PDE-DELTA INHIBITOR FOR THE TREATMENT OF CANCER

    公开(公告)号:US20170135979A1

    公开(公告)日:2017-05-18

    申请号:US14940406

    申请日:2015-11-13

    CPC classification number: A61K31/343

    Abstract: The present invention relates to the administration of a novel compound advantageously efficacious as PDEδ inhibitor and its effects on subjects with cancer. More specifically, the present invention is directed to a method for administering a compound having favorable geometric properties for interacting with the PDEδ prenyl-binding pocket, namely has certain structural components such as a three-cyclic backbone and at least one benzoyl-moiety in a side chain having at least two substituents containing highly electronegative atoms and being linked to the backbone via an aliphatic chain, for treating a subject suffering from a disease such as cancer, in particular non-small-cell lung cancer. The presence of said structural components particularly contributes to an advantageous interaction with PDEδ, in particular with amino acids deep in the binding pocket. The present invention further provides a method to target tumor cells harboring an RAS gene mutation as well as pharmaceutical compositions comprising said compound.

    METHOD OF IDENTIFYING A GENE ASSOCIATED WITH A DISEASE OR PATHOLOGICAL CONDITION OF THE DISEASE

    公开(公告)号:US20190017116A1

    公开(公告)日:2019-01-17

    申请号:US15647414

    申请日:2017-07-12

    Abstract: A method of identifying a gene associated with a disease or pathological condition of the disease includes: a) obtaining a first group of exome sequences from a first population suffering from the disease or pathological condition and a second group of exome sequences from a second population not having the disease or pathological condition; b) identifying one or more variants in the first group by comparing it with the second group, and optionally with a public database, to generate a first set of variant data; c) applying a variant quality score calibration tool with a truth sensitivity threshold to remove false-positive variants having a sensitivity lower than the threshold and background variants from the first set of variant data so as to obtain a second set of variant data; d) removing synonymous variants from the second set of variant data to obtain a third set of variant data; and e) identifying one or more deleterious variants from the third set of variant data using a gene burden analysis, optionally generating a fourth set of variant data.

    Method of identifying a gene associated with a disease or pathological condition of the disease

    公开(公告)号:US10787708B2

    公开(公告)日:2020-09-29

    申请号:US15647414

    申请日:2017-07-12

    Abstract: A method of identifying a gene associated with a disease or pathological condition of the disease includes: a) obtaining a first group of exome sequences from a first population suffering from the disease or pathological condition and a second group of exome sequences from a second population not having the disease or pathological condition; b) identifying one or more variants in the first group by comparing it with the second group, and optionally with a public database, to generate a first set of variant data; c) applying a variant quality score calibration tool with a truth sensitivity threshold to remove false-positive variants having a sensitivity lower than the threshold and background variants from the first set of variant data so as to obtain a second set of variant data; d) removing synonymous variants from the second set of variant data to obtain a third set of variant data; and e) identifying one or more deleterious variants from the third set of variant data using a gene burden analysis, optionally generating a fourth set of variant data.

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