发现和镇痛评价8-氯-1,4-二氢吡啶并[2,3- b ]吡嗪-2,3-二酮作为新型有效的d-氨基酸氧化酶抑制剂
摘要:
合成了一系列5-氮杂喹喔啉-2,3-二酮衍生物,并评估了其作为潜在的基于α-羟基内酰胺的抑制剂对d-氨基酸氧化酶(DAAO)的抑制作用。体外的强抑制活性表明5-氮可以通过增强相关的氢键相互作用来显着增强结合亲和力。研究了鞘内和全身注射8-氯-1,4-二氢吡啶并[2,3- b ]吡嗪-2,3-二酮(5-氮杂喹喔啉-2,3-二酮的代表分子)的镇痛作用。啮齿动物。这项研究不仅证实了DAAO抑制剂的镇痛作用,而且还提供了一类具有口服应用潜力的新型化学实体,可用于治疗慢性疼痛和吗啡镇痛耐受性。
The invention relates to a method of removing 3-deoxyglucosone and other alpha-dicarbonyl sugars from skin. The invention further relates to methods of inhibiting production and function of 3-deoxyglucosone and other alpha-dicarbonyl sugars in skin. The invention also relates to methods of treating 3-deoxyglucosone and other alpha-dicarbonyl sugars associated diseases and disorders of skin.
[EN] NOVEL SUBSTITUTED PHENYL COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS<br/>[FR] NOUVEAUX COMPOSÉS PHÉNYLE SUBSTITUÉS UTILISÉS EN TANT QU'INHIBITEURS DE L'INDOLÉAMINE 2,3-DIOXYGÉNASE (IDO)
申请人:MERCK SHARP & DOHME
公开号:WO2019027855A1
公开(公告)日:2019-02-07
Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (I) Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
Described herein are compounds of formula (I), formula la or formula lb The compounds of formula I, formula la or formula lb act as DGATl inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
[EN] PYRROLO [2, 3-C] PYRIDINE DERIVATIVES AS P38 KINASE INHIBITING AGENTS<br/>[FR] DÉRIVÉS DE PYRROLO[2,3-C]PYRIDINE EN TANT QU'INHIBITEURS DE KINASE P38
申请人:MERCK & CO INC
公开号:WO2009152072A1
公开(公告)日:2009-12-17
Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (A) are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
Fructoseamine 3 kinase and the formation of collagen and elastin
申请人:Tobia Annette
公开号:US20070065443A1
公开(公告)日:2007-03-22
The invention relates to the discovery that levels of collagen and elastin can be modulated by changing the flux through the Amadori Pathway and that copper containing compounds and complexes inhibit the enzyme fructoseamine-3-kinase.