HRP20150792T1 - Bicikliäśki analozi aril-sfingozin-1-fosfata - Google Patents

Bicikliäśki analozi aril-sfingozin-1-fosfata Download PDF

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HRP20150792T1
HRP20150792T1 HRP20150792TT HRP20150792T HRP20150792T1 HR P20150792 T1 HRP20150792 T1 HR P20150792T1 HR P20150792T T HRP20150792T T HR P20150792TT HR P20150792 T HRP20150792 T HR P20150792T HR P20150792 T1 HRP20150792 T1 HR P20150792T1
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HR
Croatia
Prior art keywords
tert
naphthalen
butylcyclohexyloxy
trans
methyl
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HRP20150792TT
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English (en)
Inventor
Jermaine Thomas
Xiaogao Liu
Edward Yin-Shiang Lin
Guo Zhu Zheng
Bin Ma
Richard D. Caldwell
Kevin M. Guckian
Gnanasambandam Kumaravel
Arthur G. Taveras
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Biogen Ma Inc.
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Publication of HRP20150792T1 publication Critical patent/HRP20150792T1/hr

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Claims (11)

1. Spoj, naznačen time, da ima sljedeće formule (IIa), (IIIa) ili (IIIb): [image] gdje: svaki od X1, X2, X3, X4, X5 i X6, neovisno je vodik, halo, hidroksi, nitro, cijano, alkil, haloalkil, cikloalkil, halocikloalkil, alkoksi, haloalkoksi, cikloalkoksi, halocikloalkoksi, acil, aminoacil, -N(RfRg), -N(Rf)SO2Rg, -SO2Rf, -S(O)2N(RfRg), -CO2Rf, trialkilamino, aril, ili heteroaril; W je -O-; Cy ima sljedeću formulu: [image] gdje: Z1 je -[C(RdRe)]x-; Z2 je -[C(RdRe)]y- Z3 je -[C(RdRe)]z-; svaki od x, y, i z, neovisno je 1, 2 ili 3; svaki Rd, neovisno je vodik, halo, hidroksi, alkil, alkenil, alkoksi, ili cikloalkil; svaki Re, neovisno je vodik, halo, hidroksi, alkil, alkenil, alkoksi, ili cikloalkil; R1a i R1b, neovisno su vodik, halo, hidroksi, nitro, cijano, -NRfRg, alkil, haloalkil, cikloalkil, cikloalkenil, cikloalkilalkil, cikloalkenilalkil, heterociklilalkil, arilalkil, heteroarilalkil, alkoksi, cikloalkilalkoksi, cikloalkenilalkoksi, heterociklilalkoksi, arilalkoksi, heteroarilalkoksi, acil, cikloalkilacil, cikloalkenilacil, heterociklilacil, arilacil, heteroarilacil, tioalkil, alkenil, alkinil, cikloalkenil, heterociklil, aril, ili heteroaril; ili su R1a i R1b, kada se uzimaju zajedno, C2-C5 alkilen ili C2-C5 alkenilen; R2a i R2b, neovisno su vodik, halo, hidroksi, nitro, cijano, -NRfRg, alkil, haloalkil, cikloalkil, cikloalkenil, cikloalkilalkil, cikloalkenilalkil, heterociklilalkil, arilalkil, heteroarilalkil, alkoksi, cikloalkilalkoksi, cikloalkenilalkoksi, heterociklilalkoksi, arilalkoksi, heteroarilalkoksi, acil, cikloalkilacil, cikloalkenilacil, heterociklilacil, arilacil, heteroarilacil, tioalkil, alkenil, alkinil, cikloalkenil, heterociklil, aril, ili heteroaril; ili su R1a i R2a, kada se uzimaju zajedno, C1-C5 alkilen ili C2-C5 alkenilen; gdje je svaki od R1a, R1b, R2a, i R2b neovisno supstituiran s 0 - 5 supstituenata odabranih od sljedećih: halo, hidroksi, nitro, cijano, -NRfRg, ili -CO2Rf; R3 je -L1-J-L2-T1; L1 je -C(RfRg)-; J je sljedeće: [image] gdje svaki od D1 i D3, neovisno je [image] ili [image] D2 je -[C(RfRg)]k-, -[C(RfRg)]k-N(Rf)-, -[C(RfRg)]k-O-, -N(Rf)-, ili -N(Rf)-[(CRfRg)]k-; i D4 je -[C(RfRg)]m-; pri čemu k je 1 ili 2; a m je 0, 1, 2 ili 3; pod uvjetom da N ili O ne čine više od dva atoma prstena od D1-D4; L2 je -C(RfRg)-, -C(RfG)-, -C(G)2-, -C(RfRg)-C(RfRg)-, -C(RfRg)-C(RfG)-, -C(RfRg)-C(G)2-, ili veza; pod uvjetom da barem jedan od L1, J, i L2 nije veza; T1 je -C(O)(ORf), -C(O)N(Rf)S(O)2Rf, tetrazolil, -S(O)2ORf, -C(O)NHC(O)-Rf, -Si(O)OH, -B(OH)2, -N(Rf)S(O)2Rf, -S(O)2NRf, -O-P(O)(ORf)ORf, ili -P(O)2(ORf); svaki G, neovisno je vodik, hidroksi, halogen, ili trifluorometil; svaki Rf, neovisno je vodik, hidroksi, halo, alkil, haloalkil, alkenil, alkinil, cikloalkil, cikloalkenil, aril, heteroaril, heterociklil ili NH2; pri čemu je svaki od sljedećih: alkil, cikloalkil, cikloalkenil, aril, heteroaril i heterociklil, po želji supstituiran s 1 do 5 supstituenata neovisno odabranih iz skupine koju čine: halo, okso, -CN, -CHO, -CG3, -OH, -NO2, alkil, -OCG3, alkoksi, cikloalkoksi, cikloalkenoksi, amino, alkilamino, dialkilamino, acilamino, aminoacil, alkilsulfonil, alkilaminosulfonil, i dialkilaminosulfonil; svaki Rg, neovisno je vodik, hidroksi, halo, alkil, haloalkil, alkenil, alkinil, cikloalkil, cikloalkenil, aril, heteroaril, ili heterociklil; pri čemu je svaki od sljedećih: alkil, cikloalkil, cikloalkenil, aril, heteroaril i heterociklil, po želji supstituiran s 1 do 5 supstituenata neovisno odabranih iz skupine koju čine: halo, okso, -CN, -CHO, -CG3, -OH, NO2, alkil, -OCG3, alkoksi, cikloalkoksi, cikloalkenoksi, amino, alkilamino, dialkilamino, acilamino, aminoacil, alkilsulfonil, alkilaminosulfonil, i dialkilaminosulfonil; ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema zahtjevu 1, naznačen time, da T1 je -C(O)(ORf), -C(O)N(Rf)S(O2Rf), -O-P(O)(ORf)ORf, -P(O2)(ORf), tetrazolil, ili -S(O)2ORf, ili njegova farmaceutski prihvatljiva sol.
3. Spoj prema zahtjevu 1, naznačen time, da Z1 je -CH2CH2- i Z2 je -CH2-, ili njegova farmaceutski prihvatljiva sol.
4. Spoj prema zahtjevu 1, naznačen time, da su oba R1a i R2a vodik, dok R1b je fluoro, kloro, bromo, jodo, metil, triflurormetil, etil, propil, izopropil, n-butil, i-butil, t-butil, n-pentil, izopentil, 1,1-dimetilpropil, neopentil, ciklopentil, n-heksil, cikloheksil, metoksi, trifluorometoksi, etoksi, n-propoksi, i-propoksi, n-butoksi, i-butoksi, t-butoksi, n-pentiloksi, i-pentiloksi, 1,1-dimetilpropoksi, neopentiloksi, ciklopentiloksi, n-heksiloksi, ili cikloheksiloksi, ili njegova farmaceutski prihvatljiva sol.
5. Spoj prema zahtjevu 1, naznačen time, da je spoj odabran iz skupine koju čine: 3-((6-(trans-4-tert-butilcikloheksiloksi)naftalen-2-il)metilamino)-N-(fenilsulfonil)propanamid; 3-((6-(trans-4-tert-butilcikloheksiloksi)-5-(trifluorometil)naftalen-2-il)metilamino)-N-(fenilsulfonil)propanamid; 2-((6-(trans-4-tert-butilcikloheksiloksi)naftalen-2-il)metilamino)propanska kiselina; 3-((6-(trans-4-tert-butilcikloheksiloksi)naftalen-2-il)metilamino)butanska kiselina; 2-(((6-(trans-4-tert-butilcikloheksiloksi)naftalen-2-il)metil)(metil)amino)octena kiselina; 3-((6-(trans-4-tert-butilcikloheksiloksi)naftalen-2-il)metilamino)propanska kiselina; 3-(((6-(trans-4-tert-butilcikloheksiloksi)naftalen-2-il)metil)(metil)amino)propanska kiselina; 1-((6-(trans-4-tert-butilcikloheksiloksi)naftalen-2-il)metil)azetidin-3-karboksilna kiselina; 1-((6-(trans-4-tert-butilcikloheksiloksi)naftalen-2-il)metil)pirolidin-3-karboksilna kiselina; 1-((6-(trans-4-tert-butilcikloheksiloksi)naftalen-2-il)metil)piperidin-4-karboksilna kiselina; 1-((6-(trans-4-tert-butilcikloheksiloksi)-5-(trifluorometil)naftalen-2-il)metil)azetidin-3-karboksilna kiselina; 3-((6-(trans-4-tert-butilcikloheksiloksi)-5-(trifluorometil)naftalen-2-il)metilamino)propanska kiselina; 3-((6-(trans-4-tert-butilcikloheksiloksi)naftalen-2-il)metilamino)-2,2-difluoropropanska kiselina; 2,2-difluoro-3-((6-(spiro[5.5]undekan-3-iloksi)naftalen-2-il)metilamino)propanska kiselina; 2-(((2-(trans-4-tert-butilcikloheksiloksi)naftalen-6-il)metil)amino)octena kiselina; 4-(((2-(trans-4-tert-butilcikloheksiloksi)naftalen-6-il)metil)amino)butirna kiselina; 4-(((2-(trans-4-tert-butilcikloheksiloksi)naftalen-6-il)metil)amino)butirna kiselina; (R)-1-((2-(trans-4-tert-butilcikloheksiloksi)naftalen-6-il)metil)piperidin-3-karboksilna kiselina; (S)-1-((2-(trans-4-tert-butilcikloheksiloksi)naftalen-6-il)metil)piperidin-3-karboksilna kiselina; 4-((2-(trans-4-tert-butilcikloheksiloksi)naftalen-6-il)metil)butirna kiselina; 5-((2-(trans-4-tert-butilcikloheksiloksi)naftalen-6-il)metil)pentanska kiselina; 6-((2-(trans-4-tert-butilcikloheksiloksi)naftalen-6-il)metil)heksanska kiselina; 4-(6-(trans-4-tert-butilcikloheksiloksi)-3,4-dihidroizokinolin-2(1H)-il)butanska kiselina; 4-(6-(cis-4-tert-butilcikloheksiloksi)-3,4-dihidroizokinolin-2(1H)-il)butanska kiselina; 2-(((2-(trans-4-tert-butilcikloheksiloksi)naftalen-6-il)metil)amino)etilfosfonska kiselina; 2-(2-(5-(trans-4-tert-butilcikloheksiloksi)indolin-1-il)-2-oksoetilamino)etilfosfonska kiselina; 3-amino-4-(5-(trans-4-tert-butilcikloheksiloksi)indolin-1-il)-4-okso-butanska kiselina; 3-{[6-(4-tert-butil-cikloheksiloksi)-8-metil-naftalen-2-ilmetil]-amino}-propionska kiselina; {[6-(4-tert-butil-cikloheksiloksi)-8-metil-naftalen-2-ilmetil]-amino}-octena kiselina; 4-{[6-(4-tert-butil-cikloheksiloksi)-8-metil-naftalen-2-ilmetil]-amino}-butirna kiselina; 1-[6-(4-tert-butil-cikloheksiloksi)-8-metil-naftalen-2-ilmetil]-azetidin-3-karboksilna kiselina; i 1-[6-(4-tert-butil-cikloheksiloksi)-8-metil-naftalen-2-ilmetil]-pirolidin-3-karboksilat; ili njegova farmaceutski prihvatljiva sol.
6. Farmaceutski sastav, naznačen time, da obuhvaća farmaceutski prihvatljiv nosač i spoj prema bilo kojem od zahtjeva 1 - 5, ili njegovu farmaceutski prihvatljivu sol.
7. Spoj prema bilo kojem od zahtjeva 1 - 5, ili njegova farmaceutski prihvatljiva sol, naznačen/a time, da se upotrebljava u liječenju ili prevenciji sljedećih stanja: multipla skleroza, autoimuna bolest, kronični upalni poremećaj, astma, upalna neuropatija, artritis, odbijanje transplantata, Crohnova bolest, ulcerativni kolitis, lupus eritematoza, psorijaza, ishemijska-reperfuzijska ozljeda, čvrsti tumor, tumorske metastaze, bolest povezana s angiogenezom, vaskularna bolest, stanje bolova, akutno virusno oboljenje, upalno stanje crijeva, dijabetes ovisan o inzulinu, ili dijabetes neovisan o inzulinu.
8. Spoj za uporabu prema zahtjevu 7, ili njegova farmaceutski prihvatljiva sol, naznačen/a time, da patološko stanje su neuropatski bolovi ili je to autoimuna bolest.
9. Spoj za uporabu prema zahtjevu 7, ili njegova farmaceutski prihvatljiva sol, naznačen/a time, da autoimuna bolest je uveitis, dijabetes tipa 1, reumatoidni artritis, upalna bolest crijeva ili multipla skleroza.
10. Spoj za uporabu prema zahtjevu 7, ili njegova farmaceutski prihvatljiva sol, naznačen/a time, da uporaba u liječenju ili prevenciji nadalje uključuje uporabu lijeka odabranog iz skupine koju čine: kortikosteroid, bronhodilator, antiastmatik, protuupalno sredstvo, antireumatik, imunosupresiv, antimetabolit, imunomodulator, antipsorijatik, i antidijabetik.
11. Spoj za uporabu prema zahtjevu 7, ili njegova farmaceutski prihvatljiva sol, naznačen/a time, da autoimuna bolest je multipla skleroza.
HRP20150792TT 2009-08-05 2015-07-17 Bicikliäśki analozi aril-sfingozin-1-fosfata HRP20150792T1 (hr)

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