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。
Polyene macrolide derivative
申请人:Shionogi & Co., Ltd.
公开号:US10246478B2
公开(公告)日:2019-04-02
The present invention is the following Amphotericin B derivative:
wherein each symbol is defined in description. The compound of the present invention has 16th position (X) is urea structure, cyclic structure, hydroxyalkyl or substituted monoalkylcarbamoyl. The compound of the present invention has antifungal activity.
本发明是以下两性霉素 B 衍生物:
其中各符号在说明中定义。本发明化合物的第 16 位(X)是脲结构、环状结构、羟烷基或取代的单烷基氨基甲酰基。本发明化合物具有抗真菌活性。
Blocking toll-like receptor 9 signaling with small molecule antagonist
申请人:Council of Scientific & Industrial Research
公开号:US10662177B2
公开(公告)日:2020-05-26
The present invention relates to small molecule 4-(piperazin-1-yl)quinazolin-2-amino compounds with formula (I) useful for inhibiting signalling by certain toll-like receptors (TLRs), especially TLR9. Toll-like receptors (TLRs) are members of the larger family of evolutionarily conserved pattern recognition receptors which are critical first line of defense for self-nonself discrimination by the host immune response. Aberrant TLR9 activation is implicated in autoreactive inflammation in different autoimmune diseases. The invention depicts compounds with formula (I), composition and methods can be used in a number of clinical applications, including as pharmaceutical agents and methods for treating conditions involving unwanted immune activity due to TLR9 activation.
[EN] CYANO-SUBSTITUTED PYRIDINE AND CYANO-SUBSTITUTED PYRIMIDINE COMPOUND, AND PREPARATION METHOD AND APPLICATION THEREOF<br/>[FR] COMPOSÉ DE PYRIDINE À SUBSTITUTION CYANO ET COMPOSÉ DE PYRIMIDINE À SUBSTITUTION CYANO, PROCÉDÉ DE PRÉPARATION CORRESPONDANT ET UTILISATION ASSOCIÉE<br/>[ZH] 一种氰基取代吡啶及氰基取代嘧啶类化合物、制备方法及其应用
The present invention is the following Amphotericin B derivative:
wherein each symbol is defined in description. The compound of the present invention has 16th position (X) is urea structure, cyclic structure, hydroxyalkyl or substituted monoalkylcarbamoyl. The compound of the present invention has antifungal activity.