16019-30-0Relevant academic research and scientific papers
An improved synthesis of 4-chloro-7H-pyrrolo[2,3-d]pyrimidine
Zhang, Yu-Liu,Xu, Cheng-Tao,Liu, Ting,Zhu, Yong,Luo, Yu
, p. 638 - 642 (2018/08/17)
[Figure not available: see fulltext.] An improved seven-step synthesis of 4-chloro-7H-pyrrolo[2,3-d]pyrimidine from dimethyl malonate with 31% overall yield is described. The procedure is operationally simple and practical for the synthesis of the 4-chloro-7H-pyrrolo[2,3-d]pyrimidine building block.
ATROPISOMERISM FOR ENHANCED KINASE INHIBITOR SELECTIVITY
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Page/Page column 33, (2019/01/10)
The invention provides a series of conformationally stable and selective kinase inhibitors, and methods of using the kinase inhibitors. The effect of atropisomerism on kinase selectivity was assessed, finding improved selectivity compared to rapidly inter
Exploiting Atropisomerism to Increase the Target Selectivity of Kinase Inhibitors
Smith, Davis E.,Marquez, Isaac,Lokensgard, Melissa E.,Rheingold, Arnold L.,Hecht, David A.,Gustafson, Jeffrey L.
supporting information, p. 11754 - 11759 (2015/10/05)
Many biologically active molecules exist as rapidly interconverting atropisomeric mixtures. Whereas one atropisomer inhibits the desired target, the other can lead to off-target effects. Herein, we study atropisomerism as a possibility to improve the sele
CYCLOLIC HYDRAZINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS
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Page/Page column 61, (2013/09/26)
Compounds of Formula I are provided, including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: wherein Z is selected from the group consisting of: which are useful as HIV attachment inhibitors.
Discovery of 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines as orally available g protein-coupled receptor 119 agonists
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.
, p. 10972 - 10994 (2013/02/25)
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
FUSED BICYCLIC PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 33-34, (2011/06/19)
The present invention relates to Fused Bicyclic Pyrimidine Derivatives, compositions comprising a Fused Bicyclic Pyrimidine Derivative, and methods of using the Fused Bicyclic Pyrimidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.
AZAINDOLE P2X3 AND P2X2/3 MODULATORS
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Page/Page column 65-66, (2010/06/19)
The application discloses compounds of the Formula I: or a pharmaceutically acceptable salt thereof, wherein, X, R1, R2 R3, R4, R5, R6, R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS
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Page/Page column 76, (2010/04/03)
The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metaboli
BICYCLIC HETEROCYCLE DERIVATIVES AND THEIR USE AS GPCR MODULATORS
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Page/Page column 44, (2010/04/03)
The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic
BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 73, (2010/04/03)
The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication,
