- Phenacylation of 6-methyl-beta-nitropyridin-2-ones and further heterocyclization of products
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Reaction between the derivatives of 6-methyl-beta-nitropyridin-2-one and phenacyl bromides was studied, and the yields observed were extremely low. The pyridones were converted via chloropyridines to methoxyderivatives, which were N-phenacylated. N-Phenacyl derivatives of 4,6-dimethyl-5-nitropyridin-2-one under the action of base gave 5-hydroxy-8-nitroindolizine and under acidic conditions gave 5-methyl-6-nitrooxazole[3,2-a]pyridinium salt, which underwent recycization with MeONa to 5-methoxy-8-nitroindolizine.
- Babaev, Eugene V.,Rybakov, Victor B.
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- COMBINATION OF AN AZETIDINE LPA1 RECEPTOR ANTAGONIST WITH PIRFENIDONE AND/OR NINTEDANIB FOR USE IN THE TREATMENT OF FIBROTIC DISEASES
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The present invention concerns the compounds of formula (I) wherein R1, R2, R3, X, and Y are as described in the description, and their use as antagonists of the LPA1 receptor, in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s); such as especially pirfenidone and/or nintedanib, in the prevention and/or treatment of fibrotic diseases. The invention further relates to pharmaceutical compositions comprising the compounds of formula (I) in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s) such as pirfenidone or nintedanib.
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Page/Page column 26; 29
(2021/06/11)
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- ALKOXY-SUBSTITUTED PYRIDINYL DERIVATIVES AS LPA1 RECEPTOR ANTAGONISTS AND THEIR USE IN THE TREATMENT OF FIBROSIS
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The present invention relates to pyridinyl derivatives of Formula (I) Formula (I) wherein R1, R2, R3, R4, R5, R6, Ar1, L, W, Z, m and n are as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of Formula (I), and especially to their use as LPA1 receptor modulators.
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Page/Page column 55; 57
(2019/12/28)
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- PYRIMIDINE SIGMA-COMPLEXES. 7. THE RECYCLIZATION OF 5-NITROPYRIMIDINE AND ITS METHOXY DERIVATIVES UPON REACTION WITH THE ACETYLACETONE CARBANION
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A study was carried out on the reaction of 5-nitro and 5-nitromethoxypyrimidines with the acetylacetone carbanion.Benzene and pyridine derivatives are formed as a result of recyclization.The direction of the reaction depends on the position of the substituents in the pyrimidine ring and the nature of the bases.
- Remennikov, G. Ya.,Kurilenko, L. K.,Boldyrev, I. V.,Cherkasov, V. M.
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p. 422 - 425
(2007/10/02)
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