- With insecticidal or acaricidal activity of the 2 - phenyl nicotinic acid derivatives (by machine translation)
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The invention belongs to the field of agricultural insecticidal agents. In particular relates to a with insecticidal or acaricidal activity of the 2 - phenyl nicotinic acid derivatives. Compound such as shown in formula I: in the formula of each substitue
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Paragraph 0223; 0224; 0225
(2017/04/28)
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- HETEROCYCLIC AMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS
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The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, R4, R5, X, Y and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
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Page/Page column
(2014/06/24)
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- HETEROCYCLIC AMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS
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The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, R4, R5, X, Y and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
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Page/Page column 746
(2013/03/26)
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- 2-PHENYLNICOTINIC ACID DERIVATIVE
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The present invention is to provide the compounds useful as a treating or preventing agent for gout and hyperuricemia which are 2-phenylnicotinic acid derivatives having a uric acid lowering action due to an excellent xanthine oxidase inhibitory action. Since the 2-phenylnicotinic acid derivatives of the present invention exhibit a uric acid lowering action due to an excellent xanthine oxidase inhibitory action and also hypolipemic action, their utility is very high as a treating or preventive agent for gout and hyperuricemia which are often accompanied by hyperlipemia as a complication.
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Page/Page column 8
(2009/12/23)
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- Isoxazole derivatives
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An isoxazole compound having the following formula: wherein R1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R2 represents an amino; m is 1; n is 1 to 6; ring A represents a phenyl ring or a naphthyl ring; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.
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- Processes for producing 2-Halo-nicotinic acid derivatives and precursors thereto
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Disclosed are preferred processes for the preparation of 2-halo-nicotinic acid derivatives of formula (IV): STR1 by cyclocondensation of a 4-halo-4-cyanocarbonyl compound of formula (III): STR2 wherein X is Cl or Br; Y is a carbonyl group and R1, R2 and R3 are each, independently, H, Cl, Br or an organic radical. Further preferred aspects include the preparation of the above-noted 4-halo-4-cyanocarbonyl compound via Michael addition of a 2-halonitrile with an α,β-unsaturated aldehyde or ketone, and the preparation of the 2-halonitrile by redistribution of halogen between a 2,2-dihalonitrile and a parent nitrile.
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- Versatile synthesis of 6-substituted 8-deazapteridine-2,4-diamines. Formal total synthesis of 8,10-dideazaminopterin
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A new synthesis of 4-amino-4-deoxy-8,10-dideazapteroic acid (11d) and 6-substituted and 5,6-anellated 8-deazapteridine-2,4-diamines, 10a, 10d, 25, is described. Starting from keteneaminals 1 or 12 and enaminones 4 or β-aminoketone 17 the title compounds can be prepared via functional group transformation of 2-amino-3-nitropyridines 5 or nicotinate 13a yielding 3-amino-α-picolinonitriles 9 which are cyclocondensed with guanidine.
- Troschutz,Karger
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p. 1815 - 1821
(2007/10/03)
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- Regioselective synthesis of 2-chloro 3-pyridinecarboxylates
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2-Chlorocyanoacetate was found to undergo base-catalyzed Michael addition to α,β-unsaturated ketones or aldehydes to afford 5-oxopentenenitrile derivatives. In the presence of anhydrous HCl, these compounds cyclize to yield 2-chloro-3-pyridinecarboxylates. The process is highly regiospecific and useful in the synthesis of 2,3-disubstituted pyridines.
- Zhang,Stout,Keay,Scriven,Toomey,Goe
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p. 13177 - 13184
(2007/10/03)
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- GENERAL ROUTES TO 4-OXO-4H-PYRANOPYRIDINE-3-CARBOXYLATES AND RELATED COMPOUNDS: SYNTHESIS OF THE OXYGEN AND SULFUR ISOSTERES OF NALIDIXIC ACID
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Imidazolides of 2-hydroxy- and 2-mercaptonicotinic acids with LiCH2CO2Bu-t gave ketoesters which were cyclised with MeOCH=NMe2+ MeOSO3- and i-Pr2NEt or with (RCO)2O-NEt3-DMAP to the title 2-H or 2-R bicyclic esters; the corresponding
- McCombie, Stuart W.,Lin, Sue-Ing,Tagat, Jayaram R.
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- Angiotensin II receptor antagonists
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Compounds are disclosed having the formula: STR1 The compounds of the invention are angiotensin II receptor antagonists.
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