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    • 4. 发明申请
    • Macrocyclic formulations for transmembrane drug delivery
    • 用于跨膜药物递送的大环制剂
    • US20080107735A1
    • 2008-05-08
    • US11591788
    • 2006-11-02
    • Robert J. GyurikCarl Reppucci
    • Robert J. GyurikCarl Reppucci
    • A61K9/14
    • A61K9/0014A61K47/10A61K47/22
    • Topically applied pharmaceutical products comprising (a) an active ingredient, (b) an organogel, and (c) a non-irritating permeation enhancer, are disclosed, along with and methods of use and formulations thereof. The topically applied products and methods are intended to be used to enhance any of the transdermal, subdermal, transmembrane, musculoskeletal, transungual, transonychial, and/or peronychial deliveries of a therapeutically effective amount of an active ingredient to a patient. The invention is particularly directed to topically applied pharmaceutical products for enhancing the delivery of a therapeutically effective amount of an active ingredient to a diseased or infected nail bed, nail matrix, and/or nail plate in the toenails or fingernails of a patient suffering from onychomycosis. The invention is also directed to delivery of an anti-inflammatory agent, preferably of the Cox-2 enzyme inhibitory class, topically to a site of soft tissue injury or discomfort.
    • 公开了包含(a)活性成分,(b)有机凝胶和(c)非刺激性渗透促进剂)的局部应用的药物产品,以及其使用方法和制剂。 局部施用的产品和方法旨在用于增强患者的治疗有效量的活性成分的任何透皮,皮下,跨膜,肌肉骨骼,横断面,转基因和/或肛门周围递送。 本发明特别涉及用于增强治疗有效量的活性成分向病患或受感染的甲床,指甲基质和/或指甲板在患有甲真菌病的患者的趾甲或指甲中的递送的药物产品 。 本发明还涉及将抗炎剂(优选为Cox-2酶抑制剂)局部递送至软组织损伤或不适的部位。
    • 5. 发明申请
    • Pharmaceutical compositions and methods for peptide treatment
    • 药物组合物和肽治疗方法
    • US20070265191A1
    • 2007-11-15
    • US11811304
    • 2007-06-07
    • Robert GyurikCarl Reppucci
    • Robert GyurikCarl Reppucci
    • A61K38/02A61P37/08
    • A61K9/0043A61K9/08A61K9/107A61K9/1075A61K31/12A61K31/365A61K31/485A61K38/02A61K38/08A61K38/25A61K47/06A61K47/08A61K47/10A61K47/18A61K47/186A61K47/22A61K47/32A61K47/44Y10S514/937
    • Disclosed are compositions and methods for treating a patient with a pharmaceutically active agent other than insulin selected from the group consisting of peptides, peptidomimetics, and proteins, wherein the pharmaceutical composition is in the form of an emulsified nasal spray comprising: a macrocyclic permeation enhancer, a liquid carrier comprising water, and a therapeutically effective amount of a pharmaceutically active agent other than insulin selected from the group consisting of peptides, peptidomimetics, and proteins; wherein the macrocyclic permeation enhancer is a Hsieh enhancer emulsified in the liquid carrier; and wherein the Hsieh enhancer has the following structure: wherein X and Y are oxygen, sulfur or an imino group of the structure or ═N—R with the proviso that when Y is the imino group, X is an imino group, and when Y is sulfur, X is sulfur or an imino group, A is a group having the structure wherein X and Y are defined above, m and n are integers having a value from 1 to 20 and the sum of m+n is not greater than 25, p is an integer having a value of 0 or 1, q is an integer having a value of 0 or 1, r is an integer having a value of 0 or 1, and each of R, R1, R2, R3, R4, R5 and R6 is independently hydrogen or an alkyl group having from 1 to 6 carbon atoms which may be straight chained or branched provided that only one of R1 to R6 can be an alkyl group, with the proviso that when p, q and r have a value of 0 and Y is oxygen, m+n is at least 11, and with the further proviso that when X is an imino group, q is equal to 1, Y is oxygen, and p and r are 0, then m+n is at least 11.
    • 公开了用除了选自肽,肽模拟物和蛋白质的胰岛素以外的药物活性剂治疗患者的组合物和方法,其中所述药物组合物为乳化鼻喷雾剂的形式,其包含:大环渗透促进剂, 包含水的液体载体和治疗有效量的选自肽,肽模拟物和蛋白质的胰岛素以外的药学活性剂; 其中所述大环渗透促进剂是在所述液体载体中乳化的Hsieh增强剂; 并且其中所述Hsieh增强剂具有以下结构:其中X和Y是结构中的氧,硫或亚氨基或-NR,条件是当Y是亚氨基时,X是亚氨基,当Y是硫时 X是硫或亚氨基,A是具有以上结构的基团,其中X和Y定义如上,m和n是具有1至20的整数,并且m + n的总和不大于25,p 是0或1的整数,q是0或1的整数,r是0或1的整数,R 1,R 1, R 2,R 3,R 4,R 5和R 6是 独立地是氢或具有1至6个碳原子的烷基,其可以是直链或支链的,条件是R 1至R 6中只有一个可以是烷基, 条件是当p,q和r的值为0,Y为氧时,m + n为至少11,另外条件是当X为亚氨基 gup等于1,Y为氧,p和r为0,则m + n为11以上。