NOVEL ANTIOGENESIS INHIBITING COMPOUNDS AND USE THEREOF

FIELD: chemistry. ^ SUBSTANCE: invention relates to compounds of formula (I) , where D is pyrrolidine, X is a radical selected from a group containing C=O, SO2, (C=O)-NH, CH2, O-(C=O), (C=O)-O, (C=S)-NH, Y is a radical selected from a group containing - (CH2)n-E-(CH2)m-L-(CH2)k, where E is O, k, m a...

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Hauptverfasser: KHUMMEL' GERD, SHTRAGIS ROLAND, OSTERKAMP FRANK, KNOLLE JOKHEN, RAJNEKE UL'RIKH, TSISHINSKI GUNTER, TSAN GRIT, BIRKNER SASHA
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: chemistry. ^ SUBSTANCE: invention relates to compounds of formula (I) , where D is pyrrolidine, X is a radical selected from a group containing C=O, SO2, (C=O)-NH, CH2, O-(C=O), (C=O)-O, (C=S)-NH, Y is a radical selected from a group containing - (CH2)n-E-(CH2)m-L-(CH2)k, where E is O, k, m and n are separately and independently equal to 0, 1, 2 and 3, Z is an alkyl, where the alkyl is CH2 or CH2CH2, A is a radical selected from a group containing benzyl, substituted benzyl, phenyl, substituted phenyl, alkyl and substituted alkyl, cycloalkyl, heterocyclyl, aryl, alkyloxyalkyl, substituted alkyloxyalkyl, alkyloxyaryl, B is a radical of formula (II) , where R1 is selected from a group containing H, alkyl and substituted alkyl, cycloalkyl, R2 is selected from a group containing H, benzyl, substituted benzyl, phenyl, substituted phenyl, alkyl and substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, substituted cycloalkylalkyl, G is an amino group which is substituted by a heteroaryl or substituted heteroaryl, and where Q and L each independently denotes a radical selected from a group containing (C=O)-NH, NH, CH2, NH-(C=O)-NH, NH-(C=O), NH-SO2, NRc, (C=O)-NRc, and where Ra, Rb, Rc and Rd each independently denotes a radical selected from a group containing H, alkyl, cycloalkyl, heterocyclyl, aryl, substituted aryl, as well as to use of these compounds as integrin inhibitor and for making a medicinal and a diagnostic agent, to a pharmaceutical composition based on these compounds and to methods of treating integrin-associated condition. ^ EFFECT: novel compounds which are integrin inhibitors and can be used to treat diseases where angiogenesis inhibition is necessary are obtained and described. Изобретение относится к соединениям структуры (I) , где D представляет собой пирролидин, X представляет собой радикал, выбранный из группы, содержащей С=O, SO2, (C=O)-NH, СН2, O-(С=O), (С=O)-O, (С=S)-NH, Y представляет собой радикал, выбранный из группы, содержащей - (СН2)n-Е-(СН2)m-L-(СН2)k, где Е представляет собой О, k, m и n отдельно и независимо представляют собой 0, 1, 2 и 3, Z представляет собой алкил, где алкил представляет собой СН2 или СН2СН2, А представляет собой радикал, выбранный из группы, содержащей бензил, замещенный бензил, фенил, замещенный фенил, алкил и замещенный алкил, циклоалкил, гетероциклил, арил, алкилоксиалкил, замещенный алкилоксиалкил, алкилоксиарил, В представляет собой радикал формулы (II) ! где R