公开(公告)号：US20140088052A1

公开(公告)日：2014-03-27

申请号：US14000816

申请日：2012-02-27

申请人： Shyam Biswal ,  Rajesh Thimmulappa ,  Sarvesh Kumar ,  Sanjay V. Malhotra ,  Vineet Kumar ,  Kim Jung-Hyun

发明人： Shyam Biswal ,  Rajesh Thimmulappa ,  Sarvesh Kumar ,  Sanjay V. Malhotra ,  Vineet Kumar ,  Kim Jung-Hyun

IPC分类号： A61K31/121 ,  A61K45/06 ,  C07C49/84

CPC分类号： A61K31/121 ,  A61K45/06 ,  C07C49/813 ,  C07C49/84 ,  C07C205/45

摘要： Compounds and methods for treating or preventing a disease, disorder or condition associated with an Nrf2-regulated pathway, including those associated with an autoimmune disease, comorbidity associated with diabetes, such as retinopathy and nephropathy, bone marrow transplant for leukemia and related cancers, bone marrow deficiencies, inborn errors of metabolism, and other immune disorders, oxidative stress, respiratory infection, ischemia, neurodegenerative disorders, radiation injury, neutropenia caused by chemotherapy, autoimmunity, and congenital neutropenic disorders, and for restoring a corticosteroid responsiveness, in a subject are provided.

摘要翻译： 用于治疗或预防与Nrf2调节途径相关的疾病，病症或病症的化合物和方法，包括与自身免疫性疾病相关的疾病，与糖尿病相关的共病，例如视网膜病变和肾病，白血病骨髓移植和相关癌症，骨骼 受试者骨髓缺陷，代谢紊乱，其他免疫疾病，氧化应激，呼吸道感染，局部缺血，神经退行性疾病，放射性损伤，化疗引起的中性粒细胞减少，自身免疫和先天性中性粒细胞减少症，以及恢复皮质类固醇反应等） 提供。

公开(公告)号：US10071945B2

公开(公告)日：2018-09-11

申请号：US14126178

申请日：2012-06-15

申请人： Jane B. Neckers ,  Yeong Sang Kim ,  Sunmin Lee ,  Vineet Kumar ,  Sanjay V. Malhotra

发明人： Jane B. Neckers ,  Yeong Sang Kim ,  Sunmin Lee ,  Vineet Kumar ,  Sanjay V. Malhotra

IPC分类号： A61K31/12 ,  A61K31/275 ,  A61K45/06 ,  C07C49/796 ,  C07C255/56 ,  C07C205/45 ,  C07C49/80 ,  C07C49/813 ,  C07C49/84

CPC分类号： C07C49/796 ,  A61K31/12 ,  A61K31/275 ,  A61K45/06 ,  C07C49/80 ,  C07C49/813 ,  C07C49/84 ,  C07C205/45 ,  C07C255/56 ,  A61K2300/00

摘要： Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein R1 to R5 and X1 to X5 are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed.

公开(公告)号：US20140171503A1

公开(公告)日：2014-06-19

申请号：US14126178

申请日：2012-06-15

申请人： Jane B. Neckers ,  Yeong Sang Kim ,  Sunmin Lee ,  Vineet Kumar ,  Sanjay V. Malhotra

发明人： Jane B. Neckers ,  Yeong Sang Kim ,  Sunmin Lee ,  Vineet Kumar ,  Sanjay V. Malhotra

IPC分类号： C07C49/796 ,  C07C49/813 ,  C07C255/56 ,  C07C205/45 ,  C07C49/84

CPC分类号： C07C49/796 ,  A61K31/12 ,  A61K31/275 ,  A61K45/06 ,  C07C49/80 ,  C07C49/813 ,  C07C49/84 ,  C07C205/45 ,  C07C255/56 ,  A61K2300/00

摘要： Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein R1 to R5 and X1 to X5 are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed.

摘要翻译： 公开的是可以作为雄激素受体的拮抗剂的核受体调节剂的化合物，例如式I的化合物：其中R 1至R 5和X 1至X 5如本文所述，以及其药学上可接受的盐，溶剂合物和 其立体异构体。 还公开了包含这些化合物的药物组合物，以及使用方法和治疗癌症，包括前列腺癌，其他核受体介导的癌症和其他病症。