Chen Chen

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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
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.
Dyck Brian; Tamiya Junko; Jovic Florence; Pick Rebecca R; Bradbury Margaret J; O'Brien Julie; Wen Jenny; Johns Michael; Madan Ajay; Fleck Beth A; Foster Alan C; Li Binfeng; Zhang Mingzhu; Tran Joe A; Vickers Troy; Grey Jonathan; Saunders John; Chen Chen
Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain.
Marinkovic Dragan; Tucci Fabio C; Tran Joe A; Fleck Beth A; Wen Jenny; Chen Chen
Structure-activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands.

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2008: 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
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.
Journal of medicinal chemistry 2008;51(23):7478-85.
2008: Dyck Brian; Tamiya Junko; Jovic Florence; Pick Rebecca R; Bradbury Margaret J; O'Brien Julie; Wen Jenny; Johns Michael; Madan Ajay; Fleck Beth A; Foster Alan C; Li Binfeng; Zhang Mingzhu; Tran Joe A; Vickers Troy; Grey Jonathan; Saunders John; Chen Chen
Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain.
Journal of medicinal chemistry 2008;51(22):7265-72.
2008: Marinkovic Dragan; Tucci Fabio C; Tran Joe A; Fleck Beth A; Wen Jenny; Chen Chen
Structure-activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands.
Bioorganic & medicinal chemistry letters 2008;18(17):4817-22.
2008: Regan Colin F; Guo Zhiqiang; Chen Yongsheng; Huang Charles Q; Chen Mi; Jiang Wanlong; Rueter Jaimie K; Coon Timothy; Chen Chen; Saunders John; Brown Michael S; Betz Steve F; Struthers R Scott; Yang Chun; Wen Jenny; Madan Ajay; Zhu Yun-Fei
Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties.
Bioorganic & medicinal chemistry letters 2008;18(16):4503-7.
2008: Zhang Mingzhu; Jovic Florence; Vickers Troy; Dyck Brian; Tamiya Junko; Grey Jonathan; Tran Joe A; Fleck Beth A; Pick Rebecca; Foster Alan C; Chen Chen
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(13):3682-6.
2008: Vickers Troy; Dyck Brian; Tamiya Junko; Zhang Mingzhu; Jovic Florence; Grey Jonathan; Fleck Beth A; Aparicio Anna; Johns Michael; Jin Liping; Tang Hui; Foster Alan C; Chen Chen
Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(11):3230-5.
2008: Tamiya Junko; Dyck Brian; Zhang Mingzhu; Phan Kasey; Fleck Beth A; Aparicio Anna; Jovic Florence; Tran Joe A; Vickers Troy; Grey Jonathan; Foster Alan C; Chen Chen
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(11):3328-32.
2008: Chen Chen; Chen Yongsheng; Pontillo Joseph; Guo Zhiqiang; Huang Charles Q; Wu Dongpei; Madan Ajay; Chen Takung; Wen Jenny; Xie Qiu; Tucci Fabio C; Rowbottom Martin; Zhu Yun-Fei; Wade Warren; Saunders John; Bozigian Haig; Struthers R Scott
Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity.
Bioorganic & medicinal chemistry letters 2008;18(11):3301-5.
2008: Zhao Liren; Guo Zhiqiang; Chen Yongsheng; Hu Tao; Wu Dongpei; Zhu Yun-Fei; Rowbottom Martin; Gross Timothy D; Tucci Fabio C; Struthers R Scott; Xie Qiu; Chen Chen
5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers.
Bioorganic & medicinal chemistry letters 2008;18(11):3344-9.
2008: Chen Chen; Tucci Fabio C; Jiang Wanlong; Tran Joe A; Fleck Beth A; Hoare Sam R; Wen Jenny; Chen Takung; Johns Michael; Markison Stacy; Foster Alan C; Marinkovic Dragan; Chen Caroline W; Arellano Melissa; Harman John; Saunders John; Bozigian Haig; Marks Daniel
Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.
Bioorganic & medicinal chemistry 2008;16(10):5606-18.
2008: Tran Joe A; Tucci Fabio C; Arellano Melissa; Jiang Wanlong; Chen Caroline W; Marinkovic Dragan; Fleck Beth A; Wen Jenny; Foster Alan C; Chen Chen
Design and synthesis of 3-arylpyrrolidine-2-carboxamide derivatives as melanocortin-4 receptor ligands.
Bioorganic & medicinal chemistry letters 2008;18(6):1931-8.
2008: Chen Chen; Dyck Brian; Fleck Beth A; Foster Alan C; Grey Jonathan; Jovic Florence; Mesleh Michael; Phan Kasey; Tamiya Junko; Vickers Troy; Zhang Mingzhu
Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(4):1346-9.
2008: Tran Joe A; Chen Caroline W; Tucci Fabio C; Jiang Wanlong; Fleck Beth A; Chen Chen
Syntheses of tetrahydrothiophenes and tetrahydrofurans and studies of their derivatives as melanocortin-4 receptor ligands.
Bioorganic & medicinal chemistry letters 2008;18(3):1124-30.
2008: Tran Joe A; Arellano Melissa; Fleck Beth A; Pontillo Joseph; Marinkovic Dragan; Tucci Fabio C; Wen Jenny; Saunders John; Chen Chen
Studies on the structure-activity relationship of the basic amine of phenylpiperazines as melanocortin-4 receptor antagonists.
Medicinal chemistry (Shariqah (United Arab Emirates)) 2008;4(1):67-74.
2008: Chen Chen; Jiang Wanlong; Tran Joe A; Tucci Fabio C; Fleck Beth A; Markison Stacy; Wen Jenny; Madan Ajay; Hoare Sam R; Foster Alan C; Marinkovic Dragan; Chen Caroline W; Arellano Melissa; Saunders John
Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor.
Bioorganic & medicinal chemistry letters 2008;18(1):129-36.
2008: Chen Chen
Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine.
Current medicinal chemistry 2008;15(21):2173-91.
2007: Tran Joe A; Jiang Wanlong; Tucci Fabio C; Fleck Beth A; Wen Jenny; Sai Yang; Madan Ajay; Chen Ta Kung; Markison Stacy; Foster Alan C; Hoare Sam R; Marks Daniel; Harman John; Chen Caroline W; Arellano Melissa; Marinkovic Dragan; Bozigian Haig; Saunders John; Chen Chen
Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.
Journal of medicinal chemistry 2007;50(25):6356-66.
2007: Chen Caroline W; Tran Joe A; Fleck Beth A; Tucci Fabio C; Jiang Wanlong; Chen Chen
Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 receptor.
Bioorganic & medicinal chemistry letters 2007;17(24):6825-31.
2007: Jiang Wanlong; Tran Joe A; Tucci Fabio C; Fleck Beth A; Hoare Sam R; Markison Stacy; Wen Jenny; Chen Caroline W; Marinkovic Dragan; Arellano Melissa; Foster Alan C; Chen Chen
Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human melanocortin-4 receptor.
Bioorganic & medicinal chemistry letters 2007;17(23):6546-52.
2007: Chen Chen; Jiang Wanlong; Tucci Fabio; Tran Joe A; Fleck Beth A; Hoare Sam R; Joppa Margaret; Markison Stacy; Wen Jenny; Sai Yang; Johns Michael; Madan Ajay; Chen Takung; Chen Caroline W; Marinkovic Dragan; Arellano Melissa; Saunders John; Foster Alan C
Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia.
Journal of medicinal chemistry 2007;50(22):5249-52.
2007: Jiang Wanlong; Tucci Fabio C; Tran Joe A; Fleck Beth A; Wen Jenny; Markison Stacy; Marinkovic Dragan; Chen Caroline W; Arellano Melissa; Hoare Sam R; Johns Michael; Foster Alan C; Saunders John; Chen Chen
Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.
Bioorganic & medicinal chemistry letters 2007;17(20):5610-3.
2007: Tran Joe A; Chen Caroline W; Jiang Wanlong; Tucci Fabio C; Fleck Beth A; Marinkovic Dragan; Arellano Melissa; Chen Chen
Pyrrolidines as potent functional agonists of the human melanocortin-4 receptor.
Bioorganic & medicinal chemistry letters 2007;17(18):5165-70.
2007: Tran Joe A; Tucci Fabio C; Jiang Wanlong; Marinkovic Dragan; Chen Caroline W; Arellano Melissa; Markison Stacy; Fleck Beth A; Wen Jenny; White Nicole S; Pontillo Joseph; Saunders John; Marks Daniel; Hoare Sam R; Madan Ajay; Foster Alan C; Chen Chen
Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.
Bioorganic & medicinal chemistry 2007;15(15):5166-76.
2007: 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
Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902.
Endocrinology 2007;148(2):857-67.
2007: Chen Chen
Some pharmacokinetic aspects of the lipophilic terfenadine and zwitterionic fexofenadine in humans.
Drugs in R&D 2007;8(5):301-14.
2007: Foster Alan C; Chen Chen
Melanocortin-4 receptor antagonists as potential therapeutics in the treatment of cachexia.
Current topics in medicinal chemistry 2007;7(11):1131-6.
2007: Chen Chen
Recent progress toward nonpeptide ligands for the melanocortin-4 receptor.
Progress in medicinal chemistry 2007;45():111-67.
2006: Chen Caroline W; Tran Joe A; Jiang Wanlong; Tucci Fabio C; Arellano Melissa; Wen Jenny; Fleck Beth A; Marinkovic Dragan; White Nicole S; Pontillo Joseph; Saunders John; Madan Ajay; Foster Alan C; Chen Chen
Propionylpiperazines as human melanocortin-4 receptor ligands.
Bioorganic & medicinal chemistry letters 2006;16(18):4800-3.
2006: Jiang Wanlong; Tucci Fabio C; Chen Caroline W; Arellano Melissa; Tran Joe A; White Nicole S; Marinkovic Dragan; Pontillo Joseph; Fleck Beth A; Wen Jenny; Saunders John; Madan Ajay; Foster Alan C; Chen Chen
Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor.
Bioorganic & medicinal chemistry letters 2006;16(17):4674-8.
2006: Tran Joe A; Pontillo Joseph; Fleck Beth A; Marinkovic Dragan; Arellano Melissa; Tucci Fabio C; Lanier Marion; Saunders John; Jiang Wanlong; Chen Caroline W; Foster Alan C; Chen Chen
Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor.
Bioorganic & medicinal chemistry letters 2006;16(14):3693-6.
2006: Betz Stephen F; Reinhart Greg J; Lio Francisco M; Chen Chen; Struthers R Scott
Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor.
Journal of medicinal chemistry 2006;49(2):637-47.
2006: Chen C
Recent advances in small molecule antagonists of the corticotropin-releasing factor type-1 receptor-focus on pharmacology and pharmacokinetics.
Current medicinal chemistry 2006;13(11):1261-82.
2005: Pontillo Joseph; Tran Joe A; White Nicole S; Arellano Melissa; Fleck Beth A; Marinkovic Dragan; Tucci Fabio C; Saunders John; Foster Alan C; Chen Chen
Structure-activity relationship studies on a series of cyclohexylpiperazines bearing a phanylacetamide as ligands of the human melanocortin-4 receptor.
Bioorganic & medicinal chemistry letters 2005;15(23):5237-40.
2005: Joppa M A; Ling N; Chen C; Gogas K R; Foster A C; Markison S
Central administration of peptide and small molecule MC4 receptor antagonists induce hyperphagia in mice and attenuate cytokine-induced anorexia.
Peptides 2005;26(11):2294-301.
2005: Tucci Fabio C; Hu Tao; Mesleh Michael F; Bokser Allan; Allsopp Eric; Gross Timothy D; Guo Zhiqiang; Zhu Yun-Fei; Struthers R Scott; Ling Nicholas; Chen Chen
Atropisomeric property of 1-(2,6-difluorobenzyl)-3-[(2R)-amino-2-phenethyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyluracil.
Chirality 2005;17(9):559-64.
2005: Jiang Wanlong; Chen Chen; Marinkovic Dragan; Tran Joe A; Chen Caroline W; Arellano L Melissa; White Nicole S; Tucci Fabio C
Practical asymmetric synthesis of alpha-branched 2-piperazinylbenzylamines by 1,2-additions of organometallic reagents to N-tert-butanesulfinyl imines.
The Journal of organic chemistry 2005;70(22):8924-31.
2005: Pontillo Joseph; Marinkovic Dragan; Tran Joe A; Arellano Melissa; Fleck Beth A; Wen Jenny; Tucci Fabio C; Nelson Jodie; Saunders John; Foster Alan C; Chen Chen
Optimization of piperazinebenzylamines with a N-(1-methoxy-2-propyl) side chain as potent and selective antagonists of the human melanocortin-4 receptor.
Bioorganic & medicinal chemistry letters 2005;15(20):4615-8.
2005: Tucci Fabio C; White Nicole S; Markison Stacy; Joppa Margaret; Tran Joe A; Fleck Beth A; Madan Ajay; Dyck Brian P; Parker Jessica; Pontillo Joseph; Arellano L Melissa; Marinkovic Dragan; Jiang Wanlong; Chen Caroline W; Gogas Kathleen R; Goodfellow Val S; Saunders John; Foster Alan C; Chen Chen
Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines.
Bioorganic & medicinal chemistry letters 2005;15(19):4389-95.
2005: Pontillo Joseph; Guo Zhiqiang; Wu Dongpei; Struthers R Scott; Chen Chen
Synthesis of aryl-1,2,4-triazine-3,5-diones as antagonists of the gonadotropin-releasing hormone receptor.
Bioorganic & medicinal chemistry letters 2005;15(19):4363-6.
2005: Guo Zhiqiang; Wu Dongpei; Zhu Yun-Fei; Tucci Fabio C; Regan Collin F; Rowbottom Martin W; Struthers R Scott; Xie Qiu; Reijmers Shelby; Sullivan Susan K; Sai Yang; Chen Chen
Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists.
Bioorganic & medicinal chemistry letters 2005;15(16):3685-90.
2005: Tran Joseph A; Pontillo Joseph; Arellano Melissa; Fleck Beth A; Tucci Fabio C; Marinkovic Dragan; Chen Caroline W; Saunders John; Foster Alan C; Chen Chen
Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor.
Bioorganic & medicinal chemistry letters 2005;15(14):3434-8.
2005: Pontillo Joseph; Tran Joseph A; Markison Stacy; Joppa Margaret; Fleck Beth A; Marinkovic Dragan; Arellano Melissa; Tucci Fabio C; Lanier Marion; Nelson Jodie; Saunders John; Hoare Sam R J; Foster Alan C; Chen Chen
A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice.
Bioorganic & medicinal chemistry letters 2005;15(10):2541-6.
2005: Guo Zhiqiang; Chen Yongsheng; Huang Charles Q; Gross Timothy D; Pontillo Joseph; Rowbottom Martin W; Saunders John; Struthers Scott; Tucci Fabio C; Xie Qiu; Wade Warren; Zhu Yun-Fei; Wu Dongpei; Chen Chen
Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers.
Bioorganic & medicinal chemistry letters 2005;15(10):2519-22.
2005: Lowe Richard F; Nelson Jodene; Dang Trunghau N; Crowe Paul D; Pahuja Anil; McCarthy James R; Grigoriadis Dimitri E; Conlon Paul; Saunders John; Chen Chen; Szabo Thomas; Chen Ta Kung; Bozigian Haig
Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists.
Journal of medicinal chemistry 2005;48(5):1540-9.
2005: Pontillo Joseph; Chen Chen
Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2-c]pyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists.
Bioorganic & medicinal chemistry letters 2005;15(5):1407-11.
2005: 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 Chen
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.
Journal of medicinal chemistry 2005;48(4):1169-78.
2005: Tran Joe A; Pontillo Joseph; Arellano Melissa; White Nicole S; Fleck Beth A; Marinkovic Dragan; Tucci Fabio C; Lanier Marion; Nelson Jodie; Saunders John; Foster Alan C; Chen Chen
Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines.
Bioorganic & medicinal chemistry letters 2005;15(3):833-7.
2005: Guo Zhiqiang; Wu Dongpei; Zhu Yun-Fei; Tucci Fabio C; Pontillo Joseph; Saunders John; Xie Qiu; Struthers R Scott; Chen Chen
A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists.
Bioorganic & medicinal chemistry letters 2005;15(3):693-8.
2004: Pontillo Joseph; Tran Joseph A; Fleck Beth A; Marinkovic Dragan; Arellano Melissa; Tucci Fabio C; Lanier Marion; Nelson Jodie; Parker Jessica; Saunders John; Murphy Brian; Foster Alan C; Chen Chen
Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor.
Bioorganic & medicinal chemistry letters 2004;14(22):5605-9.
2004: Rowbottom Martin W; Tucci Fabio C; Connors Patrick J; Gross Timothy D; Zhu Yun-Fei; Guo Zhiqiang; Moorjani Manisha; Acevedo Oscar; Carter Lee; Sullivan Susan K; Xie Qiu; Fisher Andrew; Struthers R Scott; Saunders John; Chen Chen
Synthesis and structure-activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5.
Bioorganic & medicinal chemistry letters 2004;14(19):4967-73.
2004: Pontillo Joseph; Tran Joseph A; Arellano Melissa; Fleck Beth A; Huntley Rajesh; Marinkovic Dragan; Lanier Marion; Nelson Jodie; Parker Jessica; Saunders John; Tucci Fabio C; Jiang Wanlong; Chen Caroline W; White Nicole S; Foster Alan C; Chen Chen
Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor.
Bioorganic & medicinal chemistry letters 2004;14(17):4417-23.
2004: Chen Chen; Wilcoxen Keith M; Huang Charles Q; Xie Yun-Feng; McCarthy James R; Webb Thomas R; Zhu Yun-Fei; Saunders John; Liu Xin-Jun; Chen Ta-Kung; Bozigian Haig; Grigoriadis Dimitri E
Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists.
Journal of medicinal chemistry 2004;47(19):4787-98.
2004: Huang Charles Q; Wilcoxen Keith M; Grigoriadis Dimitri E; McCarthy James R; Chen Chen
Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines as potent CRF1 receptor antagonists.
Bioorganic & medicinal chemistry letters 2004;14(15):3943-7.
2004: Webb Thomas R; Moran Terry; Huang Charles Q; McCarthy James R; Grigoriadis Dimitri E; Chen Chen
Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor.
Bioorganic & medicinal chemistry letters 2004;14(15):3869-73.
2004: Reinhart Greg J; Xie Qiu; Liu Xin-Jun; Zhu Yun-Fei; Fan Jun; Chen Chen; Struthers R Scott
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.
The Journal of biological chemistry 2004;279(33):34115-22.
2004: Chen Chen; Yu Jinghua; Fleck Beth A; Hoare Sam R J; Saunders John; Foster Alan C
Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists.
Journal of medicinal chemistry 2004;47(16):4083-8.
2004: 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 Chen
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.
Journal of medicinal chemistry 2004;47(14):3483-6.
2004: Chen Chen; Wilcoxen Keith M; Huang Charles Q; McCarthy James R; Chen Takung; Grigoriadis Dimitri E
Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility.
Bioorganic & medicinal chemistry letters 2004;14(14):3669-73.
2004: Rowbottom Martin W; Tucci Fabio C; Zhu Yun-Fei; Guo Zhiqiang; Gross Timothy D; Reinhart Greg J; Xie Qui; Struthers R Scott; Saunders John; Chen Chen
Synthesis and structure-activity relationships of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils as human GnRH receptor antagonists.
Bioorganic & medicinal chemistry letters 2004;14(9):2269-74.
2004: Huang Charles Q; Grigoriadis Dimitri E; Liu Zhengyu; McCarthy James R; Ramphal John; Webb Thomas; Whitten Jeffrey P; Xie Michael Y; Chen Chen
Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists.
Bioorganic & medicinal chemistry letters 2004;14(9):2083-6.
2004: Guo Zhiqiang; Zhu Yun-Fei; Gross Timothy D; Tucci Fabio C; Gao Yinghong; Moorjani Manisha; Connors Patrick J; Rowbottom Martin W; Chen Yongsheng; Struthers R Scott; Xie Qiu; Saunders John; Reinhart Greg; Chen Ta Kung; Bonneville Anne L Killam; Chen Chen
Synthesis and structure-activity relationships of 1-arylmethyl-5-aryl-6-methyluracils as potent gonadotropin-releasing hormone receptor antagonists.
Journal of medicinal chemistry 2004;47(5):1259-71.
2003: Guo Zhiqiang; Chen Yongsheng; Wu Dongpei; Zhu Yun-Fei; Struthers R Scott; Saunders John; Xie Qiu; Chen Chen
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists.
Bioorganic & medicinal chemistry letters 2003;13(20):3617-22.
2003: Huang Charles Q; Wilcoxen Keith; McCarthy James R; Haddach Mustapha; Webb Thomas R; Gu Jian; Xie Yun-Feng; Grigoriadis Dimitri E; Chen Chen
Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists.
Bioorganic & medicinal chemistry letters 2003;13(19):3375-9.
2003: Huang Charles Q; Wilcoxen Keith; McCarthy James R; Haddach Mustaph; Grigoriadis Dimitri; Chen Chen
Synthesis of 1-methyl-3-phenylpyrazolo[4,3-b]pyridines via a methylation of 4-phthalimino-3-phenylpyrazoles and optimization toward highly potent corticotropin-releasing factor type-1 antagonists.
Bioorganic & medicinal chemistry letters 2003;13(19):3371-4.
2003: Wilcoxen Keith; Huang Charles Q; McCarthy James R; Grigoriadis Dimitri E; Chen Chen
Synthesis of 3-phenylpyrazolo[4,3-b]pyridines via a convenient synthesis of 4-amino-3-arylpyrazoles and SAR of corticotropin-releasing factor receptor type-1 antagonists.
Bioorganic & medicinal chemistry letters 2003;13(19):3367-70.
2003: Tucci Fabio C; Zhu Yun-Fei; Guo Zhiqiang; Gross Timothy D; Connors Patrick J; Struthers R Scott; Reinhart Greg J; Saunders John; Chen Chen
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.
Bioorganic & medicinal chemistry letters 2003;13(19):3317-22.
2003: 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
Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists.
Bioorganic & medicinal chemistry letters 2003;13(19):3311-5.
2003: Foster Alam C; Joppa Margaret; Markison Stacy; Gogas Kathy R; Fleck Beth A; Murphy Brian J; Wolff Meira; Cismowski Mary J; Ling Nicholas; Goodfellow Val S; Chen Chen; Saunders John; Conlon Paul J
Body weight regulation by selective MC4 receptor agonists and antagonists.
Annals of the New York Academy of Sciences 2003;994():103-10.
2003: Zhu Yun-Fei; Wang Xiao-Chuan; Connors Patrick; Wilcoxen Keith; Gao Yinghong; Gross Raymond; Strack Nathalie; Gross Timothy; McCarthy James R; Xie Qiu; Ling Nicholas; Chen Chen
Quinoline-carboxylic acids are potent inhibitors that inhibit the binding of insulin-like growth factor (IGF) to IGF-binding proteins.
Bioorganic & medicinal chemistry letters 2003;13(11):1931-4.
2003: Zhu Yun-Fei; Wilcoxen Keith; Gross Timothy; Connors Patrick; Strack Nathalie; Gross Raymond; Huang Charles Q; McCarthy James R; Xie Qiu; Ling Nicholas; Chen Chen
6,7-dihydroxyisoquinoline-3-carboxylic acids are potent inhibitors on the binding of insulin-like growth factor (IGF) to IGF-binding proteins: optimization of the 1-position benzoyl side chain.
Bioorganic & medicinal chemistry letters 2003;13(11):1927-30.
2003: 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 Chen
Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists.
Journal of medicinal chemistry 2003;46(11):2023-6.
2003: 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 Chen
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.
Journal of medicinal chemistry 2003;46(9):1769-72.
2002: 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 novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists.
Bioorganic & medicinal chemistry letters 2002;12(23):3491-5.
2002: 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
Design, synthesis and structure-activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.
Bioorganic & medicinal chemistry letters 2002;12(16):2185-7.
2002: Wilcoxen Keith M; Zhu Yun Fei; Connors Patrick J; Saunders John; Gross Timothy D; Gao Yinghong; Reinhart Greg J; Struthers R Scott; Chen Chen
Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.
Bioorganic & medicinal chemistry letters 2002;12(16):2179-83.
2002: Zhu Yun-Fei; Wilcoxen Keith; Saunders John; Guo Zhiqiang; Gao Yinghong; Connors Patrick J; Gross Timothy D; Tucci Fabio C; Struthers R Scott; Reinhart Greg J; Xie Qiu; Chen Chen
A novel synthesis of 2-arylpyrrolo[1,2-a]pyrimid-7-ones and their structure-activity relationships as potent GnRH receptor antagonists.
Bioorganic & medicinal chemistry letters 2002;12(3):403-6.
2002: Zhu Yun-Fei; Struthers R Scott; Connors Patrick J; Gao Yinghong; Gross Timothy D; Saunders John; Wilcoxen Keith; Reinhart Greg J; Ling Nicholas; Chen Chen
Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists.
Bioorganic & medicinal chemistry letters 2002;12(3):399-402.
2001: Chen C; Dagnino R; Huang C Q; McCarthy J R; Grigoriadis D E
1-Alkyl-3-amino-5-aryl-1H-[1,2,4]triazoles: novel synthesis via cyclization of N-acyl-S-methylisothioureas with alkylhydrazines and their potent corticotropin-releasing factor-1 (CRF(1)) receptor antagonist activities.
Bioorganic & medicinal chemistry letters 2001;11(24):3165-8.
2001: Chen C; Zhu Y F; Liu X J; Lu Z X; Xie Q; Ling N
Discovery of a series of nonpeptide small molecules that inhibit the binding of insulin-like growth factor (IGF) to IGF-binding proteins.
Journal of medicinal chemistry 2001;44(23):4001-10.
2000: Chen C; Zhu Y F; Wilcoxen K
An improved synthesis of selectively protected L-dopa derivatives from L-tyrosine.
The Journal of organic chemistry 2000;65(8):2574-6.

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