- Acid secretion inhibitor
-
The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
- -
-
Page/Page column 50
(2008/06/13)
-
- Synthesis of C-14 and C-13, H-2-labeled IKK inhibitor: [14C] and [13C4,D3]-N-(6-chloro-7-methoxy-9H-pyrido3,4- blindol-8-yl)-2-methyl-3-pyridinecarboxamide
-
[14C]-N-(6-Chloro-7-methoxy-9H-pyrido [3,4-b]indol-8-yl)-2- methyl-3-pyridinecarboxamide (5B), an IKK inhibitor, was synthesized from [ 14C]-barium carbonate in two steps in an overall radiochemical yield of 41%. The intermediate, [carboxyl-14C]-2-methylnicotinic acid, was prepared by the lithiation and carbonation of 3-bromo-2-methylpyridine. [ 13C4,D3]-N-(6-chloro-7-methoxy-9H-pyrido[3,4-b] indol-8-yl)-2-methyl-3-pyridinecarboxamide (5C) was synthesized from [1,2,3,4-13C4]-ethyl acetoacetate and [D 4]-methanol in six steps in an overall yield of 2%. [ l3C4]-2-methylnicotic acid, was prepared by condensation of [13C4]-ethyl 3-aminocrotonate and acrolein, followed by hydrolysis with lithium hydroxide. Copyright
- Li, Yuexian,Plesescu, Mihaela,Prakash, Shimoga R.
-
p. 789 - 799
(2007/10/03)
-
- Novel 3beta-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof
-
The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a bicyclic fused heteroaromatic, such as thieno[2,3-b]pyridine, furo[2,3-b]pyridine, thieno[3,2-b]pyridine, furo[3,2-b]pyridine, thieno[2,3-b]pyrazine, furo[2,3-b]pyrazine, thieno[2,3-c]pyridine, furo[2,3-c]pyridine, thieno[3,2-c]pyridine and furo[3,2-c]pyridine; R1 represents a linear or branched C1-C6 alkoxy group, a linear or branched C1-C6 alkylthio group; R2 represents a linear, branched, cyclic C2-C8 group, a 2- or 3- thienylmethyl group, or a benzyl group optionally substituted by one or several halogens, F, Cl, Br, I, C1-C4 alkyl, C1-C4 alkoxy, CF3, CN, NO2, OH; and their pharmaceutically acceptable salts. Said compounds are anti-dopaminergic agents.
- -
-
Page/Page column 6
(2010/02/11)
-
- Nucleophilic addition to 3-substituted pyridinium salts: Expedient syntheses of (-)-L-733,061 and (-)-CP-99,994
-
(Chemical Equation Presented) The addition of nucleophiles to 3-substituted pyridinium salts prepared from N-methylbenzamide and various pyridines has been investigated. Good to excellent regioselectivities favoring the 2,3-disubstituted 1,2-dihydropyridines were observed. The resulting 1,2-dihydropyridines led to the corresponding 2,3-disubstituted pyridines upon treatment with Mn(OAc)3/NaIO4. This methodology was also successfully applied to the enantioselective syntheses of (-)-L-733,061 and (-)-CP-99,994, two members of a new class of highly potent, nonpeptide, Substance P antagonists.
- Lemire, Alexandre,Grenon, Michel,Pourashraf, Mehrnaz,Charette, Andre B.
-
p. 3517 - 3520
(2007/10/03)
-