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    • 3. 发明申请
    • CHITOSAN CONSTRUCT AND METHOD OF PREPARING THE SAME
    • CHITOSAN构造及其制备方法
    • WO2009035414A1
    • 2009-03-19
    • PCT/SG2008/000339
    • 2008-09-10
    • NATIONAL UNIVERSITY OF SINGAPOREBAI, RenbiHAN, Wei
    • BAI, RenbiHAN, Wei
    • C08L5/08C08B37/08C08J5/00D01D5/24
    • C08L5/08C08B37/003D01D1/02D01D5/24D01F9/00
    • The present invention provides a chitosan construct having a high mechanical strength. The chitosan construct may have a tensile strength > 0.1 MPa. The tensile strength may be 0.1-6 MPa. The chitosan construct may be a fibre. In particular, the chitosan construct may be a hollow fibre. The chitosan construct may be prepared from a chitosan solution having a high chitosan concentration. The chitosan concentration in the chitosan solution may be ≥ 5 wt %. A method of preparing a construct comprising chitosan is also provided. The method comprises the steps of: (i) mixing chitosan and at least one solvent to form a mixture; (ii) evaporating the mixture to form a chitosan solution; and (iii) preparing the construct from the chitosan solution, wherein the construct has a tensile strength of 0.1-6 MPa. The chitosan solution formed in step (ii) may have a chitosan concentration ≥ 5 wt %.
    • 本发明提供具有高机械强度的壳聚糖结构。 壳聚糖构建体的拉伸强度可以> 0.1MPa。 拉伸强度可以为0.1-6MPa。 壳聚糖构建体可以是纤维。 特别地,壳聚糖构建体可以是中空纤维。 壳聚糖构建体可以由具有高壳聚糖浓度的壳聚糖溶液制备。 壳聚糖溶液中的壳聚糖浓度可以为= 5wt%。 还提供了制备包含壳聚糖的构建体的方法。 该方法包括以下步骤:(i)将壳聚糖和至少一种溶剂混合以形成混合物; (ii)蒸发混合物以形成壳聚糖溶液; 和(iii)从壳聚糖溶液制备构建体,其中该构造体具有0.1-6MPa的拉伸强度。 在步骤(ii)中形成的壳聚糖溶液可具有5重量%的壳聚糖浓度。
    • 5. 发明申请
    • THIOPHENE DERIVATIVES AS FACTOR XIA INHIBITORS
    • 噻吩衍生物作为因子XIA抑制剂
    • WO2007070816A3
    • 2007-09-07
    • PCT/US2006061970
    • 2006-12-13
    • SQUIBB BRISTOL MYERS COHAN WEI
    • HAN WEI
    • C07D333/24A61K31/381A61K31/416A61P7/02A61P29/00C07D333/28C07D409/04
    • C07D333/24C07D333/28C07D409/04
    • The present invention provides compounds of Formula (I); or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, L 1 , R 3 , and R 11 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    • 本发明提供了式(I)的化合物; 或其立体异构体,互变异构体,可药用盐,溶剂化物或前药,其中变量A,L 1,R 3,R 11, 如本文所定义。 式(I)化合物可用作凝血级联和/或接触活化系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶,因子Xa,因子XIa,因子IXa,因子VIIa和/或血浆激肽释放酶。 具体而言,它涉及选择性因子XIa抑制剂的化合物。 本发明还涉及包含这些化合物的药物组合物以及使用该组合物治疗血栓栓塞性和/或炎症性疾病的方法。
    • 6. 发明申请
    • THIOPHENE DERIVATIVES AS FACTOR XIA INHIBITORS
    • THIOPHENE DERIVATIVES作为因子XIA抑制剂
    • WO2007070816A2
    • 2007-06-21
    • PCT/US2006/061970
    • 2006-12-13
    • BRISTOL-MYERS SQUIBB COMPANYHAN, Wei
    • HAN, Wei
    • C07D333/24C07D333/28C07D409/04
    • The present invention provides compounds of Formula (I); or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, L 1 , R 3 , and R 11 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    • 本发明提供式(I)的化合物; 或其立体异构体,互变异构体,药学上可接受的盐,溶剂化物或前药,其中变量A,L 1,R 3和R 11, 如本文所定义。 式(I)的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶,因子Xa,因子XIa,因子IXa,因子VIIa和/或血浆激肽释放酶。 特别地,它涉及作为选择性因子XIa抑制剂的化合物。 本发明还涉及包含这些化合物的药物组合物和使用其制备血栓栓塞和/或炎症性疾病的方法。
    • 7. 发明申请
    • HETEROCYCLIC DIHYDROPYRIMIDINE COMPOUNDS
    • 杂环二氢嘧啶化合物
    • WO2007027454A1
    • 2007-03-08
    • PCT/US2006/032382
    • 2006-08-18
    • BRISTOL-MYERS SQUIBB COMPANYHAN, WeiHU, Zilun
    • HAN, WeiHU, Zilun
    • C07D487/04A61K31/505A61P9/06
    • C07D487/04
    • Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra rapidly activating delayed rectifier, which have the structure: (Formula I); stereoisomers including enantiomers thereof and diastereomers thereof, or a pharmaceutically acceptable salt thereof, wherein Q is alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl or: (Formula II) which is aryl, substituted aryl, heteroaryl or substituted heteroaryl; R 3 is a) (Formula III), b) (Formula IV), or c) (Formula V); wherein R 1 , R 2 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are defined herein. Methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds are also provided.
    • 可用作钾通道功能抑制剂的新型杂环二氢嘧啶化合物(特别是电压门控K +通道的Kv1亚家族抑制剂,特别是与超快速活化延迟整流剂连接的抑制剂Kv1.5,其结构如下:(式I) 其中Q为烷基,取代的烷基,环烷基,取代的环烷基,环杂烷基,取代的环杂烷基或:(式II),其为芳基,取代的芳基,杂芳基或取代的杂芳基 ; R 3是a)(式III),b)(式IV)或c)(式V); 其中R 1,R 2,R 4,R 5,R 6, R 7,R 8,R 9和R 10在本文中定义。 还提供了使用这些化合物预防和治疗心律失常和IKur相关病症的方法,以及含有这些化合物的药物组合物。