- Sedinafine derivatives of the microwave-assisted method for preparing
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The invention discloses a microwave-assisted synthesis method of sildenafil derivatives, which mainly comprises the following steps: by using 2-alkoxybenzoic acid and 4-amino-1-methyl-3-n-propyl-1H-pyrazolyl-5-formamide as initial raw materials, carrying out amidation, cyclization, mononitration, nitro reduction, guanidylation and the like to obtain the sildenafil derivatives. The method greatly shortens the reaction time, enhances the reaction efficiency, has the advantages of high yield and high purity, is simple to operate and easy to control, and is beneficial to industrial production of sildenafil analogs.
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Paragraph 0071
(2016/12/07)
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- A NANOSPHERE - HISTONE ACETYLTRANSFERASE (HAT) ACTIVATOR COMPOSITION, PROCESS AND METHODS THEREOF
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The present disclosure is in relation to a composition comprising nanosphere and histone acetyltransferase (HAT) activator. The disclosed nanosphere is carbon nanosphere (CSP) which is intrinsically fluorescent and the HAT activator is N-(4-Chloro-3-trifluoromethyl- phenyl)-2-n-propoxy-benzamide [COMPOUND 1]. The said N-(4-Chloro-3-trifluoromethyl- phenyl)-2-n-propoxy-benzamide is covalently conjugated with the carbon nanosphere. The present disclosure further relates to a process for obtaining a composition comprising carbon nanosphere and Histone acetyltransferase (HAT) activator [N-(4-Chloro-3-trifluoromethyl- phenyl)-2-n-propoxy-benzamide]. The composition is capable of crossing blood brain barrier and inducing histone acetylation in brain. Further, the composition is capable of increasing neurogenesis, as well as improving long-term memory formation. The said composition thus provides for managing pathological conditions to a subject in need thereof, such as aging- related, neurodegenerative diseases (Alzheimer's in particular), neurological disorders, depression or other kinds of diseases in which increased HAT activity, neurogenesis and/or memory improvement would benefit.
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Page/Page column 16
(2013/11/18)
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- Modulators (inhibitors/ activators) of histone acetyltransferases
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Disclosed are compounds of the formulae: and method of using the compounds to treat cancer, AIDS, HIV infection, and asthma.
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Page/Page column 4
(2008/06/13)
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