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-11617758-B2 优先权日:2009-12-31 标 题 :Emulsion formulations 发明人:DHINGRA OM; BERNSTEIN JAMES S 权利人:MARIUS PHARMACEUTICALS LLC 摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic 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-2013303495-A1 优先权日:2009-12-31 标题:Emulsion formulations 发明人:DHINGRA OM; BERNSTEIN JAMES S 权利人:SOV THERAPEUTICS; DIFFERENTIAL DRUG DEV ASSOCIATES LLC 摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic 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-2010256229-A1 优先权日:2009-04-02 标题:Compositions of cholinesterase inhibitors 发明人:DU SHOUCHENG; ANDERSEN MARC W; COUGHLIN DANIEL; KOLCHINSKI ALEXANDER 权利人:COLUCID PHARMACEUTICALS INC 摘要:The present invention is directed to compositions, methods of use, and processes for the synthesis related to 3-((S)-1-(dimethylamino)ethyl)phenyl methyl-((R)-1-phenylpropan-2 yl)carbamate, and its pharmaceutically acceptable salt forms, including the hydrogen fumarate salt. The present invention also relates to a novel form polymorph of 3-((S)-1-(dimethylamino)ethyl)phenylmethyl-((R)-1-phenylpropan-2 yl)carbamate, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.
专利号:EP-3103803-B1 优先权日:2008-10-27 标 题 :Intermediates for the synthesis of mtor kinase inhibitors
专利号:US-9751877-B2 优先权日:2012-09-21 标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders 发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
1: Kaur K, Malik AK. Study on the fluorescence quenching reaction of amitriptyline and clomipramine hydrochlorides with eosin Y and its analytical application. J Fluoresc. 2013 May;23(3):533-42. doi: 10.1007/s10895-013-1185-y. Epub 2013 Mar 3. doi: 10.1016/j.aca.2013.12.021. Epub 2013 Dec 26. German. Turkish.
合成参考文献
摘要:Drugs in Japan, 6(243), 1982 摘要:Journal of Analytical Toxicology., 22(612), 1998 [] 参考文献:10.1007/s00213-012-2938-z 摘要:Schepisi C, De Carolis L, Nencini P. Effects of the 5HT2C antagonist SB242084 on the pramipexole-induced potentiation of water contrafreeloading, a putative animal model of compulsive behavior. Psychopharmacology (Berl). 2013 May;227(1):55–66. doi: 10.1007/s00213-012-2938-z. 参考文献:10.1007/bf02280765 摘要:Molinaro M, Villani P, Regazzi MB, Rondanelli R, Doveri G. Pharmacokinetics of ofloxacin in elderly patients and in healthy young subjects. European Journal of Clinical Pharmacology. 1992 Jul;43(1):105–7. doi: 10.1007/bf02280765.