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    • 94. 发明授权
    • Adamantanamines and neramexane salts of thiomolybdic and thiotungstic acids
    • 硫代钼酸和硫代酸的金刚烷胺和奈拉美辛盐
    • US07893289B2
    • 2011-02-22
    • US11992991
    • 2008-02-21
    • Om P. Goel
    • Om P. Goel
    • C07F11/00A61K31/28
    • C07C211/63C07C2601/14C07C2603/74
    • This invention concerns adamantanamines (e.g. memantine, amantadine, and rimantadine) and neramexane salts of thiomolybdic and thiotungstic acids, including their preparation and pharmaceutical compositions, as dual acting drugs. These salts are used to treat or potentially arrest the neurodegenerative pathophysiology, clinical signs and symptoms of dementia of the Alzheimer's type, Parkinson's, Huntington's, AIDS-related dementia and Schizophrenia and its cognitive deficits. Additional uses of these derivatives include antiviral activity. The novel compositions of the present invention appear particularly useful in enhancing the therapeutic benefits of copper-sequestering tetrathiomolybdates in treating elevated copper-induced toxicities in neurologically presenting Wilson's disease, and in treating diseases of the inflammatory etiology and abnormal copper biochemistry, such as tumor angiogenesis, liver cirrhosis, hepatitis, pulmonary fibrosis and other fibrotic diseases, cardiovascular disease, cerebral ischemia, renal anemia, rheumatoid arthritis, diabetes, obesity, gastrointestinal disorders, and eye diseases such as glaucoma, proliferative diabetic retinopathy, and age related macular degeneration. These compounds have excellent stability and aqueous solubility for good oral bioavailability.
    • 本发明涉及硫代钼酸和硫代酸的金刚烷胺(例如美金刚,金刚烷胺和金刚乙胺)和奈拉美生盐,包括它们的制备和药物组合物,作为双作用药物。 这些盐用于治疗或潜在地阻止阿尔茨海默氏症,帕金森氏症,亨廷顿舞蹈症,艾滋病相关性痴呆和精神分裂症及其认知缺陷的神经变性病理生理学,临床症状和痴呆症状。 这些衍生物的其它用途包括抗病毒活性。 本发明的新型组合物特别可用于增强铜螯合四硫钼酸盐在治疗神经性呈现威尔逊氏症中升高的铜诱导毒性以及治疗炎性病因学和异常铜生物化学疾病如肿瘤血管生成中的治疗益处 ,肝硬化,肝炎,肺纤维化等纤维化疾病,心血管疾病,脑缺血,肾性贫血,类风湿性关节炎,糖尿病,肥胖症,胃肠道疾病和眼部疾病如青光眼,增殖性糖尿病性视网膜病变和年龄相关性黄斑变性。 这些化合物具有优异的稳定性和水溶性,以获得良好的口服生物利用度。
    • 97. 发明申请
    • TREATMENT OF SKIN DAMAGE
    • 治疗皮肤损伤
    • US20100267825A1
    • 2010-10-21
    • US12759970
    • 2010-04-14
    • Bernard Malfroy-Camine
    • Bernard Malfroy-Camine
    • A61K31/28C12Q1/02C12M1/34A61P17/00
    • A61K31/28G01N33/5091G01N2800/20G01N2800/40
    • Methods and apparatus are disclosed for diagnosing and treating oxidative skin damage in a subject. The therapeutic method can comprise: (i) diagnosing a level of oxidative skin damage in a sample comprising stratum corneum of the subject; and (ii) recommending a therapeutic regime for treatment of oxidative skin damage in the subject, wherein said recommendation comprises a recommendation to administer a pharmaceutical formulation comprising an amount of one or more specific synthetic SOD/catalase mimetics sufficient to treat the level of oxidative skin damage of the subject as diagnosed. The diagnostic method can further include obtaining a sample from the stratum corneum of a subject; measuring the level of at least one oxidized substance in the sample; and comparing a detected level of the oxidized substance with a standard, whereby an elevated level of the oxidized substance is indicative of skin damage.
    • 公开了用于诊断和治疗受试者的氧化性皮肤损伤的方法和装置。 治疗方法可以包括:(i)诊断包含受试者的角质层的样品中的氧化皮肤损伤水平; 和(ii)建议用于治疗受试者的氧化性皮肤损伤的治疗方案,其中所述建议包括施用药物制剂的建议,其包含一定量的足以治疗氧化皮肤水平的一种或多种特异性合成SOD /过氧化氢酶模拟物 被诊断的受试者的损伤。 诊断方法还可以包括从受试者的角质层获得样品; 测量样品中至少一种氧化物质的含量; 并将氧化物质的检测水平与标准物进行比较,由此升高的氧化物质水平表示皮肤损伤。
    • 100. 发明授权
    • Pharmaceutical composition for oral administration
    • 用于口服给药的药物组合物
    • US07767709B2
    • 2010-08-03
    • US12305337
    • 2007-06-20
    • Ales FrancPetr Sova
    • Ales FrancPetr Sova
    • A61K31/28
    • A61K47/14A61K9/10A61K9/4858A61K31/282A61K33/24
    • An oral pharmaceutical composition characterized in that it consists of a suspension of a platinum complex of general formula I, wherein A and A′ independently of one another are an NH3 group or an amino or diamino group containing 1 to 18 carbon atoms, B and B′ independently of one another are a halogen atom or a hydroxy group or are an —O—C(O)—R or an —O—C(O)—R′ group wherein R and R′ independently of one another are hydrogen atom, an alkyl, alkenyl, aryl, aralkyl, alkylamino or alkoxy group which groups contain 1 to 10 carbon atoms, or functional derivatives of these groups, X and X′ independently of one another are a halogen atom or a monocarboxylate group containing 1 to 20 carbon atoms, or X and X′ together form a dicarboxylate group containing 2 to 20 carbon atoms, in at least one pharmaceutically acceptable vegetable, animal, mineral, synthetic or semisynthetic oil and/or in at least one pharmaceutically acceptable vegetable, animal, mineral, synthetic or semisynthetic oily substance, in which suspension the content of the platinum complex of general formula I is 0.5 to 50% by weight based on the total weight of the composition, and which suspension optionally contains at least one pharmaceutically acceptable excipient.
    • 一种口服药物组合物,其特征在于其由通式I的铂络合物的悬浮液组成,其中A和A'彼此独立地为NH 3基团或含有1至18个碳原子的氨基或二氨基,B和B “彼此独立的是卤素原子或羟基,或者是-O-C(O)-R或-O-C(O)-R'基团,其中R和R'彼此独立地是氢原子 ,含有1〜10个碳原子的烷基,烯基,芳基,芳烷基,烷基氨基或烷氧基,或这些基团的官能衍生物,X和X'彼此独立地是卤素原子或含有1至20个碳原子的单羧酸盐基团 碳原子或X和X'在至少一种药学上可接受的植物,动物,矿物,合成或半合成油和/或至少一种药学上可接受的植物,动物,矿物质中一起形成含有2至20个碳原子的二羧酸酯基 ,合成o r半合成油状物质,其中通式I的铂络合物的含量相对于组合物的总重量为0.5〜50重量%,该悬浮液任选地含有至少一种药学上可接受的赋形剂。