公开(公告)号：US20210122712A1

公开(公告)日：2021-04-29

申请号：US17076852

申请日：2020-10-22

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Scott D. Larsen ,  James A. Shayman ,  Kim Hutchings ,  Neil Moss ,  Qin Jiang ,  Nicholas Mayhew ,  Emily Freeman ,  Zohreh Saijadi Hashemi

IPC: C07D205/04 ,  C07D207/09 ,  C07D405/12

Abstract: Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.

公开(公告)号：US10329283B2

公开(公告)日：2019-06-25

申请号：US15738606

申请日：2016-06-27

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Scott D. Larsen ,  John J. G. Tesmer ,  Helen Waldschmidt ,  Kristoff Homan ,  Michael William Wilson

IPC: C07D405/14 ,  C07D401/14 ,  C07D401/12 ,  C07D405/12 ,  A61P9/00 ,  A61P9/12

Abstract: Disclosed herein are novel GRK inhibitors and methods for their use in treating or preventing heart disease, such as cardiac failure, cardiac hypertrophy, and hypertension. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof, wherein the substituents are as described.

公开(公告)号：US20150297577A1

公开(公告)日：2015-10-22

申请号：US14647770

申请日：2013-11-26

Applicant: The Regents of the University of Michigan

Inventor： Ronald Buckanovich ,  Scott D. Larsen ,  Kun Yang

IPC: A61K31/4439 ,  A61K45/06 ,  A61K31/437 ,  A61K31/136 ,  A61K31/4035

CPC classification number: A61K31/4439 ,  A61K31/136 ,  A61K31/337 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/437 ,  A61K31/555 ,  A61K33/24 ,  A61K45/06 ,  C07D209/04 ,  C07D401/04 ,  C07D471/04 ,  G01N33/574 ,  A61K2300/00

Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against cancer stem cells.

Abstract translation: 本发明涉及化学化合物，其发现方法及其治疗和研究用途。 特别地，本发明提供了作为抗癌干细胞的治疗剂的化合物。

公开(公告)号：US11944626B2

公开(公告)日：2024-04-02

申请号：US16311533

申请日：2017-06-20

Applicant: The Regents of the University of Michigan ,  Indiana University Research and Technology Corporation

Inventor： Scott D. Larsen ,  Brandt C. Huddle ,  Kun Yang ,  Ronald Buckanovich ,  Thomas Hurley

IPC: A61K31/519 ,  A61K31/337 ,  A61K31/4745 ,  A61K31/522 ,  A61K31/555 ,  A61K31/7068 ,  A61K39/395 ,  A61K45/06 ,  A61P31/00 ,  A61P35/00 ,  C07D487/04

CPC classification number: A61K31/519 ,  A61K31/337 ,  A61K31/4745 ,  A61K31/522 ,  A61K31/555 ,  A61K31/7068 ,  A61K39/395 ,  A61K45/06 ,  A61P31/00 ,  A61P35/00 ,  C07D487/04 ,  A61K31/522 ,  A61K2300/00 ,  A61K31/555 ,  A61K2300/00 ,  A61K31/337 ,  A61K2300/00 ,  A61K31/4745 ,  A61K2300/00 ,  A61K31/7068 ,  A61K2300/00

Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a thiopyrimidinone structure which function as inhibitors of ALDH protein, and their use as therapeutics for the treatment of cancer and other diseases.

公开(公告)号：US20230212123A1

公开(公告)日：2023-07-06

申请号：US17920794

申请日：2021-04-20

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Scott D. Larsen ,  James A. Shayman ,  Michael William Wilson ,  Neil Moss

IPC: C07D213/64 ,  C07D213/65 ,  C07D213/40 ,  C07D213/68 ,  C07D401/06 ,  C07D213/61 ,  A61K45/06

CPC classification number: C07D213/64 ,  A61K45/06 ,  C07D213/40 ,  C07D213/61 ,  C07D213/65 ,  C07D213/68 ,  C07D401/06

Abstract: Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.

公开(公告)号：US20180186779A1

公开(公告)日：2018-07-05

申请号：US15738606

申请日：2016-06-27

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Scott D. Larsen ,  John J.G. Tesmer ,  Helen Waldschmidt ,  Kristoff Homan ,  Michael William Wilson

IPC: C07D405/14 ,  C07D405/12 ,  C07D401/12 ,  C07D401/14 ,  A61P9/00 ,  A61P9/12

CPC classification number: C07D405/14 ,  A61P9/00 ,  A61P9/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12

Abstract: Disclosed herein are novel GRK inhibitors and methods for their use in treating or preventing heart disease, such as cardiac failure, cardiac hypertrophy, and hypertension. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof, wherein the substituents are as described.

公开(公告)号：US09468632B2

公开(公告)日：2016-10-18

申请号：US14647770

申请日：2013-11-26

Applicant: The Regents of the University of Michigan

Inventor： Ronald Buckanovich ,  Scott D. Larsen ,  Kun Yang

IPC: A61K31/404 ,  A61K31/4439 ,  A61K45/06 ,  A61K31/337 ,  A61K31/555 ,  A61K33/24 ,  C07D401/04 ,  C07D471/04 ,  C07D209/04 ,  G01N33/574 ,  A61K31/136 ,  A61K31/4035 ,  A61K31/437

CPC classification number: A61K31/4439 ,  A61K31/136 ,  A61K31/337 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/437 ,  A61K31/555 ,  A61K33/24 ,  A61K45/06 ,  C07D209/04 ,  C07D401/04 ,  C07D471/04 ,  G01N33/574 ,  A61K2300/00

Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against cancer stem cells.

Abstract translation: 本发明涉及化学化合物，其发现方法及其治疗和研究用途。 特别地，本发明提供了作为抗癌干细胞的治疗剂的化合物。

公开(公告)号：US20150132352A1

公开(公告)日：2015-05-14

申请号：US14397798

申请日：2013-05-02

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN ,  THE CURATORS OF THE UNIVERSITY OF MISSOURI

Inventor： Hongmin Sun ,  Bryan Yestrepsky ,  David Ginsburg ,  Scott D. Larsen

IPC: A61K31/517 ,  A01N43/54 ,  C07D471/10 ,  C07D491/107 ,  C07D487/10 ,  A61L31/16 ,  A61K31/505 ,  A61K31/5377 ,  A01N43/84 ,  A61K45/06 ,  A61L31/08 ,  C07D239/70 ,  C07D239/56

CPC classification number: A61K31/517 ,  A01N43/54 ,  A01N43/84 ,  A01N43/90 ,  A61K31/505 ,  A61K31/5377 ,  A61K45/06 ,  A61L31/08 ,  A61L31/16 ,  A61L2300/404 ,  C07D239/56 ,  C07D239/70 ,  C07D471/10 ,  C07D487/10 ,  C07D491/107

Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).

Abstract translation: 本发明涉及化学化合物，其发现方法及其治疗和研究用途。 特别地，本发明提供了作为抗细菌感染（例如生物膜）的治疗剂的化合物。

公开(公告)号：US10023564B2

公开(公告)日：2018-07-17

申请号：US15501888

申请日：2015-08-10

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Scott D. Larsen ,  Kristoff Homan ,  Helen Waldschmidt ,  John J. G. Tesmer

IPC: C07D413/14 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

Abstract: Disclosed herein are novel GRK2 inhibitors and methods for their use in treating or preventing heart disease, such as cardiac failure, cardiac hypertrophy, and hypertension. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: wherein the substituents are as described.

公开(公告)号：US20180022697A1

公开(公告)日：2018-01-25

申请号：US15546320

申请日：2016-02-01

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Scott D. Larsen ,  Akira Abe ,  Liming Shu ,  Michael William Wilson ,  Richard F. Keep ,  Duxin Sun ,  James A. Shayman

IPC: C07D207/06 ,  C07D263/20 ,  C07D207/10 ,  C07D295/13 ,  C07D205/04

CPC classification number: C07D207/06 ,  A61K31/4015 ,  C07D205/04 ,  C07D207/04 ,  C07D207/09 ,  C07D207/10 ,  C07D263/20 ,  C07D263/24 ,  C07D295/125 ,  C07D295/13

Abstract: Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.