专利号:WO-2022226312-A1 优先权日:2021-04-22 标 题:Combination nucleotide pool depletion for treatment of viral infections and cancers 发明人:KUMAR VIKRAM; HESSON DAVID; DEMAREST JAMES 权利人:CLEAR CREEK BIO INC 摘要:The invention provides methods of treating cancers and viral infections by providing a combination of agents that inhibit both nucleotide synthesis and nucleotide salvage in the cells of a subject to prevent cancer proliferation and viral replication. The invention provides methods of depleting nucleotide pools by using both inhibitors of dihydroorotate dehydrogenase (DHODH), such as brequinar, which block synthesis of pyrimidine-based nucleotides, in combination of one or more nucleotide salvage inhibitors, for example deoxycytidine kinase (dCK) inhibitors, Equilibrative nucleoside transporter (ENT) inhibitors, and Uridine-cytidine kinase (UCK) inhibitors, which inhibit salvage of purine and/or pyrimidine-based nucleotides or nucleosides
专利号:US-9051302-B2 优先权日:2008-01-15 标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents 发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN 权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG 摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.
专利号:US-11850220-B2 优先权日:2020-05-19 标题 :Synthesis of ibuprofen hybrid conjugates as anti-inflammatory and analgesic agents 发明人:PANDA SIVA 权利人:UNIV RES INST INC AUGUSTA 摘要:Disclosed herein as ibuprofen hybrid conjugates and methods of their use to reduce inflammation, pain, and fever. The ibuprofen conjugates have potent anti-inflammatory and analgesic properties with low potential for ulcerogenic activity. An exemplary compound is an ibuprofen-amino acid-4-aminophenol hybrid. Also disclosed are methods of treating or reducing inflammation, pain, and fever in a subject.
专利号:US-2013261317-A1 优先权日:2010-09-27 标题 :Methods for preparing synthetic bile acids and compositions comprising the same 发明人:MORIARTY ROBERT M; RAO PHOTON 权利人:MORIARTY ROBERT M; RAO PHOTON; KYTHERA BIOPHARMACEUTICALS INC 摘要:This invention relates generally to methods for preparing certain bile acids from non-mammalian sourced starting materials as well as to synthetic bile acids and compositions comprising such acids wherein the acids are characterized by a different C 14 population than naturally occurring bile acids as well as being free from any mammalian pathogens. This invention is also directed to the synthesis of intermediates useful in the synthesis of such bile acids. Accordingly, the C ring of the steroidal scaffold is oxidized to provide a synthetic route and intermediates to DCA. This invention also provides synthetic methods for preparing deoxycholic acid or a salt thereof starting from aromatic steroids such as estrogen, equilenin, and derivatives thereof. This invention is also directed to intermediates such as 12-oxo or delta-9,11-ene steroids as well as novel processes for their preparation. In preferred embodiments, bile acids are provided herein which have substituents on the B-ring and/or D-ring side chain and optionally on the hydroxy group of the A-ring.
专利号:WO-9709067-A1 优先权日:1995-09-05 标 题 :Combination of 5-lipoxygenase and leukotriene synthesis inhibitors with glucocorticosteroids 发明人:BURCHARDT ELMAR-REINHOLD; MUELLER-PEDDINGHAUS REINER 权利人:BAYER AG; BURCHARDT ELMAR REINHOLD; MUELLER PEDDINGHAUS REINER 摘要:The combination is disclosed of 5-lipoxygenase inhibitors as direct action lipoxygenase inhibitors (LOI) or of leukotriene synthesis inhibitors (LSI) with glucocorticosteroids (GCS). This combination is suitable for treating and preventing various acute and chronic inflammatory processes, in particular of the respiratory tract, and may therefore be used as a medicament, in particular for treating asthma.
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.
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合成参考文献
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