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公开(公告)号：US10010546B2
公开(公告)日：2018-07-03
申请号：US15827539
申请日：2017-11-30
Applicant: Buck Institute for Research on Aging , Mayo Foundation for Medical Education and Research , Unity Biotechnology, Inc.
Inventor： Remi-Martin Laberge , Judith Campisi , Marco Demaria , Nathaniel David , Alain Philippe Vasserot , James L. Kirkland , Tamar Tchkonia , Yi Zhu , Darren J. Baker , Bennett G. Childs , Jan M. A. van Deursen
IPC: A61K31/496 , A61K31/728 , A61K31/4178 , A61K9/00
CPC classification number: A61K31/496 , A61K9/0048 , A61K9/0073 , A61K31/404 , A61K31/4178 , A61K31/428 , A61K31/4375 , A61K31/495 , A61K31/5377 , A61K31/728 , A61K45/06 , A61K47/36 , A61P9/10 , A61P11/00 , A61P27/02 , C12N5/0081 , C12N2501/999 , C12N2503/02 , C12Q1/485
Abstract: Methods are provided herein for selectively killing senescent cells and for treating senescence-associated diseases and disorders by administering a senolytic agent. Senescence-associated diseases and disorders treatable by the methods using the senolytic agents described herein include cardiovascular diseases and disorders associated with or caused by arteriosclerosis, such as atherosclerosis; idiopathic pulmonary fibrosis; chronic obstructive pulmonary disease; osteoarthritis; senescence-associated ophthalmic diseases and disorders; and senescence-associated dermatological diseases and disorders.
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公开(公告)号：US09988368B1
公开(公告)日：2018-06-05
申请号：US15693061
申请日：2017-08-31
Applicant: Unity Biotechnology, Inc.
Inventor： Thomas W. von Geldern , Bradley Backes , Bing Chen
IPC: C07D403/06 , C07D233/54 , C07D233/64
CPC classification number: C07D403/06 , C07D233/54 , C07D233/64
Abstract: This invention provides a method for enantioselective synthesis of cis-imidazolines and related structures through chiral resolution. A chiral acid is used to separate enantiomeric precursors of the cis-imidazolines from a racemic mixture by selective crystallization. Both enantiomers can be cyclized into the desired cis-imidazoline by complementary pathways. Compounds can be synthesized according to the invention with an enantiomeric excess as high as 99%. Cis-imidazolines such as Nutlin-3a prepared according to this invention may be used for treating cancer, killing senescent cells, or treating senescence-associated conditions.
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公开(公告)号：US20180117038A1
公开(公告)日：2018-05-03
申请号：US15827539
申请日：2017-11-30
Applicant: Buck Institute for Research on Aging , Mayo Foundation for Medical Education and Research , Unity Biotechnology, Inc.
Inventor： Remi-Martin Laberge , Judith Campisi , Marco Demaria , Nathaniel David , Alain Philippe Vasserot , James L. Kirkland , Tamar Tchkonia , Yi Zhu
IPC: A61K31/496 , A61K31/728 , A61K31/4178
CPC classification number: A61K31/496 , A61K9/0048 , A61K9/0073 , A61K31/404 , A61K31/4178 , A61K31/428 , A61K31/4375 , A61K31/495 , A61K31/5377 , A61K31/728 , A61K45/06 , A61K47/36 , C12N5/0081 , C12N2501/999 , C12N2503/02
Abstract: Methods are provided herein for selectively killing senescent cells and for treating senescence-associated diseases and disorders by administering a senolytic agent. Senescence-associated diseases and disorders treatable by the methods using the senolytic agents described herein include cardiovascular diseases and disorders associated with or caused by arteriosclerosis, such as atherosclerosis; idiopathic pulmonary fibrosis; chronic obstructive pulmonary disease; osteoarthritis; senescence-associated ophthalmic diseases and disorders; and senescence-associated dermatological diseases and disorders.
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84.发明申请公开(公告)号：US20160017033A1
公开(公告)日：2016-01-21
申请号：US14750941
申请日：2015-06-25
Applicant: Unity Biotechnology, Inc.
Inventor： Shayne Squires
CPC classification number: C07K14/00 , A61K35/12 , A61K38/10 , A61K38/16 , A61K38/168 , A61K47/64 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K49/0004 , A61K49/0056 , A61K51/08 , A61K51/088 , A61K51/1027 , A61K2039/505 , C07K16/28 , C07K2317/24 , C07K2317/73 , C07K2317/76 , C07K2317/92 , C12N15/1037 , C12N15/86 , C12N2710/10043 , G01N33/5032 , G01N33/57492 , G01N2800/50
Abstract: Disclosed are agents (e.g., peptides, polypeptides, proteins, small molecules, antibodies, and antibody fragments that target senescent cells) and methods of their use for imaging senescent cells in vivo and for treating or preventing cancer, age-related disease, tobacco-related disease, or other diseases and disorders related to or caused by cellular senescence in a mammal. The methods include administering one or more of the agents of the invention to a mammal, e.g., a human. The agents, which specifically bind to senescent cells, can be labeled with a radioactive label or a therapeutic label, e.g., a cytotoxic agent.
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公开(公告)号：US20240245680A1
公开(公告)日：2024-07-25
申请号：US18289554
申请日：2022-05-25
Applicant: Scott KIMURA , Unity Biotechnology, Inc.
Inventor： Remi-Martin Laberge , Scott Kimura , Przemyslaw Sapieha , Pamela Tsuruda , Pieter Bas-Kwak , Nathan Gushwa , Tianna Chow
IPC: A61K31/497 , A61K31/4152 , A61K31/437 , A61K45/06 , A61P27/02
CPC classification number: A61K31/497 , A61K31/4152 , A61K31/437 , A61K45/06 , A61P27/02
Abstract: The invention relates to methods of treating certain retinal vasculopathies such as diabetic macular edema, diabetic retinopathy and dry and neovascular age-related macular degeneration, among others. In some instances, the method includes treating a patient suffering from a retinal vasculopathy by administering an agent to the patient. The agent can be one or more of the agents as described herein.
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Patent Agency Ranking
公开(公告)号：US20220017485A1
公开(公告)日：2022-01-20
申请号：US17338368
申请日：2021-06-03
Applicant: Unity Biotechnology, Inc.
Inventor： Anne-Marie Beausoleil , Ryan Hudson
IPC: C07D401/10 , C07D403/10 , A61P9/10 , A61P35/00 , A61P27/00 , C07D401/14
Abstract: The aryl sulfonamide compounds of this invention have powerful and cell-type specific Bcl inhibitory activity. Selected compounds in this class promote apoptosis in senescent cells, and are being developed for treating senescent-related conditions. Selected compounds in this class promote apoptosis in cancer cells, and can be developed as chemotherapeutic agents.
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公开(公告)号：US20210379078A1
公开(公告)日：2021-12-09
申请号：US17285420
申请日：2019-10-24
Applicant: Unity Biotechnology, Inc.
Inventor： Pieter Bas Kwak , Scott Armstrong , Pedro Beltran , Anne-Marie Beausoleil
IPC: A61K31/553 , A61K31/4725 , G01N33/50 , A61K31/519 , A61K31/4162 , A61P11/00 , A61P19/02 , A61P27/02 , A61P9/10
Abstract: This invention is based on the discovery that inhibiting more than one pathway in senescent cells leading to apoptosis has a profound effect: namely, increasing the potency or the cell specificity of the therapy. Combining a Bcl inhibitor with an Mcl 1 inhibitor increases the ability of the Bcl inhibitor to remove senescent cells from the site of an adverse condition synergistically. This increases the types of senescent cells that can be targeted, broadens the therapeutic range, and allows the user to tailor a particular combination of agents by adjusting the molar ratio for the patient being treated. Suitable indications for treatment may include any condition thought to be mediated at least in part by senescent cells, such as ophthalmic conditions, pulmonary conditions, and atherosclerosis.
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公开(公告)号：US20200338094A1
公开(公告)日：2020-10-29
申请号：US16893012
申请日：2020-06-04
Inventor： Nathaniel David , Remi-Martin Laberge
IPC: A61K31/635 , A61K31/496 , A61K31/675 , A61K9/00 , A61K9/12 , A61K8/00
Abstract: A library of heterocyclic compounds has been screened to identify particular compounds that have high inhibitory capacity for the Bcl family of regulatory proteins. Compounds identified as Bcl antagonists have been further screened to select pharmaceutical agents with both high potency and high specificity for eliminating senescent cells in comparison with replicative or quiescent cells of the same tissue type. Particular structures are identified in this disclosure that eliminate senescent cells with an EC50 in the nanomole range and a specificity around or above 100-fold. In accordance with this invention, heterocyclic compounds provided in this disclosure can be formulated for the treatment of a range of age-related conditions caused or mediated by senescent cells. Such conditions are exemplified by ophthalmic conditions, pulmonary conditions, and osteoarthritis.
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89.发明申请公开(公告)号：US20200291050A1
公开(公告)日：2020-09-17
申请号：US16063135
申请日：2016-12-16
Applicant: Unity Biotechnology, Inc.
Inventor： Bradley Backes , Thomas W. von Geldern , Bing Chen
IPC: C07F9/6558 , C07F9/6509 , A61P43/00
Abstract: Compounds represented by Formula (I) and (II) and salts thereof are described herein. The compounds or salts of Formula (I) and (II) may be used to treat senescence-associated diseases and disorders.
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90.发明申请公开(公告)号：US20200002378A1
公开(公告)日：2020-01-02
申请号：US16538557
申请日：2019-08-12
Applicant: UNITY BIOTECHNOLOGY, INC.
Inventor： Ryan Hudson , Anne-Marie Beausoleil , F. Anthony Romero , Remi-Martin Laberge
Abstract: The proteasome inhibitors of this invention include peptide-based compounds with a short linear sequence of amino acids. An oxo or thio group is attached to the N-terminal amino acid. A protein-reactive electrophilic group such as an epoxyketone, an aziridinylketone, or a beta-lactone is attached to the C-terminal amino acid. Upon contact with a proteasome complex in a target cell, the electrophilic group reacts with a functional group in or near a binding pocket or active site of the proteasome, forming a covalent bond and thereby inactivating the proteasome. These and other proteasome inhibitors can be screened for binding affinity and an ability to selectively eliminate senescent cells or cancer cells. Compounds that selectively remove senescent cells can be developed for the treatment of conditions such as osteoarthritis, ophthalmic disease, pulmonary disease, and atherosclerosis.
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