📜N,N-二甲基-对苯二胺置于三乙胺体系中,用 甲苯 用作溶剂,化学反应生成4-二甲氨基苯异氰酸酯 参考文献:Pyrazolidinone Cck And Gastrin Antagonists And Pharmaceutical 标题:Pyrazolidinone Cck And Gastrin Antagonists And Pharmaceutical 摘要:已发现新型取代吡唑啉酮具有显著的结合胆囊收缩素(cck)受体和胃泌素受体的能力,这些受体位于大脑和/或外周部位,如胰腺,胃和回肠.这些吡唑啉酮是cck和胃泌素受体拮抗剂,并在治疗消化系统疾病,中枢神经系统疾病以及温血脊椎动物的食欲调控中找到了治疗应用.描述了用于这些适应症的药物配方.
专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-9879050-B2 优先权日:2013-08-30 标 题 :Substituted urea depsipeptide analogs as activators of the CLPP endopeptidase 发明人:LEE RICHARD E; ZHAO YING; GRIFFITH ELIZABETH; ZHENG ZHONG; SINGH AMAN P 权利人:ST JUDE CHILDREN'S RES HOSPITAL 摘要:In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators the ClpP endopeptidease; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-8012972-B2 优先权日:2007-03-28 标 题:Pyridinecarboxylic acid (2-aminophenyl) amide derivative having urea structure 发明人:MOGI HIROYUKI; TAJIMA HISASHI; MISHINA NORIKO; YAMAZAKI YUSUKE; YONEDA SHINJI; WATANABE KATSUHIKO; FUJIKAWA JUNKO; YAMAMOTO MINORU 权利人:SANTEN PHARMACEUTICAL CO LTD 摘要:Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof. In the formula, R 1 and R 2 represent a hydrogen atom, a lower alkyl group or the like; R 3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, a carboxy group, a lower alkoxycarbonyl group, —OCONR a R b , —NR c R d or the like; R 4 and R 5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or the like; R a and R b represent a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group, a heterocyclic group or the like; R c and R d represent a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group or the like; X represents a lower alkylene group; Y represents a single bond, a lower alkylene group; W 1 -W 2 represents N—C or C—N; and l and m represent 0, 1, 2 or 3.
专利号:US-10822377-B2 优先权日:2015-03-04 标 题:Substituted urea depsipeptide analogs as activators of the ClpP endopeptidase 发明人:LEE RICHARD E; ZHAO YING; JIUYU LIU 权利人:ST JUDE CHILDRENS RES HOSPITAL 摘要:In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators the ClpP endopeptidease; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:EP-1200824-B1 优先权日:1999-06-15 标题:Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives
专利号:US-7615634-B2 优先权日:2003-02-10 标题:4-aminopyrimidine-5-one derivatives 发明人:BARTKOVITZ DAVID JOSEPH; CHU XIN-JIE; DING QINGJIE; JIANG NAN; LOVEY ALLEN JOHN; MOLITERNI JOHN ANTHONY; MULLIN JR JOHN GUILFOYLE; VU BINH THANH; WOVKULICH PETER MICHAEL 权利人:HOFFMANN LA ROCHE 摘要:Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.