专利号:WO-2006052263-A1 优先权日:2004-11-10 标题:Synthesis and separation of optically active isomers and cyclopropyl derivatives of spironolactone and their biological action 发明人:RANADE VASANT V; SOMBERG JOHN CHARIN 权利人:RANADE VASANT V 摘要:Methods for separation and synthesis of the optically active 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone are provided. Preferred stereoisomerically purified 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone have fewer effects mediated by gonadal steroid receptors relative to effects mediated by minteralocorticoid progesterone receptors, compared to the stereoisomerically unpurified form of the compound. These optically active compounds can be useful for obtaining reduction in moderate essential hypertension and in the treatment of congestive heart failure in humans with minimized undesirable side effects such as gynecomastia, tender breast enlargement and menstrual irregularities in women, and loss of libido in
专利号:US-2009325918-A1 优先权日:2008-06-16 标 题:Synthesis and separation of optically active isomers and cyclopropyl derivatives of spironolactone and their biological action 发明人:SOMBERG JOHN C; RANADE VASSANT V 权利人:SOMBERG JOHN C; RANADE VASSANT V 摘要:Methods for separation and synthesis of the optically active 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone are provided. Preferred stereoisomerically purified 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone have fewer effects mediated by gonadal steroid receptors relative to effect mediated by minteralocorticoid progesterone receptors, compared to the stereoisomerically unpurified form of the compound. These optically active compounds can be useful for obtaining reduction in moderate essential hypertension and it the treatment of congestive heart failure in humans with minimized undesirable side effects such as gynecomastia, tender breast enlargement and menstrual irregularities in women, and loss of libido in men.
专利号:US-12295961-B2 优先权日:2009-12-31 标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols 发明人:DHINGRA OM 权利人:MARIUS PHARMACEUTICALS INC 摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
专利号:US-2023382819-A1 优先权日:2020-10-14 标 题:Processes for synthesis of alpha-emitting radiopharmaceuticals 发明人:MORSE DAVID L; WADAS THADDEUS J; PANDYA DARPAN; TAFRESHI NARGES; BUDZEVICH MIKALAI 权利人:H LEE MOFFITT CANCER CT & RES; UNIV IOWA RES FOUND 摘要:The present disclosure provides processes for the preparation of alpha emitting radiopharmaceutical compositions, in particular DOTATATE complexes of alpha emitting radionuclides, as well as use of such prepared compositions in the treatment of cancers.
专利号:US-2010247433-A1 优先权日:2005-10-14 标题:Use of non-canonical amino acids as metabolic markers for rapidly-dividing cells 发明人:TIRRELL DAVID; DIETERICH DANIELA C; LINK AARON J; SCHUMAN ERIN 权利人:CALIFORNIA INST OF TECHN 摘要:The invention provides methods, reagents and systems to preferentially mark fast-proliferating cells/tissues (such as cancer), by incorporating non-natural amino acids into proteins, preferably in vivo, using the endogenous protein synthesis machinery of an organism. The incorporated non-natural amino acids contain reactive groups for further chemical reagents, which may serve as a “handleâ€? to for a number of uses, such as imaging of cancer cells, targeting drugs to preferentially kill cancer cells, and proteomic analysis in the context of large scale or high throughput screening for candidate drug leads that affects the proliferation of a target cell, etc.
专利号:US-7282237-B2 优先权日:1999-06-06 标 题:Method for surface modification, a novel support matrix and the use of the matrix 发明人:DERAND HELENE; NASMAN LEGAL REPRESENTATIVE RO; NASMAN LEGAL REPRESENTATIVE HA 权利人:GE HEALTHCARE BIO SCIENCES AB 摘要:A method for hydrophilization and/or surface area enlargement of a porous base matrix comprising on its inner and/or outer surfaces a polymer (P′) carrying nucleophilic groups X′. The method is characterized inn (a) ethoxylating a plurality of said X′ thereby transforming them to groups comprising —(CH 2 CH 2 O) n H, or (b) (i) ethoxylating a polymer (P″) carrying nucleophilic groups X″ thereby transforming P″ to a polyhydroxy polymer (P′″) carrying a plurality of —(CH 2 CH 2 O) n H groups, whereafter (ii) P′″ is attached to the base matrix. n is an integer ≧1. nn A support matrix which is obtainable by the method. The support matrix has a sufficient rigidity and swellability to permit liquid flow of a velocity >5 cm/h through the matrix when in form of particles packed to a bed or in form of a porous monolithic plug. n The use of the support matrix defined in liquid chromatography, cell culturing, stepwise solid phase synthesis of organic molecules, affinity adsorption in suspensions, solid phase catalysis with an immobilized catalyst.
参考文献:10.1186/2042-6410-2-7 摘要:Santos-Galindo M, Acaz-Fonseca E, Bellini MJ, Garcia-Segura LM. Sex differences in the inflammatory response of primary astrocytes to lipopolysaccharide. Biology of Sex Differences. 2011 Jul 11;2(1):7. doi: 10.1186/2042-6410-2-7.