23772-87-4Relevant academic research and scientific papers
MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
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, (2021/02/19)
This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR), pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis using such modulators and pharmaceutical compositions, and processes for making such modulators.
SMALL MOLECULE MODULATORS OF IL-17
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, (2021/12/31)
The present invention relates to a compound according to formula (I), (I) and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
AMINO-ACID ANILIDES AS SMALL MOLECULE MODULATORS OF IL-17
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, (2020/07/14)
The present invention relates to a compound according to formula I (I) and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia
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Page/Page column 82, (2008/06/13)
A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome and dyslipidemia.
New prolyl endopeptidase inhibitors: In vitro and in vivo activities of azabicyclo[2.2.2]octane, azabicyclo[2.2.1]heptane, and perhydroindole derivatives
Portevin, Bernard,Benoist, Alain,Rémond, Georges,Hervé, Yolande,Vincent, Michel,Lepagnol, Jean,De Nanteuil, Guillaume
, p. 2379 - 2391 (2007/10/03)
A series of potent and selective prolylendopeptidase (PEP) inhibitors of the α-keto heterocyclic type has been obtained by replacing the classical central proline of 1-[1-(4-phenylbutanoyl)-L-prolyl]pyrrolidine (SUAM 1221, 3) by non-natural amino acids PHI, ABO, and ABH. These 4-phenylbutanoyl side- chain-containing inhibitors exhibited potent in vitro inhibitory potencies with IC50 around 30 nM (compounds 24 and 25). Modulation of the side chain by replacement of the terminal phenyl ring by the dicyclopropyl moiety afforded derivatives 30 and 32 with improved potencies (IC50 between 10 and 20 nM). Furthermore, replacing the linear 4-phenylbutanoyl side chain by the (2-phenylcyclopropyl)carbonyl entity provided potent inhibitors with IC50 culminating at 0.9 nM on a rat cortex enzymatic preparation (compound 70). The configuration of the cyclopropyl ring had to be R,R in order to obtain not only a strong PEP inhibition in vitro but also a good activity in vivo, exemplified by inhibitor 68, which gave ID50 ip and po of 0.3 and 1 mg/kg, respectively. Finally, demonstration of the cognition-enhancing properties of compound 54 was given in the passive avoidance test using scopolamine- induced amnesia in the rat, where it dose dependently inhibited the scopolamine-induced decrease in avoidance response.
GUANIDINE COMPOUNDS
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, (2008/06/13)
A compound of formula (I): STR1 in which: R 1 represents substituted or unsubstituted phenyl or (C 3-C 7) cycloalkyl, R 2 represents trifluoromethyl or (C. sub.3-C 4) cycloalkyl,A represents--CH 2--,--CH=N--, . dbd.N--or--NH--,R 3 and R 4, which may be identical or different, represent hydrogen or linear or branched (C 1-C 6) alkyl or, with the nitrogen atoms to which they are attached, form a 5-or 6-membered heterocycle, R represents either hydrogen in the case where A=--CH 2--,--CH= N--or--NH--, or a bond of the group A when the latter is equal to = N--,its enantiomers and epimers as well as its addition salts with a pharmaceutically acceptable acid.
Synthesis of aldehydes by a one-carbon homologation of ketones and aldehydes via --α,β-unsaturated isocyanides
Moskal, Janusz,Leusen, Albert M. van
, p. 137 - 141 (2007/10/02)
Ketones and aldehydes react via a Wittig-Horner-Emmons reaction using diethyl(isocyanomethyl)phosphonate to form α,β-unsaturated isocyanides (4), which are either hydrolyzed as such, under acid conditions, or hydrolyzed after oxidation to α,β-unsaturated isocyanates (6) to give aldehydes containing one additional carbon atom.The scope of the reaction is demonstrated by 20 examples.
