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    • 1. 发明申请
    • LIPOPROTEINS, LIPOPEPTIDES AND ANALOGS, AND METHODS FOR MAKING AND USING THEM
    • 脂蛋白,脂蛋白和类似物,以及制备和使用它们的方法
    • US20100266675A1
    • 2010-10-21
    • US12600930
    • 2008-05-21
    • William GerwickWolfgang WrasidloDennis CarsonDwayne StupackTakashi Suyama
    • William GerwickWolfgang WrasidloDennis CarsonDwayne StupackTakashi Suyama
    • A61K9/127C07K2/00A61K38/00A61P35/00
    • C07C323/60C07C233/47
    • The invention provides novel compositions—lipopeptides and analogs, including somocystinamide A, and somocystinamide A variants and analogs, and pharmaceutical compositions, liposomes and nanoparticles comprising them, and methods of making and using them. In one embodiment, these lipopeptides and analogs are used to induce apoptosis in a cell, which can be a normal cell, a dysfunctional cell and/or a cancer (tumor) cell. In alternative embodiments, the compositions of the invention, including the lipopeptides and analogs of the invention, and the pharmaceutical compositions comprising them, are used to treat or ameliorate (including slowing the progression of) normal, dysfunctional (e.g., abnormally proliferating) and/or tumor associated blood vessels, including endothelial and/or capillary cell growth; including neovasculature related to (within, providing a blood supply to) a tumor.
    • 本发明提供了新颖的组合物 - 脂肽和类似物,包括胞质酰胺A和胞囊酰胺A变体和类似物,以及包含它们的药物组合物,脂质体和纳米颗粒,以及制备和使用它们的方法。 在一个实施方案中,这些脂肽和类似物用于诱导细胞凋亡,细胞可以是正常细胞,功能障碍细胞和/或癌症(肿瘤)细胞。 在替代实施方案中,本发明的组合物,包括本发明的脂肽和类似物以及包含它们的药物组合物用于治疗或改善(包括减缓正常,功能障碍(例如异常增殖)和/ 或肿瘤相关血管,包括内皮细胞和/或毛细胞生长; 包括与肿瘤相关的新血管生成(内部,提供血液供应)。
    • 2. 发明授权
    • Methods for treating or ameliorating a melanoma and killing melanoma cells
    • 用于治疗或改善黑素瘤并杀死黑素瘤细胞的方法
    • US09045401B2
    • 2015-06-02
    • US12600930
    • 2008-05-21
    • William GerwickWolfgang WrasidloDennis CarsonDwayne StupackTakashi Suyama
    • William GerwickWolfgang WrasidloDennis CarsonDwayne StupackTakashi Suyama
    • A61K9/127C07C323/60C07C233/47
    • C07C323/60C07C233/47
    • The invention provides novel compositions—lipopeptides and analogs, including somocystinamide A, and somocystinamide A variants and analogs, and pharmaceutical compositions, liposomes and nanoparticles comprising them, and methods of making and using them. In one embodiment, these lipopeptides and analogs are used to induce apoptosis in a cell, which can be a normal cell, a dysfunctional cell and/or a cancer (tumor) cell. In alternative embodiments, the compositions of the invention, including the lipopeptides and analogs of the invention, and the pharmaceutical compositions comprising them, are used to treat or ameliorate (including slowing the progression of) normal, dysfunctional (e.g., abnormally proliferating) and/or tumor associated blood vessels, including endothelial and/or capillary cell growth; including neovasculature related to (within, providing a blood supply to) a tumor.
    • 本发明提供了新颖的组合物 - 脂肽和类似物,包括胞质酰胺A和胞囊酰胺A变体和类似物,以及包含它们的药物组合物,脂质体和纳米颗粒,以及制备和使用它们的方法。 在一个实施方案中,这些脂肽和类似物用于诱导细胞凋亡,细胞可以是正常细胞,功能障碍细胞和/或癌症(肿瘤)细胞。 在替代实施方案中,本发明的组合物,包括本发明的脂肽和类似物以及包含它们的药物组合物用于治疗或改善(包括减缓正常,功能障碍(例如异常增殖)和/ 或肿瘤相关血管,包括内皮细胞和/或毛细胞生长; 包括与肿瘤相关的新血管生成(内部,提供血液供应)。
    • 7. 发明申请
    • USE OF ETODOLAC TO TREAT HYPERPLASIA
    • US20070299042A1
    • 2007-12-27
    • US11615396
    • 2006-12-22
    • Dennis CarsonLorenzo LeoniMary Corr
    • Dennis CarsonLorenzo LeoniMary Corr
    • A61K31/407A61K31/496A61K31/56A61P35/00
    • A61K31/12A61K31/18A61K31/40A61K31/407A61K31/4745A61K31/496A61K31/50A61K31/56A61K31/675A61K31/7052
    • The present invention provides a therapeutic method to treat non-malignant diseases characterized by the excessive tissue growth, e.g., hyperplastic diseases, comprising administering to a mammal (e.g., human) afflicted with excessive tissue growth, an effective amount of a derivative of an indole compound of formula (I):formula (I): wherein R1 is lower alkyl, (hydroxy)lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, phenyl, benzyl or 2-thienyl; R2, R3, R4 and R5 are the same or different and are each hydrogen or lower alkyl; each R6 is individually hydrogen, lower alkyl, hydroxy, (hydroxy)lower alkyl, lower alkoxy, benzyloxy, lower alkanoyloxy, nitro or halo, R7 is hydrogen, lower alkyl or lower alkenyl, X is oxy and thio, Y is carbonyl, —(CH2)1-3—, —(C1-C3)alkyl(CO)—, or —(CH2)1-3SO2—; Z is hydroxy, lower alkoxy, (C2-C4)acyloxy, —N(R8)(R9), phenylamino, (ω-(4-pyridyl)(C2-C4 alkoxy), (ω-((R8)(R9) amino)(C2-C4 alkoxy), an amino acid ester of (ω-(HO)(C2-C4))alkoxy, —N(R8)CH(R8)CO2H, 1′-D-glucuronyloxy, —SO3H, —PO4H2, —N(NO)(OH), —SO2NH2, —PO(OH)(NH2), —OCH2CH2N(CH3)3+, or tetrazolyl; wherein R8 and R9 are each H, (C1-C3)alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R8), S or nonperoxide O; n is 0, 1, 2, or 3; wherein R8 and R9 are each H, (C1-C3)alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R8), S or nonperoxide O; each alkyl or phenyl group of R1, R2, R3, R4,R5, R6, R7 and Z is optionally substituted with 1, 2, or 3 (C1-C4)alkyl groups; or a pharmaceutically acceptable salt thereof.