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.

公开(公告)号：US10813998B2

公开(公告)日：2020-10-27

申请号：US16285358

申请日：2019-02-26

Applicant: Wisconsin Alumni Research Foundation

Inventor： Jamey Weichert ,  Anatoly Pinchuk ,  Wolfgang Axel Tome

IPC: A61K41/00 ,  A61K49/10 ,  A61K51/04 ,  A61K49/08 ,  G01N33/574 ,  G01N33/58 ,  C07F9/6515 ,  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 thereof. 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：US20190184014A1

公开(公告)日：2019-06-20

申请号：US16285358

申请日：2019-02-26

Applicant: Wisconsin Alumni Research Foundation

Inventor： Jamey Weichert ,  Anatoly Pinchuk ,  Wolfgang Axel Tome

IPC: A61K41/00 ,  A61N5/10 ,  A61K49/08 ,  A61K49/10 ,  C07F9/11 ,  C07F9/09 ,  C07F9/6561 ,  C07F9/6524 ,  C07F9/6515 ,  G01N33/60 ,  A61K51/04 ,  C07F9/10 ,  G01N33/58 ,  G01N33/574

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 thereof. 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：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：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.