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公开(公告)号：US20210008203A1
公开(公告)日：2021-01-14
申请号：US17032132
申请日：2020-09-25
Applicant: Wisconsin Alumni Research Foundation
Inventor： Jamey Weichert , Anatoly Pinchuk , Wolfgang Axel Tome
IPC: A61K41/00 , A61K49/08 , A61K49/10 , G01N33/574 , G01N33/58 , C07F9/6515 , C07F9/6524 , C07F9/6561 , C07F9/09 , C07F9/11 , A61K51/04 , A61N5/10 , C07F9/10 , G01N33/60
Abstract: Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: or a salt therof. R1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is —H, —OH, —COOH, —COOX, —OCOX, or —OX, wherein X is an alkyl or an arylalkyl; R2 is —N+H3, —N+H2Z, —N+HZ2, or —N+Z3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.
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公开(公告)号：US20190184040A1
公开(公告)日：2019-06-20
申请号：US16222364
申请日：2018-12-17
Applicant: Wisconsin Alumni Research Foundation
Inventor： Jamey Weichert , Reinier Hernandez , Ray Zhang , Anatoly Pinchuk
CPC classification number: A61K51/0474 , A61B5/055 , A61K9/0019 , C07B59/002
Abstract: Dual-modality contrast agents are disclosed herein, having the general formula: R1 includes a chelating moiety that is chelated to a Mn2+ isotope. The disclosed contrast agents differentially target a wide range of malignant tumor tissues, and can be simultaneously used as contrast agents for both magnetic resonance imaging (MRI) and positron emission topography (PET) imaging. Accordingly, the disclosed contrast agent can be used in diagnosing and monitoring solid tumor cancers.
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公开(公告)号：US20180022768A1
公开(公告)日：2018-01-25
申请号：US15343604
申请日：2016-11-04
Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
Inventor： Jamey Weichert , Anatoly Pinchuk , Reinier Hernandez
IPC: C07F9/6524 , G01N33/60 , A61N5/10 , A61K51/04
CPC classification number: C07F9/6524 , A61K51/0482 , A61K51/0489 , A61N5/10 , C07B59/004 , G01N33/574 , G01N33/60
Abstract: Alkylphosphocholine analogs incorporating a chelating moiety that chelates a radioactive metal isotope are disclosed herein. The alkylphophocholine analogs, which can be used to treat or detect solid tumors, have the formula: R1 includes a chelating agent that is chelated to a metal atom, wherein the metal atom is a positron or single photon emitting metal isotope with a half life of greater than or equal to 4 hours, or an alpha, beta or Auger emitting metal isotope with a half life of greater than 6 hours and less than 30 days; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is —H, —OH, —COOH, —COOX, —OCOX, or —OX, wherein X is an alkyl or an arylalkyl; R2 is —N+H3, —N+H2Z, —N+HZ2, or —N+Z3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2.
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公开(公告)号：US20250090645A1
公开(公告)日：2025-03-20
申请号：US18904511
申请日：2024-10-02
Applicant: Wisconsin Alumni Research Foundation
Inventor： Jamey Weichert , Paul M. Sondel , Anatoly Pinchuk , Zachary Morris , Mario Otto , Bryan Bednarz
IPC: A61K39/00 , A61K39/39 , A61K39/395 , A61K51/04
Abstract: A method of treating a malignant solid tumor in a subject is disclosed herein. The method includes the steps of administering to the subject an immunomodulatory dose of a radiohalogenated compound that is differentially taken up by and retained within malignant solid tumor tissue, and performing in situ tumor vaccination in the subject by intratumorally injecting into (or treating via a separate method) at least one of the malignant solid tumors a composition that includes one or more agents capable of stimulating specific immune cells within the tumor microenvironment. In certain exemplary embodiments, the radiohalogenated compound has the formula: wherein R1 is a radioactive halogen isotope, n is 18 and R2 is —N+(CH3)3.
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公开(公告)号：US20220105207A1
公开(公告)日：2022-04-07
申请号：US17552984
申请日：2021-12-16
Applicant: Wisconsin Alumni Research Foundation
Inventor： Jamey Weichert , Reinier Hernandez , Ray Zhang , Anatoly Pinchuk
Abstract: Dual-modality contrast agents are disclosed herein, having the general formula: R1 includes a chelating moiety that is chelated to a Mn2+ isotope. The disclosed contrast agents differentially target a wide range of malignant tumor tissues, and can be simultaneously used as contrast agents for both magnetic resonance imaging (MRI) and positron emission topography (PET) imaging. Accordingly, the disclosed contrast agent can be used in diagnosing and monitoring solid tumor cancers.
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Patent Agency Ranking
公开(公告)号：US11186598B2
公开(公告)日：2021-11-30
申请号：US16891181
申请日：2020-06-03
Applicant: Wisconsin Alumni Research Foundation
Inventor： Jamey Weichert , Anatoly Pinchuk , Reinier Hernandez
IPC: A61K51/00 , A61M36/14 , C07F9/6524 , C07B59/00 , G01N33/574 , A61K51/04 , A61N5/10 , G01N33/60
Abstract: Alkylphosphocholine analogs incorporating a chelating moiety that chelates a radioactive metal isotope are disclosed herein. The alkylphophocholine analogs, which can be used to treat or detect solid tumors, have the formula: R1 includes a chelating agent that is chelated to a metal atom, wherein the metal atom is a positron or single photon emitting metal isotope with a half life of greater than or equal to 4 hours, or an alpha, beta or Auger emitting metal isotope with a half life of greater than 6 hours and less than 30 days; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is —H, —OH, —COOH, —COOX, —OCOX, or —OX, wherein X is an alkyl or an arylalkyl; R2 is —N+H3, —N+H2Z, —N+HZ2, or —N+Z3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2.
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公开(公告)号：US20240066156A1
公开(公告)日：2024-02-29
申请号：US18345385
申请日：2023-06-30
Applicant: Wisconsin Alumni Research Foundation
Inventor： Jamey Weichert , Paul Sondel , Anatoly Pinchuk , Zachary Morris , Mario Otto , Bryan Bednarz , Peter Carlson
IPC: A61K51/04 , A61K9/00 , A61K38/20 , A61K39/395 , C07K16/30
CPC classification number: A61K51/0408 , A61K9/0019 , A61K38/2013 , A61K39/39558 , A61K51/0497 , C07K16/3084 , A61K2039/545
Abstract: The disclosed method of treating a malignant solid tumor in a subject includes the steps of administering to the subject an immunomodulatory dose of a radioactive phospholipid metal chelate compound that is differentially retained within malignant solid tumor tissue, and performing in situ tumor vaccination in the subject by introducing into at least one of the malignant solid tumors one or more agents capable of stimulating specific immune cells within the tumor microenvironment, or by performing another method of in situ tumor vaccination. In a non-limiting example, the radioactive phospholipid metal chelate compound has the formula:
wherein R1 comprises a chelating agent that is chelated to a metal atom, wherein the metal atom is an alpha, beta or Auger emitting metal isotope with a half life of greater than 6 hours and less than 30 days. In one such embodiment, a is 1, n is 18, m is 0, b is 1, and R2 is —N+(CH3)3.-
公开(公告)号：US20230310610A1
公开(公告)日：2023-10-05
申请号：US18175246
申请日：2023-02-27
Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
Inventor： Jamey Weichert , Anatoly Pinchuk , Wolfgang Axel Tome
IPC: A61K41/00 , A61K49/08 , A61K49/10 , G01N33/574 , G01N33/58 , C07F9/6515 , C07F9/6524 , C07F9/6561 , C07F9/09 , C07F9/11 , A61K51/04 , A61N5/10 , C07F9/10 , G01N33/60
CPC classification number: A61K41/009 , A61K49/085 , A61K49/10 , A61K49/106 , G01N33/574 , G01N33/58 , C07F9/6515 , C07F9/6524 , C07F9/6561 , C07F9/091 , C07F9/11 , A61K51/0482 , A61N5/1039 , A61N5/1048 , A61N5/1077 , C07F9/10 , G01N33/60 , A61K2039/505
Abstract: Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula:
or a salt therof. R1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is —H, —OH, —COOH, —COOX, —OCOX, or —OX, wherein X is an alkyl or an arylalkyl; R2 is —N+H3, —N+H2Z, —N+HZ2, or —N+Z3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.-
公开(公告)号：US11730834B2
公开(公告)日：2023-08-22
申请号：US16914563
申请日：2020-06-29
Applicant: Wisconsin Alumni Research Foundation
Inventor： Jamey Weichert , Paul Sondel , Anatoly Pinchuk , Zachary Morris , Mario Otto , Bryan Bednarz , Peter Carlson
CPC classification number: A61K51/0408 , A61K9/0019 , A61K38/2013 , A61K39/39558 , A61K51/0497 , C07K16/3084 , A61K2039/53 , A61K2039/545 , A61K2039/55533 , A61K2039/585
Abstract: The disclosed method of treating a malignant solid tumor in a subject includes the steps of administering to the subject an immunomodulatory dose of a radioactive phospholipid metal chelate compound that is differentially retained within malignant solid tumor tissue, and performing in situ tumor vaccination in the subject by introducing into at least one of the malignant solid tumors one or more agents capable of stimulating specific immune cells within the tumor microenvironment, or by performing another method of in situ tumor vaccination. In a non-limiting example, the radioactive phospholipid metal chelate compound has the formula:
wherein R1 comprises a chelating agent that is chelated to a metal atom, wherein the metal atom is an alpha, beta or Auger emitting metal isotope with a half life of greater than 6 hours and less than 30 days. In one such embodiment, a is 1, n is 18, m is 0, b is 1, and R2 is —N+(CH3)3.-
公开(公告)号：US11623007B2
公开(公告)日：2023-04-11
申请号：US17032132
申请日：2020-09-25
Applicant: Wisconsin Alumni Research Foundation
Inventor： Jamey Weichert , Anatoly Pinchuk , Wolfgang Axel Tome
IPC: A61K41/00 , A61K49/10 , A61K51/04 , C07F9/6515 , A61K49/08 , G01N33/574 , G01N33/58 , C07F9/6524 , C07F9/6561 , C07F9/09 , C07F9/11 , A61N5/10 , C07F9/10 , G01N33/60 , A61K39/00
Abstract: Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: or a salt therof. R1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is —H, —OH, —COOH, —COOX, —OCOX, or —OX, wherein X is an alkyl or an arylalkyl; R2 is —N+H3, —N+H2Z, —N+HZ2, or —N+Z3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.
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