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Inhibitors with cyclopentadiene derivatives
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
ALVAREZ SANCHEZ, RUBEN,BANNER, DAVID,CECCARELLI, SIMONA M.,GRETHER, UWE,HAAP, WOLFGANG,HILPERT, HANS,KUEHNE, HOLGER,MAUSER, HARALD,PLANCHER, JEAN-MARC
申请号:
PE2011002052
公开号:
PE20120537A1
申请日:
2010.06.08
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
A compound made from a derivative of cyclopentadiene (I),WHERE A1 IS ABSENT OR OXYGEN, CH2O, CH2, CARBONYL, CONR11; R1 IS H, CARBOXY, MORPHOLINYL, PIPERIDINYL, AMONG OTHERS; R2 IS H; R3 and R4 ARE H, C1-C8 ALKYL, PHENYL; R5 IS C1-C8 ALKYL, PHENYL, NAPHTHYL, AMONG OTHERS; R11 IS H OR C1-C8 ALKYL. THEY ARE PREFERRED COMPOUNDS: CYANOMETHYL-AMIDE ACID (1R, 2R, 4R) -4-BENZENOSULFONYL-2- (MORPHOLINE-4-CARBONYL) -CYCLOPENTANOCARBOXYLIC, (1-CIANO-CICLOPROPIL) -AMID ACID (1R, 2R ) -4-BENZENOSULFONYL-2- (MORPHOLINE-4-CARBONYL) -CYCLOPENTANOCARBOXYLIC, CYANOMETHYL-AMIDE ACID (1R, 2R, 4R) -4- (2-CHLORINE-BENZENE-SULPHONYL) -2- (MORPHOLINE-4- CARBONIL) -CYCLOPENTANOCARBOXILICO,There are others A preparation procedure and a drug synthesis were also mentioned. These compounds are inhibitors of velvet protein S or L, and are effective tools for the treatment of diabetes, carcinogenicity, diabetes nefropatia, etc.REFERIDA A UN COMPUESTO DERIVADO DE CICLOPENTANO DE FORMULA (I), DONDE A1 ESTA AUSENTE O ES OXIGENO, CH2O, CH2, CARBONILO, CONR11; R1 ES H, CARBOXI, MORFOLINILO, PIPERIDINILO, ENTRE OTROS; R2 ES H; R3 Y R4 SON H, ALQUILO C1-C8, FENILO; R5 ES ALQUILO C1-C8, FENILO, NAFTILO, ENTRE OTROS; R11 ES H O ALQUILO C1-C8. SON COMPUESTOS PREFERIDOS: CIANOMETIL-AMIDA DEL ACIDO (1R,2R,4R)-4-BENCENOSULFONIL-2-(MORFOLINA-4-CARBONIL)-CICLOPENTANOCARBOXILICO, (1-CIANO-CICLOPROPIL)-AMIDA DEL ACIDO (1R,2R,4R)-4-BENCENOSULFONIL-2-(MORFOLINA-4-CARBONIL)-CICLOPENTANOCARBOXILICO, CIANOMETIL-AMIDA DEL ACIDO (1R,2R,4R)-4-(2-CLORO-BENCENO-SULFONIL)-2-(MORFOLINA-4-CARBONIL)-CICLOPENTANOCARBOXILICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA CISTEINA-PROTEASA CATEPSINA S O L Y SON UTILES EN EL TRATAMIENTO DE LA DIABETES, ATEROSCLEROSIS, NEFROPATIA DIABETICA, ENTRE OTRAS
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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