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TRIPEPTIDI, INHIBITORI HEPATITISA C
专利权人:
BOEHRINGER INGELHEIM (CANADA) LTD.
发明人:
SIMONEAU, BRUNO,BAILEY, MURRAY D.,LLINAS-BRUNET, MONTSE,CAMERON, DALE,FAUCHER, ANNE-MARIE,WERNIC, DOMINIK M.,GOUDREAU, NATHALIE,POUPART, MARC-ANDRÉ,RANCOURT, JEAN,TSANTRIZOS, YOULA S.,HALMOS, TEDDY,GH,SIMONEAU, Bruno,BAILEY, Murray D.,LLINAS-BRUNET, Montse,CAMERON, Dale,FAUCHER, Anne-Marie,W
申请号:
YUP9401
公开号:
RS53562B1
申请日:
1999.08.09
申请国别(地区):
YU
年份:
2015
代理人:
摘要:
A racemate, diastereoisomer and optical isomer of a compound of formula (I):wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; orB is an acyl derivative of formula R4—C(O)—; a carboxyl derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; andY is H or C1-6 alkyl;R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl;R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21,or R20 is a C6 or C10 aryl or C7-14 aralkyl optionally substituted, or R20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C6 or C10 aryl, C7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; andR1 is H; C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl, or C2-6 alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof.Postupak odvajanja enantiomerae smeše metil estra 1-amino-2-vinilciklopropil karboksilne kiseline, ili njegove N-zaštićene smeše, obuhvata korake tretiranja navedene smeše sa esterazom kako bi se dobio željeni enantiomer metil estra 1 -amino-2-vinilciklopropiI karboksilne kiseline ili njegov N-zaštitni oblik.Prijava sadrži još 7 patentih zahteva.
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