Search Results - "LANIER, Marion C"

Selection, synthesis, and structure–activity relationship of tetrahydropyrido[4,3- d]pyrimidine-2,4-diones as human GnRH receptor antagonists by Lanier, Marion C., Feher, Miklos, Ashweek, Neil J., Loweth, Colin J., Rueter, Jaimie K., Slee, Deborah H., Williams, John P., Zhu, Yun-Fei, Sullivan, Susan K., Brown, Michael S.

“…A series of tetrahydropyrido[4,3- d]pyrimidine-2,4-dione was selected in silico and evaluated as small molecules antagonists against the h-GnRH receptor. SAR…”
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Lead Optimization of 4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A Adenosine Receptor Antagonists for the Treatment of Parkinson’s Disease by Zhang, Xiaohu, Tellew, John E, Luo, Zhiyong, Moorjani, Manisha, Lin, Emily, Lanier, Marion C, Chen, Yongsheng, Williams, John P, Saunders, John, Lechner, Sandra M, Markison, Stacy, Joswig, Tanya, Petroski, Robert, Piercey, Jaime, Kargo, William, Malany, Siobhan, Santos, Mark, Gross, Raymond S, Wen, Jenny, Jalali, Kayvon, O’Brien, Zhihong, Stotz, Carol E, Crespo, María I, Díaz, José-Luis, Slee, Deborah H

“…4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)-pyrimidines bearing substituted pyridyl groups as C-6 substituents were prepared as selective adenosine hA2A…”
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Identification of Novel, Water-Soluble, 2-Amino-N-pyrimidin-4-yl Acetamides as A2A Receptor Antagonists with In Vivo Efficacy by Slee, Deborah H, Zhang, Xiaohu, Moorjani, Manisha, Lin, Emily, Lanier, Marion C, Chen, Yongsheng, Rueter, Jaimie K, Lechner, Sandra M, Markison, Stacy, Malany, Siobhan, Joswig, Tanya, Santos, Mark, Gross, Raymond S, Williams, John P, Castro-Palomino, Julio C, Crespo, María I, Prat, Maria, Gual, Silvia, Díaz, José-Luis, Wen, Jenny, O’Brien, Zhihong, Saunders, John

“…Potent adenosine hA2A receptor antagonists are often accompanied by poor aqueous solubility, which presents issues for drug development. Herein we describe the…”
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2-Amino-N-pyrimidin-4-ylacetamides as A2A Receptor Antagonists: 1. Structure−Activity Relationships and Optimization of Heterocyclic Substituents by Slee, Deborah H, Chen, Yongsheng, Zhang, Xiaohu, Moorjani, Manisha, Lanier, Marion C, Lin, Emily, Rueter, Jaimie K, Williams, John P, Lechner, Sandra M, Markison, Stacy, Malany, Siobhan, Santos, Mark, Gross, Raymond S, Jalali, Kayvon, Sai, Yang, Zuo, Zhiyang, Yang, Chun, Castro-Palomino, Julio C, Crespo, María I, Prat, Maria, Gual, Silvia, Díaz, José-Luis, Saunders, John

“…Previously we have described a novel series of potent and selective A2A receptor antagonists (e.g., 1) with excellent aqueous solubility. While these compounds…”
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2-Amino-N-pyrimidin-4-ylacetamides as A2A Receptor Antagonists: 2. Reduction of hERG Activity, Observed Species Selectivity, and Structure−Activity Relationships by Slee, Deborah H, Moorjani, Manisha, Zhang, Xiaohu, Lin, Emily, Lanier, Marion C, Chen, Yongsheng, Rueter, Jaimie K, Lechner, Sandra M, Markison, Stacy, Malany, Siobhan, Joswig, Tanya, Santos, Mark, Gross, Raymond S, Williams, John P, Castro-Palomino, Julio C, Crespo, María I, Prat, Maria, Gual, Silvia, Díaz, José-Luis, Jalali, Kayvon, Sai, Yang, Zuo, Zhiyang, Yang, Chun, Wen, Jenny, O’Brien, Zhihong, Petroski, Robert, Saunders, John

“…Previously we have described a series of novel A2A receptor antagonists with excellent water solubility. As described in the accompanying paper, the…”
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Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists by XIAOHU ZHANG, RUETER, Jaimie K, MARKISON, Stacy, JOSWIG, Tanya, MALANY, Siobhan, SANTOS, Mark, CASTRO-PALOMINO, Julio C, CRESPO, Maria I, PRAT, Maria, GUAL, Silvia, DIAZ, José-Luis, SAUNDERS, John, YONGSHENG CHEN, SLEE, Deborah H, MOORJANI, Manisha, LANIER, Marion C, LIN, Emily, GROSS, Raymond S, TELLEW, John E, WILLIAMS, John P, LECHNER, Sandra M

“…A series of N-pyrimidinyl-2-phenoxyacetamide adenosine A(2A) antagonists is described. SAR studies led to compound 14 with excellent potency (K(i) = 0.4 nM),…”
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2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability by Moorjani, Manisha, Luo, Zhiyong, Lin, Emily, Vong, Binh G, Chen, Yongsheng, Zhang, Xiaohu, Rueter, Jaimie K, Gross, Raymond S, Lanier, Marion C, Tellew, John E, Williams, John P, Lechner, Sandra M, Malany, Siobhan, Santos, Mark, Crespo, María I, Díaz, José-Luis, Saunders, John, Slee, Deborah H

“…In this report, the strategy and outcome of expanding SAR exploration to improve solubility and metabolic stability are discussed. Compound 35 exhibited…”
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2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A2A antagonists with improved solubility and metabolic stability by MOORJANI, Manisha, ZHIYONG LUO, WILLIAMS, John P, LECHNER, Sandra M, MALANY, Siobhan, SANTOS, Mark, CRESPO, Maria I, DIAZ, José-Luis, SAUNDERS, John, SLEE, Deborah H, LIN, Emily, VONG, Binh G, YONGSHENG CHEN, XIAOHU ZHANG, RUETER, Jaimie K, GROSS, Raymond S, LANIER, Marion C, TELLEW, John E

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2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A(2A) antagonists with reduced hERG liability by Moorjani, Manisha, Zhang, Xiaohu, Chen, Yongsheng, Lin, Emily, Rueter, Jaimie K, Gross, Raymond S, Lanier, Marion C, Tellew, John E, Williams, John P, Lechner, Sandra M, Malany, Siobhan, Santos, Mark, Ekhlassi, Paddi, Castro-Palomino, Julio C, Crespo, María I, Prat, Maria, Gual, Silvia, Díaz, José-Luis, Saunders, John, Slee, Deborah H

“…In this report, the design and synthesis of a series of pyrimidine based adenosine A(2A) antagonists are described. The strategy and outcome of expanding SAR…”
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2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A2A antagonists with reduced hERG liability by MOORJANI, Manisha, XIAOHU ZHANG, MALANY, Siobhan, SANTOS, Mark, EKHLASSI, Paddi, CASTRO-PALOMINO, Julio C, CRESPO, Maria I, PRAT, Maria, GUAL, Silvia, DIAZ, José-Luis, SAUNDERS, John, SLEE, Deborah H, YONGSHENG CHEN, LIN, Emily, RUETER, Jaimie K, GROSS, Raymond S, LANIER, Marion C, TELLEW, John E, WILLIAMS, John P, LECHNER, Sandra M

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Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2- c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists by Chen, Mi, Guo, Zhiqiang, Lanier, Marion C., Zhao, Liren, Betz, Stephen F., Huang, Charles Q., Loweth, Colin J., Ashweek, Neil J., Liu, Xin-Jun, Struthers, R. Scott, Bradbury, Margaret J., Behan, James W., Wen, Jenny, O’Brien, Zhihong, Saunders, John, Zhu, Yun-Fei

“…SAR of a series of novel and potent non-peptide GnRH receptor antagonists is disclosed. A novel series of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-…”
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N -[6-Amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A 2A Receptor Antagonists with Improved Drug Like Properties and in Vivo Efficacy by Lanier, Marion C., Moorjani, Manisha, Luo, Zhiyong, Chen, Yongsheng, Lin, Emily, Tellew, John E., Zhang, Xiaohu, Williams, John P., Gross, Raymond S., Lechner, Sandra M., Markison, Stacy, Joswig, Tanya, Kargo, William, Piercey, Jaime, Santos, Mark, Malany, Siobhan, Zhao, Marilyn, Petroski, Robert, Crespo, María I., Díaz, José-Luis, Saunders, John, Wen, Jenny, O’Brien, Zhihong, Jalali, Kayvon, Madan, Ajay, Slee, Deborah H.

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N-[6-Amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2AReceptor Antagonists with Improved Drug Like Properties and in Vivo Efficacy by LANIER, Marion C, MOORJANI, Manisha, MARKISON, Stacy, JOSWIG, Tanya, KARGO, William, PIERCEY, Jaime, SANTOS, Mark, MALANY, Siobhan, ZHAO, Marilyn, PETROSKI, Robert, CRESPO, Maria I, DIAZ, Jose-Luis, ZHIYONG LUO, SAUNDERS, John, WEN, Jenny, O'BRIEN, Zhihong, JALALI, Kayvon, MADAN, Ajay, SLEE, Deborah H, YONGSHENG CHEN, LIN, Emily, TELLEW, John E, XIAOHU ZHANG, WILLIAMS, John P, GROSS, Raymond S, LECHNER, Sandra M

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Lead Optimization of 4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A 2A Adenosine Receptor Antagonists for the Treatment of Parkinson’s Disease by Zhang, Xiaohu, Tellew, John E., Luo, Zhiyong, Moorjani, Manisha, Lin, Emily, Lanier, Marion C., Chen, Yongsheng, Williams, John P., Saunders, John, Lechner, Sandra M., Markison, Stacy, Joswig, Tanya, Petroski, Robert, Piercey, Jaime, Kargo, William, Malany, Siobhan, Santos, Mark, Gross, Raymond S., Wen, Jenny, Jalali, Kayvon, O’Brien, Zhihong, Stotz, Carol E., Crespo, María I., Díaz, José-Luis, Slee, Deborah H.

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N-[6-Amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A Receptor Antagonists with Improved Drug Like Properties and in Vivo Efficacy by Lanier, Marion C, Moorjani, Manisha, Luo, Zhiyong, Chen, Yongsheng, Lin, Emily, Tellew, John E, Zhang, Xiaohu, Williams, John P, Gross, Raymond S, Lechner, Sandra M, Markison, Stacy, Joswig, Tanya, Kargo, William, Piercey, Jaime, Santos, Mark, Malany, Siobhan, Zhao, Marilyn, Petroski, Robert, Crespo, María I, Díaz, José-Luis, Saunders, John, Wen, Jenny, O’Brien, Zhihong, Jalali, Kayvon, Madan, Ajay, Slee, Deborah H

“…In the present article, we report on a strategy to improve the physical properties of a series of small molecule human adenosine 2A (hA2A) antagonists. One of…”
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2-Amino- N -pyrimidin-4-ylacetamides as A 2A Receptor Antagonists: 1. Structure−Activity Relationships and Optimization of Heterocyclic Substituents by Slee, Deborah H., Chen, Yongsheng, Zhang, Xiaohu, Moorjani, Manisha, Lanier, Marion C., Lin, Emily, Rueter, Jaimie K., Williams, John P., Lechner, Sandra M., Markison, Stacy, Malany, Siobhan, Santos, Mark, Gross, Raymond S., Jalali, Kayvon, Sai, Yang, Zuo, Zhiyang, Yang, Chun, Castro-Palomino, Julio C., Crespo, María I., Prat, Maria, Gual, Silvia, Díaz, José-Luis, Saunders, John

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2-Amino- N -pyrimidin-4-ylacetamides as A 2A Receptor Antagonists: 2. Reduction of hERG Activity, Observed Species Selectivity, and Structure−Activity Relationships by Slee, Deborah H., Moorjani, Manisha, Zhang, Xiaohu, Lin, Emily, Lanier, Marion C., Chen, Yongsheng, Rueter, Jaimie K., Lechner, Sandra M., Markison, Stacy, Malany, Siobhan, Joswig, Tanya, Santos, Mark, Gross, Raymond S., Williams, John P., Castro-Palomino, Julio C., Crespo, María I., Prat, Maria, Gual, Silvia, Díaz, José-Luis, Jalali, Kayvon, Sai, Yang, Zuo, Zhiyang, Yang, Chun, Wen, Jenny, O’Brien, Zhihong, Petroski, Robert, Saunders, John

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2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A sub(2A) antagonists with improved solubility and metabolic stability by Moorjani, Manisha, Luo, Zhiyong, Lin, Emily, Vong, Binh G, Chen, Yongsheng, Zhang, Xiaohu, Rueter, Jaimie K, Gross, Raymond S, Lanier, Marion C, Tellew, John E, Williams, John P, Lechner, Sandra M, Malany, Siobhan, Santos, Mark, Crespo, Maria I, Diaz, Jose-Luis, Saunders, John, Slee, Deborah H

“…In this report, the strategy and outcome of expanding SAR exploration to improve solubility and metabolic stability are discussed. Compound 35 exhibited…”
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Identification of Novel, Water-Soluble, 2-Amino- N -pyrimidin-4-yl Acetamides as A 2A Receptor Antagonists with In Vivo Efficacy by Slee, Deborah H., Zhang, Xiaohu, Moorjani, Manisha, Lin, Emily, Lanier, Marion C., Chen, Yongsheng, Rueter, Jaimie K., Lechner, Sandra M., Markison, Stacy, Malany, Siobhan, Joswig, Tanya, Santos, Mark, Gross, Raymond S., Williams, John P., Castro-Palomino, Julio C., Crespo, María I., Prat, Maria, Gual, Silvia, Díaz, José-Luis, Wen, Jenny, O’Brien, Zhihong, Saunders, John

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Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A sub(2A) receptor antagonists by Zhang, Xiaohu, Rueter, Jaimie K, Chen, Yongsheng, Moorjani, Manisha, Lanier, Marion C, Lin, Emily, Gross, Raymond S, Tellew, John E, Williams, John P, Lechner, Sandra M, Markison, Stacy, Joswig, Tanya, Malany, Siobhan, Santos, Mark, Castro-Palomino, Julio C, Crespo, Mari'a I, Prat, Maria, Gual, Silvia, Diaz, Jose-Luis, Saunders, John, Slee, Deborah H

“…A series of N-pyrimidinyl-2-phenoxyacetamide adenosine A sub(2A) antagonists is described. SAR studies led to compound 14 with excellent potency (K sub(i) =…”
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