155581-88-7Relevant articles and documents
NEW ANALOGS AS ANDROGEN RECEPTOR AND GLUCOCORTICOID RECEPTOR MODULATORS
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Paragraph 0289; 0290; 0291; 0293; 0294, (2019/05/16)
The present invention relates to novel dihydropyridine derivatives of formula (I): as modulators of nuclear receptors selected from androgen receptor and glucocorticoid receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by modulation of androgen receptor and/or glucocorticoid receptor, selected from cancer, metastasizing cancers, benign prostate hyperplasia, polycystic ovary syndrome (PCOS), hair loss, hirsutism, acne, hypogonadism, muscle wasting diseases, cachexia, Cushing's syndrome, anti-psychotic drug induced weight gain, obesity, post-traumatic stress disorder and alcoholism.
New variant of the Pfizinger reaction. Synthesis and chemical transformations of substituted 2-aminomethyl-quinoline-3,4-dicarboxylic acids
Kravchenko, Dmitri V.,Kysil, Volodymyr M.,Tkachenko, Sergey E.,Maliarchouk, Sergey,Okun, Ilya M.,Ivachtchenko, Alexandre V.
, p. 15 - 18 (2007/10/03)
We present a convenient synthesis of novel 8-sulfonyl-4-(morpholin-4-ium-4- ylmethyl)-1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines using a modification of the classical Pfitzinger reaction. According to our method, the 5-sulfonylated isatins were reacted with a mixture of ethyl 4-chloro-3- oxobutanoate and morpholine. The resulting quinoline-3,4-dicarboxylic acids were then successively converted into the corresponding furo[3,4-c]quinoline-1,3- diones and pyrrolo[3,4-c]quinoline-1,3-diones. The latters appeared to be effective nonpeptide inhibitors of caspase-3 enzyme.
