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    Treatment of mammals afflicted with tumors with compounds having RXR retinoid receptor agonist activity
    108.
    发明授权
    Treatment of mammals afflicted with tumors with compounds having RXR retinoid receptor agonist activity 失效
    用具有RXR类视黄醇受体激动剂活性的化合物治疗患有肿瘤的哺乳动物

    公开(公告)号：US5399586A

    公开(公告)日：1995-03-21

    申请号：US29801

    申请日：1993-03-11

    申请人： Peter A. J. Davies ,  Roshantha A. Chandraratna

    发明人： Peter A. J. Davies ,  Roshantha A. Chandraratna

    IPC分类号： C07D333/08 ,  A61K31/00 ,  A61K31/192 ,  A61K31/38 ,  A61K31/381 ,  A61K45/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D333/10 ,  C07D333/16 ,  C07D333/24 ,  C07D333/38 ,  C07D333/40 ,  A61K31/19

    CPC分类号： A61K31/381 ,  A61K31/00 ,  A61K31/192 ,  A61K31/38

    摘要： Retinoid-like compounds which act as agonists of the RXR retinoid receptor sites induce apoptosis of tumor cells in cell cultures, and are used as drugs to treat tumors in mammals including humans. Compounds which are specific agonists of RXR receptors and also compounds which are agonists of both RAR and RXR agonist (pan-agonists) induce apoptosis, although the RXR agonist compounds are preferred as drugs to avoid undesirable side effects associated with RAR agonist activity. The RXR agonists compounds are administered to mammals afflicted with tumors in pharmaceutical compositions adapted for systemic topical or for intralesional administration. The range of concentration of the active ingredient RXR agonist compound in the pharmaceutical compositions is approximately between 0.001 and 5 percent by weight, and such that the composition delivers approximately 0.1 mg to 100 mg of the active ingredient per kg body weight of the patient, per day of treatment.

    摘要翻译： 作为RXR类视黄醇受体位点的激动剂的维甲酸样化合物诱导细胞培养物中肿瘤细胞的凋亡，并且用作治疗包括人在内的哺乳动物肿瘤的药物。 作为RXR受体的特异性激动剂的化合物以及作为RAR和RXR激动剂（泛激动剂）的激动剂的化合物诱导凋亡，尽管RXR激动剂化合物优选作为药物以避免与RAR激动剂活性相关的不期望的副作用。 将RXR激动剂化合物施用于适用于全身性局部或用于病灶内施用的药物组合物中的肿瘤。 药物组合物中活性成分RXR激动剂化合物的浓度范围约为0.001至5重量％，并且使得组合物每千克体重的患者每次递送约0.1毫克至100mg的活性成分 治疗日。