公开(公告)号：EP3448838A2

公开(公告)日：2019-03-06

申请号：EP17790411.7

申请日：2017-04-27

申请人： Samumed, LLC

发明人： KC, Sunil Kumar ,  MITTAPALLI, Gopi Kumar ,  HOFILENA, Brian Joseph ,  MARAKOVITS, Joseph Timothy ,  CHIRUTA, Chandramouli ,  MAK, Chi Ching ,  CAO, Jianguo

IPC分类号： C07D217/22 ,  A61K31/472 ,  A61K31/4725 ,  C07D217/12

公开(公告)号：EP3284744A1

公开(公告)日：2018-02-21

申请号：EP17169783.2

申请日：2013-03-13

申请人： Samumed, LLC

发明人： HOOD, John ,  WALLACE, David, Mark ,  KC, Sunil, Kumar

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/496 ,  A61K31/5377 ,  A61P35/00 ,  A61P31/10 ,  A61P31/12 ,  A61P19/00 ,  A61P25/28

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状的吲唑化合物。 更具体地说，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，血管生成，阿尔茨海默氏病，肺病和骨关节炎）为特征的病症中的用途， Wnt通路信号传导介导的细胞事件的调节，以及由Wnt通路和/或Wnt信号传导组分中的一个或多个的突变或失调引起的遗传疾病和神经病症/障碍/疾病。 还提供了治疗Wnt相关疾病状态的方法。

公开(公告)号：EP2760285B1

公开(公告)日：2017-06-21

申请号：EP13772420.9

申请日：2013-03-13

申请人： Samumed, LLC

发明人： HOOD, John ,  WALLACE, David, Mark ,  KC, Sunil, Kumar

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/496 ,  A61K31/5377 ,  A61P35/00 ,  A61P31/10 ,  A61P31/12 ,  A61P19/00 ,  A61P25/28

CPC分类号： C07D471/04 ,  C07B2200/13

公开(公告)号：EP2968249A1

公开(公告)日：2016-01-20

申请号：EP14753569.4

申请日：2014-02-21

申请人： Samumed, LLC

发明人： KUMAR KC, Sunil ,  WALLACE, David Mark ,  HOOD, John ,  BARROGA, Charlene

IPC分类号： A61K31/33

CPC分类号： C07D411/06 ,  C07D213/50 ,  C07D231/56 ,  C07D235/06 ,  C07D263/56 ,  C07D307/80 ,  C07D311/58 ,  C07D317/46 ,  C07D317/54 ,  C07D319/16 ,  C07D319/18 ,  C07D327/06 ,  C07D333/54 ,  C07D339/08 ,  C07D401/06 ,  C07D405/06 ,  C07D407/06 ,  C07D409/06 ,  C07D413/06

摘要： The present disclosure provides γ-diketones 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 or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

公开(公告)号：EP3305073A1

公开(公告)日：2018-04-11

申请号：EP17187452.2

申请日：2010-12-15

申请人： Samumed, LLC

发明人： HOOD, John ,  KC, Sunil Kumar ,  WALLACE, David Mark

IPC分类号： A01N43/52 ,  A01N43/56 ,  A61K31/415 ,  C07D471/04 ,  C07D471/14 ,  A61P35/00 ,  A61P25/28 ,  A61P19/02 ,  A61P19/08 ,  A61P31/10 ,  A61P31/12 ,  A61P17/06 ,  A61P27/06

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： 本文提供了式I化合物及其药学上可接受的盐和包含其的组合物，用于各种方法，包括治疗诸如结肠癌，卵巢癌，胰腺癌，乳腺癌，肝癌，前列腺癌和血液学癌症的癌症：

公开(公告)号：EP3119393A4

公开(公告)日：2018-02-28

申请号：EP15765201

申请日：2015-03-20

申请人： SAMUMED LLC

发明人： HOOD JOHN ,  KC SUNIL KUMAR ,  WALLACE DAVID MARK ,  MITTAPALLI GOPI KUMAR ,  HOFILENA BRIAN JOSEPH ,  MAK CHI CHING ,  BOLLU VENKATAIAH ,  EASTMAN BRIAN

IPC分类号： A61K31/416 ,  A61P19/00 ,  A61P35/00 ,  C07D401/14

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.

公开(公告)号：EP3001903A1

公开(公告)日：2016-04-06

申请号：EP15174246.7

申请日：2010-12-15

申请人： Samumed, LLC

发明人： HOOD, John ,  KC, Sunil Kumar ,  WALLACE, David Mark

IPC分类号： A01N43/52 ,  A01N43/56 ,  A61K31/415 ,  C07D471/04 ,  C07D471/14 ,  A61P35/00 ,  A61P25/28 ,  A61P19/02 ,  A61P19/08 ,  A61P31/10 ,  A61P31/12 ,  A61P17/06 ,  A61P27/06

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，肝癌，前列腺癌和血液癌：

公开(公告)号：EP2760285A1

公开(公告)日：2014-08-06

申请号：EP13772420.9

申请日：2013-03-13

申请人： Samumed, LLC

发明人： HOOD, John ,  WALLACE, David, Mark ,  KC, Sunil, Kumar

IPC分类号： A01N43/54

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. One embodiment disclosed herein includes a compound having the structure of Formula I:

公开(公告)号：EP2755483A1

公开(公告)日：2014-07-23

申请号：EP12830938.2

申请日：2012-09-13

申请人： Samumed, LLC

发明人： HOOD, John ,  KC, Sunil Kumar

IPC分类号： A01N43/56 ,  A61K31/415

CPC分类号： C07D401/14 ,  A61K31/416 ,  A61K45/06 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D405/14 ,  C07D413/12

摘要： Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis 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：EP2605652A1

公开(公告)日：2013-06-26

申请号：EP11818727.7

申请日：2011-08-17

申请人： Samumed, LLC

发明人： KC, Sunil, Kumar ,  WALLACE, David, Mark ,  HOOD, John ,  BARROGA, Charlene, F.

IPC分类号： A01N35/00 ,  A61K31/12

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 ²-diketones, ³-diketones or ³-hydroxyketones or analogs thereof, that activate Wnt/²-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.