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公开(公告)号：US10399964B2
公开(公告)日：2019-09-03
申请号：US15940152
申请日：2018-03-29
发明人： Blake R. Peterson
IPC分类号： C07D407/12 , A61P35/00 , G01N33/58
摘要： A compound can be a fluorescent taxane derivative having a structure of Formula 1, salt, stereoisomer, tautomer, polymorph, or solvate thereof. Formula 1 can be defined as: L, L-NH, or L-NH—C═O is a linker; and R is a substituent, where —OH, —O−, —NH2, and NH—CH3 are examples. Examples of linkers can include glycine, beta-alanine, gamma-aminobutyric acid (GABA). Pharmaceutical compositions can include the compound and a pharmaceutically acceptable carrier, and may be configured for intravenous injection. The fluorescent taxane derivative can be used to treat cancer and non-cancer diseases. The fluorescent taxane derivative can be used to monitor cellular efflux and determine whether a cell will efflux paclitaxel.
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公开(公告)号：US20220056002A1
公开(公告)日：2022-02-24
申请号：US17416172
申请日：2019-12-20
IPC分类号： C07D311/16 , G01N33/547
摘要： A photocleavable heterobifunctional linker can include a structure of Formula (A) wherein coumarin is any coumarin or coumarin derivative; R, R9, and R10 are each independently a chemical moiety; R1 is a hydrogen, protecting group, leaving group, substrate, or capture entity; R2 is a hydrogen, hydroxyl, halide, alkoxy, anhydride, amino, protecting group, leaving group, substrate, or capture entity; L1 is a sub-linker; and L2 is a sub-linker. A capture device can include the photocleavable bifunctional linker having a structure of Formula (A) as provide herein, wherein R1 is a substrate. A method of capturing a target substance can include: providing the capture device having the photocleavable bifunctional linker with the structure of Formula (A) and contacting a target substance to the capture moiety such that the target substance is captured. Irradiating the linker with light can cleave the linker, thereby releasing the target substance from the substrate.
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公开(公告)号：US20180282314A1
公开(公告)日：2018-10-04
申请号：US15940152
申请日：2018-03-29
发明人： Blake R. Peterson
IPC分类号： C07D407/12 , A61P35/00 , G01N33/58
CPC分类号： C07D407/12 , A61P35/00 , G01N33/582
摘要： A compound can be a fluorescent taxane derivative having a structure of Formula 1, salt, stereoisomer, tautomer, polymorph, or solvate thereof. Formula 1 can be defined as: L, L-NH, or L-NH—C═O is a linker; and R is a substituent, where —OH, —O−, —NH2, and NH—CH3 are examples. Examples of linkers can include glycine, beta-alanine, gamma-aminobutyric acid (GABA). Pharmaceutical compositions can include the compound and a pharmaceutically acceptable carrier, and may be configured for intravenous injection. The fluorescent taxane derivative can be used to treat cancer and non-cancer diseases. The fluorescent taxane derivative can be used to monitor cellular efflux and determine whether a cell will efflux paclitaxel.
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公开(公告)号：US20170218022A1
公开(公告)日：2017-08-03
申请号：US15480120
申请日：2017-04-05
发明人： Blake R. Peterson
CPC分类号： C07K7/08 , A61K47/554 , A61K47/65 , A61K47/6811 , A61K47/6849 , A61K47/6851 , A61K47/6889 , C07K16/2887 , C07K16/32 , C07K2317/24 , C07K2317/73 , C07K2319/06 , C07K2319/74
摘要： A peptide can have a sequence of one of SEQ ID NOs: 78-91. A conformationally-constrained kinked peptide includes: a conformationally-constraining portion and a kinked portion linked to the conformationally-constraining portion that conformationally constrains the kinked portion having a peptide sequence of one of SEQ NOs: 78-97. A cell-targeting compound can include a conformationally-constrained kinked peptide having a peptide sequence of one of SEQ ID NOs: 78-97. The peptide sequence can be one of SEQ ID NOs: 78-97, or 78-91, or 92-97. A cell-targeting compound can include a conformationally-constrained kinked peptide linked to a branched linker with one branch arm linked to a specific targeting moiety and one branch ann linked to a general targeting moiety. The specific targeting moiety can be an antibody. The general targeting moiety can be a lipid or cholesterol derivative.
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公开(公告)号：US10663471B2
公开(公告)日：2020-05-26
申请号：US16362280
申请日：2019-03-22
发明人： Blake R. Peterson , Digamber Rane
IPC分类号： G01N33/58 , G01N33/533 , G01N33/50 , C09B57/00
摘要： A compound can be a pro-fluorophore peroxynitrite sensor that generates a fluorophore when cleaved by peroxynitrite, having a structure of Formula A: wherein: moiety A is an ER-targeting fluorophore; Y is a linker; and moiety B is a phenol, substituted or unsubstituted, wherein the structure of Formula A is less fluorescent than the ER-targeting fluorophore moiety A.
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公开(公告)号：US20190310263A1
公开(公告)日：2019-10-10
申请号：US16362280
申请日：2019-03-22
发明人： Blake R. Peterson , Digamber Rane
IPC分类号： G01N33/58 , G01N33/533 , G01N33/50 , C09B57/00
摘要： A compound can be a pro-fluorophore peroxynitrite sensor that generates a fluorophore when cleaved by peroxynitrite, having a structure of Formula A: wherein: moiety A is an ER-targeting fluorophore; Y is a linker; and moiety B is a phenol, substituted or unsubstituted, wherein the structure of Formula A is less fluorescent than the ER-targeting fluorophore moiety A.
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公开(公告)号：US10766928B2
公开(公告)日：2020-09-08
申请号：US15480120
申请日：2017-04-05
发明人： Blake R. Peterson
摘要： A peptide can have a sequence of one of SEQ ID NOs: 78-91. A conformationally-constrained kinked peptide includes: a conformationally-constraining portion and a kinked portion linked to the conformationally-constraining portion that conformationally constrains the kinked portion having a peptide sequence of one of SEQ NOs: 78-97. A cell-targeting compound can include a conformationally-constrained kinked peptide having a peptide sequence of one of SEQ ID NOs: 78-97. The peptide sequence can be one of SEQ ID NOs: 78-97, or 78-91, or 92-97. A cell-targeting compound can include a conformationally-constrained kinked peptide linked to a branched linker with one branch arm linked to a specific targeting moiety and one branch arm linked to a general targeting moiety. The specific targeting moiety can be an antibody. The general targeting moiety can be a lipid or cholesterol derivative.
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公开(公告)号：US09701715B2
公开(公告)日：2017-07-11
申请号：US14438194
申请日：2013-10-03
发明人： Blake R. Peterson
CPC分类号： C07K7/08 , A61K38/10 , A61K47/42 , A61K47/48246 , A61K47/64 , C12N2310/30 , C12N2310/3513 , C12N2310/3515
摘要： A conformationally-constrained kinked peptide includes: a conformationally-constraining portion and a kinked portion linked to the conformationally-constraining portion that conformationally constrains the kinked portion, the kinked portion comprising an endosomal-disrupting peptide. The peptide can include a peptide sequence of one of SEQ ID NOs: 1, 5-38, or 40-54 or 61-69. The conformationally-constrained kinked portion can be a majority portion or minority of the peptide. The peptide can include one of Formulae 1-1C, wherein: CC-Peptide includes a peptide that conformationally constrains the ED-KP; Peptide independently includes natural, unnatural, essential or non-essential aromatic, aliphatic, or other amino acids having L or D configuration; ED-KP includes an endosomal-disrupting kinked peptide; Xaa, Xaa1, and Xaa2 are independently one or more natural or non-natural amino acids, essential amino acids, or non-essential amino acids, or derivatives of amino acids having L or D configuration; L1 and L2 are independently linkers; and n1, n2, n3, and n4 are independently 0-50.
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公开(公告)号：US09636419B2
公开(公告)日：2017-05-02
申请号：US14512862
申请日：2014-10-13
发明人： Blake R. Peterson , Liang Xu , Matthew Levy
CPC分类号： A61K47/48569 , A61K47/542 , A61K47/6851 , A61K47/6897
摘要： A method of delivering a cargo agent into cytosol of a cell can include: providing the delivery system of one of the embodiments described herein having the first and second delivery platforms; and administering the delivery system to a cell so as to cause targeting of two features on the cell so as to: cause endocytosis of the first and second delivery platforms of the delivery system into a common endosome, destabilize the endosome of the cell having the delivery system, release the cargo agent from the second linker; and release the cargo agent from the destabilized endosome into cytosol of the cell. A method of treating a disease can include: performing the method of method of delivering a cargo agent into cytosol of a cell in a subject having a disease, wherein the cargo agent is a therapeutic agent for the disease.
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公开(公告)号：US20150274780A1
公开(公告)日：2015-10-01
申请号：US14438194
申请日：2013-10-03
发明人： Blake R. Peterson
CPC分类号： C07K7/08 , A61K38/10 , A61K47/42 , A61K47/48246 , A61K47/64 , C12N2310/30 , C12N2310/3513 , C12N2310/3515
摘要： A conformationally-constrained kinked peptide includes: a conformationally-constraining portion and a kinked portion linked to the conformationally-constraining portion that conformationally constrains the kinked portion, the kinked portion comprising an endosomal-disrupting peptide. The peptide can include a peptide sequence of one of SEQ ID NOs: 1, 5-38, or 40-69. The conformationally-constrained kinked portion can be a majority portion or minority of the peptide. The peptide can include one of Formulae 1-1C, wherein: CC-Peptide includes a peptide that conformationally constrains the ED-KP; Peptide independently includes natural, unnatural, essential or non-essential aromatic, aliphatic, or other amino acids having L or D configuration; ED-KP includes an endosomal-disrupting kinked peptide; Xaa, Xaa1, and Xaa2 are independently one or more natural or non-natural amino acids, essential amino acids, or non-essential amino acids, or derivatives of amino acids having L or D configuration; L1 and L2 are independently linkers; and n1, n2, n3, and n4 are independently 0-50.
摘要翻译： 构象约束的扭结肽包括：构象约束部分和连接到构象约束扭曲部分的构象约束部分的扭结部分，扭结部分包含内体破坏肽。 肽可以包括SEQ ID NO：1,538或40-69之一的肽序列。 构象约束的扭结部分可以是肽的多数部分或少数。 肽可以包括式1-1C之一，其中：CC-肽包括构象地约束ED-KP的肽; 肽独立地包括具有L或D构型的天然，非天然，必需或非必需的芳族，脂族或其他氨基酸; ED-KP包括内体破坏性扭结肽; Xaa，Xaa1和Xaa2独立地是一个或多个天然或非天然氨基酸，必需氨基酸或非必需氨基酸，或具有L或D构型的氨基酸的衍生物; L1和L2分别是接头; n1，n2，n3和n4独立地为0-50。
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