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公开(公告)号：US11441195B2
公开(公告)日：2022-09-13
申请号：US17254157
申请日：2019-06-19
IPC分类号： A61K49/00 , C12Q1/6886 , A61K31/03 , A61K31/519 , A61K45/06
摘要： This disclosure describes the characteristics of the “energetic” cancer stem cell (e-CSC) phenotype. This distinct sub-population of cancer stem cells (CSCs) has a unique energetic profile compared to bulk CSCs, being more glycolytic, having higher mitochondrial mass and elevated oxidative metabolism. e-CSCs also show an increased capacity to undergo cell cycle progression, enhanced anchorage-independent growth, and ALDH-positivity. The e-CSC phenotype presents new targets for cancer therapeutics, and in particular the anti-oxidant response, mitochondrial energy production, and mitochondrial biogenesis of e-CSCs makes them highly susceptible to mitochondrial inhibitors that target e-CSC anti-oxidant response, mitochondrial energy production, and mitochondrial biogenesis. Gene products for e-CSCs are disclosed, as well as classes of mitochondrial inhibiting therapeutic agents. Also disclosed are methods for identifying and separating e-CSCs from bulk cell populations.
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公开(公告)号：US10512618B2
公开(公告)日：2019-12-24
申请号：US16204173
申请日：2018-11-29
IPC分类号： A61K31/137 , A61P31/00 , A61P15/16 , A61P35/00 , A61K31/14 , A61K31/155 , A61K31/66 , G16C20/50 , A61K9/00 , A61K31/40 , A61K31/436 , A61K31/519 , A61K31/5513
摘要： The present disclosure relates to inhibitors of mitochondrial function. Methods of screening compounds for mitochondrial inhibition are disclosed. Also described are methods of using mitochondrial inhibitors called mitoriboscins—mitochondrial-based therapeutic compounds having anti-cancer and antibiotic properties—to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitochondrial inhibitors to provide anti-aging benefits. Specific mitoriboscin compounds and groups of mitoriboscins are also disclosed.
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公开(公告)号：US11964983B2
公开(公告)日：2024-04-23
申请号：US18008636
申请日：2021-06-10
IPC分类号： C07D487/14 , C07D487/20
CPC分类号： C07D487/14 , C07D487/20
摘要： This disclosure describes embodiments of selective and potent CDK 4/6 inhibitors that show advantageous inhibition of cancer growth, even at low concentrations. As described herein, compounds of the present approach comprise substituted pyridinylpiperazine-pyrrolopyrimidine compounds having a fatty acid moiety. The compounds described herein may be used as pharmaceutical compounds for anti-cancer therapies, and are useful for the treatment, prevention and/or amelioration of cancer. Formula (a)
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公开(公告)号：US11738034B2
公开(公告)日：2023-08-29
申请号：US17199087
申请日：2021-03-11
摘要： Tri-phenyl-phosphonium (TPP) is a non-toxic chemical moiety that functionally behaves as a mitochondrial targeting signaling in living cells. TPP-related compounds may be utilized to target mitochondria in cancer stem cells (CSC5), and may be used for treating and/or preventing tumor recurrence, metastasis, drug resistance, and/or radiotherapy resistance, as well as for anticancer therapies. Various TPP-related compounds validated for oxygen consumption inhibition (OCR), were non-toxic, and had little or no effect on ATP production in normal human fibroblasts. Yet these compounds selectively target adherent “bulk” cancer cells. These compounds also inhibit the propagation of CSCs in suspension. TPP-related compounds provide a novel chemical strategy for effectively targeting both i) “bulk” cancer cells and ii) CSCs, while specifically minimizing or avoiding off-target side-effects in normal cells, among other useful therapies.
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公开(公告)号：US11547679B2
公开(公告)日：2023-01-10
申请号：US16670326
申请日：2019-10-31
IPC分类号： A61K31/55 , C07D403/04 , A61P31/00 , A61P35/00 , A61K31/137 , C07D295/135 , C07C217/74 , C07D223/04 , C07D401/04 , C07C235/46 , C07D491/107 , C07C275/24 , C07D513/04 , C07D207/06 , A61P15/16 , A61K31/14 , A61K31/155 , A61K31/66 , G16C20/50 , A61K9/00 , A61K31/40 , A61K31/436 , A61K31/519 , A61K31/5513
摘要： The present disclosure relates to inhibitors of mitochondrial function. Methods of screening compounds for mitochondrial inhibition are disclosed. Also described are methods of using mitochondrial inhibitors called mitoriboscins—mitochondrial-based therapeutic compounds having anti-cancer and antibiotic properties—to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitochondrial inhibitors to provide anti-aging benefits. Specific mitoriboscin compounds and groups of mitoriboscins are also disclosed.
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6.发明申请公开(公告)号：US20200207775A1
公开(公告)日：2020-07-02
申请号：US16803628
申请日：2020-02-27
IPC分类号： C07D487/04 , C40B30/06 , C40B40/14 , C07D265/36 , C07D209/42 , C07D417/12 , G16C20/50
摘要： The present disclosure relates to compounds that bind to at least one of ACAT1/2 and OXCT1/2 and inhibit mitochondrial ATP production, referred to herein as mitoketoscins. Methods of screening compounds for mitochondrial inhibition and anti-cancer properties are disclosed. Also described are methods of using mitoketoscins to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitoketoscins to provide anti-aging benefits. Specific mitoketoscin compounds are also disclosed.
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7.发明申请公开(公告)号：US20200170967A1
公开(公告)日：2020-06-04
申请号：US16670326
申请日：2019-10-31
IPC分类号： A61K31/137 , A61P31/00 , A61P15/16 , A61P35/00 , A61K31/14 , A61K31/155 , A61K31/66 , C07D295/135 , C07C217/74 , C07D223/04 , C07D401/04 , C07C235/46 , C07D403/04 , C07D491/107 , C07C275/24 , C07D513/04
摘要： The present disclosure relates to inhibitors of mitochondrial function. Methods of screening compounds for mitochondrial inhibition are disclosed. Also described are methods of using mitochondrial inhibitors called mitoriboscins—mitochondrial-based therapeutic compounds having anti-cancer and antibiotic properties—to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitochondrial inhibitors to provide anti-aging benefits. Specific mitoriboscin compounds and groups of mitoriboscins are also disclosed.
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公开(公告)号：US11197872B2
公开(公告)日：2021-12-14
申请号：US16606485
申请日：2018-04-20
IPC分类号： A61K31/65 , A61K31/375 , A61K31/341 , A61K31/36 , A61K31/47 , A61K31/7004 , A61K31/7048
摘要： The present disclosure relates to compounds and methods of eradicating cancer stem cells by combining inhibitors of oxidative metabolism and glycolytic metabolism. Also described are compounds and methods of identifying a combination of inhibitors of oxidative metabolism and glycolytic metabolism to treat cancer stem cells.
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公开(公告)号：US20210186898A9
公开(公告)日：2021-06-24
申请号：US16670326
申请日：2019-10-31
IPC分类号： A61K31/137 , A61P31/00 , A61P15/16 , A61P35/00 , A61K31/14 , A61K31/155 , A61K31/66 , C07D295/135 , C07C217/74 , C07D223/04 , C07D401/04 , C07C235/46 , C07D403/04 , C07D491/107 , C07C275/24 , C07D513/04
摘要： The present disclosure relates to inhibitors of mitochondrial function. Methods of screening compounds for mitochondrial inhibition are disclosed. Also described are methods of using mitochondrial inhibitors called mitoriboscins—mitochondrial-based therapeutic compounds having anti-cancer and antibiotic properties—to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitochondrial inhibitors to provide anti-aging benefits. Specific mitoriboscin compounds and groups of mitoriboscins are also disclosed.
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公开(公告)号：US10980821B2
公开(公告)日：2021-04-20
申请号：US16766472
申请日：2018-11-21
摘要： Tri-phenyl-phosphonium (TPP) is a non-toxic chemical moiety that functionally behaves as a mitochondrial targeting signaling in living cells. TPP-related compounds may be utilized to target mitochondria in cancer stem cells (CSCs), and may be used for treating and/or preventing tumor recurrence, metastasis, drug resistance, and/or radiotherapy resistance, as well as for anti-cancer therapies. Various TPP-related compounds validated for oxygen consumption inhibition (OCR), were non-toxic, and had little or no effect on ATP production in normal human fibroblasts. Yet these compounds selectively target adherent “bulk” cancer cells. These compounds also inhibit the propagation of CSCs in suspension. TPP-related compounds provide a novel chemical strategy for effectively targeting both i) “bulk” cancer cells and ii) CSCs, while specifically minimizing or avoiding off-target side-effects in normal cells, among other useful therapies.
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