Substituted N-benzylindol-3-ylglyoxylic acid derivatives having antitumor action

    公开(公告)号:US06432987B1

    公开(公告)日:2002-08-13

    申请号:US09736431

    申请日:2000-12-15

    IPC分类号: A01N4340

    摘要: The invention relates to novel, substituted N-benzyl-indol-3-ylglyoxylic acid derivatives of the following formula and their use for the treatment of oncoses The invention further relates to their physiologically tolerable acid addition salts and if possible their N-oxides. In addition, the invention relates to pharmaceutical preparations containing at least one of the compounds of the abovementioned formula or their salts or N-oxides with physiologically tolerable inorganic or organic acids and, if appropriate, pharmaceutically utilizable vehicles and/or diluents or excipients and also administration forms of the compounds of the abovementioned formula containing at least one of the compounds of this formula or their salts in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments

    Methods of treatment using novel LHRH antagonists having improved solubility properties
    10.
    发明授权
    Methods of treatment using novel LHRH antagonists having improved solubility properties 有权
    使用具有改善的溶解性的新型LHRH拮抗剂的治疗方法

    公开(公告)号:US07732412B2

    公开(公告)日:2010-06-08

    申请号:US11459583

    申请日:2006-07-24

    IPC分类号: A61K38/00

    CPC分类号: A61K38/10 C07K7/06 C07K7/23

    摘要: The invention relates to peptides which contain N-methylated amino acid units and have improved water solubility. The invention also relates methods for treating a hormone-dependent tumor or a non-malignant indication that is treatable by LH-RH suppression, the method comprising administering to a patient in need of the treatment a therapeutically effective amount of a compound of the invention. Hormone-dependent cancers that can be treated with the methods of the invention include prostate cancer, breast cancer, ovarian cancer, endometrial cancer, and pancreatic cancer. Non-malignant indications which can be treated by the methods of the invention include benign prostate hyperplasia (BPH), endometriosis, acne, polycystic ovarian disease, dysmenorrhea, precocious puberty, and uterine fibroids and other leiomyomas.

    摘要翻译: 本发明涉及含有N-甲基化氨基酸单元并具有改善的水溶性的肽。 本发明还涉及用于治疗激素依赖性肿瘤或可通过LH-RH抑制治疗的非恶性指征的方法,所述方法包括向需要治疗的患者施用治疗有效量的本发明化合物。 可用本发明方法治疗的依赖于激素的癌症包括前列腺癌,乳腺癌,卵巢癌,子宫内膜癌和胰腺癌。 可以通过本发明的方法治疗的非恶性适应症包括良性前列腺增生(BPH),子宫内膜异位症,痤疮,多囊卵巢疾病,痛经,早熟性青春期和子宫肌瘤和其他平滑肌瘤。