[EN] AZOLE METHYLIDENE CYANIDE DERIVATIVES AND THEIR USE AS PROTEIN KINASE MODULATORS<br/>[FR] DERIVES DE CYANURE D'AZOLE METHYLIDENE ET LEUR UTILISATION COMME MODULATEURS DE PROTEINE KINASE
申请人:APPLIED RESEARCH SYSTEMS
公开号:WO2003106455A1
公开(公告)日:2003-12-24
The present invention is related to azole derivatives notably for use as pharmaceutically active
compounds, as well as to pharmaceutical formulations containing such azole
derivatives. Said azole derivatives are modulators of the protein kinase signalling
pathways, particularly the one involving c-Jun N-terminal kinase and/or Glycogen
Kinase Synthase 3. The present invention is furthermore related to novel azole
derivatives as well as to methods of their preparation. X is O, S or NR0,
with R0 being H or an unsubstituted or substituted C1 -C6
alkyl; A is 2-pyridyl, 3-pyridyl, 4-pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl
or triazinyl group.
π-Allyl palladium approach toward the diazabicyclo[3.2.1]octane core of the naphthyridinomycin alkaloids
作者:Grace H.C. Woo、Se-Ho Kim、Peter Wipf
DOI:10.1016/j.tet.2006.06.114
日期:2006.11
A novel and efficient protocol for the synthesis of the 3,8-diazabicyclo[3.2.1]octanesystem found in the naphthyridinomycin, dnacin, and tetrazomine families of alkaloids is described. The key transformation involves an intramolecular palladium-catalyzed allylic alkylation. The cyclization proceeds smoothly under mild conditions (20 mol % Pd2dba3, 1.5 equiv DBU, 65 °C, THF, 20 min) to afford 3,8-diazabicyclo[3
The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.
The synthesis, reduction and cyclisation of N-(3-butynyl)- morpholin-and-thiomorpholin-2,6-diones
作者:M.S. Hadley、F.d. King、R.T. Martin
DOI:10.1016/s0040-4039(00)81335-0
日期:1983.1
A nove one-step synthesis of N-(3-butenyl) imides (1) from dicarboxylic acids, and the sodium borohydride reduction/formic acid cyclisation of the N-(3-butenyl)-morpholin- and thiomorpholin-2,6-diones are described.
Preparation of 2-(2-cyanoethyl)sulfanyl-1H-isoindole-1,3-(2H)-dione and related sulfur-transfer agents
作者:Jana Klose、Colin B. Reese、Quanlai Song
DOI:10.1016/s0040-4020(97)00924-1
日期:1997.10
The title compound 3 and 4-[(2-cyanoethyl)sulfanyl]morpholine-3,5-dione 12 are both conveniently prepared in good yield from 2-cyanoethyl disulfide, which itself is readily prepared in one step from S-(2-cyanoethyl)isothiouronium chloride 4. In the same way, dimethyl and diphenyl disulfides are converted into 2-methylsulfanyl- and 2-phenylsulfanyl-1H-isoindole-1,3-(2H)-diones 8a and 8b, respectively