- Design, synthesis and pharmacological evaluation of indolylsulfonamide amines as potent and selective 5-HT6 receptor antagonists
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A series of N′-[3-(indole-1-sulfonyl) aryl]-N,N-dimethyl ethane-1,2-diamines and N′-[3-(indole-1-sulfonyl) aryl]-N,N-dimethyl propane-1,3-diamines was designed and synthesized as 5-HT6 receptor ligands. These compounds, when screened in a functional reporter gene-based assay, displayed potent antagonistic activity with Kb values in the range of 1.8-60 nM. The lead compound 9y has shown good ADME surrogate properties, acceptable pharmacokinetic profile and is active in animal models of cognition like novel object recognition test and Morris water maze. It was selected for detailed profiling.
- Nirogi, Ramakrishna V. S.,Bandyala, Thrinath Reddy,Reballi, Veena,Konda, Jagadishu Babu,Daulatabad, Anand V.,Khagga, Mukkanti
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- Aminoaryl sulphonamide derivatives as functional 5-HT6 ligands
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The present invention provides aminoaryl sulphonamide derivatives of formula (I), useful in the treatment of a CNS disorder related to or affected by the 5-HT6 receptor. Pharmacological profiles of these components include high affinity binding with 5-HT6 receptors along with good selectivity towards the receptor. The present invention also includes stereoisomers, the salts, methods of preparation and medicine containing the aminoaryl sulphonamide derivatives.
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Page/Page column 8
(2010/07/08)
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- AMINOARYL SULPHONAMIDE DERIVATIVES AS FUNCTIONAL 5-HT6 LIGANDS.
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The present invention provides aminoaryl sulphonamide derivatives of formula (I), useful in the treatment of a CNS disorder related to or affected by the 5-HTg receptor. Pharmacological profile of these compounds includes high affinity binding with 5-HTg receptor along with good selectivity towards the said receptor. The present invention also includes the stereoisomers, the salts, methods of preparation and medicine containing the said aminoaryl sulphonamide derivatives.
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Page/Page column 18
(2010/11/26)
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- PREVENTIVES/REMEDIES FOR POSTOPERATIVE STRESS
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The present invention provides pharmaceutical composition for prophylaxis or/and therapy of a postoperative stress, which comprises a CRF antagonist.
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