发明名称 NEW MACROCYCLIC AMIDINOUREA DERIVATIVES, METHODS OF PREPARATION AND USES THEREOF AS CHITINASE INHIBITORS
摘要 The present invention relates to macrocyclic amidinourea derivatives of formula 8, methods of preparation and uses thereof, pharmaceutical compositions in particular to be used as chitinase inhibitors in the treatment of a fungal infection.;
申请公布号 US2016137617(A1) 申请公布日期 2016.05.19
申请号 US201414899872 申请日期 2014.06.18
申请人 CYGNET BIOSCIENCES B.V. 发明人 SANFILIPPO Stefania;POSTERARO Brunella;SANGUINETTI Maurizio;BOTTA Maurizio;MACCARI Giorgio;DE LUCA Filomena;DOCQUIER Jean-Denis;DEODATO Davide
分类号 C07D273/00;C07C271/20;C07D413/04;A61K31/4192;A61K31/395;A61K45/06 主分类号 C07D273/00
代理机构 代理人
主权项 1. A compound having the general formula 8: wherein n1 is a number from 0 to 4;n2 is a number from 1 to 7;R1 is H; linear or branched C1-C6 alkyl; propargyl, cyclopropylmethyl, but-2-en-1-yl, γ-methylallyl, β-methylallyl, γ,γ-dimethylallyl, benzyl, allyl, pyridin-ylmethyl;methylcarbamoyl, ethylcarbamoyl, propylcarbamoyl, or prop-2-enylcarbamoyl;R2 is H or R3 is OH, nitro, NH2, NHR8, NR9R10, C1-C6 alkyl, COOH, CONH2, CONR11H, CONR12R13, cyano, F, Cl, Br;wherein R8, R9, R10, R11, R12, R13, are the same or each independently C1-C6 alkyl, methylcyclopropyl or propan-2-yl;X is CH2 or C(=0);Y is CH2,or X—Y is wherein R4, R5, R6, R7 are the same or each independently H, OH, nitro, NH2, NHR14, NR15R16, C1-C6 alkyl, COOH, CONH2, CONR17H, CONR18R19, cyano, F, Cl, Br;wherein R14, R15, R16, R17, R18, R19 are the same or each independently C1-C6 alkyl, methylcyclopropyl or propan-2-yl;Z is CH2, or pharmaceutically acceptable salts thereof.
地址 Willemstad CW