59133-48-1

Upstream product

• 56464-51-8 3-(cyanomethylamino)-1-phenyl-2-buten-1-one 
• 93-91-4 1-phenylbutan-1,3-dione 
• 540-61-4 2-aminoacetonitrile 
• 56464-51-8 2-[(4-oxo-4-phenylbut-2-en-2-yl)amino]acetonitrile 

Relevant academic research and scientific papers

PYRROLO- AND PYRAZOLO-TRIAZOLODIAZEPINES AS BET-PROTEIN INHIBITORS FOR TREATING HYPERPROLIFERATIVE DISEASES

What is described are BET protein-inhibitory, especially BRD2-, BRD3- and BRD4-inhibitory, bicyclo- and spino-substituted pyrrolo- and pyrazolodiazepines of the general formula I in which X, Y, n, m, R1, R2, R3, R4 and R5 are each as defined in the description, to intermediates for preparation of the inventive compounds, to pharmaceutical compositions comprising the inventive compounds, and to the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for tumour disorders. Also described is the use of the compounds according to the invention as BET protein inhibitors for benign hyperplasias, for atherosclerotic disorders, for sepsis, for autoimmune disorders, for vascular disorders, for viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for male fertility control.

4-SUBSTITUTED PYRROLO- AND PYRAZOLO-DIAZEPINES

BET protein-inhibitory, especially BRD2-, BRD3- and BRD4-inhibitory, 4-substituted pyrrolo- and pyrazolodiazepines of the general formula I are described, in which X, Y, n, m, p, R1, R2, R3, R4 and R5 are each as defined in the description, as are pharmaceutical compositions comprising the inventive compounds, and the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of neoplastic disorders. Also described is the use of the inventive compounds as BET protein inhibitors in benign hyperplasias, in atherosclerotic disorders, in sepsis, in autoimmune disorders, in vascular disorders, in viral infections, in neurodegenerative disorders, in inflammatory disorders and in male fertility control.

Aminopyrrole derivatives

Pharmacologically-active aminopyrrole derivatives of the formula STR1 wherein: R is selected from hydrogen, (C1-4)alkyl, benzyl and chlorobenzyl; R1 is selected from hydrogen, (C1-4)alkyl, phenyl and phenyl substituted by a radical selected from methyl, ethyl, methoxy, ethoxy, benzyloxy, fluoro, chloro and bromo; R2 and R3 individually represent hydrogen or (C1-4)alkyl or, taken together, represent an isopropylidene, a benzylidene or a chlorobenzylidene radical; R4 is selected from (C2-4)alkanoyl; carbo(C1-3)alkoxy; benzoyl, benzoyl substituted by a radical selected from chloro, methoxy or ethoxy; carbamoyl, methylcarbamoyl and phenyl carbamoyl; R5 is selected from hydrogen, (C1-4)alkyl, carbo(C1-3)alkoxy, carbomethoxymethyl, carbethoxymethyl, trifluoromethyl and carbamoyl, with the proviso that when R is hydrogen, R1 and R5 are methyl and R4 is carbethoxy, R2 and R3 cannot simultaneously represent hydrogen; And a salt thereof with a pharmaceutically acceptable acid. The compounds have anti-inflammatory and CNS-depressant utility. They are also useful as analgesics and antipyretics and display a very low degree of anti-ulcerogenic activity.