745048-07-1Relevant articles and documents
PIPERIDINE DERIVATIVES AND COMPOSITIONS FOR THE INHIBITION OF NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE (NAMPT)
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Page/Page column 124-125, (2013/02/27)
The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below: Formula (I)
RADIOLABELED COMPOUNDS AND METHODS THEREOF
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Page/Page column 170; 172, (2011/12/14)
The present invention relates to radiodiagnostic compounds, methods of making those compounds, and methods of use thereof as imaging agents for preferably a HA serotonin 5-HT1A receptor for use in PET or SPECT, preferably PET. Compositions comprising an imaging-effective amount of radiolabeled compounds are also disclosed. The present invention also relates to non-radiolabeled compounds, methods of making those compounds, and methods of use thereof to treat various neurological and/or psychiatric disorders.
PYRIDINYL DERIVATIVES COMPRISING A CYANOGUANIDINE OR SQUARIC ACID MOIETY
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Page/Page column 25, (2011/10/13)
The present application discloses compounds of the formula (I) wherein X = opt.subst. pyrid-3-yl or pyrid-4-yl; Q = opt.subst. Ci-6 alkylene or a single bond; Y is formula (i) wherein D is = N-CN, or formula (ii) B = is opt.subst. C1-6 alkylene; A = (formula) Z = -J-V, wherein J = -C(=0)-, -C(=O)-O, -S(=O)2-, -P(=O)(OR4)-, -C(=O)-NR4- and -C(=S)-NR4-, and V = opt.subst. C1-12-alkyl, opt.subst. C3-12-cycloalkyl, -[CH2CH2O]1-10-( opt.subst. C1-6-alkyl), opt.subst. C1-12- alkenyl, opt.subst. aryl, opt.subst. heterocyclyl, or opt.subst. heteroaryl; q = 0-2, and r = 0- 2; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor
Tahtaoui, Chouaib,Parrot, Isabelle,Klotz, Philippe,Guillier, Fabrice,Galzi, Jean-Luc,Hibert, Marcel,Ilien, Brigitte
, p. 4300 - 4315 (2007/10/03)
Following a recent description of fluorescence resonance energy transfer between enhanced green fluorescent protein (EGFP)-fused human muscarinic M1 receptors and Bodipy-labeled pirenzepine, we synthesized seven fluorescent derivatives of this antagonist in order to further characterize ligand-receptor interactions. These compounds carry Bodipy [558/568], Rhodamine Red-X [560/580], or Fluorolink Cy3 [550/570] fluorophores connected to pirenzepine through various linkers. All molecules reversibly bind with high affinity to M1 receptors (radioligand and energy transfer binding experiments) provided that the linker contains more than six atoms. The energy transfer efficiency exhibits modest variations among ligands, indicating that the distance separating EGFP from the fluorophores remains almost constant. This also supports the notion that the fluorophores may bind to the receptor protein. Kinetic analyses reveal that the dissociation of two Bodipy derivatives (10 or 12 atom long linkers) is sensitive to the presence of the allosteric modulator brucine, while that of all other molecules (15-24 atom long linkers) is not. The data favor the idea that these analogues might interact with both the acetylcholine and the brucine binding domains.