STEFAN DR. BURLE,STEPHAN DR. SIEGEL,BERNARD DR. HAENDLER,AMAURY ERNESTO DR. FERNANDEZ-MONTALVAN,URSULA DR. MNNING,SABINE DR. KRAUSE,PASCALE DR. LEJEUNE,NORBERT DR. SCHMEES,MATTHIAS DR. BUSEMANN,SIMON
申请号:
ARP130102888
公开号:
AR092129A1
申请日:
2013.08.14
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
It is suggested that 2,3-benzodiazepine is a beta protein inhibitor, especially Brd4 inhibitor, an intermediate product for the manufacture of compounds, a pharmaceutical containing compounds, as well as a preventive and therapeutic use in highly proliferative diseases, Especially tumor diseases In addition, the report also describes the use of B protein inhibitors in benign hyperplasia, material diseases, septicemia, autoimmune diseases, vascular diseases, viral infections, neurodegenerative diseases and inflammation.in atherosclerotic diseases and in the control of male fertility. Claim 1: Compounds of general formula (1) wherein X represents an oxygen or sulfur atom, and A represents a monocyclic heteroaryl ring with 5 or 6 ring atoms or represents a phenyl ring, and R¹ᵃ represents hydrogen, halogen, cyano, carboxy, amino or aminosulfonyl, or represents a C₁₋₆ alkoxy moiety,alcoxi C -alquilo CC₁₋₃ alkoxy-C₂₋₃ alkoxy,alquil C -amino alquil C -carbonilamino alquil C -amino-alquilo CN - (heterosexual) - c832131 asphalt;N - (heterosexual) - alcox c832131;hydroxy-C₁₋₆ alkyl,hydroxy C₁₋₆ alkoxy,halo-C₁₋₆ alkyl,hello-alcoxi C₁₋₆,e. C83218316c26g carbide or alcoxi c83321c83183326a carbide, or a single ring isomerization residue with 3 to 8 ring atoms. If necessary, halogen, cyanogen, nitrogen, hydroxyl, amino, oxo, carboxi, c8332121c8383266ct can be used to replace it once or more;C₁₋₆ alkoxy,C₁₋₆ alkoxy-C₁₋₆ alkyl,C₁₋₆ hydroxyalkyl,C₁₋₆-amino alkyl, amino-C₁₋₆ alkyl,C₁₋₆-amino-C₁₋₆ alkyl,halo-C₁₋₆ alkyl,hello-alcoxi C₁₋₆,C₃₋₁₀ cycloalkyl,1. Phenyl, halogenated phenyl, phenyl-c83218c33832626;Piridini, - No. 8310; (= O) - r8313;-C (3DO) -NR R-C (3DO) -R-S (3DO) -NR R-S (3DO) -R-S (3DO) -R-Nh-s (= O) c8322-r8313 and / or monocyclic isomerization consisting of 3 to 8 ring atoms, or representing monocyclic isomerization consisting of 5 to 6 ring atoms, which can be replaced once or more by halogen, hydroxyl, amino, cyanogen, nitrogen, carboxi, c831836262 tar in the same or d