1627947-11-8Relevant articles and documents
Selective synthesis of functionalized trifluoromethylated pyrrolidines, piperidines, and azepanes starting from 1-tosyl-2-(trifluoromethyl)aziridine
Dolfen, Jeroen,Kenis, Sara,Van Hecke, Kristof,De Kimpe, Norbert,D'Hooghe, Matthias
, p. 10650 - 10653 (2014)
This paper reports on the generation and alkylation of the 1-tosyl-2-(trifluoromethyl)aziridin-2-yl anion with ω,ω′- dihaloalkanes, followed by a novel ring-expansion protocol toward 2-CF 3-pyrrolidines, 2-CF3-piperidines, and 3-CF 3-azepanes. A variety of halogen, oxygen, nitrogen, sulfur, and carbon nucleophiles was used to trigger this ring rearrangement, resulting in CF3-azaheterocycles bearing different types of functionalized side chains. CF3-azaheterocycles: The alkylation of the 1-tosyl-2-(trifluoromethyl)aziridin-2-yl anion with ω,ω′- dihaloalkanes, followed by a novel ring-expansion protocol leads to 2-CF 3-pyrrolidines, 2-CF3-piperidines, and 3-CF 3-azepanes. A variety of halogen, oxygen, nitrogen, sulfur, and carbon nucleophiles was used to trigger this ring rearrangement, resulting in CF3-azaheterocycles bearing different types of functionalized side chains (see scheme; HMPA=hexamethylphosphoramide, Ts=para-toluenesulfonyl).
CONDENSED HETEROCYCLES AS BCL-2 INHIBITORS
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Page/Page column 527; 530; 534; 537, (2021/04/10)
The disclosure includes compounds of Formula (A) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11, h, j, m, n, k, v, s, g, V, W, L, Z1 Q1, Q2, Q3, Q4, Q5, Q6, and Q7, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.
HOT MELT EXTRUDED SOLID DISPERSIONS CONTAINING A BCL2 INHIBITOR
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Page/Page column 281; 287-288, (2021/09/04)
A pro-apoptotic solid dispersion comprises, a Bcl -2 family protein inhibitory compound of Formula A as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier, and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula A, the water-soluble polymeric carrier, and the surfactant to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to provide a solid matrix comprising the polymeric carrier, and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl -2 family proteins, for example cancer or an immune or autoimmune disease.
