公开(公告)号：US20160068547A1

公开(公告)日：2016-03-10

申请号：US14847287

申请日：2015-09-08

申请人： Samumed, LLC

发明人： Sunil Kumar KC ,  David Mark Wallace ,  Jianguo Cao ,  Chandramouli Chiruta ,  John Hood

IPC分类号： C07D519/00

CPC分类号： A61K31/416 ,  A61K31/4188 ,  C07D519/00

摘要： Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

摘要翻译： 公开了用于治疗各种疾病和病症的阿扎丁唑化合物。 更具体地说，本发明涉及氮杂咔唑化合物或其类似物在治疗特征在于激活Wnt途径信号传导（例如癌症，异常细胞增殖，血管发生，纤维化病症，骨或软骨疾病和 骨关节炎），由Wnt途径信号传导介导的细胞事件的调节，以及由于Wnt途径的突变或失调引起的遗传疾病和神经病症/疾病/疾病和/或Wnt信号成分中的一种或多种。 还提供了治疗Wnt相关疾病状态的方法。

公开(公告)号：US20160068529A1

公开(公告)日：2016-03-10

申请号：US14847299

申请日：2015-09-08

申请人： Samumed, LLC

发明人： Sunil Kumar KC ,  David Mark Wallace ,  Jianguo Cao ,  Chandramouli Chiruta ,  John Hood

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

摘要翻译： 公开了用于治疗各种疾病和病症的阿扎丁唑化合物。 更具体地说，本发明涉及氮杂咔唑化合物或其类似物在治疗特征在于激活Wnt途径信号传导（例如癌症，异常细胞增殖，血管发生，纤维化病症，骨或软骨疾病和 骨关节炎），由Wnt途径信号传导介导的细胞事件的调节，以及由于Wnt途径的突变或失调引起的遗传疾病和神经病症/疾病/疾病和/或Wnt信号成分中的一种或多种。 还提供了治疗Wnt相关疾病状态的方法。

公开(公告)号：US20150266825A1

公开(公告)日：2015-09-24

申请号：US14664517

申请日：2015-03-20

申请人： Samumed, LLC

发明人： John Hood ,  Sunil Kumar KC ,  David Mark Wallace ,  Gopi Kumar Mittapalli ,  Brian Joseph Hofilena ,  Chi Ching Mak ,  Venkataiah Bollu ,  Brian Eastman

IPC分类号： C07D231/56 ,  C07D405/14 ,  C07D498/08 ,  C07D405/12 ,  C07D401/12 ,  C07D401/14 ,  C07D401/04

CPC分类号： C07D231/56 ,  C07B59/002 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D498/08

摘要： Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, fibrotic disorders, cartilage (chondral) defects, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, and neurological conditions/disorders/diseases linked to overexpression of DYRK1A.

摘要翻译： 公开了用于治疗各种疾病和病症的吲唑化合物。 更具体地，本公开涉及吲哚化合物或其类似物在治疗以Wnt途径信号传导（例如癌症，异常细胞增殖，血管发生，阿尔茨海默病，肺病，纤维化病症， 软骨（软骨）缺陷和骨关节炎），由Wnt通路信号传导介导的细胞事件的调节，以及与DYRK1A的过度表达有关的神经病症/病症/疾病。

公开(公告)号：US08921413B2

公开(公告)日：2014-12-30

申请号：US14086529

申请日：2013-11-21

申请人： Samumed, LLC

发明人： Sunil Kumar KC ,  David Mark Wallace ,  John Hood ,  Charlene F. Barroga

IPC分类号： C07D319/18 ,  A61K31/357 ,  C07C49/784 ,  C07D213/50 ,  C07D405/06 ,  C07D405/10 ,  C07D407/10 ,  C07D409/06 ,  C07D409/10

CPC分类号： A61K31/4436 ,  A61K9/0014 ,  A61K31/12 ,  A61K31/357 ,  A61K31/381 ,  A61K31/4402 ,  A61K31/4433 ,  C07C49/784 ,  C07D213/50 ,  C07D319/16 ,  C07D319/18 ,  C07D405/06 ,  C07D405/10 ,  C07D407/10 ,  C07D409/06 ,  C07D409/10

摘要： The present invention discloses β-diketones, γ-diketones or γ-hydroxyketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

摘要翻译： 本发明公开了用于激活Wnt / / b-c-catenin信号传导的β-二酮，γ-二酮或γ-羟基酮或其类似物，从而治疗或预防与信号转导相关的疾病，如骨质疏松症和骨关节病; 成骨不全，骨缺损，骨折，牙周病，耳硬化症，伤口愈合，颅面缺损，溶瘤性骨病，与中枢神经系统分化和发育相关的创伤性脑损伤，包括帕金森病，中风，缺血性脑病，癫痫 ，阿尔茨海默病，抑郁症，双相性精神障碍，精神分裂症; 眼睛疾病如年龄相关性黄斑变性，糖尿病性黄斑水肿或视网膜色素变性以及与干细胞分化和生长相关的疾病，包括脱发，造血相关疾病和组织再生相关疾病。

公开(公告)号：US08901150B2

公开(公告)日：2014-12-02

申请号：US14331427

申请日：2014-07-15

申请人： Samumed, LLC

发明人： John Hood ,  Sunil Kumar KC ,  David Mark Wallace

IPC分类号： C07D401/14 ,  A61K31/437

CPC分类号： A61K31/5377 ,  A61K31/415 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  C07D401/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D519/00

摘要： Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:

摘要翻译： 本文提供了根据式I的化合物及其药学上可接受的盐，以及包含其的组合物，用于各种方法，包括治疗癌症如结肠癌，卵巢癌，胰腺癌，乳腺癌，肝癌，前列腺癌和血液癌：

公开(公告)号：US08815897B2

公开(公告)日：2014-08-26

申请号：US13855874

申请日：2013-04-03

申请人： Samumed, LLC

发明人： John Hood ,  Sunil Kumar K C ,  David Mark Wallace

IPC分类号： A61K31/435

CPC分类号： A61K31/5377 ,  A61K31/415 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  C07D401/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D519/00

摘要： Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:

公开(公告)号：US20140005170A1

公开(公告)日：2014-01-02

申请号：US14019940

申请日：2013-09-06

申请人： Samumed, LLC

发明人： John Hood ,  David Mark Wallace ,  Sunil Kumar KC

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  C07B2200/13

摘要： Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

摘要翻译： 公开了用于治疗各种疾病和病症的吲唑化合物。 更具体地，本发明涉及吲唑化合物或其类似物在治疗以Wnt途径信号传导（例如癌症，异常细胞增殖，血管发生，阿尔茨海默病，肺部疾病和骨关节炎）的活化为特征的疾病中的用途， 由Wnt途径信号传导介导的细胞事件的调节，以及由于Wnt途径的突变或失调和/或一种或多种Wnt信号成分导致的遗传疾病和神经病症/疾病/疾病。 还提供了治疗Wnt相关疾病状态的方法。

公开(公告)号：US20130267495A1

公开(公告)日：2013-10-10

申请号：US13800963

申请日：2013-03-13

申请人： SAMUMED, LLC

发明人： John Hood ,  David Mark Wallace ,  Sunil Kumar KC

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  C07B2200/13

摘要： Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

公开(公告)号：US20130225576A1

公开(公告)日：2013-08-29

申请号：US13855874

申请日：2013-04-03

申请人： Samumed, LLC

发明人： John Hood ,  Sunil Kumar KC ,  David Mark Wallace

IPC分类号： C07D471/04

CPC分类号： A61K31/5377 ,  A61K31/415 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  C07D401/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D519/00

摘要： Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:

公开(公告)号：US10899757B2

公开(公告)日：2021-01-26

申请号：US15773737

申请日：2016-11-07

申请人： Samumed, LLC

发明人： John Hood ,  David Mark Wallace ,  Sunil Kumar KC ,  Yusuf Yazici ,  Christopher Swearingen ,  Luis A Dellamary

IPC分类号： C07D471/04 ,  A61K31/444 ,  A61P19/02 ,  A61P29/00 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K9/00

摘要： Indazole compounds for treating various diseases and pathologies are provided. More particularly, the use of an indazole compound or analogs thereof, in the treatment of inflammatory diseases or disorders is provided.