Novel amides and esters prodrugs of olmesartan: Synthesis, bioconversion, and pharmacokinetic evaluation
摘要:
Synthesis of novel amides and esters prodrugs of olmesartan is described. Their in vitro stability in rat plasma was tested. The results showed that the ester derivative IIa with n-octyl substituted dioxolone moiety was rapidly converted into olmesartan within 30 min. The pharmacokinetic parameters of IIa were studied and compared with those of olmesartan medoxomil. Compound IIa is proposed to be a promising prodrug of olmesartan. (C) 2010 Published by Elsevier Ltd.
Novel amides and esters prodrugs of olmesartan: Synthesis, bioconversion, and pharmacokinetic evaluation
摘要:
Synthesis of novel amides and esters prodrugs of olmesartan is described. Their in vitro stability in rat plasma was tested. The results showed that the ester derivative IIa with n-octyl substituted dioxolone moiety was rapidly converted into olmesartan within 30 min. The pharmacokinetic parameters of IIa were studied and compared with those of olmesartan medoxomil. Compound IIa is proposed to be a promising prodrug of olmesartan. (C) 2010 Published by Elsevier Ltd.
Novel diamine compounds, production of the same and polyamideimide
申请人:Tomoegawa Paper Co., Ltd.
公开号:US05019642A1
公开(公告)日:1991-05-28
A diamine compound represented by general formula (I): ##STR1## wherein R is as defined in the specification a group of formula (II) ##STR2## where R.sup.1 and R.sup.2 as defined in the specification or a group of formula (III) ##STR3## where R.sup.1 and R.sup.2 have the same meanings as defined above, and Z is as defined in the specification, or --SO.sub.2 --. The diamine compound is produced by reducing a dinitro compound of general formula (IV) ##STR4## wherein R has the same meaning as defined above. Imidation of the diamine compound with a tetracarboxylic acid dianhydride produces a polyamideimide resin having a repeating unit represented by general formula (V): ##STR5## wherein Ar and Ar.sup.1, which are as defined in the specification R.sup.3 is a group of general formula (VI) below: ##STR6## where R has the same meaning as defined above; R.sup.4 is as defined in the specification and m and n are each zero or a positive integer which satisfy m.gtoreq.2n.
Novel diamine compounds, production of the same and polyamideimide resins produced therefrom
申请人:TOMOEGAWA PAPER CO. LTD.
公开号:EP0387106B1
公开(公告)日:1994-02-02
US5019642A
申请人:——
公开号:US5019642A
公开(公告)日:1991-05-28
Novel amides and esters prodrugs of olmesartan: Synthesis, bioconversion, and pharmacokinetic evaluation
作者:Jin-Hun Park、Jeong-Soo Chang、Mohammed I. El-Gamal、Won-Kyoung Choi、Woong San Lee、Hye Jin Chung、Hyun-Il Kim、Young-Jin Cho、Bong Sang Lee、Hong-Ryeol Jeon、Yong Sup Lee、Young Wook Choi、Jaehwi Lee、Chang-Hyun Oh
DOI:10.1016/j.bmcl.2010.07.089
日期:2010.10
Synthesis of novel amides and esters prodrugs of olmesartan is described. Their in vitro stability in rat plasma was tested. The results showed that the ester derivative IIa with n-octyl substituted dioxolone moiety was rapidly converted into olmesartan within 30 min. The pharmacokinetic parameters of IIa were studied and compared with those of olmesartan medoxomil. Compound IIa is proposed to be a promising prodrug of olmesartan. (C) 2010 Published by Elsevier Ltd.