocikličkog prstena, fenila, -O(Ph), ili -CH2(Ph), ili, bez obzira na gornju definiciju, dva neovisna slučaja R°, na istom supstituentu ili različitim supstituentima, koji su uzeti zajedno s atomom(ima) u kojima pojedina R° skupina je vezana, tvori 5-8-ero člani heterociklil, aril, ili heteroarilni prsten ili 3-8-ero člani cikloalkilni prsten koji ima 0-3 heteroatoma neovisno odabrana iz skupine dušika, kisika, ili sumpora; alifatska skupina R° je opcijski supstituirana sa NH2, NH(C1-4 alifatski), N(C1-4 alifatski)2, halogen, C1-4 alifatski, OH, O(C1-4 alifatski), NO2, CN, CO(2H, CO2(C1-4 alifatski), O(halo C1-4 alifatski), ili halo(C1-4 alifatski), pri čemu je svaka od gore navedenih C1-4 alifatskih skupina nesupstituirana; svaki pojedini R*je neovisno odabran iz vodika ili je C1-6 alifatskog opcijski supstituiranog sa NH2, NH(C1-4 alifatski), N(C1-4 alifatski)2, halogen, C1-4 alifatski, OH, O(C1-4 alifatski), NO2, CN, CO2H, CO2(C1-4 alifatski), O(halo C1-4 alifatski), ili halo(C1-4 alifatski), pri čemu je svaka od gore navedenih C1-4 alifatskih skupina nesupstituirana; i R je vodik ili C1-6 alifatska skupina, opcijski supstituirana sa =O, =S, - NH2, NH(C1-4 alifatski), N(C1-4 alifatski)2, halogen, C1-4 alifatski, OH, O(C1-4 alifatski), NO2, CN, CO2H, CO2(C1-4 alifatski), O(halo C1-4 alifatski), ili halo (C1-4 alifatski), pri čemu je svaka od gore navedenih C1-4 alifatskih skupina nesupstituirana. Patent sadrži još 10 patentnih zahtjeva.

Claims (11)

1. Spoj formule (II): [image] pri čemu X je N; Y je NR°, ili O; n je 0; m je 0; p je 0; R1 je -N(H)R2; R2 je vodik; R3 je 2-piridil; R5 je vodik, ili -CN; naznačen time, da je svaki pojedini neovisni slučaj R° odabran iz vodika, opcionalno supstituiranog C1-6 alifatskog, nesupstituiranog 5-6-ero članog heteroarila ili heterocikličkog prstena (pod uvjetom da je dušikov atom u heterocikličkom prstenu opcijski supstituiran sa -R+ ili -C(O)R+, pri čemu R+ je (C1-6alkil), bolje (C1-4alkil), fenil, -O(Ph), ili -CH2(Ph), ili, bez obzira na gornju definiciju, dva neovisna slučaja R°, na istom supstituentu ili različitim supstituentima, uzeta zajedno sa atomom(ima) u kojima je pojedina R° grupa vezana, formira 5-8-ero člani heterociklil, aril, ili heteroarilni prsten ili 3-8-ero člani cikloalkilni prsten koji ima 0-3 heteroatoma nezavisno odabrana iz dušika, kisika, ili sumpora; pri čemu svaki nezavisni slučaj R° je odabran iz vodika, opcijski supstituiranog C1-6alifatskog, nesupstituiranog 5-6-ero članog heteroarila ili heterocikličkog prstena, fenila, -O(Ph), ili -CH2(Ph), ili, bez obzira na gornju definiciju, dva neovisna slučaja R°, na istom supstituentu ili različitim supstituentima, koji su uzeti zajedno s atomom(ima) u kojima pojedina R° skupina je vezana, tvori 5-8-ero člani heterociklil, aril, ili heteroarilni prsten ili 3-8-ero člani cikloalkilni prsten koji ima 0-3 heteroatoma neovisno odabrana iz skupine dušika, kisika, ili sumpora; alifatska skupina R° je opcijski supstituirana sa NH2, NH(C1-4 alifatski), N(C1-4 alifatski)2, halogen, C1-4 alifatski, OH, O(C1-4 alifatski), NO2, CN, CO(2H, CO2(C1-4 alifatski), O(halo C1-4 alifatski), ili halo(C1-4 alifatski), pri čemu je svaka od gore navedenih C1-4 alifatskih skupina nesupstituirana; svaki pojedini R*je neovisno odabran iz vodika ili je C1-6 alifatskog opcijski supstituiranog sa NH2, NH(C1-4 alifatski), N(C1-4 alifatski)2, halogen, C1-4 alifatski, OH, O(C1-4 alifatski), NO2, CN, CO2H, CO2(C1-4 alifatski), O(halo C1-4 alifatski), ili halo(C1-4 alifatski), pri čemu je svaka od gore navedenih C1-4 alifatskih skupina nesupstituirana; i R je vodik ili C1-6 alifatska skupina, opcijski supstituirana sa =O, =S, - NH2, NH(C1-4 alifatski), N(C1-4 alifatski)2, halogen, C1-4 alifatski, OH, O(C1-4 alifatski), NO2, CN, CO2H, CO2(C1-4 alifatski), O(halo C1-4 alifatski), ili halo (C1-4 alifatski), pri čemu je svaka od gore navedenih C1-4 alifatskih skupina nesupstituirana.
2. Spoj prema zahtjevu 1, koji ima formulu (I-b) ili (I-c): [image] naznačen time, da je navedeni spoj odabran iz skupine koja se sastoji od: [image] [image]
3. Spoj prema zahtjevu 1, naznačen time, da je navedeni spoj odabran iz skupine koja se sastoji od: [image] [image] [image]
4. Farmaceutski sastojak naznačen time, da sadrži: spoj prema bilo kojem od zahtjeva 1-3 ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljiv nosač, kemijski dodatak, ili sredstvo.
5. Sastojak prema zahtjevu 4, naznačen time, da nadalje sadrži dodatni terapeutski agens izabran iz kemoterapeutskog ili anti-proliferativnog agensa, agensa za liječenje Alzheimerove bolesti, agensa za liječenje Parkinsonove bolesti, agensa za liječenje multiple skleroze (MS), agensa za liječenje astme, agensa za liječenje šizofrenije, protuupalnog agensa, imunomodulatornog ili imunosupresivnog agensa, neurotrofičnog faktora, agensa za liječenje kardiovaskularnih bolesti, agensa za liječenje destruktivnih koštanih poremećaja, agensa za liječenje poremećaja jetre, agensa za liječenje poremećaja u krvi, ili agensa za liječenje poremećaja imunodeficijencije.
6. in Vitro metoda inhibicije FLT-3, aktivnosti kinaze u biološkom uzorku, naznačena time, da sadrži korak dovođenja u kontakt spomenutog biološkog uzorka sa: a) sastojkom prema zahtjevu 4; ili b) spojem prema bilo kojem od zahtjeva 1-3, ili njegovom farmaceutski prihvatljivom soli.
7. Sastojak prema zahtjevu 4, ili spoj prema bilo kojem od zahtjeva 1-3, ili njihova farmaceutski prihvatljiva sol, naznačen time, da je za upotrebu u inhibiranju aktivnosti FLT-3 kinaze kod pacijenta.
8. Sastojak prema zahtjevu 4; ili sastojak prema bilo kojem od zahtjeva 1-3, naznačen time, da je za upotrebu u liječenju ili ublažavanju težine bolesti odabranih iz alergijskih bolesti, proliferativnih bolesti, autoimunih oboljenja, stanja povezanih s transplantacijom organa, upalnih oboljenja, oboljenja povezanih s imunološki sustavom ili destruktivnih bolesti kostiju.
9. Spoj prema bilo kojem od zahtjeva 1-3, ili sastojak prema zahtjevu 4, za upotrebu prema zahtjevu 8, naznačen time, da je za upotrebu istovremeno sa, prije, ili poslije dodatnog terapeutskog agensa odabranog iz kemoterapijskog ili antiproliferativnog agensa, agensa za liječenje Alzheimerove bolesti, agensa za liječenje Parkinsonove bolesti, agensa za liječenje multiple skleroze (MS), agensa za liječenje astme, agensa za liječenje šizofrenije, protuupalnog agensa, immunomodulatornog ili imunosupresivnog agensa, naurotrofnog faktora, agensa za liječenje kardiovaskularnih oboljenja, agensa za liječenje destruktivnih koštanih poremećaja, agensa za liječenje poremećaja jetre, agensa za liječenje poremećaja u krvi, ili agensa za liječenje poremećaja imunodeficijencije.
10. Spoj prema bilo kojem od zahtjeva 1-3, ili sastojak prema zahtjevu 4, za upotrebu prema zahtjevu 9, naznačen time, da je bolest izabrana iz skupine raka, Alzheimerove bolesti, restenoze, angiogeneze, glomerulonefritisa, citomegalovirusa, HIV-a, herpesa, psorijaze, ateroskleroze, alopecije, autoimunog oboljenja, virusne infekcije, neurodegenerativnog poremećaja, poremećaja povezanog s apoptozom timocita, ili proliferativnog poremećaja; hematološkog poremećaja, poglavito, akutne mijelogene leukemije (AML), akutne promijelocitne leukemija (APL), i akutne limfocitne leukemije (ALL); Imunoloških odgovora kao što je alergija ili tip I hipersenzitivnih reakcija, astma, autoimune bolesti kao što su odbacivanje transplantata, reakcija transplantata protiv primatelja, reumatoidni artritis, amiotrofična lateralna skleroza, i multipla skleroza, neurodegenerativni poremećaji kao što je obiteljska amiotrofična lateralna skleroza (FALS), kao i u krutom i hematološkom malignom tkivu kao što su leukemije i limfomi; pri čemu karcinom je karcinom pankreasa, prostate, ili jajnika.
11. Upotreba spoja prema bilo kojem od zahtjeva 1-3, ili sastojak prema bilo kojem od zahtjeva 4-5, naznačena time, da je za proizvodnju lijeka za liječenje ili ublažavanju težine bolesti odabranih iz alergijskih bolesti, proliferativnih bolesti, autoimunih oboljenja, bolesti povezanih s transplantacijom organa, upalnih oboljenja, imunološki povezanih oboljenja ili destruktivnih bolesti kostiju; karcinoma, Alzheimerove bolesti, restenoze, angiogeneze, glomerulonefritisa, citomegalovirusa, HIV-a, herpesa, psorijaze, ateroskleroze, alopecije, autoimunog oboljenja, virusne infekcije, neurodegenerativnog poremećaja, poremećaja povezanog s apoptozom timocita, ili proliferativnog poremećaja; hematološkog poremećaja, poglavito, akutne mijelogene leukemije (AML), akutne promijelocitne leukemija (APL), i akutne limfocitne leukemije (ALL); Imunoloških odgovora kao što je alergija ili tip I hipersenzitivnih reakcija, astma, autoimune bolesti kao što su odbacivanje transplantata, reakcija transplantata protiv primatelja, reumatoidni artritis, amiotrofična lateralna skleroza, i multipla skleroza, neurodegenerativni poremećaji kao što je obiteljska amiotrofična lateralna skleroza (FALS), kao i u krutom i hematološkom malignom tkivu kao što su leukemije i limfomi; karcinoma pankreasa, prostate, ili jajnika.
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