9 results about "Benzisoxazole" patented technology

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system diseases. Pharmaceutical compositions and methods of making various benzisoxazole and benzisothiazole compounds are provided. These compounds are considered to be modulators of the serotonin 2A (5-HT2A) receptor.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system diseases. Pharmaceutical compositions and methods of making various benzisoxazole and benzisothiazole compounds are provided. These compounds are considered to be modulators of the serotonin 2A (5-HT2A) receptor.

The application provides a benzene [d] isoxazole compound and an application thereof. The compound has the structure shown in the following formula I. The benzene [d] isoxazole compound provided by the application can induce degradation of BET protein and / or GSPT1 protein, and has an anti-proliferation effect on cancer cells. Therefore, the compound and the composition provided by the application can be used for preparing a drug for treating or preventing tumor formation, inflammation, viral infection, cell proliferative disorder, autoimmune disease, sepsis and the like.

The present invention relates to compounds of formula (I)or pharmaceutically acceptable salts thereof, wherein Ring A, R1-R8, and n are defined herein. The novel benzisoxazole sulfonamide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in patients. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in patients.

The invention relates to a compound for use in a method of treating or preventing a KMO mediated disorder in a subject in need thereof; wherein said compound is a benzisoxazole of formula (I) or a pharmaceutically acceptable salt thereof, wherein said method comprises administering said compound to the subject as an intravenous infusion at a dose rate of between about 200 µg / h and about 2.5 mg / h for a period of at least 12 hours.

The invention discloses a preparation method of a 2-substituted quinazoline derivative, which comprises the following step: heating and stirring three components, namely an ammonium salt, a benzyl alcohol compound and a 2, 1-benzisoxazole compound in an organic solvent to obtain the 2-substituted quinazoline derivative. According to the method, ammonium iodide which is low in price and easy to obtain is used as a nitrogen source and an oxidizing agent, benzyl alcohol is used as a carbon source, and efficient construction from a 2, 1-benzisoxazole skeleton to a 2-substituted quinazoline skeleton is achieved through a carbon-nitrogen diatom inserted ring expansion reaction under the mild conditions of no metal and no additive. The synthetic method developed by the invention has a good application prospect in the industrial fields of biological medicines, pesticides and the like, and is particularly suitable for efficiently preparing the quinazoline compound with biological activity under simple and convenient conditions. The synthetic method developed by the invention has a good application prospect in the industrial fields of biological medicines, pesticides and the like, and a theoretical basis is provided for commercialized application of the derivatives in the field of medicines.

The invention relates to the technical field of preparation of quinazolinone derivatives. The invention provides a method for preparing a quinazolinone derivative, which comprises the following steps of: adding a compound with a general formula 1, benzisoxazole, 2, 3-dichloro-5, 6-dicyanobenzoquinone and cuprous iodide into 1, 2-dichloroethane to react, and the chemical equation of the reaction is shown in the specification; wherein R is hydrogen, methyl, ethyl or methoxyl. The method provided by the invention takes copper as a catalyst, and has the characteristics of high stereoselectivity and single product geometric configuration. The copper catalyst is cheap and low in toxicity, and meets green chemical requirements; reaction conditions are mild, and industrial amplification is easy; meanwhile, by-products are few, and atom economy is good.

This disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azaphen-4-yl)acetamide or a pharmaceutically acceptable salt thereof for the treatment of thrombocytosis.

The application belongs to the technical field of organic synthesis, and particularly relates to an amino nitrile compound with a remote chiral center and a preparation method and application thereof. The nickel-hydrogen catalytic asymmetric hydrogenation reaction provided by the application is realized through non-covalent pi-pi interaction between a cyano group in an olefin substrate and a chiral bisoxazoline ligand. The method not only realizes efficient and high-selectivity conversion of various olefin substrates and amine electrophilic reagents, but also is compatible with secondary alkyl amine electrophilic reagents, amide electrophilic reagents and benzisoxazole electrophilic reagents, thereby providing a reliable way for synthesizing chiral amino nitrile compounds (formula I) with a remote (beta-, gamma- and delta-) stereogenic center and various structures.