专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-7816375-B2 优先权日:2000-09-11 标 题 :Ligands for monoamine receptors and transporters, and methods of use thereof 发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HOLLAND JOANNE M; PERSONS PAUL E; RADEKE HEIKE; WANG FENGJIANG; SHAO LIMING 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
专利号:WO-2025125811-A1 优先权日:2023-12-12 标题:Heterocyclic compounds and their use for the treatment of neurological disorders 发明人:PLOWRIGHT ALLEYN THOMAS; PFEIFFER THOMAS; MÄRCHER-RØRSTED EMIL; DUCKWORTH EDWARD JOSEPH 权利人:ONTRACK THERAPEUTICS LTD 摘要:The present invention relates to novel synthetic compounds of Formula (I) and (II) related to naturally occurring flavonoids such as 7,8-dihydroxyflavone (7,8-DHF). The invention further relates to the method of synthesis, the use of these compounds as research tools and their use as pharmaceuticals.
专利号:EP-1695964-A1 优先权日:2000-11-15 标题 :Quinoline derivatives for use as intermediates in the synthesis of heterocyclylalcoyl piperidines
专利号:CN-1247191-A 优先权日:1993-06-14 标题 :Imidazole compounds as raw materials for the synthesis of imidazole lipoxygenase inhibitors
参考标题:Design And Synthesis Of Novel, Potent And Selective Hypoxanthine Analogs As Adenosine A 1 Receptor Antagonists And Their Biological Evaluation 作者:Summon Koul,Vidya Ramdas,Dinesh A. Barawkar,Yogesh B. Waman,Neela Prasad,Santosh Kumar Madadi,Yogesh D. Shejul,Rajesh Bonagiri,Sujay Basu,Suraj Menon,Srinivasa B. Reddy,Sandhya Chaturvedi,Srinivas Rao Chennamaneni,Gaurav Bedse,Rhishikesh Thakare,Jayasagar Gundu,Sumit Chaudhary,Siddhartha De,Ashwinkumar V. Meru,Venkata Palle,Anita Chugh,Kasim A. Mookhtiar |发布日期:2017.3 摘要:Multipronged Approach Was Used To Synthesize A Library Of Diverse C-8 Cyclopentyl Hypoxanthine Analogs From A Common Intermediate Iii. Several Potent And Selective Compounds Were Identified And Evaluated For Pharmacokinetic (Pk) Properties In Wistar Rats. One Of The Compounds 14 With Acceptable Pk Parameters Was Selected For Testing In In Vivo Primary Acute Diuresis Model. The Compound Demonstrated
合成参考文献
摘要:Waldvogel, S. R., Science of Synthesis Knowledge Updates, (2010) 1, 487. 摘要:Selt, M.; Waldvogel, S. R., Science of Synthesis: Special Topics, (2021) 1, 275.