100524-07-0Relevant articles and documents
Practical synthesis of N -substituted cyanamides via tiemann rearrangement of amidoximes
Lin, Chia-Chi,Hsieh, Tsung-Han,Liao, Pen-Yuan,Liao, Zhen-Yuan,Chang, Chih-Wei,Shih, Yu-Chiao,Yeh, Wen-Hsiung,Chien, Tun-Cheng
supporting information, p. 892 - 895 (2014/03/21)
A facile and general synthesis of various N-substituted cyanamides was accomplished by the Tiemann rearrangement of amidoximes with benzenesulfonyl chlorides (TsCl or o-NsCl) and DIPEA.
HETEROARYL-PYRAZOLE DERIVATIVE
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Paragraph 0518; 0519; 0520; 0525; 0526, (2013/06/05)
A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.
QUINOLINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
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Page 76, (2008/06/13)
There are provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R19, R20 and R34 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
1,2,4-Oxadiazole derivatives of phenylalanine: potential inhibitors of substance P endopeptidase
Borg, S.,Luthman, K.,Nyberg, F.,Terenius, L.,Hacksell, U.
, p. 801 - 810 (2007/10/02)
The synthesis and the biological activity of a series of benzyl or aryl substituted 1,2,4-oxadiazole derivatives of phenyl-alanine are described.A base-promoted intermolecular cyclization reaction was performed using racemic tert-butyloxycarbonyl protected phenylalanine methyl ester and an amidoxime.After deprotection of the amino function the compounds were evaluated for their affinity to rat brain NK1-receptors and as inhibitors of a specific substance P cleaving enzyme, substance P endopeptidase (SPE), isolated from human cerebrospinal fluid.The results indicate that several compounds are weak inhibitors of SPE.However, all compounds lacked appreciable NK1-receptor affinity.Keywords: 1,2,4-oxadiazoles / substance P endopeptidase / Phe-Phe mimetics / amide bioisostere / NK1-receptor affinity