| Title: | Novel Pyrroles as Nicotinic Acetylcholine Receptor Modulators | ||
| Patent/Patent Application Number: | WO 2012131576 A1 | Publication Date: | October 4, 2012 |
| Priority Application: | IN 2011-KO458 | Priority Date: | March 31, 2011 |
| Inventors: | Sinha, N.; Jana, G.; Tilekar, A. R.; Karche, N. P.; Palle, V. P.; Kamboj, R. K. | ||
| Assignee Company: | Lupin Limited, India | ||
| Disease Area: | Neurodegenerative Disease | Biological Target: | Nicotinic Acetylcholine Receptor α7 Subunit (α7 nAChR) |
| Summary: | The patent application claims pyrrole derivatives as modulators of the nicotinic acetylcholine receptor for the treatment of neurodegenerative disorders including Alzheimer's disease and Parkinson's disease. | ||
| Important Compound Classes: |  |
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| Key Structures: |  |
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| Biological Assays: | Compounds were tested in a cell-based real-time kinetic assay in human IMR-32 cells with native expression of α7 nAChR. | ||
| Pharmacological Data: | Compounds showed an increase in the activity (agonist response) between 20- and 25-fold at 1 μM concentration. No additional data were reported. | ||
| Claims: | Claims 12–16: Use of compounds for the treatment of a variety of diseases such as Huntingtons's disease, Alzheimer's disease, Parkinson's disease, dementia, cognitive impairment, ADHD, and inflammation. | ||
Author Present Address
† Adjunct Associate Professor, Department of Pharmacology and Physiology, Drexel University, College of Medicine, New College Building, 245 N. 15th Street, Philadelphia, PA 19102.
The authors declare no competing financial interest.