专利号:US-2006030625-A1 优先权日:2004-08-06 标 题 :Dietary neurotransmitter precursors for balanced synthesis of neurotransmitters 发明人:HART CHERYLE RAM; GROSSMAN RONALD S; RAM HERBERT 权利人:HART CHERYLE RAM; GROSSMAN RONALD S; RAM HERBERT 摘要:Dietary supplements for treating a neurotransmitter deficiency include one or more precursors of the deficient neurotransmitter and a cofactor for activating in vivo enzymatic synthesis of the deficient neurotransmitter. The dietary supplements can also include an appropriate neurotransmitter, such as an amino acid. When administered through the oral mucosa, increases in levels of the deficient neurotransmitters and relief from deficiency symptoms are obtained.
专利号:US-6777554-B2 优先权日:2001-02-05 标题 :Preparation of N-methylparoxetine and related intermediate compounds 发明人:FINKELSTEIN NINA 权利人:TEVA PHARMA 摘要:The present invention provides a process for preparing N-methylparoxetine, an intermediate in the synthesis of paroxetine, by reacting sesamol-tetrabutylammonium salt with CIPMA. The present invention is not limited to the synthesis of N-methylparoxetine, but also includes other similar compounds.
专利号:US-8569265-B2 优先权日:2011-05-06 标题:Deuterated analogs of (4S)-4-ethyl-4-hydroxy-11-[2- (trimethylsilyl)ethyl]-1H-pyrano[3′, 4′:6,7] indolizino [1,2-b]quinoline-3,14(4H, 12H)-dione and methods of use thereof 发明人:CHEN XINGHAI; HUANG QIULI; KOCHAT HARRY; MALAKHOV ANDREY; HAUSHEER FREDERICK H 权利人:CHEN XINGHAI; HUANG QIULI; KOCHAT HARRY; MALAKHOV ANDREY; HAUSHEER FREDERICK H; BIONUMERIK PHARMACEUTICALS INC 摘要:The present invention discloses: (i) two novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (ii) methods of synthesis of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (iii) pharmaceutically-acceptable formulations comprising said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents; and (iv) methods of administration of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof.
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-2011040105-A1 优先权日:2008-04-16 标题 :Processes useful for the synthesis of (r)-1--2-methyl-pyrrolidine 发明人:HUBER CHRISTIAN H; KHULMAN YOUNG MI; TANDEL SAGUN K; JOHANNSEN STEPHEN R; WANG TINGMIN; ANGELL PAUL 权利人:ARENA PHARM INC 摘要:Processes useful for making a pharmaceutically useful compound according to Formula (I), forms of such a compound, and intermediates useful in such processes are described.
专利号:US-7807837-B2 优先权日:2004-05-07 标 题 :Scalable synthesis of imidazole derivatives 发明人:JONES TODD K; MANI NEELAKANDHA 权利人:JANSSEN PHARMACEUTICA NV 摘要:Imidazole derivatives, compositions containing them, methods of preparing them, including regioselective scale-up synthetic methods, and methods of using them.
1: Tong WQ, Lach JL, Chin TF, Guillory JK. Structural effects on the binding of amine drugs with the diphenylmethyl functionality to cyclodextrins. I. A microcalorimetric study. Pharm Res. 1991 Jul;8(7):951-7.
合成参考文献
摘要:Journal of Pharmacology and Experimental Therapeutics., 82(23), 1944 摘要:Journal of Pharmacology and Experimental Therapeutics., 59(365), 1937 摘要:Acta Poloniae Pharmaceutica. For English translation, see APPFAR., 33(145), 1976 [] 摘要:Archives Internationales de Pharmacodynamie et de Therapie., 59(149), 1938