HRP20161545T1 - Supstituirani derivati 3-heteroaroilamino-propionske kiseline i njihova upotreba kao lijekova - Google Patents

Supstituirani derivati 3-heteroaroilamino-propionske kiseline i njihova upotreba kao lijekova Download PDF

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HRP20161545T1
HRP20161545T1 HRP20161545TT HRP20161545T HRP20161545T1 HR P20161545 T1 HRP20161545 T1 HR P20161545T1 HR P20161545T T HRP20161545T T HR P20161545TT HR P20161545 T HRP20161545 T HR P20161545T HR P20161545 T1 HRP20161545 T1 HR P20161545T1
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phenyl
methoxy
carbonyl
amino
pyridine
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HRP20161545TT
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Sven Ruf
Thorsten Sadowski
Klaus Wirth
Herman Schreuder
Christian Buning
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Sanofi
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Claims (12)

1. Spoj s formulom I, u bilo kojem od njegovih stereoizomernih oblika ili smjesa stereoizomernih oblika u bilo kojem omjeru, ili njegova fiziološki prihvatljiva sol, ili fiziološki prihvatljiv solvat bilo kojeg od njih, [image] naznačen time da A je odabran iz niza koji sadrži C(R1) i N; D je odabran iz niza koji sadrži C(R2) i N; E je odabran iz niza koji sadrži C(R3); L je odabran iz niza koji sadrži C(R4) i N; gdje barem jedan i najviše dva od A, D ili L je N; G je odabran iz niza koji sadrži R71-O-C(O)-, R72-N(R73)-C(O)- i tetrazol-5-il; R1 je odabran iz niza koji sadrži vodik, halogen, (C1-C6)-alkil, HO-, (C1-C6)-alkil-O-, (C1-C6)-alkil-S(O)m- i NC-; R2 je odabran iz niza koji sadrži vodik, halogen, (C1-C7)-alkil, (C1-C6)-alkil-O-, (C1-C6)-alkil-CO-, (C1-C6)-alkil-CO-HN-, -NR12R13, Het2, (C3-C7)-cikloalkil-CsH2s- i Ar-CsH2s-, pri čemu s je cijeli broj izabran iz niza koji sadrži 0, 1, 2 i 3; R3 je R11-O-; R4 je odabran iz niza koji sadrži vodik, halogen, (C1-C6)-alkil, (C1-C6)-alkil-O-, HO-, NR12R13, Het2; R10 je odabran iz niza koji sadrži vodik, halogen, (C1-C6)-alkil, (C1-C6)-alkil-O-, (C1-C6)-alkil-S(O)m-, HO-, -NR12R13, Het2, fenil-CsH2s-(O)t-, pri čemu s je cijeli broj izabran iz niza koji sadrži 0, 1, 2 i 3, te pri čemu t je cijeli broj izabran iz niza koji sadrži 0 i 1; uz uvjet da jedan od R1, R2, R3, R4 ili R10 je ciklički supstituent; R11 je odabran iz niza koji sadrži vodik i (C1-C10)-alkil; R12 i R13 su međusobno neovisno izabrani iz niza koji sadrži vodik i R15; R15 je (C1-C6)-alkil koji je proizvoljno supstituiran s jednim ili više istih ili različitih supstituenata odabranih iz niza koji čine halogen, HO- i (C1-C6)-alkil-O-; R30 je odabran iz niza koji sadrži R31, (C3-C7)-cikloalkil, R32-CuH2u- i Het3-CuH2u-, pri čemu u je cijeli broj izabran iz niza koji sadrži 0, 1, 2 i 3; R31 je (C1-C10)-alkil koji je proizvoljno supstituiran s jednim ili više jednakih ili različitih supstituenta odabranih iz niza koji čine halogen, (C3-C7)-cikloalkil, HO-, (C1-C6)-alkil-O-, (C1-C6)-alkil-S(O)m- i NC-; R32 je odabran iz niza koji sadrži fenil i aromatski 5-člani ili 6-člani monociklički heterocikl koji sadrži jedan, dva ili tri jednaka ili različita heteroatoma u prstenu odabrana iz niza koji sadrži dušik, kisik i sumpor i vezan je preko atoma ugljika u prstenu, pri čemu su fenil i heterocikl svi proizvoljno supstituirani s jednim ili više jednakih ili različitih supstituenta odabranih iz niza koji čine halogen, (C1-C6)-alkil, (C3-C7)-cikloalkil, R33, HO-, (C1-C6)-alkil-O-, R33-O-, R33-(C1-C4)-alkil-O-, -O-CH2-O-, -O-CF2-O-, (C1-C6)-alkil-S(O)m-, H2N-S(O)2-, (C1-C4)-alkil-NH-S(O)2-, di((C1-C4)-alkil)N-S(O)2-, H2N-, (C1-C6)-alkil-NH-, di((C1-C6)-alkil)N-, Het1, (C1-C4)-alkil-C(O)-NH-, Ar-C(O)-NH-, (C1-C4)-alkil-S(O)2-NH- i NC-; R33 je odabran iz niza koji sadrži fenil i aromatski 5-člani ili 6-člani monociklički heterocikl koji sadrži jedan, dva ili tri jednaka ili različita heteroatoma u prstenu odabrana iz niza koji sadrži dušik, kisik i sumpor i vezan je preko atoma ugljika u prstenu, pri čemu su fenil i heterocikl svi proizvoljno supstituirani s jednim ili više jednakih ili različitih supstituenta odabranih iz niza koji čine halogen, (C1-C6)-alkil, (C3-C7)-cikloalkil, HO-, (C1-C6)-alkil-O-, (C1-C6)-alkil-S(O)m-, H2N-S(O)2-, (C1-C4)-alkil-NH-S(O)2-, di((C1-C4)-alkil)N-S(O)2- i NC-; R40 je odabran iz niza koji sadrži vodik i (C1-C4)-alkil; ili R30 i R40 zajedno su (CH2)x koji je proizvoljno supstituiran s jednim ili više istih ili različitih (C1-C4)-alkil supstituenata, pri čemu x je cijeli broj izabran iz niza koji sadrži 2, 3, 4 i 5; R50 je vodik; R60 je vodik; R71 je odabran iz niza koji sadrži vodik i (C1-C8)-alkil koji je proizvoljno supstituiran s jednim ili više istih ili različitih supstituenata odabranih iz niza koji čine (C1-C6)-alkil-O- i (C1-C6)-alkil-C(O)-O-; R72 i R73 su međusobno neovisno izabrani iz niza koji sadrži vodik i (C1-C2)-alkil -; Ar, neovisno jedna od druge skupine Ar, je odabrana iz niza koji sadrži fenil i aromatski 6-člani monociklički heterocikl koji sadrži jedan, dva ili tri jednaka ili različita heteroatoma u prstenu odabrana iz niza koji sadrži dušik, kisik i sumpor i vezana je preko atoma ugljika u prstenu, pri čemu su fenil i heterocikl svi proizvoljno supstituirani s jednim ili više jednakih ili različitih supstituenta odabranih iz niza koji čine halogen, (C1-C6)-alkil, HO-(C1-C6)-alkil, Het4, -(CH2)x-fenil, (C1-C6)-alkil-O-, (C3-C7)-cikloalkil-(CH2)x-O-, -CF3, -CO-(C1-C6)-alkil, -NR12R13, Het2, -CO-NR12R13, CO-Het2, (C1-C6)-alkil-S(O)m-, H2N-S(O)2- i NC-; i pri čemu fenil može biti supstituiran s -CH=CH-CH=CH-, -O-CH2-O-, -O-CH2-CH2-O-, -O-CF2-O- ili -N((C1-C3)-alkil)-CH=CH-; Het1, neovisno jedna od druge skupine Het1, je zasićeni ili nezasićeni 4-člani do 8-člani monociklički heterocikl koji sadrži dušikov atom prstena preko kojeg je Het1 vezan i proizvoljno jedan ili dva ista ili različita dodatna heteroatoma u prstenu odabrana iz niza koji čine dušik, kisik i sumpor, koji je proizvoljno supstituiran s jednim ili više jednakih ili različitih supstituenta odabranih iz niza koji čine halogen, (C1-C4)-alkil, HO-, (C1-C4)-alkil-O-, okso i NC-; Het2 je zasićeni 4-člani do 7-člani monociklički heterocikl koji sadrži dušikov atom prstena preko kojeg je Het2 vezan i proizvoljno jedan dodatni heteroatom u prstenu odabran iz niza koji čine dušik, kisik i sumpor, koji je proizvoljno supstituiran s jednim ili više jednakih ili različitih supstituenta odabranih iz niza koji čine halogen, (C1-C4)-alkil, HO- i (C1-C4)-alkil-O-; Het3, neovisno jedna od druge skupine Het3, je zasićeni 4-člani do 7-člani monociklički heterocikl koji sadrži jedan ili dva ista ili različita heteroatoma u prstenu odabrana iz niza koji čine dušik, kisik i sumpor i vezan je preko atoma ugljika u prstenu, koji je proizvoljno supstituiran s jednim ili više jednakih ili različitih supstituenta odabranih iz niza koji čine fluor, (C1-C4)-alkil i okso; m, međusobno neovisno je broj m, koji je cijeli broj izabran iz niza koji sadrži 0, 1 i 2; pri čemu sve cikloalkilne skupine, međusobno neovisno, su proizvoljno supstituirane s jednim ili više jednakih ili različitih supstituenta odabranih iz niza koji čine fluor i (C1-C4)-alkil; pri čemu sve skupine alkil, CsH2s, CuH2u i (CH2)x, međusobno neovisno, i neovisno od bilo kojih drugih supstituenata, su proizvoljno supstituirane s jednim ili više fluorovih supstituenata.
2. Spoj s formulom I, u bilo kojem od njegovih stereoizomernih oblika ili smjesa stereoizomernih oblika u bilo kojem omjeru, ili njegova fiziološki prihvatljiva sol, ili fiziološki prihvatljiv solvat bilo kojeg od njih, kako je zatraženo u zahtjevu 1, naznačen time da G je odabran iz niza koji sadrži R71-O-C(O)- i R72-N(R73)-C(O)-; R30 je R32-CuH2u-, pri čemu u je cijeli broj izabran iz niza koji sadrži 0 i 1; R32 je odabran iz niza koji sadrži fenil i aromatski 6-člani monociklički heterocikl koji sadrži jedan ili dva dušikova atoma kao heteroatome prstena, pri čemu su fenil i heterocikl svi proizvoljno supstituirani s jednim ili više jednakih ili različitih supstituenta odabranih iz niza koji čine halogen, (C1-C6)-alkil, (C3-C7)-cikloalkil, R33, HO-, (C1-C6)-alkil-O-, R33-O-, R33-(C1-C4)-alkil-O-, -O-CH2-O-, -O-CF2-O-, (C1-C6)-alkil-S(O)m-, di((C1-C4)-alkil)N-S(O)2-, H2N-, di((C1-C6)-alkil)N-, Het1, (C1-C4)-alkil-C(O)-NH-, Ar-C(O)-NH- i NC-; R33 je odabran iz niza koji sadrži fenil i aromatski 6-člani monociklički heterocikl koji sadrži jedan ili dva dušikova atoma kao heteroatome prstena, pri čemu su fenil i heterocikl svi proizvoljno supstituirani s jednim ili više jednakih ili različitih supstituenta odabranih iz niza koji čine halogen, (C1-C6)-alkil, (C3-C7)-cikloalkil, HO-, (C1-C6)-alkil-O-, (C1-C6)-alkil-S(O)m-, H2N-S(O)2-, di((C1-C4)-alkil)N-S(O)2- i NC-; R40 je vodik.
3. Spoj s formulom I, u bilo kojem od njegovih stereoizomernih oblika ili smjesa stereoizomernih oblika u bilo kojem omjeru, ili njegova fiziološki prihvatljiva sol, ili fiziološki prihvatljiv solvat bilo kojeg od njih, prema bilo kojem ili više od zahtjeva 1 i 2, naznačen time da G je R71-O-C(O)-; R30 je R32 -CuH2u-, pri čemu u je 0; R32 je odabran iz niza koji sadrži fenil, pri čemu je fenil proizvoljno supstituiran s jednim ili više jednakih ili različitih supstituenta odabranih iz niza koji čine halogen, (C1-C6)-alkil, (C3-C7)-cikloalkil, R33, HO-, (C1-C6)-alkil-O-, R33-O-, R33-(C1-C4)-alkil-O-, -O-CH2-O-, -O-CF2-O-, (C1-C6)-alkil-S(O)m-, di((C1-C4)-alkil)N-S(O)2-, H2N-, di((C1-C6)-alkil)N-, Het1, (C1-C4)-alkil-C(O)-NH-, Ar-C(O)-NH-i NC-; R33 je odabran iz niza koji sadrži fenil, pri čemu je fenil proizvoljno supstituiran s jednim ili više jednakih ili različitih supstituenta odabranih iz niza koji čine halogen, (C1-C6)-alkil, (C3-C7)-cikloalkil, HO-, (C1-C6)-alkil-O-, (C1-C6)-alkil-S(O)m-, H2N-S(O)2-, di((C1-C4)-alkil)N-S(O)2- i NC-; R40 je vodik.
4. Spoj s formulom I, u bilo kojem od njegovih stereoizomernih oblika ili smjesa stereoizomernih oblika u bilo kojem omjeru, ili njegova fiziološki prihvatljiva sol, ili fiziološki prihvatljiv solvat bilo kojeg od njih, prema bilo kojem ili više od zahtjeva 1 do 3, naznačen time da formula I je odabrana iz niza podformula I-1, I-2, I-4 i I-6 [image] [image] [image]
5. Spoj s formulom I-1, u bilo kojem od njegovih stereoizomernih oblika ili smjesa stereoizomernih oblika u bilo kojem omjeru, ili njegova fiziološki prihvatljiva sol, ili fiziološki prihvatljiv solvat bilo kojeg od njih, kako je zatraženo u zahtjevu 4, naznačen time da [image] R2 je Ar-CsH2s-, pri čemu s je cijeli broj izabran iz niza koji sadrži 0; R3 je odabran iz niza koji sadrži vodik, halogen, R11-O-, HO-, (C1-C6)-alkil i (C1-C6)-alkil-O-; poželjno HO- i (C1-C6)-alkil R4 je vodik; R10 je vodik.
6. Spoj s formulom I, u bilo kojem od njegovih stereoizomernih oblika ili smjesa stereoizomernih oblika u bilo kojem omjeru, ili njegova fiziološki prihvatljiva sol, ili fiziološki prihvatljiv solvat bilo kojeg od njih, prema bilo kojem ili više od zahtjeva 4 do 5, naznačen time da R3 je -O-CH3.
7. Spoj s formulom I, ili njegova fiziološki prihvatljiva sol, ili fiziološki prihvatljiv solvat bilo kojeg od njih, prema bilo kojem ili više od zahtjeva 1 do 6, naznačen time da se bira od: (S)-3-[(5-metoksi-6-fenil-piridin-2-karbonil)-amino]-3-o-tolil-propanske kiseline (S)-3-(2,4-diklor-fenil)-3-[(5-metoksi-6-fenil-piridin-2-karbonil)-amino]-propanske kiseline (S)-3-{[6-(2-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-[(5-metoksi-6-fenil-piridin-2-karbonil)-amino]-3-p-tolil-propanske kiseline (S)-3-[(5-metoksi-6-o-tolil-piridin-2-karbonil)-amino]-3-p-tolil-propanske kiseline (S)-3-{[5-metoksi-6-(2-trifluormetil-fenil)-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(3-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[5-metoksi-6-(2-metoksi-fenil)-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(2-klor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(2-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(2,4-difluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(2,3-diklor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(2-klor-5-trifluormetil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(3-fluor-2-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(2-klor-5-trifluormetil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(2,3-difluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(2,5-difluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(2,5-diklor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(3,5-dimetil-izoksazol-4-il)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(4-fluor-2-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(2,3-dimetil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(5-fluor-2-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(4-fluor-2-metoksi-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(5-fluor-2-metoksi-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(2-fluor-5-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(3-klor-2-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(3-fluor-2-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(5-klor-2-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-(2-fluor-fenil)-3-[(5-metoksi-6-fenil-piridin-2-karbonil)-amino]-propanske kiseline (S)-3-{[6-(2,4-diklor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-(2-fluor-fenil)-3-[(5-metoksi-6-o-tolil-piridin-2-karbonil)-amino]-propanske kiseline (S)-3-(2-fluor-fenil)-3-{[5-metoksi-6-(2-trifluormetil-fenil)-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-fluor-fenil)-3-{[5-metoksi-6-(2-metoksi-fenil)-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-{[6-(2-klor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-(2-fluor-fenil)-3-{[6-(2-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-{[6-(2,4-difluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(2,3-diklor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(2,3-difluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(2,5-difluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(4-fluor-2-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(3,5-dimetil-izoksazol-4-il)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(2,3-dimetil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(5-fluor-2-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(4-fluor-2-metoksi-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(5-fluor-2-metoksi-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(2-fluor-5-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(3-klor-2-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(5-klor-2-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-{[6-(3-klor-2-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-(2-fluor-fenil)-3-{[5-metoksi-6-(2-metil-furan-3-il)-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-{[6-(2-klor-3-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-fluor-fenil)-propanske kiseline (S)-3-(2-klor-fenil)-3-[(5-metoksi-6-fenil-piridin-2-karbonil)-amino]-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(2,4-diklor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(4-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-{[5-metoksi-6-(3-trifluormetil-fenil)-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(2,4-diklor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(4-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(4-klor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-[(5-metoksi-6-p-tolil-piridin-2-karbonil)-amino]-3-o-tolil-propanske kiseline (S)-3-{[6-(3-klor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[5-metoksi-6-(2-metoksi-fenil)-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-[(5-metoksi-6-m-tolil-piridin-2-karbonil)-amino]-3-o-tolil-propanske kiseline (S)-3-{[6-(2-klor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(3,4-difluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(2,5-difluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(2,5-diklor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(3,5-dimetil-izoksazol-4-il)-5-metoksi-piridin-2-karbonil]-amino}-3-O-tolil-propanske kiseline (S)-3-{[6-(2,3-dimetil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(2,4-dimetil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(4-fluor-2-metoksi-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-O-tolil-propanske kiseline (S)-3-{[6-(2-klor-5-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-O-tolil-propanske kiseline (S)-3-(2-klor-fenil)-3-[(6-metoksi-5-o-tolil-piridin-3-karbonil)-amino]-propanske kiseline (S)-3-(2-klor-fenil)-3-{[5-metoksi-6-(2-metoksi-fenil)-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-[(5-metoksi-6-m-tolil-piridin-2-karbonil)-amino]-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(2-klor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(2-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(2,4-difluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(2,3-diklor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(2,3-difluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(2,5-difluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(4-fluor-2-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(2,3-dimetil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(5-fluor-2-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(4-fluor-2-metoksi-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-{[6-(4-klor-2-metoksi-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-klor-fenil)-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(5-fluor-2-metoksi-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(2-fluor-5-trifluormetil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-{[5-metoksi-6-(2-trifluormetil-fenil)-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(2,4-difluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(4-fluor-2-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(4-cijano-2-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-O-tolil-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(2-fluor-5-metoksi-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(2-fluor-5-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-{[6-(3-klor-2-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-klor-fenil)-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(3-fluor-2-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-{[6-(5-klor-2-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-klor-fenil)-propanske kiseline (S)-3-(2-klor-fenil)-3-[(5-metoksi-6-pirazin-2-il-piridin-2-karbonil)-amino]-propanske kiseline (S)-3-{[6-(3-klor-2-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-klor-fenil)-propanske kiseline (S)-3-(2-klor-fenil)-3-{[5-metoksi-6-(2-metil-furan-3-il)-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-{[6-(2-klor-3-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-klor-fenil)-propanske kiseline (S)-3-{[6-(2-klor-3-metil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-klor-fenil)-propanske kiseline.
8. Spoj s formulom I, ili njegova fiziološki prihvatljiva sol, ili fiziološki prihvatljiv solvat bilo kojeg od njih, prema bilo kojem ili više od zahtjeva 1 do 6, naznačen time da se bira od (S)-3-[(5-metoksi-6-fenil-piridin-2-karbonil)-amino]-3-o-tolil-propanske kiseline (S)-3-(2,4-diklor-fenil)-3-[(5-metoksi-6-fenil-piridin-2-karbonil)-amino]-propanske kiseline (S)-3-[(5-fenil-piridin-2-karbonil)-amino]-3-o-tolil-propanske kiseline (S)-3-(2-klor-fenil)-3-[(5-metoksi-6-naftalen-2-il-piridin-2-karbonil)-amino]-propanske kiseline (S)-3-(2-klor-fenil)-3-[(5-metoksi-6-pirazin-2-il-piridin-2-karbonil)-amino]-propanske kiseline (S)-3-(2-klor-fenil)-3-[(6-metoksi-5-naftalen-2-il-piridin-3-karbonil)-amino]-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(2,3-dimetil-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-klor-fenil)-3-{[6-(2-klor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-fluor-fenil)-3-{[5-metoksi-6-(1,3,5-trimetil-1H-pirazol-4-il)-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-(2-fluor-fenil)-3-{[5-metoksi-6-(1-metil-1H-indol-5-il)-piridin-2-karbonil]-amino}-propanske kiseline (S)-3-[(5-metoksi-6-m-tolil-piridin-2-karbonil)-amino]-3-o-tolil-propanske kiseline (S)-3-{[6-(2-klor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(3,5-dimetil-izoksazol-4-il)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(4-klor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline (S)-3-{[6-(4-klor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-p-tolil-propanske kiseline (S)-3-{[6-(5-Acetil-tiofen-2-il)-5-metoksi-piridin-2-karbonil]-amino}-3-(2-klor-fenil)-propanske kiseline (S)-3-{[6-(2-fluor-fenil)-5-metoksi-piridin-2-karbonil]-amino}-3-o-tolil-propanske kiseline.
9. Postupak za dobivanje spoja s formulom I ili njegove fiziološki prihvatljive soli ili fiziološki prihvatljivog solvata bilo kojeg od njih prema bilo kojem ili više od zahtjeva 1 do 8, koji sadrži reakciju spoja s formulom II sa spojem s formulom III, [image] naznačen time da skupine A, D, E, L, G, R10, R30, R40, R50 i R60 u spojevima s formulama II i III su definirane kao u spojevima formule I, te dodatne funkcionalne skupine mogu biti prisutne u zaštićenom obliku ili u obliku prekursorskih skupina, i skupina J u spoju s formulom II je HO-, (C1-C4)-alkil-O- ili halogen.
10. Spoj s formulom I prema bilo kojem ili više od zahtjeva 1 do 8 ili njegova fiziološki prihvatljiva sol ili fiziološki prihvatljiv solvat bilo kojeg od njih naznačen time da je za uporabu kao farmaceutski proizvod.
11. Farmaceutski pripravak, naznačen time da sadrži barem jedan spoj s formulom I prema bilo kojem ili više od zahtjeva 1 do 8 ili njegova fiziološki prihvatljiva sol ili fiziološki prihvatljiv solvat bilo kojeg od njih i farmaceutski prihvatljiv nosač.
12. Uporaba spoja s formulom I prema bilo kojem ili više od zahtjeva 1 do 8 ili njegove fiziološki prihvatljive soli ili fiziološki prihvatljivog solvata bilo kojeg od njih naznačena time da je za proizvodnju lijeka za liječenje zatajenja srca, kongestivnog zatajenja srca, kardiomiopatije, infarkta miokarda, lijeve ventrikularne disfunkcije, srčane hipertrofije, valvularnih bolesti srca, hipertenzije, ateroskleroze, periferne arterijske okluzivne bolesti, restenoze, poremećaja vaskularne propusnosti, liječenje edema, tromboze, reumatoidnog artritisa, osteoartritisa, zatajenja bubrega, cistične fibroze, kroničnog bronhitisa, kronične opstruktivne plućne bolesti, astme, imunoloških bolesti, komplikacija povezanih s dijabetesom, fibroznih bolesti, boli, ishemije ili reperfuzijskog oštećenja ili neurodegenerativnih bolesti, ili za kardioprotekciju ili renoprotekciju ili kao diuretik (sa samostalno liječenje ili u kombinaciji s utvrđenim diureticima).
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