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HRP20171913T1 - Aminopirimidinilni spojevi kao inhibitori jak - Google Patents

Aminopirimidinilni spojevi kao inhibitori jak Download PDF

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Publication number
HRP20171913T1
HRP20171913T1 HRP20171913TT HRP20171913T HRP20171913T1 HR P20171913 T1 HRP20171913 T1 HR P20171913T1 HR P20171913T T HRP20171913T T HR P20171913TT HR P20171913 T HRP20171913 T HR P20171913T HR P20171913 T1 HRP20171913 T1 HR P20171913T1
Authority
HR
Croatia
Prior art keywords
alkyl
amino
pyrimidin
diazabicyclo
oct
Prior art date
Application number
HRP20171913TT
Other languages
English (en)
Inventor
Andrew Fensome
Ariamala Gopalsamy
Brian S. GERSTENBERGER
Ivan Viktorovich Efremov
Zhao-Kui Wan
Betsy PIERCE
Jean-Baptiste Telliez
John I Trujillo
Liying Zhang
Li Xing
Eddine Saiah
Original Assignee
Pfizer Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=54148580&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20171913(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer Inc. filed Critical Pfizer Inc.
Publication of HRP20171913T1 publication Critical patent/HRP20171913T1/hr

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Claims (21)

1. Spoj sa strukturom: [image] , ili njegova farmaceutski prihvatljiva sol, naznačen time što X je N ili CR, gdje je R vodik, deuterij, C1-C4 alkil, C1-C4 alkoksi, C3-C6 cikloalkil, aril, heteroaril, aril(C1-C6 alkil), CN, amino, alkilamino, dialkilamino, CF3 ili hidroksil; A se bira iz skupine koju čine veza, C=O, --SO2--, --(C=O)NR0--, te --(CRaRb)q--, gdje je R0 H ili C1-C4 alkil, a Ra i Rb su neovisno vodik, deuterij, C1-C6 alkil, C3-C6 cikloalkil, aril, aril(C1-C6 alkil), heteroaril, (C1-C6 alkil)heteroaril, heteroaril(C1-C6 alkil), te heterocikl(C1-C6 alkil); A′ se bira iz skupine koju čine veza, C=O, --SO2--, --(C=O)NR0′, --NR0′(C=O)--, te --(CRa′Rb′)q--, gdje je R0′ H ili C1-C4 alkil, a Ra′ i Rb′ su neovisno vodik, deuterij, C1-C6 alkil, C3-C6 cikloalkil, aril, aril(C1-C6 alkil), heteroaril, (C1-C6 alkil)heteroaril, heteroaril(C1-C6 alkil), te heterocikl(C1-C6 alkil); Z je --(CH2)h-- ili veza, gdje jedna ili više metilenskih jedinice mogu biti supstituirane s jednim ili više C1-C3 alkila, CN, OH, metoksi ili halogena, te gdje navedeni alkil može biti supstituiran s jednim ili više atoma fluora ; R1 i R1′ su neovisno koji se bira iz skupine koju čine vodik, deuterij, C1-C4 alkil, C3-C6 cikloalkil, aril, heteroaril, aril(C1-C6 alkil), CN, amino, alkilamino, dialkilamino, alkoksi, heteroaril(C1-C6 alkil), te heterocikl(C1-C6 alkil), gdje navedeni alkil, aril, cikloalkil, heterocikl ili heteroaril može biti dodatno supstituiran s jednim ili više supstituenata, koje se bira iz skupine koju čine C1-C6 alkil, halogen, CN, hidroksi, metoksi, amino, C1-C4 alkilamino, di(C1-C4 alkil)amino, CF3, --SO2(C1-C6 alkil), te C3-C6 cikloalkil; R2 se bira iz skupine koju čine vodik, deuterij, C1-C6 alkil, C3-C6 cikloalkil, halogen, te cijano, gdje navedeni alkil može biti supstituiran s jednim ili više atoma fluora; R3 se bira iz skupine koju čine vodik, deuterij, te amino; R4 je monociklički ili biciklički aril, ili monociklički ili biciklički heteroaril, gdje navedeni aril ili heteroaril može biti supstituiran s jednim ili više supstituenata, koje se bira iz skupine koju čine C1-C6 alkil, heterocikloalkil, halogen, CN, hidroksi, --CO2H, C1-C6 alkoksi, amino, --N(C1-C6 alkil)(CO)(C1-C6 alkil), --NH(CO)(C1-C6 alkil), --(CO)NH2, --(CO)NH(C1-C6 alkil), --(CO)N(C1-C6 alkil)2, --(C1-C6 alkil)amino, --N(C1-C6 alkil)2, --SO2-(C1-C6 alkil), --(SO)NH2, te C3-C6 cikloalkil, gdje navedeni alkil, cikloalkil, alkoksi ili heterocikloalkil može biti supstituiran s jednim ili više C1-C6 alkila, halogena, CN, OH, alkoksi, amino, --CO2H, --(CO)NH2, --(CO)NH(C1-C6 alkil) ili --(CO)N(C1-C6 alkil)2, te gdje navedeni alkil može biti dodatno supstituiran s jednim ili više atoma fluora; R5 se neovisno bira iz skupine koju čine vodik, C1-C6 alkil, C1-C6 alkoksi, te hidroksil; h je 1, 2 ili 3; j i k su neovisno 0, 1, 2 ili 3; m i n su neovisno 0, 1 ili 2; i q je 0, 1 ili 2.
2. Spoj u skladu s patentnim zahtjevom 1 sa strukturom: [image] , ili njegova farmaceutski prihvatljiva sol, naznačen time što X je N; A se bira iz skupine koju čine veza, C=O, --SO2--, --(C=O)NR0--, te --(CRaRb)q--, gdje je R0 H ili C1-C4 alkil, a Ra i Rb su neovisno vodik, deuterij, C1-C6 alkil, C3-C6 cikloalkil, aril, aril(C1-C6 alkil), heteroaril, (C1-C6 alkil)heteroaril, heteroaril(C1-C6 alkil), te heterocikl(C1-C6 alkil); R1 se bira iz skupine koju čine vodik, deuterij, C1-C4 alkil, C3-C6 cikloalkil, aril, heteroaril, aril(C1-C6 alkil), CN, amino, alkilamino, dialkilamino, fluoralkil, alkoksi, heteroaril(C1-C6 alkil), heterocikl i heterocikl(C1-C6 alkil), gdje navedeni alkil, aril, cikloalkil, heterocikl ili heteroaril može biti dodatno supstituiran s jednim ili više supstituenata, koje se bira iz skupine koju čine C1-C6 alkil, halogen, CN, hidroksi, metoksi, amino, C1-C4 alkilamino, di(C1-C4 alkil)amino, CF3, --SO2(C1-C6 alkil), te C3-C6 cikloalkil; R2 se bira iz skupine koju čine vodik, deuterij, C1-C6 alkil, C3-C6 cikloalkil, halogen, te cijano, gdje navedeni alkil može biti supstituiran s jednim ili više atoma fluora; R3 se bira iz skupine koju čine vodik i deuterij; R4 je monociklički ili biciklički aril, ili monociklički ili biciklički heteroaril, gdje navedeni aril ili heteroaril može biti supstituiran s jednim ili više supstituenata, koje se bira iz skupine koju čine C1-C6 alkil, heterocikloalkil, halogen, CN, hidroksi, --CO2H, C1-C6 alkoksi, amino, --N(C1-C6 alkil)(CO)(C1-C6 alkil), --NH(CO)(C1-C6 alkil), --(CO)NH2, --(CO)NH(C1-C6 alkil), --(CO)N(C1-C6 alkil)2, --(C1-C6 alkil)amino, --N(C1-C6 alkil)2, --SO2-(C1-C6 alkil), --(SO)NH2, te C3-C6 cikloalkil, gdje navedeni alkil, cikloalkil, alkoksi ili heterocikloalkil može biti supstituiran s jednim ili više C1-C6 alkila, halogena, CN, OH, alkoksi, amino, --CO2H, --(CO)NH2, --(CO)NH(C1-C6 alkil) ili --(CO)N(C1-C6 alkil)2, te gdje navedeni alkil može biti dodatno supstituiran s jednim ili više atoma fluora; h je 1, 2 ili 3; j je 0,1, 2 ili 3; i q je 0, 1 ili 2; R5 se neovisno bira iz skupine koju čine vodik, C1-C6 alkil, C1-C6 alkoksi, te hidroksil.
3. Spoj u skladu s patentnim zahtjevom 1 sa strukturom: [image] , ili njegova farmaceutski prihvatljiva sol, naznačen time što X je N; A se bira iz skupine koju čine veza, C=O, --SO2--, --(C=O)NR0--, te --(CRaRb)q--, gdje je R0 H ili C1-C4 alkil, a Ra i Rb su neovisno vodik, deuterij, C1-C6 alkil, C3-C6 cikloalkil, aril, aril(C1-C6 alkil), heteroaril, (C1-C6 alkil)heteroaril, heteroaril(C1-C6 alkil), te heterocikl(C1-C6 alkil); R1 se bira iz skupine koju čine vodik, deuterij, C1-C4 alkil, C3-C6 cikloalkil, aril, heteroaril, aril(C1-C6 alkil), CN, amino, alkilamino, dialkilamino, fluoralkil, alkoksi, heteroaril(C1-C6 alkil), heterocikl i heterocikl(C1-C6 alkil), gdje navedeni alkil, aril, cikloalkil, heterocikl ili heteroaril može biti dodatno supstituiran s jednim ili više supstituenata, koje se bira iz skupine koju čine C1 - C6 alkil, halogen, CN, hidroksi, metoksi, amino, C1-C4 alkilamino, di(C1-C4 alkil)amino, CF3, --SO2-(C1-C6 alkil), te C3-C6 cikloalkil; R2 se bira iz skupine koju čine vodik, deuterij, C1-C6 alkil, C3-C6 cikloalkil, halogen, te cijano, gdje navedeni alkil može biti supstituiran s jednim ili više atoma fluora; R3 se bira iz skupine koju čine vodik i deuterij; R4 je monociklički ili biciklički aril, ili monociklički ili biciklički heteroaril, gdje navedeni aril ili heteroaril može biti supstituiran s jednim ili više supstituenata, koje se bira iz skupine koju čine C1-C6 alkil, heterocikloalkil, halogen, CN, hidroksi, --CO2H, C1-C6 alkoksi, amino, --N(C1-C6 alkil)(CO)(C1-C6 alkil), --NH(CO)(C1-C6 alkil), --(CO)NH2, --(CO)NH(C1-C6 alkil), --(CO)N(C1-C6 alkil)2, --(C1-C6 alkil)amino, --N(C1-C6 alkil)2, --SO2-(C1-C6 alkil), --(SO)NH2, te C3-C6 cikloalkil, gdje navedeni alkil, cikloalkil, alkoksi ili heterocikloalkil može biti supstituiran s jednim ili više C1-C6 alkila, halogena, CN, OH, alkoksi, amino, --CO2H, --(CO)NH2, --(CO)NH(C1-C6 alkil) ili --(CO)N(C1-C6 alkil)2, te gdje navedeni alkil može biti dodatno supstituiran s jednim ili više atoma fluora; R5 se bira iz skupine koju čine vodik, C1-C6 alkil, C1-C6 alkoksi, te hidroksil; j je 0, 1, 2 ili 3; i q je 0, 1 ili 2; R5 se neovisno bira iz skupine koju čine vodik, C1-C6 alkil, C1-C6 alkoksi, te hidroksil.
4. Spoj sa strukturom: [image] , ili njegova farmaceutski prihvatljiva sol, naznačen time što A′ se bira iz skupine koju čine veza, C=O, --SO2--, --(C=O)NR0′, --NR0′(C=O)--, te --(CRa′Rb′)q--, gdje je R0′ H ili C1-C4 alkil, a Ra′ i Rb′ su neovisno vodik, deuterij, C1-C6 alkil, C3-C6 cikloalkil, aril, aril(C1-C6 alkil), heteroaril, (C1-C6 alkil)heteroaril, heteroaril(C1-C6 alkil), te heterocikl(C1-C6 alkil); R1′ se bira iz skupine koju čine vodik, deuterij, C1-C4 alkil, C3-C6 cikloalkil, aril, heteroaril, aril(C1-C6 alkil), CN, amino, alkilamino, dialkilamino, fluoralkil, alkoksi, heteroaril(C1-C6 alkil), hetrocikl i heterocikl(C1-C6 alkil), gdje navedeni alkil, aril, cikloalkil, heterocikl ili heteroaril može biti dodatno supstituiran s jednim ili više supstituenata, koje se bira iz skupine koju čine C1-C6 alkil, halogen, CN, hidroksi, metoksi, amino, C1-C4 alkilamino, di(C1-C4 alkil)amino, CF3, --SO2(C1-C6 alkil), te C3-C6 cikloalkil; R2 se bira iz skupine koju čine vodik, deuterij, C1-C6 alkil, C3-C6 cikloalkil, halogen, te cijano, gdje navedeni alkil može biti supstituiran s jednim ili više atoma fluora; R3 se bira iz skupine koju čine vodik i deuterij; R4 je monociklički ili biciklički aril, ili monociklički ili biciklički heteroaril, gdje navedeni aril ili heteroaril može biti supstituiran s jednim ili više supstituenata, koje se bira iz skupine koju čine C1-C6 alkil, heterocikloalkil, halogen, CN, hidroksi, --CO2H, C1-C6 alkoksi, amino, --N(C1-C6 alkil)(CO)(C1-C6 alkil), --NH(CO)(C1-C6 alkil), --(CO)NH2, --(CO)NH(C1-C6 alkil), --(CO)N(C1-C6 alkil)2, --(C1-C6 alkil)amino, --N(C1-C6 alkil)2, --SO2-(C1-C6 alkil), --(SO)NH2, te C3-C6 cikloalkil, gdje navedeni alkil, cikloalkil, alkoksi ili heterocikloalkil može biti supstituiran s jednim ili više C1-C6 alkila, halogena, CN, OH, alkoksi, amino, --CO2H, --(CO)NH2, --(CO)NH(C1-C6 alkil) ili --(CO)N(C1-C6 alkil)2, te gdje navedeni alkil može biti dodatno supstituiran s jednim ili više atoma fluora; R5 se neovisno bira iz skupine koju čine vodik, C1-C6 alkil, C1-C6 alkoksi, te hidroksil; R7 i R8 su neovisno vodik, C1-C4 alkil, aril, heteroaril, (aril)C1-C6 alkil, (heteroaril)C1-C6 alkil, (heterocikl)C1-C6 alkil, (C1-C6 alkil)aril, (C1-C6 alkil)heteroaril ili (C1-C6 alkil)heterocikl, gdje navedeni alkil može biti dodatno supstituiran s jednim ili više supstituenata, koje se bira iz skupine koju čine halogen, hidroksi, metoksi, amino, CF3, te C3-C6 cikloalkil; k je 0, 1, 2 ili 3; m i n su oba 1; i q je 0, 1 ili 2.
5. Spoj u skladu s patentnim zahtjevom 1, naznačen time što se bira iz skupine koju čine: [(1S)-2,2-difluorciklopropil]{(1R,5S)-3-[2-({5-fluor-6-[(3S)-3-hidroksipirolidin-1-il]piridin-3-il}amino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]okt-8-il}metanon; (1R,5S)-N-etil-3-[2-(1,2-tiazol-4-ilamino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]oktan-8-karboksamid; 4-{(1R,5S)-8-[(2,2-difluorciklopropil)metil]-3,8-diazabiciklo[3.2.1]okt-3-il}-N-(1H-pirazol-4-il)pirimidin-2-amin; (1R,5S)-3-(2-{[5-klor-6-(metilkarbamoil)piridin-3-il]amino}pirimidin-4-il)-N-etil-3,8-diazabiciklo[3.2.1]oktan-8-karboksamid; ciklopropil[(1R,5S)-3-(2-{[1-(2-hidroksietil)-1H-pirazol-4-il]amino}pirimidin-4-il)-3,8-diazabiciklo[3.2.1]okt-8-il]metanon; N-(1-metil-1H-pirazol-4-il)-4-{(1R,5S)-8-[1-(metilsulfonil)azetidin-3-il]-3,8-diazabiciklo[3.2.1]okt-3-il}pirimidin-2-amin; 4-({4-[(1R,5S)-8-{[(1S)-2,2-difluorciklopropil]karbonil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N,6-dimetilpiridin-2-karboksamid; 5-({4-[(1R,5S)-8-{[(1R,2S)-2-fluorciklopropil]karbonil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N,3-dimetilpiridin-2-karboksamid; ciklopropil[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]metanon; 3-{(1R,5S)-3-[2-(1H-pirazol-4-ilamino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]okt-8-il}butanonitril; 5-({4-[(1R,5S)-8-(ciklopropilkarbonil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N-etil-3-metilpiridin-2-karboksamid; 3-[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]butanonitril; 5-({4-[(1R,5S)-8-(ciklopropilkarbonil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-3-metilpiridin-2-karboksamid; (1R,5S)-N-etil-3-(2-{[5-fluor-6-(metilkarbamoil)piridin-3-il]amino}pirimidin-4-il)-3,8-diazabiciklo[3.2.1]oktan-8-karboksamid; 3-klor-5-({4-[(1R,5S)-8-(ciklopropilkarbonil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N-metilpiridin-2-karboksamid; (1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-N-(propan-2-il)-3,8-diazabiciklo[3.2.1]oktan-8-karboksamid; (3,3-difluorciklobutil)[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]metanon; 1-({(1R,5S)-3-[2-(1H-pirazol-4-ilamino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]okt-8-il}metil)ciklopropankarbonitril; 3-[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]butanonitril; (1S,2R)-2-{[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]karbonil}ciklopropankarbonitril; (1R,2S)-2-{[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]karbonil}ciklopropankarbonitril; [(1R,2R)-2-fluorciklopropil][(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]metanon; [(1R,2R)-2-fluorciklopropil][(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]metanon; (1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]oktan-8-karboksamid; (1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-N-[5-(trifluormetil)piridin-2-il]-3,8-diazabiciklo[3.2.1]oktan-8-karboksamid; N,3-dimetil-5-[(4-{(1R,SS)-8-[(3-metiloksetan-3-il)metil]-3,8-diazabiciklo[3.2.1]okt-3-il}pirimidin-2-il)amino]piridin-2-karboksamid; {3-[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]-1-(metilsulfonil)azetidin-3-il}acetonitril; 4-({4-[8-(cijanoacetil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N-etilbenzamid; (1R,5S)-N-(cijanometil)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]oktan-8-karboksamid; 5-({4-[(1R,5S)-8-{[(1S,2R)-2-fluorciklopropil]karbonil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N,3-dimetilpiridin-2-karboksamid; 5-({4-[(1R,5S)-8-(cis-3-cijanociklobutil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N,3-dimetilpiridin-2-karboksamid; 5-({4-[(1R,5S)-8-{[(1R)-2,2-difluorciklopropil]metil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N,3-dimetilpiridin-2-karboksamid; N,3-dimetil-5-({4-[(1R,5S)-8-(1,2-oksazol-5-ilmetil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)piridin-2-karboksamid; 2-[5-({4-[(1R,5S)-8-{[(1S)-2,2-difluorciklopropil]karbonil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)piridin-2-il]-2-metilpropanonitril; 3-{(1R,5S)-3-[2-(1H-pirazol-4-ilamino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]okt-8-il}propanonitril; (1R,5S)-N-etil-3-[2-(1H-pirazol-4-ilamino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]oktan-8-karboksamid; 4-[(1R,5S)-8-{[(1S)-2,2-difluorciklopropil]metil}-3,8-diazabiciklo[3.2.1]okt-3-il]-N-(1-metil-1H-pirazol-4-il)pirimidin-2-amin; [(1S)-2,2-difluorciklopropil][(1R,5S)-3-(2-{[5-fluor-6-(2-hidroksietil)piridin-3-il]amino}pirimidin-4-il)-3,8-diazabiciklo[3.2.1]okt-8-il]metanon; [(1S)-2,2-difluorciklopropil][(1R,5S)-3-(2-{[5-fluor-6-(3-hidroksiazetidin-1-il)piridin-3-il]amino}pirimidin-4-il)-3,8-diazabiciklo[3.2.1]okt-8-il]metanon; [(1R,5S)-3-(2-{[5-klor-6-(2-hidroksietoksi)piridin-3-il]amino}pirimidin-4-il)-3,8-diazabiciklo[3.2.1]okt-8-il][(1S)-2,2-difluorciklopropil]metanon; {3-[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]oksetan-3-il}acetonitril; [(1R,5S)-3-(2-{[5-klor-6-(2-hidroksietil)piridin-3-il]amino}pirimidin-4-il)-3,8-diazabiciklo[3.2.1]okt-8-il][(1S)-2,2-difluorciklopropil]metanon; 2-[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]piridin-4-karbonitril; 3-[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]ciklobutankarbonitril; 2-[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]-1,3-oksazol-5-karbonitril; (1R,5S)-N-(2-cijanoetil)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]oktan-8-karboksamid; N-(1-metil-1H-pirazol-4-il)-4-[(1R,5S)-8-(1,2-oksazol-4-ilmetil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-amin; 4-({4-[(1R,5S)-8-{[(1S)-2,2-difluorciklopropil]karbonil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-6-(hidroksimetil)-N-metilpiridin-2-karboksamid; (1-fluorciklopropil)[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]metanon; N-(1-metil-1H-pirazol-4-il)-4-[(1R,5S)-8-(1,3-tiazol-2-ilmetil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-amin; ciklopropil{(1R,5S)-3-[2-(1,2-tiazol-4-ilamino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]okt-8-il}metanon; [(1S)-2,2-difluorciklopropil]{(1R,5S)-3-[2-({5-fluor-6-[(3R)-3-hidroksipirolidin-1-il]piridin-3-il}amino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]okt-8-il}metanon; 5-({4-[(1R,5S)-8-{[(1S)-2,2-difluorciklopropil]metil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N,3-dimetilpiridin-2-karboksamid; 4-[(1R,5S)-8-{[(1R)-2,2-difluorciklopropil]metil}-3,8-diazabiciklo[3.2.1]okt-3-il]-N-(1-metil-1H-pirazol-4-il)pirimidin-2-amin; 6-({4-[(1R,5S)-8-(ciklopropilkarbonil)-3,8-diazabiciklo[3.2.1]okt-3-il]-5-fluorpirimidin-2-il}amino)imidazo[1,2-a]piridin-2-karboksamid; 5-({4-[(1R,5S)-8-(ciklopropilkarbonil)-3,8-diazabicicio[3.2.1]okt-3-il]-5-fluorpirimidin-2-il}amino)piridin-2-sulfonamid; 5-({4-[(1R,5S)-8-(trans-3-cijanociklobutil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N,3-dimetilpiridin-2-karboksamid; 1,2-oksazol-5-il{(1R,5S)-3-[2-(1H-pirazol-4-ilamino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]okt-8-il}metanon; N-(1-metil-1H-pirazol-4-il)-4-[(1R,5S)-8-(metilsulfonil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-amin; (1S,2S)-2-{[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]metil}ciklopropankarbonitril; 3-({4-[(1R,5S)-8-(ciklopropilkarbonil)-3,8-diazabiciklo[3.2.1]okt-3-il]-5-fluorpirimidin-2-il}amino)-N-propil-1H-pirazol-5-karboksamid; (1S,2S)-2-{[(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]metil}ciklopropankarbonitril; ciklopropil{(1R,5S)-3-[5-fluor-2-(piridazin-4-ilamino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]okt-8-il}metanon; 4-({4-[6-(2,2-difluorpropanoil)-3,6-diazabiciklo[3.1.1]hept-3-il]-5-fluorpirimidin-2-il}amino)-N-etil-2-metilbenzamid; (1S,2S)-2-cijano-N-[(1S,5R,6R)-3-(2-{[6-(2-hidroksietoksi)piridin-3-il]amino}-5-metilpirimidin-4-il)-6-metil-3-azabiciklo[3.1.0]heks-1-il]ciklopropankarboksamid; N-[(1S,5R)-3-(5-klor-2-{[1-(2-hidroksietil)-1H-pirazol-4-il]amino}pirimidin-4-il)-3-azabiciklo[3.1.0]heks-1-il]ciklopropankarboksamid; (1S)-2,2-difluor-N-[(1S,5R,6R)-3-(5-fluor-2-{[1-(oksetan-3-il)-1H-pirazol-4-il]amino}pirimidin-4-il)-6-metil-3-azabiciklo[3.1.0]heks-1-il]ciklopropankarboksamid; (1S)-2,2-difluor-N-[(1S,5S)-3-{5-fluor-2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-5-(hidroksimetil)-3-azabiciklo[3.1.0]heks-1-il]ciklopropankarboksamid; N-{(1S,5R,6R)-3-[5-fluor-2-({6-[(2S)-1-hidroksipropan-2-il]piridin-3-il}amino)pirimidin-4-il]-6-metil-3-azabiciklo[3.1.0]heks-1-il}ciklopropankarboksamid; 5-[(4-{(1S,5R,6R)-1-[(ciklopropilkarbonil)amino]-6-metil-3-azabiciklo[3.1.0]heks-3-il}-5-fluorpirimidin-2-il)amino]-N,3-dimetilpiridin-2-karboksamid; N-{(1S,5R,6R)-3-[2-({5-klor-6-[(1R)-1-hidroksietil]piridin-3-il}amino)-5-fluorpirimidin-4-il]-6-metil-3-azabiciklo[3.1.0]heks-1-il}ciklopropankarboksamid; (1R)-2,2-difluor-N-[(1R,5S,6S)-3-{5-fluor-2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-6-metil-3-azabiciklo[3.1.0]heks-1-il]ciklopropankarboksamid; 5-[(4-{(1R,5S,6S)-1-[(ciklopropilkarbonil)amino]-6-metil-3-azabiciklo[3.1.0]heks-3-il}-5-fluorpirimidin-2-il)amino]-N,3-dimetilpiridin-2-karboksamid; N-[(1R,5S)-3-(5-klor-2-{[1-(2-hidroksietil)-1H-pirazol-4-il]amino}pirimidin-4-il)-3-azabiciklo[3.1.0]heks-1-il]ciklopropankarboksamid; N-{(1S,5R,6R)-3-[5-fluor-2-({6-[(2R)-1-hidroksipropan-2-il]piridin-3-il}amino)pirimidin-4-il]-6-metil-3-azabiciklo[3.1.0]heks-1-il}ciklopropankarboksamid; i (1S)-2,2-difluor-N-[(1R,5S,6S)-3-{5-fluor-2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-6-metil-3-azabiciklo[3.1.0]heks-1-il]ciklopropankarboksamid; ili njihove farmaceutski prihvatljive soli.
6. Spoj u skladu s patentnim zahtjevom 2, naznačen time što se bira iz skupine koju čine: N-etil-4-({5-fluor-4-[6-(2-fluor-2-metilpropanoil)-3,6-diazabiciklo[3.1.1]hept-3-il]pirimidin-2-il}amino)-2-metilbenzamid; N-etil-4-({5-fluor-4-[6-(trifluoracetil)-3,6-diazabiciklo[3.1.1]hept-3-il]pirimidin-2-il}amino)-2-metilbenzamid; N-etil-2-metil-4-({4-[6-(trifluoracetil)-3,6-diazabiciklo[3.1.1]hept-3-il]pirimidin-2-il}amino)benzamid; 4-({4-[6-(ciklopropilkarbonil)-3,6-diazabiciklo[3.1.1]hept-3-il]pirimidin-2-il}amino)-N-etil-2-metilbenzamid; i 4-({4-[6-(2,2-difluorpropanoil)-3,6-diazabiciklo[3.1.1]hept-3-il]pirimidin-2-il}amino)-N-etilbenzamid ili njihove farmaceutski prihvatljive soli.
7. Spoj u skladu s patentnim zahtjevom 3, naznačen time što se bira iz skupine koju čine: 4-({4-[8-(ciklopropilkarbonil)-3,8-diazabiciklo[3.2.1]okt-3-il]-5-fluorpirimidin-2-il}amino)-N-etilbenzamid; N-etil-4-({5-fluor-4-[8-(trifluoracetil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-2-metilbenzamid; (1R,5S)-3-(2-{[5-metil-6-(metilkarbamoil)piridin-3-il]amino}pirimidin-4-il)-N-(2,2,2-trifluoretil)-3oktan-8-karboksamid; (1R,5S)-N-(cijanometil)-3-(2-{[5-metil-6-(metilkarbamoil)piridin-3-il]amino}pirimidin-4-il)-3,8-diazabiciklo[3.2.1]oktan-8-karboksamid; 5-({4-[(1R,5S)-8-{[(1S)-2,2-difluorciklopropil]karbonil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N,3-dimetilpiridin-2-karboksamid; tert-butil-3-(2-{[4-(etilkarbamoil)-3-metilfenil]amino}-5-fluorpirimidin-4-il)-3,8-diazabiciklo[3.2.1]oktan-8-karboksilat; 5-({4-[(1R,5S)-8-{[(1R,2R)-2-cijanociklopropil]karbonil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N,3-dimetilpiridin-2-karboksamid; 3-klor-5-({4-[(1R,5S)-8-{[(1S)-2,2-difluorciklopropil]karbonil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N-metilpiridin-2-karboksamid; N-(1-metil-1H-pirazol-4-il)-4-[(1R,5S)-8-(1,2-tiazol-5-ilmetil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-amin; [(1S)-2,2-difluorciklopropil]{(1R,5S)-3-[2-({6-[(2S)-1-hidroksipropan-2-il]piridin-3-il}amino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]okt-8-il}metanon; 3-klor-5-({4-[1R,5S)-8-{[(1R,2R)-2-cijanociklopropil]karbonil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N-metilpiridin-2-karboksamid; [(1S)-2,2-difluorciklopropil][(1R,5S)-3-(2-{[5-fluor-6-(hidroksimetil)piridin-3-il]amino}pirimidin-4-il)-3,8-diazabiciklo[3.2.1]okt-8-il]metanon; 5-[(4-{(1R,5S)-8-[(2,2-difluorciklopropil)karbonil]-3,8-diazabiciklo[3.2.1]okt-3-il}pirimidin-2-il)amino]-3-metilpiridin-2-karboksamid; 5-({4-[(1R,5S)-8-(ciklopropilkarbonil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-N,3-dimetilpiridin-2-karboksamid; (1R,5S)-N-etil-3-(2-{[5-metil-6-(metilkarbamoil)piridin-3-il]amino}pirimidin-4-il)-3,8-diazabiciklo[3.2.1]oktan-8-karboksamid; [(1S)-2,2-difluorciklopropil]{(1R,5S)-3-[2-({6-[(2R)-1-hidroksipropan-2-il]piridin-3-il}amino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]okt-8-il}metanon; N-(1-metil-1H-pirazol-4-il)-4-[(1R,5S)-8-(1,2-oksazol-5-ilmetil)-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-amin; ciklopropil{(1R,SS)-3-[2-(1H-pirazol-4-ilamino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]okt-8-il}metanon; 5-({4-[(1R,5S)-8-{[(1R,2R)-2-cijanociklopropil]karbonil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-3-fluor-N-metilpiridin-2-karboksamid; [(1R)-2,2-difluorciklopropil]{(1R,5S)-3-[2-(1H-pirazol-4-ilamino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]okt-8-ilmetanon; i 5-({4-[(1R,5S)-8-{[(1R)-2,2-difluorciklopropil]karbonil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-3-fluor-N-metilpiridin-2-karboksamid; ili njihove farmaceutski prihvatljive soli.
8. Spoj u skladu s patentnim zahtjevom 4, naznačen time što se bira iz skupine koju čine: (1R)-2,2-difluor-N-[(1S,5R,6R)-3-{5-fluor-2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-6-metil-3-azabiciklo[3.1.0]heks-1-il]ciklopropankarboksamid; N-[(1S,5R,6R)-3-(2-{[5-klor-6-(hidroksimetil)piridin-3-il]amino}-5-fluorpirimidin-4-il)-6-metil-3-azabiciklo[3.1.0]heks-1-il]ciklopropankarboksamid; i N-[(1S,5R,6R)-3-(5-fluor-2-{[6-(2-hidroksietil)piridin-3-il]amino}pirimidin-4-il)-6-metil-3-azabiciklo[3.1.0]heks-1-il]ciklopropankarboksamid; ili njihove farmaceutski prihvatljive soli.
9. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj [(1S)-2,2-difluorciklopropil]{(1R,5S)-3-[2-(1H-pirazol-4-ilamino)pirimidin-4-il]-3,8-diazabiciklo[3.2.1]okt-8-il}metanon; ili njegova farmaceutski prihvatljiva sol.
10. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj [(1S)-2,2-difluorciklopropil][(1R,5S)-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il}-3,8-diazabiciklo[3.2.1]okt-8-il]metanon; ili njegova farmaceutski prihvatljiva sol.
11. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj 5-({4-[(1R,5S)-8-{[(1S)-2,2-difluorciklopropil]karbonil}-3,8-diazabiciklo[3.2.1]okt-3-il]pirimidin-2-il}amino)-3-fluor-N-metilpiridin-2-karboksamid; ili njegova farmaceutski prihvatljiva sol.
12. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj (1R,5S)-N-etil-3-{2-[(1-metil-1H-pirazol-4-il)amino]pirimidin-4-il-3,8-diazabiciklo[3.2.1]oktan-8-karboksamid; ili njegova farmaceutski prihvatljiva sol.
13. Farmaceutski ili veterinarski pripravak, naznačen time što sadrži spoj u skladu s patentnim zahtjevom 1, ili njegovu farmaceutski prihvatljivu sol, kao i farmaceutski prihvatljivu podlogu.
14. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski prihvatljiva solvat navedenog spoja ili soli, naznačen time što je namijenjen upotrebi u liječenju ili sprječavanju poremećaja ili stanja koje se bira između upale, autoimune bolest, upale živčanog tkiva, artritisa, reumatoidnog artritisa, spondiloartropatija, sistemnog eritematoznog lupusa, lupoznog nefritisa, osteoartritisa, gihtičnog artritisa, boli, groznice, sarkoidoze pluća, silikoze, kardiovaskularne bolesti, ateroskleroze, infarkta miokarda, tromboze, kongestivne srčane insuficijencije i reperfuzijske ozljede srca, kardiomiopatije, inzulta, ishemije, reperfuzijske ozljede, edema na mozgu, traume mozga, neurodegeneracije, bolesti jetre, upalne bolesti crijeva, Crohnove bolesti, ulceroznog kolitisa, nefritisa, retinitisa, retinopatije, degeneracije makule, glaukoma, dijabetesa (tip 1 i tip 2), dijabetične neuropatije, virusne i bakterijske infekcije, mialgije, endotoksičnog šok, sindrom toksičnog šoka, osteoporoze, multiple skleroze, endometrioze, menstrualnih grčeva, vaginitisa, kandidijaze, raka, fibroze, pretilosti, mišićne distrofije, polimiozitisa, dermatomiozitis, autoimunog hepatitisa, primarne bilijarne ciroze, primarnog sklerozantnog kolangitisa, vitiliga, alopecije, Alzheimerove bolesti, crvenila kože, egzema, psorijaze, atopičnog dermatitisa i opeklina od sunca.
15. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski prihvatljiva solvat navedenog spoja ili soli, naznačen time što je namijenjen upotrebi u liječenju ili sprječavanju poremećaja ili stanja koje se bira između akutne mijeloidne leukemije, akutne limfoblastne leukemije T-stanica, multiplog mijeloma, rak gušterače, tumora na mozgu, glioma, uključujući astrocitom, oligodendrogliom, te glioblastom, akutne traume CNS-a uključujući traumatsku ozljedu mozga, encefalitis, inzult, te ozljedu kralježnične moždine, epilepsije, napadaja, PD, ALS, frontotemporalne demencije, te neuropsihijatrijskih poremećaja, uključujući shizofreniju, bipolarni poremećaj, depresiju, depresiju otporna na liječenje, PTSD, anksioznost, te encefalopatije uzrokovane autoprotutijelima.
16. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski prihvatljiva solvat navedenog spoja ili soli, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevom 14, gdje je poremećaj ili stanje ulcerozni kolitis.
17. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski prihvatljiva solvat navedenog spoja ili soli, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevom 14, gdje je poremećaj ili stanje Crohnova bolest.
18. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski prihvatljiva solvat navedenog spoja ili soli, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevom 14, gdje je poremećaj ili stanje alopecija.
19. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski prihvatljiva solvat navedenog spoja ili soli, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevom 14, gdje je poremećaj ili stanje psorijaza.
20. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski prihvatljiva solvat navedenog spoja ili soli, naznačen time što je u kombinaciji s drugim farmakološki aktivnim spojem.
21. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski prihvatljiva solvat navedenog spoja ili soli, naznačen time što je namijenjen upotrebi kao medikament.
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