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    • 6. 发明公开
    • 염소화 시약의 제조 공정 및 염소화 당의 제조에 있어 그의용도
    • 生产氯仿试剂的过程及其在制备氯化糖中的应用
    • KR1020090007556A
    • 2009-01-19
    • KR1020087022691
    • 2007-02-28
    • 브이.비. 메디케어 프리베이트 엘티디.
    • 라트남,라케쉬오로라,선디프모피주딘,모하메드
    • C07H1/00C07H13/02C07H15/00C07H5/02
    • C07H1/00C07H5/02C07H13/02C07H15/00
    • Preparation of chlorinating reagent or chlorination reaction itself for use in a reaction such as production of high intensity sweetener trichlorogalactosucrose (TGS) from partially protected sucrose comprising reaction of dimethylformamide (DMF) with thionyl chloride or another sulphur containing inorganic acid chlorides including sulphuryl chloride is faced with a problem of prolific release of gaseous by-products, that at times may lead to violent explosion also. This problem is solved by innovative addition of solid powder inert to the constituents of the chlorination reaction mixture to the reaction, or by adding DMF to acid chloride solution in that order. The invention also leads to use of isolated solid Vilsmeier reagent being used for chlorination in a solvent other than DMF making it possible to avoid altogether problems arising from use of DMF which include irrecoverable loss in alkaline as well as acid conditions, interference in crystallization of TGS and the like.
    • 制备氯化试剂或氯化反应本身用于反应,例如从部分保护的蔗糖生产高强度甜味剂三氯半乳蔗糖(TGS),包括二甲基甲酰胺(DMF)与亚硫酰氯或另一种含硫的无机酰氯(包括磺酰氯)的反应 存在气态副产物多产释放的问题,有时也可能导致剧烈的爆炸。 通过将氯化反应混合物的成分惰性的固体粉末添加到反应中,或者通过向该酰氯溶液中依次加入DMF来解决这个问题。 本发明还导致使用分离的固体维尔斯迈尔试剂用于在DMF以外的溶剂中进行氯化,使得可以避免使用DMF引起的一切问题,其包括在碱性和酸性条件下不可恢复的损失,TGS的结晶干扰 等等。
    • 7. 发明公开
    • 항혈전 화합물
    • 抗生素化合物
    • KR1020060125888A
    • 2006-12-06
    • KR1020067017903
    • 2005-03-03
    • 사노피
    • 부이스만,로저,크리스티안드코트,마틴모일레만,디르크,게리트반보엑켈,콘스탄트
    • C07H11/00C07H15/00C07H15/04C07K5/00
    • C07K5/06113A61K38/00C07H11/00C07H15/04C07H15/08C07K9/003
    • The present invention relates compounds of the formula (A) oligosaccharide-spacer-GpIIb/IIIa antagonist (A), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising four to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT- III mediated) anti-Xa activity per se; the spacer is a bond or an essentially pharmacologically inactive linking residue; the GpIIb/IIIa antagonist is a residue mimicking the RGD and/or K(QA)GD fragment of fibrinogen, typically comprising an optionally esterified carboxylate moiety and a basic moiety located within the residue at a distance of 10- 20 Å from each other; or a pharmaceutically acceptable salt thereof or a prodrug or a solvate thereof. The compounds of the invention have antithrombotic activity and can be used in treating or preventing thrombotic diseases.
    • 本发明涉及式(A)寡糖 - 间隔基-GpIIb / IIIa拮抗剂(A)的化合物,其中寡糖是包含四至二十五个单糖单元的带负电荷的寡糖残基,电荷通过带正电荷的抗衡离子补偿,以及 其中所述寡糖残基源自具有(AT-III介导的)抗Xa活性本身的寡糖; 间隔基是键或基本上药理学上无活性的连接残基; GpIIb / IIIa拮抗剂是模拟纤维蛋白原的RGD和/或K(QA)GD片段的残基,通常包含任选酯化的羧酸酯部分和位于残留物内的距离彼此相距10-20的碱性部分; 或其药学上可接受的盐或其前药或溶剂化物。 本发明化合物具有抗血栓形成活性,可用于治疗或预防血栓形成疾病。