Halobetasol Propionate Methylene Chloride 反应 0.17H,反应生成 卤贝他索丙酸酯 参考文献:Crystalline Forms Of Halobetasol Propionate 标题:Crystalline Forms Of Halobetasol Propionate 摘要:本发明提供了一种晶体卤倍特索丙酸丙酯,所述卤倍特索丙酸丙酯选自以下组合:具有晶体i型的卤倍特索丙酸丙酯,其特征在于x射线衍射峰位置和强度如本文中的表1所述;具有晶体ii型的卤倍特索丙酸丙酯,其特征在于x射线衍射峰位置和强度如本文中的表2所述;具有晶体iii型的卤倍特索丙酸丙酯,其特征在于x射线衍射峰位置和强度如本文中的表3所述;具有晶体iv型的卤倍特索丙酸丙酯,其特征在于x射线衍射峰位置和强度如本文中的表4所述;具有晶体v型的卤倍特索丙酸丙酯,其特征在于x射线衍射峰位置和强度如本文中的表5所述;以及具有晶体vi型的卤倍特索丙酸丙酯,其特征在于x射线衍射峰位置和强度如本文中的表6所述.
专利号:US-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-2025206736-A1 优先权日:2019-11-14 标题 :Synthesis of kras g12c inhibitor compound 发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN 权利人:AMGEN INC 摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
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-2013035307-A1 优先权日:2010-01-26 标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers 发明人:PRESTWICH GLENN D; KENNEDY THOMAS P 权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P 摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.
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-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.
1: Rivera AM, Hsu S. Topical halobetasol propionate in the treatment of plaque psoriasis: a review. Am J Clin Dermatol. 2005;6(5):311-6. Review.
合成参考文献
参考文献:10.2165/00128071-200203030-00003 摘要:Cather J, Menter A. Novel Therapies for Psoriasis. American Journal of Clinical Dermatology. 2002 Apr;3(3):159–73. doi: 10.2165/00128071-200203030-00003. 参考文献:10.2165/00128071-200203010-00007|10.2165/00128071-200203020-00006|10.2165/00128071-200203030-00008|10.2165/00128071-200203040-00007|10.2165/00128071-200203050-00008|10.2165/00128071-200203060-00007|10.2165/00128071-200203070-00009|10.2165/00128071-200203080-00010|10.2165/00128071-200203090-00006 摘要:Cutaneous drug reaction case reports: from the world literature. Am J Clin Dermatol. 2002;3(9):637–43. doi: 10.2165/00128071-200203090-00006.