Novel Sphingosine 1-Phosphate Receptor Antagonists
    65.
    发明申请
    Novel Sphingosine 1-Phosphate Receptor Antagonists 有权
    新型鞘氨醇1-磷酸受体拮抗剂

    公开(公告)号:US20150045332A1

    公开(公告)日:2015-02-12

    申请号:US14386990

    申请日:2013-03-21

    申请人: Rolf E. SWENSON

    发明人: Rolf E. Swenson

    摘要: The present invention relates to sphingosine-1-phosphate (S1P) receptors and compounds of the general formula: that are useful in the treatment and prevention of conditions associated with such receptors. More specifically, the present invention relates to the synthesis and use of sphingosine 1-phosphate receptor 2 (S1P2) antagonists that are useful in the treatment of cancer, atherosclerosis, diabetic retinopathy, and other inflammatory diseases. Among these inflammatory diseases that could be treated with these S1P2 antagonist are those characterized by fibrosis including chronic lung disease, chronic kidney and liver disease, chronic heart disease, and skin diseases such as sclerosis/scleroderma. The S1P2 antagonists can also be used in the treatment of glioblastoma multiforme (brain cancer), pediatric neuroblastoma, and other cancers.

    摘要翻译: 本发明涉及鞘氨醇-1-磷酸(S1P)受体和通式的化合物:其可用于治疗和预防与此类受体相关的病症。 更具体地说,本发明涉及可用于治疗癌症,动脉粥样硬化,糖尿病性视网膜病和其它炎性疾病的鞘氨醇1-磷酸受体2(S1P2)拮抗剂的合成和用途。 可以用这些S1P2拮抗剂治疗的这些炎性疾病中的那些是以纤维化为特征的,包括慢性肺部疾病,慢性肾脏和肝脏疾病,慢性心脏病和皮肤疾病如硬化症/硬皮病。 S1P2拮抗剂也可用于治疗多形性成胶质细胞瘤(脑癌),儿科神经母细胞瘤等癌症。

    Targeting and therapeutic compounds and gas-filled microvesicles comprising said compounds
    67.
    发明授权
    Targeting and therapeutic compounds and gas-filled microvesicles comprising said compounds 有权
    靶向和治疗化合物和包含所述化合物的充气微泡

    公开(公告)号:US08293214B2

    公开(公告)日:2012-10-23

    申请号:US12448401

    申请日:2007-12-19

    IPC分类号: A61B8/00 A61K38/00

    CPC分类号: A61K49/223

    摘要: New targeting or therapeutic compounds which can be incorporated into a composition of gas-filled microvesicles. The invention further relates to gas-filled microvesicles for diagnostic and/or therapeutic use comprising said compounds and to their method of use. The new compounds are compounds of formula M-S-T, wherein: M represents a component capable of associating with an envelope of a gas-filled microvesicle; T represents a component comprising a targeting ligand or a therapeutic agent; and S represents a component comprising at least two bissulfone groups.

    摘要翻译: 可以掺入气体填充微泡组合物中的新靶向或治疗化合物。 本发明还涉及用于诊断和/或治疗用途的充气微泡,其包含所述化合物及其使用方法。 新化合物是式M-S-T的化合物,其中:M表示能与气体填充的微泡的包膜缔合的成分; T表示包含靶向配体或治疗剂的组分; S表示包含至少两个双砜基团的组分。