SI2966067T1 - Oksazepini kot ionski kanalni modulatorji - Google Patents
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Claims (29)
- OKSAZEPINI KOT IONSKI KANALNI MODULATORJI EP 2 966 067 B1 PATENTNI ZAHTEVKI1. Sestavek, ki vsebuje spojino s formulo I v kombinaciji z vsaj enim terapevtskim sredstvom:kjer: -Υ-Ζ- is -C(=NR4)-NR2- ali -C(NR5R6)=N-; R1 je aril, cikloalkil, cikloalkenil, heterociklil ali heteroaril; kjer so omenjeni aril, cikloalkil, cikloalkenil, heterociklil ali heteroaril po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, -CN, -SFs,-Si(CH3)3, -O-R20 -S-R20, -C(0)-R20, -C(0)-0R20, -N(R20)(R22), -C(O)-N(R20)(R22), -N(R20)-C(O)-R22, -N(R20)-C(O)-OR22, -N(R20) -S(=0)2-R26, -S(=0)2-R20, -0-S(=0)2-R20, -S(=O)2-N(R20)(R22), Ci-e alkil, C2-4alkenil, C2-4 alkinil, cikloalkil, aril, heteroaril in heterociklil; in kjer so omenjeni C1-6 alkil, C2-4alkenil, C2-4 alkinil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo of halo, -N02, fenil, heterociklil, heteroaril, Ci-e alkil, cikloalkil, -N(R20)(R22), -C(0)-R2°, -C(0)-0R2°, -C(0)-N(R2°), -CN in -O-R20; R2je vodik, Ci-ealkil, -C(0)-R2°, -C(0)-0R26, -C(O)- N(R26)(R26), -N(R20)-S(=O)2-R20, cikloalkil, aril, heteroaril ali heterociklil; kjer so omenjeni Ci-e alkil, cikloalkil, aril, heteroaril ali po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo Ci-e alkil, C^alkinil, halo, -NO2, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(O)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN, okso in -O-R20; kjer so omenjeni Ci-ealkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo of halo, -NO2, Ci-ealkil, cikloalkil, aril, heterociklil, heteroaril,-N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)- N(R20)(R22), -CN and-O-R20; in kjer so omenjeni Ci-ealkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, -CFe, -N(R20)(R22), -C(0)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN, -S(0)2-R2° in-O-R20; n je 0, 1, 2, 3 ali 4; vsak R3je neodvisno Ci-ealkil, cikloalkil, aril, heteroaril ali heterociklil; kjer je omenjeni Ci-e alkil po izbiri substituiran z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, cikloalkil, aril, heterociklil, heteroaril,-N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; kjer so omenjeni cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, C1-6 alkil, aralkil, cikloalkil, aril,heterociklil, heteroaril, -N(R20)(R22), -C(O)- R20, -C(O)-OR20,-C(O)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni C1-6 alkil, aralkil, cikloalkil, aril, heterociklil ali heteroaril, po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo,-NC>2, -N(R20)(R22), -C(0)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN in -O-R20; ali dve R3 pripeti k skupnemu atomu ogljika oblikujeta okso; ali dve R3 pripeti k skupnim ali sosednjim atomom ogljika oblikujeta cikloalkil or heterociklil; kjer sta omenjena cikloalkil ali heterociklil po izbiri nadalje substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ci-β alkil, aralkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(0)-R20, -C(0)-0R2°, -C(O)-N(R20)(R22), -CN in -O-R20; R4 je C1-6 alkil, cikloalkil, aril, heteroaril or heterociklil; kjer so omenjeni Ci-β alkil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)-N(R20)(R20), -CN in -O-R20; kjer so omenjeni cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ci-ealkil, aralkil, cikloalkil, aril,heterociklil, heteroaril, -N(R20)(R22), -C(O)- R20, -C(O)-OR20,-C(O)-N(R20)(R22),-CN in -O-R20; in kjer so omenjeni Ci-β alkil, aralkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo,-N02, -N(R20)(22 -C(0)-R20, -C(0)-0R2°, -C(O)-N(R20)(R20), -CN in -O-R20; ali R2 in R4 sta lahko združeni z atomom k kateremu sta pripeti, da oblikujeta heterociklil ali heteroaril; kjer sta omenjena heterociklil ali heteroaril po zbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, Ci-ealkil, cikloalkil, heteroaril, -CN,-0-r2°,-n(r2°)(r22)i -C(0)-R2°, -N(R20)-C(O)-OR20in -C(0)-0R2°; in kjer sta omenjena C1 e alkil ali heteroaril po izbiri substituirana z enim, dvema ali tremi substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo, -CN, -O-R20, Ci-ealkil, aril, in heteroaril; R5 je vodik, Ci-ealkil, cikloalkil, aril, heteroaril ali heterociklil; kjer so omenjeni Ci-ealkil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)-N(R20)(R20), -CN in -O-R20; kjer so omenjeni cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, C1-6 alkil, aralkil, cikloalkil, aril, heterociklil, heteroaril,-N(R20)(R22), -C(O)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni C1-6 alkil, aralkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo,-NO2, -N(R20)(R22), -C(0)-R20, -C(0)-0R2°; R6 je C1-6 alkil, cikloalkil, aril, heteroaril ali heterociklil; kjer so omenjeni C1-6alkil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, C1-6 alkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(0)-R20, -C(0)-0R2°, -C(O)-N(R20)(R22), -CN in -O-R20; kjer so omenjeni C1-6 alkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ci-ealkil, aralkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(O)- R20, -C(0)-0R2°, -C(O)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni Ci-ealkil, aralkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo,-N02, N(R20)(R22), -C(0)-R20, -C(0)-0R20; ali R5 in R6 sta lahko združeni skupaj z atomom k kateremu sta pripeti da oblikujeta heterociklil ali heteroaril; kjer sta omenjena heterociklil ali heteroaril po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, Ci-ealkil, cikloalkil, heterociklil, aril, heteroaril, okso, -CN, -O-R20, -N(R20)(R22), -N(R20)- C(0)-R20, -N(R20)-C(O)-OR20in -C(0)-0R20; in kjer sta omenjena Ci-ealkil ali heterociklil po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, okao, heteroaril in -O-R20; R20 in R22 sta v vsakem primeru neodvisno izbrani iz skupine, ki jo sestavljajo vodik, Ci-ealkil, cikloalkil, heterociklil, aril and heteroaril; in kjer so Ci-ealkil, cikloalkil, heterociklil, aril in heteroaril po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo, C1-4 alkil, acilamino, okso, -NO2, -SO2R26, -CN, Ci-3alkoksi, ariloksi,-CF3, -OCF3, -OCH2CF3, -C(0)-NH2, aril, cikloalkil in heteroaril; kjer je omenjeni heteroaril po izbiri nadalje substituiran z Ci^alkilom ali cikloalkilom ; ali ko sta R20 in R22 pripeti na skupni atom dušika, lahko R20 in R22 združeni oblikujeta heterociklil ali heteroaril, ki sta nato po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo, C1-4 alkil, aralkil, ariloksi, aralkiloksi, acilamino, -N02.-S02R26, -CN, Ci-3alkoxy, -CFs, -OCFa, aril, heteroaril incikloalkil; in vsak R26je neodvisno izbran iz skupine, ki jo sestavljajo vodik, C1-4 alkil, aril in cikloalkil; kjer so C1-4 alkil, aril in cikloalkil lahko nadalje substituirani z 1 do 3 substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo, Ci-4alkoksi, -CFein -OCF3; ali njena farmacevtsko sprejemljiva sol, stereoizomera, mešanica stereoizomer ali tavtomera; pod pogojem da, ko sta R2 in R4 združeni z atomom k kateremu sta pripeti, da oblikujeta po izbiri substituiran imidazolil, imidazolil ni direktno substituiran z po izbiri substituiranim triazolilom, ali R1 ni po izbiri substituiran pirazolil, 2-piridinonil ali 2-fluoropiridinil.
- 2. Sestavek po zahtevku 1, kjer je spojina s formulo I predstavljena s formulo IA: kjer:R1 je aril, cikloalkil, cikloalkenil, heterociklil ali heteroaril; kjer so omenjeni ari), cikioalkil, cikloalkenil, heterociklil ali heteroaril po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, -CN, -SF5,-Si(CH3)3, -O-R20, -S-R20, -C(0)-R20, -C(0)-0R20, -N(R20)(R22), -C(O)- N(R20)(R22), -N(R20)-C(O)-R22, -N(R20)-C(O)-OR22,-N(R20)-S(=O)2-R26, -S(=0)2-R20, -O-S(=O)2-R220-S(=O)2-N(R20)(R22), Ci-e alkil, C2-4alkenil, C2-4 alkinil, cikioalkil, aril, heteroaril in heterociklil; in vvherein so omenjeni C1-6 alkil, C2-4alkenil, C2-4 alkinil, cikioalkil, aril, heteroaril or heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, fenil, heterociklil, heteroaril, C« alkil, cikioalkil, -N(R20)(R22), -C(0)-R2°, -C(O)-OR20, -C(O)-N(R20)(R22), -CN in -O-R20; R2 je vodik, Ci-e alkil, -C(0)-R2°, -C(0)-0R26, -C(O)- N(R26)(R26), -N(R20)-S(-O)2-R20, cikioalkil, aril, heteroaril ali heterociklil; kjer so omenjeni Ci-βalkil, cikioalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo C1-6 alkil, C2-4 alkinil, halo,-N02, cikioalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(O)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN, okso in -O-R20; kjer so omenjeni C1-6 alkil, cikioalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ci-ealkil, cikioalkil, aril, heterociklil, heteroaril,-N(R20)(R22), -C(0)-R2°, -C(0)-0R2°, -C(0)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni C1-6 alkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -N02.-CF3, -N(R20)(R22), -C(0)-R2°, -C(0)-0R20, -C(O)-N(R20)(R22), -CN, -S(O)2-R20in -O-R20; n je 0,1, 2, 3 ali 4; vsak R3je neodvisno Ci-β alkil, cikloalkil, aril, heteroaril or heterociklil; kjer je omenjeni Ci-β alkil po izbiri substituiran z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, cikloalkil, aril, heterociklil, heteroaril,-N(R20)(R22), -C(0)-R2°, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; kjer so omenjeni cikloalkil, aril, heterociklil ali heteroaril po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ci-β alkil, aralkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(0)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni C1-6 alkil, aralkil, cikloalkil, aril, heterociklil ali heteroaril, po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, -N(R20)(R22), -C(O)-R22, -C(O)-OR20,-C(O)-N(R20)(R22), -CN in -O-R20; ali dve R3 pripeti k skupnemu atomu ogljika oblikujeta okso; ali dve R3 pripeti k skupnim ali sosednjimi atomi ogljika oblikujeta cikloalkil or heterociklil; kjer sta omenjena cikloalkil ali heterociklil po izbiri nadalje substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ct-e alkil, aralkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(0)-R2°, -C(0)-OR2°, -C(O)-N(R20)(R22), -CN in -O-R20; R4 je C ι-e alkil, cikloalkil, aril, heteroaril or heterociklil; kjer so omenjeni C1-6 alkil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; kjer so omenjeni cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, C1-6 alkil, aralkil, cikloalkil, aril,heterociklil, heteroaril, -N(R20)(R22), -C(O)-R20, -C(O)-OR20,-C(O)-N(R20)(R22),-CN in -O-R20; in kjer so omenjeni Ci-βalkil, aralkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo,-N02, -N(R20)(R22), -C(0)-R2°, -C(0)-0R2°, -C(O)-N(R20)(R22), -CN in -O-R20; ali R2 in R4 sta lahko združeni z atomom k kateremu sta pripeti, da oblikujeta heterociklil ali heteroaril; **· · ·»*·«·· ··· « kjer sta omenjena heterociklil ali heteroaril po zbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, Ci-ealkil, cikloalkil, heteroaril, -CN.-O-R20, -N(R20)(R22), -C(0)-R20, -N(R20)-C(O)-OR20 in -C(0)-0R20; in kjer sta omenjena C1-6 alkil ali heteroaril po izbiri substituirana z enim, dvema ali tremi substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo, -CN, -O-R20, Ci-ealkil, aril, in heteroaril; R2° jn r2o sta v vsakem primeru neodvisno izbrani iz skupine, ki jo sestavljajo vodik, Ci-ealkil,cikloalkil, heterociklil, aril in heteroaril; in kjer so Ci-e alkil, cikloalkil, heterociklil, aril in heteroaril po zbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo, Cm alkil, acilamino, okso, -NO2, -SO2R26, -CN, Ci ealkoksi, ariloksi,-CF3, -OCF3, -OCH2CF3, -C(0)-NH2, aril, cikloalkil in heteroaril; kjer je omenjeni heteroaril nadalje substituiran s Cm alkilom ali cikloalkilom; ali kadar sta R20 in R22 pripeti na skupni atom dušika, se R20 in R22 lahko združita, da oblikujeta heterociklil ali heteroaril, ki sta nato po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo, Cm alkil, aralkil, ariloksi, aralkiloksi, acilamino, -NO2, - SO2R26, -CN, Ci salkoksi, -CF3, -OCF3, aril, heteroaril in cikloalkil; in vsak R26 je neodvisno izbran iz skupine, ki jo sestavljajo vodik, Cm alkil, aril in cikloalkil; --- - ··· ···· ··· 4 kjer so C1-4 alkil, aril in cikloalkil lahko nadalje substituirani z od 1 do 3 substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hdroksil, halo, Ci-4alkoksi, -CFein -OCF3; ali njena farmacevtsko sprejemljiva sol, stereoizomera, mešanica stereoizomer ali tavtomera; pod pogojem da ko sta R2in R4 združeni z atomom k kakteremu sta pripeia da oblikujeta po izbiri substituiran imidazolil, imidazolil ni direktno substituiran z po izbiri substituiranim triazolilom, ali R1 ni po izbiri substituiran pirazolil, 2-piridinonil ali 2-fluoropiridinil.
- 3. Spojina po zahtevku 2, kjer: R1 je aril, cikloalkil, cikloalkenil, heterociklil ali heteroaril; kjer so omenjeni aril, cikloalkil, cikloalkenil, heterociklil ali heteroaril po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, -CN,-SF5,-Si(CH3)3, -O-R20, -S-R20, -C(0)-R20, -C(0)-0R20, -N(R20)(R22), -C(O)-N(R20)(R22), -N(R20)-C(O)-R22, -N(R20)-C(O)-OR22, -N(R20)-S(=O)2-R26, -S(=0)2-R2°, -0-S(=0)2-R20, -S(=O)2-N(R20)(R22), Ci-e alkil, C2-4 alkenil, C2^t alkinil, cikloalkil, aril, heteroaril in heterociklil; in kjer so omenjeni C1-6 alkil, C2-4 alkenil, C2^t alkinil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, fenil, heterociklil, heteroaril, C1-6 alkil, cikloalkil, -N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(0)-N(RV)(R2), -CN in -O-R20; n je 0; in ··· · ··· ···· ··· R2 in R4 sta lahko združeni z atomom k kateremu sta pripeti, da oblikujeta heterociklil ali heteroaril; kjer sta omenjena heterociklil ali heteroaril po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, Ci-ealkil, cikloalkil, heteroaril, -CN.-O-R20, -N(R20)(R22), -C(0)-R20, -N(R20)-C(O)-OR20 in -C(0)-0R20; in kjer sta omenjena Ci-ealkil ali heteroaril po izbiri substituirana z enim, dvema ali tremi substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo, -CN, -O-R20, Ci-ealkil, aril, in heteroaril;
- 4. Spojina po zahtevku 2, kjer: R1 je aril; kjer so omenjeni aril, cikloalkil, cikloalkenil, heterociklil ali heteroaril po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, -CN,-SF5,-Si(CH3)3, -O-R20, -S-R20, -C(0)-R20, -C(0)-0R2°, -N(R20)(R22), -C(O)-N(R20)(R22), -N(R20)-C(O)-R22, -N(R20)-C(O)-OR22, -N(R20)-S(=O)2-R26, -S(=0)2- R20, -O-S(=O)2-R20,-S(=O)2-N(R20)(R22), Ci-e alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, aril, heteroaril in heterociklil; in kjer so omenjeni Ci-ealkil, C2-4alkenil, C2-4alkinil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -N02, fenil, heterociklil, heteroaril, Ci-ealkil, cikloalkil, -N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; n je 0; in R2 in R4 sta lahko združeni z atomom k kateremu sta pripeti, da oblikujeta heterociklil ali heteroaril; kjer sta omenjena heterociklil ali heteroaril po zbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, Ci-e alkil, cikloalkil, heteroaril, -CN.-O-R20, -N(R20)(R22), -C(0)-R20, -N(R20)-C(O)-OR20 in -C(0)-0R2°; in kjer sta omenjena C1-6 alkil ali heteroaril po izbiri substituirana z enim, dvema ali tremi substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo, -CN, -O-R20, C1-6 alkil, ari), in heteroaril;
- 5. Spojina po zahtevku 2, kjer: R1 je aril po izbiri substituiran z -O-R20 ali Ci-ealkilom; in kjer je omenjeni C1-6 alkil po izbiri substituiran z enim, dvema ali tremi halo; nje 0; R2 in R4 sta lahko združeni z atomom k kateremu sta pripeti, da oblikujeta heterociklil ali heteroaril; kjer sta omenjena heterociklil ali heteroaril po zbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, C1-6 alkil, cikloalkil, heteroaril, -CN.-O-R20 -N(R20)(R22)j.C(O)-R20, -N(R20)-C(O)-OR20in -C(0)-0R2°; in kjer sta omenjena Ci-β alkil ali heteroaril po izbiri substituirana z enim, dvema ali tremi substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo, -CN, -O-R20, C1-6 alkil, aril, in heteroaril.
- 6. Spojina po zahtevku 2, kjer: R1 je fenil substituiran z -0-CF3ali CF3; in n je 0; in R2 in R4 sta lahko združeni z atomom k kateremu sta pripeti, da oblikujeta heterociklil ali heteroaril; kjer sta omenjena heterociklil ali heteroaril po zbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, Ci-ealkil, cikloalkil, heteroaril, -CN.-O-R20, -N(R20), -C(0)-R20 in -C(0)-0R2°; in kjer sta omenjena Ci-e alkil ali heteroaril po izbiri substituirana z enim, dvema ali tremi substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo, -CN, -O-R20, Ci-ealkil, aril, in heteroaril.
- 7. Spojina po zahtevku 1, kjer je spojina s formulo I izbrana iz skupine, ki jo sestavljajo:ali njena farmacevtsko sprejemljiva sol, stereoizomera, mešanica stereoizomer ali tavtomera.
- 8. Sestavek po zahtevku 1, kjer je spojina s formulo I predstavljena s formulo IB:kjer: R1 je aril, cikloalkil, cikloalkenil, heterociklil ali heteroaril; kjer so omenjeni aril, cikloalkil, cikloalkenil, heterociklil ali heteroaril po zbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, -CN, -SFs, -Si(CH3)3, -O-R20, -S-R20, -C(0)-R20, -C(0)-0R20, -N(R20)(R22), -C(O)-N(R20)(R22), -N(R20)-C(O)-R22, -N(R20)-C(O)-OR22, -N(R20)-S(=0)2-R26, -S(=0)2-R20, -0-S(=0)2-R20, -S(=O)2-N(R20)(R22), C1-6 alkil, C2-4alkenil, C2-4 alkinil, cikloalkil, aril, heteroaril and heterociklil; in kjer so omenjeni C1-6 alkil, C2-4alkenil, C2-4 alkinil, cikloalkil, aril, heteroaril or heterociklil po zbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, fenil, heterociklil, heteroaril, Ci-e alkil, cikloalkil, -N(R20)(R22), -C(0)-R20, -C(0)-0R2°, -C(O)-N(R20)(R22), -CN in -O-R20; njeO, 1,2, 3 ali 4; vsak R3je neodvisno C1-6 alkil, cikloalkil, aril, heteroaril ali heterociklil; kjer je omenjeni Ci-e alkil po izbiri substituiran z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, cikloalkil, aril, heterociklil, heteroaril,-N(R20)(R22), -C(O)-R20, -C(0)-0R2°, -C(O)-N(R20)(R22), -CN in -O-R20; kjer so omenjeni cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, C1-6 alkil, aralkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(0)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni C1-6 alkil, aralkil, cikloalkil, aril, heterociklil ali heteroaril, po zbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo,-N02, -N(R20)(R22), -C(0)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN in -O-R20; ali dve R3 pripeti k skupnemu atomu ogljika oblikujeta okso; ali dve R3 pripeti k skupnim ali sosednjimi atomi ogljika oblikujeta cikloalkil ali heterociklil; kjer sta omenjena cikloalkil ali heterociklil po izbiri nadalje substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo,-NO2, C1-6 alkil, aralkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; R5 je vodik, C1-6 alkil, cikloalkil, aril, heteroaril ali heterociklil; kjer so omenjeni C1-6 alkil, cikloalkil, aril, heteroaril ali heterociklil po zbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, cikloalkil, aril, heterociklil, heteroaril,-N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; kjer so omenjeni cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2,Ci-ealkil, aralkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(O)- R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni Ci-ealkil, aralkil, cikloalkil, aril, heterociklil ali heteroaril, po zbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo,-N02, -N(R20)(R22), -C(0)-R2°, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; R6 je C1-6alkil, cikloalkil, aril, heteroaril or heterociklil; kjer so omenjeni Ci-e alkil, cikloalkil, aril, heteroaril ali heterociklil po zbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ci-e alkil, cikloalkil, aril, heterociklil, heteroaril,-N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; kjer so omenjeni Ci-ealkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2,Ci-ealkil, aralkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(O)- R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni C1-6 alkil, aralkil, cikloalkil, aril, heterociklil ali heteroaril, po zbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo,-NC>2, -N(R20)(R22), -C(0)-R20, -C(0)-0R20; ali R5 in R6 sta lahko združeni skupaj z atomom k kateremu sta pripeti, da oblikujejo heterociklil or heteroaril; kjer sta omenjena heterociklil ali heteroalkil po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ci-β alkil, cikloalkil, heterociklil, aril, heteroaril,okso -CN, -O-R20, -N(R20)(R22), -N(R20)-C(O)-R20, -N(R20)-C(O)-OR20, in -C(O)-O-R20; in kjer sta omenjena Ci-β alkil ali heterociklil po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, okso, heteroaril in -O-R20; R20 in R22 sta v vsakem primeru neodvisno izbrani iz skupine , ki jo sestavljajo vodik, C1-6 alkil, cikloalkil, heterociklil, aril in heteroaril; in kjer so C1-6 alkil, cikloalkil, heterociklil, aril in heteroaril po izbiri substituiraniz enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo, C1-4 alkil, acilamino, okso, -NO2, -SO2R26, -CN, Ci salkoksi, ariloksi.-CFs, -OCF3, -OCH2CF3, -C(0)-NH2, aril, cikloalkil in heteroaril; kjer je omenjeni heteroaril po izbiri nadalje substituiran s C1-4 alkilom ali cikloalkilom ; ali kadar sta R20 in R22 pripeti na skupni atom dušika, se R20 in R22 lahko združita da oblikujeta heterociklil ali heteroaril, ki sta nato po izbiri substituirana z enim, ··· · dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo, Cm alkil, aralkil, ariloksi, aralkiloksi, acilamino, -N02,-S02R26, -CN, Ci salkoksi, -CF3, -OCF3, aril, heteroaril in cikloalkil; in vsak R26 je neodvisno izbran iz skupine, ki jo sestavljajo vodik, Cm alkil, aril in cikloalkil; kjer so Cm alkil, aril in cikloalkil po izbiri substituirani z 1 do 3 substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo, CMalkoksi, -CF3 in -OCF3; ali njena farmacevtsko sprejemljiva sol, stereoizomera, mešanica stereoizomer ali tavtomera..
- 9. Sestavek po zahtevku 8, kjer: R1 je aril, cikloalkil, cikloalkenil, heterociklil ali heteroaril; kjer so omenjeni aril, cikloalkil, cikloalkenil, heterociklil ali heteroaril po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, -CN, -SF5,-Si(CH3)3, -O-R20, -S-R20, -C(0)-R20, -C(0)-0R2°, -N(R20)(R22), -C(O)-N(R20)(R22), -N(R20)-C(O)-R22, -N(R20)-C(O)-OR22, -N(R20)-S(=O)2-R26, -S(=0)2-R2°, -0-S(=0)2-R2°, -S(=O)2-N(R20)(R22), C1-6 alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, aril, heteroaril in heterociklil; in kjer so omenjeni C1-6 alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, fenil, heterociklil, heteroaril, C1-6 alkil, cikloalkil, -N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; nje 0; R5 je vodik ali Ci-β alkil; in R6je Ci-e alkil, cikloalkil, aril, heteroaril ali heterociklil; kjer so omenjeni C1-6 alkil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, C1-6 alkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; kjer so omenjeni C1-6 alkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, C1-6 alkil, aralkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(O)- R20, -C(0)-0R2°, -C(O)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni C1-6 alkil, aralkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo,-N02, -N(R20)(R22), -C(0)-R20, -C(0)-0R20; ali R5 in R6 sta lahko združeni skupaj z atomom k kateremu sta pripeti, da oblikujejo heterociklil or heteroaril; kjer sta omenjena heterociklil ali heteroaril po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, Ci-β alkil, cikloalkil, heterociklil, aril, heteroaril, okso, -CN, -O-R20, -N(R20)(R22), -N(R20)-C(O)-R20, -N(R20)-C(O)-OR20 in -C(0)-0R2°; in kjer sta omenjena Ci-e alkil ali heterociklil po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo, okso, heteroaril in -O-R20.
- 10. Sestavek po zahtevku 8, kjer: Rije aril; kjer je omenjeni aril po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, -CN, -SFs, -Si(CH3)3, -O-R20, -S-R20, -C(0)-R2°, -C(0)-0R2°, -N(R20)(R22), -C(O)-N(R20)(R22), -N(R20)-C(O)-R22, -N(R20)-C(O)-OR22, -N(R20)-S(=O)2-R26, -S(=0)2-R20, -0-S(=0)2- R20, -S(-O)2-N(R20)(R22), C1-6 alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, aril, heteroaril and heterociklil; in kjer so omenjeni C1-6 alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, fenil, heterociklil, heteroaril, C1-6 alkil, cikloalkil, -N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; nje 0; R5je vodik ali C1-6 alkil; in R6je C1-15 alkil, cikloalkil, aril, heteroaril ali heterociklil; kjer so omenjeni C1-6 alkil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, C1-6 alkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(0)-R2°, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; kjer so omenjeni C1-6 alkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ci-e alkil, aralkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(O)- R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni C1-6 alkil, aralkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo,-N02, -N(R20)(R22), -C(0)-R20, -C(0)-0R2°; ali R5 in R6 sta lahko združeni skupaj z atomom k kateremu sta pripeti, da oblikujejo heterociklil or heteroaril; kjer sta omenjena heterociklil ali heteroaril po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, C1-6alkil, cikloalkil, heterociklil, aril, heteroaril, okso, -CN, -OR20, -N(R20)(R22), -N(R20)-C(O)-R20, -N(R20)-C(O)-OR20 in -C(0)-0R2°; in kjer sta omenjena C1-6 alkil ali heterociklil po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, okso, heteroaril in -O-R20.
- 11. Sestavek po zahtevku 8, kjer: R1 je aril po izbiri substituiran z -O-R20 ali Ci-ealkilom; in kjer je omenjeni Ci-e alkii po izbiri substituiran z enim, dvema ali tremi haloi; n je 0; R5je vodik ali Ci-ealkil; in R6je C1-6alkii, cikloalkil, aril, heteroaril ali heterociklil; kjer so omenjeni Ci-e alkii, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ci-e alkii, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; kjer so omenjeni C1-6alkii, cikloalkil, aril, heterociklil ali heteroaril po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ci-ealkil, aralkil, cikloalkil, aril, heterociklil, heteroaril, -N(R2o)(R22), -C(O)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni Ci-ealkil, aralkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo,-N02, -N(R20)(R22), -C(0)-R20, -C(0)-0R20; ali R5 in R6 sta lahko združeni skupaj z atomom k kateremu sta pripeti, da oblikujejo heterociklil ali heteroaril; kjer sta omenjena heterociklil ali heteroaril po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, Ci-ealkil, cikloalkil, heterociklil, aril, heteroaril, okso, -CN, -O-R20, -N(R20)(R22), -N(R20)-C(O)-R20, -N(R20)-C(O)-OR20 in -C(0)-0R20; in kjer sta omenjena Ci-ealkil ali heterociklil po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, okso, heteroaril in -O-R20.
- 12. Sestavek po zahtevku 8, kjer: Rije fenil substituiran z -0-CF3ali -CF3; nje 0; R5je vodik ali Ci-ealkil; in R6je Ci-ealkil, cikloalkil, aril, heteroaril ali heterociklil; kjer so omenjeni Ci-e alkil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ci-e alkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(0)-R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; kjer so omenjeni Ci-ealkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ci-ealkil, aralkil, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(O)- R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni Ci-ealkil, aralkil, cikloalkil, aril, heterociklil ali heteroaril po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo,-N02, -N(R20)(R22), -C(0)-R20, -C(0)-0R2°; ....... ali R5 in R6 sta lahko združeni skupaj z atomom k kateremu sta pripeti, da oblikujejo heterociklil ali heteroaril; kjer sta omenjena heterociklil ali heteroaril po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, C-i-6 alkil, cikloalkil, heterociklil, aril, heteroaril, okso, -CN, -OR20, -N(R20)(R22), -N(R20)-C(O)-R20, -N(R20)-C(O)-OR20 in -C(0)-0R20; in kjer sta omenjena Ci-ealkil ali heterociklil po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, okso, heteroaril in -O-R20.
- 13. Sestavek po zatevku 8 kjer sta skupini R5 in R6 združeni skupaj z atomom k kateremu sta pripeti, da oblikujejo heterociklilno skupino, izbrano izmed skupine, ki jo sestavljajo*·· ···· e··kjer je točka zdužitve k oksazepinskem obroču pri bivalentnem atomu dušika, kot je narisano.
- 14. Sestavek po zahtevku 1, kjer sta R2 in R4 združeni skupaj z atomom k kateremu sta pripeti, da oblikujejo heterociklil ali heteroaril izbran iz skupine, ki jo sestavljajokjer lomljene linije označujejo točke pripetja k oksazepinskemu obroču da oblikujejo triciklično skupino.
- 15. Sestavek po zahtevku 8, kjer je spojina s formulo I izbrana iz skupine, ki jo sestavljajo:ali njena farmacevtsko sprejemljiva sol, stereoizomera, mešanica stereoizomer ali tavtomera.
- 16. Sestavek, ki vsebuje spojino s formulo VII v kombinaciji z vsaj enim terapevtskim sredstvom:kjer: n is 0, 1, 2 ali 3: vsak R10 je neodvisno izbran iz skupine, ki jo sestavljajo halo, -N02.-CN, -SFs, -Si(CH3)3, -O-R20, -S-R20, -C(0)-R2°, -C(O)- OR20, -N(R20)(R22), -C(O)-N(R20)(R22), -N(R20)-C(O)-R22, -N(R20)-C(O)-OR22, -N(R20)-S(=O)2-R26, -S(=0)2-R20, -S(=O)2-N(R20)(R22), Ci-6 alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, aril, heteroaril inheterociklil; in kjer so omenjeni C1-6 alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, fenil, heterociklil, heteroaril, C1-6 alkil, cikloalkil, -N(R20)(R22), -C(0)-R20, -C(0)-0R2°, -C(O)-N(R20)(R22), -CN in -O-R20; R2je vodik, C1-« alkil, -C(0)-R2°, -C(0)-0R26, -C(O)- N(R26)(R28), -N(R20)-S(=O)2-R20, cikloalkil, aril, heteroaril or heterociklil; kjer so omenjeni C1-15 alkil, cikloalkil, aril, heteroaril ali heterociklil po izbiri substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo C1-6 alkil, C2-4 alkinil, halo, -NO2, cikloalkil, aril, heterociklil, heteroaril, -N(R20)(R22), -C(O)- R20, -C(0)-0R20, -C(O)-N(R20)(R22), -CN, okso in -O-R20; kjer so omenjeni Ci-β alkil, cikloalkil, aril, heterociklil ali heteroarii po izbiri nadalje substituirani z enim, dvema ali tremi substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, Ci-e alkil, cikloalkil, aril, heterociklil, heteroarii,-N(R20)(R22), -C(0)-R2°, -C(0)-0R2°, -C(O)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni Ci-e alkil, cikloalkil, aril, heterociklil ali heteroarii po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, -CF3, -N(R20)(R22), -C(0)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN, -S(0)2-R2° in-O-R20; R5je vodik, C1-15 alkil, Ci-4alkoksi, -C(0)-0-R26, -C(O)- N(R26)(R28), -N(R20)-S(=O)2-R20, cikloalkil, aril, heteroarii or heterociklil; kjer je omenjeni C1-15 alkil po izbiri substituiran z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, cikloalkil, aril, heterociklil, heteroarii,-N(R20)(R22), -C(0)-R2°, -C(O)- OR20, -C(O)-N(R20)(R22), -CN in -O-R20; kjer so omenjeni cikloalkil, aril, heterociklil ali heteroarii po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo halo, -NO2, C1-6 alkil, aralkil, cikloalkil, aril, heterociklil, heteroarii, -N(R20)(R22), -C(0)-R20, -C(O)-OR20, -C(O)-N(R20)(R22), -CN in -O-R20; in kjer so omenjeni Ci-e alkil, aralkil, cikloalkil, aril, heterociklil ali heteroarii po izbiri nadalje substituirani z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo,-N02, -N(R20)(R22), -C(O)-R20, -C(0)-OR2o, -C(0)-N(R2o)(R22), -CN in -O-R20; ali R2 in R5 sta lahko združeni skupaj z atomom k kateremu sta pripeti, da oblikujejo heterociklil or heteroaril; kjer sta omenjena heterociklil ali heteroaril po izbiri substituirana z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo O1-15 alkil, cikloalkil, heteroaril, -O-R20,-N(R20)(R22), -N(R20)-C(O)-OR20 in -C(0)-0R2°; in kjer je omenjeni C1-15 alkil po izbiri substituiran z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljata halo in heteroaril; R20 in R22 sta v vsakem primeru neodvisno izbrani iz skupine, ki jo sestavljajo vodik, C1 -15 alkil, C2-is alkenil, C2-15 alkinil, cikloalkil, heterociklil, aril in heteroaril; in kjer so C1-15 alkil, C2-is alkenil, C2-is alkinil, cikloalkil, heterociklil, aril, in heteroaril po izbiri substituirani z enim, dvema ali tremi substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo, C1-4 alkil, acilamino, -N02, -S02R26, -CN, CMalkoksi, -CFs, -OCFs, -OCI-hCFa, -C(O)-NH2, aril, cikloalkil and heteroaril; kjer je omenjeni heteroaril po izbiri nadalje substituiran s Ci-4alkilom ali cikloalkilom; ali kadar sta R20 in R22 pripeti k skupnemu atomu dušika , R20 in R22 se lahko združita da oblikujeta heterociklični ali heteroarilni obroč, ki je nato po izbiri nadalje substituiran z enim, dvema ali tremi substituenti neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo, C1-4 alkil, aralkil, aril, ariloksi, aralkiloksi, acilamino, -NO2, -SO2R26, -CN, C1-3 alkoksi, -CF3, -OCF3, aril, heteroaril in cikloalkil; R25 je v vsakem primeru neodvisno kovalentna vez ali C1-3 alkilen, po izbiri substituiran z eno ali dvema Ci-salkilnima skupinama; in R26 in R28 sta v vsakem primeru neodvisno izbrana iz skupine, ki jo sestavljajo vodik, C1-4 alkil, aril in cikloalkil; in kjer so C1-4 alkil, aril in cikloalkil lahko nadalje substituirani od 1 do 3 substituenti, neodvisno izbranimi iz skupine, ki jo sestavljajo hidroksil, halo, C1-4 alkoksi, -CFein -OCF3; ali njena farmacevtsko sprejemljiva sol, ester, hidrat, solvate, stereoizomera, mešanica stereoizomer, tavtomera in/ali polimorf.
- 17. Sestavek po zahtevku 16, kjer kadar se R2 in R5 združita skupaj z atomom k kateremu sta pripeti, tvorita po izbiri substituiran imidazolil, imidazolil ni neposredno substituiran s po izbiri substituiranim triazolilom, ali R1 ni po izbiri substituiran pirazolil, 2-piridinonil ali 2-fluoropiridinil.
- 18. Sestavek po zahtevku 16, ki vsebuje N-(ciklopropilmetil)-7-(4-(trifluorometil) fenil)-2,3-dihidrobenzo[f][1,4]-oksazepin-5-amin ali njeno farmacevtsko sprejemljivo soli.
- 19. Sestavek po zahtevku 16, ki vsebuje (R)-tert-butil 3-(7-(4-(trifluorometil) fenil)-2,3-dihidrobenzo[f][1,4]5-ilamino)pirolidin-1-karboksilat ali njeno farmacevtsko sprejemljivo sol.
- 20. Sestavek po kateremkoli od zahtevkov 1 do 19 za uporabo pri terapiji.
- 21. Sestavek po katerem koli od zahtevkov 1 do 19 za uporabo pri zdravljenju bolezni, ki so povezane s kardiovaskularno boleznijo ali stanji, prednostno angino, vključno s stabilno angino pektoris, nestabilno angino pektoris, anksiozno indukcijsko angino pektoris, variantno angino pektoris, aritmijami, prekinitvenimi klavdikacijami, miokardnim infarktom, vključno z miokardnim infarktom brez STE, pljučno hipertenzijo, vključno s pljučno arterijsko hipertenzijo, srčnim popuščanjem, vključno s kongestivnim srčnim popuščanjem in diastoličnim srčnim popuščanjem in srčnim popuščanjem z ohranjenim izmetalnim delom, akutnim srčnim popuščanjem ali ponavljajočo se ishemijo.
- 22. Sestavek za uporabo po zahtevku 21, kjer je drugo terapevtsko sredstvo izbrano iz skupine, ki jo sestaljajo anti-anginali, sredstva za srčno popuščanje, antitrombotična sredstva, antiaritmična sredstva, antihipertenzijska sredstva in sredstva za zniževanje lipidov.
- 23. Sestavek po kateremkoli od zahtevkov 1 do 19 za uporabo pri zdravljenju pljučnih motenj, prednostno astme, kronične obstruktivne pljučne bolezni, bronhitisa in emfizema.
- 24. Sestavek za uporabo po zahtevku 23, kjer drugo terapevtsko sredstvo izbrano iz skupine, ki jo sestavljajo agonisti beta2, antiholinergiki, kortikosteroidi in elektrolitski dodatki.
- 25. Sestavek po katerem koli od zahtevkov 1 do 19 za uporabo pri zdravljenju metabolnih motenj, prednostno diabetesa, vključno s sladkorno boleznijo tipa I in tipa II, metaboličnega sindroma, dislipidemije, debelosti, intolerance za glukozo, hipertenzije, povišanega serumskega holesterola in povišanih trigliceridov.
- 26. Sestavek za uporabo po zahtevku 25, kjer je drugo terapevtsko sredstvo izbrano iz skupine, ki jo sestavljajo antihipertenzivi, sredstva za zniževanje lipidov, inzulin, sulfonilsečnine, bigvanide, alfa-glukozidazni inhibitorji in inkretinski mimetiki.
- 27. Sestavek po kateremkoli od zahtevkov 1 do 19 za uporabo pri zdravljenju gastrointestinalnih motenj, prednostno gastroezofagealne refluksne bolezni (GERD), vnetne črevesne bolezni (IBD), gastroenteritisa, gastritisa in peptične ulkusne bolezni in pankreatitisa.
- 28. Sestavek za uporabo po zahtevku 27, kjer je drugo terapevtsko sredstvo izbrano iz skupine, ki jo sestavljajo inhibitorji protonske črpalke, inhibitorji H2, prostaglandini in antacidi.
- 29. Sestavek za uporabo v terapiji po zahtevku 20, kjer je drugo terapevtsko sredstvo izbrano iz skupine, ki jo sestavljajo antibiotiki, analgetiki, antidepresivi in sredstva proti anksioznosti.
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TW201613908A (en) | 2014-02-13 | 2016-04-16 | Gilead Sciences Inc | Solid forms of an ion channel modulator |
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