专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:WO-2025056767-A1 优先权日:2023-09-15 标题 :Process for the preparation of enantiomerically enriched aliphatic amines 发明人:BOU HAMDAN FARHAN; GODINEAU EDOUARD; SMEJKAL TOMAS; DUMEUNIER RAPHAEL; BOUSSEMGHOUNE MOHAMED ABDELOUAHAB; BLUM MATHIAS 权利人:SYNGENTA CROP PROTECTION AG 摘要:The present invention relates to a process for the preparation of enantiomerically enriched cyclobutylamines of formula (I) from α-tertiary cyclobutanones and reacting said enantiomerically enriched cyclobutylamines to enantiomerically enriched cyclobutylamides. Such compounds are useful intermediates in the synthesis of microbiocidal thiazole compounds.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
专利号:US-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
专利号:US-9757463-B2 优先权日:2012-06-15 标题 :Linear polyester and semi-linear glycidol polymer systems: formulation and synthesis of novel monomers and macromolecular structures 发明人:HARTH EVA M; BEEZER DAIN B; LI GUANGZHAO; SPEARS BENJAMIN R; STEVENS DAVID M 权利人:UNIV VANDERBILT 摘要:Disclosed herein are glycidol-based polymers, nanoparticles, and methods related thereto useful for drug delivery. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-2006165683-A1 优先权日:2001-12-05 标题:Methods and compositions for control of bone formation via modulation of sympathetic tone 发明人:KARSENTY GERARD; TAKEDA SHU; ELEFTERIOU FLORENT 权利人:KARSENTY GERARD; TAKEDA SHU; ELEFTERIOU FLORENT 摘要:This invention relates to methods for treatment, diagnosis and prevention of bone disease and comprises methods including measurement and modulation of sympathetic tone and leptin activity. Alteration of sympathetic tone in bone disease can be accomplished by decreasing or increasing leptin synthesis, leptin receptor synthesis, leptin binding to the leptin receptor, and leptin receptor activity. Alteration of sympathetic tone in bone disease can also be accomplished in the foregoing manner, in combination with traditional sympathetic nervous system agonists and/or antagonists, such as, but not limited to, a dopamine β hydroxylase antagonist or a β adrenergic antagonist for treatment or prevention of osteoporosis.
1: Zahn V, Krumbachner G. Clenbuterol - A long term uterine relaxant. J Perinat Med. 2023 Nov 2;9(2):96-100. doi: 10.1515/jpm-1981-090201. 27(1):98. doi: 10.1186/s40824-023-00432-4. 3: Hu D, Li H, Yu H, Zhao M, Ye L, Liu B, Ge N, Dong N, Wu L. Clenbuterol Prevents Mechanical Unloading-Induced Myocardial Atrophy via Upregulation of Transient Receptor Potential Channel-3. Int Heart J. 2023;64(5):901-909. doi: 10.1536/ihj.21-129. 14:1252508. doi: 10.3389/fphys.2023.1252508.
合成参考文献
参考文献:10.1007/s11596-010-0106-4 摘要:Wang H, Zhao H, Ye Y, Xiong N, Huang J, Yao D, Shen Y, Zhao X. Focal cerebral ischemia induces Alzheimer's disease-like pathological change in rats. J Huazhong Univ Sci Technolog Med Sci. 2010 Feb;30(1):29–36. doi: 10.1007/s11596-010-0106-4. 参考文献:10.1007/s00216-010-3484-3 摘要:Peters RJB, Oosterink JE, Stolker AAM, Georgakopoulos C, Nielen MWF. Generic sample preparation combined with high-resolution liquid chromatography–time-of-flight mass spectrometry for unification of urine screening in doping-control laboratories. Analytical and Bioanalytical Chemistry. 2010 Feb 16;396(7):2583–98. doi: 10.1007/s00216-010-3484-3. 参考文献:10.1186/1472-6750-10-12 摘要:Zhong L, Zhang W, Zer C, Ge K, Gao X, Kernstine KH. Protein microarray: sensitive and effective immunodetection for drug residues. BMC Biotechnol. 2010 Feb 16;10():12. 参考文献:10.1007/s11373-005-9019-9 摘要:Chou CH, Tsai YL, Hou CW, Lee HH, Chang WH, Lin TW, Hsu TH, Huang YJ, Kuo CH. Glycogen overload by postexercise insulin administration abolished the exercise-induced increase in GLUT4 protein. J Biomed Sci. 2005 Dec;12(6):991–8. doi: 10.1007/s11373-005-9019-9. 参考文献:10.1111/j.1440-1681.2011.05574.x 摘要:Head SI, Ha TN. Acute inhibitory effects of clenbuterol on force, Ca2+transients and action potentials in rat soleus may not involve the β2‐adrenoceptor pathway. Clin Exp Pharma Physio. 2011 Aug 26;38(9):638–46. doi: 10.1111/j.1440-1681.2011.05574.x.