INTERCELLULAR CALCIUM MODULATING COMPOUND

• Main Authors: WANG ZHIJUN, BRIAN DYCK, JEFFREY P WHITTEN, CAO JIANGUO, JONATHAN GREY, EVAN ROGERS, PEI YAZHONG
• Format: Patent
• Language: English; Japanese
• Published: 14.01.2016
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PROBLEM TO BE SOLVED: To provide a compound that modulates the activity of a store-operated calcium (SOC) channel, and a pharmaceutical composition containing the compound.SOLUTION: Provided is a pyrazole derivative, for example, represented by the formula 10, in which the substituents at 1,3-position are each independently H or a particular substituent, and the substituent at 5-position is a phenyl group substituted with a particular substituent. The compound is effective in the treatment of inflammation-related disease, glomerulonephritis, uveitis, liver disease, renal disease, chronic obstructive pulmonary disease, rheumatoid arthritis, inflammatory bowel disease, vasculitis, dermatitis, osteoarthritis, inflammatory muscular diseases, allergic rhinitis, vaginitis, interstitial cystitis, scleroderma, osteoporosis, eczema, organ transplant rejection, allograft or xenograft, graft rejection, graft-versus-host disease, erythematous and the like in a mammal. 【課題】ストア作動性カルシウム（ＳＯＣ）チャネルの活性を調節する化合物及び該化合物を含む医薬組成物の提供。【解決手段】例えば式１０で示される様なピラゾール誘導体であり、１，３位の置換基が、各々独立にＨ又は特定の置換基であり、５位の置換基が、特定の置換基で置換されたフェニル基であるピラゾール誘導体。【効果】該化合物は哺乳動物における炎症に関係する疾患、糸球体腎炎、ブドウ膜炎、肝臓の疾患、腎臓の疾患慢性閉塞性肺疾患、関節リウマチ、炎症性腸疾患、血管炎、皮膚炎、変形性関節症、炎症性の筋肉疾患、アレルギー性鼻炎、膣炎、間質性膀胱炎、強皮症、骨粗鬆症、湿疹、移植臓器拒絶、同種移植または異種移植、移植片拒絶、移植片対宿主病、紅斑性等の処置に有効である。【選択図】図１