Compounds with Antiparasitic Activity, Applications thereof to the Treatment of Infectious Diseases Caused by Apicomplexans
申请人:Deligny Michael
公开号:US20100292214A1
公开(公告)日:2010-11-18
The Invention relates to compounds having an antiparasitic activity, and to their use as a drug, in particular as a drug for the prevention and/or treatment of parasitic diseases caused by apicomplexans. The invention also relates to pharmaceutical compositions containing those compounds.
The invention is novel compounds having acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitory activity of the formula I
The invention further comprises a process for the preparation of compounds of the formula I, pharmaceutical compositions containing them and the use of compounds (I) for the preparation of pharmaceutical compositions useful for treating hypercholesterolemia and atherosklerosis.
本发明是具有式 I 的酰基辅酶 A:胆固醇酰基转移酶(ACAT)抑制活性的新型化合物。
本发明还包括制备式 I 化合物、含有这些化合物的药物组合物以及使用化合物 (I) 制备用于治疗高胆固醇血症和动脉粥样硬化症的药物组合物的工艺。
[EN] COMPOUNDS WITH ANTIPARASITIC ACTIVITY, APPLICATIONS THEREOF TO THE TREATMENT OF INFECTIOUS DISEASES CAUSED BY APICOMPLEXANS<br/>[FR] COMPOSÉS PRÉSENTANT UNE ACTIVITÉ ANTIPARASITAIRE, LEURS APPLICATIONS AU TRAITEMENT DE MALADIES INFECTIEUSES PROVOQUÉES PAR DES APICOMPLEXANS
申请人:COMMISSARIAT ENERGIE ATOMIQUE
公开号:WO2008146172A2
公开(公告)日:2008-12-04
[EN] The Invention relates to compounds having an antiparasitic activity, and to their use as a drug, in particular as a drug for the prevention and/or treatment of parasitic diseases caused by apicomplexans. The invention also relates to pharmaceutical compositions containing those compounds. [FR] L'invention porte sur des composés ayant une activité antiparasitaire, et sur leur utilisation en tant que médicament, en particulier en tant que médicament pour la prévention et/ou le traitement de maladies parasitaires provoquées par des apicomplexans. L'invention également sur des compositions pharmaceutiques contenant ces composés.
Compounds with antiparasitic activity, applications thereof to the treatment of infectious diseases caused by apicomplexans
申请人:Commissariat à l'Energie Atomique
公开号:EP1997805A1
公开(公告)日:2008-12-03
The Invention relates to compounds having an antiparasitic activity, and to their use as a drug, in particular as a drug for the prevention and/or treatment of parasitic diseases caused by apicomplexans. The invention also relates to pharmaceutical compositions containing those compounds.
gem-dimethyl substitution at the four benzylic carbons of the ring on the internal dynamics of two-station [2]rotaxanes. Such structural modification of the polyamide macrocycles promotes a drastic change of the internal dynamics as shown by variable-temperature (VT) 1H NMR experiments. We determined that the shuttling rates of the octamethylated macrocycle along a series of symmetrical threads were significantly
在这项研究中,我们展示了环的四个苄基碳上的偕二甲基取代对双站[2]轮烷内部动力学的影响。变温 (VT) 1 H NMR 实验表明,聚酰胺大环的这种结构修饰促进了内部动力学的巨大变化。我们确定,与未取代的环相比,八甲基化大环沿着一系列对称线的穿梭速率明显更快。这种效果在基于富马酰胺的系统中尤其明显,其速率比模型系统快 27 倍。