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-8926955-B2 优先权日:2008-12-22 标题 :Synthesis of polymer conjugates of indolocarbazole compounds 发明人:BAGNOD RAFFAELLA; BECCARIA LUCA; BERTARIONE RAVA ROSSA LUISA; CRISCUOLO DOMENICO; LORENZETTO CHIARA; MAINERO VALENTINA; MARCONI ALESSANDRA; PINCELLI CARLO; TRAVERSA SILVIO 权利人:BAGNOD RAFFAELLA; BECCARIA LUCA; BERTARIONE RAVA ROSSA LUISA; CRISCUOLO DOMENICO; LORENZETTO CHIARA; MAINERO VALENTINA; MARCONI ALESSANDRA; PINCELLI CARLO; TRAVERSA SILVIO; CREABILIS S A 摘要:The present invention relates to a process for the preparation of polymer conjugates of indolocarbaxole compounds, in particular of polymer conjugates of K-252a and derivatives thereof, by a synthetic route which results in a highly pure product, with a high product yield. In a further aspect the present invention relates to novel polymer conjugates of K-252a and derivatives thereof, wherein the chemical group linking the polymer unity to the K-252a or to the K-252a derivative compound is characterized by a 5-member oxazolidindionic cyclic structure. These novel polymer conjugates are obtained through the novel synthetic route with high purity and high yields.
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:WO-2024232849-A1 优先权日:2023-05-10 标 题:A pharmaceutical composition for increasing melanin synthesis in hair follicles 发明人:BALKAN GURSES NAZ DICLE; TULUNAY MAHIR 权利人:IFL PHARMA ILAC SANAYI VE TICARET ANONIM SIRKETI 摘要:The present invention relates to a pharmaceutical composition that is developed to convert white body hair, particularly hair, back to its original color. Particularly, the invention relates to a composition that works based on the increasing mechanism of melanin synthesis by regulating melanocyte cells. The pharmaceutical composition of the present invention is applied to the scalp via an intradermal method.