公开(公告)号：US11957657B2

公开(公告)日：2024-04-16

申请号：US17368161

申请日：2021-07-06

Applicant: Trustees of Tufts College

Inventor： William W. Bachovchin ,  Hung-sen Lai ,  Wengen Wu

IPC: A61K31/402 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/69 ,  A61K35/13 ,  A61K39/39 ,  A61K45/06 ,  A61P35/00 ,  A61P37/04 ,  A61K39/00

CPC classification number: A61K31/402 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/69 ,  A61K35/13 ,  A61K39/39 ,  A61K45/06 ,  A61P35/00 ,  A61P37/04 ,  A61K2039/505 ,  A61K31/69 ,  A61K2300/00

Abstract: Disclosed are combination therapies including administration of I-DASH inhibitors and PGE2 antagonists, and the use of such therapies in the treatment of cell proliferative diseases.

公开(公告)号：US20230390241A1

公开(公告)日：2023-12-07

申请号：US18111143

申请日：2023-02-17

Applicant: Trustees of Tufts College

Inventor： William W. Bachovchin ,  Hung-sen Lai ,  Wengen Wu

IPC: A61K31/402 ,  A61K31/69 ,  A61K45/06 ,  A61K39/39 ,  A61P37/04 ,  A61P35/00 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/4439 ,  A61K35/13

CPC classification number: A61K31/402 ,  A61K31/69 ,  A61K45/06 ,  A61K39/39 ,  A61P37/04 ,  A61P35/00 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/4439 ,  A61K35/13 ,  A61K2039/505

Abstract: Disclosed are potent immuno-DASH inhibitors, and their use in the treatment of cell proliferative diseases.

公开(公告)号：US11583516B2

公开(公告)日：2023-02-21

申请号：US16331181

申请日：2017-09-07

Applicant: Trustees of Tufts College

Inventor： William W. Bachovchin ,  Hung-sen Lai ,  Wengen Wu

IPC: A61K31/402 ,  A61K31/69 ,  A61K45/06 ,  A61K39/39 ,  A61P37/04 ,  A61P35/00 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/4439 ,  A61K35/13 ,  A61K39/00

Abstract: Disclosed are potent immuno-DASH inhibitors and their use in the treatment of cell proliferative diseases.

公开(公告)号：US11559537B2

公开(公告)日：2023-01-24

申请号：US16603502

申请日：2018-04-06

Applicant: Trustees of Tufts College

Inventor： William W. Bachovchin ,  Hung-sen Lai ,  Wengen Wu

IPC: A61K31/415 ,  A61K31/69 ,  A61P35/00 ,  A61K31/635 ,  A61K45/06

Abstract: Disclosed are combination therapies including administration of Caspase-1 dependent anticancer agents and PGE2 antagonists, and the use of such therapies in the treatment of cell proliferative diseases.

公开(公告)号：US20190209525A1

公开(公告)日：2019-07-11

申请号：US16331181

申请日：2017-09-07

Applicant: Trustees of Tufts College

Inventor： William W. Bachovchin ,  Hung-sen Lai ,  Wengen Wu

IPC: A61K31/402 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/4025 ,  A61P35/00 ,  A61P37/04 ,  A61K35/13

CPC classification number: A61K31/402 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/69 ,  A61K35/13 ,  A61K39/39 ,  A61K45/06 ,  A61K2039/505 ,  A61P35/00 ,  A61P37/04 ,  A61K2300/00

Abstract: Disclosed are potent immuno-DASH inhibitors, and their use in the treatment of cell proliferative diseases.

公开(公告)号：US20170319609A1

公开(公告)日：2017-11-09

申请号：US15655317

申请日：2017-07-20

Applicant: Trustees of Tufts College

Inventor： William W. Bachovchin ,  Hung-sen Lai ,  David G. Sanford ,  Sarah E. Poplawski ,  Wengen Wu

IPC: A61K31/704 ,  A61K47/64

CPC classification number: A61K31/704 ,  A61K47/545 ,  A61K47/62 ,  A61K47/64

Abstract: Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.

公开(公告)号：US20170119901A1

公开(公告)日：2017-05-04

申请号：US15318627

申请日：2015-06-15

Applicant: TRUSTEES OF TUFTS COLLEGE

Inventor： William W. Bachovchin ,  Hung-sen Lai ,  David G. Sanford ,  Sarah E. Poplawski ,  Wengen Wu

IPC: A61K38/00 ,  A61K31/7068 ,  A61K31/4375 ,  A61K31/4155 ,  A61K31/519 ,  A61K31/517 ,  A61K31/337 ,  A61K31/69 ,  A61K31/704 ,  A61K31/4545

CPC classification number: A61K31/337 ,  A61K31/4155 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/517 ,  A61K31/519 ,  A61K31/69 ,  A61K31/704 ,  A61K31/7068 ,  A61K47/54 ,  A61K47/64

Abstract: Disclosed are prodrugs of therapeutic or imaging agents, which prodrugs are selectively cleaved by fibroblast activating protein (FAP) to release the agents. Upon cleavage by FAP of the FAP substrate, the prodrug releases the agent in its active form or in a form that is readily metabolized to its active form. Pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation are also disclosed.

公开(公告)号：US09192646B2

公开(公告)日：2015-11-24

申请号：US14572015

申请日：2014-12-16

Applicant: Trustees of Tufts College

Inventor： William W. Bachovchin ,  Hung-sen Lai ,  Wengen Wu

IPC: A61K31/69 ,  A61K38/05 ,  C07D207/10 ,  C07D207/16 ,  C07D241/24 ,  C07D403/12 ,  A61K38/28 ,  A61K45/06 ,  C07F5/02 ,  C12N9/99

CPC classification number: A61K31/69 ,  A61K38/05 ,  A61K38/28 ,  A61K45/06 ,  C07D207/10 ,  C07D207/16 ,  C07D241/24 ,  C07D403/12 ,  C07F5/025 ,  C12N9/99

Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.

公开(公告)号：US20240366807A1

公开(公告)日：2024-11-07

申请号：US18683663

申请日：2022-08-18

Applicant: Trustees of tufts college

Inventor： William W. Bachovchin ,  Hung-sen Lai ,  Wengen Wu

IPC: A61K51/04 ,  A61P35/00 ,  C07B59/00 ,  C12N9/99

Abstract: Disclosed are compounds useful for imaging cells that overexpress FAP, and for treating cancer. Also disclosed are methods of making said compounds.

公开(公告)号：US20220370647A1

公开(公告)日：2022-11-24

申请号：US17211481

申请日：2021-03-24

Applicant: Trustees of Tufts College

Inventor： William W. Bachovchin ,  Hung-sen Lai ,  Wengen Wu

IPC: A61K51/04

Abstract: The tumor stroma, which accounts for a large part of the tumor mass, represents an attractive target for the delivery of diagnostic and therapeutic compounds. Here, the focus is notably on a subpopulation of stromal cells, known as cancer-associated fibroblasts, which are present in more than 90% of epithelial carcinomas, including pancreatic, colon, and breast cancer. Cancer-associated fibroblasts feature high expression of FAP, which is not detectable in adult normal tissue but is associated with a poor prognosis in cancer patients. The present invention provides small-molecule radiopharmaceutical and imaging agents based on a FAP-specific inhibitor.