- OGA INHIBITOR COMPOUNDS
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The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors having the structure shown in formula (I). The invention is also directed to pharmaceutical compositions comprising such compounds to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations. wherein RB is an aromatic heterobicyclic radical selected from the group consisting of (b-1) to (b-6).
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Page/Page column 49-50
(2020/01/11)
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- Preparation method of 2, 6-dimethyl-3, 5-dichloro-4-hydroxypyridine
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The invention discloses a preparation method of 2, 6-dimethyl-3, 5-dichloro-4-hydroxypyridine.The preparation method includes: using ethyl acetoacetate as raw material and weak-base ion-exchange resin as catalyst to perform dimerization reaction under 25-90 DEG C, adding water and feeding ammonia gas to perform ammoniation at 10-45 DEG C after the reaction, feeding chlorine to perform chlorination, and performing post treatment on reaction liquid to obtain the 2, 6-dimethyl-3, 5-dichloro-4-hydroxypyridine.The preparation method has the advantages that the method uses the weak-base ion-exchange resin as the catalyst and the ethyl acetoacetate as the raw material to prepare the target product through the serial connection technology, unit reaction is simplified, easiness in operation and post treatment in the reaction process is achieved, the product can be obtained only by filtering the reaction liquid, recycling the catalyst of the filter cake and recrystallizing the filtrate after the reaction, the yield can reach 91.5%, and the preparation method is simple in product separation and purification, free of pollution and green.
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Paragraph 0009; 0020; 0021
(2016/10/10)
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- Antiprotozoal agents
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Novel combinations of an antiprotozoal naphthoquinone and a 4-pyridinol or an alkanoic ester thereof wherein the antiprotozoal activity of the combination is potentiated with respect to the corresponding activity of the components of the combination. The combinations are especially useful for the treatment or porphylaxis of malaria.
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- Process for formulating a synthetic drug for use in animal feed, and resulting formulation
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A method of formulating a synthetic drug for use in animal feed, for the purpose of reducing carry-over of the synthetic drug to subsequent lots of animal feed in the feed mill.
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