- BENZODIAZEPINE DERIVATIVE AND METHOD OF PRODUCING THE SAME
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In a benzodiazepine derivative and a method of producing the derivative, isatoic anhydride or 5-chloroisatoic anhydride is reacted with amino acid ester hydrochloride for conducting a simple cyclization to obtain a produce with a low percentage of by-prod
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Paragraph 0016; 0045; 0046
(2015/09/28)
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- Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT 2C receptor
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Evaluation of selected compounds from our Corporate Compound Library in a human 5-HT2C receptor binding assay led to the discovery of WAY-629, a cyclohexyl[b][1,4]benzodiazepinoindole (Ki 56nM, Emax 90%), which is selectiv
- Sabb, Annmarie L.,Vogel, Robert L.,Welmaker, Gregory S.,Sabalski, Joan E.,Coupet, Joseph,Dunlop, John,Rosenzweig-Lipson, Sharon,Harrison, Boyd
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p. 2603 - 2607
(2007/10/03)
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- A novel one step approach to the synthesis of 3H-1,4-benzodiazepin-(1H,4H)-2,5-diones from 1,2,3-benzotriazin-4-(3H)-one
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1,2,3-Benzotriazin-4-(3H)-one(3) and its 6-chloro derivative (4) on thermal condensation with α-amino acids yielded 3H-1,4-benzodiazepin-(1H,4H)-2,5-diones(7-12) in moderate to good yield. The cyclocondensation is believed to proceed through the formation of an iminoketene intermediate (5).
- Gupta, Renu,Sirohi, Reenu,Shastri, Sudha,Kishore
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p. 363 - 366
(2007/10/03)
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- Glycine receptor antagonist pharmacophore
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Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer''s disease, amyotrophic lateral sclerosis, Huntington''s disease and Down''s syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a compound which has high binding to the glycine receptor.
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- New Synthesis of Diazepam
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An efficient preparation of 7-chloro-1-methyl-3,4-dihydro-1H-1,4-benzodiazepine-2,5-dione from 5-chloro-N-methylisatoic anhydride and glycine has been devised, and from it, by the action of phenylmagnesium chloride on its N-acetyl-derivative followed by treatment with hydroxylamine and cleavage of the resulting desacetyl oxime with sodium bisulfite, diazepam has been synthesized.The overall yield is about 50percent from 5-chloroisatoic anhydride.
- Gates, Marshall
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p. 1675 - 1681
(2007/10/02)
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