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    • 6. 发明申请
    • Potassium channel opener
    • 钾通道开启剂
    • US20040116482A1
    • 2004-06-17
    • US10664165
    • 2003-09-17
    • Yuji ImaizumiTomohiko Ohwada
    • A61K031/44A61K031/40A61K031/275A61K031/19A61K031/045A61K031/12
    • A61K31/19
    • A potassium channel opener comprising a compound (e.g., pimaric acid) represented by the formula nullInull: 1 wherein R1, R2, R3, R4, R5, R6 and R7 are each independently hydrogen, alkyl, alkenyl, halogen, hydroxy, halogenated alkyl, hydroxyalkyl, aminoalkyl, alkoxy, aryl, heteroaryl, acyl, carboxyl, alkoxycarbonyl, hydroxamate, sulfo, carbamoyl, sulfonamide, aldehyde, or nitrile; or R4 and R5 may be bonded to each other to form a ring; or R6 and R7 may be bonded to each other to form a ring; and all of three bonds represented by are single bonds, or one of the three bonds is double bond and the other bonds are single bonds, or a physiologically acceptable salt thereof as an effective ingredient.
    • 钾通道开放剂,其包含由式[I]表示的化合物(例如,海松酸):其中R 1,R 2,R 3,R 4,R 5,R 6 和R 7各自独立地为氢,烷基,烯基,卤素,羟基,卤代烷基,羟基烷基,氨基烷基,烷氧基,芳基,杂芳基,酰基,羧基,烷氧基羰基,异羟肟酸酯,磺基,氨基甲酰基,磺酰胺,醛或腈 ; 或R 4和R 5可以彼此键合形成环; 或R 6和R 7可以彼此键合形成环; 并且由表示的所有三个键都是单键,或者是 三键为双键,其他键为单键,或其生理学上可接受的盐作为有效成分。
    • 9. 发明申请
    • Therapeutic 1,2,3,6-tetrahydropyrimidine-2-one compositions and methods therewith
    • 治疗性1,2,3,6-四氢嘧啶-2-酮组合物及其方法
    • US20030207851A1
    • 2003-11-06
    • US10139193
    • 2002-05-02
    • Edward T. Wei
    • A61K031/573A61K031/513A61K031/137A61K031/045
    • A61K9/0075A61K9/0043A61K31/00A61K31/513A61K31/56A61K31/573A61K45/06A61M15/08A61M2202/064A61K2300/00
    • A therapeutic composition is provided that comprises a 1-R1-phenyl, 4-R2-phenyl substituted 1,2,3,6-tetrahydropyrimidine-2-one cold receptor agonist in a therapeutically effective amount and preferably further comprises one or more pharmaceutically active drugs such as an anti-inflammatory glucocorticosteroid, a sympathomimetic amine decongestant, an anti-histamine, a local anesthetic, menthol or a menthol analog, and mixtures thereof. The cold receptor agonist may be represented by the general formula 1-null1R-phenylnull-4-nullR2-phenylnull-1,2,3,6-tetrahydropyrimidine-2-one wherein: R1 is -hydroxy, -chloro, -fluoro, -alkyl, -acetoxy, -trifluoromethyl; and R2 is -nitro, -chloro, -fluoro, -alkyl, -trifluoromethyl. Therapeutic compositions of the invention elicit long-lasting cooling or soothing, particularly when formulated for delivery to suppress the sensations of itch and pain, such as for delivery to inflamed skin, to the mucous membranes of the anogenital areas, and to the enteric mucosa.
    • 提供了治疗组合物,其包含治疗有效量的1-R 1 - 苯基,4-R 2 - 苯基取代的1,2,3,6-四氢嘧啶-2-酮冷受体激动剂,优选还包含一种或多种药学活性 药物如抗炎糖皮质激素,拟交感胺减充血剂,抗组胺,局部麻醉剂,薄荷醇或薄荷醇类似物及其混合物。 冷受体激动剂可以由通式1- [1R-苯基] -4- [R2-苯基] -1,2,3,6-四氢嘧啶-2-酮表示,其中:R1是 - 羟基, - 氯, - 氟, - 烷基, - 乙酰氧基, - 三氟甲基; 并且R 2是 - 硝基, - 氯, - 氟, - 烷基, - 三氟甲基。 本发明的治疗组合物引起持久的冷却或舒缓,特别是当配制用于输送以抑制瘙痒和疼痛的感觉,例如用于递送至发炎的皮肤,向肛门生殖区域的粘膜和肠粘膜时。