SI2509955T1 - Pirazolni derivati kot modulatorji kalcijevega kanala, ki se aktivira s sproščanjem kalcija - Google Patents

Pirazolni derivati kot modulatorji kalcijevega kanala, ki se aktivira s sproščanjem kalcija Download PDF

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Publication number
SI2509955T1
SI2509955T1 SI201031710T SI201031710T SI2509955T1 SI 2509955 T1 SI2509955 T1 SI 2509955T1 SI 201031710 T SI201031710 T SI 201031710T SI 201031710 T SI201031710 T SI 201031710T SI 2509955 T1 SI2509955 T1 SI 2509955T1
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Slovenia
Prior art keywords
pyrazol
substituted
unsubstituted
cyclopropyl
trifluoromethyl
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SI201031710T
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English (en)
Inventor
Peyyappan 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 SI2509955T1 publication Critical patent/SI2509955T1/sl

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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
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  1. PIRAZOLNI DERIVATI KOT MODULATORJI KALCIJEVEGA KANALA, KI SE AKTIVIRA S SPROŠČANJEM KALCIJA Patentni zahtevki
    1. Spojina s formulo
    (l) ali njen tavtomer, N-oksid, farmacevtsko sprejemljiv ester ali farmacevtsko sprejemljiva sol, v kateri obroč Hy pomeni
    ki je po izbiri substituiran z R'"; R1 je ciklopropil; R2 je izbran izmed CH3, CH2F, CHF2, CF3, substituiranega ali nesubstituiranega C(3-5)Cikloalkila, CH2-ORa, CH2-NRaRb, CN in COOH; obroč Ar je izbran izmed
    Li in l_2 skupaj pomenita -NH-C(=X)- ali -C(=X)NH; A je odsoten ali je izbran izmed -(CR'R")- ali -NRa; R' in R" sta enaka ali različna in sta neodvisno izbrana izmed vodika, hidroksi, ciano, halogena, -ORa, -COORa, -S(=O)q-Ra, -NRaRb,-C(=X)-Ra, substituirane ali nesubstituirane C^alkilne skupine, substituiranega ali nesubstituiranega C(i_ 6)alkenila, substituiranega ali nesubstituiranega C(1_6)alkinila in substituiranega ali nesubstituiranega C(3-s)Cikloalkila, ali sta lahko R' in R" združena, da tvorita substituiran ali nesubstituiran nasičen ali nenasičen 3-6-členski obroč, ki lahko po izbiri vključuje enega ali več heteroatomov, ki so lahko enaki ali različni in so izbrani izmed O, NRa in S; R'" je izbran izmed vodika, hidroksi, ciano, halogena, -ORa, -COORa, - S(=O)q-Ra, -NRaRb, -C(=X)-Ra, substituirane ali nesubstituirane C(i-6)alkilne skupine, substituiranega ali nesubstituiranega C(i_6)alkenila, substituiranega ali nesubstituiranega C(i_6)alkinila in substituiranega ali nesubstituiranega C(3. 5)Cikloalkila, pri vsakem pojavljanju je X neodvisno izbran izmed O, S in -NRa; Cy je izbran izmed
    pri vsakem pojavljanju sta Ra in Rb enaka ali različna in sta neodvisno izbrana izmed vodika, nitro, hidroksi, ciano, 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-, substituiranega ali nesubstituiranega alkila, substituiranega ali nesubstituiranega alkenila, substituiranega ali nesubstituiranega alkinila, substituiranega ali nesubstituiranega cikloalkila, substituiranega ali nesubstituiranega cikloalkilalkila, substituiranega ali nesubstituiranega cikloalkenila, substituiranega ali nesubstituiranega heterociklila, substituiranega ali nesubstituiranega heterociklilalkila, substituiranega ali nesubstituiranega arila, substituiranega ali nesubstituiranega arilalkila, substituiranega ali nesubstituiranega heteroarila in substituiranega ali nesubstituiranega heteroarilalkila, ali kadar sta Ra in Rb neposredno vezana na isti atom, sta lahko združena, da tvorita substituiran ali nesubstituiran nasičen ali nenasičen 3-10-členski obroč, ki lahko po izbiri vključuje enega ali več heteroatomov, ki so lahko enaki ali različni in izbrani izmed O, NRC in S; pri vsakem pojavljanju sta lahko Rc in Rd enaka ali različna in sta neodvisno izbrana izmed vodika, nitro, hidroksi, ciano, halogena, substituiranega ali nesubstituiranega alkila, substituiranega ali nesubstituiranega alkenila, substituiranega ali nesubstituiranega alkinila, substituiranega ali nesubstituiranega cikloalkila, substituiranega ali nesubstituiranega cikloalkilalkila, substituiranega ali nesubstituiranega cikloalkenila, substituirane ali nesubstituirane heterociklične skupine, substituiranega ali nesubstituiranega heterociklilalkila, ali kadar sta dva substituenta Rc in/ali Rd neposredno vezana na isti atom, sta lahko združena, da tvorita substituiran ali nesubstituiran nasičen ali nenasičen 3-10-členski obroč, ki lahko po izbiri vključuje enega ali več heteroatomov, ki so enaki ali različni in izbrani izmed O, NH in S; pri vsakem pojavljanju je Y izbran izmed O, S in -NRa; in pri vsakem pojavljanju q neodvisno pomeni 0, 1 ali 2.
  2. 2. Spojina po zahtevku 1, v kateri je Hy
  3. 3. Spojina po katerem koli od zahtevkov 1 ali 2, v kateri L1 in L2 skupaj pomenita -NH-C(=O)-.
  4. 4. Spojina po katerem koli od zahtevkov 1-3, v kateri je A odsoten.
  5. 5. Spojina s formulo
    (IA-III) ali njen tavtomer, N-oksid, farmacevtsko sprejemljiv ester ali farmacevtsko sprejemljiva sol, v kateri R1 in R2 sta oba ciklopropil ali je eden izmed R1 in R2 CF3, drugi pa je ciklopropil; T je CF ali N in U, V, W so neodvisno CH, CF ali N; L1 in L2 skupaj pomenita -NH-C(=X)-, -NH-S(=O)q-, -C(=X)NH- ali -S(=O)qNH- ali -NH-CR'R"-; A je odsoten ali izbran izmed -(CR'R")- in -NRa; pri vsakem pojavljanju sta R' in R" enaka ali različna in neodvisno izbrana izmed vodika ali substituirane ali nesubstituirane C(1_6)alkilne skupine ali sta lahko R' in R" združena, da tvorita substituiran ali nesubstituiran nasičen ali nenasičen 3-6-
    členski obroč, ki lahko po izbiri vključuje enega ali več heteroatomov, ki so lahko enaki ali različni in izbrani izmed O, NRa in S; R'" je izbran izmed vodika ali halogena; pri vsakem pojavljanju je X neodvisno izbran izmed O, S in -NRa; Cy je izbran izmed
    pri vsakem pojavljanju sta Ra in Rb enaka ali različna in sta neodvisno izbrana izmed vodika, nitro, hidroksi, ciano, 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-, substituiranega ali nesubstituiranega alkila, substituiranega ali nesubstituiranega alkenila, substituiranega ali nesubstituiranega alkinila, substituiranega ali nesubstituiranega cikloalkila, substituiranega ali nesubstituiranega cikloalkilalkila, substituiranega ali nesubstituiranega cikloalkenila, substituiranega ali nesubstituiranega heterociklila, substituiranega ali nesubstituiranega heterociklilalkila, substituiranega ali nesubstituiranega arila, substituiranega ali nesubstituiranega arilalkila, substituiranega ali nesubstituiranega heteroarila in substituiranega ali nesubstituiranega heteroarilalkila, ali kadar sta substituenta Ra in Rb neposredno vezana na isti atom, sta lahko združena, da tvorita substituiran ali nesubstituiran nasičen ali nenasičen 3-10-členski obroč, ki lahko po izbiri vključuje enega ali več heteroatomov, ki so lahko enaki ali različni in so izbrani izmed O, NRC in S;
    pri vsakem pojavljanju sta lahko Rc in Rd enaka ali različna in sta neodvisno izbrana izmed vodika, nitro, hidroksi, ciano, halogena, substituiranega ali nesubstituiranega alkila, substituiranega ali nesubstituiranega alkenila, substituiranega ali nesubstituiranega alkinila, substituiranega ali nesubstituiranega cikloalkila, substituiranega ali nesubstituiranega cikloalkilalkila, substituiranega ali nesubstituiranega cikloalkenila, substituirane ali nesubstituirane heterociklične skupine, substituiranega ali nesubstituiranega heterociklilalkila, ali kadar sta dva substituenta Rc in/ali Rd neposredno vezana na isti atom, sta lahko združena, da tvorita substituiran ali nesubstituiran nasičen ali nenasičen 3-10-členski obroč, ki lahko po izbiri vključuje enega ali več heteroatomov, ki so enaki ali različni in so izbrani izmed O, NH in S; pri vsakem pojavljanju je Y izbran izmed O, S in -NRa; in pri vsakem pojavljanju q neodvisno pomeni 0, 1 ali 2.
  6. 6. Spojina po katerem koli od zahtevkov od 1 do 5, v kateri Li in L2 skupaj pomenita -NH-C(=O)-, -C(=O)NH- ali -NHCH?-.
  7. 7. Spojina po katerem koli od zahtevkov od 1 do 6, v kateri je A odsoten.
  8. 8. Spojina po katerem koli od zahtevkov 1 ali 5, izbrana izmed: A/-[4-(3,5-diciklopropil-1/-/-pirazol-1-il)-3-fluorofenil]-2-metilbenzamida /V-[4-(3,5-diciklopropil-1/-/-pirazol-1-il)-3-fluorofenil]-2,3-difluorobenzamida A/-[4-(3,5-diciklopropil-1H-pirazol-1-il)-3-fluorofenil]-2,6-difluorobenzamida A/-[4-(3,5-diciklopropil-1 /-/-pirazol-1 -il)-3-fluorofenil]nikotinamida /V-[4-(3,5-diciklopropil-1/7-pirazol-1-il)-3-fluorofenil]izonikotinamida /V-[4-(3,5-diciklopropil-1 /-/-pirazol-1-il)-3-fluorofenil]-4-metilpirimidin-5-karboksamida 6-(3,5-diciklopropil-1 /-/-pirazol-1 -il)-/V-o-tolilnikotinamida /V-[6-(3,5-diciklopropil- 1 /-/-pirazol-1 -il)piridin-3-il]-2-fluorobenzamida /V-[6-(3,5-diciklopropil-1/-/-pirazol-1-il)piridin-3-il]-2,3-difluorobenzamida A/-[6-(3,5-diciklopropil-1/-/-pirazol-1-il)piridin-3-il]-2,6-difluorobenzamida /V-[6-(3,5-diciklopropil-1 /-/-pirazol-1 -iI)piridin-3-il]nikotinamid dihidroklorida /V-[6-(3,5-diciklopropil-1 H-pirazol-1 -il)piridin-3-il]izonikotinamida /V-[6-(3,5-diciklopropil-1 /-/-pirazol-1-il)piridin-3-il]-3-fluoroizonikotinamida 3.5- dikloro-A/-[6-(3,5-diciklopropil-1 /-/-pirazol-1 -il)piridin-3-il]izonikotinamida /V-[6-(3,5-diciklopropil-1 H-pirazol-1 -il)piridin-3-il]-4-metilpirimidin-5-karboksamida /V-{4-[5-ciklopropil-3-(trifluorometil)-1 /-/-pirazol-1 -il]-3-fluorofenil}-2-metilbenzamida /V-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}-2,3- difluorobenzamida /V-{4-[5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]-3-fluorofenil}-2,6-difluorobenzamida /V-{4-[5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]-3-fluorofenil}nikotinamida /V-{4-[5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]-3-fluorofenil}izonikotinamida /V-{4-[5-ciklopropil-3-(trifluorometil)-1 /-/-pirazol-1 -il]-3-fluorofenil}-3-fluoroizonikotinamida 3.5- dikloro-/V-{4-[5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]-3- fluorofeniljizonikotinamida /V-{4-[5-ciklopropil-3-(trifluorometil)-1/7-pirazol-1-il]-3-fluorofenil}-4-metilpirimidin- 5-karboksamida /V-{4-[5-ciklopropil-3-(trifluorometil)-1/7-pirazol-1-il]-3-fliiorofenil}-/\/,4- dimetilpirimidin-5-karboksamida /V-{4-[4-kloro-5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]-3-fluorofenil}-2-(piridin-2-il)acetamida 1-{4-[5-ciklopropil-3-(trifluorometil)-1/7-pirazol-1-il]-3-fluorofenil}-3-(4- metilpirimidin-5-il)sečnine /V-{4-[5)-ciklopropil-3-(triflurometil)-1/-/-pirazol-1-il]3-flurofenil}-2,6-dikloro benzamida 4-[5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]-/V-(2,3-difluorofenil)-3- fluorobenzamida 4-[5-ciklopropil-3-(trifluorometil)-1 /-/-pirazol-1 -il]-/V-(2,6-difluorofenil)-3-fluorobenzamida /V-{6-(5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]piridin-3-il}-3,5- dimetilizoksazole-4-karboksamida /V-{6-(5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]piridin-3-il}-2-metilbenzamida 2-kloro-N-{6-[5-ciklopropil-3-(trifluorometil)-1 H-pirazol-1-il]piridin-3-il}benzamida N-(6-(5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il)piridin-3-il)-2-fluorobenzamida A/-{6-[5-ciklopropil-3-(tnfluorometil)-1 H-pirazol-1 -il]piridin-3-il}-2,3- difluorobenzamida /V-{6-[5-ciklopropil-3-(trifluorometil)-1 /-/-pirazol-1-il]piridin-3-il}-2,6- difluorobenzamida /V-{6-[5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]piridin-3-il}pikolinamida /V-{6-[5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]piridin-3-il}-3-metilpikolinamida /V-{6-[5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]piridin-3-il}nikotinamida /V-{6-[5-ciklopropil-3-(trifluorometil)-1 H-pirazol-1 -il]piridin-3-il}-2-metilnikotinamida /V-{6-[5-ciklopropil-3-(trifluorometil)-1 /7-pirazol-1 -il]piridin-3-il}izonikotinamida /S/-{6-[5-ciklopropil-3-(trifluorometil)-1 /-/-pirazol-1 -il]piridin-3-il}-3- fluoroizonikotinamida 3.5- dikloro-/V-{6-[5-ciklopropil-3-(trifluorometil)-1 /-/-pirazol-1-il]piridin-3-iljizonikotinamida /V-{6-[5-ciklopropil-3-(trifluorometil)-1 /-/-pirazol-1-il]piridin-3-il}-4-metilpirimidin-5-karboksamida /V-{6-[5-ciklopropil-3-(trifluorometil)-1 /-/-pirazol-1-il]piridin-3-il}-2-(piridin-2-il)acetamida /V-{6-[5-ciklopropil-3-(trifluorometil)-1/-/-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- metilpirimidin-5-karboksamida 6-[5-ciklopropil-3-(trifIuorometiI)-1 /-/-pirazol-1 -iΙ]-Λ/-(2,3-difluorofenil) nikotinamida 6-[5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]-/\/-(2,6-difluorofenil) nikotinamida /V-{2-[5-ciklopropil-3-(trifluorometil)-1 /-/-pirazol-1-il]pirimidin-5-il}-2,6-difluorobenzamida 3.5- dikloro-/V-[4-(3,5-diciklopropil-1/-/-pirazol-1-il)-3-fluorofenil]izonikotinamida /V-(2-kloro-6-fluorofenil)-4-[5-ciklopropil-3-(trifluorometil)-1 /-/-pirazol-1 -il]-3-fluorobenzamida /V-{4-[5-ciklopropil-3-(trifluorometil)-1 /7-pirazol-1-il]-3,5-difluorofenil}-4-metilpirimidin-5-karboksamida {4-[5-ci klop ropi l-3-(trif I uo rometi I)-1 H-pirazol-1 -i l]-3-f I uo rofe n il}-1 -fenilciklobutankarboksamida N-{2-[5-ciklopropil-3-(trifluorometil)-1 /-/-pirazol-1 -il]pirimidin-5-il}-4-metilpirimidin-5-karboksamida 4-[5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]-3-fluoro-/V-(4-metilpirimidin-5-il) benzamida in /V-{4-[3-ciklopropil-5-(difluorometil)-1/7-pirazol-1-il]-3-fluorofenil}-2,6-difluorobenzamida in /V-{4-[5-ciklopropil-3-(difluorometil)-1/-/-pirazol-1-il]-3-fluorofenil}-2,6- difluorobenzamida ali njen tavtomer, N-oksid, farmacevtsko sprejemljiv ester ali farmacevtsko sprejemljiva sol.
  9. 9. Spojina po katerem koli od zahtevkov 1 ali 5, ki je /V-{6-[5-ciklopropil-3-(trifluorometil)-1/-/-pirazol-1-il]piridin-3-il}-2-metilbenzamid, ali njena farmacevtsko sprejemljiva sol.
  10. 10. Spojina po katerem koli od zahtevkov 1 ali 5, ki je A/-{6-[5-ciklopropil-3-(trifluorometil)-l /-/-pirazol-1 -il]piridin-3-il}-3-fluoroizonikotinamid, ali njena farmacevtsko sprejemljiva sol.
  11. 11. Farmacevtski sestavek, ki obsega eno ali več spojin po katerem koli od zahtevkov od 1 do 10 in farmacevtsko sprejemljiv nosilec.
  12. 12. Uporaba spojine po katerem koli od zahtevkov od 1 do 10 za proizvodnjo zdravila za zdravljenje raka.
  13. 13. Uporaba spojine po katerem koli od zahtevkov od 1 do 10 za proizvodnjo zdravila za zdravljenje avtoimunskega obolenja, pri čemer je avtoimunsko obolenje kronična obstruktivna pljučna bolezen, revmatoidni artritis, vnetna črevesna bolezen, alergijski rinitis, astma, multipla skleroza, psoriaza, Crohnova bolezen, kolitis, ulcerozni kolitis, artritis, kostne bolezni, povezane s povečano kostno resorpcijo, ali kronična obstruktivna bolezen dihal.
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