164726-80-1 = 83881-52-1 反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Diethyl Ether,Toluene 标题:Method Of Obtaining 2-[2-[4-[(4-Chlorophenyl)Phenylmethyl]-1-Piperazinyl]Ethoxy]Acetic Acid [cetirizine] And Its Dihydrochloride 参考文献:Poland]
= 83881-52-1 [标题:Reaction Conditions 标题:Process For Preparation Of Cetirizine,Its Dihydrochloride,And Optical Isomers Via Hydrolysis And Corresponding Nitriles 参考文献:United Kingdom]
专利号:US-7619085-B2 优先权日:2005-03-03 标 题 :Pyroglutamate salts and their use in the optical resolution of intermediates for the synthesis of dextrocetirizine and levocetirizine 发明人:PALACIO MAGALI; ATES CELAL 权利人:UCB PHARMA SA 摘要:The present invention relates to (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylicacid salt; or (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxycetamide-(R)-pyrrolidone-5-carboxylic salt. The present invention relates also to a process for preparing (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide (I) and (R)-2-[4-(4-chlorobenzhydryl) piperazin-1-yl]-ethoxyacetamide (II) by chemical resolution of a mixture. These compounds are respectively intermediates for the synthesis of dextrocetirizine and levocetirizine.
专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
专利号:US-4894385-A 优先权日:1985-01-16 标 题:Imidazole derivatives as inhibitors of TXA2 synthesis 发明人:KAWAMOTO ISAO; ENDO ROKURO; MATSUDA KEIICHI; USHIYAMA SHIGERU; OSHIMA TAKESHI 权利人:SANKYO CO 摘要:Compounds of formula (I): ##STR1## (wherein n is 0, 1 or 2 and R 1 , R 2 , R 4 , R 5 , R 6 , X, Y and Z are a variety of groups and atoms) have the ability to inhibit the synthesis of thromboxane A 2 and hence are useful in the treatment or prophylaxis of thrombotic conditions.
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-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.
专利号:WO-2022145215-A1 优先权日:2020-12-28 标题:Video selection-synthesis device, control method therefor, and management device 发明人:TAKABAYASHI KAZUHIKO; YAMAGISHI YASUAKI 权利人:SONY GROUP CORP 摘要:The present disclosure relates to a video selection-synthesis device, a control method therefor, and a management device, with which it is possible to appropriately realize a production switcher function. The video selection-synthesis device comprises: a selection unit for making settings based on the format characteristic information of video streams outputted by a plurality of video sources and selecting one or a plurality of videos from among the videos of video streams supplied from each of the plurality of video sources; and a composition unit for composing one video screen using the one or plurality of videos selected by the selection unit. The technology of the present disclosure can be applied, for example, to a content production system, etc., that delivers, taking advantage of a 5G network, content such as a sports or entertainment live performed at an event venue.
1: Preis M, Grother L, Axe P, Breitkreutz J. In-vitro and in-vivo evaluation of taste-masked cetirizine hydrochloride formulated in oral lyophilisates. Int J Pharm. 2015 Aug 1;491(1-2):8-16. doi: 10.1016/j.ijpharm.2015.06.002. Epub 2015 Jun 5. doi: 10.1155/2015/640529. Epub 2015 Feb 25. 3: El-Say KM, El-Helw AR, Ahmed OA, Hosny KM, Ahmed TA, Kharshoum RM, Fahmy UA, Alsawahli M. Statistical optimization of controlled release microspheres containing cetirizine hydrochloride as a model for water soluble drugs. Pharm Dev Technol. 2015;20(6):738-46. doi: 10.3109/10837450.2014.920353. Epub 2014 May 26. doi: 10.1155/2014/808167. Epub 2014 Feb 18. 5: Wildermuth K, Zabel S, Rosychuk RA. The efficacy of cetirizine hydrochloride on the pruritus of cats with atopic dermatitis: a randomized, double-blind, placebo-controlled, crossover study. Vet Dermatol. 2013 Dec;24(6):576-81, e137-8. doi: 10.1111/vde.12067. Epub 2013 Sep 20. doi: 10.1111/j.1365-4632.2010.04708.x.
合成参考文献
摘要:United States Patent Document., #4525358 参考文献:10.2165/00128071-200203010-00007|10.2165/00128071-200203020-00006|10.2165/00128071-200203030-00008|10.2165/00128071-200203040-00007|10.2165/00128071-200203050-00008|10.2165/00128071-200203060-00007|10.2165/00128071-200203070-00009|10.2165/00128071-200203080-00010|10.2165/00128071-200203090-00006 摘要:Cutaneous drug reaction case reports: from the world literature. Am J Clin Dermatol. 2002;3(9):637–43. doi: 10.2165/00128071-200203090-00006. 参考文献:10.1007/s10753-014-9898-x 摘要:Lamraoui A, Adi-Bessalem S, Laraba-Djebari F. Modulation of tissue inflammatory response by histamine receptors in scorpion envenomation pathogenesis: involvement of H4 receptor. Inflammation. 2014 Oct;37(5):1689–704. doi: 10.1007/s10753-014-9898-x. 参考文献:10.2165/00003495-199346060-00008 摘要:Spencer CM, Faulds D, Peters DH. Cetirizine. A reappraisal of its pharmacological properties and therapeutic use in selected allergic disorders. Drugs. 1993 Dec;46(6):1055–80. doi: 10.2165/00003495-199346060-00008.