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504 条记录 (耗时 0.075 秒)

    Cyclin Based Inhibitors of CDK2 and CDK4
    21.
    发明申请
    Cyclin Based Inhibitors of CDK2 and CDK4 审中-公开
    细胞周期蛋白抑制剂CDK2和CDK4

    公开(公告)号：US20140296484A1

    公开(公告)日：2014-10-02

    申请号：US13940407

    申请日：2013-07-12

    申请人： University of South Carolina

    发明人： Campbell McInnes ,  Shu Liu

    IPC分类号： C07K5/11 ,  C07K5/09

    CPC分类号： C07K5/1019 ,  C07K5/0202 ,  C07K5/06095 ,  C07K5/0815 ,  C07K14/4738

    摘要： Structural and functional analysis of peptide inhibitor binding to the cyclin D and cyclin A groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.

    摘要翻译： 已经研究了肽抑制剂与细胞周期蛋白D和细胞周期蛋白A凹槽结合的结构和功能分析，并用于设计提供结构 - 活性关系的基础的肽，具有改进的结合并具有作为化学生物学探针的潜力作为潜在诊断 并且作为治疗包括癌症和炎症在内的增殖性疾病的治疗剂。

    Novel Peptides For Treating and Preventing Immune-Related Disorders, Including Treating And Preventing Infection by Modulating Innate Immunity
    23.
    发明申请
    Novel Peptides For Treating and Preventing Immune-Related Disorders, Including Treating And Preventing Infection by Modulating Innate Immunity 有权
    用于治疗和预防免疫相关疾病的新型肽，包括通过调节先天免疫治疗和预防感染

    公开(公告)号：US20130316960A1

    公开(公告)日：2013-11-28

    申请号：US13457162

    申请日：2012-04-26

    申请人： Oreola Donini ,  Annett Rozek ,  Shannon Wayne Lentz

    发明人： Oreola Donini ,  Annett Rozek ,  Shannon Wayne Lentz

    IPC分类号： C07K14/81

    CPC分类号： C07K14/8103 ,  A61K38/00 ,  C07K5/0806 ,  C07K5/081 ,  C07K5/0815 ,  C07K5/0817 ,  C07K5/1019 ,  C07K7/06 ,  C07K7/08 ,  C12Q1/37 ,  G01N33/569 ,  G01N33/6893 ,  G01N2800/24 ,  G01N2800/26 ,  G01N2800/52 ,  Y02A50/473 ,  Y02A50/481 ,  Y02A50/491

    摘要： In one aspect, the present invention provides isolated novel peptides that can be used to modulate innate immunity in a subject and/or for the treatment of an immune-related disorder, including treating and preventing infection by modulating innate immunity. Also provided are an agent reactive with the peptide, a pharmaceutical composition that includes the peptide, an isolated nucleic acid molecule encoding the peptide, a recombinant nucleic acid construct that includes the nucleic acid molecule, at least one host cell comprising the recombinant nucleic acid construct, and a method of producing the peptide using the host cell. The present invention further provides a method for treating and/or preventing infection in a subject by administering the peptide of the invention to the subject, thereby modulating innate immunity in the subject. Additionally, the present invention provides a method for predicting whether a subject would be responsive to treatment with a peptide of the invention.

    摘要翻译： 一方面，本发明提供分离的新型肽，其可用于调节受试者中的先天免疫和/或用于治疗免疫相关病症，包括通过调节先天免疫来治疗和预防感染。 还提供了与肽反应的试剂，包含肽，分离的编码该肽的核酸分子的药物组合物，包含该核酸分子的重组核酸构建体，至少一个宿主细胞，其包含重组核酸构建体 ，以及使用该宿主细胞产生该肽的方法。 本发明还提供了通过将本发明的肽给予受试者来治疗和/或预防受试者感染的方法，从而调节受试者的先天免疫。 另外，本发明提供了一种用于预测受试者是否对本发明的肽的治疗有反应的方法。

    Compositions comprising enzyme-cleavable oxycodone prodrug
    25.
    发明授权
    Compositions comprising enzyme-cleavable oxycodone prodrug 有权
    包含可酶切的羟考酮前药的组合物

    公开(公告)号：US08569228B2

    公开(公告)日：2013-10-29

    申请号：US13346062

    申请日：2012-01-09

    申请人： Thomas E. Jenkins ,  Craig O. Husfeld

    发明人： Thomas E. Jenkins ,  Craig O. Husfeld

    IPC分类号： A61K38/00 ,  C07D489/00 ,  C07D489/08

    CPC分类号： C07K5/0815 ,  A61K31/155 ,  A61K31/195 ,  A61K31/245 ,  A61K31/445 ,  A61K31/485 ,  A61K31/4965 ,  A61K38/05 ,  A61K45/06 ,  A61K47/65 ,  C07D489/08 ,  C12Q1/37 ,  A61K2300/00

    摘要： The embodiments provide Compound KC-8, N-1-[3-(oxycodone-6-enol-carbonyl-methyl-amino) -2,2-dimethyl-propylamine]-arginine-glycine-malonic acid, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug, Compound KC-8, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

    摘要翻译： 实施方案提供化合物KC-8，N-1- [3-（羟考酮-6-烯醇 - 羰基 - 甲基 - 氨基）-2,2-二甲基 - 丙胺] - 精氨酸 - 甘氨酸 - 丙二酸，或其可接受的盐，溶剂合物 ，及其水合物。 本公开还提供了组合物及其使用方法，其中组合物包含提供羟考酮的受控释放的前药，化合物KC-8。 这样的组合物可以任选地提供胰蛋白酶抑制剂，其与介导羟考酮从前药的受控释放的酶相互作用，以减弱前药的酶裂解。

    PROCESS FOR THE MANUFACTURE OF DEGARELIX AND ITS INTERMEDIATES
    26.
    发明申请
    PROCESS FOR THE MANUFACTURE OF DEGARELIX AND ITS INTERMEDIATES 有权
    制造工艺及其中间体

    公开(公告)号：US20130281661A1

    公开(公告)日：2013-10-24

    申请号：US13881744

    申请日：2011-10-26

    申请人： Jon Holbech Rasmusse ,  Jens Fomsgaard ,  Stefan Hansen ,  Palle Hedengran Rasmussen ,  Wolfgang Oliver Wachs

    发明人： Jon Holbech Rasmusse ,  Jens Fomsgaard ,  Stefan Hansen ,  Palle Hedengran Rasmussen ,  Wolfgang Oliver Wachs

    IPC分类号： C07K7/06

    CPC分类号： C07K7/06 ,  A61K38/04 ,  A61K38/08 ,  C07K1/00 ,  C07K1/02 ,  C07K1/023 ,  C07K1/026 ,  C07K1/08 ,  C07K1/10 ,  C07K5/081 ,  C07K5/0812 ,  C07K5/0815 ,  C07K7/04 ,  C07K7/23 ,  Y02P20/55

    摘要： The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degarelix, its protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degarelix itself. Degarelix can be obtained by subjecting a Degarelix precursor according to formula (II): (P1)AA1-AA2-AA3-AA4(P4)-AA5-AA6(P6)-AA7-AA8(P8)-AA9-AA10-NH2 (II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein P1 is an amino protecting groups; preferably acetyl; P4 is hydrogen or a hydroxy! protecting group, preferably a hydroxyl protecting group; P6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and P8 is an amino protecting group.

    摘要翻译： 本发明涉及用于制备十肽Degarelix，其受保护的前体和其它有用的中间体的液体（或溶液）相制备方法。 本发明还涉及可用于溶液相制备方法和Degarelix本身纯化的多肽。 通过使根据式（II）的Degarelix前体：（P1）AA1-AA2-AA3-AA4（P4）-AA5-AA6（P6）-AA7-AA8（P8）-AA9-AA10-NH2（ II）或其盐或溶剂合物，在有机溶剂中用切割剂进行处理，其中P1是氨基保护基; 优选乙酰基; P4是氢或羟基保护基，优选羟基保护基; P6是氢或氨基保护基; 优选氨基保护基; P8是氨基保护基。

    Antimicrobial and anticancer lipopeptides
    27.
    发明授权
    Antimicrobial and anticancer lipopeptides 有权
    抗菌和抗癌脂肽

    公开(公告)号：US08445636B2

    公开(公告)日：2013-05-21

    申请号：US12685202

    申请日：2010-01-11

    申请人： Yechiel Shai ,  Dorit Avrahami

    发明人： Yechiel Shai ,  Dorit Avrahami

    IPC分类号： C07K1/00

    CPC分类号： C07K5/06086 ,  A61K38/00 ,  A61K47/542 ,  C07K5/0815 ,  C07K5/1019 ,  C07K7/06 ,  C07K7/08 ,  C07K14/46

    摘要： The invention provides lipophilic conjugates comprising a peptide coupled to a fatty acid, the peptide comprising at least two positively charged amino acid residues, said peptide after conjugation to the fatty acid possessing antibacterial, antifungal, and/or anticancer activity higher than prior to conjugation. The lipophilic conjugates are suitable for treatment of infections caused by pathogenic organisms such as bacteria and fungi. The lipophilic conjugates are also suitable for sanitation, as disinfectants, or for food preservation.

    摘要翻译： 本发明提供了亲脂性缀合物，其包含与脂肪酸偶联的肽，所述肽包含至少两个带正电荷的氨基酸残基，所述肽与缀合之后具有比缀合之前更高的抗细菌，抗真菌和/或抗癌活性的脂肪酸缀合。 亲脂性缀合物适用于治疗由病原体如细菌和真菌引起的感染。 亲脂性缀合物也适用于卫生，消毒剂或食品保鲜。

    Oligomeric biosurfactants in dermatocosmetic compositions
    29.
    发明授权
    Oligomeric biosurfactants in dermatocosmetic compositions 有权
    皮肤外用组合物中的低聚生物表面活性剂

    公开(公告)号：US08431523B2

    公开(公告)日：2013-04-30

    申请号：US12995049

    申请日：2009-05-29

    申请人： Donald R. Owen ,  Lili Fan

    发明人： Donald R. Owen ,  Lili Fan

    IPC分类号： A61K38/00 ,  A61K8/00

    CPC分类号： A61K38/01 ,  A61K8/0291 ,  A61K8/06 ,  A61K8/64 ,  A61K47/6907 ,  A61Q1/02 ,  A61Q17/04 ,  A61Q19/08 ,  A61Q19/10 ,  C07K5/06026 ,  C07K5/06086 ,  C07K5/06095 ,  C07K5/06113 ,  C07K5/06147 ,  C07K5/0806 ,  C07K5/081 ,  C07K5/0815 ,  C07K5/0817 ,  C07K5/0819 ,  C07K5/1008 ,  C07K5/101 ,  C07K5/1013 ,  C07K5/1019 ,  C07K5/1021 ,  C07K7/06

    摘要： Oligomeric acylated biosurfactants (“OABs”) having low critical micelle concentrations of from about 1.0 ppm to about 200 ppm, preferably less than about 50 ppm, in an aqueous solution of Minimal Essential Media that can lower the surface tension in the aqueous MEM environment to less than about 50 dynes/cm2 and have the ability to increase metabolic soluble proteins and/or increase synthesis of extracellular skin matrix proteins and/or increase rates of cell turnover while at the same time exhibiting comparatively low toxicity—preferably, an LD50 of greater 200 ppm in 37 year-old female fibroblast cells. Another aspect of the present invention is directed to the use of OABs in formulations that are topically-applied, by which is meant the formulation is placed in direct contact with the skin, hair and nails as well as mucosa of the eyes, ears, nose, mouth, anus and vagina.

    摘要翻译： 在Minimal Essential Media的水溶液中具有约1.0ppm至约200ppm，优选小于约50ppm的低临界胶束浓度的低聚酰化生物表面活性剂（“OAB”）可以将含水MEM环境中的表面张力降低至 小于约50达因/厘米2，并且具有增加代谢可溶性蛋白质和/或增加细胞外皮肤基质蛋白质的合成和/或增加细胞周转率的能力，同时显示较低的毒性 - 优选LD 50较大 在37岁的女性成纤维细胞中为200ppm。 本发明的另一方面涉及OABs在局部应用的制剂中的用途，通过这些方法将制剂置于与皮肤，头发和指甲以及眼睛，耳朵，鼻子的粘膜直接接触 ，嘴，肛门和阴道。