N-(4-hydroxy-4-methyl-cyclohexyl)-4-phenyl-benzenesulfonamides and N-(4-hydroxy-4-methyl-cyclohexyl)-4-(2-pyridyl)benzenesulfonamides and their therapeutic use
申请人:PIMCO 2664 LIMITED
公开号:US10029979B2
公开(公告)日:2018-07-24
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain substituted N-(4-hydroxy-4-methyl-cyclohexyl)-4-phenyl-benzenesulfonamide and N-(4-hydroxy-4-methyl-cyclohexyl)-4-(2-pyridyl)benzenesulfonamide compounds (collectively referred to herein as HMC compounds) that are useful, for example, in the treatment of disorders (e.g., diseases) including, inflammation and/or joint destruction and/or bone loss; disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; inflammatory and autoimmune disorders, for example, rheumatoid arthritis; psoriasis; psoriatic arthritis; chronic obstructive pulmonary disease (COPD); asthma; atherosclerosis; inflammatory bowel disease; ankylosing spondylitis; multiple sclerosis; systemic lupus erythematosus; Sjogren's syndrome; a disorder associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, or Paget's disease; cancer, such as a haematological malignancy, such as multiple myeloma, leukemia, or lymphoma, or a solid tumor cancer, such as bladder cancer, breast cancer (female and/or male), colon cancer, renal cell carcinoma, kidney cancer, lung cancer, pancreatic cancer, gastric cancer, prostate cancer, brain cancer, skin cancer, thyroid cancer, basal cell ameloblastoma, or melanoma; a disorder associated with fibrosis, such as systemic sclerosis or scleroderma; or a rare vasculitide, such as Behçet's disease. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, for example, in therapy.
本发明一般涉及治疗化合物领域。更具体地说,本发明涉及某些取代的 N-(4-羟基-4-甲基-环己基)-4-苯基苯磺酰胺和 N-(4-羟基-4-甲基-环己基)-4-(2-吡啶基)苯磺酰胺化合物(在此统称为 HMC 化合物),这些化合物可用于治疗各种疾病(例如疾病),包括炎症和/或关节破坏和/或骨质流失;免疫系统过度和/或不适当和/或长期激活引起的疾病;炎症和自身免疫性疾病,例如类风湿性关节炎;银屑病;银屑病关节炎;慢性阻塞性肺疾病(COPD);哮喘;动脉粥样硬化;炎症性肠病;强直性脊柱炎;多发性硬化症;系统性红斑狼疮;斯约格伦综合征;与骨质流失有关的疾病,如类风湿性关节炎、骨质疏松症、癌症相关骨病或帕吉特氏病中与破骨细胞过度活动有关的骨质流失;癌症,如血液恶性肿瘤,如多发性骨髓瘤、白血病或淋巴瘤,或实体瘤癌症,如膀胱癌、乳腺癌(女性和/或男性)、结肠癌、肾细胞癌、肾癌、肺癌、胰腺癌、胃癌、前列腺癌、脑癌、皮肤癌、甲状腺癌、基底细胞母细胞瘤或黑色素瘤;与纤维化相关的疾病,如系统性硬化症或硬皮病;或罕见的血管性疾病,如白塞氏病。本发明还涉及包含此类化合物的药物组合物,以及此类化合物和组合物在治疗等方面的用途。