公开(公告)号：US20240279231A1

公开(公告)日：2024-08-22

申请号：US18562343

申请日：2022-05-20

申请人： The Board of Regents of the University of Oklahoma

发明人： Vibhudutta Awasthi ,  Venkateswararao Eeda

IPC分类号： C07D487/04 ,  C07F9/6561 ,  C07H19/14

CPC分类号： C07D487/04 ,  C07F9/6561 ,  C07H19/14

摘要： The compound DMX-5804, IUPAC name 5-(4-(2-methoxyethoxy)phenyl)-7-phenyl-3,4a,7,7a-tetrahydro-4H-pyrrolo[2,3-d]pyrimidin-4-one, is a potent and selective inhibitor of mitogen-activated protein kinase kinase kinase kinase-4 (MAP4K4). The present disclosure describes a scalable and practical synthesis process for making DMX-5804. The process (1) doesn't rely on transition metals, (2) has reduced duration of reactions, (3) is streamlined with significantly improved yields using low cost raw materials, (4) includes no microwave-assisted reactions, (5) does not require column purification, and (6) generally results in crystalized products having over a 95% purity in each step. The present disclosure also describes DMX-5804 analogs and derivatives for use in inhibiting MAP4K4, and scalable and practical processes for making such DMX-5804 analogs.

公开(公告)号：US20240150286A1

公开(公告)日：2024-05-09

申请号：US18383708

申请日：2023-10-25

申请人： The Board of Regents of the University of Oklahoma

发明人： Venkateswararao Eeda ,  Weidong Wang ,  Dan Wu

IPC分类号： C07D209/18 ,  A61P1/16 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D209/18 ,  A61P1/16 ,  A61P3/04 ,  A61P3/10

摘要： Compounds and methods for treating insulin resistance, obesity, Type 2 diabetes, Nonalcoholic fatty liver disease (NAFLD), and peroxisome proliferator-activated receptor gamma (PPARy) serine 273 phosphorylation in subjects in need of such therapy.

公开(公告)号：US11999677B2

公开(公告)日：2024-06-04

申请号：US17666692

申请日：2022-02-08

申请人： The Board of Regents of the University of Oklahoma

发明人： Weidong Wang ,  Venkateswararao Eeda

IPC分类号： C07C233/73 ,  A61K31/166 ,  A61P3/10 ,  C07C237/22 ,  C07C311/46 ,  C07D213/40 ,  C07D231/56 ,  C07D317/54

CPC分类号： C07C233/73 ,  C07D317/54

摘要： Benzylamino-oxoethyl benzamide compounds for use in treating diseases and conditions associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic β-cell dysfunction and death, for example in the treatment of Type 1 and Type 2 diabetes. The compounds can also be used in treatments for chronic heart disease, neurodegenerative diseases, retinal degeneration, and other metabolic disorders associated with ER stress.

公开(公告)号：US20220162157A1

公开(公告)日：2022-05-26

申请号：US17666692

申请日：2022-02-08

申请人： The Board of Regents of the University of Oklahoma

发明人： Weidong Wang ,  Venkateswararao Eeda

IPC分类号： C07C233/73 ,  C07D317/54

摘要： Benzylamino-oxoethyl benzamide compounds for use in treating diseases and conditions associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic β-cell dysfunction and death, for example in the treatment of Type 1 and Type 2 diabetes. The compounds can also be used in treatments for chronic heart disease, neurodegenerative diseases, retinal degeneration, and other metabolic disorders associated with ER stress.

公开(公告)号：US20200071264A1

公开(公告)日：2020-03-05

申请号：US16559160

申请日：2019-09-03

申请人： The Board of Regents of the University of Oklahoma

发明人： Weidong Wang ,  Venkateswararao Eeda

IPC分类号： C07C233/73 ,  C07D317/54

摘要： Benzylamino-oxoethyl benzamide compounds for use in treating diseases and conditions associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic β-cell dysfunction and death, for example in the treatment of Type 1 and Type 2 diabetes. The compounds can also be used in treatments for chronic heart disease, neurodegenerative diseases, retinal degeneration, and other metabolic disorders associated with ER stress.