1645-32-5Relevant articles and documents
Synthesis of?some?new substituted triazolo [4,3-a][1,4] benzodiazepine derivatives as?potent anticonvulsants
Narayana,Vijaya Raj,Ashalatha,Kumari, N. Suchetha
, p. 417 - 422 (2006)
Novel 8-chloro-6-(2-fluorophenyl)-1-(aryl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines (5a-f) were prepared by treating 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepine-2-thione with various aromatic acid hydrazides. The newly prepared compounds were characterized by spectral analysis. Compounds were tested for anticonvulsant activity. Four of the tested compounds such as 5a, 5d, 5e and 5f exhibited excellent anticonvulsant activity in comparison with standard drug, diazepam.
Preparation method of 7-chloro-5-(2-fluorophenyl)-3H-1, 4-benzodiazepin-2-methylamine
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Paragraph 0043-0044; 0046-0047; 0049-0050; 0052-0053, (2020/12/15)
The invention provides a preparation method of 7-chloro-5-(2-fluorophenyl)-3H-1, 4-benzodiazepin-2-methylamine, which comprises the following steps: (1) reacting 7-chloro-5-(2-fluorophenyl)-1, 3-dihydro-2H-1, 4-benzodiazepin-2-one with phosphorus pentasulfide to obtain 7-chloro-5-(2-fluorophenyl)-1, 3-dihydro-2H-1, 4-benzodiazepin-2-thione, and (2) enabling the 7-chloro-5-(2-fluorophenyl)-1, 3-dihydro-2H-1, 4-benzodiazepin-2-thione to react with a methylamine alcohol solution, so as to prepare the 7-chloro-5-(2-fluorophenyl)-3H-1, 4-benzodiazepin-2-methylamine. The preparation method providedby the invention is low in cost, mild in condition, safe in production, high in yield, stable and reliable in product quality, simple and convenient to operate and more suitable for industrial production.
PERIPHERALLY RESTRICTED GABA POSITIVE ALLOSTERIC MODULATORS FOR THE TREATMENT OF IRRITABLE BOWEL SYNDROME AND OTHER AILMENTS OF THE PERIPHERAL NERVOUS SYSTEM
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Paragraph 0131-0132, (2016/01/12)
The present invention provides compounds and compositions which are positive allosteric modulators of GABA-A receptors that selectively target the peripheral nervous system and organs of the body, and which do not pass through the blood-brain barrier. The compounds and compositions of the present invention are useful for treatment of diseases or disorders which are mediated by GABA-A neuronal activity, such as, for example, visceral pain, gut motility, irritable bowel syndrome, functional abdominal pain, functional idiopathic diarrhea, inflammatory bowel diseases, drug induced pain, bile salt malabsorption, lactase or other carbohydrate intolerance.