- NOVEL SUBSTITUTED PIPERAZINE AMIDE COMPOUNDS AS INDOLEAMINE 2, 3-DIOXYGENASE (IDO) INHIBITORS
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Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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- A 4, 7 - diaza spiro [2.5] octane -7 - formic acid tert-butyl synthetic method
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The invention belongs to the technical field of chemical synthesis of N-heterocycle-containing drug intermediates, and particularly relates to a synthesis method of tert-butyl 4,7-diazaspiro[2.5]octyl-7-formate. By using diethyl malonate as a raw material, cyclization reaction, Hofmann reaction, hydrolysis reaction, acylation reaction for recyclization, reduction reaction and the like are performed to conveniently synthesize the target compound product. The method has the advantages of simple synthesis technique, cheap and accessible raw materials, mild reaction conditions, high controllability, low cost and high yield, and is convenient to operate.
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Paragraph 0050; 0051; 0067; 0068
(2019/01/08)
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- IMIDAZOTHIAZOLE DERIVATIVE HAVING 4,7-DIAZASPIROY2.5¨OCTANE RING STRUCTURE
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There is provided a novel compound that inhibits the interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. The present invention provides an imidazothiazole derivative represented by the following formula (1) having various substituents that inhibits the interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity: wherein R1 R2, R3, R4, R5, Ar1, and Ar2 in formula (1) each have the same meanings as defined in the specification.
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Page/Page column 97-98
(2011/04/18)
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