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    • 4. 发明申请
    • Use of thiazole derivatives for preparing a medicine for protecting mitochondria
    • 噻唑衍生物用于制备线粒体保护药物的应用
    • US20040248885A1
    • 2004-12-09
    • US10483823
    • 2004-01-13
    • Michel AuguetPierre-Etienne Chabrier De LassauniereJeremiah Harnett
    • A61K031/5415A61K031/426C07D417/02
    • A61K31/425A61K31/426A61K31/427A61K31/497A61K31/54Y10S514/838
    • The invention concerns compounds of general formula (I), wherein: A represents one of the radicals in which R5 represents independently a hydrogen atom, or alkyl; R6, R7 and R8 independently represent a hydrogen atom, alkyl, cycloalkyl, hydroxy or alkoxy; R11 represents a hydrogen atom of alkyl; and R9, R10 and R12 independently represent a hydrogen atom, alkyl, hydroxy or alkoxy: B represents a hydrogen atom or alkyl; n represents an integer from 0 to 5; R1 and R2 independently represent a hydrogen atom, alkyl or cycloalkyl; R3 and R4 independently represent a hydrogen atom or an alkyl radical, or R3 and R4 together form with the nitrogen atom which bears them a heterocycle optionally substituted comprising in all 1 to 2 heteroatoms and 5 to 7 members. Said compounds can be used for preparing a medicine for protecting mitochondria, and in particular a medicine for preventing or treating cirrhosis. 1
    • 本发明涉及通式(I)的化合物,其中:A表示其中R 5独立地表示氢原子或烷基的基团之一; R 6,R 7和R 8独立地表示氢原子,烷基,环烷基,羟基或烷氧基; R 11表示烷基的氢原子; R 9,R 10和R 12独立地表示氢原子,烷基,羟基或烷氧基:B表示氢原子或烷基; n表示0〜5的整数, R 1和R 2独立地表示氢原子,烷基或环烷基; R 3和R 4独立地表示氢原子或烷基,或者R 3和R 4与氮原子一起形成,它们带有任选被取代的杂环,所述杂环任选地被包含在所有1至2个杂原子中, 5至7名成员。 所述化合物可用于制备用于保护线粒体的药物,特别是用于预防或治疗肝硬化的药物。
    • 9. 发明申请
    • 2-substituted bicyclic benzoheterocyclic compounds and their use as sodium channel blockers
    • 2-取代的双环苯并杂环化合物及其作为钠通道阻断剂的用途
    • US20040152696A1
    • 2004-08-05
    • US10628487
    • 2003-07-29
    • Euro-Celtique S.A.
    • Qun SunDonald J. KyleSamuel F. Victory
    • A61K031/5415A61K031/517C07D279/16C07D239/72
    • C07D239/91C07D279/08
    • This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel 2-substituted bicyclic benzoheterocyclic compounds of Formula I: 1 or a pharmaceutically-acceptable salt or solvate thereof, wherein X is nullNHnull, nullNnull or nullSnull, Y is oxygen or sulfur, and n, p, R1, R2, R3 and R4 are defined in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global or focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of acute or chronic pain, neuropathic pain or surgical pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    • 本发明涉及一种使用新的式I的2-取代双环苯并杂环化合物或其药学上可接受的盐或溶剂合物来治疗对钠离子通道阻断有反应的病症的方法,其中X是-NH-,-N =或 -S-,Y是氧或硫,n,p,R1,R2,R3和R4在说明书中定义。 本发明还涉及式I化合物用于治疗全身或局部缺血后神经元损伤,用于治疗或预防神经变性疾病如肌萎缩性侧索硬化(ALS)以及治疗,预防或改善的用途 急性或慢性疼痛,神经性疼痛或外科手术疼痛,作为抗惊厥药,抗惊厥药,抗抑郁药,作为局部麻醉剂,作为抗心律失常药物和用于治疗或预防糖尿病性神经病变。