HEPATITIS C INHIBITOR TRI-PEPTIDES

Racemati, dijastereoizomeri i optički izomeri jedinjenja formule (I) u kojoj B jeste H, grupa C6 ili C10 aril, C7-16 aralkil; Het ili (niži alkil)-Het, svaka od njih eventualno supstituisana sa c1-6 alkilom; C1-6 alkoksi; C1-6 alkanoil; hidroksi; hidroksialkil; halogena; halogenoalkil; nitro; cijana...

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Hauptverfasser: SIMONEAU, Bruno, POUPART, Marc-André, HALMOS, Teddy, WERNIC, Dominik, M, GHIRO, Elise, TSANTRIZOS, Youla, S, CAMERON, Dale, FAUCHER, Anne-Marie, RANCOURT, Jean, LLINAS-BRUNET, Montse, BAILEY, Murray, D, GOUDREAU, Nathalie
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Sprache:eng
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Zusammenfassung:Racemati, dijastereoizomeri i optički izomeri jedinjenja formule (I) u kojoj B jeste H, grupa C6 ili C10 aril, C7-16 aralkil; Het ili (niži alkil)-Het, svaka od njih eventualno supstituisana sa c1-6 alkilom; C1-6 alkoksi; C1-6 alkanoil; hidroksi; hidroksialkil; halogena; halogenoalkil; nitro; cijana;, cijanoalkil; amino eventualno supstituisana sa C1-6 alkilom; amido; ili (niži alkil) amid; ili, B jeste acil derivat formule R4-C(O)-; karboksil formule R4-0-C(O)-; amid formule R4-N(R5)-C(O)-; tioamid formule R4-N (R5)-C(S)-; ili sulfonil formule R4-SO2; R5 je H ili C1-6 alkil; aY jeste H ili C1-6 alkil; R3 jeste C1-8 alkil, C3-7 cikloalkil, ili C4-10 alkilcikloalkil, sve eventualno supstituisane sa grupom hidroksi, C1-6 alkoksi, C1-6 tioalkil, amida, (niži alkil) amid, C6 ili C10 aril, ili C7-16 aralkil; R2 jeste CH2 -R20, NH -R20, O -R20 ili S -R20, gde R20 jeste zasićena ili nezasićena C3-7 cikloalkil ili C4-10 (alkilcikloalkil) grupa, sve eventualno mono-, di- ili tri-supstituisane sa R21, ili, R20 jeste C6 ili C10 aril ili C17-14 aralkil grupa, eventualno supstituisane, ili, R20 jeste Het ili (niži alkil)-Het, obe eventualno supstituisane, Het ili (niži alkil)-Het; karboksil; karboksi(niži alkil); C6 ili C10 aril, C7-14 aralkil ili Het, a pomenute aril, aralkil ili Het su eventualno supstituisani; a R 1 je H; C1-6 alkil, C3-7 cikloalkil, C2-6 alkenil, ili C2-6 alkinil, sve eventualno supstituisane sa halogenom; ili njegova farmaceutski prihvatljiva 20 so ili estar. Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C 6 or C 10 aryl, C 7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C 1-6 alkyl; C 1-6 alkoxy; C 1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C 1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R 4 -C(O)-; a carboxyl of formula R 4 -O-C(O)-; an amide of formula R 4 -N( R 5 )-C(O)-; a thioamide of formula R 4 -N( R 5 )-C(S)-;or a sulfonyl of formula R 4 -SO 2 ; R 5 is H or C 1-6 alkyl; and Y is H or C 1-6 alkyl; R 3 is C 1-8 alkyl, C 3-7 cycloalkyl, or C 4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C 1-6 alkoxy, C 1-6 thioalkyl, amido, (lower alkyl)amido, C 6 or C 10 aryl, or C 7-16 aralkyl; R 2 is CH 2 - R 20 , NH- R 20 , O- R 20 or S- R 20 , wherein R 20 is a saturated or unsaturated C 3-7 cycloalkyl or C 4-10 (alkylcycloalkyl), all of which being opt