DK2262364T3 - Oxadiazoanthracenforbindelser til behandling af diabetes - Google Patents
Oxadiazoanthracenforbindelser til behandling af diabetes Download PDFInfo
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Claims (23)
1. Forbindelse med formlen (I):
formel (I) hvor R er -(CH2)p-G1-L1-G2, hvor L1 er udvalgt fra gruppen bestående af: en direkte binding, -CH2-, -O-, -N(R16)-, -C(O)-, -CON(R16)-, -N(R16)C(0)-, -N(R16)S02-, -S02N(R16)-, -C(0)-0-, -O-C(O)-, -S-, -S(O)-, -S(0)2- og -C=C-, hvor R16 er udvalgt fra gruppen bestående af: -hydrogen, -alkyl, - aryl, -alkylen-aryl; G1 er udvalgt fra gruppen bestående af: alkynylen, arylen, heteroarylen, kondenseret arylcycloalkylen, kondenseret cycloalkylarylen, kondenseret cycloalkylheteroarylen, kondenseret heterocyclylarylen og kondenseret heterocyclylheteroarylen, hvor G1 eventuelt er substitueret 1-4 gange med substituenter uafhængigt udvalgt fra R10, hvor R10 er Rb, G2 er udvalgt fra gruppen bestående af: -aryl, -heteroaryl, -kondenseret arylcycloalkyl, -kondenseret cycloalkylaryl, -kondenseret cycloalkylheteroaryl, -kondenseret heterocyclylaryl og -kondenseret heterocyclylheteroaryl, hvor G2 eventuelt er substitueret 1-4 gange med substituenter uafhængigt udvalgt fra R11, hvor R11 er Rb, R1 er udvalgt fra gruppen bestående af: -C02H og -C02R12, hvor R12 er udvalgt fra gruppen bestående af: -Ci-io-alkyl, -cycloalkyl og -aryl, hvor R12 eventuelt er substitueret 1 -4 gange med en gruppe uafhængigt udvalgt fra Rc; R2 er udvalgt fra gruppen bestående af: -hydrogen, -alkyl, -phenyl, -cycloalkyl, -alkylen-cycloalkyl og -alkylen-phenyl, hvor alkyl-, phenyl- og cycloalkylgrupper eventuelt er substitueret 1 -4 gange med en gruppe uafhængigt udvalgt fra Rc; R3 er udvalgt fra Ra; R4 er udvalgt fra Ra; og R5 er -G3-L2-Q2-L3-G4, hvor L2 og L3 uafhængigt er udvalgt fra gruppen bestående af: en direkte binding, -CH2-, -O-, -N(R26)-, -C(O)-, -CON(R26)-, -N(R26)C(0)-, -N(R26)CON(R27)-, -N(R26)C(0)0-, -0C(0)N(R26)-, -N(R26)S02-, -S02N(R26K -C(0)-0-, -O-C(O)-, -S-, -S(O)-, -S(0)2- og -N(R26)S02N(R27)-, hvor R26 og R27 uafhængigt er udvalgt fra gruppen bestående af: hydrogen, -alkyl, -aryl og -alkylen-aryl, hvor R26 og R27 eventuelt er substitueret 1-4 gange med Rc, eller R26 og R27 er taget sammen med de atomer, hvortil de er bundet, for at danne en heterocyklisk ring på 5 til 7 dele, der indeholder 0-2 yderligere heteroatomer uafhængigt udvalgt fra oxygen, nitrogen og svovl; Q2 er udvalgt fra gruppen bestående af: en direkte binding, Ci-10-alkylen, C2-io-alkenylen og C2-io-alkynylen, G3 er udvalgt fra gruppen bestående af: -arylen, -cycloalkylen, -heterocyclylen, -heteroarylen, -kondenseret arylcycloalkylen, -kondenseret cycloalkylarylen, kondenseret cycloalkylheteroarylen, -kondenseret heterocyclylarylen og -kondenseret heterocyclylheteroarylen, hvor G3 eventuelt er substitueret 1 -4 gange med substituenter uafhængigt udvalgt fra R8, hvor R8 er udvalgt fra Rb, G4 er udvalgt fra gruppen bestående af: -aryl, -cycloalkyl, -heterocyclyl, -heteroaryl, -kondenseret arylcycloalkyl, -kondenseret cycloalkylaryl, -kondenseret cycloalkylheteroaryl, -kondenseret heterocyclylaryl og -kondenseret heterocyclylheteroaryl, hvor G4 eventuelt er substitueret 1 -4 gange med substituenter uafhængigt udvalgt fra R9, hvor R9 er udvalgt fra Rb, Ringe B og C eventuelt er substitueret 1-4 gange med substituenter uafhængigt udvalgt fra gruppen bestående af Rb; Ra er udvalgt fra gruppen bestående af: a) -hydrogen, b) -S(0)m Rd, c) -S(0)20Rd, d) -S(0)mNRdRe, e) -C(0)Rd, f) -C02Rd, g) -C(0)NRdRe, h) -haloalkyl, i) -cycloalkyl, j) -heterocyclyl, k) -Ci-io-alkyl, l) -C2-io-alkenyl, m) -C2-io-alkynyl, n) -aryl, o) -heteroaryl, P) -c l-io-alkylen-aryl, q) -C2-io-alkynylen-aryl, r) -C l-io-alkylen-heteroaryl, s) -C2-io-alkynylen-heteroaryl og t) -C(RfR8)n-aryl, hvor alkyl-, alkenyl-, alkynyl-, aryl-, heterocyclyl-, heteroaryl- og cycloalkylgrupper eventuelt er substitueret 1 -4 gange med en gruppe uafhængigt udvalgt fra Rc; Rb er udvalgt fra gruppen bestående af: a) -cycloalkyl, b) -cyan, c) -ORd, d) -N02, e) -halogen, f) -S(0)m Rd, g) -SRd, h) -S(0)20Rd, i) -S(0)mNRdRe, j) -NRdRe, k) -0(CRfR8)„NRdRe, l) -C(0)Rd, m) -C02Rd, n) -C02(CRf Rg)„CONRd Re, 0) -0C(0)Rd, p) -C(0)NRdRe, q) -NRdC(0)Re, r) -0C(0)NRdRe, s) -NRdC(0)0Re, t) -NRdC(0)NRd Re, u) -CF3, v) -OCF3, w) -haloalkyl, x) -haloalkoxy, y) -Ci-10-alkyl, z) -C2-io-alkenyl, aa) -C2-io-alkynyl, ab) -Ci-10-alkylen-aryl, ac) -Ci-io-alkylen-heteroaryl, og ad) -heteroaryl, hvor alkyl-, alkenyl-, alkynyl-, aryl- og heteroaryl- og cycloalkylgruppeme eventuelt er substitueret 1 -4 gange med en gruppe uafhængigt udvalgt fra Rc; Rc er udvalgt fra gruppen bestående af: a) -halogen, b) -amino, c) -carboxy, d) -cyan, e) -Ci-4-alkyl, f) -O-Ci-4-alkyl, g) -o-CF3, h) -cycloalkyl, 1) -O-cycloalkyl, j) -aryl, k) -Ci-4-alkylen-aryl, l) -hydroxy, m) -CF3, n) -haloalkyl, o) -haloalkoxy, p) -O-aryl, q) -heteroaryl, r) -heteroarylen-Ci-io-alkyl, s) -heterocyclyl, t) -C02-Ci-io-alkyl, u) -C02-Ci-io-alkyl-aryl, v) -kondenseret arylcycloalkyl, w) -alkynylen-heteroaryl, x) -alkylen-aryl, y) -alkynylen-aryl, z) -nitro, aa) -N(H)-C(0)-Ci-6-alkyl, og bb) -S-Ci-e-alkyl; Rd og Re uafhængigt er udvalgt fra gruppen bestående af: hydrogen, Ci-io-alkyl, C2 io-alkenyl, C2 io-alkynyl, cycloalkyl, -Ci-io-alkylen-cycloalkyl, aryl, heteroaryl og heterocyclyl, hvor alkyl-, alkenyl-, alkynyl-, cycloalkyl-, aryl-, heteroaryl- og heterocyclylgruppeme eventuelt er substitueret med en til fire substituenter uafhængigt udvalgt fra Rc; eller Rd og Re sammen med de atomer, hvortil de er bundet, danner en heterocyklisk ring på 5 til 7 dele, der indeholder 0-2 yderligere heteroatomer uafhængigt udvalgt fra oxygen, svovl og nitrogen og eventuelt substitueret med 1 -3 gange med Rc, Rf og Rs uafhængigt er udvalgt fra gruppen bestående af: hydrogen, Ci-io-alkyl, cycloalkyl, -Ci-io-alkylen-cycloalkyl, -carboxy og aryl, hvor alkyl-, cycloalkyl- og arylgruppeme eventuelt er substitueret med en til fire substituenter uafhængigt udvalgt fra Rc; eller Rf og R8 sammen med det carbon, hvortil de er bundet, danner en ring på 5 til 7 dele, der indeholder 0-2 heteroatomer uafhængigt udvalgt fra oxygen, svovl og nitrogen eventuelt substitueret med 1-3 gange med Rc; m er et heltal fra 1 til 2; n er et heltal fra 1 til 10 og p er et heltal fra O til 2; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse ifølge krav 1, hvor R1 er -CO2H.
3. Forbindelse ifølge krav 1, hvor R2 er udvalgt fra gruppen bestående af: hydrogen og -Ci-10-alkyl, fortrinsvis, hvor R2 er hydrogen.
4. Forbindelse ifølge krav 1, hvor p er 1.
5. Forbindelse ifølge krav 1, hvor L1 er en direkte binding.
6. Forbindelse ifølge krav 1, R5 er -G3-L2-Q2-L3-G4, hvor L2 er udvalgt fra gruppen bestående af: -CH2-, -O-, -N(R26)- og -C(O)-, hvor R26 er udvalgt fra gruppen bestående af: hydrogen, -alkyl, - aryl og -alkylen-aryl; L3 er en direkte binding; Q2 er en Ci-10-alkylengruppe; G3 er en phenylengruppe, hvor G3 eventuelt er substitueret 1-4 gange med substituenter uafhængigt udvalgt fra R8, hvor R8 er udvalgt fra Rb; og G4 er udvalgt fra gruppen bestående af: cycloalkyl, phenyl, pyridinyl, benzothiopheneyl, benzothiazolyl, G4 eventuelt er substitueret 1 -4 gange med substituenter uafhængigt udvalgt fra R9, hvor R9 er udvalgt fra Rb.
7. Forbindelse ifølge krav 1, der har formlen (I-E)
eller et farmaceutisk acceptabelt salt deraf.
8. Forbindelse ifølge krav 1, hvor R4 er udvalgt fra gruppen bestående af -hydrogen, -Ci-6-alkyl og -C(0)-Ci.6-alkyl.
9. Forbindelse ifølge krav 1, hvor R5 er -G3 -L2 -Q2 -L3 -G4, hvor L2 er -O-, L3 er en direkte binding; Q2 er en Ci-io-alkylengruppe; G3 er en phenylengruppe og G4 er en phenylgruppe, hvor G4 er substitueret 1 -4 gange med substituenter uafhængigt udvalgt fra R9, hvor R9 er udvalgt fra Rb, og hvor G4 er substitueret med mindst én substituent udvalgt fra gruppen bestående af: a) -Ci-e-alkyl, b) -haloalkyl, c) -halogen, d) -alkoxy, e) -haloalkoxy, f) -CF3 og g) -O-CF3.
10. Forbindelse ifølge krav 1, der er: (S)-7-[(S)-l-carboxy-2-(4'-cyan-biphenyl-4-yl)-ethylcarbamoyl]-3-[4-(3,4-dichlor-benzyloxy)- phenyl]-2-oxo-l,2,3,5,7,8-hexahydro-4-oxa-l,6-diaza-anthracen-6-carboxylsyre-4-hydroxy- cyclohexylester, (S)-7-[(S)-l-carboxy-2-(4'-cyan-biphenyl-4-yl)-ethylcarbamoyl]-3-[4-(3,4-dichlor-benzyloxy)- phenyl]-2-oxo-l,2,3,5,7,8-hexahydro-4-oxa-l,6-diaza-anthracen-6-carboxylsyre3-hydroxy- cyclopentylester, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-(pyridin-4-carbonyl)-2,3,5,6,7,8-hexahydro-1 //-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-(pyridin-3-carbonyl)-2,3,5,6,7,8-hexahydro- l//-4-oxa-1,6-diaza-anthracen-7-carbonyl]-amino} -propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-((S)-tetrahydro-fu ran-2-carbonyl)-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthraccn-7-carbonyl]-amino}-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-((R)-tetrahydro-furan-2-carbonyl)-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino} -propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2 -oxo-6-(3 -phenyl-prop-2-ynyl)-2,3,5,6,7,8-hcxahydro-li/-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino j -propionsyre, (S)-7-[(S)-l-carboxy-2-(4'-cyan-biphenyl-4-yl)-ethylcarbamoyl]-3-[4-(3,4-dichlor-benzyloxy)- phenyl]-2-oxo-l,2,3,5,7,8-hexahydro-4-oxa-l,6-diaza-anthracen-6-carboxylsyre-isopropylester, (S)-7-[(S)-l-carboxy-2-(4'-cyan-biphenyl-4-yl)-ethylcarbamoyl]-3-[4-(3,4-dichlor-benzyloxy)- phenyl]-2-oxo-l,2,3,5,7,8-hexahydro-4-oxa-l,6-diaza-anthracen-6-carboxylsyre-isobutylester, (S)-7-[(S)-l-carboxy-2-(4'-cyan-biphenyl-4-yl)-ethylcarbamoyl]-3-[4-(3,4-dichlor-benzyloxy)- phenyl]-2-oxo-l,2,3,5,7,8-hexahydro-4-oxa-l,6-diaza-anthracen-6-carboxylsyre-2,2-dimethyl- propylester, (S)-7-[(S)-l-carboxy-2-(4'-cyan-biphenyl-4-yl)-ethylcarbamoyl]-3-[4-(3,4-dichlor-benzyloxy)- phenyl]-2-oxo-l,2,3,5,7,8-hexahydro-4-oxa-l,6-diaza-anthracen-6-carboxylsyre-tetrahydro-pyran-4- yl-ester, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-6-cyclobutancarbonyl-3-[4-(3,4-dichlor-benzyloxy)-phenyl]- 2-oxo-2,3,5,6,7,8-hexahydro-li/-4-oxa-l,6-diaza-anthracen-7-carbonyl}-amino)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-isobutyryl-2-oxo- 2,3,5,6,7,8-hexahydro-17/-4-oxa-l,6-diaza-anthracen-7-carbonyl}-amino)-propionsyre, (S)-2-({(S)-6-benzensulfonyl-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l ,6-diaza-anthracen-7-carbonyl}-amiiio)-3-(4'-cyan-biphenyl-4-yl)-propionsyre, (S)-2-({(S)-6-benzoyl-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2 -oxo-2,3,5,6,7,8-hcxahydro-l//-4-oxa- 1,6-diaza-anthracen-7-carbonyl} -amino)-3 -(4'-cyan-biphenyl-4-yl)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-6-cyclopentancarbonyl-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hcxahydro-l //-4-oxa-l,6-diaza-aiithraccn-7-carbonyl}-amino)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-(piperidin-l-carbonyl)-2,3,5,6,7,8-hexahydro- l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}-propionsyre, (S)-7-[(S)-l-carboxy-2-(4'-cyan-biphenyl-4-yl)-ethylcarbamoyl]-3-[4-(3,4-dichlor-benzyloxy)- phenyl]-2-oxo-l,2,3,5,7,8-hexahydro-4-oxa-l,6-diaza-anthracen-6-carboxylsyre cyclopropylmethylester, (S)-7-[(S)-l-carboxy-2-(4'-cyan-biphenyl-4-yl)-ethylcarbamoyl]-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-l,2,3,5,7,8-hexahydro-4-oxa-l,6-diaza-anthracen-6-carboxylsyre (R)-(tetrahydro-furan-3-yl)ester, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(furan-2-carbonyl)-2- oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthraccn-7-carbonyl]-amino}-propionsyrc, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(3-methyl-benzoyl)-2-oxo-2,3,5,6,7,8-hcxahydro-l //-4-oxa-l,6-diaza-anthraccn-7-carbonyl]-amino}-propionsyrc, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(4-fluor-benzoyl)-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l ,6-diaza-anthraccn-7-carbonyl]-amino}-propionsyrc, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(4-methoxy-benzoyl)- 2-oxo-2,3,5,6,7,8-hcxahydro-l//-4-oxa-l,6-diaza-anthraccn-7-carbonyl]-amino}-propionsyrc, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-(3-trifluormcthyl-bcnzoyl)-2,3,5,6,7,8-hcxahydro-l /7-4-oxa-1,6-diaza-anthraccn-7-carbonyl]-amino}-propionsyre, (S)-3-(4 -cyan biphenyl-4-yl)-2-({(S)-6-cyclohexancarbonyl-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hexahydro-1H- 4-oxa-1,6-diaza-anthracen-7-carbonyl} -amino)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(naphthalen-l- carbonyl)-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}- propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(naphthalen-2-carbonyl)-2-oxo-2,3,5,6,7,8-hexahydro-1H- 4-oxa-1,6-diaza-anthracen-7-carbonyl] -amino} -propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-(thiophen-2-carbonyl)-2,3,5,6,7,8-hexahydro- l//-4-oxa-l ,6-diaza-anthracen-7-carbonyl]-amino j -propionsyre, (S)-7-[(S)-l-carboxy-2-(4'-cyan-biphenyl-4-yl)-ethylcarbamoyl]-3-[4-(3,4-dichlor-benzyloxy)- phenyl]-2-oxo-l,2,3,5,7,8-hexahydro-4-oxa-l,6-diaza-anthracen-6-carboxylsyre-tert-butylester, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-6-(2-cyclopentyl-acetyl)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl}-amino)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(5-methyl-isoxazole- 3-carbonyl)-2-oxo-2,3,5,6,7,8-hexahydro-17/-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}- propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-(thiophen-2-sulfonyl)-2,3,5,6,7,8-hexahydro-1 //-4-oxa-1,6-diaza-anthraccn-7-carbonyl]-amino} -propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-dimethylcarbamoyl-2- oxo-2,3,5,6,7,8-hexahydro-17/-4-oxa-l,6-diaza-anthracen-7-carbonyl}-amino)-propionsyre, (S)-2-({(S)-6-benzyl-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa- l,6-diaza-anthracen-7-carbonyl}-amino)-3-(4'-cyan-biphenyl-4-yl)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-phenethyl- 2,3,5,6,7,8-hexahydro-l/7-4-oxa-l,6-diaza-anthracen-7-carbonyl}-amino)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-(2,4,6-trifluor-benzoyl)-2,3,5,6,7,8-hexahydro-l//-4-oxa-1,6-diaza-anthraccn-7-carbonyl]-amino}-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-(toluen-2-sulfony 1)-2,3,5,6,7,8-hcxahydro-l//-4-oxa-l,6-diaza-anthraccn-7-carbonyl]-amino}-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(2-methyl-benzyl)-2- oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}-propionsyrc, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-pyridin-2- ylmcthyl-2,3,5,6,7,8-hcxahydro-l//-4-oxa-l,6-diaza-andiraccn-7-carbonyl}-amino)-propionsyrc, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-thiophen-2- ylmcthyl-2,3,5,6,7,84icxahydro-l//-4-oxa-l,6-diaza-andiraccn-7-carbonyl}-amino)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phcnyl]-6-(2-fluor-bcnzyl)-2-oxo-2,3,5,6,7,8-hexahydro-1H- 4-oxa-1,6-diaza-anthracen-7-carbonyl]-amino} -propionsyre, (S)-2-({(S)-6-(2-chlor-benzyl)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-1,6-diaza-anthracen-7-carbonyl} -amino)-3 -(4'-cyan-biphenyl-4-yl)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(2-methoxy-benzyl)-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino} -propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(6-methyl-pyridin-2-ylmethyl)-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}-propionsyre, (S)-2-({(S)-6-(6-brom-pyridin-2-ylmethyl)-3-[4-(3,4-dichlor-benxyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl j -amino)-3-(4’-cyan-biphenyl-4-yl)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-6-(5-cyan-6-methylsulfanyl-pyridin-2-ylmethyl)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl} -amino)-propionsyre, (S)-3-(4'-cyan-biphcnyl-4-yl)-2-1 [(S)-3-[4-(3,4-dichlor-bcnzyloxy)-phenyl]-6-(l//-imidazol-2-y 1 methyl )-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-1,6-diaza-anth racen-7-carbony 1]-amino }-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2- {[(S)-3-[4-(3,4-dichlor-bcnzyloxy)-phenyl]-6-( 1 -methyl-1H-mndazol-2-yl-methyl)-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino} -propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-thiazol-2- ylmethyl-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl}-amino)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-(pyridin-2- carbonyl)-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(2-nitro-bcnzenesulfonyl)-2-oxo-2,3,5,6,7,8-hcxahydro-1//-4-oxa-1,6-diaza-anthracen-7-carbonyl]-amino}-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(3-nitro-bcnzenesulfonyl)-2-oxo-2,3,5,6,7,8-hexahydm- l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}-propionsyre, (S)-2-({(S)-6-(2-cyan-benzyl)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-1,6-diaza-anthracen-7-carbonyl} -amino)-3 -(4'-cyan-biphenyl-4-yl)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-6-cyclopropylmethyl-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hcxahydro-l//-4-oxa-l ,6-diaza-anthracen-7-carbonyl}-amino)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2 -oxo-6-(3 -pyrimidin-2- yl-prop-2-ynyl)-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}- propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-(3-thiophen-3-yl-prop-2-ynyl)-2,3,5,6,7,8-hexahydro-l//-4 -oxa-1,6-diaza-anthracen-7 -carbonyl] -amino} -propionsyre, (S)-2-({(S)-6-benzoyl-3-[4-(2,6-dichlor-bcnzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hcxahydro-l //-4-oxa- 1.6- diaza-anthracen-7-carbonyl} -amino)-3 -(4'-cyan-biphenyl-4-yl)-propionsyre, (S )-2-( !(S)-6-bcnzoyl-3-[4-(2,5-dichlor-bcnzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa- 1.6- diaza-anthracen-7-carbonyl}-amino)-3-(4'-cyan-biphenyl-4-yl)-propionsyre, (S)-2-({(S)-6-bcnzoyl-3-[4-(3-chloro-bcnzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hcxahydro-l//-4-oxa- 1.6- diaza-anthracen-7-carbonyl} -amino)-3 -(4'-cyan-biphenyl-4-yl)-propionsyre, (S)-2-({(S)-6-benzoyl-3-[4-(4-chlor-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6- diaza-anthracen-7-carbonyl}-amino)-3-(4'-cyan-biphenyl-4-yl)-propionsyre, (S)-2-({(S)-6-benzoyl-3-[4-(4-chlor-3-trifluormethyl-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8- hexahyclro-l//-4-oxa-l,6-diaza-anthraccn-7-carbonyl}-amiiio)-3-(4'-cyan-bipheiiyl-4-yl)- propionsyre, (S)-2-({(S)-6-benzoyl-3-[4-(4-methoxy-3-trifluormethyl-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8- hexahydro-l//-4-oxa-l,6-diaza-anthraccn-7-carbonyl}-amino)-3-(4'-cyan-biphenyl-4-yl)- propionsyre, (S)-7-[(S)-l-carboxy-2-(4'-cyan-biphenyl-4-yl)-ethylcarbamoyl]-3-[4-(5,6-dichlor-pyridin-3- ylmethoxy)-phenyl]-2-oxo-l,2,3,5,7,8-hexahydro-4-oxa-l,6-diaza-anthracen-6-carboxylsyre-fert- butylester, (S)-2-({(S)-6-benzoyl-3-[4-(5,6-dichlor-pyridin-3-ylmethoxy)-phenyl]-2-oxo-2,3,5,6,7,8-hexahydro- l//-4-oxa-l,6-diaza-anthracen-7-carbonyl}-amino)-3-(4'-cyan-biphenyl-4-yl)-propionsyre, (S)-2-({(S)-6-benzyl-3-[4-(5,6-dichlor-pyridin-3-ylmethoxy)-phenyl]-2-oxo-2,3,5,6,7,8-hexahydro-17/-4-oxa-l,6-diaza-anthraccn-7-carbonyl j -amino)-3-(4'-cyan-biphenyl-4-yl)-propionsyrc, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(5,6-dichlor-pyridin-3-ylmethoxy)-phenyl]-2-oxo-6-(thiophene-2-carbonyl)-2,3,5,6,7,8-hcxahydro-l 7/-4-oxa-l,6-diaza-anthraccn-7-carbonyl]-amino}-propionsyre, (S)-2-({(S)-3-[4-(3-chlor-benzyloxy)-phenyl]-2-oxo-6-thiazol-2-ylmethyl-2,3,5,6,7,8-hexahydro-177-4-oxa-1,6-diaza-anthracen-7-carbonyl} -amino)-3 -(4'-cyan-biphenyl-4-yl)-propionsyre, (S)-7-[(S)-l-carboxy-2-(4'-cyan-biphenyl-4-yl)-ethylcarbamoyl]-3-[4-(3,4-dichlor-benzyloxy)- phenyl]-l-methyl-2-oxo-l,2,3,5,7,8-hexahydro-4-oxa-l,6-diaza-anthracen-6-carboxylsyre- isopropylester, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6-(3- phenyl-prop-2-ynyl)-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}- propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6-(l-phenyl-pmpyl)-2,3,5,6,7,8-hcxahydro-l /7-4-oxa-1,6-diaza-anthracen-7-carbonyl]-amino }-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(2-ethyl-benzyl)-l-methyl-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}-propionsyre, (S)-3-(4 -cyan-biphenyl-4 yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(2-isopropyl-benzyl)- 1- mcthyl-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthraccn-7-carbonyl]-amino}- propionsyre, (S)-3-(4 -cyan-biphenyl-4-yl)-2-({(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-indan-2-yl-l-methyl- 2- oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-1,6-diaza-anthraccn-7-carbonyl}-amino)-propionsyrc, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-6-cyclopentyl-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-2,3,5,6,7,8-hexahydro-l /7-4-oxa-1,6-diaza-anthraccn-7-carbonyl}-amino)-propionsyrc, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-6-cyclohexyl-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2- oxo-2,3,5,6,7,8-hexahydro-l/7-4-oxa-l,6-diaza-aiithraccn-7-carbonyl}-amino)-propionsyrc, (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-6-cyclobutyl-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-2,3,5,6,7,8-hexahydro-1//-4-oxa-l ,6-diaza-anthraccn-7-carbonyl} -amino)-propionsyrc, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6-(l-phenyl-cyc lopcntylmcthy 1)-2,3,5,6,7,8-hcxahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino} -propionsyre, (S)-3-(4’-cyan-biphenyl-4-yl)-2-({(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-ethyl-l-methyl-2-oxo- 2.3.5.6.7.8- hcxahydro-1 /7-4-oxa-] ,6-diaza-anthraccn-7-carbonyl )-amino)-propionsyre, (S)-2-({(S)-6-(carboxy-phenyl-methyl)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo- 2.3.5.6.7.8- hexahydro-17/-4-oxa-l,6-diaza-anthracen-7-carbonyl}-amino)-3-(4’-cyan-biphenyl-4-yl)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6-(l- phenyl-ethyl)-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}- propionsyre, (S)-2-({(S)-6-(2-acetylamino-4-methyl-thiazole-5-sulfonyl)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2- oxo-2,3,5,6,7,8-hexahydro-17/-4-oxa-l,6-diaza-anthracen-7-carbonyl}-amino)-3-(4'-cyan-biphenyl- 4-yl)-propionsyre, (S)-7-((S)-2-biphenyl-4-yl-l-carboxy-ethylcarbamoyl)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo- 1.2.3.5.7.8- hcxahydro-4-oxa-l,6-diaza-anthraccn-6-carboxylsyrc-isopropylestcr, (S)-2-( i(S)-6-bcnzoyl-3-[4-(3,4-dichlor-bcnzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hcxahydro-17/-4-oxa- l,6-diaza-anthracen-7-carbonyl}-amino)-3-(4-pyridin-4-yl-phenyl)-propionsyre, (S)-2-( j(S)-6-bcnzoyl-3-[4-(3,4-dichlor-bcnzyloxy)-phcnyl]-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa- 1,6-diaza-anthracen-7-carbonyl} -amino)-3 -(4'-chlor-biphenyl-4-yl)-propionsyre, (S)-2-({(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-6-pyridin-2-ylmethyl-2,3,5,6,7,8-hexahydro-1 /7-4-oxa-l,6-diaza-anthraccn-7-carbonylj -amino)-3-(4'-methyl-biphenyl-4-yl)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(3R,7S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6-((S)-1 -phenyl-propyl )-2,3,5,6,7,8-hcxahydro-1 //-4-oxa-1,6-diaza-anthraccn-7-carbonyl]-aminoj -propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(3S,7S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6-((S)-l-phcnyl-propyl)-2,3»5,6,7,8-hcxahydro-l //-4-oxa-l ,6-diaza-anthraccn-7-carbonyl]-aminoj-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(3S,7S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6-((R)-l-phcnyl-propyl)-2,3,5,6,7,8-hcxahydro-l //-4-oxa-l ,6-diaza-anthraccn-7-carbonyl]-amino|-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(3R,7S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6- ((R)-l-phenyl-propyl)-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}- propionsyre, (S)-3-(4'-chlor-biphenyl-4-yl)-2-{[(3R,7S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6- ((S)-l-phenyl-propyl)-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}- propionsyre, (S)-2-{[(3R,7S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6-((S)-l-phenyl-propyl)- 2.3.5.6.7.8- hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}-3-(4'-methoxy-biphenyl-4-yl)-propionsyre, (S)-2-{[(3R,7S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6-((S)-l-phenyl-propyl)- 2.3.5.6.7.8- hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}-3-(4'-fluor-biphenyl-4-yl)-propionsyre, (S)-3-(4'-chlor-biphenyl-4-yl)-2-{[(3S,7S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-OXO-6- ((S)-l-phenyl-propyl)-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}- propionsyre, (S)-2-{[(3S,7S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6-((S)-l-phenyl-propyl)- 2.3.5.6.7.8- hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}-3-(4'-methoxy-biphenyl-4-yl)-propionsyre, (S)-2-{[(3S,7S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6-((S)-l-phenyl-propyl)- 2.3.5.6.7.8- hcxahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}-3-(4'-fluor-biphenyl-4-yl)-propionsyre, (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-6-(3,5-dimethyl- isoxazol-4-sulfonyl)-l-methyl-2-oxo-2,3,5,6,7,8-hexahydro-lH-4-oxa-l,6-diaza-anthracen-7- carbonyl] -amino} -propionsyre, (R) -3-(4’-cyan-biphenyl-4-yl)-2-{[(3R,7S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6-((S)-l-phenyl-propyl)-2,3,5,6,7,8-hexahydro-lH-4 -oxa-1,6-diaza-anthracen-7 -carbonyl] -amino} -propionsyre, (S) -2-({(S)-6-benzoyl-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hexahydro-lH-4-oxa- l,6-diaza-anthracen-7-carbonyl}-amino)-3-[4-(pyridin-4-yloxy)-phenyl]-propionsyre, (S)-2-({(S)-6-(2-amino-4-methyl-thiazol-5-sulfonyl)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l- methyl-2-oxo-2,3,5,6,7,8-hcxahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl}-amino)-3-(4'-cyan- biphenyl-4-yl)-propionsyre, (S)-2-({(S)-6-(2-amino-4-methyl-thiazole-5-sulfonyl)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-mcthyl-2-oxo-2,3,5,6,7,8-hcxahydro-1 /7-4-oxa-1,6-diaza-anthracen-7-carbonyl}-amino)-3-(4'-cyan-biphenyl-4-yl)-propionsyre, (S)-2-({(S)-6-(2-amino-4-methyl-thiazole-5-sulfonyl)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo- 2.3.5.6.7.8- hexahydro-17/-4-oxa-l,6-diaza-anthracen-7-carbonyl}-amino)-3-(4'-cyan-biphenyl-4-yl)-propionsyre, eller (S)-2-({(S)-6-(2-amino-4-methyl-thiazol-5-sulfonyl)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo- 2.3.5.6.7.8- hcxahydro-l/7-4-oxa-l,6-diaza-anthracen-7-carbonyl|-amino)-3-(4'-cyan-biphenyl-4-yl)-propionsyre, eller et farmaceutisk acceptabelt salt deraf.
11. Forbindelse ifølge krav 1, hvor forbindelsen er (S)-2-({(S)-6-benzoyl-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hcxahydro-l/7-4-oxa-l,6-diaza-anthraccn-7-carbonyl}-amino)-3-(4'-cyan-biphenyl-4-yl)-propionsyre eller et farmaceutisk acceptabelt salt deraf.
12. Forbindelse ifølge krav 1, hvor forbindelsen er (S)-3-(4'-cyan-biphenyl-4-yl)-2-({(S)-6-cyclopcntancarbonyl-3-[4-(3,4-dichlor-bcnzyloxy)-phenyl]-2-oxo-2,3,5,6,7,8-hcxahydro-l//-4-oxa- l,6-diaza-anthracen-7-carbonyl}-amino)-propionsyre eller et farmaceutisk acceptabelt salt deraf.
13. Forbindelse ifølge krav 1, hvor forbindelsen er (S)-7-[(S)-l-carboxy-2-(4'-cyan-biphenyl-4-yl)-ethylcarbamoyl]-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-2-oxo-l,2,3,5,7,8-hexahydro-4-oxa-l,6-diaza-anthracen-6-carboxylsyrecyclopropylmethylester eller et farmaceutisk acceptabelt salt deraf.
14. Forbindelse ifølge krav 1, hvor forbindelsen er (S)-3-(4’-cyan-biphenyl-4-yl)-2-{[(S)-3-[4-(3,4-dichlor-bcnzyloxy)-phcnyl]-6-(furan-2-carbonyl)-2-oxo-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino }-propionsyre eller et farmaceutisk acceptabelt salt deraf.
15. Forbindelse ifølge krav 1, hvor forbindelsen er (S)-3-(4’-cyan-biphenyl-4-yl)-2-({(S)-3-[4-(3,4-dichlor-benzyloxy-phenyl]-2-oxo-6-pyridin-2-ylmethyl-2,3,5,6,7,8-hexahydro-l//-4-oxa-l,6-diaza-anthracen-7-carbonyl}-amino)-propionsyre eller et farmaceutisk acceptabelt salt deraf.
16. Forbindelse ifølge krav 1, hvor forbindelsen er (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(3R,7S)-3-[4-(3,4-dichlor-benzyloxy)-phenyl]-l-methyl-2-oxo-6-((S)-l-phenyl-propyl)-2,3,5,6,7,8-hexahydro-l/7-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}-propionsyre eller et farmaceutisk acceptabelt salt deraf.
17. Forbindelse ifølge krav 1, hvor forbindelsen er (S)-3-(4'-cyan-biphenyl-4-yl)-2-{[(3S,7S)-3-[4-(3,4-dichlor-benzyloxy)-phcnyl]-l -mcthyl-2-oxo-6-((S)-l -phcnyl-propyl)-2,3,5,6,7,8-hcxahydro-l /7-4-oxa-l,6-diaza-anthracen-7-carbonyl]-amino}-propionsyre eller et farmaceutisk acceptabelt salt deraf.
18. Kombination af en forbindelse ifølge et hvilket som helst af kravene 1 til 17 og et eller flere andre terapeutiske midler.
19. Farmaceutisk sammensætning, der omfatter en forbindelse som defineret ifølge et hvilket som helst af kravene 1 til 17, eller en kombination som defineret ifølge krav 18, og en farmaceutisk acceptabel bærer eller fortyndingsmiddel.
20. Forbindelse som defineret ifølge et hvilket som helst af kravene 1 til 17, en kombination som defineret ifølge krav 18, eller en sammensætning som defineret ifølge krav 19 til anvendelse som et medikament.
21. Forbindelse, kombination eller sammensætning til anvendelse ifølge krav 20 til hæmning af tarmmotilitet, sænkning af blodsukker hos et menneske, forsinkelse eller forebyggelse af progressionen fra IGT til type 2-diabetes, forsinkelse eller forebyggelse af progressionen fra ikke-insulinkrævende type 2-diabetes til insulinkrævende type 2-diabetes, forsinkelse eller forebyggelse af type 1 -diabetes, eller appetitregulering eller behandling af en forstyrrelse i energiforbrug; fortrinsvis hvor sygdommen eller lidelsen er udvalgt fra metaboliske sygdomme, glukoseintolerance, hyperglycæmi, dyslipidæmi, type 1-diabetes, type 2-diabetes, hypertriglyceridæmi, syndrom X, insulinresistens, IGT, fedme, diabetes som en følge af fedme, diabetisk dyslipidæmi, hyperlipidæmi, kardiovaskulære sygdomme, hypertension eller komplikationer stammende fra eller forbundet med diabetes.
22. Forbindelse, kombination eller sammensætning til anvendelse ifølge krav 20 til behandlingen og/eller forebyggelse af type 2-diabetes.
23. Forbindelse, kombination eller sammensætning til anvendelse ifølge krav 20 til sænkning af blodsukker hos et menneske.
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US3459908P | 2008-03-07 | 2008-03-07 | |
PCT/US2009/036333 WO2009111700A2 (en) | 2008-03-07 | 2009-03-06 | Oxadiazoanthracene compounds for the treatment of diabetes |
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2014
- 2014-03-05 US US14/197,771 patent/US8933222B2/en active Active
- 2014-12-01 US US14/556,837 patent/US9120813B2/en active Active
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