- 专利标题： USE OF AVERMECTIN DERIVATIVE FOR INCREASING BIOAVAILABILITY AND EFFICACY OF MACROCYLIC LACTONES
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申请号： EP19215890.5申请日： 2012-10-18
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公开(公告)号： EP3701954A2公开(公告)日： 2020-09-02
- 发明人: LESPINE, Anne , PRICHARD, Roger , MENEZ, Cécile
- 申请人： Institut national de recherche pour l'agriculture, l'alimentation et l'environnement , The Royal Institution for the Advancement of Learning / McGill University
- 申请人地址： 147, rue de l'Université 75338 Paris Cedex 07 FR
- 专利权人： Institut national de recherche pour l'agriculture, l'alimentation et l'environnement,The Royal Institution for the Advancement of Learning / McGill University
- 当前专利权人： Institut national de recherche pour l'agriculture, l'alimentation et l'environnement,The Royal Institution for the Advancement of Learning / McGill University
- 当前专利权人地址： 147, rue de l'Université 75338 Paris Cedex 07 FR
- 代理机构： Schiweck Weinzierl Koch Patentanwälte Partnerschaft mbB
- 优先权： EP11306348 20111018
- 主分类号： A61K31/7048
- IPC分类号： A61K31/7048 ; A61P33/00 ; A61P35/00 ; A61P31/12 ; A61P25/08
摘要：
The present invention relates to the use of avermectin derivative as a drug for the treatment of parasitic infections. The avermectin derivative is represented by the formula I
wherein:
(i) R 1 is chosen from the group constituted of -CH(CH 3 ) 2 , -CH(CH 3 )CH 2 CH 3 , or cyclohexyle,
(ii) X represents -CH 2 -CH 2 -, or -CH=CH-,
(iii) R 2 is chosen from the group constituted of
or -OH group,
(iv) R 3 is OH or NOH,
(v) ----- represents a single bond when R 3 is OH, or a double bond when R 3 is NOH,
as an inhibitor of a membrane-bound protein which transports exogenous compounds out of target cells.
wherein:
(i) R 1 is chosen from the group constituted of -CH(CH 3 ) 2 , -CH(CH 3 )CH 2 CH 3 , or cyclohexyle,
(ii) X represents -CH 2 -CH 2 -, or -CH=CH-,
(iii) R 2 is chosen from the group constituted of
or -OH group,
(iv) R 3 is OH or NOH,
(v) ----- represents a single bond when R 3 is OH, or a double bond when R 3 is NOH,
as an inhibitor of a membrane-bound protein which transports exogenous compounds out of target cells.
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