专利号:US-8729306-B2 优先权日:2010-02-05 标 题:Process for the preparation of nitrogen substituted aminotetralins derivatives 发明人:VASSELIN DAVID; CARLY NICOLAS; ATES CELAL 权利人:VASSELIN DAVID; CARLY NICOLAS; ATES CELAL; UCB PHARMA GMBH 摘要:The present invention provides an alternative synthesis of N-substituted aminotetralines which synthesis comprises catalytic asymmetric hydrogenation of compounds of general formula (A).
专利号:US-8981121-B2 优先权日:2010-06-25 标 题 :Process for the preparation of nitrogen substituted aminotetralins derivatives 发明人:ATES CELAL; SCHULE ARNAUD; PALACIO MAGALI; DEUTSCH PAUL; VASSELIN DAVID; CARLY NICOLAS; PHADTARE GANESH; YERANDE SWAPNIL; DELATINNE JEAN-PIERRE; ESCUDERO HERNANDEZ MARIA LUISA; PINILLA VERONIQUE 权利人:ATES CELAL; SCHULE ARNAUD; PALACIO MAGALI; DEUTSCH PAUL; VASSELIN DAVID; CARLY NICOLAS; PHADTARE GANESH; YERANDE SWAPNIL; DELATINNE JEAN-PIERRE; ESCUDERO HERNANDEZ MARIA LUISA; PINILLA VERONIQUE; UCB PHARMA GMBH 摘要:The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R 1 , R 2 and R 3 are as defined for compound of formula (I).
专利号:US-10022366-B2 优先权日:2013-04-23 标 题:Extending and maintaining micropore viability of microneedle treated skin with lipid biosynthesis inhibitors for sustained drug delivery 发明人:STINCHCOMB AUDRA L; GHOSH PRIYANKA 权利人:STINCHCOMB AUDRA L; GHOSH PRIYANKA; UNIV MARYLAND; UNIV KENTUCKY RES FOUND 摘要:Microneedles and their use as a physical skin permeation enhancement technique facilitate drug delivery across the skin in therapeutically relevant concentrations. Micropores created in the skin by MNs reseal because of normal healing processes of the skin, thus limiting the duration of the drug delivery window. Pore lifetime enhancement strategies can increase effectiveness of MNs as a drug delivery mechanism by prolonging the delivery window. Fluvastatin (FLU) was used to enhance pore lifetime by inhibiting the synthesis of cholesterol, a major component of the stratum corneum lipids. The skin recovered within a 30-45-min time period following the removal of occlusion, and there was no significant irritation observed due to the treatment compared to the control sites. Thus, it can be concluded that localized skin treatment with FLU can be used to extend micropore lifetime and deliver drugs for up to 7 days across MN-treated skin.
专利号:WO-2011146610-A3 优先权日:2010-05-19 标题 :An enantioselective synthesis of chiral amines for the production of rotigotine 发明人:COBLEY CHRISTOPHER JAMES; FANJUL SOLARES TAMARA 权利人:REDDYS LAB LTD DR; REDDYS LAB INC DR; COBLEY CHRISTOPHER JAMES; FANJUL SOLARES TAMARA 摘要:Methods of preparing (S)-N-(1,2,3,4-tetrahydronaphthalen-2-yl)propion amide compounds 4 from N-(3,4-dihydronaphthalen-2-yl)propionamide compounds 3: where the constituent variables are as defined.
专利号:US-7309799-B2 优先权日:2004-06-01 标 题:Methods for the synthesis of milnacipran and congeners thereof 发明人:BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V 权利人:COLLEGIUM PHARMACEUTICAL INC 摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.
专利号:US-12201669-B2 优先权日:2021-03-11 标 题:Small molecule suppressors of APOE gene expression and cerebral vascular amyloid pathology 发明人:TSAI LI-HUEI; BLANCHARD JOEL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present disclosure provides methods of inhibiting amyloid synthesis in a subject using small molecule inhibitors. The invention also includes methods of treating disease associated with amyloid synthesis, such as Alzheimer's disease. The small molecule inhibitors disclosed herein are compounds which are non-immunosuppressant cyclosporin including the pharmaceutically acceptable salts thereof.
1. Wood, M., Dubois, V., Scheller, D., et al. Rotigotine is a potent agonist at dopamine D1 receptors as well as at dopamine D2 and D3 receptors. Br. J. Pharmacol. 172(4), 1124-1135 (2015).
合成参考文献
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