HRP20181014T1 - Pirazoli derivati modulatori kalcijevih kanala aktiviranih oslobađanjem kalcija i metode za liječenje nesitnostaničnog karcinoma pluća - Google Patents

Pirazoli derivati modulatori kalcijevih kanala aktiviranih oslobađanjem kalcija i metode za liječenje nesitnostaničnog karcinoma pluća Download PDF

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HRP20181014T1
HRP20181014T1 HRP20181014TT HRP20181014T HRP20181014T1 HR P20181014 T1 HRP20181014 T1 HR P20181014T1 HR P20181014T T HRP20181014T T HR P20181014TT HR P20181014 T HRP20181014 T HR P20181014T HR P20181014 T1 HRP20181014 T1 HR P20181014T1
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Croatia
Prior art keywords
substituted
unsubstituted
pyrazol
cyclopropyl
phenyl
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HRP20181014TT
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English (en)
Inventor
Meyyappan Muthuppalaniappan
Srikant Viswanadha
Kanthikiran Vs. Varanasi
Gayatri Swaroop Merikapudi
Swaroop Kumar V.S. Vakkalanka
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Rhizen Pharmaceuticals S.A.
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Publication of HRP20181014T1 publication Critical patent/HRP20181014T1/hr

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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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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Claims (19)

1. Spoj formule (IA-I): ili njegov tautomer, N-oksid, farmaceutski prihvatljiv ester ili farmaceutski prihvatljiva sol, naznačen time što su R1 i R2 oboje ciklopropil ili jedan od R1 i R2 je CF3 i drugi je ciklopropil; Rʺʹ je odabran iz vodika, hidroksi, cijano, halogena; -ORa, -COORa, -S(=O)q-Ra, -NRaRb, -C(=X)-Ra, supstituirane ili nesupstituirane 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; T, U, V i W su isti ili različiti i neovisno su odabrani iz CRa i N; -CH2- , -CHMe-, A je odsutan ili je odabran iz Cy je biciklični prsten odabran od supstituirane ili nesupstituirane cikloalkil skupine, supstituiranog ili nesupstituiranog heterociklila, supstituiranog ili nesupstituiranog arila i supstituiranog ili nesupstituiranog heteroarila; svako pojavljivanje Ra i Rb, su jednaki ili različiti i neovisno su odabrani iz 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 isti atom, mogu biti spojeni radi oblikovanja 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 su iz O, NRc i S; svako pojavljivanje Rc i Rd, mogu biti jednaki ili različiti i neovisno su odabrani iz 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 Rc i/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 opcijski uključi,ti jedan ili više heteroatoma, koji mogu biti jednaki ili različiti i odabrani su iz O, NH i S; svako pojavljivanje Y je odabrano iz O, S i -NRa; i svako pojavljivanje q neovisno predstavlja 0, 1 ili 2; pod uvjetom (e) da spoj formule (IA-I) nije: N-[4-[5-ciklopropil-3-(triflorometil)-1H-pirazol-1-il]fenil]-1-metil-3-(triflorometil)-1H- Tieno[2,3-c]pirazol-5-karboksamid ili N-[4-[5-ciklopropil-3-(triflorometil)-1H-pirazol-1- il]fenil]-Pirazolo[1,5-a]pirimidin-2-karboksamid.
2. Spoj sukladno patentnom zahtjevu 1, naznačeno time, da
3. Spoj sukladno patentnom zahtjevu 1, naznačeno time, da su R1 i R2 oboje ciklopropil.
4. Spoj formule (IA-II) ili njegov tautomer, N-oksid, farmaceutski prihvatljiv ester ili farmaceutski prihvatljiva sol, naznačen time što su R1 i R2 oboje ciklopropil ili jedan od R1 i R2 je CF3 i drugi je ciklopropil; Rʺʹ je izabran od vodika, hidroksi, cijano, halogena; -ORa, -COORa, -S(=O)q-Ra, -NRaRb, -C(=X)-Ra, supstituirane ili nesupstituirane 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; T, U, V i W su jednaki ili različiti i neovisno su odabrani iz CRa i N; A je odsutan, -NH-, ili -CH2-; Cy je C(8-13) biciklični supstituirani ili nesupstituirani heteroaril; svako pojavljivanje Ra i Rb su isti ili različiti i neovisno su odabrani iz 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 isti atom, mogu biti spojeni da oblikuju supstituirani ili nesupstituirani, zasićeni ili nezasićeni prsten od 3-10 članova, koji može opcijski uključiti, jedan ili više heteroatoma, koji mogu biti isti ili različiti i odabrani su iz O, NRc i S; svako pojavljivanje Rc i Rd, mogu biti jednaki ili različiti i neovisno su odabrani iz 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 Rc i/ili Rd supstituenta izravno vezana za isti atom, oni mogu biti spojeni radi oblikovanja 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 su iz O, NH i S; Y je odabran iz O, S i -NRa; i svako pojavljivanje q neovisno predstavlja 0, 1 ili 2; pod uvjetom da spoj formule (IA-II) ne uključuje N-[4-[5-ciklopropil-3-(triflorometil)-1H-pirazol-1-il]fenil]-1-metil-3-(triflorometil)-1H- Tieno[2,3-c]pirazol-5-karboksamid ili N-[4-[5-ciklopropil-3-(triflorometil)-1H-pirazol-1- il]fenil]-Pirazolo[1,5-a]pirimidin-2-karboksamid.
5. Spoj sukladno bilo kojem od patentnih zahtjeva 1 ili 4, naznačeno time, da R1 i R2 oboje predstavljaju ciklopropil.
6. Spoj sukladno bilo kojem od patentnih zahtjeva 1 ili 4, naznačeno time, da jedan od R1 i R2 je CF3 i drugi je neovisno ciklopropil.
7. Spoj sukladno bilo kojem od patentnih zahtjeva 1 ili 4, naznačeno time, da su T, U, V i W neovisno CH, CF ili N.
8. Spoj sukladno patentnom zahtjevu 4, naznačeno time, da je A je odsutan ili CH2.
9. Spoj sukladno patentnom zahtjevu 4, naznačeno time, da A je -CH2-.
10. Spoj sukladno bilo kojem od patentnih zahtjeva 1 ili 4, naznačeno time, da je Cy odabran iz
11. Spoj sukladno bilo kojem od patentnih zahtjeva 1 ili 4, odabran iz: N-[4-(3,5-diciklopropil-1H-pirazol-1-il) fenil]-1H-benzo [d] imidazol-6-karboksamida N-[4-(3,5-diciklopropil-1H-pirazol-1-il)fenil]-1H-benzo[d][1,2,3]triazol-6-karboks- amida N- [4-(3,5-diciklopropil-1H-pirazol-1-il) fenil] hinolin-6-karboksamida N- [4-(3,5-diciklopropil-1H-pirazol-1-il) fenil] hinoksalin-6-karboksamida 2- (1H-benzo[d] imidazol-1-il)-N-[4-(3,5-diciklopropil-1H-pirazol-1-il) fenil] acetamida 2-(1H-benzo[d][1,2,3]triazol-1-il)-N-[4-(3,5-diciklopropil-1H-pirazol-1-il)fenil] acetamida N- [4- (3,5-diciklopropil-1H-pirazol-1-il) fenil]-2-(1H-indol-3-il) acetamida N-[4-(3,5-diciklopropil-1H-pirazol-l-il)fenil]-2-(imidazo[1,2-a]piridin-2-il) acetamida N- [4- (3,5-diciklopropil-1H-pirazol-1-il) fenil]-2-(hinolin-6-il) acetamida 2-(1H-benzo[d][1,2,3]triazol-1-il)-N-(4-(3,5-diciklopropil-1H-pirazol-1-il)-3-fluoro- fenil) acetamida N-[4-(3,5-diciklopropil-1H-pirazol-1-il)-3-fluorofenil]-2-(kinolin-6-il) acetamida N-[6-(3,5-diciklopropil-1H-pirazol-1-il)piridin-3-il) kinolin-6-karboksamida N-[6-(3,5-diciklopropil-1H-pirazol-1-il) piridin-3-il] kinoksalin-6-karboksamida 2-(1H-benzo [d] [1,2,3] triazol-1-il)-N-[6-(3,5-diciklopropil-1H-pirazol-1-il)piridin-3-il] acetamida N-[6-(3,5-diciklopropil-1H-pirazol-1-il)piridin-3-il]-2-(kinolin-6-il) acetamida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]fenil}kinolin-6-karboksamida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]fenil}kinoksalin-6-karboksamida 2-(1H-benzo[d]imidazol-1-il)-N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il] fenil} acetamida 2-(1H-benzo[d] [1,2,3] triazol-1-il)-N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il] fenil} acetamida 2-(2H-benzo[d] [1,2,3] triazol-2-il)-N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il] fenil} acetamida 2-(3H-[1,2,3] triazolo [4,5-b] piridin-3-il)-N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il] fenil} acetamida (S)-2-(3H-[1,2,3] triazolo [4,5-b] piridin-3-il)-N-{4-[5-ciklopropil-3-(trifluorometil)- 1H-pirazol-1-il] fenil} propanamida 2-(6-amino-9H-purin-9-il)-N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il] fenil} acetamida N-(4-(5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il)fenil)-2-(1,3-dimetil-2,6-diokso-2,3-dihidro-1H-purin-7(6H)-il) acetamida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il) fenil)-2-(imidazo [1,2-a] piridin- 2- il) acetamida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il] fenil}-2-(kinolin-6-il) acetamida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]fenil}-2-(kinolin-6-il)propan- amida N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluorofenil}-1H-benzo[d] [1,2,3] triazol-6-karboksamida 2-(1H-benzo[d] [1,2,3] triazol-1-il)-N-{4-[5-ciklopropil-3-(trifIuorometil)-1H-pirazol-1-il]-3-fluorofenil} acetamida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-1H-benzo[d][1,2,3] triazol-5-karboksamida 2-(1H-benzo[d] [1,2,3] triazol-1-il)-N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il] piridin-3-il } acetamida 2-(2H-benzo[d][1,2,3] triazol-2-il)-N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il] piridin-3-il} acetamida N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-2-(kinolin-6-il)acet- amida 2-(1H-benzo[d] [1,2,3] triazol-1-il)-N-{6-[4-hloro-5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il] piridin-3-il} acetamida 4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluoro-N-(kinolin-6-ilmetil) benzamida 1-[4-(3,5-diciklopropil-1H-pirazol-1-il) fenil]-3-(kinolin-6-il) uree ili tautomera, N-oksida, farmaceutski prihvatljivog estra ili njegove farmaceutski prihvatljive soli.
12. Spoj sukladno bilo kojem od patentnih zahtjeva 1 ili 4,odabrano iz: N- [4- (3,5-diciklopropil-1H-pirazol-1-il) fenil] kinolin-6-karboksamid hidroklorida; N-[4- (3,5-diciklopropil-1H-pirazol-1-il) fenil]-2-(kinolin-6-il) acetamid hidroklorida; N-[4-(3,5-diciklopropil-1H-pirazol-1-il)-3-fluorofenil]-2-(kinolin-6-il)acetamid hidroklorida; N-[6-(3,5-diciklopropil-1H-pirazol-1-il)piridin-3-il)kinolin-6-karboksamid dihidroklorida; N-[4-(3,5-diciklopropil-1H-pirazol-l-il)fenil]-2-(imidazo[1,2-a]piridin-2-il)acetamid hidroklorida; N-[6-(3,5-diciklopropil-1H-pirazol-1-il)piridin-3-il]-2-(hinolin-6-il)acetamid dihidroklorida; N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il) fenil)-2-(imidazo [1,2-a] piridin- 2-il) acetamid hidroklorida; N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]fenil}hinolin-6-karboksamid hidroklorida; N-{6-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]piridin-3-il}-2-(hinolin-6-il)acet- amid hidroklorida; 4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il]-3-fluoro-N-(hinolin-6-ilmetil) benzamid hidroklorida; i N-{4-[5-ciklopropil-3-(trifluorometil)-1H-pirazol-1-il] fenil}-2-(hinolin-6-il) acetamid hidroklorida.
13. Spoj sukladno bilo kojem od patentnih zahtjeva 1 do 12, za moduliranje aktivnosti kalcijevog kanala (SOC) ovisno o zalihama, koja obuhvaća kontaktiranje kompleksa SOC kanala, ili njegovog dijela, sa spojem.
14. Spoj sukladno bilo kojem od patentnih zahtjeva 1 do 12, za liječenje bolesti, poremećaja, ili stanja koje bi imalo koristi od moduliranja kalcijevog kanala aktiviranog oslobađanjem kalcija (CRAC).
15. Spoj sukladno bilo kojem od patentnih zahtjeva 1 do 12, za liječenje nesitnostaničnog karcinoma pluća.
16. Spoj sukladno patentnom zahtjevu 15, naznačeno time, da kancerogene ćelije nesitnoćelijskog karcinoma pluća eksprimiraju Orai1, Orai3, Stim1, ili Stim2.
17. Spoj sukladno bilo kojem od patentnih zahtjeva 15 ili 16, naznačeno time, da pomenuto jedinjenje inhibira CRACM1/Orai1, CRACM2/Orai2, CRACM3/Orai3 ili bilo koju njihovu kombinaciju.
18. Spoj sukladno bilo kojem od patentnih zahtjeva 15 do 17, naznačeno time, da jedinjenje inhibira Stim1, ili Stim2, ili bilo koju njihovu kombinaciju.
19. Farmaceutski preparat, radi liječenja nesitnostaničnog karcinoma pluća, koji sadrži spoj formule sukladno bilo kojem od patentnih zahtjeva 1 do 12, zajedno s farmaceutski prihvatljivim nosačem.
HRP20181014TT 2009-10-08 2018-07-02 Pirazoli derivati modulatori kalcijevih kanala aktiviranih oslobađanjem kalcija i metode za liječenje nesitnostaničnog karcinoma pluća HRP20181014T1 (hr)

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IN2439CH2009 2009-10-08
IN2636CH2009 2009-10-30
US26554009P 2009-12-01 2009-12-01
IN158CH2010 2010-01-25
IN1513CH2010 2010-06-02
IN1514CH2010 2010-06-02
IN2385CH2010 2010-08-19
EP10776149.6A EP2509974B1 (en) 2009-10-08 2010-10-07 Pyrazoles derivatives modulators of calcium release-activated calcium channel and methods for treatment of non-small cell lung cancer
PCT/IB2010/002539 WO2011042798A1 (en) 2009-10-08 2010-10-07 Pyrazoles derivatives modulators of calcium release -activated calcium channel and methods for treatment of non- small cell lung cancer

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