专利号:US-6825378-B2 优先权日:2003-03-28 标 题 :Process for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid 发明人:KUMAR PRADEEP; FERNANDES RODNEY AGUSTINHO; GUPTA PRITI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention provides a process for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1). The present invention more particularly relates to a process using cyclohexylphenyl ketone for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1).
专利号:US-2024082118-A1 优先权日:2021-05-19 标 题:Topical compositions and methods of preparing the same 发明人:ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION 权利人:LANDA LABS 2012 LTD 摘要:There is disclosed a composition comprising a water-insoluble thermoplastic compound capable of stimulating collagen synthesis (CSSC), the CSSC having a molecular weight of more than 0.6 kDa and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less and a viscosity of 107 mPa·s or less. The nano-elements of CSSC can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon their application to a surface to be treated therewith. Methods for preparing the compositions and uses thereof are also provided.
专利号:WO-2017137955-A1 优先权日:2016-02-14 标题:Novel (r) and rac 3-(2-(allyloxy)-5-methylphenyl)-n,n-diisopropyl-3- phenylpropan-1-amine and its use for synthesis of (r) and rac-2-(3- (diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol 发明人:THOMBARE PRAVIN SAHADEV 权利人:CELESTIS PHARMACEUTICALS PVT LTD 摘要:The present invention relates to novel chiral 3-(2-(allyloxy)-5-methylphenyl)-N,N-diisopropyl-3-phenylpropan-1-amine (5) and racemic 3-(2-(allyloxy)-5-methylphenyl)-N,N-diisopropyl-3-phenylpropan-1-amine () and its use in improved and industrially advantageous process for preparation of chiral and racemic form of 2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol. Further, present invention relates to preparation of the same.
专利号:US-6140529-A 优先权日:1998-10-22 标 题 :Synthesis of optically active cyclohexylphenylglycolate esters 发明人:BAKALE ROGER P; LOPEZ JORGE L; MCCONVILLE FRANCIS X; VANDENBOSSCHE CHARLES P; SENANAYAKE CHRIS HUGH 权利人:SEPRACOR INC 摘要:A process for the preparation of optically active cyclohexylphenylglycolate esters is described. The process utilizes carboxylic acid activation to couple (R)- or (S)-cyclohexylphenylglycolic acid (CHPGA) with 4-N,N-diethylamino butynol or other propargyl alcohol derivatives. The preparation of the hydrochloride salt is also described. In addition, a resolution process employing tyrosine methyl ester enantiomers for preparing a single enantiomer of CHPGA from racemic CHPGA is disclosed.
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:US-10035796-B2 优先权日:2014-08-14 标题:Crystalline forms of a BACE inhibitor, compositions, and their use 发明人:KAZAKEVICH IRINA; TRZASKA SCOTT; FENG TAO 权利人:MERCK SHARP & DOHME 摘要:The present invention provides a novel synthesis of verubecestat, and two novel crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an Aβ pathology and/or a symptom or symptoms thereof. Non-limiting examples of such Aβ pathologies, including Alzheimer's disease, are disclosed herein.
1: Capalbo D, Guarino S, Di Sessa A, Esposito C, Grella C, Papparella A, Miraglia Del Giudice E, Marzuillo P. Combination therapy (desmopressin plus oxybutynin) improves the response rate compared with desmopressin alone in patients with monosymptomatic nocturnal enuresis and nocturnal polyuria and absence of constipation predict the response to this treatment. Eur J Pediatr. 2023 Jan 25. doi: 10.1007/s00431-023-04824-5. Epub ahead of print. 67(3):222-227. doi: 10.4103/ijd.IJD_799_20. 5: Edwards BA, Joosten SA. Variability in the response to atomoxetine and oxybutynin for OSA: Highlighting the need for personalized medicine. Respirology. 2023 Mar;28(3):215-216. doi: 10.1111/resp.14395. Epub 2022 Oct 18. 28(3):273-280. doi: 10.1111/resp.14383. Epub 2022 Oct 2. Erratum in: Respirology. 2022 Oct 30;: 28(3):9-14. doi: 10.46292/sci21-00091. Epub 2022 Aug 17. 8: Sun P, Wang Z, Wu T, Zuo S, Huang X, Cui Z, Zhang D. Injectable, Adhesive, and Self-Healing Composite Hydrogels Loaded With Oxybutynin Hydrochloride for the Treatment of Overactive Bladder in Rats. Front Bioeng Biotechnol. 2022 Jun 27;10:906835. doi: 10.3389/fbioe.2022.906835.
合成参考文献
参考文献:10.1155/2011/714978 摘要:Masumori N, Miyamoto S, Tsukamoto T, Furuya S, Iwasawa A, Sato T, Itoh N, Shibuya A, Oda T. The efficacy and safety of propiverine hydrochloride in patients with overactive bladder symptoms who poorly responded to previous anticholinergic agents. Adv Urol. 2011;2011():714978. 参考文献:10.1179/2045772311y.0000000012 摘要:Kennelly MJ, Bennett ME, Grill WM, Grill JH, Boggs JW. Electrical stimulation of the urethra evokes bladder contractions and emptying in spinal cord injury men: Case studies. The Journal of Spinal Cord Medicine. 2011 May;34(3):315–21. doi: 10.1179/2045772311y.0000000012. 参考文献:10.1016/j.urology.2011.05.011 摘要:Yoshida A, Seki M, Nasrin S, Otsuka A, Ozono S, Takeda M, Masuyama K, Araki I, Ehlert FJ, Yamada S. Characterization of muscarinic receptors in the human bladder mucosa: direct quantification of subtypes using 4-DAMP mustard. Urology. 2011 Sep;78(3):721.e7–721.e12. doi: 10.1016/j.urology.2011.05.011. 参考文献:10.1007/s11255-011-0030-y 摘要:Lehnert T, Weisser M, Till H, Rolle U. The effects of long-term medical treatment combined with clean intermittent catheterization in children with neurogenic detrusor overactivity. International Urology and Nephrology. 2011 Jul 21;44(2):335–41. doi: 10.1007/s11255-011-0030-y.