- SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF NUCLEASES
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The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3, R4, R5, R6 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
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Page/Page column 14-15; 40; 46-47
(2019/11/12)
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- A rapid and high-yielding synthesis of thiazoles and aminothiazoles using tetrabutylammonium salts
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A convenient method for the synthesis of thiazoles and aminothiazoles by treatment of phenacyl bromides with thioamides/thiourea in the presence of tetrabutylammonium hexafluorophosphate (Bu4NPF6) at room temperature was developed. The products having high yields were formed rapidly (within 15 min). The method is simple, rapid and practical, generating thiazole derivatives in excellent isolated yields. The structures of the newly synthesized products were identified by FT-IR, 1H NMR, 13C NMR spectroscopy and elemental analysis data. The Japan Institute of Heterocyclic Chemistry.
- Kocabas, Erdal,Sariguney, Ahmet Burak,Coskun, Ahmet
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experimental part
p. 2849 - 2854
(2011/04/16)
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- N-(4-Substituted-thiazolyl)oxamic Acid Derivatives, a New Series of Potent, Orally Actve Antiallergy Agents
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A series of N-(4-substituted-thiazolyl)oxamic acid derivatives were synthesized and tested for antiallergy activity in the rat PCA model.These compounds were conveniently prepared by treatment of the appropriate acetophenone with thiourea and iodine or by reaction of the chloroacetylbenzene with thiourea to give the corresponding aminothiazoles; subsequent condensation with ethyloxalyl chloride gave the thiazolyloxamates.Many of the analogues showed a 50percent inhibition at oxamic acid ethanolamine salt (61, PRH-836-EA), has been selected for further pharmacological evaluation.
- Hargrave, Karl D.,Hess, Friedrich K.,Oliver, James T.
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p. 1158 - 1163
(2007/10/02)
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