专利号:US-7468438-B2 优先权日:2004-03-25 标题:Process for the semisynthesis of deserpidine 发明人:FONTANA GABRIELE; BOMBARDELLI EZIO; SAMORI CRISTIAN; BALDELLI ELEONORA; GUERRINI ANDREA; BATTAGLIA ARTURO; DANIELI BRUNO 权利人:INDENA SPA 摘要:The present invention relates to an efficient procedure for the synthesis of deserpidine (Ia), starting from reserpic acid lactone (II) via the intermediate 11-O-demethyl reserpic acid lactone (III).
专利号:US-2008051323-A1 优先权日:2004-08-21 标 题 :Chloroquine drug compositions and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. n The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
专利号:US-2007060499-A1 优先权日:2005-09-15 标 题 :Chloroquine combination drugs and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
专利号:US-2008039473-A1 优先权日:2006-08-08 标题:Preparation and utility of substituted quinazoline compounds with alpha-adrenergic blocking effects 发明人:GANT THOMAS G; SARSHAR SEPEHR 权利人:AUSPEX PHARMACEUTICALS INC 摘要:The present disclosure is directed to modulators of alpha-adrenergic receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the use of such compounds for the treatment and/or management of hypertension, cardiac failure, prostatitis, and benign prostatic hyperplasia, and any other condition in which it is beneficial to modulate an alpha-adrenergic receptor.
专利号:US-2008107598-A1 优先权日:2006-10-05 标 题:Efficient Synthesis of Chelators for Nuclear Imaging and Radiotherapy: Compositions and Applications
专利号:EP-2079486-A2 优先权日:2006-10-05 标题:Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
1: Wiens B, De Luca V. Molecular and biochemical characterization of a benzenoid/phenylpropanoid meta/para-O-methyltransferase from Rauwolfia serpentina roots. Phytochemistry. 2016 Dec;132:5-15. doi: 10.1016/j.phytochem.2016.10.004. Epub 2016 Oct 19. doi: 10.1159/000438560. Epub 2015 Nov 20. doi: 10.1155/2013/940861. Epub 2013 Dec 5. 4: AbdelHafez EM, Diamanduros A, Negureanu L, Luy Y, Bean JH, Zielke K, Crowe B, Vasilyeva A, Clodfelter JE, Aly OM, Abuo-Rahma GE, Scarpinato KD, Salsbury FR Jr, King SB. Computational and synthetic studies towards improving rescinnamine as an inducer of MSH2-dependent apoptosis in cancer treatment. Mol Cancer Biol. 2013;1(1). pii: 44. 5: Vasilyeva A, Clodfelter JE, Gorczynski MJ, Gerardi AR, King SB, Salsbury F, Scarpinato KD. Parameters of Reserpine Analogs That Induce MSH2/MSH6-Dependent Cytotoxic Response. J Nucleic Acids. 2010 Sep 13;2010. pii: 162018. doi: 10.4061/2010/162018.
合成参考文献
摘要:Toxicology of Drugs and Chemicals, Deichmann, W.B., New York, Academic Press, Inc., 1969, -(517), 1969 摘要:Drugs in Japan, 6(898), 1982 摘要:Budavari, S. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. Whitehouse Station, NJ: Merck and Co., Inc., 1996., p. 1056 摘要:American Hospital Formulary Service. Volumes I and II. Washington, DC: American Society of Hospital Pharmacists, to 1984., p. 24:08 摘要:Schafer, E.W. 1972. The acute oral toxicity of 369 pesticidal, pharmaceutical and other chemicals to wild birds. Toxicology and Applied Pharmacology. 21:315-330. https://www.aphis.usda.gov/ws/nwrc/chem-effects-db/A_Schafer_ToxicolApplPharmacol1972.pdf