专利号:WO-2025136243-A1 优先权日:2023-12-20 标题:Mechanochemical synthesis of histamine h1-receptor antagonists 发明人:AYDONAT SIMAY; OZEL MERTCAN; YIGITBASI JOANNA MARIANNA; BAYTEKIN BILGE; COLACINO EVELINA 权利人:IHSAN DOGRAMACI BILKENT UNIV; CENTRE NAT RECH SCIENT 摘要:The present invention relates to mechanochemical synthesis of histamine antagonists which are benzhydryl ethers and unsymmetrically disubstitutes piperazines and salts thereof. Said antihistamine active pharmaceutical ingredients can be diphenhydramine hydrochloride, cyclizine hydrochloride and diphenylpyraline hydrochloride. These antihistamines are used in the treatment of allergies, hives, hay fever (allergic rhinitis), conjunctivitis, reactions to insect bites and sings, nausea, motion sickness, insomnia.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-6852855-B2 优先权日:1999-04-19 标 题 :Synthesis of piperazine ring 发明人:DOLITZKY BEN-ZION 权利人:TEVA PHARMA 摘要:A novel process for preparing a compound of the formula I: n n nwhereinn nR 1 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy; R 2 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy, arylalkoxy, tosyl, formyl, acetyl or amine; and R 3 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy is disclosed. These compounds are useful in the synthesis of the antidepressant mirtazapine and other tetracyclic compounds.
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-9765027-B2 优先权日:2014-08-22 标题 :Substituted 1-arylethyl-4-acylaminopiperidine derivatives as opioid/alpha-adrenoreceptor modulators and method of their preparation 发明人:VARDANYAN RUBEN S; HRUBY VICTOR J 权利人:THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZAONA; UNIV ARIZONA 摘要:The invention provides compounds that bind with high affinities to the μ-, δ- and κ-opioid receptors and α 2 -adrenoreceptor. In addition to providing these compounds with novel pharmacological binding properties, the invention also describes detailed novel methods for the preparation of representative compounds and a scheme for the synthesis of related compounds that bind to the opioid receptors and/or α 2 -adrenoreceptor.
专利号:WO-2023044581-A1 优先权日:2021-09-24 标题 :Flow synthesis of porous collagen microparticles for versatile tissue engineering applications 发明人:SINGH SUSHANT; SAMIEI EHSAN; GUENTHER AXEL; VERES TEODOR 权利人:GOVERNING COUNCIL UNIV TORONTO; NAT RES COUNCIL CANADA; SINGH SUSHANT 摘要:A microfluidic flow synthesis method for collagen-based microparticles. Macro-porous fibrillar microparticles of pure collagen and composite collagen-GAG were formed, where the particle size and porosity were controlled by the flow synthesis parameters such as precursor flow rates. Using human dermal fibroblasts (hDFB) and umbilical cord derives mesenchymal stem cells (ucMSC), the capacity of the presented collagen and collagen-GAG microparticles to serve as cell culture substrates has been shown, to enable casting of tissues, forming spheroids, and as shear-thinning bioinks for bioprinting. At high packing densities, jammed collagen-based microparticles along with cells constitute a shear-thinning bioink for extrusion bioprinting applications. Bioprinted constructs exhibit a high porosity matrix due to the space between the microparticles, facilitating macromolecular transport, and cell proliferation and migration.
参考文献:10.1186/1472-6904-10-4 摘要:Carlzon D, Gustafsson L, Eriksson AL, Rignér K, Sundström A, Wallerstedt SM. Characteristics of primary health care units with focus on drug information from the pharmaceutical industry and adherence to prescribing objectives: a cross-sectional study. BMC Clinical Pharmacology. 2010 Feb 15;10(1):4. doi: 10.1186/1472-6904-10-4. 参考文献:10.1186/1752-1947-4-6 摘要:Baune BT, Eyre H. Anti-inflammatory effects of antidepressant and atypical antipsychotic medication for the treatment of major depression and comorbid arthritis: a case report. Journal of Medical Case Reports. 2010 Jan 12;4(1):6. doi: 10.1186/1752-1947-4-6. 参考文献:10.1155/2011/893905 摘要:Ishizaki J, Mimura M. Dysthymia and Apathy: Diagnosis and Treatment. Depression Research and Treatment. 2011;2011():1–7. doi: 10.1155/2011/893905. 参考文献:10.2165/11592070-000000000-00000 摘要:Watkins CC, Pieper AA, Treisman GJ. Safety considerations in drug treatment of depression in HIV-positive patients: an updated review. Drug Saf. 2011 Aug 01;34(8):623–39. doi: 10.2165/11592070-000000000-00000. 参考文献:10.2165/11591730-000000000-00000 摘要:Wallerstedt SM, Brunlöf G, Sundström A. Rates of spontaneous reports of adverse drug reactions for drugs reported in children: a cross-sectional study with data from the Swedish adverse drug reaction database and the Swedish Prescribed Drug Register. Drug Saf. 2011 Aug 01;34(8):669–82. doi: 10.2165/11591730-000000000-00000.