DK2509955T3 - Pyrazolderivater som modulatorer af calciumfrigivelsesaktiveret calciumkanal - Google Patents

Pyrazolderivater som modulatorer af calciumfrigivelsesaktiveret calciumkanal Download PDF

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DK2509955T3
DK2509955T3 DK10779334.1T DK10779334T DK2509955T3 DK 2509955 T3 DK2509955 T3 DK 2509955T3 DK 10779334 T DK10779334 T DK 10779334T DK 2509955 T3 DK2509955 T3 DK 2509955T3
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pyrazol
cyclopropyl
substituted
unsubstituted
trifluoromethyl
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DK10779334.1T
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Peyyappan Muthuppalaniappan
Srikant Viswanadha
Gayatri Swaroop Merikapudi
Swaroop Kumar V S Vakkalanka
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Rhizen Pharmaceuticals S A
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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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Claims (13)

  1. PYRAZOLDERIVATER SOM MODULATORER AF CALCIUMFRIGIVELSESAKTIVERET CALCIUMKANAL
    1. Forbindelse med formlen
    eller en tautomer, et N-oxid, en farmaceutisk acceptabel ester eller et farmaceutisk acceptabelt salt deraf, hvor Ring Hy repræsenterer
    eventuelt substitueret med R'"; R1 er cyclopropyl; R2 er udvalgt fra CH3, CH2F, CHF2, CF3, substitueret eller ikke-substitueret C(3_5)cycloaIkyl, CH2-ORa, CH2-NRaRb, CN og COOH; Ring Ar er udvalgt fra
    Li og L2 sammen repræsenterer -NH-C(=X)- eller -C(=X)NH; A er fraværende eller er udvalgt fra -(CR'R”)- eller -NRa; R' og R” er det samme eller forskellige og er uafhængigt udvalgt fra hydrogen, hydroxy, cyano, halogen, -ORa, -COORa, -S(=O)q-Ra, -NRaRb,-C(=X)-Ra, substitueret eller ikke-substitueret C(1_6) alkylgruppe, substitueret eller ikke-substitueret C(1_6) alkenyl, substitueret eller ikke- substitueret C(l-6) alkynyl og substitueret eller ikke-substitueret C(3.5) cycloalkyl, eller R' og R" kan være forbundet, så de danner en substitueret eller ikke-substitueret mættet eller umættet 3-6-leddet ring, som eventuelt kan omfatte et eller flere heteroatomer, der kan være det samme eller forskellige og er udvalgt fra O, NRa og S; R'" er udvalgt fra hydrogen, hydroxy, cyano, halogen, -ORa, -COORa, -S(=O)q-Ra, -NRaRb, -C(=X)-Ra, substitueret eller ikke-substitueret C(i_6) alkylgruppe, substitueret eller ikke-substitueret C(i_ 6) alkenyl, substitueret eller ikke-substitueret C(i_6) alkynyl og substitueret eller ikke-substitueret C(3_5)Cycloa Ikyl. hver forekomst af X er uafhængigt udvalgt fra O, S og -NRa; Cy er udvalgt fra
    hver forekomst af Ra og Rb er det samme eller forskellige og er uafhængigt udvalgt fra hydrogen, nitro, hydroxy, cyano, halogen, -ORC, -S(=O)q-Rc, -NRcRd,-C(=Y)-Rc, -CRcRd-C(=Y)-Rc, -CRcRd-YCRcRd-,-C(=Y)-NRcRd-, -NRRd-C(=Y)-NRcRd-, -S(=O)q-NRcRd-, -NRcRd-S(=O)q-NRcRd-, -NRcRd-NRcRd-, substitueret eller ikke-substitueret alkyl, substitueret eller ikke-substitueret alkenyl, substitueret eller ikke-substitueret alkynyl, substitueret eller ikke-substitueret cycloalkyl, substitueret eller ikke-substitueret cycloalkylakyl, substitueret eller ikke-substitueret cycloalkenyl, substitueret eller ikke-substitueret heterocylyl, substitueret eller ikke-substitueret heterocyclylalkyl, substitueret eller ikke-substitueret aryl, substitueret eller ikke-substitueret arylalkyl, substitueret eller ikke-substitueret heteroaryl og substitueret eller ikke-substitueret heteroarylalkyl, eller når Ra og Rb er direkte bundet til det samme atom, kan de være forbundet så de danner en substitueret eller ikke-substitueret mættet eller umættet 3-10-leddet ring, som eventuelt kan omfatte et eller flere heteroatomer, som kan være det samme eller forskellige og er udvalgt fra O, NRC og S; hver forekomst af Rc og Rd kan være det samme eller forskellige og er uafhængigt udvalgt fra hydrogen, nitro, hydroxy, cyano, halogen, substitueret eller ikke-substitueret alkyl, substitueret eller ikke-substitueret alkenyl, substitueret eller ikke-substitueret alkynyl, substitueret eller ikke-substitueret cycloalkyl, substitueret eller ikke-substitueret cycloalkylakyl, substitueret eller ikke-substitueret cycloalkenyl, substitueret eller ikke-substitueret heterocyklisk gruppe, substitueret eller ikke-substitueret heterocyclylalkyl, eller når to Rc- og/eller Rd-substituenter er direkte bundet til det samme atom, kan de være forbundet så de danner en substitueret eller ikke-substitueret mættet eller umættet 3-10-leddet ring, som eventuelt kan omfatte et eller flere heteroatomer, som er det samme eller forskellige og er udvalgt fra O, NH og S; hver forekomst af Y er udvalgt fra O, S og -NRa; og hver forekomst af q uafhængigt repræsenterer 0, 1 eller 2;
  2. 2. Forbindelse ifølge krav 1, hvor Hy er
  3. 3. Forbindelse ifølge et hvilket som helst af kravene 1 til 2, hvor Li og L2 sammen repræsenterer -NH-C(=O)-.
  4. 4. Forbindelse ifølge et hvilket som helst af kravene 1-3, hvori A er fraværende.
  5. 5. Forbindelse med formlen
    eller en tautomer, et N-oxid, en farmaceutisk acceptabel ester eller et farmaceutisk acceptabelt salt deraf, hvor både R1 og R2 er cyclopropyl, eller en af R1 og R2 er CF3 og den anden er cyclopropyl; T er CF eller N og U, V, W uafhængigt er CH, CF eller N; Li og L2 sammen repræsenterer -NH-C(=X)-, -NH-S(=O)q-, -C(=X)NH-, eller -S(=O)qNH- eller -NH-CR'R"-; A er fraværende eller udvalgt fra -(CR'R")- og -NRa; hver forekomst af R' og R" er det samme eller forskellige og er uafhængigt udvalgt fra hydrogen eller substitueret eller ikke-substitueret C(1_6) alkylgruppe, eller R' og R" kan være forbundet, så de danner en substitueret eller ikke-substitueret mættet eller umættet 3-6-leddet ring, som eventuelt kan omfatte et eller flere heteroatomer, der kan være det samme eller forskellige og er udvalgt fra O, NRa og S; R'" er udvalgt fra hydrogen eller halogen; hver forekomst af X er uafhængigt udvalgt fra O, S og -NRa; Cy er udvalgt fra
    hver forekomst af Ra og Rb er det samme eller forskellige og er uafhængigt udvalgt fra hydrogen, nitro, hydroxy, cyano, halogen, -ORc, -S(=O)q-Rc, -NRcRd, -C(=Y)-Rc, -CRcRd-C(=Y)-Rc, -CRcRd-YCRcRd-,-C(=Y)-NRcRd-, -NRRd-C(=Y)-NRcRd-, -S(=O)q-NRcRd-, -NRcRd-S(=O)q-NRcRd-, -NRcRd-NRcRd-, substitueret eller ikke-substitueret alkyl, substitueret eller ikke-substitueret alkenyl, substitueret eller ikke-substitueret alkynyl, substitueret eller ikke-substitueret cycloalkyl, substitueret eller ikke-substitueret cycloalkylakyl, substitueret eller ikke-substitueret cycloalkenyl, substitueret eller ikke-substitueret heterocylyl, substitueret eller ikke-substitueret heterocyclylalkyl, substitueret eller ikke-substitueret aryl, substitueret eller ikke-substitueret arylalkyl, substitueret eller ikke-substitueret heteroaryl og substitueret eller ikke-substitueret heteroarylalkyl, eller når Ra og Rb-substituenter er direkte bundet til det samme atom, kan de være forbundet så de danner en substitueret eller ikke-substitueret mættet eller umættet 3-10-leddet ring, som eventuelt kan omfatte et eller flere heteroatomer, som kan være det samme eller forskellige og er udvalgt fra O, NRC og S; hver forekomst af Rc og Rd kan være det samme eller forskellige og er uafhængigt udvalgt fra hydrogen, nitro, hydroxy, cyano, halogen, substitueret eller ikke-substitueret alkyl, substitueret eller ikke-substitueret alkenyl, substitueret eller ikke-substitueret alkynyl, substitueret eller ikke-substitueret cycloalkyl, substitueret eller ikke-substitueret cycloalkylakyl, substitueret eller ikke-substitueret cycloalkenyl, substitueret eller ikke-substitueret heterocyklisk gruppe, substitueret eller ikke-substitueret heterocyclylalkyl, eller når to Rc- og/eller Rd-substituenter er direkte bundet til det samme atom, kan de være forbundet så de danner en substitueret eller ikke-substitueret mættet eller umættet 3-10-leddet ring, som eventuelt kan omfatte et eller flere heteroatomer, som er det samme eller forskellige og er udvalgt fra O, NH og S; hver forekomst af Y er udvalgt fra O, S og -NRa; og hver forekomst af q uafhængigt repræsenterer 0, 1 eller 2.
  6. 6. Forbindelse ifølge et hvilket som helst af kravene 1 til 5, hvor Li og L2 sammen repræsenterer -NH-C(=O)-, -C(=O)NH- eller -NHCH2-,
  7. 7. Forbindelse ifølge et hvilket som helst af kravene 1 til 6, hvor A er fraværende.
  8. 8. Forbindelse ifølge et hvilket som helst af kravene 1 eller 5 udvalgt fra: N-[4-(3,5-dicyclopropyl-lH-pyrazol-l-yl)-3-fluorphenyl]-2methylbenzamid N-[4-(3,5-dicyclopropyl-lH-pyrazol-l-yl)-3-fluorphenyl]-2,3-difluorbenzamid N-[4-(3,5-dicyclopropyl-lH-pyrazol-l-yl)-3-fluorphenyl]-2,6-difluorbenzamid N-[4-(3,5-dicyclopropyl-lH-pyrazol-l-yl)-3-fluorphenyl]nicotinamid N-[4-(3,5-dicyclopropyl-lH-pyrazol-l-yl)-3-fluorphenyl]isonicotinamid N-[4-(3,5-dicyclopropyl-lH-pyrazol-l-yl)-3-fluorphenyl]-4-methylpyrimidin-5-carboxamid 6-(3,5-dicyclopropyl-lH-pyrazol-l-yl)-N-o-tolylnicotinamid N-[6-(3,5-dicyclopropyl-lH-pyrazol-l-yl)pyridin-3-yl]-2-fluorbenzamid N-[6-(3,5-dicyclopropyl-lH-pyrazol-l-yl)pyridin-3-yl]-2,3-difluorbenzamid N-[6-(3,5-dicyclopropyl-lH-pyrazol-l-yl)pyridin-3-yl]-2,6-difluorbenzamid N-[6-(3,5-dicyclopropyl-lH-pyrazol-l-yl)pyridin-3-yl]nicotinamiddihydrochlorid N-[6-(3,5-dicyclopropyl-lH-pyrazol-l-yl)pyridin-3-yl]isonicotinamid N-[6-(3,5-dicyclopropyl-lH-pyrazol-l-yl)pyridin-3-yl]-3-fluorisonicotinamid 3.5- dichlor-N-[6-(3,5-dicyclopropyl-lH-pyrazol-l-yl)pyridin-3-yl]isonicotinamid N-[6-(3,5-dicyclopropyl-lH-pyrazol-l-yl)pyridin-3-yl]-4-methylpyrimidin-5-carboxamid N-{4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl}-2-methylbenzamid N-{4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl}-2,3-difluorbenzamid N-{4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl}-2,6-difluorbenzamid N-{4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl}nicotinamid N-{4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl} isonicotinamid N-{4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl}-3-fluorisonicotinamid 3.5- dichlor-N-{4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3- fluorphenyljisonicotinamid N-{4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl}-4-methylpyrimidin-5- carboxamid N-{4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl}-N,4-dimethylpyrimidin- 5-carboxamid N-{4-[4-chlor-5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl}-2-(pyridin-2- yl)acetamid 1- {4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl}-3-(4-methylpyrimidin-5-yl)urea N-{4-[5)-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]3-fluorphenyl}-2,6-dichlorbenzamid 4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-N-(2,3-difluorphenyl)-3-fluorbenzamid 4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-N-(2,6-difluorphenyl)-3-fluorbenzamid N-{6-(5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}-3,5-dimethylisoxazol-4- carboxamid N-{6-(5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}-2-methylbenzamid 2- chlor-N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}benzamid N-(6-(5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl)pyridin-3-yl)-2-fluorbenzamid N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}-2,3-difluorbenzamid N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}-2,6-difluorbenzamid N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}picolinamid N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}-3-methylpicolinamid N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}nicotinamid N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}-2-methylnicotinamid N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}isonicotinamid N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}-3-fluorisonicotinamid 3.5- dichlor-N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}isonicotinamid N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}-4-methylpyrimidin-5-carboxamid N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}-2-(pyridin-2-yl)acetamid N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}-2-(pyridin-4-yl)acetamid N-{4-[4-chlor-5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl}-4- methylpyrimidin-5-carboxamid 6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-N-(2,3-difluorphenyl) nicotinamid 6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-N-(2,6-difluorphenyl)nicotinamid N-{2-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyrimidin-5-yl}-2,6-difluorbenzamid 3.5- dichlor-N-[4-(3,5-dicyclopropyl-lH-pyrazol-l-yl)-3-fluorphenyl]isonicotinamid N-(2-chlor-6-fluorphenyl)-4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluorbenzamid N-{4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3,5-difluorphenyl}-4-methylpyrimidin- 5-carboxamid {4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl}-l- phenylcyclobutancarboxamid N-{2-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyrimidin-5-yl}-4-methylpyrimidin-5- carboxamid 4-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]-3-fluor-N-(4-methylpyrimidin-5-yl) benzamid og N-{4-[3-cyclopropyl-5-(difluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl}-2,6-difluorbenzamid og N-{4-[5-cyclopropyl-3-(difluormethyl)-lH-pyrazol-l-yl]-3-fluorphenyl}-2,6-difluorbenzamid eller en tautomer, et N-oxid, en farmaceutisk acceptabel ester eller et farmaceutisk acceptabelt salt deraf.
  9. 9. Forbindelse ifølge et hvilket som helst af kravene 1 eller 5, som er N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}-2-methylbenzamid eller et farmaceutisk acceptabelt salt deraf.
  10. 10. Forbindelse ifølge et hvilket som helst af kravene 1 eller 5, som er N-{6-[5-cyclopropyl-3-(trifluormethyl)-lH-pyrazol-l-yl]pyridin-3-yl}-3-fluorisonicotinamid eller et farmaceutisk acceptabelt salt deraf.
  11. 11. Farmaceutisk sammensætning omfattende en eller flere forbindelser ifølge et hvilket som helst af kravene 1 til 10 og en farmaceutisk acceptabel bærer.
  12. 12. Anvendelse af en forbindelse ifølge et hvilket som helst af kravene 1-10 til fremstilling af et medikament til behandling af cancer.
  13. 13. Anvendelse af en forbindelse ifølge et hvilket som helst af kravene 1-10 til fremstilling af et medikament til behandling af autoimmun forstyrrelse, hvor den autoimmune forstyrrelse er kronisk obstruktiv lungesygdom, rheumatoid arthritis, inflammatorisk tarmsygdom, allergisk rhinitis, astma, multipel sklerose, psoriasis, Crohns sygdom, colitis, ulcerativ colitis, arthritis, knoglesygdomme, der er forbundet med øget knogleresorption, eller kronisk obstruktiv luftvejssygdom.
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