HRP20181076T1 - Pirazolski derivati kao modulatori kalcijevih kanala aktiviranih oslobađanjem kalcija - Google Patents

Pirazolski derivati kao modulatori kalcijevih kanala aktiviranih oslobađanjem kalcija Download PDF

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Publication number
HRP20181076T1
HRP20181076T1 HRP20181076TT HRP20181076T HRP20181076T1 HR P20181076 T1 HRP20181076 T1 HR P20181076T1 HR P20181076T T HRP20181076T T HR P20181076TT HR P20181076 T HRP20181076 T HR P20181076T HR P20181076 T1 HRP20181076 T1 HR P20181076T1
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HR
Croatia
Prior art keywords
pyrazol
substituted
unsubstituted
cyclopropyl
trifluoromethyl
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HRP20181076TT
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English (en)
Inventor
Meyyappan Muthuppalaniappan
Srikant Viswanadha
Gayatri Swaroop Merikapudi
Swaroop Kumar V.S. Vakkalanka
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Rhizen Pharmaceuticals S.A.
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Publication of HRP20181076T1 publication Critical patent/HRP20181076T1/hr

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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
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    • A61K31/415—1,2-Diazoles
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
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Claims (13)

1. Spoj formule ili njegov tautomer, N-oksid, farmaceutski prihvatljiv ester ili njegova farmaceutski prihvatljiva sol, naznačeno time, što prsten Hy predstavlja po izboru supstituiran s R'"; R1 je ciklopropil; R2 se bira iz CH3, CH2F, CHF2, CF3, supstituiranog ili nesupstituiranog C(3-5) cikloalkila, CH2-ORa, CH2-NRaRb, CN i COOH; Prsten Ar se bira iz L1 i L2 zajedno predstavljaju -NH-C(= X)- ili -C(= X)NH; A je odsutan ili je odabran iz -(CR'R")- ili -NRa; R' i Rʺ su jednaki ili različiti i neovisno biraju između vodika, hidroksi, cijano, halogena; -ORa, -COORa, -S(=O)q-Ra, -NRaRb, -C(=X)-Ra, supstituisane ili nesupstituisane C(1-6) alkil skupine, supstituiranog ili nesupstituiranog C(1-6) alkenila, supstituiranog ili nesupstituiranog C(1-6) alkinila i supstituiranog ili nesupstituiranog C(3-5) cikloalkila; ili R' i Rʺ mogu biti spojeni da tvore supstituirani ili nesupstituirani, zasićeni ili nezasićeni prsten od 3-6 članova, koji po potrebi može sadržavati jedan ili više heteroatoma koji mogu biti jednaki ili različiti i odabrani su između O, NRa i S; Rʺʹ je odabran između vodika, hidroksi, cijano, halogena; -ORa, -COORa, -S(=O)q-Ra, -NRaRb, -C(=X)-Ra, supstituirane ili nesupstituirane C(1-6) alkil grupe, supstituiranog ili nesupstituiranog C(1-6) alkenila, supstituiranog ili nesupstituiranog C(1-6) alkinila i supstituiranog ili nesupstituiranog C(3-5) cikloalkila; svako pojavljivanje X je neovisno odabrani iz O, S i -NRa; Cy se bira iz svako pojavljivanje Ra i Rb, su jednaki ili različiti i neovisno se biraju između vodika, nitro, hidroksi, cijano, halogena, -ORc, -S(=O)q-Rc, -NRcRd, -C(=Y)-Rc, -CRcRd-C(=Y)-Rc, -CRcRd-Y-CRcRd-, -C(=Y)-NRcRd-, -NRRd-C(=Y)-NRcRd-, -S(=O)q-NRcRd-, -NRcRd-S(=O)q-NRcRd-, -NRcRd-NRcRd-, supstituiranog ili nesupstituiranog alkila, supstituiranog ili nesupstituiranog alkenila, supstituiranog ili nesupstituiranog alkinila, supstituiranog ili nesupstituiranog cikloalkila, supstituiranog ili nesupstituiranog cikloalkilalkila, supstituiranog ili nesupstituiranog cikloalkenila, supstituiranog ili nesupstituiranog heterociklila, supstituiranog ili nesupstituiranog heterociklilalkila, supstituiranog ili nesupstituiranog arila, supstituiranog ili nesupstituiranog arilalkila, supstituiranog ili nesupstituiranog heteroarila i supstituiranog ili nesupstituiranog heteroarilalkila, ili kada su Ra i Rb izravno vezani za jednaki atom, mogu biti spojeni da oblikuju supstituirani ili nesupstituirani, zasićeni ili nezasićeni prsten od 3-10 članova, koji može opcionalno uključiti, jedan ili više heteroatoma jednakih ili različitih i odabrani su između O, NRc i S; svako pojavljivanje Rc i Rd, mogu biti jednaki ili različiti i neovisno su odabrani između vodika, nitro, hidroksi, cijano, halogena, supstituiranog ili nesupstituiranog alkila, supstituiranog ili nesupstituiranog alkenila, supstituiranog ili nesupstituiranog alkinila, supstituiranog ili nesupstituiranog cikloalkila, supstituiranog ili nesupstituiranog cikloalkilalkila, supstituiranog ili nesupstituiranog cikloalkenila, supstituirane ili nesupstituirane heterociklične skupine, supstituiranog ili nesupstituiranog heterociklilalkila, ili kada su dva Rci/ili Rd supstituenta izravno vezana za jednaki atom, oni mogu biti spojeni da oblikuju supstituirani ili nesupstituirani, zasićeni ili nezasićeni prsten od 3-10 članova, koji može opcionalno uključivati, jedan ili više heteroatoma, koji mogu biti jednaki ili različiti i izabrani su između O, NH i S; svako pojavljivanje Y je izabrano između O, S i -NRa; i svako pojavljivanje q neovisno predstavlja 0, 1 ili 2;
2. Spoj sukladno patentnom zahtjevu 1, naznačeno time, da je Hy
3. Spoj sukladno bilo kojem od patentnih zahtjeva 1 ili 2, naznačeno time, što L1 i L2 zajedno predstavljaju -NH-C(=O)-.
4. Spoj sukladno bilo kojem od patentnih zahtjeva 1-3, naznačeno time, što je A je odsutan.
5. Spoj formule ili njegov tautomer, N-oksid, farmaceutski prihvatljiv ester, ili njegova farmaceutski prihvatljiva sol, gdje su R1 i R2 oboje ciklopropil ili jedan od R1 i R2 je CF3 i drugi je ciklopropil; T je CF ili N i U, V, W su neovisno CH, CF ili N; L1 i L2 zajedno predstavljaju -NH-C(=X)-, -NH-S(= O)q-, -C(= X)NH-, ili - S(= O)q- NH- ili -NH-CR'R"-; A je odsutan ili odabran između -(CR'R")- i -NRa; svako pojavljivanje R' i R", su isti ili različiti i neovisno su odabrani između vodika ili supstitursane ili nesupstituirane C(1-6) alkil skupine, ili R' i R" mogu biti spojeni da oblikuju supstituirani ili nesupstituirani, zasićeni ili nezasićeni 3-6 člani prsten, koji može opcionalno uključivati, jedan ili više heteroatoma koji mogu biti jednaki ili različiti i odabrani su između O, NRa i S; Rʺʹ je odabran između vodika ili halogena; svako pojavljivanje X je neovisno odabran između O, S i -NRa; Cy je odabran između svako pojavljivanje Ra i Rb, su jednaki ili različiti i neovisno su odabrani između vodika, nitro, hidroksi, cijano, halogena, -ORc, -S(=O)q-Rc, -NRcRd, -C(=Y)-Rc, -CRcRd-C(=Y)-Rc, -CRcRd-Y-CRcRd-, -C(=Y)-NRcRd-, -NRRd-C(=Y)-NRcRd-, -S(=O)q-NRcRd, -NRcRd-S(=O)q-NRcRd-, -NRcRd-NRcRd-, supstituiranog ili nesupstituiranog alkila, supstituiranog ili nesupstituiranog alkenila, supstituiranog ili nesupstituiranog alkinila, supstituiranog ili nesupstituiranog cikloalkila, supstituiranog ili nesupstituiranog cikloalkilalkila, supstituiranog ili nesupstituiranog cikloalkenila, supstituiranog ili nesupstituiranog heterociklila, supstituiranog ili nesupstituiranog heterociklilalkila, supstituiranog ili nesupstituiranog arila, supstituiranog ili nesupstituiranog arilalkila, supstituiranog ili nesupstituiranog heteroarila i supstituiranog ili nesupstituiranog heteroarilalkila, ili kada su Ra i Rb supstituent izravno vezani za jednaki atom, oni mogu biti spojeni da oblikuju supstituirani ili nesupstituirani, zasićeni ili nezasićeni prsten od 3-10 članova, koji može opcionalno uključite, jedan ili više heteroatoma koji mogu biti jednaki ili različiti i odabrani između O, NRc i S; svako pojavljivanje Rc i Rd, mogu biti jednaki ili različiti i neovisno odabrani između vodika, nitro, hidroksi, cijano, halogena, supstituiranog ili nesupstituiranog alkila, supstituiranog ili nesupstituiranog alkenila, supstituiranog ili nesupstituiranog alkinila, supstituiranog ili nesupstituiranog cikloalkila, supstituiranog ili nesupstituiranog cikloalkilalkila, supstituiranog ili nesupstituiranog cikloalkenila, supstituirane ili nesupstituirane heterociklične skupine, supstituiranog ili nesupstituiranog heterociklilalkila, ili kada su dva Rci/ili Rd supstituenta izravno vezana za jednaki atom, oni mogu biti spojeni da oblikuju supstituirani ili nesupstituirani, zasićeni ili nezasićeni prsten od 3-10 članova, koji može opcionalno uključiti, jedan ili više heteroatoma, koji mogu biti jednaki ili različiti i odabrani između O, NH i S; svako pojavljivanje Y je odabrani između O, S i -NRa; i svako pojavljivanje q neovisno predstavlja 0, 1 ili 2.
6. Spoj sukladno bilo kojem od patentnih zahtjeva 1 do 5, naznačeno time, što L1 i L2 zajedno predstavljaju -NH-C(=O)-, -C(=O)NH- ili -NHCH2-.
7. Spoj sukladno bilo kojem od patentnih zahtjeva 1 do 6, naznačeno time, što je A odsutan.
8. Spoj sukladno bilo kojem od patentnih zahtjeva 1 do 5, odabrani između: N-[4-(3,5-diciklopropil-1H-pirazol-1-il)-3-fluorofenil]-2-metil benzamida N-[4-(3,5-diciklopropil-1H-pirazol-1-il)-3-flurofenil]]-2,3-difluorobenzamida N-[4-(3,5-diciklopropil-1H-pirazol-1-il)-3-flurofenil]]-2,6-difluorobenzamida N-[4-(3,5-diciklopropil-1H-pirazol-1-il)-3-fluorofenil] nikotinamida N-[4-(3,5-diciklopropil-1H-pirazol-l-il)-3-flurofenil] izonikotinamida N-[4-(3,5-diciklopropil-1H-pirazol-l-il)-3-flurofenil]-4-metilpirimidin-5-karboksamida 6-(3,5-diciklopropil-1H-pirazol-1-il)-N-o-tolilnikotinamida N-[6-(3,5-diciklopropil-1H-pirazol-1-il) piridin-3-il]-2-fluorobenzamida N-[6-(3,5-diciklopropil-1H-pirazol-1-il) piridin-3-il]-2,3-difluorobenzamida N-[6-(3,5-diciklopropil-1H-pirazol-1-il) piridin-3-il]-2,6-difluorobenzamida N-[6-(3,5-diciklopropil-1H-pirazol-l-il) piridin-3-il] nikotinamid dihidrohlorida N-[6-(3,5-diciklopropil-1H-pirazol-l-il) piridin-3-il] izonikotinamida N-[6-(3,5-diciklopropil-1H-pirazol-1-il) piridin-3-il]-3-fluoroizonikotinamida 3,5-dihloro-N-[6-(3,5-diciklopropil-1H-pirazol-1-il) piridin-3-il] izonikotinamida N-[6-(3,5-diciklopropil-1H-pirazol-1-il) piridin-3-il]-4-metilpirimidin-5-karboksamida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}-2-metilbenz- amida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}-2,3-difluoro- benzamida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}-2,6-difluoro- benzamida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil} nikotinamida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil} izonikotinamida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}-3-fluoroizo- nikotinamida 3,5-dihloro-N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}izo-nikotinamida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}-4-metilpirimi- din-5-karboksamida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}-N,4-dimetilpiri- midin-5-karboksamida N-{4-[4-hloro-5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}-2- (piridin-2-il) acetamida 1-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}-3-(4-metilpirimi- din-5-il) uree N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}-2,6-dikloro benzamida 4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-N-(2,3-difluorofenil)-3-fluorobenz- amida 4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-N-(2,6-difluorofenil)-3-fluorobenz- amida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-3,5-dimetilizoksaz- ol-4-karboksamida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-2-metilbenzamida 2-hloro-N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il] piridin-3-il} benzamida N-(6-(5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il)piridin-3-il)-2-fluorobenzamida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-2,3-difluorobenza- mida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-l-il]piridin-3-il}-2,6-difluorobenza- mida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il] piridin-3-il} pikolinamida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-3-metilpikolin- amida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il] piridin-3-il} nikotinamida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-2-metilnikotin- amida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il} izonikotinamida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-3-fluoroizonikotin- amida 3,5-dihloro-N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}izo-nikotinamida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-4-metilpirimidin-5-karboksamida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-2-(piridin-2-il) acetamida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-2-(piridin-4-il) acetamida N-{4-[4-kloro-5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}-4-metil-pirimidin-5-karboksamida 6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-N-(2,3-difluorofenil) nikotinamida 6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-N-(2,6-difluorofenil) nikotinamida N-{2-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]pirimidin-5-il}-2,6-difluoro- benzamida 3,5-dikloro-N-[4-(3,5-diciklopropil-1H-pirazol-1-il)-3-fluorofenil] izonikotinamida N-(2-kloro-6-fluorofenil)-4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluoro- benzamida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3,5-difluorofenil}-4-metilpiri- midin-5-karboksamida {4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}-1-fenilciklobutan- karboksamida N-{2-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]pirimidin-5-il}-4-metilpirimid- in-5-karboksamida 4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluoro-N-(4-metilpirimidin-5-il) benzamida i N-{4-[3-ciklopropil-5-(difluorometil)-1H-pirazol-1-il]-3-fluorofenil}-2,6-difluoro- benzamida i N-{4-[5-ciklopropil-3-(difluorometil)-1H-pirazol-1-il]-3-fluorofenil}-2,6-difluoro- benzamida ili njegovog tautomera, N-oksida, farmaceutski prihvatljivog estera, ili njegove farmaceutski prihvatljive soli.
9. Spoj sukladno bilo kojem od patentnih zahtjeva 1 ili 5, koje je N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-2-metilbenzamid, ili njegova farmaceutski prihvatljiva sol.
10. Spoj sukladno bilo kojem od patentnih zahtjeva 1 ili 5, koje je N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-3-fluoroizonikotinamid, ili njegova farmaceutski prihvatljiva sol.
11. Farmaceutski preparat, koji sadrži jedan ili više spojeva sukladno bilo kojem od patentnih zahtjeva 1 do 10 i farmaceutski prihvatljiv nosač.
12. Uporaba spoja sukladno bilo kojem od patentnih zahtjeva 1 do 10, za proizvodnju lijeka radi liječenja karcinoma.
13. Uporaba spoja sukladno bilo kojem od patentnih zahtjeva 1 do 10, za proizvodnju lijeka radi liječenja autoimunog poremećaja, naznačena time, što je autoimuni poremećaj kronična opstruktivna bolest pluća, reumatoidni artritis, inflamatorna bolest crijeva, alergijski rinitis, astma, multiple skleroza, psorijaza, Chronova bolest, kolitis, ulcerozni kolitis, artritis, bolesti kostiju povezane s povećanom resorpcijom kostiju ili kronične opstruktivne bolesti dišnih puteva.
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