HRP20161481T1 - Derivati heteroarila kao modulatori nachr alfa7 - Google Patents

Derivati heteroarila kao modulatori nachr alfa7 Download PDF

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Publication number
HRP20161481T1
HRP20161481T1 HRP20161481TT HRP20161481T HRP20161481T1 HR P20161481 T1 HRP20161481 T1 HR P20161481T1 HR P20161481T T HRP20161481T T HR P20161481TT HR P20161481 T HRP20161481 T HR P20161481T HR P20161481 T1 HRP20161481 T1 HR P20161481T1
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HR
Croatia
Prior art keywords
alkyl
optionally substituted
methyl
group
propionylthiophen
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HRP20161481TT
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English (en)
Inventor
Neelima Sinha
Gourhari Jana
Sachchidanand Sachchidanand
Sanjay Pralhad Kurhade
Navnath Popat Karche
Anil Kashiram Hajare
Ajay Ramchandra Tilekar
Venkata P. Palle
Rajender Kumar Kamboj
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Lupin Limited
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45873193&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20161481(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Lupin Limited filed Critical Lupin Limited
Publication of HRP20161481T1 publication Critical patent/HRP20161481T1/hr

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Claims (15)

1. Spoj formule I, njegovi tautomerni oblici, njegovi stereoizomeri i njegove farmaceutski prihvatljive soli, [image] naznačen time što, u spoju formule I, Z je izabran iz grupe koja se sastoji od -S-, -O- i -N(Ra)-; Ra je izabran iz grupe koja se sastoji od vodika, izborno supstituiranog alkila, izborno supstituiranog alkenila, izborno supstituiranog alkinila, izborno supstituiranog cikloalkila, izborno supstituiranog arila, izborno supstituiranog heteroarila, izborno supstituiranog heterociklila; R1 je izabran iz grupe koja se sastoji od izborno supstituiranog arila, izborno supstituiranog heteroarila, izborno supstituiranog cikloalkila, izborno supstituiranog heterociklila; R2 je izabran iz grupe koja se sastoji od vodika, izborno supstituiranog alkila, izborno supstituiranog alkenila, izborno supstituiranog alkinila, halogena, perhaloalkila, izborno supstituiranog cikloalkila, cijano, nitro, (R7)(R8)N-, R7aC(=O)N(R7)-, (R7)(R8)NC(=A1)N(R9)-, R7aOC(=O)NR9-, R7aSO2N(R8)-, R7A1- i R7aC(=O)-; R3 je izabran iz grupe koja se sastoji od izborno supstituiranog alkila, izborno supstituiranog alkenila, izborno supstituiranog alkinila, izborno supstituiranog cikloalkila, izborno supstituiranog heterociklila, pri čemu je svaki od navedenog izborno supstituiranog cikloalkila i izborno supstituiranog heterociklila izborno formiran u prsten ili izborno premošćen, (R7)(R8)N-, (R7)N(OR8)- i R7A1-; [R4]m je ’R4’ grupa ponovljena ’m’ puta, svako R4 je nezavisno izabrano iz grupe koja se sastoji od halogena, cijano, izborno supstituiranog alkila, izborno supstituiranog alkenila, izborno supstituiranog alkinila, izborno supstituiranog heteroalkila, izborno supstituiranog cikloalkila, izborno supstituiranog heterociklila, R7aC(=O)-, R7aSO2-R7A1-, (R7a)C(=O)N(R9)-, (R7)(R8)N-, (R7)(R8)NC(=A1)N(R9)-; gdje m = 0 do 3; ili dvije R4 grupe i atomi ugljika za koji su vezani formiraju izborno supstituirani 5- do 6- člani ciklični sustav koji izborno sadrži 1 do 4 hetero atoma/grupa izabranih iz grupe koja se sastoji od -N-, -S-, -O-, - C(=O)- i -C(=S)-; R5 i R6 su nezavisno izabrani iz grupe koja se sastoji od vodika, R7aC(=O)-, izborno supstituiranog alkila, izborno supstituiranog alkenila, izborno supstituiranog alkinila, izborno supstituiranog cikloalkila, izborno supstituiranog heterociklila, izborno supstituiranog arila, i izborno supstituiranog heteroarila; ili R5 i R6 zajedno sa atomom dušika za koji su vezani formiraju 3- do 10- člani izborno supstituirani zasićeni/nezasićeni heterociklični sustav prstena koja sadrži jedan do tri hetero atoma/grupe izabrane iz grupe koja se sastoji od -S-, -N-,-O-, - C(=O)- i -C(=S)-; gdje R7, R8 i R9 su nezavisno izabrani iz grupe koja se sastoji od vodika, izborno supstituiranog alkila, izborno supstituiranog alkenila, izborno supstituiranog alkinila, izborno supstituiranog heteroalkila, izborno supstituiranog arila, izborno supstituiranog heteroarila, izborno supstituiranog cikloalkila i izborno supstituiranog heterociklila; A1 je izabran iz grupe koja se sastoji od O i S; R7a je izabran iz grupe koja se sastoji od izborno supstituiranog alkila, izborno supstituiranog alkenila, izborno supstituiranog alkinila, izborno supstituiranog heteroalkila, izborno supstituiranog arila, izborno supstituiranog heteroarila, izborno supstituiranog cikloalkila i izborno supstituiranog heterociklila; gdje, termin "izborno supstituirani alkil", označava grupu nesupstituiranu ili supstituiranu sa 1 do 6 supstituenata izabranih nezavisno iz grupe koja se sastoji od okso, halogen, nitro, cijano, aril, hereroaril, cikloalkil, R10aSO2-, R10A1-, R10aOC(=O)-, R10aC(=O)O-, (R10)(H)NC(=O)-, (R10)(alkil)NC(=O)-, R10aC(=O)N(H)-, (R10)(H)N-, (R10)(alkil)N-, (R10)(H)NC(=A1)N(H)- i (R10)(alkil)NC(=A1)N(H)-; termin "izborno supstituirani alkenil", označava alkenil grupu nesupstituiranu ili supstituiranu sa 1 do 6 supstituenata izabranih nezavisno iz grupe koja se sastoji od okso, halogena, nitro, cijano, arila, hereroarila, cikloalkila, R10aSO2-, R10A1-, R10aOC(=O)-, R10aC(=O)O-, (R10)(H)NC(=O)-, (R10)(alkil)NC(=O)-, R10aC(=O)N(H)-, (R10)(H)N-, (R10)(alkil)N-, (R10)(H)NC(=A1)N(H)- i (R10)(alkil)NC(=A1)N(H)-; termin "izborno supstituirani alkinil", označava alkinil grupu nesupstituiranu ili supstituiranu sa 1 do 6 supstituenata izabranih nezavisno iz grupe koja se sastoji od okso, halogena, nitro, cijano, arila, hereroarila, cikloalkila, R10aSO2-, R10A1-, R10aOC(=O)-, R10aC(=O)O-, (R10)(H)NC(=O)-, (R10)(alkil)NC(=O)-, R10aC(=O)N(H)-, (R10)(H)N-, (R10)(alkil)N-, (R10)(H)NC(=A1)N(H)- i (R10)(alkil)NC(=A1)N(H)-; termin "izborno supstituirani heteroalkil" označava heteroalkil grupu nesupstituiranu ili supstituiranu sa 1 do 6 supstituenata izabranih nezavisno iz grupe koja se sastoji od okso, halogena, nitro, cijano, arila, hereroarila i cikloalkila; termin "izborno supstituirani cikloalkil" označava cikloalkil grupu nesupstituiranu ili supstituiranu sa 1 do 6 supstituenata izabranih nezavisno iz grupe koja se sastoji od okso, halogena, nitro, cijano, arila, hereroarila, alkila, alkenila, alkinila, R10aC(=O)-, R10aSO2-, R10A1-, R10aOC(=O)-, R10aC(=O)O-, (R10)(H)NC(=O)-, (R10)(alkil)NC(=O)-, R10aC(=O)N(H)-, (R10)(H)N-, (R10)(alkil)N-, (R10)(H)NC(=A1)N(H)- i (R10)(alkil)NC(=A1)N(H)-; termin "izborno supstituirani aril" označava (i) aril grupu nesupstituiranu ili supstituiranu sa 1 do 3 supstituenata izabranih nezavisno iz grupe koja se sastoji od halogena, nitro, cijano, hidroksi, C1 do C6 alkila, C2 do C6 alkenila, C2 do C6 alkinila, C3 do C6 cikloalkila, C1 do C6 perhaloalkila, alkil-O-, alkenil-O-, alkinil-O-, perhaloalkil-O-, alkil-N(alkil)-, alkil-N(H)-, H2N-, alkil-SO2-, perhaloalkil-SO2-, alkil-C(=O)N(alkil)-, alkil-C(=O)N(H)-, alkil-N(alkil)C(=O)-, alkil-N(H)C(=O)-, H2NC(=O)-, alkil-N(alkil)SO2-, alkil-N(H)SO2-, H2NSO2-, 3- do 6- članog heterociklusa koji sadrži 1 do 2 heteroatoma izabrana iz grupe koja se sastoji od N, O i S, pri čemu je navedeni 3- do 6- člani heterociklus izborno supstituiran sa alkilom, alkenilom, alkinilom ili alkil-C(=O)- ili (ii) navedeni supstituirani ili nesupstituirani aril prsten izborno fuzioniran sa cikloalkan prstenom ili heterocikličnim prstenom koji sadrži 1 do 3 heteroatoma izabrana od S, O, N, preko veze, pri čemu je navedeni cikloalkan prsten ili heterociklični prsten izborno supstituiran sa okso, alkil, alkenil, alkinil ili alkil-C(=O)-; termin "izborno supstituirani heterociklil" označava (i) heterociklil grupu nesupstituiranu ili supstituiranu na ugljicima prstena sa 1 do 6 supstituenata izabranih nezavisno iz grupe koja se sastoji od okso, halogena, nitro, cijano, arila, hereroarila, alkila, alkenila, alkinila, R10A1-, R10aOC(=O)-, R10aC(=O)O-, (R10)(H)NC(=O)-, (R10)(alkil)NC(O)-, R10aC(=O)N(H)-, (R10)(H)N-, (R10)(alkil)N-, (R10)(H)NC(=A1)N(H)- i (R10)(alkil)NC(=A1)N(H)-; (ii) heterociklil grupu izborno supstituiranu na dušiku(dušicima) prstena sa jednim ili više supstituenata izabranih iz grupe koja se sastoji od hereroarila, alkila, alkenila, alkinila, R10aC(=O)-, R10aSO2-, R10aOC(=O)-, (R10)(H)NC(=O)-, (R10)(alkil)NC(=O)- i arila nesupstituiranog ili supstituiranog sa 1 do 3 supstituenata izabranih nezavisno od halogena, alkila, alkenila, alkinila, cijano ili nitro; termin "izborno supstituirani heteroaril" označava heteroaril grupu nesupstituiranu ili supstituiranu sa 1 do 3 supstituenata izabranih nezavisno iz grupe koja se sastoji od halogena, nitro, cijano, hidroksi, C1 do C6 alkila, C2 do C6 alkenila, C2 do C6 alkinila, C3 do C6 cikloalkila, C1 do C6 perhaloalkila, alkil-O-, alkenil-O-, alkinil-O-, perhaloalkil-O-, alkil-N(alkil)-, alkil-N(H)-, H2N-, alkil-SO2-, perhaloalkil-SO2-, alkil-C(=O)N(alkil)-, alkil-C(=O)N(H)-, alkil-N(alkil)C(=O)-, alkil-N(H)C(=O)-, H2NC(=O)-, alkil-N(alkil)SO2-, alkil-N(H)SO2-, H2NSO2-, i 3- do 6-članog heterociklusa koji sadrži 1 do 2 heteroatoma izabrana iz grupe koja se sastoji od N, O i S, pri čemu je heterociklus izborno supstituiran sa jednim do četiri supstituenta izabranih iz grupe koja se sastoji od alkila, alkenila, alkinila ili alkil-C(=O); termin "izborno supstituirani 5- do 6- člani ciklični sustav" označava 5- do 6- člani ciklični sustav nesupstituiran ili supstituiran sa 1 do 3 supstituenta izabrana iz grupe koja se sastoji od okso, halogena, nitro, cijano, arila, hereroarila, alkila, alkenila, alkinila, R10aC(=O)-, R10aSO2-, R10A1-, R10aOC(=O)-, R10aC(=O)O-, (R10)(H)NC(=O)-, (R10)(alkil)NC(=O)-, R10aC(=O)N(H)-, (R10)(H)N-, (R10)(alkil)N-, (R10)(H)NC(=A1)N(H)- i (R10)(alkil)NC(=A1)N(H)-; termin "3- do 10- člani izborno supstituirani zasićeni/nezasićeni heterociklični sustav prstena" označava 3- do 10- člani zasićeni/nezasićeni heterociklični sustav prstena nesupstituiran ili supstituiran sa 1 do 3 supstituenta izabrana iz grupe koja se sastoji od okso, halogena, nitro, cijano, arila, hereroarila, alkila, alkenila, alkinila, R10aC(=O)-, R10aSO2-, R10A1-, R10aOC(=O)-, R10aC(=O)O-, (R10)(H)NC(=O)-, (R10)(alkil)NC(=O)-, R10aC(=O)N(H)-, (R10)(H)N-, (R10)(alkil)N-, (R10)(H)NC(=A1)N(H)- i (R10)(alkil)NC(=A1)N(H)-; gdje je R10 izabran od vodika, alkila, alkenila, alkinila, arila, heteroarila, cikloalkila ili heterociklila; i R10a je izabran iz grupe koja se sastoji od alkila, alkenila, alkinila, perhaloalkila, arila, heteroarila, cikloalkila ili heterociklila.
2. Spoj formule I, njegovi tautomerni oblici, njegovi stereoizomeri i njegove farmaceutski prihvatljive soli, prema patentnom zahtjevu 1, naznačen time što R2 je izabran iz grupe koja se sastoji od vodika, izborno supstituiranog alkila i (R7)(R8)N-.
3. Spoj formule I, njegovi tautomerni oblici, njegovi stereoizomeri i njegove farmaceutski prihvatljive soli, prema bilo kojem od patentnih zahtjeva 1-2, naznačen time što R3 je izabran iz grupe koja se sastoji od izborno supstituiranog alkila, izborno supstituiranog heterociklila, R7A1-, (R7)(R8)N- i (R7)N(OR8)-, poželjnije iz grupe koja se sastoji od slijedećih: metil, etil, n-propil, metoksi, etoksi, dimetilamino, N-metoksi-N-metil amino, N-(2-hidroksi etil)-N-propilamino, acetilaminometil i piperidinil.
4. Spoj formule I, njegovi tautomerni oblici, njegovi stereoizomeri i njegove farmaceutski prihvatljive soli, prema bilo kojem od patentnih zahtjeva 1-3, naznačen time što su R5 i R6 nezavisno izabrani iz grupe koja se sastoji od vodika, izborno supstituiranog alkila ili oba R5 i R6 zajedno sa atomom dušika za koji su vezani formiraju 3- do 10- člani izborno supstituirani zasićeni/nezasićeni heterociklični sustav prstena koji sadrži jedan do tri hetero atoma/grupe izabrane iz grupe koja se sastoji od -S-, -N-, -O-, -C(=O)- i -C(=S)-.
5. Spoj formule I, njegovi tautomerni oblici, njegovi stereoizomeri i njegove farmaceutski prihvatljive soli, prema bilo kojem od patentnih zahtjeva 1-4, naznačen time što m je 0, 1 ili 2, i R4 je ili su izabrani od izborno supstituirane alkil grupe ili grupa ili dva R4 zajedno sa atomima ugljika za koji su vezani formiraju izborno supstituirani 5- do 6- člani ciklični sustav prstena koji izborno sadrži 1 do 4 hetero atoma/grupe izabrane iz grupe koja se sastoji od -N-, -S-, -O-, -C(=O)- i -C(=S)-.
6. Spoj formule I, njegovi tautomerni oblici, njegovi stereoizomeri i njegove farmaceutski prihvatljive soli, prema bilo kojem od patentnih zahtjeva 1-5, naznačen time što m je 0, 1 ili 2, i R4 je ili su izabrani od metil grupe ili grupa ili dva R4 zajedno sa atomima ugljika za koji su vezani formiraju šestočlani karbociklus.
7. Spoj formule I, njegovi tautomerni oblici, njegovi stereoizomeri i njegove farmaceutski prihvatljive soli, prema bilo kojem od patentnih zahtjeva 1-6, naznačen time što Ra je izabran od vodika i izborno supstituiranog alkila.
8. Spoj formule I, njegovi tautomerni oblici, njegovi stereoizomeri i njegove farmaceutski prihvatljive soli, prema bilo kojem od patentnih zahtjeva 1-7, naznačen time što R2 je izabran iz grupe koja se sastoji od vodika, izborno supstituiranog alkila i (R7)(R8)N-; R3 je izabran iz grupe koja se sastoji od izborno supstituiranog alkila, izborno supstituiranog heterociklila, R7A1-, (R7)(R8)N- i (R7)N(OR8)-; R5 i R6 su izabrani nezavisno iz grupe koja se sastoji od vodika, izborno supstituiranog alkila ili oba R5 i R6 zajedno sa atomom dušika za koji su vezani tako da formiraju 3- do 10-člani izborno supstituirani zasićeni/nezasićeni heterociklični sustav prstena koji sadrži jedan do tri hetero atoma/grupe izabrane iz grupe koja se sastoji od -S-, -N-, -O-, -C(=O)- i -C(=S)-; m je 0, 1 ili 2, i R4 je ili su izabrani od izborno supstituirane alkil grupe ili grupa ili dva R4 zajedno sa atomima ugljika za koje su vezani formiraju izborno supstituirani 5- do 6- člani ciklični sustav koji izborno sadrži 1 do 4 hetero atoma/grupe izabrane iz grupe koja se sastoji od -N-, -S-, -O-, -C(=O)- i -C(=S)-; i Ra je izabran iz grupe koja se sastoji od vodika i izborno supstituiranog alkila.
9. Spoj formule I, njegovi tautomerni oblici, njegovi stereoizomeri i njegove farmaceutski prihvatljive soli, prema bilo kojem od patentnih zahtjeva 1-8, naznačen time što R1 je izabran iz grupe koja se sastoji od piridila, furanila, indolila, N-metilizoindolila, benzofuranila, piperazinila, 4-(4-fluorofenil)piperazinila, morfolinila, indolinila, 2-oksoindolinila, 2,3-dihidrobenzo[b][1,4]dioksinila, benzopiranila i fenila izborno supstituiranog sa 1 do 2 supstituenta izabrana iz grupe koja se sastoji od halo, ciklopropila, trifluorometila, metoksi, etoksi, trifluorometoksi, metila, etila, dimetilamino, monometilamino, terc-butila i 4-metilpiperazinila; R2 je izabran iz grupe koja se sastoji od vodika, metila, dimetilamino i dimetilaminometila; R3 je izabran iz grupe koja se sastoji od metila, etila, n-propila, metoksi, etoksi, dimetilamino, N-metoksi-N-metil amino, N-(2-hidroksi etil)-N-propil amino, acetilaminometila i piperidinila; R5 i R6 su izabrani nezavisno iz grupe koja se sastoji od vodika, metila ili R5 i R6 zajedno s atomom dušika za koji su vezani formiraju piperidin prsten; m je 0, 1 ili 2, i R4 je izabran od metil grupa ili dva R4 zajedno sa atomima ugljika za koje su vezani formiraju šestočlani karbociklus; i Ra je izabran iz grupe koja se sastoji od vodika, metila, etila i ciklopropilmetila.
10. Spoj formule I njegovi tautomerni oblici, njegovi stereoizomeri i njegove farmaceutski prihvatljive soli, prema bilo kojem od patentnih zahtjeva 1-9, naznačen time što R1 je izabran iz grupe koja se sastoji od 4-klorofenila, 2-klorofenila, 3-klorofenila, 4-fluorofenila, 4-ciklopropilfenila, 4-trifluorometilfenila, 4-metoksifenila, 4-etoksifenila, 3-etoksifenila, 4-tolila, 4-terc-butil fenila, 4-dimetilaminofenila, 3-fluorofenila, fenila, 4-etilfenila, 3,4-diklorofenila, 2,4-diklorofenila, 2,4-difluorofenila, 3-kloro-4-fluorofenila, 3-kloro-4-metoksifenila, piperazin-1-ila, 4-(fluorofenil)piperazinila, morfolino, piridin-4-ila, piridin-3-ila, furan-3-ila, 1H-indol-5-ila, 1-metil-1H-indol-5-ila, benzofuran-5-ila, indolin-5-ila, 4-(4-metilpiperazinil-1-il)fenila i 2,3-dihidrobenzo[b][1,4]dioksin-6-ila).
11. Spoj formule I njegovi tautomerni oblici, njegovi stereoizomeri i njegove farmaceutski prihvatljive soli, prema bilo kojem od patentnih zahtjeva 1-10, naznačen time što Z je S.
12. Spoj formule I, njegovi tautomerni oblici, njegovi stereoizomeri i njegove farmaceutski prihvatljive soli, prema bilo kojem od patentnih zahtjeva 1-11, naznačen time što je spoj izabran iz grupe koja se sastoji od slijedećih: 4-(5-(4-klorofenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(2-klorofenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(3-klorofenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(4-fluorofenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(4-ciklopropilfenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(4-metil-2-propionil-5-(4-(trifluorometil)fenil)tiofen-3-il)benzen sulfonamid; 4-(5-(4-metoksifenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(4-etoksifenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(4-metil-2-propionil-5-(4-(trifluorometoksi)fenil)tiofen-3-il) benzensulfonamid; 4-(4-metil-2-propionil-5-(4-tolil)tiofen-3-il)benzensulfonamid; 4-(5-(4-(terc-butil)fenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-((5-(4-dimetilamino)fenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(3-fluorofenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(4-metil-5-fenil-2-propioniltiofen-3-il)benzensulfonamid; 4-(5-(3-etoksifenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(4-etilfenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(3,4-diklorofenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(2,4-diklorofenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(2,4-difluorofenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(3-kloro-4-fluorofenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(3-kloro-4-metoksifenil)-4-metil-2-propioniltiofen-3-il) benzensulfonamid; 4-(4-metil-5-(piperazin-1-il)-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(4-(4-fluorofenil)piperazin-1-il)-4-metil-2-propioniltiofen-3-il)benzensulfonamid; 4-(4-metil-5-morfolino-2-propioniltiofen-3-il)benzensulfonamid; 4-(4-metil-2-propionil-5-(piridin-4-il)tiofen-3-il)benzensulfonamid; 4-(4-metil-2-propionil-5-(piridin-3-il)tiofen-3-il)benzensulfonamid; 4-(5-(furan-3-il)-4-metil-2-propioniltiofen-3-il)benzensulfonamid; 4-(5-(1H-indol-5-il)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(4-metil-5-(1-metil-1H-indol-5-il)-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(benzofuran-5-il)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(indolin-5-il)-4-metil-2-propioniltiofen-3-il)benzensulfonamid; 4-(4-metil-5-(4-(4-metilpiperazin-1-il)fenil)-2-propioniltiofen-3-il)benzensulfonamid; 4-(5-(4-klorofenil)-2-propioniltiofen-3-il)benzensulfonamid; 4-(5-(4-klorofenil)-4-(dimetilamino)-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(4-klorofenil)-4-((dimetilamino)metil)-2-propioniltiofen-3-il) benzensulfonamid; 5-(4-klorofenil)-N,N,4-trimetil-3-(4-sulfamoilfenil)tiofen-2-karboksamid; 5-(4-klorofenil)-N-metoksi-N,4-dimetil-3-(4-sulfamoilfenil) tiofen-2-karboksamid; 5-(4-klorofenil)-N-(2-hidroksietil)-4-metil-N-propil-3-(4-sulfamoilfenil)tiofen-2-karboksamid; 4-(5-(4-klorofenil)-4-metil-2-(piperidine-1-karbonil)tiofen-3-il) benzensulfonamid; 4-(2-acetil-5-(4-klorofenil)-4-metiltiofen-3-il)benzensulfonamid; 4-(5-(4-klorofenil)-4-metil-2-propioniltiofen-3-il)-2-metilbenzen sulfonamid; Metil 4-metil-5-(2-oksoindolin-5-il)-3-(4-sulfamoilfenil)tiofen-2-karboksilat; Etil 4-metil-5-(2-oksoindolin-5-il)-3-(4-sulfamoilfenil)tiofen-2-karboksilat; 4-(4-metil-5-(4-mehilaminofenil)-2-propioniltiofen-3-il)benzen sulfonamid; 4-(5-(4-klorofenil)-4-metil-2-propioniltiofen-3-il)-N,N-dimetilbenzensulfonamid; 4-(5-(4-klorofenil)-4-metil-2-propioniltiofen-3-il)-N-metilbenzensulfonamid; 4-(5-(3,4-difluorofenil)-4-metil-2-propioniltiofen-3-il)benzen sulfonamid; 1-(5-(4-klorofenil)-4-metil-3-(4-(piperidin-1-ilsulfonil)fenil) tiofen-2-il)propan-1-on 4-(5-(4-klorofenil)-1,4-dimetil-2-propionil-1H-pirol-3-il) benzen sulfonamid; 5-(4-klorofenil)-N,N,1,4-tetrametil-3-(4-sulfamoilfenil)-1H-pirol-2-karboksamid; 4-(5-(4-klorofenil)-1-etil-4-metil-2-propionil-1H-pirol-3-il)benzen sulfonamid; 4-(5-(4-klorofenil)-1-(ciklopropilmetil)-4-metil-2-propionil-1H-pirol-3-il) benzen sulfonamid; 4-(5-(4-klorofenil)-4-metil-2-propionil-1H-pirol-3-il) benzen sulfonamid; 4-(5-(4-fluorofenil)-1,4-dimetil-2-propionil-1H-pirol-3-il) benzen sulfonamid; 4-(5-(4-metoksifenil)-1,4-dimetil-2-propionil-1H-pirol-3-il) benzen sulfonamid; 4-(2-butiril -5- (4- klorofenil) -1,4-dimetil -1H pirol -3- yl) benzen sulfonamid; 4-(5-(2,4-diklorofenil)-1,4-dimetil-2-propionil-1H-pirol-3-il) benzen sulfonamid; 4-(5-(2,3-dihidrobenzo[b][1,4]dioksin- 6 -il) -1,4- dimetil -2-propionil-1H-pirol-3-il) benzen sulfonamid; etil 5-(4-klorofenil)-4-metil-3-(4-sulfamoil-5,6,7,8-tetrahidronaphthalen-1-il)tiofen-2-karboksilat; i etil 5-(4-klorofenil)-3-(4-sulfamoilfenil)furan-2-karboksilat.
13. Farmaceutski pripravak koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1-12 i farmaceutski prihvatljivi nosač.
14. Uporaba spoja prema patentnom zahtjevu 1 u pripremi lijeka za prevenciju ili liječenje bolesti ili njenih simptoma ili poremećaja posredovanog djelomično ili potpuno preko nikotinskih acetilkolinskih receptora, naznačena time što je poremećaj ili stanje ili bolest izabrano/izabrana iz grupe koja se sastoji od Alzheimerove bolesti, blagog kognitivnog oštećenja, senilne demencije, vaskularne demencije, demencije od Parkinsonove bolesti, poremećaja smanjene pažnje, poremećaja smanjene pažnje i hiperaktivnosti, demencije povezana sa Lewyevim tijelima, kompleksa SIDAe i demencije, Pickove bolesti, demencije povezane sa Downovim sindromom, Huntingtonove bolesti, kognitivnih deficita povezanih sa traumatskom povredom mozga, kognitivnog opadanja povezanog sa moždanim udarom, neuroprotekcije poslije moždanog udara, deficita kognitivne i senzorimotorne filtracije povezanih sa shizofrenijom, kognitivnih deficita povezanih sa bipolarnim poremećajem, kognitivnih oštećenja povezanih sa depresijom, akutnom boli, post-kirurškom ili postoperativnom boli, kroničnom boli inflamacije, inflamatornom boli, neuropatskom boli, prestankom pušenja, potrebe za rastom novih krvnih žila povezanih sa zarastanjem rana, potrebe za rastom novih krvnih žila povezanih sa vaskularizacijom presadaka kože i nedostatkom cirkulacije, artritisa, reumatoidnog artritisa, psorijaze, Kronove bolesti, ulceroznog kolitisa, reervoara, inflamatorne bolesti crijeva, celijakije, periodontitisa, sarkoidoze, pankreatitisa, obacivanja transplantiranog organa, akutne imune bolesti povezane sa transplantacijom organa, kronične imune bolesti povezane sa transplantacijom organa, septičkog šoka, sindroma toksičnog šoka, sindroma sepse, depresije i reumatoidnog spondilitisa.
15. Spoj prema patentnom zahtjevu 1 za uporabu u prevenciji ili liječenju bolesti ili poremećaja posredovanog djelomično ili potpuno preko nikotinskih acetilkolinskih receptora, naznačen time što je poremećaj ili stanje ili bolest izabrano/izabrana iz grupe koja se sastoji od Alzheimerove bolesti, blagog kognitivnog oštećenja, senilne demencije, vaskularne demencije, demencije od Parkinsonove bolesti, poremećaja smanjene pažnje, poremećaja smanjene pažnje i hiperaktivnosti, demencije povezana sa Lewyevim tijelima, kompleksa SIDAe i demencije, Pickove bolesti, demencije povezane sa Downovim sindromom, Huntingtonove bolesti, kognitivnih deficita povezanih sa traumatskom povredom mozga, kognitivnog opadanja povezanog sa moždanim udarom, neuroprotekcije poslije moždanog udara, deficita kognitivne i senzorimotorne filtracije povezanih sa shizofrenijom, kognitivnih deficita povezanih sa bipolarnim poremećajem, kognitivnih oštećenja povezanih sa depresijom, akutne boli, post-kirurške ili postoperativne boli, kronične boli, inflamacije, inflamatorne boli, neuropatske boli, prestanka pušenja, potrebe za rastom novih krvnih žila povezane sa zarastanjem rana, potrebe za rastom novih krvnih žila povezane sa vaskularizacijom presadaka kože i nedostatkom cirkulacije, artritisa, reumatoidnog artritisa, psorijaze, Kronove bolesti, ulceroznog kolitisa, rezervoara, inflamatorne bolesti crijeva, celijakije, periodontitisa, sarkoidoze, pankreatitisa, odbacivanja transplantiranog organa, akutne imune bolesti povezane sa transplantacijom organa, kronične imune bolesti povezane sa transplantacijom organa, septičkog šoka, sindroma toksičnog šoka, sindroma sepse, depresije i reumatoidnog spondilitisa.
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