HRP20150839T1 - Spojevi aril-fenil-sulfonamido-cikloalkila i njihova uporaba - Google Patents

Spojevi aril-fenil-sulfonamido-cikloalkila i njihova uporaba Download PDF

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HRP20150839T1
HRP20150839T1 HRP20150839TT HRP20150839T HRP20150839T1 HR P20150839 T1 HRP20150839 T1 HR P20150839T1 HR P20150839T T HRP20150839T T HR P20150839TT HR P20150839 T HRP20150839 T HR P20150839T HR P20150839 T1 HRP20150839 T1 HR P20150839T1
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HRP20150839TT
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Iain Robert Greig
Rose Mary Sheridan
Raymond Fisher
Matthew John Tozer
Juha Andrew Clase
Andrew Smith
Andrew Robert Tuffnell
Robert Jurgen Van 't Hof
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Pimco 2664 Limited
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Claims (29)

1. Spoj, naznačen time, da je odabran od spojeva sljedeće formule, i njegove farmaceutski prihvatljive soli, njegovi hidrati i solvati: [image] gdje: - A je neovisno: [image] - Ar je neovisno fenil, piridinil ili pirimidinil; i p je neovisno cijeli broj od 0 do 3; i gdje: q je neovisno cijeli broj od 0 do 3; i gdje: -RSN je neovisno -H ili zasićeni alifatski C1-4alkil; i gdje: -DQ je neovisno -D1-Q1 ili D2=O; -D1- je neovisno ciklopentan-di-il, cikloheksan-di-il, cikloheptan-di-il, biciklo[3.1.1]heptan-di-il ili biciklo[3.2.1]oktan-di-il, te je po želji supstituiran s jednom ili više skupina -R°; -D2= je neovisno ciklopentan-il-iliden, cikloheksan-il-iliden, cikloheptan-il-iliden, biciklo[3.1.1]heptan-il-iliden ili biciklo[3.2.1]oktan-il-iliden, te je po želji supstituiran s jednom ili više skupina -RD; svaki -RD je neovisno odabran od sljedećih: -F, -Cl, -Br, -I, -RDD, -CF3, -OH, -ORDD, -NH2, -NHRDD i -NRDD; i svaki -RDD je neovisno zasićeni alifatski C1-4alkil; i gdje -Q1 je neovisno odabran od sljedećih: [image] [image] pri čemu: svaki -R1N je neovisno -H, -RCN ili -RCF; svaki -R2N je neovisno -H, -RCN ili -RCF; svaki -RCN je neovisno zasićeni alifatski C1-4alkil; i svaki -RCF ako je prisutan, neovisno je zasićeni alifatski C1-4fluoroalkil; ili: -NR1NR2N je neovisno azetidino, pirolidino, imidazolidino, pirazolidino, piperidino, piperazino, morfolino, tiomorfolino, azepino ili diazepino, od kojih je svaki po želji supstituiran s jednom ili više skupina neovisno odabranih od zasićenog alifatskog C1-4alkila; -R1A je neovisno -H, -RC ili -RF; i -R2A je neovisno -H, -RC ili -RF; ili -R1A i -R2A zajedno tvore zasićenu alifatsku C2-4alkilen-skupinu; -R1B je neovisno -H, -RC ili -RF; i -R2B je neovisno -H, -RC ili -RF; ili -R1B i -R2B zajedno tvore zasićenu alifatsku C2-4alkilen-skupinu; ili -R1B i -R2B zajedno tvore =O; -R3A je neovisno -H, -RC ili -RF; i -R4A je neovisno -H, -RC ili -RF; ili -R3A i -R4A zajedno tvore zasićenu alifatsku C2-4alkilen-skupinu; -R5A je neovisno -H, -RC, -RF ili -RJ; i -R6A je neovisno -H, -RC ili -RF; ili -R5A i -R6A zajedno tvore zasićenu alifatsku C2-4alkilen-skupinu; -R3B je neovisno -H, -RC ili -RF; i -R4B je neovisno -H, -RC ili -RF; ili -R3B i -R4B zajedno tvore zasićenu alifatsku C2-4alkilen-skupinu; -R5B je neovisno -H, -RC, -RF, -OH ili -OR°; i -R6b je neovisno -H, -RC ili -RF; ili -R5B i -R6B zajedno tvore zasićenu alifatsku C2-4alkilen-skupinu; svaki -RC je neovisno zasićeni alifatski C1-4alkil; svaki -RF je neovisno zasićeni alifatski C1-4fluoroalkil; -R° je neovisno zasićeni alifatski C1-4alkil; -RJ je neovisno -NH2, -NHRJN1, -NRJN1 ili -NRJN2RJN3; svaki -RJN1 je neovisno zasićeni alifatski C1-4alkil; i -NRJN2RJN3 je neovisno azetidino, pirolidino, imidazolidino, pirazolidino, piperidino, piperazino, morfolino, tiomorfolino, azepino ili diazepino, od kojih je svaki po želji supstituiran s jednom ili više skupina neovisno odabranih od zasićenog alifatskog C1-4alkila; te pri čemu je svaki -RX neovisno sljedeće: -F, -Cl, -Br, -I, -RXX, -OH, -ORXX, -SH, -SRXX, -CF3, -OCF3, -SCF3, -NH2, -NHRXX, -NRXX –NRYYRZZ, -C(=O)RXX, -OC(=O)RXX, -C(=O)OH, -C(=O)ORXX, -C(=O)NH2, -C(=O)NHRXX, -C(=O)NRXX2, -C(=O)ORYYRZZ, -OC(=O)NH2, -OC(=O)NHRXX, -OC(=O)NRXX2, -OC(=O)NRYYRZZ, -NHC(=O)RXX, -NRXXC(=O)RXX, -NHC(=O)ORXX, -NRXXC(=O)ORXX, -NHC(=O)NH2, -NHC(=O)NHRXX, -NHC(=O)NRXX2, -NHC(=O)NRYYRZZ, -NRXXC(=O)NH2, -NRXXC(=O)NHRXX, -NRXXC(=O)NRXX2, -NRXXC(=O)NRYYRZZ, -CN, -NO2, -S(=O)2NH2, -S(=O)2NHRXX, -S(=O)2NRXX2, -S(=O)2NRYYRZZ, -S(=O)RXX, -S(=O)2RXX, -OS(=O)2RXX, -S(=O)2OH ili -S(=O)2ORXX; gdje: svaki –RXX je neovisno zasićeni alifatski C1-6alkil, fenil ili benzil, pri čemu su navedeni fenil i benzil po želji supstituirani s jednom ili više skupina odabranih od sljedećih: -F, -Cl, -Br, -I, -CF3, -OCF3, -RXXX, -OH, -ORXXX ili -SRXXX, gdje svaki -RXXX je neovisno zasićeni alifatski C1-4alkil; i svaki –NRYYRZZ je neovisno azetidino, pirolidino, imidazolidino, pirazolidino, piperidino, piperazino, morfolino, tiomorfolino, azepino ili diazepino, svaki po želji supstituiran s jednom ili više skupina neovisno odabranih od zasićenog alifatskog C1-4alkila.
2. Spoj prema zahtjevu 1, naznačen time, da: svaki –RX je neovisno sljedeći: -F, -Cl, -Br, -I, -RXX, -OH, -ORXX, -SRXX, -CF3, -OCF3, -CN ili -NO2; i svaki –RXX je neovisno zasićeni alifatski C1-4alkil.
3. Spoj prema zahtjevu 1 ili 2, naznačen time, da -A je neovisno: [image] gdje: =W- je -CH= i -Y= je -CH=; -RX2 je neovisno -H ili –RX2S; -RX4 je neovisno -H ili -RX4S; -RX2S je neovisno –RX-; i -RX4S je neovisno –RX.
4. Spoj prema zahtjevu 1 ili 2, naznačen time, da -A je neovisno: [image] gdje: =W- je -CH= i -Y= je -N=; -RX2 je neovisno -H ili –RX2S; -RX4 je neovisno -H ili -RX4S; -RX2S je neovisno –RX; i -RX4S je neovisno –RX.
5. Spoj prema zahtjevu 3 ili 4, naznačen time, da: -RX2 je neovisno -RX2S; -RX4 je neovisno -RX4S.
6. Spoj prema bilo kojem od zahtjeva 3 do 5, naznačen time, da: -rx2S je neovisno -F, -Cl ili -CF3; i -RX4S je neovisno -F, -Cl ili -CF3.
7. Spoj prema bilo kojem od zahtjeva 3 do 5, naznačen time, da: -RX2S je neovisno -F; i -RX4S je neovisno -F.
8. Spoj prema bilo kojem od zahtjeva 3 do 5, naznačen time, da: -Rx2s je neovisno -Cl; i -Rx4S je neovisno -Cl.
9. Spoj prema bilo kojem od zahtjeva 1 do 8, naznačen time, da vodeća fenilna skupina je: [image] koja je [image] gdje: -RXC1 je neovisno -H ili –RXCC; -RXC2 je neovisno -H; svaki –RXCC je neovisno -F, -Cl ili –RXCCC; i svaki -RXCCC je neovisno -Me ili -Et.
10. Spoj prema zahtjevu 9, naznačen time, da: -RXC1 je neovisno -H; i -RXC2 je neovisno -H.
11. Spoj prema bilo kojem od zahtjeva 1 do 10, naznačen time, da -RSN je neovisno -H.
12. Spoj prema zahtjevu 1, naznačen time, da -DQ je neovisno -D1-Q1.
13. Spoj prema bilo kojem od zahtjeva 1 do 12, naznačen time, da -D1- je neovisno cikloheksan-1,4-di-il.
14. Spoj prema bilo kojem od zahtjeva 1 do 12, naznačen time, da -D1- je neovisno 4-metil- cikloheksan-1,4-di-il.
15. Spoj prema bilo kojem od zahtjeva 1 do 14, naznačen time, da -Q1 je neovisno: [image]
16. Spoj prema bilo kojem od zahtjeva 1 do 14, naznačen time, da -Q1 je neovisno: [image] gdje: -R1A je neovisno -H ili –RC; -R2A je neovisno -H ili –RC; i svaki -RC je neovisno -Me ili -Et.
17. Spoj prema bilo kojem od zahtjeva 1 do 14, naznačen time, da -Q1 je neovisno: [image] gdje: ili: -R1N je neovisno -H ili -RCN; -R2N je neovisno -H ili -RCN; i svaki -RCN je neovisno -Me ili -Et; ili: -NR1NR2N je neovisno pirolidino, piperidino, piperazino ili morfolino, od kojih je svaki po želji supstituiran s jednom ili više skupina odabranih od zasićenog alifatskog C1-4alkila.
18. Spoj prema bilo kojem od zahtjeva 1 do 14, naznačen time, da -Q1 je neovisno: [image] gdje: -R1B je neovisno -H ili -RC; -R2B je neovisno -H ili -RC; i svaki -RC je neovisno -Me ili -Et; i pri čemu: -R1N je neovisno -H ili -RCN; -R2N je neovisno -H ili -RCN; i svaki -RCN je neovisno -Me ili -Et; ili: -NR1NR2N je neovisno pirolidino, piperidino, piperazino ili morfolino, od kojih je svaki po želji supstituiran s jednom ili više skupina neovisno odabranih od zasićenog alifatskog C1-4alkila.
19. Spoj prema zahtjevu 1, naznačen time, da: -A je neovisno: [image] gdje: =W-je -CH= i -Y= je -CH=; -RX2 je neovisno -RX2S; -RX4 je neovisno -RX4S; -R je neovisno -F; i -RX4S je neovisno -F; vodeća fenilen-skupina: [image] je: [image] gdje: -RXC1 je neovisno -H; i -RXC2 je neovisno -H; -RSN je neovisno -H; -DQ je neovisno -D1-Q1; -D1- je neovisno 4-metil-cikloheksan-1,4-di-il; i -Q1 je neovisno: [image]
20. Spoj prema zahtjevu 1, naznačen time, da je odabran od sljedećih spojeva, i njihovih farmaceutski prihvatljivih soli, njihovih hidrata i solvata: [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]
21. Spoj prema zahtjevu 1, naznačen time, da je to sljedeći spoj ili njegova farmaceutski prihvatljiva sol, njegov hidrat ili solvat: [image]
22. Spoj prema zahtjevu 1, naznačen time, da je to sljedeći spoj ili njegova farmaceutski prihvatljiva sol, njegov hidrat ili solvat: [image]
23. Spoj prema zahtjevu 1, naznačen time, da je to sljedeći spoj ili njegova farmaceutski prihvatljiva sol, njegov hidrat ili solvat: [image]
24. Spoj prema zahtjevu 1, naznačen time, da je to sljedeći spoj ili njegova farmaceutski prihvatljiva sol, njegov hidrat ili solvat: [image]
25. Farmaceutski sastav, naznačen time, da obuhvaća spoj prema bilo kojem od zahtjeva 1 do 24 i farmaceutski prihvatljiv nosač, razrjeđivač ili pomoćno sredstvo.
26. Postupak za proizvodnju farmaceutskog sastava, naznačen time, da obuhvaća spajanje miješanjem spoja prema bilo kojem od zahtjeva 1 do 24 i farmaceutski prihvatljivog nosača, razrjeđivača ili pomoćnog sredstva.
27. Spoj prema bilo kojem od zahtjeva 1 do 24, naznačen time, da se upotrebljava u postupku liječenja ljudskog ili životinjskog tijela pomoću terapije.
28. Spoj prema bilo kojem od zahtjeva 1 do 24, naznačen time, da se upotrebljava u postupku liječenja sljedećih stanja: upalni poremećaj ili autoimuni poremećaj; poremećaj povezan s upalom i/ili s aktiviranjem imunološkog sustava; poremećaj posredovan prekomjernim i/ili neprikladnim i/ili produljenim aktiviranjem imunološkog sustava; upala; poremećaj povezan s upalom ili s aktiviranjem imunološkog sustava; reumatoidni artritis; psorijaza; psorijatički artritis; kronična opstrukcijska plućna bolest (COPD); ateroskleroza; ankilozantni spondilitis; upalna bolest crijeva; imunološka reakcija koja vodi do odbacivanja organa ili usatka nakon transplantacije; tumor koji prekomjerno izražava TNFa, IL-1, RANKL ili NFkB, ili u kojem inhibicija TNFa, IL-1, RANKL ili NFkB, olakšava ili poboljšava djelovanje citotoksičnih tumorocidnih sredstava; hematološka malignost; hematološka malignost povezana s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; višestruki mijelom, leukemija ili limfom; višestruki mijelom, leukemija ili limfom povezan s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; rak čvrstog tumora; rak čvrstog tumora povezan s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; rak mjehura, rak dojke (ženski i/ili muški), rak debelog crijeva, rak bubrega, rak pluća, rak gušterače, rak prostate, rak mozga, rak kože, rak štitnjače ili melanom; rak mjehura, rak dojke (ženski i/ili muški), rak debelog crijeva, rak bubrega, rak pluća, rak gušterače, rak prostate, rak mozga, rak kože, rak štitnjače ili melanom povezan s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; limfoblastični limfom T-stanica, limfom plaštenih stanica ili akutna limfoblastična leukemija; hematološka malignost povezana s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; limfoblastični limfom T-stanica, limfom plaštenih stanica ili akutna limfoblastična leukemija povezana s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; karcinom renalnih stanica, rak dojke (ženski i/ili muški), rak želudca, rak prostate, rak debelog crijeva ili ameloblastom bazalnih stanica; rak čvrstog tumora povezan s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; karcinom renalnih stanica, rak dojke (ženski i/ili muški), rak želudca, rak prostate, rak debelog crijeva ili ameloblastom bazalnih stanica povezan s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; gubitak kostiju; razaranje zglobova; gubitak kostiju povezan s reumatoidnim artritisom, s osteoporozom, s bolesti kostiju povezane s rakom ili s Pagetovom bolesti kostiju; reumatoidni artritis, osteoporoza, bolest kostiju povezana s rakom ili Pagetova bolest kostiju; neoplazija kostiju; ili aseptično opuštanje prostetičkih implantata.
29. Uporaba spoja prema bilo kojem od zahtjeva 1 do 24, naznačena time, da je za proizvodnju lijeka za liječenje sljedećih stanja: upalni poremećaj ili autoimuni poremećaj; poremećaj povezan s upalom i/ili s aktiviranjem imunološkog sustava; poremećaj posredovan prekomjernim i/ili neprikladnim i/ili produljenim aktiviranjem imunološkog sustava; upala; poremećaj povezan s upalom ili s aktiviranjem imunološkog sustava; reumatoidni artritis; psorijaza; psorijatički artritis; kronična opstrukcijska plućna bolest (COPD); ateroskleroza; ankilozantni spondilitis; upalna bolest crijeva; imunološka reakcija koja vodi do odbacivanja organa ili usatka nakon transplantacije; tumor koji prekomjerno izražava TNFα, IL-1, RANKL ili NFkB, ili u kojem inhibicija TNFα, IL-1, RANKL ili NFkB, olakšava ili poboljšava djelovanje citotoksičnih tumorocidnih sredstava; hematološka malignost; hematološka malignost povezana s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; višestruki mijelom, leukemija ili limfom; višestruki mijelom, leukemija ili limfom povezan s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; rak čvrstog tumora; rak čvrstog tumora povezan s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; rak mjehura, rak dojke (ženski i/ili muški), rak debelog crijeva, rak bubrega, rak pluća, rak gušterače, rak prostate, rak mozga, rak kože, rak štitnjače ili melanom; rak mjehura, rak dojke (ženski i/ili muški), rak debelog crijeva, rak bubrega, rak pluća, rak gušterače, rak prostate, rak mozga, rak kože, rak štitnjače ili melanom povezan s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; limfoblastični limfom T-stanica, limfom plaštenih stanica ili akutna limfoblastična leukemija; hematološka malignost povezana s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; limfoblastični limfom T-stanica, limfom plaštenih stanica ili akutna limfoblastična leukemija povezana s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; karcinom renalnih stanica, rak dojke (ženski i/ili muški), rak želudca, rak prostate, rak debelog crijeva ili ameloblastom bazalnih stanica; rak čvrstog tumora povezan s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; karcinom renalnih stanica, rak dojke (ženski i/ili muški), rak želudca, rak prostate, rak debelog crijeva ili ameloblastom bazalnih stanica povezan s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; gubitak kostiju; razaranje zglobova; gubitak kostiju povezan s reumatoidnim artritisom, s osteoporozom, s bolesti kostiju povezane s rakom ili s Pagetovom bolesti kostiju; reumatoidni artritis, osteoporoza, bolest kostiju povezana s rakom ili Pagetova bolest kostiju; neoplazija kostiju; ili aseptično opuštanje prostetičkih implantata.
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