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    Methods of Inhibiting Pathological Angiogenesis
    41.
    发明申请
    Methods of Inhibiting Pathological Angiogenesis 有权

    公开(公告)号：US20220072015A1

    公开(公告)日：2022-03-10

    申请号：US17412003

    申请日：2021-08-25

    Applicant: Unity Biotechnology, Inc.

    Inventor： Pam Tsuruda ,  Jill Hopkins ,  Harry Sweigard ,  Yan Poon ,  Jamie Dananberg ,  Daniel Marquess ,  Nathaniel David

    IPC: A61K31/635 ,  A61P27/02

    Abstract: This invention is based on the discovery that many eye conditions associated with aging are mediated at least in part by cells bearing a senescent phenotype. Senescent cells accumulate with age, and express factors that contribute to the pathophysiology of age related conditions. The data show that in age-matched patients, the severity of age-related conditions correlates with the abundance of senescent cells, and that clearing senescent cells can help abrogate the condition. Small molecule drugs that remove senescent cells from affected tissue in the eye are provided that have special efficacy in treating ophthalmic conditions. They not only inhibit progression of the disease, they can also reverse some of the pathophysiology—such as neovascularization and vaso-obliteration—that lead to vision loss. These senolytic agents have an appropriate dose and specificity profile to be effective in the clinical management of previously intractable ophthalmic conditions.

    Methods of inhibiting pathological angiogenesis
    42.
    发明授权
    Methods of inhibiting pathological angiogenesis 有权

    公开(公告)号：US11129838B2

    公开(公告)日：2021-09-28

    申请号：US16791960

    申请日：2020-02-14

    Applicant: Unity Biotechnology, Inc.

    Inventor： Pam Tsuruda ,  Jill Hopkins ,  Harry Sweigard ,  Yan Poon ,  Jamie Dananberg ,  Daniel Marquess ,  Nathaniel David

    IPC: A61K31/635 ,  A61P27/02 ,  A61K9/00 ,  A61K47/26 ,  A61K47/20 ,  A61K47/10

    Abstract: This invention is based on the discovery that many eye conditions associated with aging are mediated at least in part by cells bearing a senescent phenotype. Senescent cells accumulate with age, and express factors that contribute to the pathophysiology of age related conditions. The data show that in age-matched patients, the severity of age-related conditions correlates with the abundance of senescent cells, and that clearing senescent cells can help abrogate the condition. Small molecule drugs that remove senescent cells from affected tissue in the eye are provided that have special efficacy in treating ophthalmic conditions. They not only inhibit progression of the disease, they can also reverse some of the pathophysiology—such as neovascularization and vaso-obliteration—that lead to vision loss. These senolytic agents have an appropriate dose and specificity profile to be effective in the clinical management of previously intractable ophthalmic conditions.

    Phospholidines that are Bcl Family Antagonists for Use in Clinical Management of Conditions Caused or Mediated by Senescent Cells and for Treating Cancer
    45.
    发明申请
    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：US20210070788A1

    公开(公告)日：2021-03-11

    申请号：US16920131

    申请日：2020-07-02

    Applicant: Unity Biotechnology, Inc.

    Inventor： Anne-Marie Beausoleil ,  Ryan Hudson

    IPC: C07F9/6584 ,  A61P35/00 ,  A61P3/10 ,  A61P19/02

    Abstract: This disclosure provides compounds with Bcl inhibitory activity based on a new chemical scaffold. 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.

    Acyl phosphonamidates and acyl benzylamines that are Bcl family antagonists for use in clinical management of conditions caused or mediated by senescent cells and for treating cancer
    49.
    发明授权
    Acyl phosphonamidates and acyl benzylamines 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：US10703745B2

    公开(公告)日：2020-07-07

    申请号：US16425665

    申请日：2019-05-29

    Applicant: Unity Biotechnology, Inc.

    Inventor： Anne-Marie Beausoleil ,  Ryan Hudson

    IPC: C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D241/04 ,  A61P31/00

    Abstract: This disclosure provides compounds with Bcl inhibitory activity based on a new chemical scaffold. Acyl phosphonamidate compounds may include a P-phenyl phosphonamidate moiety which is N-acylated with an aroyl or heteroaroyl group. The P-phenyl phosphonamidate moiety can be optionally substituted at phosphorus with thio (═S) instead of oxo (═O), and/or with a thioxy group or a second amino group instead of an oxy group. One of the heteroatoms attached to phosphorus can be cyclically linked to a carbon atom of the adjacent phenyl ring 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.

    Technology to inhibit vascular changes that lead to vision loss in the eye
    50.
    发明授权
    Technology to inhibit vascular changes that lead to vision loss in the eye 有权

    公开(公告)号：US10588916B2

    公开(公告)日：2020-03-17

    申请号：US16160840

    申请日：2018-10-15

    Applicant: Unity Biotechnology, Inc.

    Inventor： Pam Tsuruda ,  Jill Hopkins ,  Harry Sweigard ,  Yan Poon ,  Jamie Dananberg ,  Daniel Marquess ,  Nathaniel David

    IPC: A61K31/635 ,  A61P27/02 ,  A61K9/00 ,  A61K47/26 ,  A61K47/20 ,  A61K47/10

    Abstract: This invention is based on the discovery that many eye conditions associated with aging are mediated at least in part by cells bearing a senescent phenotype. Senescent cells accumulate with age, and express factors that contribute to the pathophysiology of age related conditions. The data show that in age-matched patients, the severity of age-related conditions correlates with the abundance of senescent cells, and that clearing senescent cells can help abrogate the condition. Small molecule drugs that remove senescent cells from affected tissue in the eye are provided that have special efficacy in treating ophthalmic conditions. They not only inhibit progression of the disease, they can also reverse some of the pathophysiology—such as neovascularization and vaso-obliteration—that lead to vision loss. These senolytic agents have an appropriate dose and specificity profile to be effective in the clinical management of previously intractable ophthalmic conditions.

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