Preparation of oxime dual NK1/NK2 antagonists with reduced NK3 affinity

Gregory A. Reichard; Cheryl A. Grice; Neng Yang Shih; James Spitler; Sapna Majmundar; Steven D. Wang; Sunil Paliwal; John C. Anthes; John J. Piwinski

doi:10.1016/S0960-894X(02)00462-6

Preparation of oxime dual NK₁/NK₂ antagonists with reduced NK₃ affinity

Gregory A. Reichard
, Cheryl A. Grice
, Neng Yang Shih
, James Spitler
, Sapna Majmundar
, Steven D. Wang
, Sunil Paliwal
, John C. Anthes
, John J. Piwinski

Department of Chemistry and Chemical Biology

Merck
Johnson & Johnson

Research output: Contribution to journal › Article › peer-review

10 Scopus citations

Abstract

By employing a stereosimplification approach, a thorough SAR exploration of the piperidine region of Sch 206272 was possible through a practical and efficient synthesis of substituted cyclic ureas. This SAR study led to the identification of a benzimidazolinone series of compounds which display single digit nanomolar NK₁/NK₂ affinity and near micromolar binding for the NK₃ receptor.

Original language	English
Pages (from-to)	2355-2358
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	12
Issue number	17
DOIs	https://doi.org/10.1016/S0960-894X(02)00462-6
State	Published - 2 Sep 2002

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title = "Preparation of oxime dual NK1/NK2 antagonists with reduced NK3 affinity",

abstract = "By employing a stereosimplification approach, a thorough SAR exploration of the piperidine region of Sch 206272 was possible through a practical and efficient synthesis of substituted cyclic ureas. This SAR study led to the identification of a benzimidazolinone series of compounds which display single digit nanomolar NK1/NK2 affinity and near micromolar binding for the NK3 receptor.",

author = "Reichard, \{Gregory A.\} and Grice, \{Cheryl A.\} and Shih, \{Neng Yang\} and James Spitler and Sapna Majmundar and Wang, \{Steven D.\} and Sunil Paliwal and Anthes, \{John C.\} and Piwinski, \{John J.\}",

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AU - Reichard, Gregory A.

AU - Grice, Cheryl A.

AU - Shih, Neng Yang

AU - Spitler, James

AU - Majmundar, Sapna

AU - Wang, Steven D.

AU - Paliwal, Sunil

AU - Anthes, John C.

AU - Piwinski, John J.

PY - 2002/9/2

Y1 - 2002/9/2

N2 - By employing a stereosimplification approach, a thorough SAR exploration of the piperidine region of Sch 206272 was possible through a practical and efficient synthesis of substituted cyclic ureas. This SAR study led to the identification of a benzimidazolinone series of compounds which display single digit nanomolar NK1/NK2 affinity and near micromolar binding for the NK3 receptor.

AB - By employing a stereosimplification approach, a thorough SAR exploration of the piperidine region of Sch 206272 was possible through a practical and efficient synthesis of substituted cyclic ureas. This SAR study led to the identification of a benzimidazolinone series of compounds which display single digit nanomolar NK1/NK2 affinity and near micromolar binding for the NK3 receptor.

UR - https://www.scopus.com/pages/publications/0037009237

UR - https://www.scopus.com/pages/publications/0037009237#tab=citedBy

U2 - 10.1016/S0960-894X(02)00462-6

DO - 10.1016/S0960-894X(02)00462-6

M3 - Article

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AN - SCOPUS:0037009237

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EP - 2358

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 17

ER -

Preparation of oxime dual NK₁/NK₂ antagonists with reduced NK₃ affinity

Abstract

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