- OXADIAZOLES AS FUNGICIDES
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The present invention relates to novel oxadiazoles of Formula (I) wherein, R1, L1, A1, A2, A3, A4, L2 and R2 are as defined in the detailed description. The present in
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Page/Page column 91
(2020/05/15)
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- BENZYL-, (PYRIDIN-3-YL)METHYL- OR (PYRIDIN-4-YL)METHYL-SUBSTITUTED OXADIAZOLOPYRIDINE DERIVATIVES AS GHRELIN O-ACYL TRANSFERASE (GOAT) INHIBITORS
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The present invention relates to compounds of general formula (I), wherein the groups R1 and R2 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
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- Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: Synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4′-yl(oyl)] piperazines
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Among the different PLA2s identified to date, the group IIA secretory PLA2 (sPLA2 GIIA) is implied in diverse pathological conditions. In this work we describe the synthesis, inhibitory activities, and structure-activity relationships (SAR) of a new class of substituted piperazine derivatives. The in vitro fluorimetric assay using two groups of enzymes, GIB and GIIA, revealed several compounds as highly potent inhibitors (IC50 = 0.1 μM). The in vivo activity assessed by ip or per os administration in a carrageenan-induced edema test in rats showed that two compounds proved to be as potent as indomethacin (10 mg/kg).
- Boukli, Latifa,Touaibia, Mohamed,Meddad-Belhabich, Nadia,Djimde, Atime,Park, Chang-Ha,Kim, Jung-Joo,Yoon, Joo-Hyoung,Lamouri, Aazdine,Heymans, Francoise
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p. 1242 - 1253
(2008/09/17)
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- Novel inhibitor compounds specific of secreted non-pancreatic human a2phospholipase of group II
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The present invention relates to a compound of the following formula (I) and pharmaceutical compositions containing the compound of formula (I): wherein D, Y, A, B, p, q, W and R have the same meanings as defined in the specification.
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Page/Page column 4
(2010/02/11)
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- NOVEL AMIDE COMPOUNDS WITH MCH ANTAGONISTIC EFFECT AND MEDICAMENTS COMPRISING SAID COMPOUNDS
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The invention relates to amide compounds of general formula (I), in which the groups and residues A, B, b, W, X, Y, Z, R1, R2 and R3 have the meanings given in claim 1. The invention further relates to medicaments comprising at least one of said amides. Said medicaments are suitable for the treatment of metabolic disorders and/or eating disorders, in particular, obesity, bulimia, anorexia, hyperphagia, and diabetes as a result of the MCH receptor antagonism.
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Page/Page column 100
(2008/06/13)
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- New carboxamide compounds having melanin concentrating hormone antagonistic activity, pharmaceutical preparations comprising these compounds and process for their manufacture
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The present invention relates to carboxamide compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1, R2, R3 and k have the meanings given in claim 1. Moreover the invention relates to process for preparing the above mentioned carboxamides as well as pharmaceutical compositions containing at least one carboxamide according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
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Page/Page column 35
(2010/02/09)
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- Complete assignment of 1H and 13C NMR spectra of a set of sulphinyl and sulphonyl monomers toward poly(p-phenylenevinylene) precursors
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The complete assignment of the 1H and 13C NMR spectra of sulphinyl and sulphonyl monomers toward poly(p-phenylenevinylene) precursors is presented. For all compounds the same protocol could be used. Resonance assignments were achieve
- Van Breemen, Albert J. J. M.,Adriaensens, Peter J.,Issaris, Anna C. J.,De Kok, Margreet M.,Vanderzande, Dirk J. M.,Gelan, Jan M. J. V.
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p. 129 - 134
(2007/10/03)
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By anodic oxidation of paramethylbenzylsulfonate, ester and nitrite 1 in Et3N,3HF/CH3CN, regioselective functionalization at benzylic positions is obtained (benzylic fluorides 2 and acetamides 3 are formed). In order to examin the de
- Laurent, Eliane,Marquet, Bernard,Tardivel, Robert
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p. 3969 - 3980
(2007/10/02)
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