专利号:US-2012177593-A1 优先权日:2009-07-20 标 题 :Synthesis of dendrimer conjugates 发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH 权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.
专利号:US-8546532-B2 优先权日:2008-04-17 标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders 发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS 权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC 摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
专利号:US-2012029226-A1 优先权日:2009-02-06 标题:Method for the synthesis of chiral alpha-aryl propionic acid derivatives 发明人:KAPTEIN BERNARDUS; VLIEG ELIAS; NOORDUIN WILLEM LIEUWE 权利人:KAPTEIN BERNARDUS; VLIEG ELIAS; NOORDUIN WILLEM LIEUWE 摘要:The present invention provides a method for the synthesis of optically pure α-aryl propionic acid derivatives comprising subjecting the corresponding racemic α-aryl propionic acid derivatives to high sheer or impact forces, such as grinding.
专利号:US-12264143-B2 优先权日:2020-12-17 标 题:Synthesis of cannabinoids and cannabinoid precursors, and related compounds, formulations, and methods of use 发明人:SAMMIS GLENN M; ROGGEN MARKUS 权利人:NALU BIO INC 摘要:Methods are provided for the synthesis of cannabinoids, including cannabidiol (CBD), cannabinol (CBN), cannabichromene (CBC), cannabidiolic acid (CBDA), cannabigerol (CBG), cannabigerolic acid (CBGA), cannabidivarin (CBDV), cannabidibutol (CBD-C4), dihydrocannabidiol (DCBD), tetrahydrocannabivarin (THCV), analogs thereof, and precursors to the foregoing. One method employs phloroglucinol or a phloroglucinol analog as a starting material. The syntheses are stereospecific, efficient, selective, and cost-effective, with little or no potential for generation of THC ((−)-trans-Δ9-tetrahydro-cannabinol) or any other psychoactive side product. Telescoped syntheses are also provided, as are new cannabinoids, pharmaceutical formulations, and methods of use.
专利号:US-5043328-A 优先权日:1986-05-09 标 题 :Formulations containing unsaturated fatty acids for the synthesis of prostaglandins and hydroxy-fatty acids in biological systems 发明人:WEITHMANN KLAUS U 权利人:HOECHST AG 摘要:The present invention relates to formulations containing unsaturated fatty acids for the synthesis of prostaglandins and hydroxy-fatty acids in biological systems and to the use of such formulations for the preparation of medicaments which are suitable for curing prostaglandin deficiencies in humans or animal, for example healing or preventing diseases of the gastro-intestinal tract.
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.
1: Abdel-Aziz AA, Al-Badr AA, Hafez GA. Flurbiprofen. Profiles Drug Subst Excip Relat Methodol. 2012;37:113-81. doi: 10.1016/B978-0-12-397220-0.00004-0. Epub 2012 Mar 19. 31(789):31-2. 32(1):76-80. doi: 10.1038/clpt.1982.129. 61(8):1396-406. doi: 10.1111/j.1742-1241.2007.01452.x. Epub 2007 Jun 26. 26(6):e723-e726. doi: 10.1097/MJT.0000000000000879. 28(2):100-14. doi: 10.2165/00003088-199528020-00002. 34(6):894-900. doi: 10.1002/chir.23441. Epub 2022 Apr 12. 80(3A):10-5. doi: 10.1016/0002-9343(86)90104-x. 20:995-1002. doi: 10.12659/MSM.890102. 10: Geerts H. Drug evaluation: (R)-flurbiprofen--an enantiomer of flurbiprofen for the treatment of Alzheimer's disease. IDrugs. 2007 Feb;10(2):121-33. 18(6):417-38. doi: 10.2165/00003495-197918060-00001. 60(1):43-8. doi: 10.3949/ccjm.60.1.43. 48(2):400-8. doi: 10.1016/j.brainresrev.2004.12.029. Epub 2005 Jan 28. 5(1):85-7. doi: 10.1185/03007997709108982. 50(7):749-756. doi: 10.1007/s00595-019-01951-1. Epub 2020 Jan 10. 31(6):457-467. doi: 10.1002/chir.23071. Epub 2019 May 7. 27(6):707-712. doi: 10.1111/vec.12638. Epub 2017 Aug 23. 18(1):133. doi: 10.1186/s12944-019-1064-x.
合成参考文献
参考文献:10.1007/s00228-010-0784-7 摘要:Chopade AR, Mulla WA. Novel strategies for the treatment of inflammatory hyperalgesia. European Journal of Clinical Pharmacology. 2010 Feb 13;66(5):429–44. doi: 10.1007/s00228-010-0784-7. 参考文献:10.18632/aging.100021 摘要:Choi SH, Bosetti F. Cyclooxygenase-1 null mice show reduced neuroinflammation in response to beta-amyloid. Aging (Albany NY). 2009 Feb 11;1(2):234–44. 参考文献:10.2147/opth.s7633 摘要:Reddy R, Kim SJ. Critical appraisal of ophthalmic ketorolac in treatment of pain and inflammation following cataract surgery. Clin Ophthalmol. 2011;5():751–8. 参考文献:10.1002/chir.20978 摘要:Ribeiro AE, Gomes PS, Pais LS, Rodrigues AE. Chiral separation of flurbiprofen enantiomers by preparative and simulated moving bed chromatography. Chirality. 2011 Sep;23(8):602–11. doi: 10.1002/chir.20978. 参考文献:10.4103/0972-124x.75908 摘要:Dhadse P, Gattani D, Mishra R. The link between periodontal disease and cardiovascular disease: How far we have come in last two decades J Indian Soc Periodontol. 2010 Jul;14(3):148–54.