发明名称 Aryl-phenyl-sulfonamido-cycloalkyl compounds and their use
摘要 The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc.;
申请公布号 US9616037(B2) 申请公布日期 2017.04.11
申请号 US201615075356 申请日期 2016.03.21
申请人 PIMCO 2664 Limited 发明人 Greig Iain Robert;Sheridan Rose Mary;Fisher Raymond;Tozer Matthew John;Clase Juha Andrew;Smith Andrew;Tuffnell Andrew Robert;Van't Hof Robert Jurgen
分类号 A61K31/18;A61K31/505;A61K31/44;C07C311/20;C07C311/28;C07D213/52;C07D213/61;C07D239/26;C07D239/30;C07D295/135;C07D207/04;A61K31/4418;C07C311/29;C07D213/34 主分类号 A61K31/18
代理机构 Swanson & Bratschun, L.L.C. 代理人 Swanson & Bratschun, L.L.C.
主权项 1. A method of treatment of rheumatoid arthritis in a patient in need of said treatment comprising administering to said patient a therapeutically effective amount of a compound selected from compounds of the following formula, and pharmaceutically acceptable salts thereof: wherein: either: ═W— is —CH═ and —Y═ is —CH═;or: ═W— is —CH═ and —Y═ is —N═;—RX2 is —RX2S;—RX4 is —RX4S;—RX2S is —RX;—RX4S is —RX;each —RX is independently —F, —Cl, —Br, —I, —RXX, —OH, —ORXX, —SRXX, —CF3, —OCF3, —CN, or —NO2;each —RXX is independently saturated aliphatic C1-4alkyl;—RXC1 is independently —H or —RXCC;—RXC2 is independently —H;—RXCC is independently —F, —Cl, or —RXCCC;—RXCCC is independently-Me or -Et;—RSN is —H;-DQ is -D1-Q1;either: -D1 is cyclohexane-1,4-di-yl;or: -D1- is 4-methyl-cyclohexane-1,4-di-yl; and-Q1 is —OH.
地址 London GB