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    Compounds and method for treating autoimmune diseases
    4.
    发明授权
    Compounds and method for treating autoimmune diseases 有权

    公开(公告)号：US11220496B2

    公开(公告)日：2022-01-11

    申请号：US16551431

    申请日：2019-08-26

    申请人： Rigel Pharmaceuticals, Inc.

    发明人： Esteban Masuda ,  Rajinder Singh ,  Vanessa Taylor ,  Donald G. Payan

    IPC分类号： C07D413/12 ,  C07F9/653 ,  A61K31/675 ,  A61K45/06 ,  A61K31/506

    摘要： Compounds and embodiments of a method for treating and/or preventing autoimmune diseases are disclosed. The method includes administering to a subject having an autoimmune disease, such as an inflammatory bowel disease, a therapeutically effective amount of a compound according to formula I wherein X and Y independently are O or NR1; each R1 is independently H or C1-C6 alkyl; ring A is aryl; each R2 independently is H, alkyl, alkoxy, amide, cyano, halo, haloalkyl, hydroxyalkyl, heteroalkyl, heterocyclyl, sulfonyl, sulfonamide, or two R2 groups, taken together with the atom or atoms to which they are attached, combine to form a 4-10 membered ring system; p is 0, 1, 2, 3, or 4; R3 and R4 independently are H or C1-C6 alkyl; and R5 is halo, cyano, or C1-C6 alkyl.

    Phospholidines that are Bcl family antagonists for use in clinical management of conditions caused or mediated by senescent cells and for treating cancer
    5.
    发明授权
    Phospholidines that are Bcl family antagonists for use in clinical management of conditions caused or mediated by senescent cells and for treating cancer 有权

    公开(公告)号：US10745429B2

    公开(公告)日：2020-08-18

    申请号：US16425276

    申请日：2019-05-29

    申请人： Unity Biotechnology, Inc.

    发明人： Anne-Marie Beausoleil ,  Ryan Hudson

    IPC分类号： C07F9/653 ,  C07F9/6533 ,  C07F9/6584 ,  A61P35/00 ,  A61P3/10 ,  A61P19/02

    摘要： This disclosure provides compounds with Bcl inhibitory activity based on a new chemical scaffold, as shown in Formula (I). The phospholidine compounds can include a P-phenyl phospholidine moiety which is substituted with an N-aryl or N-heteroaryl group. The P-phenyl phospholidine moiety can be optionally substituted at phosphorus with thio (═S) instead of oxo (═O). A second heteroatom attached to phosphorus can be cyclically linked to the N-substituted nitrogen atom of the phospholidine that is attached to the phosphorus to provide, together with the phosphorus atom through which they are connected, a heterocyclic ring. By incorporating such a cyclic constraint between two phosphorus substituents of the core linking moiety a favorable binding conformation can be promoted in the compounds. Selected compounds promote apoptosis in senescent cells, and can be developed for treating senescent-related conditions, such as osteoarthritis, ophthalmic disease, pulmonary disease, and atherosclerosis. Selected compounds promote apoptosis in cancer cells, and can be developed as chemotherapeutic agents.