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    Use of phospho-Akt as a biomarker of drug response
    1.
    发明授权
    Use of phospho-Akt as a biomarker of drug response 有权

    公开(公告)号：US10724072B2

    公开(公告)日：2020-07-28

    申请号：US15992813

    申请日：2018-05-30

    申请人： Basilea Pharmaceutica AG

    发明人： Heidi Alexandra Lane ,  Felix Bachmann

    IPC分类号： A61K31/4245 ,  A61K31/4439 ,  C12Q1/48 ,  G01N33/574 ,  C07D413/04 ,  C07D413/14

    摘要： Use of phospho-Akt as a biomarker for predicting the response, such as resistance, to a compound, wherein phospho-Akt is Akt that has been phosphorylated on one or more residues, with the proviso that fir Akt1, Akt2, and Akt3 the designation phospho-Akt is used to indicate phosphorylation at a site other than T308, T309 or T305 respectively, wherein the compound is a compound of general formula (I) wherein R represents phenyl, thienyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; X represents a group C═Y, wherein Y stands for oxygen or nitrogen substituted by hydroxy or lower alkoxy; R1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; R2, R3 and R6 represent hydrogen; R4 and R5, independently of each other, represent hydrogen, lower alkyl or lower alkoxy, or R4 and R5 together represent methylenedioxy, and pharmaceutically acceptable derivatives thereof; or wherein R represents phenyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkoxycarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, formyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; X represents oxygen; R1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; R2, R3 and R6 represent hydrogen; R4 and R5, independently of each other, represent hydrogen, lower alkyl or lower alkoxy, or R4 and R5 together represent methylenedioxy; and pharmaceutically acceptable derivatives thereof. Methods of treatment of neoplastic and autoimmune diseases with these compounds we also disclosed.

    Furazanobenzimidazoles
    10.
    再颁专利
    Furazanobenzimidazoles 有权
    呋喃并苯并咪唑

    公开(公告)号：USRE42890E1

    公开(公告)日：2011-11-01

    申请号：US12796135

    申请日：2004-05-19

    申请人： Martin Eberle ,  Felix Bachmann ,  Alessandro Strebel ,  Subho Roy ,  Sudhir Srivastava ,  Goutam Saha

    发明人： Martin Eberle ,  Felix Bachmann ,  Alessandro Strebel ,  Subho Roy ,  Sudhir Srivastava ,  Goutam Saha

    IPC分类号： A61K31/4245 ,  C07D413/04

    CPC分类号： C07D413/04 ,  C07D413/14

    摘要： The invention relates to compounds of formula (I) wherein R represents aryl or heteroaryl, X is oxygen, a carbonyl group, an oxime derivative of a carbonyl group or an α,β-unsaturated carbonyl group, and the substituents R1 to R6 have the meanings given in the specification, for use as medicaments, to novel compounds of formula (I), to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same

    摘要翻译： 本发明涉及式（I）化合物，其中R表示芳基或杂芳基，X为氧，羰基，羰基肟衍生物或α，β-不饱和羰基，取代基R 1至R 6具有 本说明书中用作药物的含义，式（I）的新型化合物，合成这些化合物的方法，含有式（I）化合物的药物组合物，使用式（I）化合物 ）用于制备用于治疗肿瘤和自身免疫疾病的药物组合物，以及使用这样的式（I）化合物或含有其的药物组合物治疗肿瘤和自身免疫性疾病的方法