3-(2-Phenylethenyl)Pyridazine置于sodium Periodate,四氧化锇体系中,用 水,丙酮,叔丁醇 作为反应溶剂,化学反应 48.0H,以81%的收率获得产物哒嗪-3-甲醛 参考文献:Synthesis And Structure-activity Relationships Of Amide Derivatives Of (4,4-Difluoro-1,2,3,4-Tetrahydro-5H-1-Benzazepin-5-Ylidene)Acetic Acid As Selective Arginine Vasopressin V2 Receptor Agonists 标题:Synthesis And Structure-activity Relationships Of Amide Derivatives Of (4,4-Difluoro-1,2,3,4-Tetrahydro-5H-1-Benzazepin-5-Ylidene)Acetic Acid As Selective Arginine Vasopressin V2 Receptor Agonists 摘要:A Series Of (4,4-Difluoro-1,2,3,4-Tetrahydro-5H-1-Benzazepin-5-Ylidene)Acetamide Derivatives Was Synthesized,And Their Structure-Activity Relationships Were Examined In Order To Identify Potent And Selective Arginine Vasopressin V-2 Receptor Agonists. Attempts To Substitute Other Chemical Groups In Place Of The 2-Pyridilmethyl Moiety Of 1A Led To The Discovery That Potent V-2 Binding Affinity Could Be Obtained With A Wide Range Of Functional Groups. This Structural Tolerance Allowed For The Manipulation Of Other Attributes,Such As Selectivity Against V-1A Receptor Affinity Or Avoidance Of The Undesirable Inhibition Of Cytochrome P450 (Cyp),Without Losing Potent Affinity For The V-2 Receptor. Some Representative Compounds Obtained In This Study Were Also Found To Decrease Urine Volume In Awake Rats. (C) 2009 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmc.2009.03.001
专利号:US-7612106-B2 优先权日:2004-12-23 标题 :Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof 发明人:BOATMAN P DOUGLAS; SCHRADER THOMAS O; SEMPLE GRAEME; SKINNER PHILIP J; JUNG JAE-KYU 权利人:ARENA PHARM INC 摘要:The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. n nAlso provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.
专利号:US-9938258-B2 优先权日:2012-11-29 标 题:Substituted 2,3-dihydrobenzofuranyl compounds and uses thereof 发明人:BALOGLU ERKAN; SHECHTER SHARON; SHACHAM SHARON; MCCAULEY DILARA; SENAPEDIS WILLIAM; GOLAN GALI; KALID ORI 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to substituted 2,3-dihydrobenzofuranyl compounds, and more particularly to a compound represented by Structural Formula I: n nor a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.
专利号:CN-115557900-B 优先权日:2022-11-11 标 题:Synthesis method of 3-substituted pyridazine derivative