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    • 1. 发明授权
    • Substituted-4-quinolones
    • 取代的4-喹诺酮
    • US07482362B2
    • 2009-01-27
    • US10450930
    • 2001-12-17
    • David Idris PritchardBarrie Walsham BycroftSiri Ram ChhabraDoreen Hooi
    • David Idris PritchardBarrie Walsham BycroftSiri Ram ChhabraDoreen Hooi
    • A01N43/42A61K31/47C07D215/00
    • A61K31/4709A61K31/47A61K31/496A61K2039/55511A61K2039/57
    • Substituted-4-quinolones of the formula (I): wherein R1 is a straight or branched chain, saturated or ethylenically-unsaturated aliphatic hydrocarbyl group containing 1 to 18 carbon atoms which may optionally be substituted by one or more substituent groups selected from halo, 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl and NR6R7, wherein each of R6 and R7 is independently selected from H and 1-6C alkyl or R6 and R7 together with the N atom to which they are attached form a saturated heterocyclic group selected from piperidino, piperazino and morpholino; R2 is a group selected from H, —OH, halo, —CHO, —CO2H and CONHR8 wherein R8 is H or a 1-6C alkyl; each of R3, R4 and R5 is independently selected form H, —CH3, —OCH3 and halo; or a non-toxic pharmaceutically-acceptable salt thereof, have use in the manufacture of a medicament for the treatment of a disease of a living animal body, including a human, which disease is responsive to the activity of an immunosuppressant. The preferred compound of the formula 1 is 2-n-heptyl-3-hydroxy-4(1H)-quinolone.
    • 式(I)的取代的4-喹诺酮:其中R 1是含有1至18个碳原子的直链或支链,饱和或不饱和的脂族烃基,其可任选被一个或多个选自以下的取代基取代:卤素, 1-6C烷氧基,羧基,1-6C烷氧基羰基和NR6R7,其中R6和R7各自独立地选自H和1-6C烷基或R6和R7与它们所连接的N原子一起形成饱和杂环基, 来自哌啶子基,哌嗪基和吗啉代; R2是选自H,-OH,卤素,-CHO,-CO 2 H和CONHR 8的基团,其中R 8是H或1-6 C烷基; R 3,R 4和R 5各自独立地选自H,-CH 3,-OCH 3和卤素; 或其无毒的药学上可接受的盐可用于制备用于治疗活动动物体(包括人)的疾病的药物,所述疾病对免疫抑制剂的活性有反应。 优选的式1化合物是2-正庚基-3-羟基-4(1H) - 喹诺酮。
    • 5. 发明授权
    • Treatment of wounds
    • 丝氨酸丝氨酸蛋白酶
    • US07144721B1
    • 2006-12-05
    • US10111252
    • 2000-10-20
    • David Idris Pritchard
    • David Idris Pritchard
    • C12N9/64C07K1/00
    • A61L15/32A61K38/00C07K14/43577
    • An isolated protein, for use in treatment of wounds, is characterized in that it is secreted by the organism Lucilia sericata and it exhibits proteolytic activity against FITC-casein at a pH of 8.0 to 8.5. The protein exhibits proteolytic activity against Tosyl-Gly-Pro-Arg-AMC but not against Suc-Ala-Ala-Phe-AMC, and its proteolytic activity against FITC-casein and Tosyl-Gly-Pro-Arg-AMC is inhibited by the serine proteinase inhibitors PMSF and AMPSF. The protein is also bound by immobilized aminobenzamidine.
    • 用于治疗伤口的分离的蛋白质的特征在于其由丝氨酸球菌分泌,并且其在8.0至8.5的pH下显示出针对FITC-酪蛋白的蛋白水解活性。 该蛋白质表现出对Tosyl-Gly-Pro-Arg-AMC的蛋白水解活性,但不对Suc-Ala-Ala-Phe-AMC表现出蛋白水解活性,其对FITC-酪蛋白和Tosyl-Gly-Pro-Arg-AMC的蛋白水解活性受到 丝氨酸蛋白酶抑制剂PMSF和AMPSF。 蛋白质也被固定化的氨基脒结合。
    • 9. 发明授权
    • Synergistic compositions of N-acylhomoserine lactones and 4-quinolones
    • US07371779B2
    • 2008-05-13
    • US10481373
    • 2002-07-03
    • David Idris Pritchard
    • David Idris Pritchard
    • C07D31/341
    • A61K31/47A61K31/365
    • A composition having immunosuppressant activity comprises at least one compound of the formula (I) in which R is an acyl group of the formula (II) wherein one of R1 and R2 is H and the other is selected from OR4, SR4 and NHR4, wherein R4 is H or 1-6C alkyl, or R1 and R2 together with the carbon atom to which they are joined form a keto group, and R3 is a straight or branched chain, saturated or unsaturated aliphatic hydrocarbyl group containing from 8 to 11 carbon atoms and is optionally substituted by one or more substituent groups selected from halo, 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl and NR5R6 wherein each of R5 and R6 is selected from H and 1-6C alkyl or R5 and R6 together with the N atom form a morpholino or piperazino group, or any enantiomer thereof; and at least one compound of the formula (III): wherein R7 is a straight or branched chain, saturated or ethylenically-unsaturated aliphatic hydrocarbyl group containing from 1 to 18 carbon atoms which may optionally be substituted by one or more substituent groups selected from halo, 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl and NR12R13, wherein each of R12 and R13 is independently selected from H and 1-6C alkyl or R12 and R13 together with the N atom to which they are attached form a saturated heterocyclic group selected from piperidino, piperazino and morpholino; R8 is a group selected from H, —OH, halo, —CHO, —CO2H and CONHR14 wherein R14 is H or a 1-6C alkyl; each of R9, R10 and R11 is independently selected from H, —CH3, —OCH3 and halo; or a non-toxic pharmaceutically-acceptable salt thereof. The determined immunosuppressant activity of the composition is greater than the sum of the activities of the individual components of the composition when determined separately