- THERAPEUTIC COMPOUNDS
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The present invention relates to compounds that are Nrf2 activators. The compounds have the structural formula I defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with Nrf2 activation.
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Paragraph 00357-00358
(2020/06/10)
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- A facile synthesis of amide derivatives of [1,2,4]triazolo[4,3-a]pyridine
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A facile synthesis for preparation of amide derivatives of [1,2,4]triazolo[4,3-a]pyridine can be achieved by the nucleophilic displacement of chloromethyl derivative with methyl amine followed by the reaction with acid analogues in the presence of 1-[bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxide hexafluorophosphate (HATU). Reaction of 2-chloropyridine with hydrazine hydrate (99 %) gave 2-hydrazinopyridine (2). Compound 3 was obtained in good yields by treating 2-hydrazinopyridine with chloroacetyl chloride. Further 3-chloromethyl-[1,2,4]triazolo[4,3-a]pyridine (4) is obtained by treatment of compound 3 with POCl3. Nucleophilic displacement of compound 4 with methyl amine gave methyl-[1,2,4]triazolo[4,3-a]pyridin-3-ylmethyl-amine (5). Finally protecting and deprotecting of compound 5 with Boc anhydride and HCl in dioxane gives hydrochloride salt of compound 5 i.e. (6) The reaction of hydrochloride salt of methyl-[1,2,4]triazolo[4,3-a]pyridin-3-ylmethyl-amine with 10 different acids yields amide analogues.
- Gandikota, N. Murthy,Bolla, R. Sekhar,Viswanath, I. V. Kasi,Bethi, Sridharreddy
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p. 1920 - 1924
(2017/07/27)
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- NOVEL 2-(PIPERAZIN-1-YL)- AND 2-([1,4]DIAZEPAN-1-YL)- IMIDAZO[4,5-D]PYRIDAZIN-4-ONE, PRODUCTION AND USE THEREOF AS MEDICAMENT FOR THE TREATMENT OF DIABETES MELLITUS
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The invention relates to substituted imidazo[4,5-d]pyridazin-4-ones of general formula (I), in which R1 to R3 and n are as defined in claims 1 to 8, the tautomers, enantiomers, diastereomers, mixtures and salts thereof which have useful pharmacological properties, in particular, an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
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Page/Page column 24
(2010/02/12)
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