- Exploring SAR features in diverse library of 4-cyanomethyl-pyrazole-3-carboxamides suitable for further elaborations as CB1 antagonists
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A chemically diverse library of secondary and tertiary 4-cyanomethyl-1,5-diphenyl-1H-pyrazole-3-carboxamides was synthesized to enable mapping of the SAR, in the eastern amide region, with regard to CB1 antagonist activity, This study was initiated as a prelude to the design and synthesis of possible CB1 antagonists that do not readily pass the blood-brain-barrier. In general a range of modifications were found to be tolerated in this part of the molecule, although polar and especially charged groups did to a degree reduce the CB1 antagonistic activity. Several compounds with single-digit or even sub-nanomolar potency, suitable for further elaboration of the nitrile moiety, were identified.
- Cooper, Martin,Receveur, Jean-Marie,Bjurling, Emelie,Norregaard, Pia K.,Nielsen, Peter Aadal,Skoeld, Niklas,Hoegberg, Thomas
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scheme or table
p. 26 - 30
(2010/03/04)
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- CANNABINOID RECEPTOR MODULATORS
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Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein:X is a bond, or a divalent radical selected from -C(R10)(R11)-*, -C(R10)(R11)
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Page/Page column 39
(2009/07/17)
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- CB1 RECEPTOR MODULATORS
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Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention
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Page/Page column 34
(2008/12/06)
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