- Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent
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A series of novel benzamide derivatives, altering the 4-fluorophenylalkyl moiety in cisapride, were synthesized as 5-HT4 receptor agonists, and SAR of these analogs was examined on in vitro and in vivo prokinetic activities. These compounds were synthesized for high 5-HT4 receptor binding affinities and low hERG affinities. Several types of analogs were obtained and screened for 5-HT4 binding, hERG blocking, agonism, and gastric emptying assessment. Among the analogues, compound 23g showed promising results compared with the other analogs with respect to gastric emptying rates in rats. Therefore, we suggest that it may be a clinical candidate for the development of a potent prokinetic agent to treat GI disorders.
- Park, Jung Sang,Im, Weonbin,Choi, Sunghak,Park, Sook Jin,Jung, Jun Min,Baek, Ki Seon,Son, Han Pyo,Sharma, Satyasheel,Kim, In Su,Jung, Young Hoon
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- NOVEL BENZAMIDE DERIVATIVES AND PROCESS FOR THE PREPARTION THEREOF
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The present invention provides a novel benzamide derivative represented by formula 1 and an isomer, a pharmaceutically acceptable salt or hydrate thereof, and a composition for activating a 5-HT4 receptor comprising the same, as an active ingredi
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Page/Page column 8
(2010/05/13)
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- MODULATORS OF MUSCARINIC RECEPTORS
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The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
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Page/Page column 43-44
(2008/06/13)
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- NOVEL BENZAMIDE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
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The present invention provides a novel benzamide derivative represented by formula 1 and an isomer, a pharmaceutically acceptable salt or hydrate thereof, and a composition for activating a 5-HT4 receptor comprising the same, as an active ingre
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Page/Page column 19
(2008/12/07)
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- Modulators of muscarinic receptors
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The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
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Page/Page column 118
(2010/11/29)
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- SPIRO CONDENSED PIPERIDNES AS MODULATORS OF MUSCARINIC RECEPTORS
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The present invention relates to modulators of muscarnic receptors of formula (I). The present invention also provides impositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
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Page/Page column 43-44
(2008/06/13)
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- MODULATORS OF MUSCARINIC RECEPTORS
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The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
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Page/Page column 80; 81
(2010/10/20)
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- MODULATORS OF MUSCARINIC RECEPTORS
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The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
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Page/Page column 67-68
(2010/11/08)
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- Antipicornaviral pyridazinamines
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Piperidinyl, pyrrolidinyl, azepinyl and piperazinyl pyridazines of formula STR1 wherein one or two carbon atoms of the STR2 moiety may be substituted with C1-4 alkyl, C1-4 alkyloxy or two carbon atoms of the CH2 groups of said moiety may be bridged with a C2-4 alkanediyl radical; X represents CH or N; R1 represents hydrogen, C1-4 alkyl, halo, hydroxy, trifluoromethyl, cyano, C1-4 alkyloxy, C1-4 alkylthio, C1-4 alkylsulfinyl, C1-4 alkylsulfonyl, C1-4 alkyloxycarbonyl, C1-4 alkylcarbonyl or aryl; R2 and R3 each independently represent hydrogen or C1-4 alkyl; Alk represents C1-4 alkanediyl; R4 and R5 each independently represent hydrogen, C1-4 alkyl or halo; and Het represents STR3 the addition salts and stereochemically isomeric forms thereof, said compounds having antipicornaviral activity. Pharmaceutical compositions containing these compounds as active ingredient, and a method of preparing said compounds and pharmaceutical compositions.
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- Saturated heterocyclic carboxamide derivatives
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A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity. STR1
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- 2-((4-piperidyl)methyl)benzofuro(2,3-C)pyridine derivatives, and their application in therapy
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A compound of formula (I) STR1 in which R is a benzyl, benzoyl, 3-chlorobenzoyl, 3-methylbenzoyl or (C1 -C6 alkoxy)carbonyl group, or a pharmacologically acceptable acid addition salt thereof.
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