HRP20220132T1 - Aromatski amidi karboksilne kiseline kao antagonisti bradikininskog b1 receptora - Google Patents

Aromatski amidi karboksilne kiseline kao antagonisti bradikininskog b1 receptora Download PDF

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Publication number
HRP20220132T1
HRP20220132T1 HRP20220132TT HRP20220132T HRP20220132T1 HR P20220132 T1 HRP20220132 T1 HR P20220132T1 HR P20220132T T HRP20220132T T HR P20220132TT HR P20220132 T HRP20220132 T HR P20220132T HR P20220132 T1 HRP20220132 T1 HR P20220132T1
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Croatia
Prior art keywords
fluoro
alkyl
phenyl
cyclopropyl
amino
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HRP20220132TT
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English (en)
Inventor
Stefan BÄURLE
Adam James Davenport
Christopher STIMSON
Jens Nagel
Nicole Schmidt
Andrea Rotgeri
Ina Gröticke
Alexandra RAUSCH
Jürgen KLAR
Thomas Dyrks
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Bayer Pharma Aktiengesellschaft
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Publication of HRP20220132T1 publication Critical patent/HRP20220132T1/hr

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    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
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Claims (22)

1. Spoj opće formule (I): [image] R1 predstavlja • fenil, • 5- ili 6-člani heteroaril, pri čemu navedeni 5-člani heteroaril sadrži 1, 2 ili 3 heteroatoma ili skupine koje sadrže heteroatom neovisno odabrane iz skupine koju čine S, N, NH, i O, te pri čemu navedeni 6-člani heteroaril sadrži 1 ili 2 dušikova atoma, ili • biciklički 8- do 10-člani heteroaril koji sadrži 1, 2 ili 3 heteroatoma ili skupine koje sadrže heteroatom neovisno odabrane od NH, N, O, S, SO i SO2, pri čemu navedeni R1 je po izboru supstituiran na jednom ili više ugljikovih atoma sa 1 do 3 supstituenta R1a koji su isti ili različiti, pri čemu R1a predstavlja C1-C5-alkil, C3-C7-cikloalkil, -(C1-C3-alkil)-(C3-C7-cikloalkil), -OC1-C5-alkil, -OC3-C7-cikloalkil, NHR4, N(R4)2, NH(C3-C7-cikloalkil), halogen, CN, NHSO2R4, SO2R4, 5- do 7-člani laktam, ili 4- do 7-člani heterocikloalkil koji sadrži 1 ili 2 heteroatoma ili skupine koje sadrže heteroatom neovisno odabrane od NH, -NR4, N, O, S, SO i SO2,i pri čemu neovisno, ako R1 predstavlja 5- člani heteroaril ili biciklički 8- do 10-člani heteroaril, svaki atom dušika u prstenu, ako je prisutan, iz navedenog R1 je po izboru supstituiran sa supstituentom R1b, pri čemu R1b predstavlja C1-C5-alkil,-(C1-C3-alkil)-(C3-C7-cikloalkil), C3-C7-cikloalkil, SO2R4, ili 4- do 7-člani heterocikloalkil koji sadrži 1 ili 2 heteroatoma ili skupine koje sadrže heteroatom neovisno odabrane od NH, -NR4, N, O, S, SO i SO2,i ako R1a predstavlja C1-C5-alkil, C3-C7-cikloalkil, -(C1-C3-alkil)-(C3-C7-cikloalkil), -OC1-C5-alkil ili -OC3-C7-cikloalkil i/ ili ako R1b predstavlja C1-C5-alkil, -(C1-C3-alkil)-(C3-C7-cikloalkil), ili C3-C7-cikloalkil, navedeni C1-C5-alkil, C3-C7-cikloalkil, -(C1-C3-alkil)-(C3-C7-cikloalkil), -OC1-C5-alkil i -OC3-C7-cikloalkil neovisno su po izboru supstituirani s jednim ili više supstituenata neovisno odabranih iz skupine koju čine metil, etil, OH, OR4 i F, i ako R1a i/ ili R1b predstavljaju 4- do 7-člani heterocikloalkil, svaki ugljikov atom iz navedenog 4- do 7-članog heterocikloalkila je po izboru supstituiran s jednim ili više supstituenata neovisno odabranih iz skupine koju čine OH, OR4 i F; R2 predstavlja • -(CH2)p-(C5-C7-cikloalkil), • -(CH2)p-fenil, • 5- ili 6-člani heteroaril pri čemu navedeni 5-člani heteroaril sadrži 1, 2 ili 3 heteroatoma ili skupine koje sadrže heteroatom neovisno odabrane iz skupine koju čine S, N, NH, i O, te pri čemu navedeni 6-člani heteroaril sadrži 1 ili 2 dušikova atoma, ili • biciklički 8- do 10-člani heteroaril koji sadrži 1, 2 ili 3 heteroatoma ili skupine koje sadrže heteroatom neovisno odabrane od NH, N, O, S, SO i SO2, pri čemu je navedeni R2 po izboru supstituiran na jednom ili više ugljikovih atoma sa 1 do 3 supstituenta R2a koji su isti ili različiti, pri čemu R2a predstavlja C1-C5-alkil, C3-C7-cikloalkil, -(C1-C3-alkil)-(C3-C7-cikloalkil), -OC1-C5-alkil, -OC3-C7-cikloalkil, halogen, OH ili CN, i pri čemu neovisno, ako R2 predstavlja 5-člani heteroaril ili biciklički 8- do 10-člani heteroaril, svaki dušikov atom u prstenu, ako je prisutan, iz navedenog R2 je po izboru supstituiran sa supstituentom R2b, pri čemu R2b predstavlja C1-C5-alkil, C3-C7-cikloalkil ili -(C1-C3-alkil)-(C3-C7-cikloalkil), i ako R2a predstavlja C1-C5-alkil, C3-C7-cikloalkil, -(C1-C3-alkil)-(C3-C7-cikloalkil), -OC1-C5-alkil ili -OC3-C7-cikloalkil i/ili ako R2b predstavlja C1-C5-alkil, C3-C7-cikloalkil ili -(C1-C3-alkil)-(C3-C7-cikloalkil), navedeni C1-C5-alkil, C3-C7-cikloalkil, -(C1-C3-alkil)-(C3-C7-cikloalkil), -OC1-C5-alkil i -OC3-C7-cikloalkil neovisno su po izboru supstituirani s jednim ili više supstituenata neovisno odabranih iz skupine koju čine OH, OR4, i F; p predstavlja 0 ili 1; R3 predstavlja H ili F; R4 predstavlja C1-C5-alkil, po izboru supstituiran s 1 do 5 fluorovih atoma; R5 predstavlja H, halogen, CN, C1-C5-alkil, ili -OC1-C5-alkil, pri čemu navedeni C1-C5-alkil i -OC1-C5-alkil su po izboru supstituirani s 1 do 5 fluorovih atoma; i R6 i R7 neovisno predstavljaju H ili C1-C3-alkil, pri čemu je navedeni C1-C3-alkil po izboru supstituiran s 1 do 5 fluorovih atoma; ili izomer, enantiomer, dijastereomer, racemat, hidrat, solvat, ili njegova sol, naročito njegova farmaceutski prihvatljiva sol, ili mješavina istih.
2. Spoj prema patentnom zahtjevu 1, naznačen time što R1 predstavlja 5-člani heteroaril koji sadrži 1, 2 ili 3 heteroatoma ili skupine koje sadrže heteroatom neovisno odabrane iz skupine koju čine S, N, NH, i O, naročito pirazolil, tiazolil, imidazolil ili tiofenil, pri čemu je navedeni R1 po izboru supstituiran na jednom ili više ugljikovih atoma sa 1 ili 2 supstituenta R1a koji su isti ili različiti, pri čemu R1a predstavlja C1-C5-alkil, C3-C7-cikloalkil, -(C1-C3-alkil)-(C3-C7-cikloalkil), -OC1-C5-alkil,-OC3-C7-cikloalkil, halogen ili CN, i pri čemu neovisno svaki dušikov atom u prstenu, ako je prisutan, iz navedenog R1 je po izboru supstituiran sa supstituentom R1b, pri čemu R1b predstavlja C1-C5-alkil, -(C1-C3-alkil)-(C3-C7-cikloalkil) ili C3-C7-cikloalkil, i ako R1a predstavlja C1-C5-alkil, C3-C7-cikloalkil, -(C1-C3-alkil)-(C3-C7-cikloalkil), -OC1-C5-alkil ili -OC3-C7-cikloalkil i/ili ako R1b predstavlja C1-C5-alkil, -(C1-C3-alkil)-(C3-C7-cikloalkil) ili C3-C7-cikloalkil, navedeni C1-C5-alkil, C3-C7-cikloalkil, -(C1-C3-alkil)-(C3-C7-cikloalkil), -OC1-C5-alkil i -OC3-C7-cikloalkil neovisno su po izboru supstituirani s jednim ili više supstituenata neovisno odabranih iz skupine koju čine metil, etil, OH, OR4 i F.
3. Spoj prema bilo kojem od patentnih zahtjeva 1 ili 2, naznačen time što R1 predstavlja pirazol-4-il, nesupstituiran ili supstituiran na dušikovom atomu na poziciji 1 sa supstituentom R1b, pri čemu R1b predstavlja C1-C5-alkil, -(C1-C3-alkil)-(C3-C7-cikloalkil) ili C3-C7-cikloalkil, pri čemu navedeni R1b je po izboru supstituiran s jednim ili više supstituenata neovisno odabranih iz skupine koju čine metil, etil, OH, OR4 i F.
4. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time što R2 predstavlja fenil supstituiran s 1 ili 2 supstituenta R2a koji su isti ili različiti, pri čemu R2a predstavlja C1-C5-alkil, OC1-C5-alkil, F ili Cl, pri čemu ako je supstituent ili najmanje jedan od navedenih supstituenata C1-C5-alkil,-OC1-C5-alkil ili Cl, poželjno je postavljen para na ugljikov atom koji povezuje fenil s ostatkom molekule, i pri čemu navedeni C1-C5-alkil i -OC1-C5-alkil neovisno su po izboru supstituirani s 1 do 5 fluorovih atoma.
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time što R6 i R7 predstavljaju H.
6. Spoj prema bilo kojem od patentnih zahtjeva 1, 2, 4 i 5, naznačen time što R1 predstavlja pirazolil, naročito pirazol-4-il, po izboru supstituiran na jednom ili više ugljikovih atoma sa 1 ili 2 supstituenta R1a koji su isti ili različiti, pri čemu R1a predstavlja C1-C5-alkil, C3-C7-cikloalkil, -(C1-C3-alkil)-(C3-C7-cikloalkil), -OC1-C5-alkil, -OC3-C7-cikloalkil, halogen ili CN, i pri čemu je neovisno svaki dušikov atom iz navedenog R1 po izboru supstituiran sa supstituentom R1b, pri čemu R1b predstavlja C1-C5-alkil, -(C1-C3-alkil)-(C3-C7-cikloalkil) ili C3-C7-cikloalkil, i ako R1a predstavlja C1-C5-alkil, C3-C7-cikloalkil, -(C1-C3-alkil)-(C3-C7-cikloalkil), - OC1-C5-alkil ili -OC3-C7-cikloalkil i/ili ako R1b predstavlja C1-C5-alkil, -(C1-C3-alkil)-(C3-C7-cikloalkil) ili C3-C7-cikloalkil, navedeni C1-C5-alkil, C3-C7-cikloalkil, - (C1-C3-alkil)-(C3-C7cikloalkil), -OC1-C5-alkil i -OC3-C7-cikloalkil neovisno su po izboru supstituirani s jednim ili više supstituenata neovisno odabranih iz skupine koju čine metil, OH, OR4 i F; R5 predstavlja H, F, Cl ili metil, naročito H ili F; i R6 i R7 predstavljaju H.
7. Spoj prema bilo kojem od patentnih zahtjeva 1 do 6, naznačen time što R2 predstavlja fenil supstituiran s 1 ili 2 supstituenta R2a koji su isti ili različiti, pri čemu R2a predstavlja C1-C5-alkil, -OC1-C5-alkil, F ili Cl, i pri čemu ako je supstituent ili najmanje jedan od navedenih supstituenata C1-C5-alkil,-OC1-C5-alkil ili Cl, poželjno je postavljen para na ugljikov atom koji povezuje fenil s ostatkom molekule, i pri čemu su navedeni C1-C5-alkil i -OC1-C5-alkil neovisno po izboru supstituirani s 1 do 5 fluorovih atoma; R5 predstavlja H, F, Cl ili metil, naročito H ili F; i R6 i R7 predstavljaju H.
8. Spoj prema bilo kojem od patentnih zahtjeva 1 do 7, naznačen time što R1 predstavlja pirazolil, naročito pirazol-4-il, po izboru supstituiran na jednom ili više ugljikovih atoma sa 1 ili 2 supstituenta R1a koji su isti ili različiti, pri čemu R1a predstavlja C1-C5-alkil, C3-C7-cikloalkil, -(C1-C3-alkil)-(-C3-C7-cikloalkil), -OC1-C5-alkil, -OC3-C7-cikloalkil, halogen ili CN, pri čemu neovisno svaki dušikov atom iz navedenog R1 je po izboru supstituiran sa supstituentom R1b, pri čemu R1b predstavlja C1-C5-alkil, -(C1-C3-alkil)-(C3-C7-cikloalkil) ili C3-C7-cikloalkil, i ako R1a predstavlja C1-C5-alkil, C3-C7-cikloalkil, -(C1-C3-alkil)-(C3-C7-cikloalkil), - OC1-C5-alkil ili -OC3-C7-cikloalkil i/ili ako R1b predstavlja C1-C5-alkil, -(C1-C3-alkil)-(C3-C7-cikloalkil) ili C3-C7-cikloalkil, navedeni C1-C5-alkil, C3-C7-cikloalkil, - (C1-C3-alkil)-(C3-C7-cikloalkil), -OC1-C5-alkil i -OC3-C7-cikloalkil neovisno su po izboru supstituirani s jednim ili više supstituenata neovisno odabranih iz skupine koju čine metil, OH, OR4 i F; R2 predstavlja fenil supstituiran s 1 ili 2 supstituenta R2a koji su isti ili različiti, pri čemu R2a predstavlja C1-C5-alkil, -OC1-C5-alkil, F ili Cl, pri čemu ako je supstituent ili najmanje jedan od navedenih supstituenata C1-C5-alkil,-OC1-C5-alkil ili Cl, poželjno je postavljen para na ugljikov atom koji povezuje fenil s ostatkom molekule, i pri čemu su navedeni C1-C5-alkil i -OC1-C5-alkil neovisno po izboru supstituirani s 1 do 5 fluorovih atoma; R5 predstavlja H, F, Cl ili metil, naročito H ili F; i R6 i R7 predstavljaju H.
9. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8, naznačen time što R1 predstavlja pirazol-4-il, supstituiran na dušikovom atomu na položaju 1 sa supstituentom R1b, pri čemu R1b predstavlja C1-C5-alkil, -(C1-C3-alkil)-(C3-C7-cikloalkil) ili C3-C7-cikloalkil, pri čemu je navedeni R1b po izboru supstituiran s jednim ili više supstituenata neovisno odabranih iz skupine koju čine metil, OH, OR4 i F; R2 predstavlja fenil supstituiran s 1 ili 2 supstituenta R2a koji su isti ili različiti, pri čemu R2a predstavlja metil, trifluorometil, trifluorometoksi, F ili Cl, i pri čemu ako je supstituent ili najmanje jedan od navedenih supstituenata F, poželjno je postavljen orto na atom ugljika koji povezuje fenil s ostatkom molekule, i pri čemu ako je supstituent ili najmanje jedan od navedenih supstituenata metil, trifluorometil, trifluorometoksi ili Cl, poželjno je postavljen para na ugljikov atom koji povezuje fenil s ostatkom molekule; R5 predstavlja H, F, Cl ili metil, naročito H ili F; i R6 i R7 predstavljaju H.
10. Spoj prema bilo kojem od patentnih zahtjeva 1 do 9, naznačen time što R3 predstavlja H; i R5 predstavlja H.
11. Spoj prema bilo kojem patentnom zahtjevu od 1 do 9, naznačen time što R3 predstavlja H; i R5 predstavlja F.
12. Spoj prema bilo kojem patentnom zahtjevu od 1 do 10, naznačen time što R1 predstavlja pirazol-4-il supstituiran na dušikovom atomu na položaju 1 sa supstituentom odabranim iz skupine koju čine metil, etil, propil, propan-2-il, 2-metilpropil, tert-butil, butan-2-il, ciklobutil, 2,2-dimetilpropil, 3-metilbutan-2-il, ciklopentil, cikloheksil, 1-ciklopropilmetil, 1-ciklopropiletil, 1-ciklobutilmetil, 1-(1-metilciklopropil)metil i 2,2,2-trifluoroetil, naročito etil, propan-2-il, 2-metilpropil, butan-2-il, ciklobutil, 2,2-dimetilpropil, 1-ciklopropilmetil, 1-ciklopropiletil, 1-(1-metilciklopropil)metil, i 1-ciklobutilmetil; R2 predstavlja fenil supstituiran s 1 ili 2 supstituenta R2a koji su isti ili različiti, pri čemu R2a predstavlja metil, trifluorometil, trifluorometoksi, F ili Cl, pri čemu ako je supstituent ili najmanje jedan od navedenih supstituenata F, poželjno je postavljen orto na atom ugljika koji povezuje fenil s ostatkom molekule, i pri čemu ako je supstituent ili najmanje jedan od navedenih supstituenata metil, trifluorometil, trifluorometoksi ili Cl, poželjno je postavljen para na ugljikov atom koji povezuje fenil s ostatkom molekule; R3 predstavlja H; R5 predstavlja H ili F, poželjno H; i R6 i R7 predstavljaju H.
13. Spoj prema bilo kojem od patentnih zahtjeva 1 ili 2, naznačen time što R1 predstavlja tiazol-5-il, po izboru supstituiran na ugljikovom atomu na poziciji 2 sa supstituentom R1a izabranim iz skupine koju čine metil, etil, propil, propan-2-il, ciklopropil, 2-metilpropil, tert-butil, butan-2-il, ciklobutil, 2,2-dimetilpropil, 3-metilbutan-2-il, ciklopentil, cikloheksil, 1-ciklopropilmetil, 1-ciklopropiletil, 1-ciklobutilmetil, 1-(1-metilciklopropil)metil i 2,2,2-trifluoroetil, naročito etil, propan-2-il, 2-metilpropil, butan-2-il, ciklobutil, 2,2-dimetilpropil, ciklopentil, 1-ciklopropilmetil, 1-ciklopropiletil, 1-(1-metilciklopropil)metil i 1-ciklobutilmetil; R2 predstavlja fenil supstituiran s 1 ili 2 supstituenta R2a koji su isti ili različiti, pri čemu R2a predstavlja metil, trifluorometil, trifluorometoksi, F ili Cl, i pri čemu ako je supstituent ili najmanje jedan od navedenih supstituenata F, poželjno je postavljen orto na atom ugljika koji povezuje fenil s ostatkom molekule, i pri čemu ako je supstituent ili najmanje jedan od navedenih supstituenata metil, trifluorometil, trifluorometoksi ili Cl, poželjno je postavljen para na ugljikov atom koji povezuje fenil s ostatkom molekule; R5 predstavlja H, F, Cl ili metil, naročito H ili F; i R6 i R7 predstavljaju H.
14. Spoj prema bilo kojem od zahtjeva 1 do 13 naznačen time što je odabran iz skupine koju čine 2-(1-benzotiofen-2-il)-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-[6-(1,1-difluoropropil)piridin-3-il]-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-ciklobutil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(6-etoksipiridin-3-il)-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(6-etoksipiridin-3-il)-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-ciklobutil-1H-pirazol-4-il)-3-fluoro-5-({[1-(2-fluoro-4-metilfenil)ciklopropil]karbonil}amino)benzojeva kiselina; 2-[6-(1,1-difluoropropil)piridin-3-il]-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]-2-[6-(trifluorometil)piridin-3-il]benzojeva kiselina; 5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]-2-[1-(2,2,2-trifluoroetil)-1H-pirazol-4-il]benzojeva kiselina; 5-({[1-(4-klorofenil)ciklopropil]karbonil}amino)-2-(l-ciklobutil-lH-pirazol-4-il)-3-fluorobenzojeva kiselina; 2-(1-ciklobutil-1H-pirazol-4-il)-3-fluoro-5-[({1-[4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-ciklobutil-1H-pirazol-4-il)-3-fluoro-5-[([1-[4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-ciklobutil-1H-pirazol-4-il)-5-({[1-(3,4-difluorofenil)ciklopropil]karbonil}amino)-3-fluorobenzojeva kiselina; 2-(1-ciklobutil-1H-pirazol-4-il)-3-fluoro-5-[({1-[3-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-ciklobutil-1H-pirazol-4-il)-5-({[1-(2,4-difluorofenil)ciklopropil]karbonil}amino)-3-fluorobenzojeva kiselina; 5-({[1-(4-kloro-2-fluorofenil)ciklopropil]karbonil}amino)-2-(1-ciklobutil-1H-pirazol-4-il)-3-fluorobenzojeva kiselina; 2-(1-ciklobutil-1H-pirazol-4-il)-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}cabonil)amino]benzojeva kiselina; 2-(1-ciklobutil-1H-pirazol-4-il)-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-ciklobutil-1H-pirazol-4-il)-3-fluoro-5-([{1-(5-fluoropiridin-2-il)ciklopropil]karbonil}amino)benzojeva kiselina; 2-(1-ciklobutil-3-fluoro-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 5-([{1-(4-kloro-3-fluorofenil)ciklopropil]karbonil}amino)-2-(1-ciklobutil-1H-pirazol-4-il)benzojeva kiselina; 2-(1-ciklobutil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 5-({[1-(4-kloro-2-fluorofenil)ciklopropil]karbonil}amino)-2-(1-ciklobutil-1H-pirazol-4-il)benzojeva kiselina; 5-({[1-(5-kloro-2-fluorofenil)ciklopropil]karbonil}amino)-2-(1-ciklobutil-1H-pirazol-4-il)benzojeva kiselina; 2-(1-etil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-etil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]-2-[1-(propan-2-il)-1H-pirazol-4-il]benzojeva kiselina; 5-[([1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]-2-[1-(propan-2-il)-1H-pirazol-4-il]benzojeva kiselina; 2-(1-tert-butil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-tert-butil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]-2-[1-(2-metilpropil)-1H-pirazol-4-il]benzojeva kiselina; 5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]-2-[1-(2-metilpropil)-1H-pirazol-4-il]benzojeva kiselina; 2-[1-(2,2-dimetilpropil)-1H-pirazol-4-il]-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-[1-(2,2-dimetilpropil)-1H-pirazol-4-il]-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 3-fluoro-5-({[1-(2-fluoro-4-metilfenil)ciklopropil]karbonil}amino)-2-[1-(propan-2-il)-1H-pirazol-4-il]benzojeva kiselina; 3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]-2-[1-(propan-2-il)-1H-pirazol-4-il]benzojeva kiselina; 3-fluoro-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]-2-[1-(propan-2-il)-1H-pirazol-4-il]benzojeva kiselina; 2-(4-tert-butil-1H-imidazol-1-il)-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(4-tert-butil-1H-imidazol-1-il)-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]-2-[1-(2-metilpropil)-1H-pirazol-4-il]benzojeva kiselina; 2-[6-(difluorometil)piridin-3-il]-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-[6-(difluorometil)piridin-3-il]-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-[6-(1,1-difluoropropil)piridin-3-il]-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-[6-(1,1-difluoropropil)piridin-3-il]-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 3-kloro-2-(1-ciklobutil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 3-kloro-2-(1-ciklobutil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 3-kloro-2-[6-(1,1-difluoropropil)piridin-3-il]-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 3-kloro-2-[6-(1,1-difluoropropil)piridin-3-il]-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-ciklobutil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]-3-metilbenzojeva kiselina; 2-(1-ciklobutil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]-3-metilbenzojeva kiselina; 2-[1-(ciklobutilmetil)-1H-pirazol-4-il]-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-[1-(ciklobutilmetil)-1H-pirazol-4-il]-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-ciklopentil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-cikloheksil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-cikloheksil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-[1-(ciklopropilmetil)-1H-pirazol-4-il]-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-[1-(ciklopropilmetil)-1H-pirazol-4-il]-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]-2-(6-metilpiridin-3-il)benzojeva kiselina; 2-{1-[(2S)-butan-2-il]-1H-pirazol-4-il}-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-{1-[(2R)-butan-2-il]-1H-pirazol-4-il}-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-{1-[(2S)-butan-2-il]-1H-pirazol-4-il}-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-{1-[(2R)-butan-2-il]-1H-pirazol-4-il}-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-etil-1H-pirazol-4-il)-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(1-etil-1H-pirazol-4-il)-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 5-({[1-(4-kloro-2-fluorofenil)ciklopropil]karbonil}amino)-3-fluoro-2-[1-(propan-2-il)-1H-pirazol-4-il]benzojeva kiselina; 5-({[1-(4-kloro-2-fluorofenil)ciklopropil]karbonil}amino)-2-(2-ciklobutil-1,3-tiazol-5-il)benzojeva kiselina; 2-(2-ciklobutil-1,3-tiazol-5-il)-5-({[1-(2-fluoro-4-metilfenil)ciklopropil]karbonil}amino)benzojeva kiselina; 2-(2-ciklobutil-1,3-tiazol-5-il)-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(2-ciklobutil-1,3-tiazol-5-il)-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]-2-{1-[(1-metilciklopropil)metil]-1H-pirazol-4-il}benzojeva kiselina; 5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]-2-{1-[(1-metilciklopropil)metil]-1H-pirazol-4-il}benzojeva kiselina; 2-{1-[(1S)-1-ciklopropiletil]-1H-pirazol-4-il}-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(6-etilpiridin-3-il)-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(6-etilpiridin-3-il)-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(6-etilpiridin-3-il)-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 3-fluoro-5-[({1-[2-fluoro-4-(trifluorometoksi)fenil]ciklopropil}karbonil)amino]-2-(1-metil-1H-indazol-6-il)benzojeva kiselina; 2-(2-ciklopentil-1,3-tiazol-5-il)-5-[(fl-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; 2-(2-ciklobutil-1,3-tiazol-5-il)-3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; i 3-fluoro-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]-2-[1-(2,2,2-trifluoroetil)-1H-pirazol-4-il]benzojeva kiselina; ili njihova farmaceutski prihvatljiva sol.
15. Spoj prema bilo kojem od patentnih zahtjeva 1 do 14, naznačen time što je spoj 2-(1-ciklobutil-1H-pirazol-4-il)-5-[({1-[2-fluoro-4-(trifluorometil)fenil]ciklopropil}karbonil)amino]benzojeva kiselina; ili njegova farmaceutski prihvatljiva sol.
16. Farmaceutski pripravak, naznačen time što sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 15, i farmaceutski prihvatljiv razrjeđivač ili nosač.
17. Spoj prema bilo kojem od patentnih zahtjeva 1 do 15, ili farmaceutski pripravak prema patentnom zahtjevu 16 naznačen time što je za upotrebu u liječenju ili profilaksi bolesti ili sindroma bolesti, stanja ili simptoma.
18. Spoj za uporabu prema patentnom zahtjevu 17, naznačen time što su navedena bolest ili sindromi bolesti, stanja, ili simptomi koji su povezani s bolom i/ili upalom.
19. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 17 ili 18, naznačen time što su navedena bolest ili sindromi bolesti, stanja ili simptomi povezani s boli odabrani iz skupine koju čine • visceralna bol npr. vezana za pankreatitis, intersticijski cistitis, bubrežne kolike, ili prostatitis, kroničnu bol u zdjelici, ili bol povezanu s infiltrirajućom endometriozom; • neuropatska bol kao što je postherpetična neuralgija, akutni zoster bol, bol povezan s ozljedom živca, dinije, uključujući vulvodiniju, fantomska bol u udovima, bol povezana s avulzijama korijena, bol povezana s radikulopatijom, bolna traumatska mononeuropatija, bolna neuropatija zbog uklještenja, bol povezana sa sindrom karpalnog tunela, ulnarna neuropatija, bol povezana sa sindromom tarzalnog tunela, bolna dijabetička neuropatija, bolna polineuropatija, trigeminalna neuralgija, ili bol povezana s obiteljskom amiloidnom polineuropatijom; • sindromi središnje boli potencijalno uzrokovani gotovo bilo kojom lezijom na bilo kojoj razini živčanog sustava uključujući, ali ne ograničavajući se na bol povezanu s moždanim udarom, multiplom sklerozom, i ozljedom leđne moždine; • post kirurški sindromi boli (uključujući sindrom boli nakon mastektomije, sindrom boli nakon posttorakotomije, bol u batrljku), bol u kostima i zglobovima (osteoartritis), bol u kralježnici (uključujući akutnu i kroničnu križobolju, bol u vratu, bol povezanu sa spinalnom stenozom), bol u ramenu, bol pri ponavljajućim pokretima, zubobolju, bol povezanu s upalom grla, bol od raka, bol od opeklina uključujući bol od opekotina od sunca, miofascijalnu bol (bol povezana s ozljedom mišića, fibromijalgija), postoperativna i perioperativna bol (uključujući, ali ne ograničavajući se na opću kirurgiju, ortopediju, i ginekološku kirurgiju); i • akutna i kronična bol, kronična bol u zdjelici, bol povezana s endometriozom, bol povezana s dismenorejom (primarna i sekundarna), bol povezana s fibroidima maternice, bol povezana s vulvodinijom, kao i bol povezana s anginom, ili upalna bol različitog porijekla (uključujući ali nije ograničeno na bol povezanu s osteoartritisom, reumatoidnim artritisom, reumatskom bolešću, tenosinovitisom, gihtom, ankilozirajućim spondilitisom i burzitisom).
20. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 17 do 19, naznačen time što su navedeni sindromi bolesti ili bolesti, stanja, ili simptomi odabrani između ili vezani za bilo koju skupinu koju čine • ginekološki poremećaji i/ili bolesti, ili učinci i/ili simptomi koji negativno utječu na zdravlje žena uključujući endometriozu, miome maternice, preeklampsiju, nedostatak hormona, grčeve maternice, ili obilna menstrualna krvarenja; • bol respiratornog ili ekskrecijskog sustava uključujući bilo koji od upalnih hiperreaktivnih dišnih puteva, upalne događaje povezane s bolešću dišnih puteva poput kronične opstruktivne plućne bolesti, astme uključujući alergijsku astmu (atopijsku ili neatopijsku) kao i bronhokonstrikciju uzrokovanu vježbanjem, profesionalnu astmu, virusno ili bakterijsko pogoršanje astme, druge nealergijske astme i sindrom piskanja kod dojenčadi, astmu pogoršanje astme, druge nealergijske astme i sindrom piskanja kod dojenčadi, kroničnu opstruktivnu plućnu bolest uključujući emfizem, sindrom respiratornog distresa kod odraslih, bronhitis, upalu pluća, kašalj, ozljedu pluća, fibrozu pluća, alergijski rinitis (sezonski i višegodišnji), vazomotorni rinitis, angioedem (uključujući nasljedni angioedem i angioedem izazvan lijekovima uključujući onaj uzrokovan enzimom koji konvertira angiotenzin (ACE) ili ACE/ inhibitorima neutralne endopeptidaze kao što je omepatrilat), pneumokonioza, uključujući aluminozu, antrakozu, azbestozu, halikozu, ptilozu, siderozu, silikozu, tabakozu i bisinozu, bolest crijeva uključujući Crohnovu bolest i ulcerozni kolitis, sindrom iritabilnog crijeva, pankreatitis, nefritis, cistitis (intersticijski cistitis), fibrozu bubrega, zatajenje bubrega, hiperaktivni mokraćni mjehur, te prekomjerno aktivan mokraćni mjehur; • dermatološka bol uključujući pruritus, svrbež, upalne poremećaje kože uključujući psorijazu, ekcem, i atopijski dermatitis; • oštećenje zglobova ili kostiju uključujući reumatoidni artritis, giht, osteoporozu, osteoartritis, i ankilozantni spondilitis; • zahvaćenost središnjeg i perifernog živčanog sustava uključujući neurodegenerativne bolesti uključujući Parkinsonovu i Alzheimerovu bolest, amiotrofičnu lateralnu sklerozu (ALS), epilepsiju, demenciju, glavobolju uključujući cluster glavobolju, migrenu uključujući profilaktičku i akutnu upotrebu, moždani udar, zatvorenu traumu glave, te multiplu sklerozu; • infekcija uključujući HIV infekciju, i tuberkulozu; • traume povezane s edemom uključujući cerebralni edem, opekline, opekline od sunca, uganuća ili prijelom; • trovanja uključujući aluminozu, antrakozu, azbestozu, halikozu, ptilozu, siderozu, silikozu, tabakozu, i bisinozni uveitis; • klaster dijabetes ili metabolizam kao dijabetes tipa 1, dijabetes tipa 2, dijabetičke vaskulopatije, dijabetička neuropatija, dijabetička retinopatija, postkapilarna rezistencija ili dijabetički simptomi povezanih s inzulitisom (npr. hiperglikemija, diureza, proteinurija i povećano izlučivanje nitrita i kalikreina u mokraći), dijabetički makularni edem, metabolički sindrom, inzulinska rezistencija, pretilost, metabolizam masti ili mišića; • kaheksija povezana s ili izazvana bilo kojim od karcinoma, AIDS-om, celijakijom, kroničnom opstruktivnom plućnom bolesti, multiplom sklerozom, reumatoidnim artritisom, kongestivnim zatajenjem srca, tuberkulozom, obiteljskom amiloidnom polineuropatijom, trovanjem živom (akrodinija), i nedostatkom hormona; • kardiovaskularni sustav uključujući kongestivno zatajenje srca, aterosklerozu, kongestivno zatajenje srca, infarkt miokarda, i fibrozu srca; i • druga stanja uključujući septički šok, sepsu, atrofiju mišića, grčeve gastrointestinalnog trakta, benignu hiperplaziju prostate, te bolesti jetre kao što su nealkoholna i alkoholna bolest masne jetre, nealkoholni i alkoholni steatohepatitis, fibroza jetre, ili ciroza jetre.
21. Spoj za uporabu prema patentnom zahtjevu 20, naznačen time što su navedeni sindromi bolesti ili bolesti, stanja, ili simptomi povezani s endometriozom ili bolom povezanim s endometriozom, naročito s dismenorejom, dispareunijom, disurijom, ili dishezijom.
22. Spoj za uporabu prema patentnom zahtjevu 20, naznačen time što su navedeni sindromi bolesti ili bolesti, stanja, ili simptomi odabrani između ili koji se odnose na prekomjerno aktivan mokraćni mjehur, fibrozu pluća, bubrega, srca i/ili jetre, dijabetes tipa 1 i/ili tipa 2, metabolički sindrom, giht, reumatoidni artritis, i osteoartritis uključujući povezane simptome.
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