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Thur Y.,Nycomed Pharma Pvt. Ltd | Bhalerao A.,Nycomed Pharma Pvt. Ltd | Munshi Z.,Nycomed Pharma Pvt. Ltd | Pansare N.,Nycomed Pharma Pvt. Ltd | And 17 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

SAR studies were performed on a series of 2-arylamido-5,7-dihydro-4H- thieno[2,3-c]pyran-3-carboxamide derivatives as cannabinoid receptor agonists. Starting from a HTS hit both potency and selectivity could be improved. Modifications to the thiophene fusion and C-3 amides were studied. A representative compound 3t produced analgesia when dosed orally in inflammatory pain models of writhing and carrageenan-induced allodynia. © 2012 Elsevier Ltd. All rights reserved. Source

Velankar A.D.,Nycomed Pharma Pvt. Ltd | Quintini G.,Nycomed GmbH | Prabhu A.,Nycomed Pharma Pvt. Ltd | Weber A.,Nycomed GmbH | And 12 more authors.
Bioorganic and Medicinal Chemistry | Year: 2010

Interleukin-2 inducible T-cell kinase (ITK) is one of five kinases that belong to the Tec kinase family that plays an important role in T-cell and mast cell signaling. Various reports point to a role of ITK in the treatment of allergic asthma. For example, it was shown that mice lacking ITK have reduced airway hyperresponsiveness, inflammation and tracheal responses in an allergic asthma model. In this article, we disclose novel ITK inhibitors based on (4 or 5-aryl)pyrazolyl-indole scaffold that were also found to be selective for ITK over other kinases like IRK, CDK2, GSK3ß and PKA. © 2010 Elsevier Ltd. All rights reserved. Source

Padiya K.J.,Nycomed Pharma Pvt. Ltd | Gavade S.,Nycomed Pharma Pvt. Ltd | Kardile B.,Nycomed Pharma Pvt. Ltd | Tiwari M.,Nycomed Pharma Pvt. Ltd | And 6 more authors.
Organic Letters | Year: 2012

The first "In Water" imidazolecarbonylation of amine is described. A one pot reaction of carbonylimidazolide in water with a nucleophile provides an efficient and general method for the preparation of urea, carbamates and thiocarbamates. Use of an anhydrous solvent and an inert atmosphere could be avoided. Product precipitate out from the reaction mixture and can be obtained in high purity by filtration, resulting in a simple and scalable method. © 2012 American Chemical Society. Source

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