发明名称 N-CARBOXYALKYL-AURISTATIN AND USE THEREOF
摘要 The present application relates to new derivatives of monomethylauristatin F, substituted on the N terminus by a carboxyalkyl group, processes for preparing these derivatives, their use for the treatment and/or prevention of diseases and to produce medication for the treatment and/or prevention of diseases, particularly hyperproliferative and/or angiogenic disorders such as cancer disorders, for example. Such treatments can occur as monotherapies or in combination with other medication or further therapeutic measures.
申请公布号 US2015148298(A1) 申请公布日期 2015.05.28
申请号 US201514615005 申请日期 2015.02.05
申请人 SEATTLE GENETICS, INC. 发明人 LERCHEN Hans-Georg;El Sheikh Sherif;Stelet-Ludwig Beatrix;Golfier Sven;Schuhmacher Joachim;Gnoth Jean Mark;Krenz Ursula
分类号 C07K5/113 主分类号 C07K5/113
代理机构 代理人
主权项 1. Compound of the formula (I) Wherein L stands for a straight-chain (C1-C12)-alkandiyl, which may be substituted with methyl up to four times and in which (a) two carbon atoms may be connected to each other in 1,2-, 1,3- or 1,4 relation, if necessary including carbon atoms that are located between them to form a (C3-C6)-cycloalkyl-ring or a phenyl ring or (b) up to three CH2 groups not adjacent to each other may be substituted for an O, R1 stands for hydrogen or methyl, R2 stands for isopropyl, isobutyl, sec.-butyl, tert.-butyl, 1-hydroxyethyl, phenyl, benzyl, 4-hydroxybenzyl, 1-phenylethyl, diphenylmethyl, 1H-imidazol-4-ylmethyl or 1H-indol-3-ylmethyl, Or R1 and R2, together with the carbon atom to which they are both connected, form a 2-phenylcyclopropan-1,1-diyl group of the formula Wherein # marks the points of attachment with other parts of the molecule, And T stands for a group with formula —C(═O)—OR3, —C(═O)—NR4R5, —C(═O)—NH—NH—R6 or —CH2—O—R7 in which R3 stands for hydrogen, (C1-C6)-alkyl or (C3-C10)-cycloalkyl, wherein (C1-C6)-alkyl may be substituted with phenyl, naphthyl or (C3-C10)-cycloalkyl,R4 stands for hydrogen or (C1-C6)-alkyl,R5 stands for hydrogen, (C1-C6)-alkyl or (C3-C10)-cycloalkyl, wherein (C1-C6)-alkyl may be substituted with phenyl,OrR4 and R5 are connected to each other and, together with the nitrogen atom they are attached to, form a 5- to 7-membered, saturated aza-heterocyclic compound, which may contain a further ring-heteroatom such as >N—H, >N—CH3 or —O—; and is located either at the 1,3- or 1,4-location in relation to the aforementioned nitrogen atom,R6 stands for (C1-C6)-alkyl, (C1-C6)-alkylcarbonyl, phenyl or benzoyl, andR7 stands for (C1-C6)-alkyl, which may be substituted with phenyl, Where phenyl may also be substituted with (C1-C6)-alkoxycarbonyl or carboxyl, and also their salts, solvates and solvates of the salts.
地址 Bothell WA US