HRP20141143T1 - Novi antagonisti receptora ccr2 i njihove uporabe - Google Patents

Novi antagonisti receptora ccr2 i njihove uporabe Download PDF

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HRP20141143T1
HRP20141143T1 HRP20141143AT HRP20141143T HRP20141143T1 HR P20141143 T1 HRP20141143 T1 HR P20141143T1 HR P20141143A T HRP20141143A T HR P20141143AT HR P20141143 T HRP20141143 T HR P20141143T HR P20141143 T1 HRP20141143 T1 HR P20141143T1
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alkyl
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alkylene
heterocyclyl
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Heiner Ebel
Sara Frattini
Kai Gerlach
Riccardo Giovannini
Christoph Hoenke
Rocco Mazzaferro
Marco Santagostino
Stefan Scheuerer
Christofer Tautermann
Thomas Trieselmann
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Boehringer Ingelheim International Gmbh
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Claims (16)

1. Spoj, naznačen time, da ima formulu (I), [image] gdje R1 je skupina odabrana od sljedećih: -H, -halogen, -CN, -O-C1-C4-alkil, -C1-C4-alkil, -CH=CH2, -C=CH, -CF3, -OCF3, -OCF2H, i -OCFH2: gdje R7 je prsten odabran od sljedećih: -C3-C8-cikloalkil, -C3-C8-helerociklil, -C5-C10-aril, i -C5-C10-heteroaril, gdje je prsten R7 opcijski supstituiran s jednom ili više skupina odabranih od sljedećih: -CF3, -O-CF3, -S-CF3, -CN, -C1-C6,-alkil, -C(CH3)2CN, i -halogen, ili gdje je prsten R7 opcijski supstituiran s jednom ili više skupina odabranih od sljedećih: -C1-C6-alkil, -O-C1-C6-alkil, -C5-C10-aril, -C5-C10-heteroaril, -C1-C8-cikloalkil, -C1-C8-heterociklil, -C2-C6-alkenil, i -C2-C6-alkinil, opcijski supstituiran s jednom ili više skupina odabranih od sljedećih: -OH, -NH2, -C1-C3-alkil, -O-C1-C6-alkil, -CN, -CF3, -OCF3, halogen, -metil, i =O, ili gdje je prsten R7 opcijski dalje bivalentno supstituiran na dva susjedna atoma prstena, tako da se anelirani prsten formira pomoću jedne i I i više skupina odabranih od sljedećih: -C1-C6-alkilen, -C2-C6-alkenilen i -C4-C6-alkinilen, u kojima jedan ili dva ili tri ugljikova centra, mogu opcijski biti zamijenjena s 1 ili 2 ili 3 heteroatoma odabrana od N, O i S, dok je bi valentna skupina opcijski supstituirana s jednom ili više skupina odabranih od sljedećih: -OH, -NH2, -C1-C3-alkil, -O-C1-C6-alkil, -CN, -CF3, -OCF3, halogen, i =O; gdje je R2 odabran od sljedećih: -H, -halogen, -CN, -O-C2-C4-alkil, -C1-C4-alkil, -CH=CH2, -C=CH, -CF3, -OCF3, -OCF2H, i -OCFH2; gdje je R3 odabran od sljedećih: -H, -metil, -etil, -propil, -i-propil, -ciklopropil, -OCH3, -CF3, i -CN; gdje n je 1, 2 ili 3; gdje G i E su neovisno odabrani od C-H ili N; gdje Z je C, a R4 i R5 su neovisno odabrani od sljedećih: -H, -C1-C6-alkil, -NH2, -C3-C8-cikloalkil, -C3-C8-heterociklil,-C5-C10-aril, -C5-C10-heteroaril, i -C(O)-N(R8, R8'), s R8 i R8' neovisno odabranima od -H, i -C1-C6-alkil, ili gdje Z je N, i R4 označava par elektrona, a R5 je odabran između sljedećih: -H, -C1-C6-alkil, -NH2, -C3-C8-cikloalkil, -C3-C8-heterociklil, -C5-C10-aril,-C5-C10-heteroaril, i -C(O)-N(R8,R8'), s R8 i R8' neovisno odabranima od -H, i -C1-C6-alkil, i ako su R4 i R5 različiti od para elektrona ili od -H, opcijski su neovisno supstituirani s jednom ili više skupina odabranih od sljedećih:-halogen, -OH, -CF3, -CN, -C1-C6-alkil, -O-C1-C6-alkil, -O-C1-C8-cikloalkil, -O-C1-C8-heterociklil, -O-C5-C10-aril, -O-C5-C10-heteroaril, -C0-C6-alkilen-CN, -C0-C4-alkilen-O-C1-C4-alkil, -C0-C4-alkilen-O-C3-C8-cikloalkil, -C0-C4-alkilen-O-C3-C8-heterociklil, -C0-C4-alkilen-O-C5-C10-aril, -C0-C4-alkilen-O-C5-C10-heteroaril, -C0-C4-alkilen-Q-C0-C4-alkil-N(R9, R9'), -C0-C4-alkilen-N(R10)-Q-C1-C4-alkil, -C0-C4-alkilen-N(R10)-Q-C3-C8-cikloalkil, -C0-C4-alkilen-N(R10)-Q-C3-C8-heterociklil, -C0-C4-alkilen-N(R10)-Q-C5-C10-aril, -C0-C4-alkilen-N(R10)-Q-C5-C10-heteroaril, -C0-C4-alilen-Q-N(R11, R11'), -C0-C4-alkilen-N(R12)-Q-N(R13, R13'), -C0-C4-alkilen-R14, -C0-C4-alkilen(R20, R20'), -C0-C4-alkilen-Q-C1-C6-alkil, -C0-C4-alkilen-Q-C3-C8-cikloalkil, -C0-C4-alkilen-Q-C3-C8-heterociklil, -C0-C4-alkilen-O-C5-C10-aril, -C0-C4-alkilen-Q-C5-C10-heteroaril, -C0-C4-alkilen-O-Q-N(R15,R15'), i -C0-C4-alkilen-N(R16)-Q-O-(R17), gdje je Q odabran od -C(O)-, i -SO2, gdje su R10, R12, R16 neovisno odabrani od sljedećih: -H, -C1-C6-alkil, i -C3-C6-cikloalkil, gdje su R9, R9', R11, R11', R13, R13', R15, R15', neovisno odabrani od sljedećih: -H, -C1-C6-alkil, i -C3-C6-cikloalkil, ili gdje R9 i R9', R11, i R11', R13 i R13', R15 i R15' zajedno formiraju -C3-C6-alkilen-skupinu, gdje su R14 i R17 neovisno odabrani od sljedećih: -H, -C1-C6-alkil, -C5-C10-aril, -C5-C10-heteroaril, -C3-C8-cikloalkil, i -C3-C8-heterociklil, gdje spomenuti -C3-C8-heterociklil opcijski sadrži dušik i/ili -SO2- u prstenu, i gdje su R14 i R17 opcijski supstituirani s jednom ili više skupina odabranih od sljedećih: -OH, -OCH3, -CF3, -COOH, -OCF3, -CN, -halogen ,-C1-C4-alkil, =O, i -SO2-C1-C4-alkil, gdje R20 i R20' zajedno formiraju spiro-C3-C8-karbocikl ili spiro-C3-C8-heterocikl koji sadrži jednu ili više skupina odabranih od O u prstenu, i gdje je spomenuti spirocikl opcijski dalje bivalentno supstituiran s aneliranim prstenom formirajući skupinu odabranu od sljedećih: -C1-C6-alkilen,-C2-C6-alkenilen, i -C4-C6-alkinilen, i gdje je spomenuti spirocikl opcijski dalje supstituiran s jednom ili više skupina odabranih od sljedećih: -OH, -OCH3, -CF3,-COOH, -OCF3,-CN, -halogen, ili gdje Z je C, i R4 označava -H, a R5 je skupina sa strukturom -L1-R18 gdje je L1 odabran od sljedećih:-NH-, -N(C1-C4-alkil)-, i veza, gdje je R18 odabran od sljedećih: -C5-C10-aril, -C5-C10-heteroaril, -C3-C8-cikloalkil, i -C3-C8-heterociklil, gdje je R18 opcijski supstituiran s jednom ili više skupina odabranih od sljedećih: halogen, -CF3, -OCF3, -CN, -OH, -O-C1-C4-alkil, -C1-C6-alkil, -NH-C(O-C1-C6-alkil, -N(C1-C4-alkil)-C(O)-C1-C6-alkil, -C(O)-C1-C6-alkil, -S(O)2-C1-C6-alkil, -NH-S(O)2-C1-C6-alkil, -N(C1-C4-alkil)-S(O)2-C1-C6-alkil, i -C(O)-O-C1-C6-alkil, i gdje su R4, R5 i R18 opcijski dalje supstituirani sa spiro-C3-C8-cikloalkilom ili spiro-C1-C8-heterociklilom, tako da se zajedno s R4, R5 i/ili R18 formira spirocikl, gdje spomenuti spiro-C1-C8-heterociklil opcijski sadrži jednu ili više skupina odabranih od sljedećih: dušik,-C(O)-, -SO2-, i -N(SO2-C1-C4-alkil)- u prstenu, ili gdje su R4, R5 i R18 opcijski dalje bivalentno supstituirani s jednim ili više spirocikličkih ili aneliranih prstena formirajući skupinu odabranu od sljedećih: -C1-C6-aIkilen, -C2-C6-alkenilen, i -C4-C6-alkinilen, u kojima jedan ili dva ugljikova centra mogu opcijski biti zamijenjeni s jednim ili dva heteroatoma odabrana između N, O i S i koji mogu biti opcijski supstituirani s jednom ili više skupina na jednom atomu prstena ili na dva susjedna atoma prstena, odabrana od sljedećih: -OH, -NH2, -C1-C3-alkil, -O-C1-C6-alkil, -CN, -CF3, -OCF3, i halogen; gdje je R6 odabran od sljedećih: -H, -C1-C4-alkil, -OH, -O-C1-C4-alkil, -halogen, -CN, -CF3' i -OCF3; kao i u obliku njihovih adicijskih kiselinskih soli s farmakološki prihvatljivim kiselinama.
2. Spoj prema zahtjevu 1, naznačen time, da Z je C, i R4 i R5 su neovisno odabrani od sljedećih: -H, -i-propil, -amino, -pirolidinil, -piperidinil, -morfolinil, -azepanil, -oksazepanil, -piperazinil, -azetidinil, -tetrahidropiranil, -ciklopentil, -cikloheksil, i -C(O)-N(R8,R8'), s R8 i R8' neovisno odabranima od -H i -C1-C6-alkila, gdje su R4 i R5, ako su različiti od -H, opcijski neovisno supstituirani s jednom ili više skupina odabranih od sljedećih: -fluoro, -metil, -etil, propil, -i-propil, - butil, -i-butil, -t-butil, -hidroksi, -CF3, -OCF3, -CN, -O-CH3, -O-C2H5, -O-C3H7, -CH2-CN, -CH2-O-CH3, -(CH2)2-O-CH3, -C(O)-CH3, -C(O)-C2H5, -C(O)-C3H7, -COOH, -C(O)-NH2, -C(O)-NH-CH3, -C(O)-N(CH3)2, -NH-C(O)-CH3, -N(CH3)C(O)-CH3, -NH-C(O)-C2H5, -N(CH3)-C(O)-C2H5, -NH-C(O)-C3H7, -N(CH3)-C(O)-C3H7,-NH-SO2-CH3, -N(CH3)-SO2-CH3,-N(C2H5)-SO2-CH3, -N(C3H7)-SO2-CH3, -NH-SO2-C2H5, -N(CH3)-SO2-C2H5, -N(C2H5)-SO2-C2H3, -N(C3H7)-SO2-C2H5, -NH-SO2-C3H7, -N(CH3)-SO2-C3H7, -N(C2H5)-SO2-C3H7, -N(C3H7)-SO2-C3H7, -NH-SO2-C3H5, -N(CH3)-SO2-C3H5, -N(C2H5)-SO2-C3H5, -N(C3H7)-SO2-C2H5, -CH2-NH-SO2-CH3, -CH2-N(CH3)-SO2-CH3, -CH2-NH-SO2-C2H5, -CH2-N(CH3)-SO2-C2H5, -CH2-NH-SO2-C3H7, -CH2-N(CH3)-SO2-C3H7, -CH2-NH-SO2-C1H5, -CH2-N(CH3)-SO2-C3H5, -NH-C(O)-NH2, -N(CH3)-C(O)-NH2, -NH-C(O)-NH-CH3, -N(CH3)-C(O)-NH-CH3, -NH-C(O)-N(CH3)2, -N(CH3)-C(O)-N(CH3)2, -SO2-NH2, -SO2-NH(CH3), -SO2-N(CH3)2, -C(O)-NH-C2H5, -C(O)-N(CH3-C2H5, -C(O)-N(CH3)-C3H7, -C(O)-N(CH3)-C4H9, -C(O)-NH-CH(CH3)-C2H5, -C(O)-N(CH3)-CH(CH3)-C2H5, -CH2-C(O)-NH2, -CH2-C(O)-NH-CH3, -CH2-C(O)-N(CH3)2, -N(CH3)-SO2-N(CH3)2, -(C6-ariI)-COOH, -fenil, -piridin-4-il, -CH2-3-metil-oksetan-3-il, -O-1,2-difluoro-fen-5-il, -O-piridin-2-il, -pirolidin-2-on-1-il, -3,5-dimetil 1-[1,2,4]triazol-4-il, 3-metil-[1,2,4]oksadiazoI-5-il, [image] ili gdje Z je C, i R4 označava -H, a R5 je skupina sa strukturom –L1-R18, gdje je L1 odabran od sljedećih: -NH-, -N(CH3)-, i -N(C2H5) i gdje je R18 odabran od sljedećih: -tetrahidropiranil, -ciklopropil, -ciklobutil, -ciklopentil, -cikloheksil, -cikloheptil, -ciklooktil, -pirolidini 1, -piperidinil. -piperazinil, -morfolinil, -kromanil, -oktahidro-pirano-pirolil, -oktahidro-pirano-piridinil, -oktahidro-pirano-oksazinil, -oksaspirodekanil, i -tetrahidro-naftiridinil, gdje je R18 opcijski supstituiran s jednom ili više skupina oda branih od sljedećih: -F, -CF3, -OCF3, -CN, -OH, -O-CH3, -CH3, -NH-C(O)-CH3, -N(CH3)-C(O)-CH3, -C(O)-CH3, -S(O)2-CH3, -NH-S(O)2-CH3, -N(CH3)-S(O)2-CH3, -N(CH3)-S(O)2-CH2-CH3, i -C(O)-O-C2H5, i gdje su R4, R5 i R18 opcijski dalje bivalentno supstituirani s jednom ili više skupina odabranih od sljedećih: [image] najednom atomu prstena ili na dva susjedna atoma prstena, tako da se formiraju spirociklički ili anelirani prsteni.
3. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je R7odabran od sljedećih: -C5-C6-aril, -C5-C6-heteroaril, -C3-C8-cikloalkil, i -C3-C8-heterociklil, gdje je prsten R7 opcijski supstituiran s jednom ili više skupina odabranih od sljedećih: -CF3,-O- CF3, -S-CF3, -CN, -metil, -C(CH3)2-CN, i -halogen.
4. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je R7 odabran od sljedećih: -C5-C6-aril, i -C5-C6-heteroaril, gdje je prsten R7 opci jski supstituiran s jednim ili više skupina odabranih od sljedećih: -CF3, -O-CF3, -S-CF3, -CN, -metil, -F, -Cl, -C(CH3)2-CN, i -Br.
5. Spoj prema bilo kojem od prethodnih zahtjeva 1, 3 i 4, naznačen time, da Z je C, i R4 označava -H, a R5 je skupina sa strukturom –L1-R18, gdje je L1 odabran od sljedećih: -NH-, -N(CH3)-, -N(C2H5) i veza, i gdje je R18 odabran od sljedećih: -C6-heterociklil koji ima 1 ili 2 heteroatoma odabranih od N i O, i gdje je R18 opcijski supstituiran s jednom ili više skupina odabranih od sljedećih: -F, -CF3, -OCF3, -CN, -OH, -O-CH3,-CH3, -NH-C(O)-CH3, -N(CH3)-C(O)-CH3, -C(O)-CH3, -S(O)2-CH3, -NH-S(O)2-CH3, -N(CH3)-S(O)2-CH3, -N(CH3)-S(O)2-CH2-CH3, i -C(O)-O-C2H5, ili gdje Z je C, i R4 i R5 su neovisno odabrani od sljedećih: -H, -C1-C6-alkil, i -N(R19,R19'), gdje R19 i R19' zajedno formiraju -C2-C6-alkilen-skupinu, poželjno -C4-C5-alkilen-skupinu tako da se formira prsten, gdje je takav prsten opcijski supstituiran s jednom ili više skupina odabranih od sljedećih: -F, -CF3, -OCF3, -CN, -OH, -O-CH3, -CH3, -NH-C(O)-CH3, -N(CH3)-C(O)-CH3, -C(O)-CH3, -S(O)2-CH3, -NH-S(O)2-CH3, -N(CH3)-S(O)2-CH3, -N(CH3)-S(O)2-CH2-CH3) -(C6-aril)-COOH, -C(O)-O-C2H5, [image]
6. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je R2 odabran od sljedećih: -H, -metil, -etil, -propil, -i-propil, -butil, -i-butil, -t-butil, -F, -Cl, -Br, -I, -CN, -CH=CH2, i -C≡CH.
7. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je R3 odabran od sljedećih: -H, -CF3, -O-CH3, i -metil.
8. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je R6 odabran od sljedećih: -H, -CH3, -C2H5, -O-CH3, -O-C2H5, -F, -CF3, i -OCF3.
9. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da R1 je-H.
10. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da n je 2.
11. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da G i E su N.
12. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da Z je C.
13. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je odabran iz skupine koju čine: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image]
14. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je odabran iz skupine koja se sastoji od sljedećih: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image]
15. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da se upotrebljava kao lijek.
16. Spoj prema bilo kojem od zahtjeva 1 do 14, naznačen time, da se upotrebljava u liječenju osteoartritisa, dijabetske nefropatije, bolova u križima, neuropatskih bolova ili bolesti s bolovima.
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