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    Peptides intermediates for making GnRH antagonists
    2.
    发明授权
    Peptides intermediates for making GnRH antagonists 失效
    用于制备GnRH拮抗剂的肽中间体

    公开(公告)号：US06747125B1

    公开(公告)日：2004-06-08

    申请号：US08727798

    申请日：1996-10-07

    申请人： Carl A. Hoeger ,  Jean E. F. Rivier ,  Paula Guess Theobald ,  John S. Porter

    发明人： Carl A. Hoeger ,  Jean E. F. Rivier ,  Paula Guess Theobald ,  John S. Porter

    IPC分类号： C07K1600

    CPC分类号： C07D249/14 ,  A61K38/00 ,  C07C277/08 ,  C07C279/28 ,  C07K1/006 ,  C07K7/23 ,  Y10S514/80 ,  Y10S930/11 ,  Y10S930/13

    摘要： Peptides which include unnatural amino acids and which either promote or inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such peptides that are GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads and may be used to treat steroid-dependent tumors. The agonists can be used for control of reproduction processes, to treat precocious puberty, endometriosis, and the like. The peptides are analogs of the decapeptide GnRH wherein there is at least one residue of an unnatural amino acid in the 3-, 5-, 6- and/or 8-positions. Unnatural amino acids having the following formula are incorporated in a preferred group of synthesized peptides:

    摘要翻译： 包括非天然氨基酸并且促进或抑制垂体分泌促性腺激素并抑制性腺释放类固醇的肽。 施用有效量的这种肽作为GnRH拮抗剂可防止雌性哺乳动物卵的排卵和/或由性腺释放类固醇，并可用于治疗类固醇依赖性肿瘤。 激动剂可用于控制繁殖过程，治疗早熟青春期，子宫内膜异位症等。 肽是十肽GnRH的类似物，其中在3-，5-，6-和/或8-位有至少一个非天然氨基酸残基。 具有下列结构式的非天然氨基酸被掺入优选的一组合成肽中：

    Composition and method for enhancing transport across gastrointestinal tract cell layers
    6.
    发明授权
    Composition and method for enhancing transport across gastrointestinal tract cell layers 有权
    促进胃肠道细胞层转运的组合物和方法

    公开(公告)号：US06423334B1

    公开(公告)日：2002-07-23

    申请号：US09163510

    申请日：1998-09-30

    申请人： David J. Brayden ,  Jacqueline M. Dee

    发明人： David J. Brayden ,  Jacqueline M. Dee

    IPC分类号： A61K900

    CPC分类号： A61K47/14 ,  Y10S514/80 ,  Y10S514/802 ,  Y10S514/807 ,  Y10S514/808 ,  Y10S514/822

    摘要： A composition for enteral administration having a non-ionic vegetable oil GIT absorption enhancer capable of increasing the enteral absorbability of drugs, especially oral absorbability of hydrophilic and macromolecular drugs. The non-ionic vegetable oil GIT absorption enhancer, particularly Babassu oil or a derivative thereof, is capable of enhancing the uptake of a drug from the gastrointestinal tract so as to allow therapeutically effective amounts of the drug to be transported across the GIT of an animal such as a human without significant toxic side effects.

    摘要翻译： 一种用于肠内给药的组合物，其具有能够增加药物的肠内吸收性的非离子植物油GIT吸收促进剂，特别是亲水性和大分子药物的口服吸收性。 非离子植物油GIT吸收促进剂，特别是巴布苏油或其衍生物能够增强药物从胃肠道的摄取，以便允许治疗有效量的药物跨越动物的GIT转运 如人体无明显毒副作用。

    Pharmaceutical administration form for peptides, process for its preparation, and use
    7.
    发明申请
    Pharmaceutical administration form for peptides, process for its preparation, and use 有权
    肽的药物管理形式，其制备方法和用途

    公开(公告)号：US20020039996A1

    公开(公告)日：2002-04-04

    申请号：US09861009

    申请日：2001-05-18

    发明人： Horst Bauer ,  Michael Damm ,  Werner Sarlikiotis

    IPC分类号： A61K038/17

    CPC分类号： A61K47/40 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/19 ,  A61K47/12 ,  A61K47/26 ,  Y10S514/80

    摘要： The invention relates to pharmaceutical administration forms suitable for parenteral administration, which contains nullsicnull peptides prone to aggregation in the form of their acetate, gluconate, glucuronate, lactate, citrate, ascorbate, benzoate or phosphate salts in dissolved or dispersed form and additionally comprises nullsicnull one of the acids mentioned as free acid.

    摘要翻译： 本发明涉及适合肠胃外给药的药物给药形式，其包含易于以其溶解或分散形式的乙酸盐，葡萄糖酸盐，葡糖醛酸盐，葡萄糖醛酸盐，乳酸盐，柠檬酸盐，抗坏血酸盐，苯甲酸盐或磷酸盐形式的聚集的肽，并且另外包含 [sic]被称为游离酸的一种酸。

    GnRH antagonists being modified in positions 5 and 6
    8.
    发明授权
    GnRH antagonists being modified in positions 5 and 6 有权
    GnRH拮抗剂在5和6位修饰

    公开(公告)号：US06214798B1

    公开(公告)日：2001-04-10

    申请号：US09402698

    申请日：2000-01-03

    申请人： Graeme Semple ,  Guangcheng Jiang

    发明人： Graeme Semple ,  Guangcheng Jiang

    IPC分类号： A61K3800

    CPC分类号： C07K7/23 ,  A61K38/00 ,  Y02P20/55 ,  Y10S514/80 ,  Y10S930/11

    摘要： Peptides are provided which have improved duration of GnRH antagonistic properties. These antagonists may be used to regulate fertility and to treat steroid-dependent tumors and for other short-term and long-term treatment indications. These antagonists have a derivative of aminoPhe or its equivalent in the 5- or the 5- and 6-positions. This derivative is modified so as to contain a carbamoyl group or heterocycle, including a urea moiety, in its side chain. Decapeptides having the formula: Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(L-hydroorotyl)-D-4Amf(Q2)-Leu-Lys(isopropyl)-Pro-Xaa10, wherein Q2 is Cbm or MeCbm and Xaa10 is D-Ala-ol or Ala-ol are particularly effective and continue to exhibit very substantial suppression of LH secretion at 96 hours following injection.

    摘要翻译： 提供具有改善的GnRH拮抗性能持续时间的肽。 这些拮抗剂可用于调节生育力和治疗类固醇依赖性肿瘤和其他短期和长期治疗适应症。 这些拮抗剂在5-或5-和6-位具有氨基Phe的衍生物或其等同物。 该衍生物被修饰为在其侧链中含有氨基甲酰基或杂环，包括脲部分。 具有下式的十肽：其中Q2是Cbm或MeCbm，Xaa10是D-Ala-ol或Ala-ol是特别有效的，并且在注射后96小时继续表现出非常实质的LH分泌抑制。

    Pharmaceutical formulations for sustained drug delivery
    9.
    发明授权
    Pharmaceutical formulations for sustained drug delivery 失效
    用于持续给药的药物制剂

    公开(公告)号：US06180608B2

    公开(公告)日：2001-01-30

    申请号：US08988851

    申请日：1997-12-11

    申请人： Malcolm L. Gefter ,  Nicholas Barker ,  Gary Musso ,  Christopher J. Molineaux

    发明人： Malcolm L. Gefter ,  Nicholas Barker ,  Gary Musso ,  Christopher J. Molineaux

    IPC分类号： A61K3800

    CPC分类号： B82Y5/00 ,  A61K38/09 ,  A61K47/61 ,  A61K47/6949 ,  Y10S514/80

    摘要： Sustained delivery formulations comprising a water-insoluble complex of a peptidic compound (e.g., a peptide, polypeptide, protein, peptidomimetic or the like) and a carrier macromolecule are disclosed. The formulations of the invention allow for loading of high concentrations of peptidic compound in a small volume and for delivery of a pharmaceutically active peptidic compound for prolonged periods, e.g., one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. In a preferred embodiment, the peptidic compound of the complex is an LHRH analogue, preferably an LHRH antagonist, and the carrier macromolecule is an anionic polymer, preferably carboxymethylcellulose. Methods of making the complexes of the invention, and methods of using LHRH-analogue-containing complexes to treat conditions treatable with an LHRH analogue, are also disclosed.

    摘要翻译： 公开了包含肽化合物（例如肽，多肽，蛋白质，拟肽等）和载体大分子的水不溶性络合物的持续递送制剂。 本发明的制剂允许在施用复合物之后将较高体积的肽化合物加载至少量的药物活性肽化合物延长的时期，例如一个月。 本发明的络合物可以研磨或粉碎成细粉末。 以粉末形式，络合物形成稳定的水性悬浮液和分散体，适于注射。 在优选的实施方案中，复合物的肽化合物是LHRH类似物，优选LHRH拮抗剂，载体大分子是阴离子聚合物，优选羧甲基纤维素。 还公开了制备本发明复合物的方法，以及使用含LHRH类似物的复合物治疗可用LHRH类似物治疗的病症的方法。