HRP20171572T1 - Tripeptidi kao inhibitori epoksi keton proteaze - Google Patents

Tripeptidi kao inhibitori epoksi keton proteaze Download PDF

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Publication number
HRP20171572T1
HRP20171572T1 HRP20171572TT HRP20171572T HRP20171572T1 HR P20171572 T1 HRP20171572 T1 HR P20171572T1 HR P20171572T T HRP20171572T T HR P20171572TT HR P20171572 T HRP20171572 T HR P20171572T HR P20171572 T1 HRP20171572 T1 HR P20171572T1
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Croatia
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image
group
compound according
pharmaceutically acceptable
compound
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HRP20171572TT
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Dustin Mcminn
Henry Johnson
Simeon Bowers
David C. Moebius
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Onyx Therapeutics, Inc.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=51581125&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20171572(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Onyx Therapeutics, Inc. filed Critical Onyx Therapeutics, Inc.
Publication of HRP20171572T1 publication Critical patent/HRP20171572T1/hr

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    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
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Claims (15)

1. Spoj s Formulom (X): [image] naznačen time da: m i n svaki neovisno su 0, 1 ili 2, i m + n = 2, 3, ili 4; p je 0 ili 1; q je 0, 1, ili 2; K je odabran iz skupine koja sadrži CR5R6, NR7, N(C=O)OR7, -NH-(C=O)-, O, S, SO, i SO2; E je N ili CR7; R1 je odabran iz skupine koja sadrži H, C1-6alkil, C2-6alkenil, C2-6alkinil, C3-6cikloalkil, i 3-6 člani heterocikloalkil, pri čemu R1 je proizvoljno supstituiran s jednim ili više supstituenata koji se biraju iz skupine koju čine halo, OR7, SR7, N(R7)2, CN, i (C=O)N(R7)2; R2 je C1-2alkilen-G ili (C=O)-G; pri čemu je G odabran iz skupine koja sadrži aril, heteroaril, te piridinon, pod uvjetom da kada R2 je CH2fenil, fenil je supstituiran s jednim ili više supstituenata koji se biraju iz skupine koju čine OR7, halo, C1-3alkil, OCF3, SO2R7, (C=O)N(R7)2, CN, i SO2N(R7)2; R3 je odabran iz skupine koja sadrži C3-7cikloalkil, C3-7cikloalkenil, 3-7 člani heterocikloalkil, i 3-7 člani heterocikloalkenil, pri čemu je R3 proizvoljno supstituiran s jednim ili više supstituenata koji se biraju iz skupine koju čine halo, =O, OR7, SR7, N(R7)2, O(C=O)N(R7)2, i C1-6alkil; R4 je H ili C1-3alkil; R5 i R6 se svaki neovisno biraju iz skupine koju čine H, OH, halo, C1-3alkil, i CF3, ili R5 i R6 zajedno s ugljikom na koji su spojeni tvore C=O ili [image] pri čemu W je O ili NR7, i r je 1, 2 ili 3; i svaki R7 je neovisno H ili C1-6alkil, ili njihova farmaceutski prihvatljiva sol.
2. Spoj prema zahtjevu 1, naznačen time da [image] je odabran iz skupine koja sadrži: [image] [image] [image] [image] [image] [image] i [image]
3. Spoj prema zahtjevu 1 ili 2, naznačen time da [image] je odabran iz skupine koja sadrži: [image]
4. Spoj prema bilo kojem od zahtjeva 1 do 3, naznačen time da R1 je C1-3alkil ili je odabran iz skupine koju čine CH3, CH2OH, CH(OH)CH3, CH2CN.
5. Spoj prema bilo kojem od zahtjeva 1 do 4, naznačen time da R2 je CH2-heteroaril ili CH2-aril.
6. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time da R2 je odabran iz skupine koja sadrži [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image]
7. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time da R2 je odabran iz skupine koja sadrži: [image]
8. Spoj prema bilo kojem od zahtjeva 1 do 7, naznačen time da R3 je (i) ciklopropil, ciklobutil, ciklopentil, cikloheksil, ciklopentenil, cikloheksenil, tetrahidrofuranil, tetrahidropiranil, pirolidinil, pirolidinonil, dihidropiranil ili dihidrofuranil, ili (ii) odabran iz skupine koju čine [image]
9. Spoj prema zahtjevu 1 koji ima formulu: [image] naznačen time da: K je CH(OH) ili O; E je N ili CR7; R1 je CH3, CH2O CH(OH)CH3, ili CH2CN; R2 je [image] i R3 je [image]
10. Spoj prema zahtjevu 9 naznačen time da ima strukturu odabranu iz skupine koja sadrži: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] ili njihova farmaceutski prihvatljiva sol.
11. Spoj prema zahtjevu 10 naznačen time da ima strukturu odabranu iz skupine koja sadrži: [image] [image] [image] [image] [image] [image] [image] i [image] ili njihova farmaceutski prihvatljiva sol.
12. Spoj prema zahtjevu 10 naznačen time da ima strukturu odabranu iz skupine koja sadrži: [image] [image] [image] [image] [image] [image] ili njihova farmaceutski prihvatljiva sol.
13. Farmaceutski pripravak naznačen time da sadrži spoj prema bilo kojem od zahtjeva 1 do 12, ili njegova farmaceutski prihvatljiva sol, i farmaceutski prihvatljiv nosač ili razrjeđivač.
14. Spoj prema bilo kojem od zahtjeva 1 do 12 ili pripravak prema zahtjevu 13 naznačen time da je za uporabu u postupku inhibicije imunoproteazoma stanice, te postupak sadrži dovođenje u kontakt stanice sa spojem ili pripravkom u učinkovitoj količini za inhibiranje imunoproteazoma u stanici.
15. Spoj ili pripravak za uporabu prema zahtjevu 14, naznačen time da spoj inhibira β5i (LMP7), te proizvoljno dodatno inhibira jedan ili oba LMP2 i MECL-1.
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