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公开(公告)号：US10981892B2
公开(公告)日：2021-04-20
申请号：US16897905
申请日：2020-06-10
发明人： Anne-Marie Beausoleil , Ryan Hudson
IPC分类号： C07F9/6509 , C07D401/12 , A61P11/00 , A61P9/10 , A61P27/00 , A61P35/00 , C07D401/10 , C07D401/14 , C07D403/10
摘要： 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：US20210070788A1
公开(公告)日：2021-03-11
申请号：US16920131
申请日：2020-07-02
发明人： Anne-Marie Beausoleil , Ryan Hudson
IPC分类号： C07F9/6584 , A61P35/00 , A61P3/10 , A61P19/02
摘要： 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.
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公开(公告)号：US10717722B2
公开(公告)日：2020-07-21
申请号：US16446360
申请日：2019-06-19
发明人： Anne-Marie Beausoleil , Ryan Hudson
IPC分类号： C07D207/337 , C07D401/12 , C07D401/10 , C07D403/10 , A61P9/10 , A61P35/00 , A61P27/00 , C07D401/14
摘要： The aryl sulfonamide compounds of this invention have powerful and cell-type specific Bcl inhibitory activity. Compounds of this invention include compounds according to formula (I): 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：US10703745B2
公开(公告)日：2020-07-07
申请号：US16425665
申请日：2019-05-29
发明人： Anne-Marie Beausoleil , Ryan Hudson
IPC分类号： C07D401/12 , C07D413/12 , C07D413/14 , C07D241/04 , A61P31/00
摘要： 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.
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公开(公告)号：US20200317640A1
公开(公告)日：2020-10-08
申请号：US16897905
申请日：2020-06-10
发明人： Anne-Marie Beausoleil , Ryan Hudson
IPC分类号： C07D401/10 , C07D403/10 , A61P9/10 , A61P35/00 , A61P27/00 , C07D401/14
摘要： 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：US10745429B2
公开(公告)日：2020-08-18
申请号：US16425276
申请日：2019-05-29
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.
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公开(公告)号：US10689416B2
公开(公告)日：2020-06-23
申请号：US16393651
申请日：2019-04-24
IPC分类号： C07K7/06 , A61K38/06 , A61P27/02 , A61P9/10 , A61P19/02 , A61P35/00 , A61K31/496 , A61K31/519 , A61K38/05 , A61K38/07 , C07D201/00 , C07D303/32 , C07K5/06 , C07K5/08 , C07K5/083 , C07K5/10 , C07K5/107 , A61K38/00
摘要： 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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公开(公告)号：US10519197B1
公开(公告)日：2019-12-31
申请号：US16538557
申请日：2019-08-12
摘要： 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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公开(公告)号：US20190382371A1
公开(公告)日：2019-12-19
申请号：US16446360
申请日：2019-06-19
发明人： Anne-Marie Beausoleil , Ryan Hudson
IPC分类号： C07D401/10 , C07D403/10 , C07D401/14 , A61P35/00 , A61P27/00 , A61P9/10
摘要： 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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10.发明申请公开(公告)号：US20190248837A1
公开(公告)日：2019-08-15
申请号：US16393651
申请日：2019-04-24
摘要： 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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