公开(公告)号：US09642835B2

公开(公告)日：2017-05-09

申请号：US13867658

申请日：2013-04-22

Applicant: STC.UNM ,  University of Kansas

Inventor： Angela Wandinger-Ness ,  Larry Sklar ,  Zurab Surviladze ,  Tudor Oprea ,  Laurie Hudson ,  Jeffrey Aube ,  Jennifer E. Golden ,  Chad E. Schroeder ,  Denise S. Simpson ,  Julica J. Noth

IPC: A61K31/415 ,  A61K45/06 ,  C07D231/06 ,  A61K31/403 ,  A61K31/407

CPC classification number: A61K31/407 ,  A61K31/403 ,  A61K31/415 ,  A61K45/06 ,  C07D231/06 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158 ,  G01N33/573 ,  Y02A50/473 ,  Y02A50/486 ,  A61K2300/00

Abstract: The present invention relates to molecules which function as selective modulators (i.e., inhibitors and agonists, preferably inhibitors) of the Ras-homologous (Rho) family of small GTPases, in particular, Cdc42 GTPase and their use to treat diseases, for example cancers, including metastatic cancer, where Cdc42 GTPase is overexpressed or hyperactivated, genetic and acquired diseases where activation of Cdc42 GTPase plays a pivotal role (e.g., neurodegenerative diseases), rheumatoid arthritis, atherosclerosis, diabetes type I, autosomal polycystic kidney diease, cystic kidney disease, precystic kidney disease and microbial infections. Additionally, compounds according to the present invention may be used to inhibit rejection (graft host response) in transplant patients (pursuant to transplantation), to promote immunosuppression, anti-inflammatory response and to mobilize stem cell (migration) in patients in need, among others.

公开(公告)号：US11219625B2

公开(公告)日：2022-01-11

申请号：US15746043

申请日：2016-07-22

Applicant: YALE UNIVERSITY ,  THE UNIVERSITY OF KANSAS

Inventor： Joseph N. Contessa ,  Jennifer E. Golden ,  Daniel P. Flaherty

IPC: A61K31/5377 ,  A61K31/402 ,  A61K31/426 ,  A61K31/427 ,  A61K31/454 ,  C07D295/192 ,  C07D213/75 ,  A61P35/00 ,  A61K45/06 ,  C07D277/46 ,  C07D277/82 ,  C07D295/155 ,  C07D417/12

Abstract: The present invention includes novel compounds and methods for preventing or treating diseases associated with N-linked glycosylation in a subject in need thereof. The methods comprise administering to the subject an effective amount of at least one compound of the invention.

公开(公告)号：US20150119411A1

公开(公告)日：2015-04-30

申请号：US14405772

申请日：2013-06-05

Applicant: University of Kansas ,  Southern Research Institute

Inventor： Jennifer E. Golden ,  Jeffrey Aube ,  Denise S. Simpson ,  Daniel P. Flaherty ,  Daljit S. Matharu ,  William E. Severson ,  Lynn Rasmussen

IPC: C07D239/96 ,  C12N7/00 ,  C07D405/12

CPC classification number: C07D239/96 ,  A61K31/517 ,  C07D405/12 ,  C12N7/00 ,  C12N2760/18563

Abstract: Described herein are compounds, pharmaceutical compositions and methods for treating a respiratory syncytial virus infection in a subject, or for inhibiting replication of respiratory syncytial virus.

Abstract translation: 本文描述了用于治疗受试者中呼吸道合胞病毒感染或抑制呼吸道合胞病毒复制的化合物，药物组合物和方法。

公开(公告)号：US10787439B2

公开(公告)日：2020-09-29

申请号：US15672574

申请日：2017-08-09

Applicant: University of Kansas ,  The Regents of the University of Michigan ,  Wayne State University ,  Sanford-Burnham Medical Research Institute

Inventor： Jennifer E. Golden ,  Jeffrey Aube ,  Daniel P. Flaherty ,  Andrew M. Fribley ,  Randal J. Kaufman ,  Thomas D. Y. Chung ,  Anthony B. Pinkerton ,  Michael Pablo Hedrick

IPC: A61K31/4525 ,  C07D405/12 ,  C07D307/71 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07C303/36

Abstract: N-substituted sulfonylphenyl-5-nitrofuranyl-2-carboxamide derived compounds, which selectively activate the apoptotic, but not the adaptive arm, of the Unfolded Protein Response are provides as is their use in the treatment of diseases such as diabetes, Alzheimer's, Parkinson's, hemophilia, lysosomal storage diseases and cancer.

公开(公告)号：US09499496B2

公开(公告)日：2016-11-22

申请号：US14405772

申请日：2013-06-05

Applicant: University of Kansas ,  Southern Research Institute

Inventor： Jennifer E. Golden ,  Jeffrey Aube ,  Denise S. Simpson ,  Daniel P. Flaherty ,  Daljit S. Matharu ,  William E. Severson ,  Lynn Rasmussen

IPC: C07D239/96 ,  C07D405/12 ,  C12N7/00 ,  A61K31/517

CPC classification number: C07D239/96 ,  A61K31/517 ,  C07D405/12 ,  C12N7/00 ,  C12N2760/18563

Abstract: Described herein are compounds, pharmaceutical compositions and methods for treating a respiratory syncytial virus infection in a subject, or for inhibiting replication of respiratory syncytial virus.

Abstract translation: 本文描述了用于治疗受试者中呼吸道合胞病毒感染或抑制呼吸道合胞病毒复制的化合物，药物组合物和方法。

公开(公告)号：US20150203477A1

公开(公告)日：2015-07-23

申请号：US14408736

申请日：2013-06-18

Applicant: University of Kansas ,  The Regents of the University of Michigan ,  Wayne State University ,  Sanford-Burnham Medical Research Institute

Inventor： Jennifer E. Golden ,  Jeffrey Aube ,  Daniel P. Flaherty ,  Andrew M. Fribley ,  Randal J. Kaufman ,  Thomas D.Y. Chung ,  Anthony B. Pinkerton ,  Michael Pablo Hedrick

IPC: C07D405/12 ,  C07C303/36 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/496 ,  C07D307/71 ,  A61K31/4525

CPC classification number: C07D405/12 ,  A61K31/4525 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07C303/36 ,  C07D307/71

Abstract: N-substituted sulfonylphenyl-5-nitrofuranyl-2-carboxamide derived compounds, which selectively activate the apoptotic, but not the adaptive arm, of the Unfolded Protein Response are provides as is their use in the treatment of diseases such as diabetes, Alzheimer's, Parkinson's, hemophilia, lysosomal storage diseases and cancer.

Abstract translation: N-取代的磺酰基苯基-5-硝基呋喃-2-甲酰胺衍生化合物，其选择性地激活未折叠蛋白质反应的凋亡但不适应臂，其用途可用于治疗疾病如糖尿病，阿尔茨海默氏症，帕金森病 ，血友病，溶酶体贮积病和癌症。

公开(公告)号：US20180086749A1

公开(公告)日：2018-03-29

申请号：US15573240

申请日：2016-05-10

Applicant: University of Kansas ,  University of Louisville Research Foundation, Inc.

Inventor： Jennifer E. Golden ,  Donghoon Chung

IPC: C07D417/12 ,  C07D417/04 ,  C07D277/82

CPC classification number: C07D417/12 ,  C07D277/82 ,  C07D417/04

Abstract: The present technology is directed to compounds, compositions, and methods to treat a viral infection. The compound is according to Formula I or a solvate and/or pharmaceutically acceptable salt thereof. The technology is especially suited to treat Chikungunya virus, Zika virus, Venezuelan equine encephalitis virus, and/or respiratory syncytial virus infection.

公开(公告)号：US20170334889A1

公开(公告)日：2017-11-23

申请号：US15672574

申请日：2017-08-09

Applicant: University of Kansas ,  The Regents of the University of Michigan ,  Wayne State University ,  Sanford-Burnham Medical Research Institute

Inventor： Jennifer E. Golden ,  Jeffrey Aube ,  Daniel P. Flaherty ,  Andrew M. Fribley ,  Randal J. Kaufman ,  Thomas D.Y. Chung ,  Anthony B. Pinkerton ,  Michael Pablo Hedrick

IPC: C07D405/12 ,  C07C303/36 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/496 ,  C07D307/71 ,  A61K31/4525

Abstract: N-substituted sulfonylphenyl-5-nitrofuranyl-2-carboxamide derived compounds, which selectively activate the apoptotic, but not the adaptive arm, of the Unfolded Protein Response are provides as is their use in the treatment of diseases such as diabetes, Alzheimer's, Parkinson's, hemophilia, lysosomal storage diseases and cancer.

公开(公告)号：US09732067B2

公开(公告)日：2017-08-15

申请号：US14408736

申请日：2013-06-18

Applicant: University of Kansas ,  The Regents of the University of Michigan ,  Wayne State University ,  Sanford-Burnham Medical Research Institute

Inventor： Jennifer E. Golden ,  Jeffrey Aube ,  Daniel P. Flaherty ,  Andrew M. Fribley ,  Randal J. Kaufman ,  Thomas D. Y. Chung ,  Anthony B. Pinkerton ,  Michael Pablo Hedrick

IPC: C07D405/12 ,  C07C303/36 ,  A61K31/4525 ,  C07D307/71 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06

CPC classification number: C07D405/12 ,  A61K31/4525 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07C303/36 ,  C07D307/71

Abstract: N-substituted sulfonylphenyl-5-mitrofuranyl-2-carboxamide derived compounds, which selectively activate the apoptotic, but not the adaptive arm, of the Unfolded Protein Response are provided as is their use in the treatment of diseases such as diabetes, Alzheimer's, Parkinson's, hemophilia, lysosomal storage diseases and cancer.

公开(公告)号：US20130345277A1

公开(公告)日：2013-12-26

申请号：US13867658

申请日：2013-04-22

Applicant: STC.UNM ,  Kansas University Center for Technology Commercialization, Inc.

Inventor： Angela Wandinger-Ness ,  Larry Sklar ,  Zurab Surviladze ,  Tudor Oprea ,  Laurie Hudson ,  Jeffrey Aube ,  Jennifer E. Golden ,  Chad E. Schroeder ,  Denise S. Simpson ,  Julica J. Noth

IPC: A61K31/415 ,  A61K45/06 ,  C07D231/06

CPC classification number: A61K31/407 ,  A61K31/403 ,  A61K31/415 ,  A61K45/06 ,  C07D231/06 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158 ,  G01N33/573 ,  Y02A50/473 ,  Y02A50/486 ,  A61K2300/00

Abstract: The present invention relates to molecules which function as selective modulators of the Ras-homologous (Rho) family of small GTPases, in particular, Cdc42 GTPase and their use to treat diseases, for example cancers, including metastatic cancer, genetic and acquired diseases where activation of Cdc42 GTPase plays a pivotal role, such as neurodegenerative diseases, rheumatoid arthritis, atherosclerosis, diabetes type I, autosomal polycystic kidney disease, cystic kidney disease, precystic kidney disease, microbial infections, including Chlamydia infections, E. coli infections, H. pylori infections and its secondary effects including gastric ulcers, Coxiella Brunetti (Q-fever) infections and Streptococcus pneumonia infections, fungal infections including Paracoccidiodes brasiliensis and Candida albicans and their secondary effects including lung edema. Additionally, compounds according to the present invention may be used to inhibit rejection in transplant patients (pursuant to transplantation), to promote immunosuppression, anti-inflammatory response and to mobilize stem cell (migration) in patients in need, among others.

Abstract translation: 本发明涉及用作小GTP酶的Ras同源（Rho）家族，特别是Cdc42GTP酶的选择性调节剂的分子及其用于治疗疾病的用途，例如癌症，包括转移性癌症，遗传和获得性疾病，其中激活 的Cdc42 GTPase起着关键的作用，如神经退行性疾病，类风湿关节炎，动脉粥样硬化，I型糖尿病，常染色体多囊肾病，囊性肾病，前期肾脏疾病，微生物感染，包括衣原体感染，大肠杆菌感染，幽门螺杆菌 感染及其次要作用包括胃溃疡，布氏梭菌（Qex fever）感染和肺炎链球菌感染，包括巴西隐孢子虫和白色念珠菌在内的真菌感染及其副作用，包括肺水肿。 此外，根据本发明的化合物可以用于抑制移植患者的排斥（根据移植），以促进免疫抑制，抗炎反应和在需要的患者中调动干细胞（迁移）等。