- Discovery of 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines as orally available g protein-coupled receptor 119 agonists
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GPR119 is a 7-transmembrane receptor that is expressed in the enteroendocrine cells in the intestine and in the islets of Langerhans in the pancreas. Indolines and 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines were discovered as G protein-coupled receptor 119
- Katamreddy, Subba R.,Carpenter, Andrew J.,Ammala, Carina E.,Boros, Eric E.,Brashear, Ron L.,Briscoe, Celia P.,Bullard, Sarah R.,Caldwell, Richard D.,Conlee, Christopher R.,Croom, Dallas K.,Hart, Shane M.,Heyer, Dennis O.,Johnson, Paul R.,Kashatus, Jennifer A.,Minick, Doug J.,Peckham, Gregory E.,Ross, Sean A.,Roller, Shane G.,Samano, Vicente A.,Sauls, Howard R.,Tadepalli, Sarva M.,Thompson, James B.,Xu, Yun,Way, James M.
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p. 10972 - 10994
(2013/02/25)
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- GPR119 AGONISTS FOR THE TREATMENT OF DIABETES AND RELATED DISORDERS
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The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly Type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.
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Page/Page column 80
(2010/11/29)
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- Synthesis of pyrrolopyrimidine CRF-R1 antagonists containing a tricyclic core via an intramolecular heck reaction
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A synthetic route to pharmaceutically important tricyclic pyrrolopyrimidines was developed. The method employs a palladium-mediated Heck cyclization as the critical step in the construction of the final six membered ring.
- Dyck, Brian,McCarthy, James R.
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p. 191 - 195
(2007/10/03)
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- CONDENSED N-HETEROCYCLIC COMPOUNDS AND THEIR USE AS CRF RECEPTOR ANTAGONISTS
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The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof (Formula (I)) wherein the dashed line may represent a double bond; R is aryl or heteroaryl, each of which m
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- CRF receptor antagonists and methods relating thereto
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CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein n, m, A, B, C, R, R1, R2and Ar are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same
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- CRF receptor antagonists and methods relating thereto
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CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein n, m, A, B, C, R, R1, R2and Ar are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same
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