公开(公告)号：US09642835B2

公开(公告)日：2017-05-09

申请号：US13867658

申请日：2013-04-22

申请人： STC.UNM ,  University of Kansas

发明人： 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分类号： A61K31/415 ,  A61K45/06 ,  C07D231/06 ,  A61K31/403 ,  A61K31/407

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

摘要： 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：US20130345277A1

公开(公告)日：2013-12-26

申请号：US13867658

申请日：2013-04-22

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

发明人： 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分类号： A61K31/415 ,  A61K45/06 ,  C07D231/06

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

摘要： 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.

摘要翻译： 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。