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HRP20220990T1 - 3-supstituirane propionske kiseline kao inhibitori alfa v integrina - Google Patents

3-supstituirane propionske kiseline kao inhibitori alfa v integrina Download PDF

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HRP20220990T1
HRP20220990T1 HRP20220990TT HRP20220990T HRP20220990T1 HR P20220990 T1 HRP20220990 T1 HR P20220990T1 HR P20220990T T HRP20220990T T HR P20220990TT HR P20220990 T HRP20220990 T HR P20220990T HR P20220990 T1 HRP20220990 T1 HR P20220990T1
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tetrahydro
naphthyridin
propanoic acid
propyl
pyrazol
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HRP20220990TT
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Guohua Zhao
Pratik Devasthale
Xiang-Yang Ye
Kumaravel Selvakumar
Suresh Dhanusu
Palanikumar BALASUBRAMANIAN
Leatte R. GUERNON
Rita Civiello
Xiaojun Han
Michael F. Parker
Swanee E. Jacutin-Porte
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Bristol-Myers Squibb Company
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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Claims (8)

1. Spoj formule: [image] [image] [image] pri čemu: X je C1-6 alkilen supstituiran sa 0, 1, ili 2 R7b; R1 je segment mimetika arginina odabran iz grupe koja se sastoji od [image] [image] [image] [image] [image] [image] [image] R2 je vodik ili C1-6 alkil; R3 je odabran iz grupe koja se sastoji iz vodika, [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] ili R2 i R3 uzeti zajedno sa atomom za koji su vezani formiraju karbociklil ili heterociklil, pri čemu je svaki od karbociklila i heterociklila nezavisno supstituiran sa 0, 1, 2, ili 3 R12; R4 je vodik; R5 je H ili R5a; a R5a je metil, etil, izopropil, n-butil, izopentil, ili strukturni segment odabran od [image] [image] [image] R7b je svaki nezavisno halo, cijano, hidroksil, amino, C1-6 alkil, haloalkil, hidroksialkil, aminoalkil, alkoksi, haloalkoksi, amido, karbamat, ili sulfonamid; R12, je nezavisno halo, cijano, nitro, OH, amino, C1-6 alkil, alkoksi, aminoalkil, haloalkil, haloalkoksi, haloaminoalkil, karbociklil sa 3 do 6 članova, ili heterociklil sa 3 do 6 članova, 6- do 10-člani aril, ili 5- do 10-člani heteroaril; pri čemu su aril i heteroaril, sami po sebi ili kao dio druge grupe, svaki nezavisno supstituirani sa jednom ili više grupa nezavisno odabranih od halo, cijano, hidroksil, amino, C1-6 alkil, haloalkil, hidroksialkil, aminoalkil, alkoksi, haloalkoksi, amido, karbamat, i sulfonamida; i karbociklil i heterociklil, sami po sebi ili kao dio druge grupe, su svaki nezavisno supstituirani sa jednom ili više grupa nezavisno odabranih od halo, cijano, hidroksil, amino, okso, C1-6 alkil, haloalkil, hidroksialkil, aminoalkil, alkoksi, haloalkoksi, amido, karbamat, ili sulfonamid; ili farmaceutski prihvatljiva sol istog.
2. Spoj prema patentnom zahtjevu 1 odabrano iz grupe koja se sastoji od (±)-3-(6-Metoksipiridin-3-il)-3-(3-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)buti1)-1H-pirazol-1-il)propanske kiseline; (±)-3-(6-Metoksipiridin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(6-Metoksipiridin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (R)-3-(6-Metoksipiridin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(6-Metoksipiridin-3-il)-3-(1-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propi1)-1H-pirazol-4-il)propanske kiseline; (S)-3-(6-Metoksipiridin-3-il)-3-(1-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-4-il)propanske kiseline; (R)-3-(6-Metoksipiridin-3-il)-3-(1-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-4-il)propanske kiseline; (±)-3-(6-Metoksipiridin-3-il)-3-(1-(4-(5,6,7,8-tetrahidro-l,8-naftiridin-2-il)butil)-1H-pirazol-4-il)propanske kiseline; (S)-3-(6-Hidroksipiridm-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(6-Metoksipiridm-3-il)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (R)-3-(6-Metoksipiridin-3-il)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (S)-3-(6-Metoksipiridin-3-il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R)-3-(6-Metoksipiridin-3-il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S)-3-(6-Metoksipiridin-3-il)-3-(5-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (R)-3-(6-Metoksipiridin-3-il)-3-(5-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (S)-3-(6-Metoksipiridin-3-il)-3-(5-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R)-3-(6-Metoksipiridin-3-il)-3-(5-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (±)-3-(2-Metilpirimidin-5-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(3-Fluoro-4-metoksifenil)-3-(l-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-4-il)propanske kiseline; (±)-3-(3,5-Dihlorofenil)-3-(1-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-4-il)propanske kiseline; (±)-3-(2-Etoksipirimidin-5-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(Hinoksalin-2-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(Hinolin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(2,3-Dihidrobenzofuran-5-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(3-(3,5-Dimetil-1H-pirazol-1-il)fenil)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(3-Morfolinofenil)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(Pirido[2,3-b]pirazin-7-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(2-Metoksipirimidin-5-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(2,3-Dihidro-[1,4]dioksino[2,3-b]piridin-7-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(3-Fluoro-4-metoksifenil)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (R)-3-(3-Fluoro-4-metoksifenil)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (S)-3-(3-Fluoro-4-metoksifenil)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R)-3-(3-Fluoro-4-metoksifenil)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S)-(3-Fluoro-4-metoksifenil)-3-(5-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (R)-(3-Fluoro-4-metoksifenil)-3-(5-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (S)-3-(3-Fluoro-4-metoksifenil)-3-(5-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R)-3-(3-Fluoro-4-metoksifenil)-3-(5-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; 3-(3-fluoro-4-metoksifenil)-3-(1-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)-1H-pirazol-4-il)propanske kiseline; (S)-3-(1-Metil-6-okso-1,6-dihidropiridin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; Etil (S)-3-(6-metoksipiridin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanoata; (±)-3-(3-Fluoro-4-metoksifenil)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(2-(Azetidin-1-il)pirimidin-5-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(2,3-Dihidro-[1,4]dioksino[2,3-b]piridin-7-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (R)-3-(2,3-Dihidro-[1,4]dioksino[2,3-b]piridin-7-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propi1)-1H-pirazol-1-il)propanske kiseline; (±)-3-(2-(Azetidin-1-il)pirimidin-5-il)-3-(5-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(2-Metilpirimidin-5-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (R)-3-(2-Metilpirimidin-5-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(2-Etoksipirimidin-5-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(6-Metoksipiridazin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(6-Metoksipiridazin-3-il)-3-(5-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(5-Metoksipirazin-2-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(5-Metoksipirazin-2-il)-3-(5-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(6-Metoksipiridin-3-il)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(6-Metoksipiridm-3-il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridm-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±3)-(5-metoksipiridin-3-il)-3-(5-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(5-metoksipiridin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (R)-3-(5-metoksipiridin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-[5-(pirolidin-1-il)piridin-3-il]-3-{3-[3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil]-1H-pirazol-1-il}propanske kiseline; (S)-3-[5-(morfol-4-il)piridm-3-il]-3-{3-[3-(5,6,7,8-teirahidro-1,8-naftiridm-2-il)propil]-1H-pirazol-1-il}propanske kiseline; (R)-3-[5-(morfolin-4-il)piridin-3-il]-3-{3-[3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil]-1H-pirazol-1-il}propanske kiseline; (S)-3-(5-metilpiridin-3-il)-3-{3-[3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil]-1H-pirazol-1-il}propanske kiseline; (R)-3-(5-metilpiridin-3-il)-3-{3-[3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil]-1H-pirazol-1-il}propanske kiseline; (±)-3-[5-(dimetilkarbamoil)piridin-3-il]-3-{3-[3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil]-1H-pirazol-1-il}propanske kiseline; (±)-4-{[4-(2-karboksi-1-{3-[3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil]-1H-pirazol-1-il}etil)piridin-2-il]amino}butanske kiseline; 3-(5-(2-metoksietoksi)piridin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (R)-3-(2-etoksipirimidin-5-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(2-metoksipirimidin-5il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (R)-3-(2-metoksipirimidin-5-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; 3-(pirimidin-5-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(2-hidroksipirimidin-5-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(2-metilpirimidin-5-il)-3-(3-(3-((S)-1,2,3,4-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; 3-(2-metilpirimidin-5-il)-3-(5-(3-((S)-1,2,3,4-tetrahidro-1,8-naftiridm-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(2-metilpirimidin-5-il)-3-(3-(3-((R)-1,2,3,4-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(2-metoksipirimidin-5-il)-3-(3-(3-((S)-1,2,3,4-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(2-metoksipirimidin-5-il)-3-(3-(3-((R)-1,2,3,4-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(2-metilpirimidin-5-il)-3-(3-(3-(6,7,8,9-tetrahidro-5H-pirido[2,3-b]azepin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(2-metilpirimidin-5-il)-3-(3-(3-(6,7,8,9-tetrahidro-5H-pirido[2,3-b]azepin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (R)-3-(2-metilpirimidin-5-il)-3-(3-(3-(6,7,8,9-tetrahidro-5H-pirido[2,3-b]azepin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(6-metoksipiridin-3-il)-3-(3-(3-(6,7,8,9-tetrahidro-5H-pirido[2,3-b]azepin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(6-metoksipiridin-3-il)-3-(3-(3-(6,7,8,9-tetrahidro-5H-pirido[2,3-b]azepin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (R)-3-(6-metoksipiridin-3-il)-3-(3-(3-(6,7,8,9-tetrahidro-5H-pirido[2,3-b]azepin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (±)-3-(2-metoksipirimidin-5-il)-3-(3-(3-(6,7,8,9-tetrahidro-5H-pirido[2,3-b]azepin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(2-metoksipirimidin-5-il)-3-(3-(3-(6,7,8,9-tetrahidro-5H-pirido[2,3-b]azepin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (R)-3-(2-metoksipirimidin-5-il)-3-(3-(3-(6,7,8,9-tetrahidro-5H-pirido[2,3-b]azepin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(1-benzil-6-okso-1,6-dihidropiridin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; (S)-3-(6-(Benziloksi)piridin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanoat; (S)-3-(1-(ciklopropilmetil)-6-okso-1,6-dihidropiridin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propi1)-1H-pirazol-1-il)propanske kiseline; (S)-3-(6-(ciklopropilmetoksi)piridin-3-il)-3-(3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-1-il)propanske kiseline; 3-(6-metoksipiridin-3-il)-3-(1-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)-1H-pirazol-3-il)propanske kiseline; (S)-3-(3-(dimetilkarbamoil)fenil)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (R)-3-(3-(dimetilkarbamoil)fenil)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (S)-3-(hinoksalin-6-il)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (R)-3-(hinoksalin-6-il)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (S)-3-(6-(dimetilamino)piridin-3-il)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (R)-3-(6-(dimetilamino)piridin-3-il)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (S)-3-(3,4-dimetoksifenil)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (R)-3-(3,4-dimetoksifenil)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (S)-3-(3-morfolinofenil)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (R)-3-(3-morfolinofenil)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (S)-3-(4-(dimetilkarbamoil)fenil)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (R)-3-(4-(dimetilkarbamoil)fenil)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (S)-3-(2-etoksipirimidin-5-il)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (R)-3-(2-etoksipirimidin-5-il)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (S)-3-(4-(dimetilkarbamoil)-3-fluorofenil)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (R)-3-(4-(dimetilkarbamoil)-3-fluorofenil)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (S)-3-(6-(dimetilamino)piridin-3-il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R)-3-(6-(dimetilamino)piridin-3-il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S)-3-(4-(dimetilkarbamoil)-3-fluorofenil)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R)-3-(4-(dimetilkarbamoil)-3-fluorofenil)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S)-3-(4-(dimetilkarbamoil)fenil)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R)-3-(4-(dimetilkarbamoil)fenil)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S)-3-(3-(dimetilkarbamoil)fenil)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R)-3-(3-(dimetilkarbamoil)fenil)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S)-3-(3,4-dimetoksifenil)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R)-3-(3,4-dimetoksifenil)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S)-3-(2-Metoksipirimidin-5-il)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (R)-3-(2-Metoksipirimidin-5-il)-3-(4-(4-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)butil)tiazol-2-il)propanske kiseline; (S)-3-(2-metoksipirimidin-5il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R)-3-(2-metoksipirimidin-5-il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (±)-3-(2-metilpirimidin-5-il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S)-3-(2-metilpirimidin-5-il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R)-3-(2-metilpirimidin-5-il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S)-3-(5-metilpiridin-3-il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R)-3-(5-metilpiridin-3-il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S)-3-(3-fluoro-4-metoksifenil)-3-(2-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-4-il)propanske kiseline; (R)-3-(3-fluoro-4-metoksifenil)-3-(2-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-4-il)propanske kiseline; (S,S)-3-(6-metoksipiridin-3-il)-3-(4-(3-(1,2,3,4-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S,R)-3-(6-metoksipiridin-3-il)-3-(4-(3-(1,2,3,4-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R,S)-3-(6-metoksipiridin-3-il)-3-(4-(3-(1,2,3,4-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R,R)-3-(6-metoksipiridin-3-il)-3-(4-(3-(1,2,3,4-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S,S)-3-(6-metoksipiridin-3-il)-3-(4-(3-(1,2,3,4-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S,R)-3-(6-metoksipiridin-3-il)-3-(4-(3-(1,2,3,4-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R,S)-3-(6-metoksipiridin-3-il)-3-(4-(3-(1,2,3,4-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (R,R)-3-(6-metoksipiridin-3-il)-3-(4-(3-(1,2,3,4-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; (S)-3-(3,5-dimetil-1H-pirazol-1-il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; i (R)-3-(3,5-dimetil-1H-pirazol-1-il)-3-(4-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)tiazol-2-il)propanske kiseline; ili farmaceutski prihvatljiva sol istog.
3. Farmaceutska kompozicija koja sadrži spoj prema patentnom zahtjevu 1, ili farmaceutski prihvatljivu sol istog, i nosač.
4. Spoj prema bilo kojem od patentnih zahtjeva 1 do 2, ili farmaceutski prihvatljiva sol istog, za primjenu u terapiji.
5. Spoj prema patentnom zahtjevu 1, ili farmaceutski prihvatljiva sol istog za primjenu u liječenju bolesti, poremećaja ili stanja odabranih od patološke fibroze, odbacivanja transplantata, karcinoma, osteoporoze ili inflamatornih poremećaja kod pacijenta kojem je to potrebno.
6. Spoj ili farmaceutski prihvatljiva sol istog za primjenu prema patentnom zahtjevu 5, pri čemu patološka fibroza je fibroza pluća, jetre, bubrežna, srčana, dernalna, okularna ili fibroza gušterače.
7. Spoj ili farmaceutski prihvatljiva sol istog za primjenu prema patentnom zahtjevu 5, pri čemu bolest, poremećaj, ili stanje je idiopatska plućna fibroza (IPF), nealkoholni steatohepatitis (NASH), kronična bolest bubrega, dijabetesna bolest bubrega i sistemska skleroza.
8. Spoj ili farmaceutski prihvatljiva sol istog za primjenu prema patentnom zahtjevu 5, pri čemu karcinom je karcinom mjehura, krvi, kostiju, mozga, dojke, centralnog nervnog sustava, grlića materice, debelog crijeva, endometrija, jednjaka, žučne vrećice, genitalija, genitourinarnog trakta, glave, bubrega, grkljana, jetre, pluća, mišićnog tkiva, vrata, oralne ili nazalne sluzokože, jajnika, gušterače, prostate, kože, slezene, tankog crijeva, debelog crijeva, želuca, testisa ili štitne žlijezde.
HRP20220990TT 2016-11-08 2017-11-07 3-supstituirane propionske kiseline kao inhibitori alfa v integrina HRP20220990T1 (hr)

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