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APPLICATION OF CXCR4 ANTAGONISTS
专利权人:
ЮНИВЕРСИТИ ОФ ВАШИНГТОН (US);ДЖЕНЗИМ КОРПОРЕЙШН (US)
发明人:
ДЕЙЛ Дэвид К. (US),БРИДЖЕР Гари Дж. (US),ХСУ Фрэнк Дж. (US)
申请号:
RU2013155601/15
公开号:
RU2013155601A
申请日:
2012.05.15
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
1. A method of treating or preventing WHIM syndrome in a person in need thereof, comprising administering to said person a CXCR4 antagonist in an amount effective to treat or prevent WHIM syndrome, wherein the CXCR4 antagonist is a compound of formula I, or a pharmaceutically acceptable salt or metal complex thereof where Z is a cyclic polyamine containing 9-32 ring members, of which 2-8 are nitrogen atoms, wherein said nitrogen atoms are separated from each other by at least 2 carbon atoms, and where said the erocycle may optionally contain additional heteroatoms in addition to nitrogen and / or may be fused to an additional ring system; Z ′ either represents Z or has the formula-N (R) - (CR) -X, where each R is independently H or straight, branched or cyclic alkyl (1-6C), n is 1 or 2, and X is an aromatic ring including heteroaromatic rings, or is mercaptan, or Z ′ has the formula-Ar (Y), where Ar is an aromatic or heteroaromatic fragment, and each Y is independently non-interfering with mestitelem, and j is equal to 0-3; and the “linker” is a bond, alkylene (1-6C) or may contain aryl, fused aryl, oxygen atoms contained in an alkylene chain, or may contain keto groups or nitrogen or sulfur atoms. The method according to claim 1, characterized in that Z and Z ′ are both cyclic polyamines. The method according to claim 1, characterized in that Z and Z ′ are identical. The method according to claim 1, characterized in that Z is a cyclic polyamine that contains 10-24 members and contains 4 nitrogen atoms. The method according to claim 1, characterized in that Z and Z ′ are both 1.4,1. Способ лечения или профилактики синдрома WHIM у человека, нуждающегося в этом, включающий введение указанному человеку антагониста CXCR4 в количестве, эффективном для лечения или профилактики синдрома WHIM, отличающийся тем, что антагонистом CXCR4 является соединение формулы I,или его фармацевтически приемлемая соль или металлокомплекс, гдеZ является циклическим полиамином, содержащим 9-
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