首页> 外国专利> compound, pharmaceutical composition, and methods for inhibiting a soluble epoxide hydrolase, the progression of nephropathy, and the obstruction of obstructive pulmonary disease, an interstitial lung disease or asthma in a patient, to treat soluble epoxide hydrolase-modulated diseases, to reduce renal deterioration, blood pressure, vascular inflammation, renal inflammation in a patient, and the formation of a biologically active diol, to regulate endothelial cell function in a patient, to decrease endothelial cell inflammation in a patient, and to monitor the activity of a soluble epoxide hydrolase

compound, pharmaceutical composition, and methods for inhibiting a soluble epoxide hydrolase, the progression of nephropathy, and the obstruction of obstructive pulmonary disease, an interstitial lung disease or asthma in a patient, to treat soluble epoxide hydrolase-modulated diseases, to reduce renal deterioration, blood pressure, vascular inflammation, renal inflammation in a patient, and the formation of a biologically active diol, to regulate endothelial cell function in a patient, to decrease endothelial cell inflammation in a patient, and to monitor the activity of a soluble epoxide hydrolase

机译:化合物,药物组合物和用于抑制可溶性环氧化物水解酶,肾病的进展以及阻塞患者的阻塞性肺疾病,间质性肺病或哮喘的方法,以治疗可溶性环氧化物水解酶调节的疾病,以减少肾脏恶化,血压,血管炎症,患者的肾脏炎症以及生物活性二醇的形成,以调节患者的内皮细胞功能,减少患者的内皮细胞炎症,并监测可溶性环氧化物水解酶的活性

摘要

COMPOUND, PHARMACEUTICAL COMPOSITION, AND, METHODS FOR INHIBITING A SOLUBLE HYDROLASE EPÁXIDE, THE PROGRESSION OF NEPHROPATHY, AND THE PROGRESSION OF OBSTRUCTIVE PULMONARY DISEASE, AN INTERSTITIAL LUNG DISEASE IN A PATENTED, PHARMACEUTICAL, PHARMACEUTICAL, PHARMACEUTICAL, PHARMACEUTICAL, PHARMACEUTICAL KIDNEY DETERIORATION, BLOOD PRESSURE, VASCULAR INFLAMMATION, KIDNEY INFLAMMATION IN A PATIENT, AND THE FORMATION OF A BIOLOGICALLY ACTIVE DIOL, TO REGULATE ENDOTHELIAL CELL FUNCTION IN A PATIENT, INTO A LOT OF PEOPLE, IN LAMINATION MONITOR THE ACTIVITY OF A SOLUBLE HYDROLASE EPAXIDE. Compounds of formula (I) where R ^ 1 ^ is a selected member of the group consisting of C ~ 1 ~ -C ~ 8 ~ alkyl, C ~ 0 ~ -C ~ 8 ~ arylalkyl, C ~ 3 ~ -C cycloalkyl ~ 12 ~ and heterocyclyl, Y ^ 1 ^ is selected from the group consisting of a bond, C (R ^ 5 ^) ~ 2 ~, NR ^ 5 ^ and O; Y ^ 2 ^ is selected from the group consisting of a bond, NR ^ 5 ^ and O; each R ^ 2 ^, R ^ 3 ^ and R ^ 5 ^ is independently selected from the group consisting of H, alkyl and COR ^ 6 ^; A is heterocyclyl, optionally substituted with 1 to 2 R 7 7 substituents; L is selected from the group consisting of a direct bond, C ~ 1 ~ -C ~ 12 ~ alkylene, C ~ 1 ~ -C ~ 12 ~ heteroalkylene, C ~ 3 ~ -C ~ 6 ~ cycloalkylene, arylene, heteroarylene, - CO-, -SO and -Se-; R ^ 4 ^ is selected from the group consisting of H, C ~ 1 ~ -C ~ 8 ~ alkyl, C ~ 2 ~ -C ~ 6 ~ alkenyl, C ~ 2 ~ -C ~ 6 ~ alkynyl, C ~ 1 heteroalkyl ~ -C ~ 8 ~, C ~ 0 ~ -C ~ 8 ~ arylalkyl, C ~ 3 ~ C ~ 12 ~ cycloalkyl and heterocyclyl are claimed. The compounds are inhibitors of soluble epoxide hydrolase (sEH) and useful for the treatment of hypertension, inflammation, adult respiratory distress syndrome; diabetic complications; end-stage kidney disease; Raynaud's syndrome and arthritis.
机译:专利,药物,药物,药物,药物,药物,药物,药物,药物,药物和药物,血管炎症,患者肾脏炎症以及生物活性二元醇的形成,以调节患者中的内皮细胞功能,使大量人在覆膜过程中监测可溶性水解酶的活性。式(I)的化合物,其中R ^ 1 ^是C〜1〜-C〜8〜烷基,C〜0〜-C〜8〜芳烷基,C〜3〜-C环烷基〜 12〜和杂环基,Y ^ 1 ^选自由键,C(R ^ 5 ^)〜2〜,NR ^ 5 ^和O组成的组; Y ^ 2 ^选自由键,NR ^ 5 ^和O组成的组;每个R ^ 2 ^,R ^ 3 ^和R ^ 5 ^独立地选自H,烷基和COR ^ 6 ^; A是杂环基,任选地被1-2个R 7 7取代基取代; L选自由以下组成的组:直接键,C〜1〜-C〜12〜亚烷基,C〜1〜-C〜12〜杂亚烷基,C〜3〜-C〜6〜环亚烷基,亚芳基,杂亚芳基,- CO-,-SO和-Se-; R ^ 4 ^选自H,C〜1〜-C〜8〜烷基,C〜2〜-C〜6〜烯基,C〜2〜-C〜6〜炔基,C〜1杂烷基要求保护的是〜-C〜8〜,C〜0〜-C〜8〜芳烷基,C〜3〜C〜12〜环烷基和杂环基。该化合物是可溶性环氧化物水解酶(sEH)的抑制剂,可用于治疗高血压,炎症,成人呼吸窘迫综合征。糖尿病并发症;终末期肾脏疾病;雷诺氏综合症和关节炎。

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