专利号:US-10413555-B2 优先权日:2014-11-25 标题:Treatment of skin atrophy with a combination of triiodothyroacetic acid (TRIAC) and dehydroepiandrosterone (DHEA) 发明人:FAERGEMANN JAN; JOHANNSSON GUDMUNDUR; OHLSSON CLAES; BATCHELLER DEREK GREGORY; JOHNSSON JÖRGEN; TÖRNELL JAN 权利人:TROPHEA DEV AB 摘要:The aim of the present study was to investigate the effect of a combination of triiodothyroacetic acid (TRIAC) and dehydroepiandrosterone (DHEA) compared with TRIAC, DHEA or placebo alone on corticosteroid induced effect on collagen synthesis in humans. Six healthy male human volunteers aged 40-65 participated. Four areas of abdominal skin were pre-treated for 3 weeks with betamethasone valerate cream. The same areas were then treated with one of the following alternatives in the same cream vehicle: TRIAC, DHEA, TRIAC+DHEA and placebo for 2 weeks. Then suction blisters were raised in each of these areas with a vacuum pump. The blister fluid from each area was collected and frozen until analysis. Analysis of amino terminal propeptide of human type I procollagen (PINP) in suction blister fluid was performed using a commercially available immunoassay (Orion Diagnostics) kit. This study has for the first time shown that a combination of TRIAC and DHEA could effectively stimulate collagen synthesis in skin pretreated with betamethasone valerate demonstrated by an increase in PINP, and that the combination was more effective than TRIAC or DHEA alone. This combination could be used to effectively treat skin atrophy in corticosteroid induced skin atrophy. It could also be used to treat skin atrophy due to other circumstances such as e. g. sun damaged skin and skin atrophy due to high age. Another interesting application would be to combine TRIAC and DHEA with a potent corticosteroid in order to prevent corticosteroid induced skin atrophy. If this combination still is effective in the treatment of eczema and psoriasis and without the risk of skin atrophy this combination will be a major breakthrough for the use of potent topical corticosteroids.
专利号:US-11186551-B2 优先权日:2020-04-29 标题 :Composition of scalable thyrointegrin antagonists with improved retention in tumors 发明人:MOUSA SHAKER A; HAY BRUCE A 权利人:NANOPHARMACEUTICALS LLC 摘要:Chemical compounds/compositions, methods of synthesis, and methods of use. The compounds/compositions are directed toward thyrointegrin antagonists conjugated to a polymer. The compounds/compositions further comprise an additional substituent also conjugated to the polymer. The compounds/compositions demonstrate increased uptake across the blood brain barrier along with increased retention therein and retention within tumor. The compounds/compositions may also include improved synthesis scalability, improved purity, improved aqueous solubility, and a solid product or intermediate. The compounds/compositions may demonstrate improved antiangiogenic effect and improved efficacy against conditions, particularly cancers, requiring blood brain barrier permeability, for example, glioblastoma (GBM).
专利号:WO-2022260918-A1 优先权日:2021-06-07 标 题:Composition and method for dual targeting in treatment of neuroendocrine tumors 发明人:MOUSA SHAKER; RAJABI MEHDI; KARAKUS OZLEM O 权利人:NANOPHARMACEUTICALS LLC 摘要:Chemical compositions and methods of synthesis thereof. The compositions disclosed and described herein are directed toward thyroid hormone ανβ3 integrin receptor antagonists conjugated to targets of the norepinephrine transporter (NET) or the catecholamine transporter. The compositions have a dual targeting effect and increased targeting efficiency in the treatment and diagnostic imaging of neuroendocrine tumors.
专利号:US-11077082-B2 优先权日:2018-04-11 标题 :Composition and method for dual targeting in treatment of neuroendocrine tumors 发明人:MOUSA SHAKER; RAJABI MEHDI; KARAKUS OZLEM O 权利人:NANOPHARMACEUTICALS LLC 摘要:Chemical compositions and methods of synthesis thereof. The compositions disclosed and described herein are directed toward thyroid hormone αvβ3 integrin receptor antagonists conjugated to targets of the norepinephrine transporter (NET) or the catecholamine transporter. The compositions have a dual targeting effect and increased targeting efficiency in the treatment and diagnostic imaging of neuroendocrine tumors.
专利号:JP-2021505618-A 优先权日:2017-12-06 标题:Solid-phase synthesis of NIR fluorescent probe
专利号:US-11351137-B2 优先权日:2018-04-11 标题 :Composition and method for dual targeting in treatment of neuroendocrine tumors 发明人:MOUSA SHAKER; RAJABI MEHDI; KARAKUS OZLEM O 权利人:NANOPHARMACEUTICALS LLC 摘要:Chemical compositions and methods of synthesis thereof. The compositions disclosed and described herein are directed toward thyroid hormone αvβ3 integrin receptor antagonists conjugated to targets of the norepinephrine transporter (NET) or the catecholamine transporter. The compositions have a dual targeting effect and increased targeting efficiency in the treatment and diagnostic imaging of neuroendocrine tumors.
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合成参考文献
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