公开(公告)号：US20210038586A1

公开(公告)日：2021-02-11

申请号：US17075065

申请日：2020-10-20

Applicant: The University of Toledo

Inventor： William A. Maltese ,  Zehui Li ,  Christopher J. Trabbic ,  Paul W. Erhardt

IPC: A61K31/4439 ,  A61K31/53 ,  A61K31/5377

Abstract: Vacuole- or exosome-inducing indole-based chalcone and substituted triazole-hydrazone compounds that induce endosomal vacuolization and increase exosome yield, but do not trigger growth arrest or cell death, and methods of making and using are described.

公开(公告)号：US20210038571A1

公开(公告)日：2021-02-11

申请号：US17020062

申请日：2020-09-14

Applicant: The University of Toledo

Inventor： Bruce E. Heck ,  Dong Hyun Kim ,  Paul W. Erhardt ,  Brian J. Kress

IPC: A61K31/426 ,  G06F21/31 ,  A61K45/06 ,  A61K31/5575 ,  C07D277/30 ,  H04W12/06 ,  C07D277/22 ,  C07D277/24

Abstract: Peroxisome proliferator activated receptor (PPAR) compounds, and methods of using the same for treating bone fractures, treating osteoporosis and/or metabolic bone diseases, and inducing osteogenesis and/or chondrogenesis, are disclosed.

公开(公告)号：US20190147147A1

公开(公告)日：2019-05-16

申请号：US16246614

申请日：2019-01-14

Applicant: The University of Toledo

Inventor： Bruce E. Heck ,  Dong Hyun Kim ,  Paul W. Erhardt ,  Brian J. Kress

IPC: G06F21/31 ,  A61K31/5575 ,  C07D277/24 ,  H04W12/06 ,  C07D277/30 ,  C07D277/22 ,  A61K31/426 ,  A61K45/06

Abstract: Peroxisome proliferator activated receptor (PPAR) compounds, and methods of using the same for treating bone fractures, treating osteoporosis and/or metabolic bone diseases, and inducing osteogenesis and/or chondrogenesis, are disclosed.

公开(公告)号：US11524004B2

公开(公告)日：2022-12-13

申请号：US17020062

申请日：2020-09-14

Applicant: The University of Toledo

Inventor： Bruce E. Heck ,  Dong Hyun Kim ,  Paul W. Erhardt ,  Brian J. Kress

IPC: A61K31/4192 ,  A61K31/426 ,  C07D249/04 ,  A61P19/08 ,  G06F21/31 ,  A61K45/06 ,  A61K31/5575 ,  C07D277/30 ,  H04W12/06 ,  C07D277/22 ,  C07D277/24 ,  H04W12/04 ,  H04W12/08

Abstract: Peroxisome proliferator activated receptor (PPAR) compounds, and methods of using the same for treating bone fractures, treating osteoporosis and/or metabolic bone diseases, and inducing osteogenesis and/or chondrogenesis, are disclosed.

公开(公告)号：US10181018B2

公开(公告)日：2019-01-15

申请号：US15699054

申请日：2017-09-08

Applicant: The University of Toledo

Inventor： Bruce E. Heck ,  Dong Hyun Kim ,  Paul W. Erhardt ,  Brian J. Kress

IPC: C07D277/20 ,  C07D277/46 ,  C07D277/48 ,  G06F21/31 ,  H04W12/06 ,  A61K45/06 ,  A61K31/426 ,  A61K31/5575 ,  C07D277/22 ,  C07D277/24 ,  H04W12/04 ,  H04W12/08

Abstract: Peroxisome proliferator activated receptor (PPAR) compounds, and methods of using the same for treating bone fractures, treating osteoporosis and/or metabolic bone diseases, and inducing osteogenesis and/or chondrogenesis, are disclosed.

公开(公告)号：US20180012002A1

公开(公告)日：2018-01-11

申请号：US15699054

申请日：2017-09-08

Applicant: The University of Toledo

Inventor： Bruce E. Heck ,  Dong Hyun Kim ,  Paul W. Erhardt ,  Brian J. Kress

IPC: G06F21/31 ,  H04W12/06 ,  H04W12/04 ,  H04W12/08

CPC classification number: G06F21/31 ,  A61K31/426 ,  A61K31/5575 ,  A61K45/06 ,  C07D277/30 ,  H04W12/04 ,  H04W12/06 ,  H04W12/08 ,  A61K2300/00

Abstract: Peroxisome proliferator activated receptor (PPAR) compounds, and methods of using the same for treating bone fractures, treating osteoporosis and/or metabolic bone diseases, and inducing osteogenesis and/or chondrogenesis, are disclosed.

公开(公告)号：US09023871B2

公开(公告)日：2015-05-05

申请号：US14246558

申请日：2014-04-07

Applicant: The University of Toledo

Inventor： William A. Maltese ,  Paul W. Erhardt ,  Christopher Trabbic ,  Jean H. Overmeyer

IPC: C07D401/06 ,  A61K31/404 ,  A61K31/4439 ,  C07D209/12 ,  A61K45/06 ,  C07D403/06 ,  C07D209/08 ,  C40B40/04

CPC classification number: A61K31/404 ,  A61K31/4439 ,  A61K45/06 ,  C07D209/08 ,  C07D209/12 ,  C07D401/06 ,  C07D403/06 ,  C40B40/04 ,  A61K2300/00

Abstract: The present invention provides materials and methods to induce cell death by methuosis, a non-apoptotic cell death mechanism, to induce vacuolization without cell death, or to induce cell death without vacuolization. Small molecules herein are useful for treating cell proliferation disorders or anomalies, particularly, but not exclusively, cancer. Methods related to the research and pharmaceutical use of the small molecules are also provided herein.

Abstract translation: 本发明提供了通过甲基化诱导细胞死亡的材料和方法，非凋亡性细胞死亡机制，以诱导空泡化而没有细胞死亡，或者在没有空泡化的情况下诱导细胞死亡。 本文中的小分子可用于治疗细胞增殖障碍或异常，特别是但不排他地是癌症。 本文还提供了与小分子的研究和药物应用相关的方法。

公开(公告)号：US11986467B2

公开(公告)日：2024-05-21

申请号：US17861946

申请日：2022-07-11

Applicant: The University of Toledo

Inventor： Amit K. Tiwari ,  Chandrabose Karthikeyan ,  Haneen A. Amawi ,  Paul W. Erhardt ,  Piyush Trivedi

IPC: A61K31/4439 ,  A61K31/122 ,  C07D401/14 ,  C07D513/04

CPC classification number: A61K31/4439 ,  A61K31/122 ,  C07D401/14 ,  C07D513/04

Abstract: Compounds, compositions, and methods useful for inducing cancer cell death via methuosis, autophagy, or a combination thereof, are described. The compounds have a 4-pyridyl group linked by a heterocyclic group to an aryl, heteroaryl, aralkyl, or heteroaryl alkyl.

公开(公告)号：US11602531B2

公开(公告)日：2023-03-14

申请号：US17075065

申请日：2020-10-20

Applicant: The University of Toledo

Inventor： William A. Maltese ,  Zehui Li ,  Christopher J. Trabbic ,  Paul W. Erhardt

IPC: A61K31/4439 ,  C12N5/00 ,  C12N1/38 ,  A61K31/53 ,  A61K31/5377

Abstract: Vacuole- or exosome-inducing indole-based chalcone and substituted triazole-hydrazone compounds that induce endosomal vacuolization and increase exosome yield, but do not trigger growth arrest or cell death, and methods of making and using are described.

公开(公告)号：US10776461B2

公开(公告)日：2020-09-15

申请号：US16246614

申请日：2019-01-14

Applicant: The University of Toledo

Inventor： Bruce E. Heck ,  Dong Hyun Kim ,  Paul W. Erhardt ,  Brian J. Kress

IPC: C07D277/20 ,  C07D277/22 ,  C07D277/28 ,  G06F21/31 ,  H04W12/06 ,  A61K45/06 ,  A61K31/426 ,  A61K31/5575 ,  C07D277/30 ,  C07D277/24 ,  H04W12/04 ,  H04W12/08

Abstract: Peroxisome proliferator activated receptor (PPAR) compounds, and methods of using the same for treating bone fractures, treating osteoporosis and/or metabolic bone diseases, and inducing osteogenesis and/or chondrogenesis, are disclosed.