876918-30-8Relevant articles and documents
Preparation of Polyfunctionalized Aromatic Nitriles from Aryl Oxazolines
Hess,Guelen,Alandini,Mourati,Guersoy,Knochel
, (2021/12/06)
A selective ortho,ortho’-functionalization of readily available aryl oxazolines by two successive magnesiations with sBu2Mg in toluene followed by trapping reactions with electrophiles, such as (hetero)aryl iodides or bromides, iodine, tosyl cyanide, ethyl cyanoformate or allylic bromides (39 examples, 62–99 % yield) is reported. Treatment of these aryl oxazolines with excess oxalyl chloride and catalytic amounts of DMF (50 °C, 4 h) provided the corresponding nitriles (36 examples, 73–99 % yield). Conversions of these nitriles to valuable heterocycles are reported, and a tentative mechanism is proposed.
Synthesis and bioevaluation of 1-phenylimidazole-4-carboxylic acid derivatives as novel xanthine oxidoreductase inhibitors
Li, Jing,Li, Xiaolei,Li, Yuanyuan,Zhang, Lei,Zhou, Haiyan,Zhu, Xinying
, (2019/12/30)
As part of a continuing study, we designed and synthesized four series of 1-phenylimidazole-4-carboxylic acid derivatives as xanthine oxidoreductase (XOR) inhibitors, evaluated their in vitro inhibitory potencies against XOR and hypouricemic effects in mi
Phenylimidazole XOR (Xanthine Oxidoreductase) inhibitor and preparation and application thereof
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Paragraph 0142-0144, (2019/09/17)
The invention belongs to the technical field of pharmaceutical and chemical industries and discloses a phenylimidazole XOR (Xanthine Oxidoreductase) inhibitor and the preparation and the application of the phenylimidazole XOR inhibitor. The structure of t
Synthesis and bioevaluation of 1-phenyl-pyrazole-4-carboxylic acid derivatives as potent xanthine oxidoreductase inhibitors
Li, Jing,Wu, Fangping,Liu, Xingguo,Zou, Yake,Chen, Huixiong,Li, Zheng,Zhang, Lei
, p. 20 - 30 (2017/09/19)
A diverse library of 1-phenyl-pyrazole-4-carboxylic acid derivatives were synthesized and evaluated for their inhibitory potency against xanthine oxidoreductase (XOR) in vitro and vivo, and the structure-activity relationship (SAR) analyses were also pres
Nitrogen-substituted phenyl pyrazole xanthine oxidoreductase inhibitor and preparation and application thereof
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Paragraph 0058, (2017/07/13)
The invention belongs to the technical field of pharmaceutical and chemical industry and discloses nitrogen-substituted phenyl pyrazole xanthine oxidoreductase inhibitor and preparation and application thereof. The nitrogen-substituted phenyl pyrazole xan
ACYLGUANIDINES AS TRYPTOPHAN HYDROXYLASE INHIBITORS
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Page/Page column 43, (2015/06/25)
The present invention is directed to acylguanidines which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPHl), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
REMEDY OR PREVENTIVE FOR DIGESTIVE ULCER
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, (2008/12/09)
An object of the present invention is to provide an agent for treating or preventing digestive ulcer that is effective even to ulcer of small intestine and others, for which gastric acid secretion inhibitors such as proton pump inhibitors are ineffective, and is superior to allopurinol in the efficaciousness and the safety. The pharmaceutical composition of the present invention comprising a non-purine xanthine oxidase inhibitor as the active ingredient is useful as an agent for treating or preventing ulcer that forms in digestive tracts by the attack of gastric acid, pepsin, stress, Helicobacter pylori bacteria, NSAID, etc. In particular, it is useful as an ulcer remedy heretofore unknown in the art as it is effective even for ulcer in small intestine for which gastric/duodenal ulcer remedies that inhibit gastric acid secretion such as proton pump inhibitors are ineffective.
2-PHENYLPYRIDINE DERIVATIVE
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, (2008/06/13)
The present invention relates to a novel 2-phenylpyridine derivative or a salt thereof, wherein the pyridine ring is substituted with a carboxyl group or the like and the benzene ring has an electron-withdrawing group such as a cyano group and an electron-donating group such as a substituted alkoxy group at the same time. Since the compound of the invention has good xanthine oxidase-inhibitory action and uric acid-lowering action and does not have a structure derived from nucleic acid, the compound has advantages of high safety and excellent effects as compared with conventional compounds and is useful as a therapeutic or preventive agent for hyperuricemia, gout, inflammatory bowel diseases, diabetic kidney diseases, diabetic retinopathy, or the like.
2-PHENYLTHIOPHENE DERIVATIVE
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Page/Page column 16, (2008/06/13)
The present invention relates to a 2-phenylthiophene derivative or a salt thereof, wherein the thiophene ring is substituted with a carboxyl group or the like and the benzene ring has an electron-withdrawing group such as a cyano group and an electron-donating group such as a substituted alkoxy group at the same time. Since the compound of the invention has good xanthine oxidase-inhibitory action and uric acid-lowering action and does not have a structure derived from nucleic acid, the compound has advantages of high safety and excellent effects as compared with conventional compounds and is useful as a therapeutic or preventive agent for hyperuricemia, gout, inflammatory bowel diseases, diabetic kidney diseases, diabetic retinopathy, or the like.
Substituted compounds derived from N-(benzyl)phenylacetamide, preparation and uses
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Page/Page column 41, (2010/10/20)
This invention relates to poly-substituted derivatives of the N-(benzyl)phenylacetamide type, pharmaceutical compositions comprising same, therapeutic uses thereof, more particularly in the fields of human and animal health. This invention also relates to a process for the preparation of such derivatives.