14773-41-2Relevant academic research and scientific papers
7. 8 - dimethoxy - 2, 3, 4, 5 - tetrahydro - 1 H - benzo [c] azepine hydrochloride and its preparation method (by machine translation)
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Paragraph 0018; 0028; 0035; 0036, (2017/11/16)
The invention discloses 7, 8 - dimethoxy - 2, 3, 4, 5 - tetrahydro - 1 H - benzo [c] azepine hydrochloride and its preparation method, in order to 3, 4 - dimethoxy c acid as initiator, in thionyl chloride catalytic, then ammonolysis to obtain 3, 4 - dimet
Discovery and biological evaluation of novel cyanoguanidine P2X7 antagonists with analgesic activity in a rat model of neuropathic pain
Perez-Medrano, Arturo,Donnelly-Roberts, Diana L.,Honore, Prisca,Hsieh, Gin C.,Namovic, Marian T.,Peddi, Sridhar,Shuai, Qi,Wang, Ying,Faltynek, Connie R.,Jarvis, Michael F.,Carroll, William A.
scheme or table, p. 3366 - 3376 (2010/04/03)
We disclose the design of a novel series of cyanoguanidines that are potent (IC50 ? 10-100 nM) and selective (≥100-fold) P2X7 receptor antagonists against the other P2 receptor subtypes such as the P2Y2, P2X4, and P2X3. We also found that these P2X7 antagonists effectively reduced nociception in a rat model of neuropathic pain (Chung model). Particularly, analogue 53 proved to be effective in the Chung model, with an ED50 of 38 μmol/kg after intraperitoneal administration. In addition compound 53 exhibited antiallodynic effects following oral administration and maintained its efficacy following repeated administration in the Chung model. These results suggest an important role of P2X7 receptors in neuropathic pain and therefore a potential use of P2X7 antagonists as novel therapeutic tools for the treatment of this type of pain.
TRISUBSTITUTED THIAZOLE COMPOUNDS, PREPARATIONS METHODS, PHARMACEUTICAL COMPOSITIONS AND MEDICALS USES THEREOF
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Page/Page column 41, (2009/12/23)
The present invention relates to 2,4,5-trisubstituted thiazole compounds of formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof for the inhibition of plasma PLTP activity and/or plasma CETP activity, wherein the substituents are as defined in the specification; a process for the preparation of the compounds of formula (I); a pharmaceutical composition comprising the compound of formula (I) and its use for the preparation of a medicament for treatment and/or prevention of diseases associated with the increased plasma PLTP activity and/or the increased plasma CETP activity in a mammal, such as atherosclerosis, cardiovascular diseases and peripheral vascular diseases, etc.
2,4,5-TRISUBSTITUTED THIAZOLE COMPOUNDS,PREPARATION METHODS, PHARMACEUTICAL COMPOSITIONS AND MEDICAL USES THEREOF
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Page/Page column 59, (2009/04/23)
The present invention relates to 2,4,5-trisubstituted thiazole compounds of formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof for the inhibition of plasma PLTP activity and/or plasma CETP activity, wherein the substituents are as defined in the specification; a process for the preparation of the compounds of formula (I); a pharmaceutical composition comprising the compound of formula (I) and its use for the preparation of a medicament for treatment and/or prevention of diseases associated with the increased plasma PLTP activity and/or the increased plasma CETP activity in a mammal, such as atherosclerosis, cardiovascular diseases and peripheral vascular diseases, etc.
A Facile Approach to 2-Arylethylamines via Polymeric Palladium Catalyst
Zhuangyu, Zhang,Yi, Pan,Hongwen, Hu,Tsi-yu, Kao
, p. 3563 - 3574 (2007/10/02)
2-Arylethylamines were synthesized in moderate yields via Heck reaction of acrylamide with iodobenzenes in the presence of polymeric catalyst P-ph-phen.Pd(0) followed by hydrogenation and subsequent Hofmann reaction.
