Controlled releases of actives in skin
    2.
    发明授权
    Controlled releases of actives in skin 有权
    皮肤活性物质的控制释放

    公开(公告)号:US08414871B2

    公开(公告)日:2013-04-09

    申请号:US12525529

    申请日:2008-01-31

    IPC分类号: A61K8/72

    摘要: Topical compositions are provided in which active compounds for topical delivery through the stratum corneum are complexed with nanospheres of a triblock copolymer having an A-B-A structure wherein each A end block is a water-soluble, hydrophilic and non-toxic polymer or oligomer; and the hydrophobic middle B block is a hydrophobic polymer or oligomer with the same or different repeating units having the structure according to formula:(I) wherein X is —C—R—C— or —C—; Z is between 2 and about 100, inclusive; R1 is CH═CH or (CH2), wherein n is from 0 to 18, inclusive; R2 is selected from hydrogen and straight and branched alkyl, alkoxy, alkylaryl and alkoxyaryl groups containing up to 18 carbon atoms; and R is selected from a bond or straight and branched alkyl, alkoxy, alkylaryl and alkoxyaryl groups containing up to 18 carbon atoms.

    摘要翻译: 提供了局部组合物,其中通过角质层局部递送的活性化合物与具有A-B-A结构的三嵌段共聚物的纳米球络合,其中每个A端嵌段是水溶性的,亲水的和无毒的聚合物或低聚物; 疏水性中间B嵌段是具有相同或不同的具有下式结构的重复单元的疏水聚合物或低聚物:其中X是-C(= O)-R-C(= O) - 或-C (= O) - ; Z在2至约100之间(含); R1为CH = CH或(CH2)n,其中n为0至18,包括端值; R2选自氢和含有至多18个碳原子的直链和支链烷基,烷氧基,烷基芳基和烷氧基芳基; 并且R选自含有至多18个碳原子的键或直链和支链烷基,烷氧基,烷基芳基和烷氧基芳基。

    Polymer compositions comprising antifibrotic agents, and methods of treatment, pharmaceutical compositions, and methods of preparation therefor
    4.
    发明授权
    Polymer compositions comprising antifibrotic agents, and methods of treatment, pharmaceutical compositions, and methods of preparation therefor 失效
    包含抗纤维化剂的聚合物组合物,治疗方法,药物组合物及其制备方法

    公开(公告)号:US06517824B1

    公开(公告)日:2003-02-11

    申请号:US08650324

    申请日:1996-05-20

    IPC分类号: A61K3174

    摘要: A method for treating pulmonary hypertension and other diseases involving a defect in collagen metabolism, by administration of an effective amount of a liposome encapsulated copolymer conjugate antifibrotic composition, is disclosed. The antifibrotic agent is preferably a proline analog, such as cis-4-hydroxy-L-proline (cHyp). Consistent, high loadings (>98%) of the antifibrotic agent are achieved by first forming a dipeptide with L-lysine, after which the dipeptide is copolymerized with the polymer component to form the copolymer conjugate. The polymer is preferably poly(ethylene glycol) having a weight average molecular weight of from about 500 to about 15,000. There is thus provided the efficient delivery and rateable release of the antifibrotic agent to inhibit collagen accumulation and thereby treat the diseases involved. Accordingly, there is a substantial reduction in the quantity of antifibrotic agent necessary, and thus a corresponding reduction in the potential for toxicity that would otherwise result from its prolonged administration.

    摘要翻译: 公开了通过施用有效量的脂质体包封的共聚物缀合抗纤维化组合物来治疗涉及胶原代谢缺陷的肺动脉高压和其它疾病的方法。 抗纤维化剂优选为脯氨酸类似物,例如顺式-4-羟基-L-脯氨酸(cHyp)。 通过首先用L-赖氨酸形成二肽来实现抗纤维化剂的一致,高负荷(> 98%),之后将二肽与聚合物组分共聚以形成共聚物缀合物。 聚合物优选为重均分子量为约500至约15,000的聚(乙二醇)。 因此,提供了抗纤维化剂的有效递送和有效释放以抑制胶原蛋白积累,从而治疗所涉及的疾病。 因此,所需的抗纤维化剂的量显着减少,因此由于其延长施用而导致的毒性潜力的相应降低。

    Method for indirect tire pressure monitoring
    9.
    发明授权
    Method for indirect tire pressure monitoring 有权
    间接轮胎压力监测方法

    公开(公告)号:US07991523B2

    公开(公告)日:2011-08-02

    申请号:US10587748

    申请日:2005-02-02

    IPC分类号: G01M17/00 G06F7/00

    CPC分类号: G01L17/00 G01M17/025

    摘要: Disclosed is a method of indirect tire pressure monitoring. The method includes: learning test variables (DIAG, SIDE, AXLE), which describe the rotational movements of the wheels; determining rolling circumference differences (ΔDIAG, ΔSIDE, ΔAXLE) from actually determined test variables and the learnt test variables; learning at least one torsion natural frequency fp for at least one tire from the oscillation behavior of the individual tires; determining at least one shift of the torsion natural frequency Δfp from at least one actually determined torsion natural frequency and from the at least one learnt torsion natural frequency; and combining the rolling circumference differences (ΔDIAG, ΔSIDE, ΔAXLE) with the at least one shift of the torsion natural frequency fp in a joint warning strategy for detecting and warning of tire inflation pressure loss.

    摘要翻译: 公开了一种间接轮胎压力监测的方法。 该方法包括:学习描述车轮旋转运动的测试变量(DIAG,SIDE,AXLE); 确定滚动圆周差异(&Dgr; DIAG,&Dgr; SIDE,&Dgr; AXLE)与实际确定的测试变量和学习的测试变量; 从单个轮胎的振荡行为学习至少一个轮胎的至少一个扭转固有频率fp; 从至少一个实际确定的扭转固有频率和至少一个学习的扭转固有频率确定扭转固有频率Dgr; fp的至少一个偏移; 并将滚动圆周差异(&Dgr; DIAG,&Dgr; SIDE,&Dgr; AXLE)与用于检测和警告轮胎充气压力损失的联合警告策略中的扭转固有频率fp的至少一个移位相结合。