HRP20180973T1 - Supstituirani tiazolski ili oksazolski antagonisti p2x7 receptora - Google Patents

Supstituirani tiazolski ili oksazolski antagonisti p2x7 receptora Download PDF

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Publication number
HRP20180973T1
HRP20180973T1 HRP20180973TT HRP20180973T HRP20180973T1 HR P20180973 T1 HRP20180973 T1 HR P20180973T1 HR P20180973T T HRP20180973T T HR P20180973TT HR P20180973 T HRP20180973 T HR P20180973T HR P20180973 T1 HRP20180973 T1 HR P20180973T1
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Croatia
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compound
formula
hydrogen
halogen
substituted
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HRP20180973TT
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English (en)
Inventor
Paolo Pevarello
Stefan Lohmer
Chiara Liberati
Pierfausto Seneci
Cristina PESENTI
Adolfo Prandi
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Axxam S.P.A.
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Publication of HRP20180973T1 publication Critical patent/HRP20180973T1/hr

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    • A61K31/445—Non condensed piperidines, e.g. piperocaine
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    • C07D417/06—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 only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic System
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages

Claims (12)

1. Spoj sljedeće formule (I) ili njegova farmaceutski prihvatljiva sol: uključujući bilo koji njegov stereokemijski izomerni oblik, gdje n je 1 ili 2; Y predstavlja kisik ili sumpor; svaki od R1 i R2 je neovisno odabran iz skupine koju čine vodik, deuterij, halogen, C1-C4 alkil, koji može biti supstituiran s hidroksi ili halogenom, kao što je hidroksimetil, fluormetil, difluormetil, trifluormetil, C3-C6 cikloalkil, koji može biti supstituiran s hidroksi ili halogenom, ili C3-C4 alkiloksi; svaki od R3 i R4je neovisno odabran iz skupine koju čine vodik, halogen, C1-C4 alkil, difluormetil, trifluormetil, C1-C4 alkiloksi, NR9R10, gdje su R9 i R10 neovisno vodik ili C1-C4 alkil, ili 2-tiazolidin-1,1-dion; ili dvije R3 skupine ili R3 i R4 skupine uzete zajedno tvore šesteročlani heterociklički prsten koji sadrži dušikov atom; R5 je odabran od vodika, halogena, ili je heterociklički prsten odabran od pirimidin-2-il, piridin-2-il ili pirazin-2-il, koji može biti supstituiran halogenom, C1-C4 alkilom, fluormetilom, difluormetilom, trifluormetilom ili C1-C4 alkiloksi; R7je vodik ili C1-C4 alkil; radikal predstavlja azetidin, pirolidin, piperidin, morfolin, oksazepan ili 1,2,3,4-tetrahidroizokinolin prsten koji može biti supstituiran, gdje je svaki od R6 neovisno odabran iz skupine koju čine vodik, halogen, C1-C4 alkil, C3-C6 cikloalkil, C3-C6 spirocikloalkil, difluormetil, trifluormetil, C1-C4 alkiloksi, aril, heteroaril, C1-C4 ariloksi ili C1-C4 arilalkoksi gdje arilna skupina ili heteroarilna skupina može biti supstituirana halogenom, C1-C4 alkilom, fluormetilom, difluormetilom, trifluormetilom ili C1-C4 alkiloksi.
2. Spoj formule (I) prema patentnom zahtjevu 1 naznačeno time da je R7 vodik a n je 1.
3. Spoj formule (I) prema patentnim zahtjevima 1 ili 2 naznačeno time da oba R1 i R2jesu vodik ili jedan jest vodik a drugi je metil, etil, propil, fert-butil, koji može biti supstituiran s hidroksi ili fluorom, C3-C6 cikloalkil, koji može biti supstituiran s hidroksi ili fluorom.
4. Spoj formule (I) prema bilo kojim od prethodnih patentnih zahtjeva naznačeno time da je R5 vodik a svaki od R3 i R4su neovisno vodik, halogen, C1-C4 alkil, C1-C4 alkiloksi, NR9R10, gdje su R9 i R10 neovisno vodik ili C1-C4 alkil, ili 2-tiazolidin-1,1-dion; ili dvije R3 skupine ili R3 i R4 skupine uzete zajedno tvore šesteročlani heterociklički prsten koji sadrži dušikov atom.
5. Spoj formule (I) prema patentnim zahtjevima 1-4 naznačeno time da je R4 vodik, R3 u meta-položaju jest vodik a R3 u ortho-položaju odabran je iz skupine koju čine halogen, ili C1-C4 alkil, a R5 je heterociklički prsten odabran od pirimidin-2-il, piridin-2-il ili pirazin-2-il, koji može biti supstituiran halogenom.
6. Spoj formule (I) prema bilo kojem od prethodnih patentnih zahtjeva naznačeno time daje prsten A odabran iz skupine koju čine gdje R6 jest vodik, halogen, benziloksi ili fenoksi, fenil, pirazol, C3-C6 cikloalkil, koji može biti supstituiran halogenom, preferirano supstituiran fluorom.
7. Spoj formule (I) prema patentnom zahtjevu 1 odabran iz skupine koju čine:
8. Postupak priprave spoja formule (I) kao što je definiran u patentnom zahtjevu 1 koji obuhvaća korak reakcije spoja formule (II): gdje su značenja n, Y, A te R1, R2 i R6 kao što su definirana u patentnom zahtjevu 1, sa spojem formule (III) gdje su značenja R3, R4 i R5 kao što su definirana u patentnom zahtjevu 1; ili sa spojem Formule (IIIa): gdje su značenja R3, R4 i R5 kao što su definirana u patentnom zahtjevu 1, a W je pogodna izlazna skupina te mogućnost je prevođenja dobivenog spoja formule (1) u odgovarajuću sol nastalu adicijom, i/ili pripravljanje odgovarajućih stereokemijskih izomernih oblika.
9. Farmaceutski pripravak koji sadrži spoj formule (I) prema patentnim zahtjevima 1-7 i farmaceutski prihvatljiv razrjeđivač i/ili nosač.
10. Spoj formule (I) prema patentnim zahtjevima 1-7 za upotrebu kao lijek.
11. Spoj formule (I) prema patentnim zahtjevima 1-7 za upotrebu u liječenju stanja ili bolesti odabranih od stanja ili bolesti posredovanih receptorom P2X7.
12. Spoj formule (I) prema patentnim zahtjevima 1-7 za upotrebu u sprječavanju i/ili liječenju neurodegenerativnih, kognitivnih, psihijatrijskih poremećaja, neoropatske boli, kronične boli, neuroinflamacije izazvane HIV-om te oštećenja CNS, epilepsije, upalnih procesa mišićno-koštanog sustava, fibroze jetre, poremećaja gastrointestinalnog trakta, poremećaja genito-urinarnog trakta, oftalmičnih bolesti, kronične opstruktivne plućne bolesti (COPD), karcinoma i proliferativnih bolesti.
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