ME02047B - Nova jedinjenja koja se vezuju za fxr (nr1 h4) i moduliraju njegovu aktivnost - Google Patents

Nova jedinjenja koja se vezuju za fxr (nr1 h4) i moduliraju njegovu aktivnost

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Publication number
ME02047B
ME02047B MEP-2015-18A MEP1815A ME02047B ME 02047 B ME02047 B ME 02047B ME P1815 A MEP1815 A ME P1815A ME 02047 B ME02047 B ME 02047B
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Montenegro
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cyclopropyl
phenyl
prophylaxis
treatment
methoxy
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MEP-2015-18A
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Claus Kremoser
Ulrich Abel
Christoph Steeneck
Olaf Kinzel
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Gilead Sciences Inc
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Publication of ME02047B publication Critical patent/ME02047B/me

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Claims (15)

1. Jedinjenje prema sledećoj formuli (1), njegov enantiomer, diastereomer, tautomer ili farmaceutski prihvatljiva sogdeR je izabran iz grupe koju čini COOR6, CONR7R8, tetrazolil ili H, gde je R6 nezavisno izabran iz grupe koju čini H, ili C1-6 alkil, i R7 i R8 međusobno nezavisno izabrani iz grupe koju čine H, C1-6 alkil, C1-6 haloalkil, C1-6 alkilen-R9, SO2-C1-6 alkil gde je R9 izabran iz grupe koju čine COOH, OH, ili SO3H;A je izabran iz grupe koju čine fenil, piridil, pirazolil, indolil, tienil, benzotienil, indazolil, benzizoksazolil, benzofuranil, benzotriazolil, furanil, benzotiazolil, tiazolil, svaki izborno supstituisan sa jednom ili dve grupe nezavisno izabrane iz grupe koju čine OH, C1-6 alkil, C3-6 cikloalkil, ili halogen;Q je izabran iz grupe koju čine fenil, piridil, tiazolil, tiofenil, pirimidil, svaki izborno supstituisan sa jednom ili dve grupe nezavisno izabrane iz grupe koju čini C1-6 alkil, halogen ili CF3;gdeX= CH, N, NO;R1 je izabran iz grupe koju čine vodonik, C1-C3 alkil, C3-C6 cikloalkil, C4-C5 alkilcikloalkil, gde C1-3 alkil je izborno supstituisan sa 1 do 3 supstituenta nezavisno izabrana od halogena, hidroksi ili C1-6 alkoksi;R2 i R3 su nezavisno izabrani iz grupe koju čini vodonik, C1-C3 alkil, C1-C3 haloalkil, C1-C3 alkoksi, C1-C3 haloalkoksi i halogen.
2. Jedinjenje prema patentnom zahtevu 1 gde R je izabran iz grupe koju čini COOR6, CONR7R8, tetrazolil ili H, sa R6, R7 i R8 nezavisno izabran iz grupe koju čini H i C1-6 alkil; A je izabran iz grupe koju čini fenil, piridil, indolil, tienil, benzotienil, indazolil, benzizoksazolil, benzofuranil, benzotriazolil, furanil, benzotiazolil, tiazolil, svaki izborno supstituisan sa jednom ili dve grupe nezavisno izabran iz grupe koju čini OH, C1-6 alkil i C3-6 cikloalkil; Q je izabrani iz grupe koju čini fenil, piridil, tiazolil, tiofenil, pirimidil, svaki izborno supstituisan sa jednom ili dve grupe nezavisno izabran iz grupe koju čini C1-6 alkil, halogen i CF3; gde X= CH, N, NO; R1 je izabran iz grupe koju čini vodonik, C1-C3 alkil, C1-C3 haloalkil, C3-C6 cikloalkil i C4-C5 alkilcikloalkil; R2 i R3 su nezavisno izabrani iz grupe koju čini vodonik, C1-C3 alkil, C1-C3 haloalkil, C1-C3 alkoksi, C1-C3 haloalkoksi i halogen.
3. Jedinjenje prema patentnom zahtevu 1 ili 2, sa sledećom strukturom gde X1 je CH ili N; R4 i R5 su nezavisno izabrani iz grupe koju čini H, C1-6 alkil, halogen i CF3; R-A je izabran od ili R1 je izabran iz grupe koju čini izopropil, t-butil i ciklopropil; R2 i R3 su nezavisno izabrani iz grupe koju čini halogen, C1-C3 alkil, metoksi i trifluorometoksi.
4. Jedinjenje prema bilo kom od patentnih zahteva 1 do 3, gde A je fenil; Q je izborno supstituisani fenil, poželjno supstituisan sa jednim supstituentom, poželjno halogenom; X je CH; R1 je cikloalkil; i R2 i R3 svaki su halogen.
5. Jedinjenje prema bilo kom od patentnih zahteva 1 do 4 izabrano od: 3-((2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)benzojeve kiseline (-)-3-((2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)benzojeve kiseline (+)-3-(2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)benzojeve kiseline 3-((2-(2-hloro-4-((3-(2,6-dihlorofenil)-5-izopropilizoksazol-4-il)metoksi)fenil)ciklopropil)benzojeve kiseline 3-((2-(2-hloro-4-((5-ciklopropil-3-(3,5-dihloropiridin-4-il)izoksazol-4-il)metoksi)fenil)ciklopropil)benzojeve kiseline 4-((4-((4-(2-(3-carboksifenil)ciklopropil)-3-hlorophenoksi)metil)-5-ciklopropilizoksazol-3-il)-3,5-dihloropiridin 1-oksida 3-((2-(2-hloro-4-((1-(2,6-dihlorofenil)-4-izopropil-1H-1,2,3-triazol-5-il)metoksi)fenil)ciklopropil)benzojeve kiseline 4-(((4-(2-(6-(1H-tetrazol-5-il)piridin-3-il)ciklopropil)-3-hlorophenoksi)metil)-5-ciklopropil-3-(2,6-dihlorofenil)izoksazola 5-((2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)pikolinske kiseline.
6. Jedinjenje prema bilo kom od patentnih zahteva 1 do 4 izabrano od 3-((2-(6-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)-2-(trifluorometil)piridin-3-il)ciklopropil)benzojeve kiseline 4-((2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)benzojeve kiseline 1,3-dihidroksi-2-(hidroksimetil)propan-2-aminijum 4-(2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)benzoata (+)-4-(2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)benzojeve kiseline (-)-4-((2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)benzojeve kiseline 6-((2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)-1-metil-1H-indazol-3-karboksilne kiseline (+)-6-(2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)-1-metil-1H-indazol-3-karboksilne kiseline (-)-6-((2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)-1-metil-1H-indazol-3-karboksilne kiseline 4-((2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)-N-(metilsulfonil)benzamida 2-((4-(2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)benzamido)etansulfo kiseline 4-(((4-(2-(4-(1H-tetrazol-5-il)fenil)ciklopropil)-3-hloropenoksi)metil)-5-ciklopropil-3-(2,6-dihlorofenil)izoksazola 4-((2-(2-hloro-4-((3-(2,6-dihlorofenil)-5-(2-hidroksipropan-2-il)izoksazol-4-il)metoksi)fenil)ciklopropil)benzojeve kiseline 5-((2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)-1-izopropil-1H-pirazol-3-karboksilne kiseline 6-((2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)-1-izopropil-1H-indazol-3-karboksilne kiseline 4-((2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)-2,6-dimetilbenzojeve kiseline 4-((2-(2-hloro-4-((5-ciklopropil-3-(2-(trifluorometoksi)fenil)izoksazol-4-il)metoksi)fenil)ciklopropil)benzojeve kiseline (+)-2-(4-(2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)benzamido)etansulfokiseline (-)-2-((4-(2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)benzamido)etansulfokiseline 2-((4-(2-(2-hloro-4-((5-ciklopropil-3-(2,6-dihlorofenil)izoksazol-4-il)metoksi)fenil)ciklopropil)benzamido)sirćetne kiseline 4-((2-(2-hloro-4-((4-(2,6-dihlorofenil)-1-izopropil-1H-1,2,3-triazol-5-il)metoksi)fenil)ciklopropil)benzojeve kiseline.
7. Jedinjenje prema bilo kom od patentnih zahteva 1 do 6 za korišćenje u profilaksi i/ili tretmanu bolesti posredovanih sa FXR.
8. Jedinjenje prema patentnom zahtevu 7 za upotrebu u profilaksi i/ili tretmanu intrahepatičkog ili nekih drugih oblika ekstrahepatičkih holestatičnih stanja, ili fibroze jetre koja je rezultat hroničnih holestatičnih stanja ili akutnih intrahepatičkih holestatičnih stanja; i/ili za upotrebu u profilaksi i/ili tretmanu opstruktivnih ili hroničnih inflamatornih bolesti jetre; i/ili za upotrebu u profilaksi i/ili tretmanu ciroze jetre; i/ili za upotrebu u profilaksi i/ili tretmanu steatoze jetre i povezanih sindroma, holestatičnih ili fibrotičkih efekata koji su povezani sa cirozom jetre izazvane alkoholom ili sa virusnim oblikom hepatitisa; i/ili za upotrebu u profilaksi i/ili lečenju otkazivanja jetre ili ishemije jetre nakon velike hirurške intervencije na jetre; i/ili za upotrebu u profilaksi i/ili tretmanu steatohepatitisa povezanog sa hemoterapijom (CASH); i/ili za upotrebu u profilaksi i/ili tretmanu akutnog otkazivanja jetre; i/ili za upotrebu u profilaksi i/ili tretmanu inflamatorne bolesti creva.
9. Jedinjenje prema patentnom zahtevu 7 za upotrebu u profilaksi i/ili tretmanu poremećaja lipida i lipoproteina; i/ili za upotrebu u profilaksi i/ili tretmanu dijabetesa tipa II i kliničkih komplikacija tipa I i tipa II dijabetesa, uključujući dijabetičku nefropatiju, dijabetičku neuropatiju, dijabetičku retinopatiju i druge uočene efekte klinički manifestovane kod dugotrajnog dijabetesa; i/ili za upotrebu u profilaksi i/ili tretmanu stanja i bolesti koji rezultuju iz hronične masne i fibrotičke degeneracije organa usled akumulacije lipida i specifično triglicerida i naknadne aktivacije profibrotičkih puteva, kao što je bolest ne-alkoholna masna jetra (NAFLD), ili ne-alkoholni steatohepatitis (NASH); i/ili za upotrebu u profilaksi i/ili tretmanu gojaznosti ili metaboličkog sindroma (kombinovana stanja dislipidemije, dijabetesa ili abnormalno visokog indeksa telesne mase); i/ili za upotrebu u profilaksi i/ili tretmanu akutnog infarkta miokarda, akutnog šloga, ili tromboze koja se dešava kao krajnji ishod hronične opstruktivne ateroskleroze.
10. Jedinjenje prema patentnom zahtevu 7 za upotrebu u profilaksi i/ili tretmanu ne-malignih hiperproliferativnih poremećaja i malignih hiperproliferativnih poremećaja, specifično hepatocelularnog karcinoma, adenoma debelog creva i polipoze, adenokarcinoma debelog creva, raka dojke, adenokarcinoma pankreasa, Barrett-ovog ezofagusa i drugih oblika neoplastičnih bolesti gastrointestinalnog trakta i jetre.
11. Upotreba jedinjenja prema bilo kom od patentnih zahteva 1 do 6 za pripremu medikamenta za profilaksu i/ili tretman bolesti posredovanih sa FXR.
12. Upotreba prema patentnom zahtevu 11 za profilaksu i/ili tretman hroničnih intrahepatičkih ili nekih drugih ekstrahepatičkih holestatičnih stanja, ili fibroze jetre koja je rezultat hroničnih holestatičnih stanja ili akutnih holestatičnih stanja; i/ili za upotrebu u profilaksi i/ili tretmanu opstruktivnih ili hroničnih inflamatornih bolesti jetre; i/ili za upotrebu u profilaksi i/ili tretmanu ciroze jetre; i/ili za upotrebu u profilaksi i/ili tretmanu steatoze jetre i povezanih sindroma, holestatičnih ili fibrotičkih efekata koji su povezani sa cirozom jetre izazvane alkoholom ili sa virusnim oblikom hepatitisa; i/ili za upotrebu u profilaksi i/ili lečenju otkazivanja jetre ili ishemije jetre nakon velike hirurške intervencije na jetre; i/ili za upotrebu u profilaksi i/ili tretmanu steatohepatitisa povezanog sa hemoterapijom (CASH); i/ili za upotrebu u profilaksi i/ili tretmanu akutnog otkazivanja jetre; i/ili za upotrebu u profilaksi i/ili tretmanu inflamatorne bolesti creva.
13. Upotreba prema patentnom zahtevu 11 za profilaksu i/ili tretman poremećaja lipida ili lipoproteina; i/ili za upotrebu u profilaksi i/ili tretmanu dijabetesa tipa II i kliničkih komplikacija tipa I i tipa II dijabetesa, uključujući dijabetičku nefropatiju, dijabetičku neuropatiju, dijabetičku retinopatiju i druge uočene efekte klinički manifestovane kod dugotrajnog dijabetesa; i/ili za upotrebu u profilaksi i/ili tretmanu stanja i bolesti koji rezultuju iz hronične masne i fibrotičke degeneracije organa usled akumulacije lipida i specifično triglicerida i naknadne aktivacije profibrotičkih puteva, kao što je bolest ne-alkoholna masna jetra (NAFLD), ili ne-alkoholni steatohepatitis (NASH); i/ili za upotrebu u profilaksi i/ili tretmanu gojaznosti ili metaboličkog sindroma (kombinovana stanja dislipidemije, dijabetesa ili abnormalno visokog indeksa telesne mase); i/ili za upotrebu u profilaksi i/ili tretmanu akutnog infarkta miokarda, akutnog šloga, ili tromboze koja se dešava kao krajnji ishod hronične opstruktivne ateroskleroze.
14. Upotreba prema patentnom zahtevu 11 za profilaksu i/ili tretman ne-malignih hiperproliferativnih poremećaja i malignih hiperproliferativnih poremećaja, specifično hepatocelularnog karcinoma, adenoma debelog creva i polipoze, adenokarcinoma debelog creva, raka dojke, adenokarcinoma pankreasa, Barrett-ovog ezofagusa i drugih oblika neoplastičnih bolesti gastrointestinalnog trakta i jetre.
15. Jedinjenje prema bilo kom od patentnih zahteva 1 do 6 za upotrebu kao medikamenta.
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