公开(公告)号：US12213981B2

公开(公告)日：2025-02-04

申请号：US18201864

申请日：2023-05-25

Applicant: L.E.A.F. HOLDINGS GROUP LLC

Inventor： Clet Niyikiza ,  Victor Mandla Moyo

IPC: A61K31/519 ,  A61K47/26 ,  A61K47/54 ,  A61K47/64 ,  A61K47/68 ,  A61K47/69 ,  A61K49/00 ,  A61P35/00

Abstract: The disclosure relates generally to alpha polyglutamated pralatrexate, formulations containing liposomes filled with alpha polyglutamated pralatrexate, methods of making the alpha polyglutamated pralatrexate and liposome containing formulations, and methods of using polyglutamated alpha polyglutamated pralatrexate and liposome containing formulations to treat hyperproliferative disorders (e.g., cancer) and disorders of the immune system (e.g., an autoimmune disease such as rheumatoid arthritis).

公开(公告)号：US12048766B2

公开(公告)日：2024-07-30

申请号：US16967203

申请日：2019-02-07

Applicant: L.E.A.F. HOLDINGS GROUP LLC

Inventor： Clet Niyikiza ,  Victor Mandla Moyo

IPC: A61K9/127 ,  A61K31/4015 ,  A61K31/513 ,  A61K31/519 ,  A61K45/06 ,  A61K47/26 ,  A61K47/69 ,  A61K49/00 ,  A61P35/00

CPC classification number: A61K9/127 ,  A61K9/1271 ,  A61K9/1272 ,  A61K9/1277 ,  A61K31/4015 ,  A61K31/513 ,  A61K31/519 ,  A61K45/06 ,  A61K47/26 ,  A61K47/6913 ,  A61K49/0054 ,  A61P35/00

Abstract: The disclosure relates generally to gamma polyglutamated tetrahydrofolate compositions, including delivery vehicles such as liposomes containing the gamma polyglutamated tetrahydrofolate, and methods of making and using the gamma polyglutamated tetrahydrofolate compositions to treat hyperproliferative disorders (e.g., cancer) and disorders of the immune system (e.g., inflammation and autoimmune diseases such as rheumatoid arthritis). The disclosed compositions also have uses in combination therapy with one or more therapeutic agents to enhance the effectiveness or to reduce the toxicities associated with the therapeutic agent(s).

公开(公告)号：US11701432B2

公开(公告)日：2023-07-18

申请号：US17875724

申请日：2022-07-28

Applicant: L.E.A.F. HOLDINGS GROUP LLC

Inventor： Clet Niyikiza ,  Victor Mandla Moyo

IPC: A61K47/69 ,  A61K47/64 ,  A61K47/54 ,  A61K47/68 ,  A61P19/02 ,  A61P35/00 ,  A61K9/127 ,  A61K31/517 ,  A61K31/519 ,  A61K45/06 ,  A61K47/10 ,  C07K16/28 ,  B82Y5/00

CPC classification number: A61K47/6913 ,  A61K9/1271 ,  A61K31/517 ,  A61K31/519 ,  A61K45/06 ,  A61K47/10 ,  A61K47/545 ,  A61K47/64 ,  A61K47/645 ,  A61K47/6801 ,  A61K47/6849 ,  A61K47/6911 ,  A61P19/02 ,  A61P35/00 ,  C07K16/28 ,  A61K2300/00 ,  B82Y5/00 ,  C07K2317/73 ,  A61K31/519 ,  A61K2300/00

Abstract: The disclosure relates generally to polyglutamated antifolates, formulations containing liposomes filled with the polyglutamated antifolates, methods of making the polyglutamated antifolates and liposome containing formulations, and methods of using the polyglutamated antifolates and liposome containing formulations to treat hyerproliferative disorders (e.g., cancer) and disorders of the immune system (e.g., an autoimmune disease such as rheumatoid arthritis).

公开(公告)号：US20230000997A1

公开(公告)日：2023-01-05

申请号：US17632956

申请日：2020-08-06

Applicant: L.E.A.F. HOLDINGS GROUP LLC

Inventor： Clet NIYIKIZA ,  Victor Mandla MOYO ,  Bolin GENG

IPC: A61K47/64 ,  A61K31/519 ,  A61K9/127

Abstract: Provided herein are methods of preparing polyglutamated compounds, such as polyglutamated antifolates, and/or pharmaceutical compositions such as liposomal compositions comprising the same, Also provided herein are substantially pure polyglutamated compounds, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition such as liposomal composition comprising the same. The present disclosure further provides methods of using the polyglutamated compounds and compositions to treat diseases including hyperproliferative diseases such as cancer, disorders of the immune system such as rheumatoid arthritis, and infectious diseases such as HIV, malaria, and schistomiasis.

公开(公告)号：US20220088218A1

公开(公告)日：2022-03-24

申请号：US17544182

申请日：2021-12-07

Applicant: L.E.A.F. HOLDINGS GROUP LLC

Inventor： Clet NIYIKIZA ,  Victor Mandla MOYO

IPC: A61K47/69 ,  A61K31/519 ,  C07K16/28 ,  A61K47/64 ,  A61K47/68 ,  A61K9/127 ,  A61K31/517 ,  A61K45/06 ,  A61K47/54 ,  A61P19/02 ,  A61P35/00 ,  A61K47/10

Abstract: The disclosure relates generally to polyglutamated antifolates, formulations containing liposomes filled with the polyglutamated antifolates, methods of making the polyglutamated antifolates and liposome containing formulations, and methods of using the polyglutamated antifolates and liposome containing formulations to treat hyerproliferative disorders (e.g., cancer) and disorders of the immune system (e.g., an autoimmune disease such as rheumatoid arthritis).

公开(公告)号：US20210283055A1

公开(公告)日：2021-09-16

申请号：US17052412

申请日：2019-05-03

Applicant: L.E.A.F. HOLDINGS GROUP LLC

Inventor： Clet NIYIKIZA ,  Victor Mandla MOYO ,  Bolin GENG ,  Zhenghong XU ,  Kaniz KHALIFA ,  Gwangseong KIM

IPC: A61K9/127 ,  A61K31/202

Abstract: Provided herein are pharmaceutical compositions comprising carotenoids, including liposomes that encapsulate carotenoids including ionizable carotenoids such as trans-crocetin. The provided compositions have uses in treating diseases, disorders and conditions associated with, but not limited to, infection, endotoxemia, inflammation, sepsis, ischemia, hypoxia, shock, stroke, lung injury, wound healing, traumatic injury, reperfusion injury, cardiovascular disease, kidney disease, liver disease, inflammatory disease, metabolic disease, pulmonary disorders, blood related disorders and hyperproliferative diseases such as cancer. Methods of making, delivering, and using the pharmaceutical compositions are also provided.

公开(公告)号：US20210154196A1

公开(公告)日：2021-05-27

申请号：US16967316

申请日：2019-02-07

Applicant: L.E.A.F. HOLDINGS GROUP LLC

Inventor： Clet NIYIKIZA ,  Victor Mandla MOYO

IPC: A61K31/519 ,  A61K9/127 ,  A61K47/64 ,  A61K47/69 ,  A61K47/26 ,  A61K31/282 ,  A61K39/395 ,  A61K39/39 ,  A61K33/243 ,  A61P35/00

Abstract: The disclosure relates generally to gamma polyglutamated methotrexate compositions, including delivery vehicles such as liposomes containing the gamma polyglutamated methotrexate, and methods of making and using the gamma polyglutamated methotrexate compositions to treat hyperproliferative disorders (e.g., cancer) and disorders of the immune system (e.g., inflammation and autoimmune diseases such as rheumatoid arthritis).

公开(公告)号：US10940112B2

公开(公告)日：2021-03-09

申请号：US15587018

申请日：2017-05-04

Applicant: L.E.A.F. Holdings Group LLC

Inventor： Clet Niyikiza ,  Victor Moyo ,  Zhenghong Xu ,  Kaniz Khalifa

IPC: A61K9/127 ,  C07K16/28 ,  A61K45/06 ,  A61K47/68 ,  A61K47/69 ,  A61K33/243 ,  A61P31/18 ,  A61K31/337 ,  A61K31/555 ,  A61K31/4745 ,  A61P35/00 ,  A61K31/7068 ,  C07K16/30

Abstract: This disclosure relates to a targeted PEGylated liposomal gemcitabine (PLG) composition comprising a PEGylated liposome encapsulating one or more agents comprising gemcitabine and a targeting moiety; pharmaceutical composition and methods comprising PLG or producing PLG; and manufacturing equipment for performing the methods.

公开(公告)号：US20180236098A1

公开(公告)日：2018-08-23

申请号：US15675701

申请日：2017-08-11

Applicant: L.E.A.F. Holdings Group LLC

Inventor： Clet NIYIKIZA ,  Victor Mandla MOYO

IPC: A61K47/69 ,  A61K47/54 ,  A61K47/10 ,  A61P35/00 ,  A61P19/02

CPC classification number: A61K47/6913 ,  A61K31/519 ,  A61K45/06 ,  A61K47/10 ,  A61K47/545 ,  A61K47/645 ,  A61K47/6849 ,  A61K2300/00 ,  A61P19/02 ,  A61P35/00 ,  C07K16/28 ,  C07K2317/73

Abstract: The disclosure relates generally to polyglutamated antifolates, formulations containing liposomes filled with alpha or D-gamma polyglutamated antifolates, methods of making the polyglutamated antifolates and liposome containing formulations, and methods of using polyglutamated antifolates and liposome containing formulations to treat hyerproliferative disorders (e.g., cancer) and disorders of the immune system (e.g., an autoimmune disease such as rheumatoid arthritis).

公开(公告)号：US20250066468A1

公开(公告)日：2025-02-27

申请号：US18734619

申请日：2024-06-05

Applicant: L.E.A.F. HOLDINGS GROUP LLC

Inventor： Clet NIYIKIZA ,  Jose VARGHESE

IPC: C07K16/28 ,  A61K9/00 ,  A61K9/08 ,  A61K9/127 ,  A61K9/19 ,  A61K31/519 ,  A61K45/06 ,  A61K47/68 ,  A61K47/69

Abstract: The disclosure provides a liposomal antifolate composition comprising a liposome including an interior space, a bioactive antifolate agent disposed within said interior space, a steric stabilizer attached to an exterior of the liposome, and a targeting moiety comprising a protein with specific affinity for at least one folate receptor, said targeting moiety attached to at least one of the steric stabilizer and the exterior of the liposome.