HRP20220331T1 - Spojevi aminopirazin diola kao inhibitori pi3k-y - Google Patents

Spojevi aminopirazin diola kao inhibitori pi3k-y Download PDF

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HRP20220331T1
HRP20220331T1 HRP20220331TT HRP20220331T HRP20220331T1 HR P20220331 T1 HRP20220331 T1 HR P20220331T1 HR P20220331T T HRP20220331T T HR P20220331TT HR P20220331 T HRP20220331 T HR P20220331T HR P20220331 T1 HRP20220331 T1 HR P20220331T1
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Stacey Shepard
Andrew P. Combs
Nikoo Falahatpisheh
Lixin Shao
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Incyte Corporation
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Claims (19)

1. Spoj, naznačen time, da je predstavljen Formulom (I): [image] ili njegova farmaceutski prihvatljiva sol; u kojoj: X1 je N ili CR1; R1 se bira od sljedećih: H, D, halogen, C1-6 alkil, C1-6 alkoksi, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C1-6 haloalkoksi, CN, OH, i NH2; R2 je C(O)NRc1Rd1; svaki od R3, R4 i R5 se neovisno bira od sljedećih: H, D, halogen, CN, OH, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkoksi, C1-6 haloalkoksi, cijano-C1-6 alkil, HO-C1-6 alkil, C1-6 alkoksi-C1-6 alkil, C3-6 cikloalkil, amino, C1-6 alkilamino, di(C1-6 alkil)amino, i C(O)NRc Rd, pri čemu je C1-6 alkil opcionalno supstituiran s 1, 2, 3, 4, 5, ili 6 D; svaki od R6, R7 i R8 se neovisno bira od sljedećih: H, D, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-10 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, (4-10-člani heterocikloalkil)-C1-6 alkil-, C(O)Rb3, C(O)NRc3 Rd3, C(O)NRc3 (ORa3), C(O)ORa3, C(=NRe3)Rb3, C(=NOH)Rb3, C(=NCN)Rb3, i C(=NRe3)NRc3Rd3, pri čemu je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-10 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od R6, R7, i R8, opcionalno supstituiran s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RB supstituenata; i pri čemu je C1-6 haloalkil od R6, R7, ili R8 opcionalno supstituiran s 1, 2, 3, ili 4 neovisno odabrana Y supstituenta; svaki Y se neovisno bira od D, halogena, C1-6 alkila, i C1-6 haloalkila; ili R6 i R7 supstituenti, zajedno s prstenovim atomima s kojima su vezani, tvore C3-10 cikloalkil ili 4-7-člani heterocikloalkil, od kojih je svaki opcionalno supstituiran s 1, 2, 3, ili 4 neovisno odabrana RB supstituenta; ili R7 i R8 supstituenti, zajedno s prstenovim atomima s kojima su vezani, tvore C3-10 cikloalkil ili 4-7-člani heterocikloalkil, od kojih je svaki opcionalno supstituiran s 1, 2, 3, ili 4 neovisno odabrana RB supstituenta; svaki od Rc i Rd se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-, pri čemu je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od Rc i Rd, opcionalno supstituiran s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RM supstituenata; svaki od Rc1 i Rd1 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C3-10 cikloalkil, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-10 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-, pri čemu je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-10 cikloalkil, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-10 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od Rc1 i Rd1, opcionalno supstituiran s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RA supstituenata; ili bilo koji od Rc1 i Rd1, koji je vezan na isti N atom, zajedno s N atomom s kojim su vezani, tvore 4-članu, 5-članu, 6-članu, ili 7-članu heterocikloalkil skupinu, pri čemu je 4-člana, 5-člana, 6-člana, ili 7-člana heterocikloalkil skupina opcionalno supstituirana s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RA supstituenata; svaki od Ra3, Rb3, Rc3, i Rd3 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-10 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-, pri čemu je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-10 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od Ra3, Rb3, Rc3, i Rd3, opcionalno supstituiran s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RB supstituenata; ili bilo koji od Rc3 i Rd3, koji je vezan na isti N atom, zajedno s N atomom s kojim su vezani, tvore 5-članu ili 6-članu heteroaril skupinu ili 4-članu, 5-članu, 6-članu, ili 7-članu heterocikloalkil skupinu, pri čemu je 5-člana ili 6-člana heteroaril skupina, ili 4-člana, 5-člana, 6-člana, ili 7-člana heterocikloalkil skupina opcionalno supstituirana s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RB supstituenata; svaki Re3 se neovisno bira od sljedećih: H, OH, CN, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, C1-6 haloalkoksi, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-10 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-; svaki RA se neovisno bira od sljedećih: D, halogen, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, (4-10-člani heterocikloalkil)-C1-6 alkil-, CN, NO2, ORa4, SRa4, NHORa4, C(O)Rb4, C(O)NRc4Rd4, C(O)NRc4(ORb4), C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4NRc4Rd4, NRc4C(O)Rb4, NRc4C(O)ORa4, NRc4C(O)NRc4Rd4, C(=NRe4)Rb4, C(=NOH)Rb4, C(=NCN)Rb4, C(=NRe4)NRc4Rd4, NRc4C(=NRe4)NRc4Rd4, NRc4C(=NRe4)Rb4, NRc4C(=NOH)NRc4Rd4, NRc4C(=NCN)NRc4Rd4, NRc4S(O)Rb4, NRc4S(O)NRc4Rd4, NRc4S(O)2Rb4, NRc4S(O)2NRc4Rd4, S(O)Rb4, S(O)NRc4Rd4, S(O)2Rb4, S(O)2NRc4Rd4, OS(O)(=NRe4)Rb4, OS(O)2Rb4, SF5, P(O)Rf4Rg4, OP(O)(ORh4)(ORi4), P(O)(ORh4)(ORi4), i BRj4Rk4, pri čemu su C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od RA, opcionalno supstituirani s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RD supstituenata; svaki RB se neovisno bira od sljedećih: D, halogen, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, (4-10-člani heterocikloalkil)-C1-6 alkil-, CN, NO2, ORa2, SRa2, NHORa2, C(O)Rb2, C(O)NRc2Rd2, C(O)NRc2(ORb2), C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, C(=NRe2)Rb2, C(=NOH)Rb2, C(=NCN)Rb2, C(=NRe2)NRc2Rd2, NRc2C(=NRe2)NRc2Rd2, NRc2C(=NRe2)Rb2, NRc2C(=NOH)NRc2Rd2, NRc2C(=NCN)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)NRc2Rd2, NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, S(O)2NRc2Rd2, OS(O)(=NRe2)Rb2, OS(O)2Rb2, SF5, P(O)Rf2Rg2, OP(O)(ORh2)(ORi2), P(O)(ORh2)(ORi2), i BRj2Rk2, pri čemu su C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od RB, opcionalno supstituirani s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RM supstituenata; svaki od Ra2, Rb2, Rc2, i Rd2 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-, pri čemu je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od Ra2, Rb2, Rc2, i Rd2, opcionalno supstituiran s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RM supstituenata; ili bilo koji od Rc2 i Rd2 koji je vezan na isti N atom, zajedno s N atomom s kojim su vezani, tvore 5-članu ili 6-članu heteroaril skupinu ili 4-članu, 5-članu, 6-članu, ili 7-članu heterocikloalkil skupinu, pri čemu je 5-člana ili 6-člana heteroaril skupina, ili 4-člana, 5-člana, 6-člana, ili 7-člana heterocikloalkil skupina opcionalno supstituirana s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RM supstituenata; svaki Re2 se neovisno bira od sljedećih: H, OH, CN, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, C1-6 haloalkoksi, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-; svaki od Rf2 i Rg2 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, C1-6 haloalkoksi, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-; svaki od Rh2 i Ri2 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-; svaki od Rj2 i Rk2 se neovisno bira od OH, C1-6 alkoksi, i C1-6 haloalkoksi; ili bilo koji od Rj2 i Rk2 koji je vezan na isti B atom, zajedno s B atomom s kojim su vezani, tvore 5-članu ili 6-članu heterocikloalkil skupinu opcionalno supstituiranu s 1, 2, 3, ili 4 supstituenta neovisno odabrana od C1-6 alkila i C1-6 haloalkila; svaki od Ra4, Rb4, Rc4, i Rd4 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-, pri čemu je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od Ra4, Rb4, Rc4, i Rd4, opcionalno supstituiran s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RD supstituenata; ili bilo koji od Rc4 i Rd4 koji je vezan na isti N atom, zajedno s N atomom s kojim su vezani, tvore 5-članu ili 6-članu heteroaril skupinu, ili 4-članu, 5-članu, 6-članu, ili 7-članu heterocikloalkil skupinu, pri čemu je 5-člana ili 6-člana heteroaril skupina, ili 4-člana, 5-člana, 6-člana, ili 7-člana heterocikloalkil skupina opcionalno supstituirana s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RD supstituenata; svaki Re4 se neovisno bira od sljedećih: H, OH, CN, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, C1-6 haloalkoksi, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-; svaki od Rf4 i Rg4 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, C1-6 haloalkoksi, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-; svaki od Rh4 i Ri4 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-; svaki od Rj4 i Rk4 se neovisno bira od OH, C1-6 alkoksi, i C1-6 haloalkoksi; ili bilo koji od Rj4 i Rk4 koji je vezan na isti B atom, zajedno s B atomom s kojim su vezani, tvore 5-članu ili 6-članu heterocikloalkil skupinu opcionalno supstituiranu s 1, 2, 3, ili 4 supstituenta neovisno odabrana od C1-6 alkila i C1-6 haloalkila; svaki RD se neovisno bira od sljedećih: H, D, halogen, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, (4-10-člani heterocikloalkil)-C1-6 alkil-, CN, NO2, ORa5, SRa5, NHORa5, C(O)Rb5, C(O)NRc5Rd5, C(O)NRc5(ORb5), C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)ORa5, NRc5C(O)NRc5Rd5, C(=NRe5)Rb5, C(=NOH)Rb5, C(=NCN)Rb5, C(=NRe5)NRc5Rd5, NRc5C(=NRe5)NRc5Rd5, NRc5C(=NRe5)Rb5, NRc5C(=NOH)NRc5Rd5, NRc5C(=NCN)NRc5Rd5, NRc5S(O)Rb5, NRc5S(O)NRc5Rd5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rc5, S(O)2NRc5Rd5, OS(O)(=NRe5)Rb5, OS(O)2Rb5, SF5, P(O)Rf5Rg5, OP(O)(ORh5)(ORi5), P(O)(ORh5)(ORi5), i BRj5Rk5, pri čemu je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od RD, opcionalno supstituiran s 1, 2, 3, ili 4 neovisno odabrana RE supstituenta; svaki Ra5, Rb5, Rc5, i Rd5 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-, pri čemu je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od Ra5, Rb5, Rc5, i Rd5, opcionalno supstituiran s 1, 2, 3, ili 4 neovisno odabrana RE supstituenta; ili bilo koji od Rc5 i Rd5 koji je vezan na isti N atom, zajedno s N atomom s kojim su vezani, tvore 5-članu ili 6-članu heteroaril skupinu ili 4-članu, 5-članu, 6-članu, ili 7-članu heterocikloalkil skupinu, pri čemu je 5-člana ili 6-člana heteroaril skupina ili 4-člana, 5-člana, 6-člana, ili 7-člana heterocikloalkil skupina opcionalno supstituirana s 1, 2, 3, ili 4 neovisno odabrana RE supstituenta; svaki Re5 se neovisno bira od sljedećih: H, OH, CN, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, C1-6 haloalkoksi, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-; svaki od Rf5 i Rg5 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, C1-6 haloalkoksi, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10 -člani heterocikloalkil)-C1-6 alkil-; svaki od Rh5 i Ri5 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-; svaki od Rj5 i Rk5 se neovisno bira od OH, C1-6 alkoksi, i C1-6 haloalkoksi; ili bilo koji od Rj5 i Rk5 koji je vezan na isti B atom, zajedno s B atomom s kojim su vezani, tvore 5-članu ili 6-članu heterocikloalkil skupinu opcionalno supstituiranu s 1, 2, 3, ili 4 supstituenta neovisno odabrana od C1-6 alkila i C1-6 haloalkila; svaki RE se neovisno bira od sljedećih: H, D, halogen, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-, CN, NO2, ORa6, SRa6, NHORa6, C(O)Rb6, C(O)NRc6Rd6, C(O)NRc6(ORb6), C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)ORa6, NRc6C(O)NRc6Rd6, C(=NRe6)Rb6, C(=NOH)Rb6, C(=NCN)Rb6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, NRc6C(=NRe6)Rb6, NRc6C(=NOH)NRc6Rd6, NRc6C(=NCN)NRc6Rd6, NRc6S(O)Rb6, NRc6S(O)NRc6Rd6, NRc6S(O)2Rb6, NRc6S(O)2NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rc6, S(O)2NRc6Rd6, OS(O)(=NRe6)Rb6, OS(O)2Rb6, SF5, P(O)Rf6Rg6, OP(O)(ORh6)(ORi6), P(O)(ORh6)(ORi6), i BRj6Rk6, pri čemu je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od RE, opcionalno supstituiran s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RG supstituenata; svaki Ra6, Rb6, Rc6, i Rd6 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-, pri čemu je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od Ra6, Rb6, Rc6, i Rd6, opcionalno supstituiran s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RG supstituenata; ili bilo koji od Rc6 i Rd6 koji je vezan na isti N atom, zajedno s N atomom s kojim su vezani, tvore 5-članu ili 6-članu heteroaril skupinu ili 4-članu, 5-članu, 6-članu, ili 7-članu heterocikloalkil skupinu, pri čemu je 5-člana ili 6-člana heteroaril skupina ili 4-člana, 5-člana, 6-člana, ili 7-člana heterocikloalkil skupina opcionalno supstituirana s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RG supstituenata; svaki Re6 se neovisno bira od sljedećih: H, OH, CN, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, C1-6 haloalkoksi, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-; svaki od Rf6 i Rg6 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, C1-6 haloalkoksi, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-; svaki od Rh6 i Ri6 se neovisno bira od sljedećih: H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-; svaki od Rj6 i Rk6 se neovisno bira od OH, C1-6 alkoksi, i C1-6 haloalkoksi; ili bilo koji od Rj6 i Rk6 koji je vezan na isti B atom, zajedno s B atomom s kojim su vezani, tvore 5-članu ili 6-članu heterocikloalkil skupinu opcionalno supstituiranu s 1, 2, 3, ili 4 supstituenta neovisno odabrana od C1-6 alkila i C1-6 haloalkila; svaki RG se neovisno bira od sljedećih: H, D, halogen, CN, NO2, SF5, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil; i svaki RM se neovisno bira od sljedećih: H, D, OH, NO2, CN, halogen, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, cijano-C1-6 alkil, HO-C1-6 alkil, C1-6 alkoksi-C1-6 alkil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-7 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, (4-10-člani heterocikloalkil)-C1-6 alkil, C1-6 alkoksi, C1-6 haloalkoksi, amino, C1-6 alkilamino, di(C1-6 alkil)amino, tio, C1-6 alkiltio, C1-6 alkilsulfinil, C1-6 alkilsulfonil, karbamil, C1-6 alkilkarbamil, di(C1-6 alkil)karbamil, karboksi, C1-6 alkilkarbonil, C1-4 alkoksikarbonil, C1-6 alkilkarbonilamino, C1-6 alkilsulfonilamino, aminosulfonil, C1-6 alkilaminosulfonil, di(C1-6 alkil)aminosulfonil, aminosulfonilamino, C1-6 alkilaminosulfonilamino, di(C1-6 alkil)aminosulfonilamino, aminokarbonilamino, C1-6 alkilaminokarbonilamino, i di(C1-6 alkil)aminokarbonilamino.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R1 je H, D ili C1-6 alkil.
3. Spoj prema bilo kojem od patentnih zahtjeva 1 i 2, naznačen time, da se svaki RA neovisno bira od sljedećih: D, halogen, C1-6 alkil, C1-6 haloalkil, CN, ORa4 i NRc4Rd4; pri čemu je svaki C1-6 alkil, C2-6 alkenil, i C2-6 alkinil od RA, opcionalno supstituiran s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RD supstituenata; svaki Ra4, Rc4, i Rd4 se neovisno bira od H, C1-6 alkila, i C1-6 haloalkila, pri čemu je svaki C1-6 alkil od Ra4, Rc4, i Rd4, opcionalno supstituiran s 1, 2, 3, 4, 5, 6, 7, ili 8 neovisno odabranih RD supstituenata; i svaki RD se neovisno bira od D, OH, CN, halogen, C1-6 alkila, C1-6 haloalkila, C1-6 alkoksi, C1-6 haloalkoksi, amino, C1-6 alkilamino, i di(C1-6 alkil)amino.
4. Spoj prema bilo kojem od patentnih zahtjeva 1 i 2, ili njegova farmaceutski prihvatljiva sol, naznačen time, da se svaki Rc1 i Rd1 neovisno bira od sljedećih: H, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-10 cikloalkil, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-10 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-, pri čemu je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-10 cikloalkil, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-10 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od Rc1 i Rd1, opcionalno supstituiran s 1, 2, 3, ili 4 neovisno odabrana RA supstituenta; ili bilo koji od Rc1 i Rd1 koji je vezan na isti N atom, zajedno s N atomom s kojim su vezani, tvore 4-članu, 5-članu, 6-članu, ili 7-članu heterocikloalkl skupinu, pri čemu je 4-člana, 5-člana, 6-člana, ili 7-člana heterocikloalkil skupina opcionalno supstituirana s 1, 2, 3, ili 4 neovisno odabrana RA supstituenta.
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R4 je H, D, ili C1-6 alkil, pri čemu je C1-6 alkil opcionalno supstituiran s 1, 2, ili 3 D.
6. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R5 je H, D, ili C1-6 alkil, pri čemu je C1-6 alkil opcionalno supstituiran s 1, 2, ili 3 D.
7. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R5 jest H.
8. Spoj prema bilo kojem od patentnih zahtjeva 1 do 7, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R6 je H, D, C1-6 alkil, ili pri čemu svaki halogen jest F, dok je haloalkil opcionalno supstituiran s 1 ili 2 neovisno odabrana Y supstituenta, gdje je svaki Y supstituent neovisno odabran od D, halogena, C1-6 alkila i C1-6 haloalkila.
9. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol, naznačen time, da se R7 bira od sljedećih: H, D, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-10 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-, pri čemu je C1-6 alkil opcionalno supstituiran s 1, 2, ili 3 D.
10. Spoj prema bilo kojem od patentnih zahtjeva 1 do 9, ili njegova farmaceutski prihvatljiva sol, naznačen time, da se R8 bira od sljedećih: H, D, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-10 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-, pri čemu je C1-6 alkil opcionalno supstituiran s 1, 2, ili 3 D.
11. Spoj prema bilo kojem od patentnih zahtjeva 1 do 9, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R8 jest H.
12. Spoj prema bilo kojem od patentnih zahtjeva 1 do 11, naznačen time, da ima Formulu (II): [image] ili njegova farmaceutski prihvatljiva sol.
13. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: X1 je N ili CH; R2 je C(O)NRc1Rd1; svaki od Rc1 i Rd1 se neovisno bira od sljedećih: H, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-10 cikloalkil, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-10 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil-, pri čemu je svaki C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-10 cikloalkil, 4-10-člani heterocikloalkil, C6-10 aril-C1-6 alkil-, C3-10 cikloalkil-C1-6 alkil-, (5-10-člani heteroaril)-C1-6 alkil-, i (4-10-člani heterocikloalkil)-C1-6 alkil- od Rc1 i Rd1, opcionalno supstituiran s 1, 2, 3, ili 4 neovisno odabrana RA supstituenta; ili bilo koji od Rc1 i Rd1, koji je vezan na isti N atom, zajedno s N atomom s kojim su vezani, tvore 4-članu, 5-članu, 6-članu, ili 7-članu heterocikloalkil skupinu, pri čemu je 4-člana, 5-člana, 6-člana, ili 7-člana heterocikloalkil skupina opcionalno supstituirana s 1 ili 2 neovisno odabrana RA supstituenta; svaki RA se neovisno bira od sljedećih: D, halogen, okso, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, CN, NO2 i ORa4, pri čemu je C1-6 alkil, C2-6 alkenil, i C2-6 alkinil od RA, opcionalno supstituiran s 1 ili 2 neovisno odabrana RD supstituenta; svaki Ra4 se neovisno bira od H i C1-6 alkila, pri čemu je C1-6 alkil opcionalno supstituirani CN, NO2 ili OH; svaki RD jest OH; svaki od R3, R4, i R5 se neovisno bira od H, D, halogena, CN, OH, C1-3 alkila, i C1-3 haloalkila, pri čemu je C1-3 alkil opcionalno supstituiran s 1, 2, 3, 4, 5, ili 6 D; i svaki od R6, R7, i R8 se neovisno bira od H, D, C1-6 alkila i C1-6 haloalkila.
14. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: X1 je N; R2 je C(O)NRc1Rd1; Rc1 je H; Rd1 se bira od sljedećih: etil, propil, izopropil, butil, terc-butil, ciklobutil, cikloheksil, biciklo[1.1.1]pentanil, biciklo[2.1.1]heksanil, biciklo[2.2.1]heptanil, metil-ciklopropil, metil-ciklobutil, metil-fenil, etil-fenil, oksetanil, tetrahidrofuranil, tetrahidropiranil, pirorolidinil, i tianil, pri čemu je etil, propil, izopropil, terc-butil, ciklobutil, cikloheksil, biciklo[1.1.1]pentanil, biciklo[2.1.1]heksanil, biciklo[2.2.1]heptanil, metil-ciklopropil, metil-ciklobutil, metil-fenil, etil-fenil, oksetanil, tetrahidrofuranil, tetrahidropiranil, pirorolidinil, i tianil od Rd1, opcionalno supstituiran s 1 ili 2 neovisno odabrana RA supstituenta; ili bilo koji od Rc1 i Rd1, koji je vezan na isti N atom, zajedno s N atomom s kojim su vezani, tvore azetidinil ili pirolidinil, pri čemu je azetidinil ili pirolidinil opcionalno supstituiran s 1 ili 2 neovisno odabrana RA supstituenta; svaki RA se neovisno bira od okso, metila, CH2F, CHF2, CF3, -OCH3, -CH2OH, CN, i OH; R3 se bira od H, metila, i CD3; svaki od R4 i R5 jest H; R6 se bira od CH2F, CHF2 i CF3; i svaki od R7 i R8 jest H.
15. Spoj prema patentnom zahtjevu 1, naznačen time, da se bira od sljedećih: 3-Amino-6-(2-(metil-d3)-5-(1,1,1-trifluoro-2,3-dihidroksipropan-2-il)fenil)-N- (tetrahidro-2H-piran-4-il)pirazin-2-karboksamid; 3-Amino-6-(5-(1,1-difluoro-2,3-dihidroksipropan-2-il)-2-(metil-d3)fenil)-N-(4- hidroksibiciklo[2.2.1]heptan-1-il)pirazin-2-karboksamid; 3-Amino-6-(2-(metil-d3)-5-(1,1,1-trifluoro-2,3-dihidroksibutan-2-il)fenil)-N-(tetrahidro-2H-piran-4-il)pirazin-2-karboksamid; 3-Amino-6-(2-metil-5-(1,1,1-trifluoro-2,3-dihidroksi-3-metilbutan-2-il)fenil)-N-(tetrahidro-2H-piran-4-il)pirazin-2-karboksamid; 3-amino-N-((1s,3R)-3-cijanociklobutil)-6-(2-(metil-d3)-5-((S)-1,1,1-trifluoro-2,3- dihidroksipropan-2-il)fenil)pirazin-2-karboksamid; 3-amino-N-((1S,2S)-2-hidroksicikloheksil)-6-(2-(metil-d3)-5-((S)-1,1,1-trifluoro-2,3-dihidroksipropan-2-il)fenil)pirazin-2-karboksamid; 3-amino-N-((trans)-3-hidroksitetrahidro-2H-piran-4-il)-6-(2-(metil-d3)-5-((S)-1,1,1-trifluoro-2,3-dihidroksipropan-2-il)fenil)pirazin-2-karboksamid; 3-amino-N-((1s,3R)-3-hidroksi-3-(trifluorometil)ciklobutil)-6-(2-(metil-d3)-5-((S)-1,1,1-trifluoro-2,3-dihidroksipropan-2-il)fenil)pirazin-2-karboksamid; 3-amino-N-((1s,3R)-3-hidroksi-1-metilciklobutil)-6-(2-(metil-d3)-5-((S)-1,1,1-trifluoro-2,3-dihidroksipropan-2-il)fenil)pirazin-2-karboksamid; (S)-3-amino-N-(4-(hidroksimetil)biciklo[2.1.1]heksan-1-il)-6-(2-(metil-d3)-5-(1,1,1-trifluoro-2,3-dihidroksipropan-2-il)fenil)pirazin-2-karboksamid; (S)-3-amino-N-(3-(hidroksimetil)biciklo[1.1.1]pentan-1-il)-6-(2-(metil-d3)-5-(1,1,1-trifluoro-2,3-dihidroksipropan-2-il)fenil)pirazin-2-karboksamid; 3-amino-N-((S)-1-hidroksipropan-2-il)-6-(2-(metil-d3)-5-((S)-1,1,1-trifluoro-2,3- dihidroksipropan-2-il)fenil)pirazin-2-karboksamid; (S)-3-amino-N-(2-cijano-2-metilpropil)-6-(2-(metil-d3)-5-(1,1,1-trifluoro-2,3- dihidroksipropan-2-il)fenil)pirazin-2-karboksamid; (S)-3-amino-N-(4-hidroksibiciklo[2.2.1]heptan-1-il)-6-(2-(metil-d3)-5-(1,1,1 trifluoro-2,3-dihidroksipropan-2-il)fenil)pirazin-2-karboksamid; 3-amino-N-((R)-1-hidroksipropan-2-il)-6-(2-(metil-d3)-5-((S)-1,1,1-trifluoro-2,3- dihidroksipropan-2-il)fenil)pirazin-2-karboksamid; (S)-3-amino-N-(4-hidroksibiciklo[2.1.1]heksan-1-il)-6-(2-(metil-d3)-5-(1,1,1-trifluoro-2,3-dihidroksipropan-2-il)fenil)pirazin-2-karboksamid; 3-amino-6-(5-((S)-1,1-difluoro-2,3-dihidroksipropan-2-il)-2-(metil-d3)fenil)-N-((1S,2S)-2-hidroksicikloheksil)pirazin-2-karboksamid; 3-amino-6-(5-((S)-1,1-difluoro-2,3-dihidroksipropan-2-il)-2-(metil-d3)fenil)-N- ((1R,2R)-2-hidroksicikloheksil)pirazin-2-karboksamid; (S)-3-amino-N-(4-cijanobiciklo[2.1.1]heksan-1-il)-6-(5-(1,1-difluoro-2,3- dihidroksipropan-2-il)-2-(metil-d3)fenil)pirazin-2-karboksamid; (S)-3-amino-6-(5-(1,1-difluoro-2,3-dihidroksipropan-2-il)-2-(metil-d3)fenil)-N- (tetrahidro-2H-piran-4-il)pirazin-2-karboksamid; (S)-3-amino-6-(5-(1,1-difluoro-2,3-dihidroksipropan-2-il)-2-metilfenil)-N-(tetrahidro-2H-piran-4-il)pirazin-2-karboksamid; 3-amino-6-(5-((S)-1,1-difluoro-2,3-dihidroksipropan-2-il)-2-metilfenil)-N-((S)-1- hidroksipropan-2-il)pirazin-2-karboksamid; 3-amino-6-(5-(1,1-difluoro-2,3-dihidroksipropan-2-il)-2-metilfenil)-N-(4- hidroksibiciklo[2.2.1]heptan-1-il)pirazin-2-karboksamid; (3-amino-6-(5-((S)-1,1-difluoro-2,3-dihidroksipropan-2-il)-2-metilfenil)pirazin-2-il)((R)-2-(hidroksimetil)pirolidin-1-il)metanon; (S)-3-amino-6-(5-(1,1-difluoro-2,3-dihidroksipropan-2-il)-2-metilfenil)-N-izopropilpirazin-2-karboksamid; 3-amino-6-(5-((S)-1,1-difluoro-2,3-dihidroksipropan-2-il)-2-metilfenil)-N-(3- metiltetrahidrofuran-3-il)pirazin-2-karboksamid; i 3-Amino-N-(4-cijanobiciklo[2.1.1]heksan-1-il)-6-(5-(1,1-difluoro-2,3-dihidroksipropan-2-il)-2-metilfenil)pirazin-2-karboksamid; ili njihov enantiomer, dijastereomer ili tautomer; ili njihova farmaceutski prihvatljiva sol.
16. Spoj prema patentnom zahtjevu 1, naznačen time, da je (S)-3-amino-N-(4-cijanobiciklo[2.1.1]heksan-1-il)-6-(5-(1,1-difluoro-2,3-dihidroksipropan-2-il)-2-(metil-d3)fenil)pirazin-2-karboksamid; ili njegov enantiomer, dijastereomer ili tautomer; ili njegova farmaceutski prihvatljiva sol.
17. Spoj prema patentnom zahtjevu 1, naznačen time, da je (S)-3-amino-N-(4-cijanobiciklo[2.1.1]heksan-1-il)-6-(5-(1,1-difluoro-2,3-dihidroksipropan-2-il)-2-(metil-d3)fenil)pirazin-2-karboksamid; ili njegov enantiomer, dijastereomer ili tautomer; ili njegova farmaceutski prihvatljiva sol.
18. Farmaceutski pripravak, naznačen time, da sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 17, ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljivo pomoćno sredstvo ili nosač.
19. Spoj prema bilo kojem od patentnih zahtjeva 1 do 17, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u postupku liječenja bolesti ili poremećaja kod pacijenta, pri čemu je ta bolest ili poremećaj povezan/a s abnormalnom ekspresijom ili aktivnošću PI3Kγ kinaze, pri čemu postupak obuhvaća davanje pacijentu terapijski učinkovite količine spoja prema bilo kojem od patentnih zahtjeva 1 do 17, ili njegove farmaceutski prihvatljive soli, dok se bolest ili poremećaj bira od sljedećih: (a) autoimuna bolest ili poremećaj, rak, kardiovaskularna bolest, ili neurodegenerativna bolest; ili (b) rak pluća, melanom, rak gušterače, rak dojke, rak prostate, rak jetre, rak debelog crijeva, rak endometrija, rak mokraćnog mjhehura, rak kože, rak tijela maternice, rak bubrega, rak želuca, seminom, teratokarcinom, astrocitom, neuroblastom, gliom, ili sarkom; ili (c) Askinov tumor, botrioidni sarkom, hondrosarkom, Ewingov sarkom, maligni hemangioendoteliom, maligni švanom, osteosarkom, sarkom mekog dijela alveola, angiosarkom, filoidni cistosarkom, dermatofibrosarkom protuberans, dezmoidni tumor, dezmoplastični tumor malih okruglih stanica, epitelni sarkom, izvankoštani hondrosarkom, izvankoštani osteosarkom, fibrosarkom, gastrointestinalni stromalni tumor (GIST), hemangiopericitom, hemangiosarkom, Kaposijev sarkom, leiomiosarkom, liposarkom, limfangiosarkom, limfosarkom, maligni tumor periferne živčane ovojnice (MPNST), neurofibrosarkom, rabdomiosarkom, sinovijalni sarkom, ili nediferencirani pleomorfni sarkom; ili (d) akutna mijeloična leukemija, akutna monocitna leukemija, limfom malih limfocita, kronična limfocitna leukemija (CLL), kronična mijeloična leukemija (CML), multipli mijelom, akutna limfoblastična leukemija T-stanica (T-ALL), kožni limfom T-stanica, velika granularna limfocitna leukemija, zrela (periferna) neoplazma T-stanica (PTCL), anaplastični limfom velikih stanica (ALCL), ili limfoblastični limfom; ili (e) prolimfocitna leukemija T-stanica, granularna limfocitna leukemija T-stanica, agresivna leukemija NK-stanica, mikoza fungoida/Sezaryjev sindrom, naplastični limfom velikih stanica (tipa T-stanica), limfom T-stanica enteropatskog tipa, leukemija T-stanica kod odraslih/ limfom T-stanica kod odraslih, ili angioimunoblastični limfom T-stanica; ili (f) sustavni ALCL ili primarni kožni ALCL; ili (g) Burkittov limfom, akutna mijeloblastična leukemija, kronična mijeloična leukemija, ne-Hodgkinov limfom, Hodgkinov limfom, leukemija kosmatih stanica, limfom plaštenih stanica, limfom malih limfocita, folikularni limfom, ksenoderoma pigmentozum, keratoktantom, limfoplazmacitni limfom, limfom ekstranodalne marginalne zone, Waldenstromova makroglobulinemija, prolimfocitna leukemija, akutna limfoblastična leukemija, mijelofibroza, limfom limfnog tkiva povezanog sa sluznicom (MALT), mediastinalni (timusni) veliki B-stanični limfom, limfomatoidna granulomatoza, limfom marginalne zone slezene, primarni efuzijski limfom, intravaskularni veliki B-stanični limfom, leukemija stanica plazme, ekstramedularni plazmocitom, tinjajući mijelom (aka asimptomatski mijelom), monoklonska gamopatija neutvrđenog značaja (MGUS), ili difuzni veliki B-stanični limfom; ili (h) ponavljajući NHL, uporni NHL, periodični folikularni NHL, indolentno NHL (iNHL), ili agresivni NHL (aNHL); ili (i) difuzni limfom velikih B-stanica aktiviranih B limfocita (ABC) ili difuzni limfom velikih B-stanica germinativnog centra B-stanica (GCB); ili (j) endemijski Burkittov limfom, sporadični Burkittov limfom, ili limfom nalik na Burkittov limfom; ili (k) reumatoidni artritis, multipla skleroza, sustavni eritematozni lupus, astma, alergija, alergijski rinitis, pankreatitis, psorijaza, anafilaksa, glomerulonefritis, upalna bolest crijeva, tromboza, meningitis, encefalitis, dijabetička retinopatija, benigna hipertrofija prostate, miastenija gravis, Sjögrenov sindrom, osteoartritis, restenoza, ili ateroskleroza; ili (l) srčana hipertrofija, kardijska miocitna disfunkcija, akutni koronarni sindrom, kronična opstrukcijska plućna bolest (KOPB), kronični bronhitis, povišeni krvni tlak, ishemija, ishemijska reperfuzija, vazokonstrikcija, anemija, bakterijska infekcija, virusna infekcija, odbacivanje usatka, bubrežna bolest, anafilaktički šok, fibroza, atrofija koštanih mišića, hipertrofija koštanih mišića, angiogeneza, sepsa, bolest usadak protiv domaćina, alogena ili ksenogena transplantacija, glomeruloskleroza, progresivna renalna fibroza, idiopatska trombocitopenijska purpura (ITP), autoimuna hemolitička anemija, vaskulitis, sustavni eritematozni lupus, lupus nefritis, pemfigus, membranska nefropatija; ili (m) povratna ITP ili uporna ITP; ili (n) Behçetova bolest, Coganov sindrom, arteritis divovskih stanica, reumatska polimijalgija (PMR), Takayasuov arteritis, Buergerova bolest (tromboangiitis obliterans), vaskulitis središnjeg živčanog sustava, Kawasakijeva bolest, nodozni poliarteritis, Churg-Straussov sindrom, miješovita vaskulitis krioglobulinemija (osnovna ili inducirana virusom hepatitisa C (HCV)), Henoch-Schönlein purpura (HSP), hipersenzitivni vaskulitis, mikroskopski poliangiitis, Wegenerova granulomatoza, ili sustavni vaskulitis (AASV) povezan s anti-neutrofilnim citoplazmatskim protutijelom (ANCA); ili (o) Alzheimerova bolest, trauma središnjeg živčanog sustava, ili moždani udar.
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