专利号:US-8236960-B2 优先权日:2004-09-27 标 题 :Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy) phenylmethyl)carbamide and its tartrate salt and crystalline forms 发明人:THYGESEN MIKKEL BOAS; SCHLIENGER NATHALIE; TOLF BO-RAGNAR; ANDERSSON CARL-MAGNUS A; BLATTER FRITZ; BERGHAUSEN JOERG 权利人:THYGESEN MIKKEL BOAS; SCHLIENGER NATHALIE; TOLF BO-RAGNAR; ANDERSSON CARL-MAGNUS A; BLATTER FRITZ; BERGHAUSEN JOERG; ACADIA PHARM INC 摘要:Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl) -N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2 -methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates.
专利号:US-2004030209-A1 优先权日:2000-11-30 标 题:Method for the production of alkyl aryl sulphonates 发明人:NARBESHUBER THOMAS; STEINBRENNER ULRICH; KRACK GERHARD 摘要:The preparation of alkylaryl compounds takes place by n 1) preparation of a mixture of, on statistical average, predominantly monobranched C 10-14 -olefins by n a) reaction of a C 4 -olefin mixture over a metathesis catalyst for the preparation of an olefin mixture comprising 2-pentene and/or 3-hexene, and optional removal of 2-pentene and/or 3-hexene, followed by dimerization of the resulting 2-pentene and/or 3-hexene over a dimerization catalyst to give a mixture comprising C 10-12 -olefins, and optionally removal of the C 10-12 -olefins, or n b) extraction of predominantly monobranched paraffins from kerosene cuts and subsequent dehydrogenation, or n c) Fischer-Tropsch synthesis of olefins or paraffins, where the paraffins are dehydrogenated, or n d) dimerization of shorter-chain internal olefins, or n e) isomerization of linear olefins or paraffins, where the isomerized paraffins are dehydrogenated, n 2) reaction of the olefin mixture obtained in stage 1) with an aromatic hydrocarbon in the presence of an alkylation catalyst which contains zeolites of the faujasite type.
专利号:US-2024325572-A1 优先权日:2021-07-15 标 题 :N-heterocyclyl substituted 2-cyano-3-(naphthalen-2-yl)acrylamide derivatives as fluorophors for detection of amyloid and amyloid-like proteins for diagnosis of neurodegenerative disorders 发明人:SARRAF STELLA T 权利人:AMYDIS INC 摘要:Provided herein is the design and synthesis of novel molecular rotor fluorophores of formula I useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are the compounds for use in methods for diagnosis and treatment of diseases associated with an amyloid or amyloid like proteins, such as e.g. Alzheimer's disease or traumatic brain injury (TBI), Parkinson's disease, vascular dementia, amyotrophic lateral sclerosis, Down syndrome, traumatic brain injury, chronic traumatic encephalopathy, schizophrenia or depression. Exemplary compounds are e.g. N-heterocyclyl substituted 2-cyano-3-(naphthalen-2-yl)acrylamide derivatives, such as e.g. (E)-2-cyano-N-(2-(2-hydroxy)ethoxy)ethyl)-3-(6-(pyrrolidin-1-yl)naphthalen-2-yl) acrylamide (example 1): Experimental data on in-vitro binding studies with amyloid beta is provided.
专利号:US-7790899-B2 优先权日:2004-09-27 标 题 :Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms 发明人:TOLF BO-RAGNAR; SCHLIENGER NATHALIE; THYGESEN MIKKEL BOAS 权利人:ACADIA PHARM INC 摘要:Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide and methods for obtaining the salt. Further disclosed are various crystalline forms of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its hemi-tartrate salt including various polymorphs and solvates.
专利号:WO-2022223696-A1 优先权日:2021-04-22 标 题 :Process for synthesis of n-alkyl-n-phenyl hydrazine 发明人:ENDRES ANDREAS; NANDURKAR NITIN SUBHASH; KATE KIRAN; SATHE SHANTANU SHRIKANT 权利人:COLORANTS INT LTD 摘要:The invention provides a process for synthesizing N-alkyl-N-phenyl hydrazine which is devoid of any organic solvents and can be carried out at lower temperatures. The process is environmental-friendly and gives better yield and high purity of the N-alkyl-N-phenyl hydrazine.
专利号:US-2006062846-A1 优先权日:2004-09-17 标题 :Alfuzosin tablets and synthesis 发明人:SCHEER MATHIAS; REY HELENE; FISCHER MARC; KRAMER DIRK 权利人:CIMEX PHARMA AG 摘要:A monolithic composition includes alfuzosin in a polymeric matrix adapted to release 13-33% of the alfuzosin within 2 hours, 40-60% of the alfuzosin within 7 hours, and greater than 80% of the alfuzosin within 20 hours of administration. A unit dosage form includes: a heterogeneous mixture of alfuzosin hydrochloride anhydrate, lactose monohydrate, hydroxypropylmethylcellulose, polyvinylpyrrolidone and magnesium stearate, wherein the heterogeneous mixture is heterogeneously distributed throughout the unit dosage form. A manufacturing process includes: mixing a hydrophilic polymer and alfuzosin to provide a blend; granulating the blend to provide granules; drying the granules on a dryer to provide dried granules; sizing the dried granules to provide sized granules; mixing the sized granules with a lubricant to obtain a mixture; and compressing the mixture to obtain a tablet. A method of treating benign prostatic hyperplasia, includes administering to a patient the composition or unit dosage form once a day.
摘要:U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals., NX#00154 摘要:S13 | EUCOSMETICS | Combined Inventory of Ingredients Employed in Cosmetic Products (2000) and Revised Inventory (2006) | DOI:10.5281/zenodo.2624118 摘要:International Journal of Toxicology 29(Suppl. 2):115-132, 2010 参考文献:10.1186/1472-6815-2-1 摘要:Malik V, Tyagi I, Varma A, Phadke RV. Use of the direct puncture technique in management of capillaro-venous malformations: case report. BMC Ear, Nose and Throat Disorders. 2002 Mar 19;2(1):1. doi: 10.1186/1472-6815-2-1. 参考文献:10.1007/s00383-008-2124-x 摘要:Granata C, Oddone M, Toma P, Mattioli G. Retrograde percutaneous sclerotherapy of left idiopathic varicocele in children: results and follow-up. Pediatric Surgery International. 2008 Mar 26;24(5):583–7. doi: 10.1007/s00383-008-2124-x.