17617-05-9Relevant articles and documents
PROKINETICIN 1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PAIN
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Page/Page column 48, (2012/01/13)
Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: wherein A1, L1, D, and Q are defined herein.
Prokineticin 1 receptor antagonists
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Page/Page column 49-50, (2008/12/04)
The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.
PROKINETICIN 2 RECEPTOR ANTAGONISTS
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Page/Page column 127, (2010/11/28)
The present invention relates to certain novel compounds of Formula (I): and methods for the treatment of prokineticin 2 or prokinetin 2 receptor mediated disorders.
Inhibition of human cytomegalovirus protease N(o) with monocyclic β- lactams
Deziel,Malenfant
, p. 1437 - 1442 (2007/10/03)
Monocyclic β-lactams have been identified as potent and selective inhibitors of the human cytomegalovirus protease (HCMV) N(o). Two series of these inhibitors are described, a peptidyl series of compounds and non- peptidic molecules featuring lower molecular weights. The SAR work that lead to the discovery of these inhibitors, together with their synthesis is also disclosed.
Synthesis and Biological Activity of trans-(+/-)-N-Methyl-2-(3-pirydyl)-2-tetrahydrothiopyrancarbothioamide 1-Oxide (RP 49356) and Analogues: A New Class of Potassium Channel Opener
Brown, Thomas J.,Chapman, Robert F.,Cook, David C.,Hart, Terance W.,McLay, Iain M.,et al.
, p. 3613 - 3624 (2007/10/02)
The synthesis and biological activity of trans-(+/-)-N-methyl-2-(3-pyridyl)-2-tetrahydrothiopyrancarbothioamide 1-oxide (8a, RP 49356) and analoques is reported.These compounds constitute a new structural class of K+-channel opener.The effects of changes in the pyridyl group, thioamide, and thiane ring on in vitro K+-channel opening activity are discussed.A 3-pyridyl or 3-quinolyl group, a small N-alkyl thioamide function, and a thiane oxide ring, in which the sulfoxide is in a trans relationship to thioamide, are preferred for activity.Selected compounds were tested intravenously in the normotensive anaesthetized rat for hypotensive effects, and the activities reflect their in vitro K+-channel opening activity.This led to further evaluation of compound 8a and the selection of the (-)-enantiomer 8b (RP 52891) for development as an antihypertensive and antianginal agent.
ALKYLAMIDE DERIVATIVES WITH H2-RECEPTOR ANTAGONISTIC AND CYTOPROTECTIVE ACTION
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, (2008/06/13)
Alkylamide derivatives having the formula, These compounds have a strong antiulcer action depend on histamine H 2-receptor antagonistic action and a cytoprotective action upon gastric mucous membrance.
Synthesis and Antisecretory and Antiulcer Activities of Derivatives and Analogues of 2-(2-Pyridyl)tetrahydrothiophene-2-carbothioamide
Aloup, Jean-Claude,Bouchaudon, Jean,Farge, Daniel,James, Claude,Deregnaucourt, Jean,Hardy-Houis, Monique
, p. 24 - 29 (2007/10/02)
New thioamide derivatives of 2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide (29) and related compounds (in which the tetrahydrothiophene ring was replaced by tetrahydrothiopyran, tetrahydrofuran, 1,3-dithiane, or 1,3-oxathiane and where the pyridine ring was repleaced by other nitrogen heterocycles) were synthesized and tested for their antisecretory and antiulcer activities.These thioamides were prepared according to one of the following methods: (i) reaction of an isothiocyanate with the carbanion of the corresponding cyclic precursor (for secondary thioamides); (ii) reaction of ammonia or an amine with the dithio ester prepared from the same precursor (for primary, secondary, and tertiary thioamides).These thioamides were evaluated by the Shay method to measure their antisecretory activity and by the stress-induced-ulcer method to test their antiulcer activity.Structure-activity relationships are discussed.N-Methyl-2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide (R.P. 40749,30) exhibited activities that were at least 10 times higher than those reported for cimetidine.
ACTIVITE ESTEROLYTIQUE DE COMPOSES ASSOCIANT UNE FONCTION THIOL ET UNE BASE HETEROCYCLIQUE. EXEMPLES DE PROCESSUS BIFONCTIONNEL
Brembilla, Alain,Roizard, Denis,Lochon, Pierre
, p. 577 - 588 (2007/10/02)
The synthesis of 19 compounds associating a thiol function and a basic heterocycle (i.e. benzimidazole, pyridine, thiazole) is described.Their esterolytic activity towards para nitrophenyl acetate (PNPA) is compared with that of simple monofunctional thiols.The influence of the substituents and of the nature of the basic heterocycle shows that the apparition of a cooperative effect depends both on the relative pKa values (thiol and heterocyclic) and on the possibility of proton exchange via the heterocyclic moiety.Examples of bifonctional process are reported in the case of benzimidazolylmethanethiol compounds, due to a basic assistancce on the neutral form of the thiol function.