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PEPTIDOMIMETIC COMPOUNDS, STEREOSELECTIVE PROCESS FOR THEIR PREPARATION AND THEIR USE AS BIOLOGICALLY ACTIVE SYNTHESIS INTERMEDIATE PRODUCTS
PEPTIDOMIMETIC COMPOUNDS, STEREOSELECTIVE PROCESS FOR THEIR PREPARATION AND THEIR USE AS BIOLOGICALLY ACTIVE SYNTHESIS INTERMEDIATE PRODUCTS
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机译:肽类化合物,其制备的立体选择过程及其用作生物活性合成中间体的产品
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摘要
The invention relates to novel cyclic peptidomimetic compounds having an azabicycloalkane structure, useful as intermediates in the preparation of alphaVBeta3 and alphaVBeta5 integrin antagonists, intended, for example, for the treatment of altered angiogenic phenomena; the invention also concerns a process for the stereoselective synthesis of said cyclic peptidomimetic compounds and biologically active derivatives thereof. Formula (I) wherein: n is 1 or 2, R1 is H, (C1-C4)alkyl,benzyl or a protective group; R2 is H or a protective group; R3 is H or heteroalkyl or a protective group; Their salts, racemic mixtures,individual enantiomers ,individual diastereoisomers and mixtures thereof in any proportion.
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机译:本发明涉及具有氮杂双环烷烃结构的新型环状拟肽化合物,可用作制备αVBeta3和αVBeta5整联蛋白拮抗剂的中间体,例如,用于治疗改变的血管生成现象。本发明还涉及立体选择性地合成所述环状拟肽化合物及其生物活性衍生物的方法。式(I)其中:n为1或2,R 1为H,(C 1 -C 4)烷基,苄基或保护基; R 2为H或保护基; R3是H或杂烷基或保护基;它们的盐,外消旋混合物,单个对映异构体,单个非对映异构体及其混合物的任何比例。
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