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Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists. 2010
Derek C Cole, and
Jonathan L Gross, and
Thomas A Comery, and
Suzan Aschmies, and
Warren D Hirst, and
Cody Kelley, and
Ji-In Kim, and
Katie Kubek, and
Xiaoping Ning, and
Brian J Platt, and
Albert J Robichaud, and
William R Solvibile, and
Joseph R Stock, and
Gregory Tawa, and
Marla J Williams, and
John W Ellingboe
Chemical Sciences, Wyeth Research, 401 N Middletown Rd. Pearl River, NY 10965, United States. coledc@wyeth.com
Using a focused screen of biogenic amine compounds we identified a novel series of H(3)R antagonists. A preliminary SAR study led to reduction of MW while increasing binding affinity and potency. Optimization of the physical properties of the series led to (S)-6n, with improved brain to plasma exposure and efficacy in both water intake and novel object recognition models.
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Thomas A Comery, and
Suzan Aschmies, and
Warren D Hirst, and
Cody Kelley, and
Ji-In Kim, and
Katie Kubek, and
Xiaoping Ning, and
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Albert J Robichaud, and
William R Solvibile, and
Joseph R Stock, and
Gregory Tawa, and
Marla J Williams, and
John W Ellingboe
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Cody Kelley, and
Ji-In Kim, and
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Derek C Cole, and
Jonathan L Gross, and
Thomas A Comery, and
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Katie Kubek, and
Xiaoping Ning, and
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William R Solvibile, and
Joseph R Stock, and
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Marla J Williams, and
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Jonathan L Gross, and
Thomas A Comery, and
Suzan Aschmies, and
Warren D Hirst, and
Cody Kelley, and
Ji-In Kim, and
Katie Kubek, and
Xiaoping Ning, and
Brian J Platt, and
Albert J Robichaud, and
William R Solvibile, and
Joseph R Stock, and
Gregory Tawa, and
Marla J Williams, and
John W Ellingboe
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Archiv der Pharmazie,
Derek C Cole, and
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Thomas A Comery, and
Suzan Aschmies, and
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Cody Kelley, and
Ji-In Kim, and
Katie Kubek, and
Xiaoping Ning, and
Brian J Platt, and
Albert J Robichaud, and
William R Solvibile, and
Joseph R Stock, and
Gregory Tawa, and
Marla J Williams, and
John W Ellingboe
May 2010,
Bioorganic & medicinal chemistry letters,
Derek C Cole, and
Jonathan L Gross, and
Thomas A Comery, and
Suzan Aschmies, and
Warren D Hirst, and
Cody Kelley, and
Ji-In Kim, and
Katie Kubek, and
Xiaoping Ning, and
Brian J Platt, and
Albert J Robichaud, and
William R Solvibile, and
Joseph R Stock, and
Gregory Tawa, and
Marla J Williams, and
John W Ellingboe
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Jonathan L Gross, and
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Ji-In Kim, and
Katie Kubek, and
Xiaoping Ning, and
Brian J Platt, and
Albert J Robichaud, and
William R Solvibile, and
Joseph R Stock, and
Gregory Tawa, and
Marla J Williams, and
John W Ellingboe
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Jonathan L Gross, and
Thomas A Comery, and
Suzan Aschmies, and
Warren D Hirst, and
Cody Kelley, and
Ji-In Kim, and
Katie Kubek, and
Xiaoping Ning, and
Brian J Platt, and
Albert J Robichaud, and
William R Solvibile, and
Joseph R Stock, and
Gregory Tawa, and
Marla J Williams, and
John W Ellingboe
November 1999,
Archiv der Pharmazie,
Derek C Cole, and
Jonathan L Gross, and
Thomas A Comery, and
Suzan Aschmies, and
Warren D Hirst, and
Cody Kelley, and
Ji-In Kim, and
Katie Kubek, and
Xiaoping Ning, and
Brian J Platt, and
Albert J Robichaud, and
William R Solvibile, and
Joseph R Stock, and
Gregory Tawa, and
Marla J Williams, and
John W Ellingboe
August 1998,
Die Pharmazie,
Derek C Cole, and
Jonathan L Gross, and
Thomas A Comery, and
Suzan Aschmies, and
Warren D Hirst, and
Cody Kelley, and
Ji-In Kim, and
Katie Kubek, and
Xiaoping Ning, and
Brian J Platt, and
Albert J Robichaud, and
William R Solvibile, and
Joseph R Stock, and
Gregory Tawa, and
Marla J Williams, and
John W Ellingboe
July 1976,
British journal of pharmacology,
