CAS: 22179-78-8; 4-Fluoro-N-Hydroxybenzimidamide

上下游产品

4-fluorobenzonitrile 1-Bromo-4-fluorobenzene 4-fluorobenzaldehyde 4-fluorobenzaldoxime O-(4,4-Dinitropentanoyl)-4-fluorobenzamidoxime 3-(4-fluorophenyl)-1,2,4-oxadiazole-5-carbohydrazide 4-[3-(4-fluoro-phenyl)-[1,2,4]oxadiazol-5-yl]-phenol 3-(4-Fluorophenyl)-1,2,4-oxadiazol-5(4H)-one

对氟苯腈置于羟胺体系中,化学反应 4.0H,反应生成4-氟苯甲酰胺肟
参考文献:N-酰基hydr和1,2,4-恶二唑的缀合导致活性抗疟药的鉴定
标题:N-酰基hydr和1,2,4-恶二唑的缀合导致活性抗疟药的鉴定
摘要:由几种疟原虫引起的疟疾是全球范围内威胁生命的主要寄生虫感染.由于寄生虫对喹啉类药物有抗药性,因此有必要寻找抗疟药.在这里,我们报告两个新的1,2,4-恶二唑系列与n-酰基azo偶合物的结构设计,合成和抗寄生虫评价,两个组均被认为是特权结构,以及对16个抗疟活性的研究.描述的类似物.与未取代的衍生物相比,通过改变连接在苯环上的取代基,可以保留,增强或增加抗寄生虫活性.N中连接的二茂铁基和肉桂基部分取代取代的芳基环-酰基hydr消除了抗寄生虫反应,证明了与活性有关的结构特征.活性化合物显示出与甲氟喹相似的体外效价,但并非全部抑制β-血红素的形成.此外,活性化合物在hepg2细胞中显示出低细胞毒性,并且在未感染的红细胞中不会引起溶血.与氯喹相比,在伯氏疟原虫感染的小鼠中,该化合物减少了寄生虫血症,但在增加小鼠存活率方面显示出有限的功效,这表明仍需要药理学方面的改进.
Doi:10.1016/j.Bmc.2016.09.013

专利信息

专利号:US-8772301-B2
优先权日:2009-12-18
标题 :Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
发明人：HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D
权利人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D; SUNOVION PHARMACEUTICALS INC
摘要:Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

专利号:US-2019152962-A1
优先权日:2016-07-14
标题 :Cyclopropyl derivatives as ror-gamma modulators
发明人：DESAI RANJIT; KUMAR SANJAY S; PANDYA VRAJESH; DESAI JIGAR; RAVAL SAURIN
权利人:CADILA HEALTHCARE LTD
摘要:The present invention provides compounds which are modulators of RORγ and their use for the treatment of diseases or conditions mediated by RORγ. Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them (Formula I).