专利号:US-6815214-B2 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of diketopiperazines 发明人:BOYCE JIM P; HOWBERT J JEFFRY; TABONE JOHN C 权利人:CELLTECH R & D INC 摘要:The synthesis of novel diketopiperazines, their use in inhibiting cellular events such as those involving NFK-α, NFK-β and in the treatment of inflammation events, a combinatorial library of diverse diketopiperazines and process for their synthesis as a library and as individual compounds. In particular novel diketopiperazines are disclosed including their synthesis and use in cellular events such as activation of the transcription factor, nuclear factor, TNF-α, TNF-β and also apoptosis.
专利号:US-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
专利号:US-4935536-A 优先权日:1987-05-21 标 题 :Protecting groups for asparagine and glutamine in peptide synthesis 发明人:HUDSON DEREK 权利人:MILLIPORE CORP 摘要:Trialkoxybenzyl (Taob) protected asparagine and glutamine, a method of synthesis and a method of use are provided. The Taob protected Asn and Gln have the following formulae: ##STR1## wherein Z is an alkyl group having from 1 to 10 carbon atoms; X and W are any α-protecting group which can be selectively removed while maintaining Taob intact; Y is H or any group sufficiently active or activatable to react with NH 2 -- or NHâ•? to generate an amide bond; n is 1 for asparagine or 2 for glutamine. These derivatives are stable in solution, have good solubility in organic solvents and couple directly without side reactions.
专利号:US-6933303-B2 优先权日:2001-10-19 标 题:Heteroaryl-fused nitrogen heterocycles as therapeutic agents 发明人:MJALLI ADNAN M M; ANDREWS ROBERT C; XIE RONGYUAN; YARRAGUNTA RAVINDRA R; REN TAN 权利人:TRANSTECH PHARMA INC 摘要:This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases, the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.
专利号:US-2005080086-A1 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of diketopiperazines
专利号:US-2003069305-A1 优先权日:2000-12-22 标题:Pharmaceutical uses and synthesis of benzobicyclooctanes
[参考文献]: Yusuke Ohta, Et Al. Facile Synthesis Of 3-(Aminomethyl)Isoquinolines By Copper-Catalysed Domino Four-Component Coupling And Cyclisation. Chem Commun (Camb). 2008 Feb 21:(7):835-7.
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).