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：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

IPC: A61K51/04 ,  A61K39/395 ,  A61K9/00 ,  A61K38/20 ,  A61K39/00 ,  C07K16/30

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：US20180126012A1

公开(公告)日：2018-05-10

申请号：US15809427

申请日：2017-11-10

Applicant: Wisconsin Alumni Research Foundation

Inventor： Jamey Weichert ,  Paul Sondel ,  Ravi Patel ,  Zachary Morris ,  Peter Carlson ,  Reinier Hernandez ,  Joseph Grudzinski

IPC: A61K51/04 ,  A61P35/00 ,  A61K41/00 ,  A61K51/10 ,  A61K9/00 ,  A61P35/04 ,  A61K38/20 ,  A61K39/395

CPC classification number: A61K51/0485 ,  A61K9/0019 ,  A61K38/2013 ,  A61K39/39541 ,  A61K39/39558 ,  A61K41/0038 ,  A61K51/0408 ,  A61K51/0489 ,  A61K51/0497 ,  A61K51/1045 ,  A61K2039/505 ,  A61N5/00 ,  A61N5/1001 ,  A61N2005/1021 ,  A61P35/00 ,  A61P35/04 ,  A61P37/04 ,  C07K14/52 ,  C07K16/2818 ,  C07K16/3084 ,  C07K2319/35 ,  A61K2300/00

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 ether metal chelate, a radiohalogenated phospholipid ether, or other targeted radiotherapy (TRT) agent that is differentially retained within malignant solid tumor tissue, and either (a) 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 (b) performing immunotherapy in the subject by systemically administering to the subject an immunostimulatory agent, such as an immune checkpoint inhibitor. In a non-limiting example, the radioactive phospholipid ether metal chelate or radiohalogenated phospholipid ether 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, or wherein R1 comprises a radioactive halogen isotope. 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：US20230398239A1

公开(公告)日：2023-12-14

申请号：US18182850

申请日：2023-03-13

Applicant: Wisconsin Alumni Research Foundation

Inventor： Jamey Weichert ,  Paul Sondel ,  Ravi Patel ,  Zachary Morris ,  Peter Carlson ,  Reinier Hernandez ,  Joseph Grudzinski

IPC: A61K51/04 ,  A61P35/00 ,  A61K41/00 ,  A61K51/10 ,  A61K39/395 ,  A61P35/04 ,  A61K38/20 ,  C07K16/30 ,  C07K14/52 ,  A61P37/04 ,  C07K16/28 ,  A61N5/00 ,  A61N5/10

CPC classification number: A61K51/0485 ,  A61P35/00 ,  A61K41/0038 ,  A61K51/1045 ,  A61K39/39558 ,  A61P35/04 ,  A61K51/0489 ,  A61K38/2013 ,  A61K51/0408 ,  C07K16/3084 ,  C07K14/52 ,  A61P37/04 ,  C07K16/2818 ,  A61K51/0497 ,  A61K39/39541 ,  A61N5/00 ,  A61N5/1001 ,  A61K9/0019

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 ether metal chelate, a radiohalogenated phospholipid ether, or other targeted radiotherapy (TRT) agent that is differentially retained within malignant solid tumor tissue, and either (a) 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 (b) performing immunotherapy in the subject by systemically administering to the subject an immunostimulatory agent, such as an immune checkpoint inhibitor. In a non-limiting example, the radioactive phospholipid ether metal chelate or radiohalogenated phospholipid ether 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, or wherein R1 comprises a radioactive halogen isotope. 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：US11633506B2

公开(公告)日：2023-04-25

申请号：US15809427

申请日：2017-11-10

Applicant: Wisconsin Alumni Research Foundation

Inventor： Jamey Weichert ,  Paul Sondel ,  Ravi Patel ,  Zachary Morris ,  Peter Carlson ,  Reinier Hernandez ,  Joseph Grudzinski

IPC: A61K51/04 ,  A61P35/00 ,  A61K41/00 ,  A61K51/10 ,  A61K39/395 ,  A61P35/04 ,  A61K38/20 ,  C07K16/30 ,  C07K14/52 ,  A61P37/04 ,  C07K16/28 ,  A61N5/00 ,  A61N5/10 ,  A61K9/00 ,  A61K39/00

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 ether metal chelate, a radiohalogenated phospholipid ether, or other targeted radiotherapy (TRT) agent that is differentially retained within malignant solid tumor tissue, and either (a) 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 (b) performing immunotherapy in the subject by systemically administering to the subject an immunostimulatory agent, such as an immune checkpoint inhibitor. In a non-limiting example, the radioactive phospholipid ether metal chelate or radiohalogenated phospholipid ether 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, or wherein R1 comprises a radioactive halogen isotope. 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：US10751430B2

公开(公告)日：2020-08-25

申请号：US15658535

申请日：2017-07-25

Applicant: Wisconsin Alumni Research Foundation

Inventor： Jamey Weichert ,  Paul Sondel ,  Anatoly Pinchuk ,  Zachary Morris ,  Mario Otto ,  Bryan Bednarz ,  Peter Carlson

IPC: A61K51/04 ,  A61K39/395 ,  A61K38/20 ,  C07K16/30 ,  A61K39/00 ,  A61K9/00

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：US20200330621A1

公开(公告)日：2020-10-22

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

IPC: A61K51/04 ,  A61K39/395 ,  A61K9/00 ,  A61K38/20 ,  C07K16/30

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：US20180021461A1

公开(公告)日：2018-01-25

申请号：US15658535

申请日：2017-07-25

Applicant: Wisconsin Alumni Research Foundation

Inventor： Jamey Weichert ,  Paul Sondel ,  Anatoly Pinchuk ,  Zachary Morris ,  Mario Otto ,  Bryan Bednarz ,  Peter Carlson

IPC: A61K51/04 ,  C07K16/30 ,  A61K38/20 ,  A61K9/00

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.