Search Results - "Reinhart, Greg J"

Discovery of Sodium R-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (Elagolix), a Potent and Orally Available Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor by Chen, Chen, Wu, Dongpei, Guo, Zhiqiang, Xie, Qiu, Reinhart, Greg J, Madan, Ajay, Wen, Jenny, Chen, Takung, Huang, Charles Q, Chen, Mi, Chen, Yongsheng, Tucci, Fabio C, Rowbottom, Martin, Pontillo, Joseph, Zhu, Yun-Fei, Wade, Warren, Saunders, John, Bozigian, Haig, Struthers, R. Scott

“…The discovery of novel uracil phenylethylamines bearing a butyric acid as potent human gonadotropin-releasing hormone receptor (hGnRH-R) antagonists is…”
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Synthesis and Structure–activity relationships of 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor by Tucci, Fabio C., Zhu, Yun-Fei, Guo, Zhiqiang, Gross, Timothy D., Connors, Patrick J., Struthers, R.Scott, Reinhart, Greg J., Saunders, John, Chen, Chen

“…A new class of small molecule GnRH antagonists, the 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils, was designed and a novel stereoselective…”
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Species Selectivity of Nonpeptide Antagonists of the Gonadotropinreleasing Hormone Receptor Is Determined by Residues in Extracellular Loops II and III and the Amino Terminus by Reinhart, Greg J., Xie, Qiu, Liu, Xin-Jun, Zhu, Yun-Fei, Fan, Jun, Chen, Chen, Struthers, R. Scott

“…Efforts to develop orally available gonadotropin-releasing hormone (GnRH) receptor antagonists have led to the discovery of several classes of potent…”
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Overlapping, Nonidentical Binding Sites of Different Classes of Nonpeptide Antagonists for the Human Gonadotropin-Releasing Hormone Receptor by Betz, Stephen F, Reinhart, Greg J, Lio, Francisco M, Chen, Struthers, R. Scott

“…Peptide agonists and antagonists of the human gonadotropin-releasing hormone receptor (GnRH-R) are widely used to treat a range of reproductive hormone related…”
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Pharmacological Characterization of a Novel Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor, NBI-42902 by Struthers, R. Scott, Xie, Qui, Sullivan, Susan K, Reinhart, Greg J, Kohout, Trudy A, Zhu, Yun-Fei, Chen, Chen, Liu, Xin-Jun, Ling, Nicholas, Yang, Weidong, Maki, Richard A, Bonneville, Anne K, Chen, Ta-Kung, Bozigian, Haig P

“…Suppression of the hypothalamic-pituitary-gonadal axis by peptides that act at the GnRH receptor has found widespread use in clinical practice for the…”
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3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a Potent and Orally Active Antagonist of the Human Gonadotropin-Releasing Hormone Receptor. Design, Synthesis, and in Vitro and in Vivo Characterization by Tucci, Fabio C, Zhu, Yun-Fei, Struthers, R. Scott, Guo, Zhiqiang, Gross, Timothy D, Rowbottom, Martin W, Acevedo, Oscar, Gao, Yinghong, Saunders, John, Xie, Qiu, Reinhart, Greg J, Liu, Xin-Jun, Ling, Nicholas, Bonneville, Anne K. L, Chen, Takung, Bozigian, Haig, Chen

“…Further structure−activity relationship studies of a series of substituted uracils at the 1, 3, and 5 positions resulted in the discovery of several potent…”
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Determination of the Binding Mode of Thienopyrimidinedione Antagonists to the Human Gonadotropin Releasing Hormone Receptor Using Structure−Activity Relationships, Site-Directed Mutagenesis, and Homology Modeling by Betz, Stephen F, Lio, Francisco M, Gao, Yinghong, Reinhart, Greg J, Guo, Zhiqiang, Mesleh, Michael F, Zhu, Yun-Fei, Struthers, R. Scott

“…We have investigated the specific interactions of a series thienopyrimidinediones with the gonadotropin-releasing hormone receptor (GnRH-R). Competitive…”
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Species selectivity of nonpeptide antagonists of the gonadotropin-releasing hormone receptor is determined by residues in extracellular loops II and III and the amino terminus by Reinhart, Greg J, Xie, Qiu, Liu, Xin-Jun, Zhu, Yun-Fei, Fan, Jun, Chen, Chen, Struthers, R Scott

“…Efforts to develop orally available gonadotropin-releasing hormone (GnRH) receptor antagonists have led to the discovery of several classes of potent…”
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Design and Structure−Activity Relationships of 2-Alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as Potent GnRH Receptor Antagonists by Zhu, Yun-Fei, Guo, Zhiqiang, Gross, Timothy D, Gao, Yinghong, Connors, Patrick J, Struthers, R. Scott, Xie, Qiu, Tucci, Fabio C, Reinhart, Greg J, Wu, Dongpei, Saunders, John, Chen

“…SAR studies of 7-phenylpyrrolo[1,2-a]pyrimid-4-ones 1 and 2, and 2-phenylimidazolo[1,2-a]pyrimidines 3 and 4, as nonpeptide human GnRH receptor antagonists,…”
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3-(2-Aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl- uracils as Orally Bioavailable Antagonists of the Human Gonadotropin Releasing Hormone Receptor by Tucci, Fabio C, Zhu, Yun-Fei, Guo, Zhiqiang, Gross, Timothy D, Connors, Patrick J, Gao, Yinghong, Rowbottom, Martin W, Struthers, R. Scott, Reinhart, Greg J, Xie, Qiu, Chen, Ta Kung, Bozigian, Haig, Killam Bonneville, Anne L, Fisher, Andrew, Jin, Liping, Saunders, John, Chen

“…Uracils possessing N-3 side chains derived from various amino alcohols were designed and synthesized as potent human gonadotropin releasing hormone receptor…”
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Identification of 1-Arylmethyl-3- (2-aminoethyl)-5-aryluracil as Novel Gonadotropin-Releasing Hormone Receptor Antagonists by Zhu, Yun-Fei, Gross, Timothy D, Guo, Zhiqiang, Connors, Patrick J, Gao, Yinghong, Tucci, Fabio C, Struthers, R. Scott, Reinhart, Greg J, Saunders, John, Chen, Ta Kung, Killam Bonneville, Anne L, Chen

“…Based on SAR from bicyclic GnRH antagonists such as 6-aminomethyl-7-arylpyrrolo[1,2-a]pyrimid-4-ones (1) and 2-aryl-3-aminomethylimidazolo[1,2-a]pyrimid-5-ones…”
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Synthesis and initial structure–Activity relationships of a novel series of imidazolo[1,2- a]pyrimid-5-ones as potent GnRH receptor antagonists by Wilcoxen, Keith M., Zhu, Yun-Fei, Connors, Patrick J., Saunders, John, Gross, Timothy D., Gao, Yinghong, Reinhart, Greg J., Struthers, R.Scott, Chen, Chen

“…SAR studies of 2-arylimidazolo[1,2- a]pyrimid-5-ones 10a– m, which were derived from initial lead 3a, resulted in the discovery of a series of potent…”
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Synthesis and structure-activity relationships of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils as human GnRH receptor antagonists by ROWBOTTOM, Martin W, TUCCI, Fabio C, ZHU, Yun-Fei, ZHIQIANG GUO, GROSS, Timothy D, REINHART, Greg J, QUI XIE, STRUTHERS, R. Scott, SAUNDERS, John, CHEN CHEN

“…The synthesis of a series of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils is discussed. SAR around N-1 of the uracil was explored,…”
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Initial Structure–Activity Relationship Studies of a Novel Series of Pyrrolo[1,2- a]pyrimid-7-ones as GnRH Receptor Antagonists by Zhu, Yun-Fei, Struthers, R.Scott, Connors, Jr, Patrick J., Gao, Yinghong, Gross, Timothy D., Saunders, John, Wilcoxen, Keith, Reinhart, Greg J., Ling, Nicholas, Chen, Chen

“…Initial SAR studies on 1-aminomethyl-2-aryl-3-cyano-pyrrolo[1,2- a]pyrimid-7-one-6-carboxylates as human GnRH receptor antagonists were discussed…”
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A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2- a]pyrimid-4-ones as potent, stable GnRH receptor antagonists by Tucci, Fabio C., Zhu, Yun-Fei, Guo, Zhiqiang, Gross, Timothy D., Connors, Patrick J., Struthers, R.Scott, Reinhart, Greg J., Wang, Xiaochuan, Saunders, John, Chen, Chen

“…A new class of small molecule GnRH antagonists, the 7-aryl-8-fluoro-pyrrolo[1,2- a]pyrimid-4-ones, was designed and a novel synthesis for these compounds was…”
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Synthesis and Structure–Activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists by Guo, Zhiqiang, Zhu, Yun-Fei, Tucci, Fabio C., Gao, Yinghong, Struthers, R.Scott, Saunders, John, Gross, Timothy D., Xie, Qiu, Reinhart, Greg J., Chen, Chen

“…The novel synthesis and SAR studies of 6-methyluracils as human GnRH receptor antagonists are discussed. Introduction of a small methyl substituent at the…”
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Design, synthesis and structure–Activity relationships of novel imidazolo[1,2- a]pyrimid-5-ones as potent GnRH receptor antagonists by Gross, Timothy D., Zhu, Yun-Fei, Saunders, John, Wilcoxen, Keith M., Gao, Yinghong, Connors, Patrick J., Guo, Zhiqiang, Struthers, R.Scott, Reinhart, Greg J., Chen, Chen

“…SAR studies of lead GnRH receptor antagonists 2a and 2b reported earlier resulted in the discovery of compound 10b which showed much higher potency ( K i=4.6…”
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A Novel Synthesis of 2-Arylpyrrolo[1,2- a]pyrimid-7-ones and Their Structure–Activity Relationships as Potent GnRH Receptor Antagonists by Zhu, Yun-Fei, Wilcoxen, Keith, Saunders, John, Guo, Zhiqiang, Gao, Yinghong, Connors, Jr, Patrick J., Gross, Timothy D., Tucci, Fabio C., Scott Struthers, R., Reinhart, Greg J., Xie, Qiu, Chen, Chen

“…In the process of developing GnRH receptor antagonists, a novel base-catalyzed cyclization of compounds 5a– b was discovered, which led to the formation of the…”
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3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)-6-methyl-ur acils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor by TUCCI, Fabio C, ZHU, Yun-Fei, TA KUNG CHEN, BOZIGIAN, Haig, BONNEVILLE, Anne L, FISHER, Andrew, LIPING JIN, SAUNDERS, John, CHEN CHEN, ZHIQIANG GUO, GROSS, Timothy D, CONNORS, Patrick J, YINGHONG GAO, ROWBOTTOM, Martin W, STRUTHERS, R. Scott, REINHART, Greg J, QIU XIE

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