首页>
外国专利>
New tubulysin analogs, useful for treating tumor or cancer diseases, immunologically induced or autoimmune diseases, inflammatory diseases or rheumatoid arthritis or for surface modification of implants
New tubulysin analogs, useful for treating tumor or cancer diseases, immunologically induced or autoimmune diseases, inflammatory diseases or rheumatoid arthritis or for surface modification of implants
Analogs (I) of tubulysins (natural cytotoxic tetrapeptides) are new. Tubulysin analogs of formula (I) (with the exception of the natural tubulysins of formula (I')) and their salts, solvates and hydrates are new. A = optionally substituted 5- or 6-membered heteroarylene; X = O, S, NR13 or CR14R15; Y = O, S or NR16; R1 - R16 = H, alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl; or two groups together form part of a cycloalkyl or heterocycloalkyl ring system; Ra = H, alkyl, alkenyl, aryl or heteroaryl; Rb = H, OH, alkyl, aryl or heteroaryl.
展开▼
机译：微管溶素（天然细胞毒性四肽）的类似物（I）是新的。式（I）的花粉溶素类似物（式（I'）的天然微管溶素除外）及其盐，溶剂化物和水合物是新的。 A =任选取代的5-或6-元杂亚芳基; X = O，S，NR13或CR14R15; Y = O，S或NR16; R1-R16 ＝ H，烷基，烯基，炔基，杂烷基，芳基，杂芳基，环烷基，烷基环烷基，杂烷基环烷基，杂环烷基，芳烷基或杂芳烷基;或两个基团一起形成环烷基或杂环烷基环系统的一部分; Ra ＝ H，烷基，烯基，芳基或杂芳基; Rb ＝ H，OH，烷基，芳基或杂芳基。
展开▼
