专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:US-9676783-B2 优先权日:2008-10-22 标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds 发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN 权利人:ARRAY BIOPHARMA INC 摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
专利号:US-6552018-B1 优先权日:1997-01-27 标 题:Pyrazole derivatives 发明人:EJIMA AKIO; OHSUKI SATORU; OHKI HITOSHI; NAITO HIROYUKI 权利人:DAIICHI SEIYAKU CO 摘要:The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): n wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: n These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)- 1 piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.
专利号:DK-2725028-T3 优先权日:2008-10-22 标题:Substituted pyrazolo [1,5-a] pyrimidine compounds as intermediates in the synthesis of kinase inhibitors TRK
专利号:EP-2725028-A1 优先权日:2008-10-22 标题 :Substituted pyrazolo[1,5-]pyrimidine compounds as intermediates in the synthesis of TRK kinase inhibitors
专利号:EP-2725028-B1 优先权日:2008-10-22 标题 :Substituted pyrazolo[1,5-]pyrimidine compounds as intermediates in the synthesis of TRK kinase inhibitors
参考文献:10.1007/s11356-019-07133-3 摘要:Dhakal R, Li X, Parkin SR, Lehmler H. Synthesis of mono- and dimethoxylated polychlorinated biphenyl derivatives starting from fluoroarene derivatives. Environmental Science and Pollution Research. 2019 Dec 31;27(9):8905–25. doi: 10.1007/s11356-019-07133-3.