Volume 27, Issue 11
Heterocyclic Compounds
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ChemInform Abstract: 1-(1-(4-((N-Acetyl-4-piperidinyl)oxy)-2-methoxybenzoyl)piperidin-4-yl)- 4H-3,1-benzoxazin-2(1H)-one (L-371,257): A New, Orally Bioavailable, Non-Peptide Oxytocin Antagonist.

P. D. WILLIAMS

P. D. WILLIAMS

Dep. Med. Chem., Merck Res. Lab., West Point, PA 19486, USA

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B. V. CLINESCHMIDT

B. V. CLINESCHMIDT

Dep. Med. Chem., Merck Res. Lab., West Point, PA 19486, USA

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J. M. ERB

J. M. ERB

Dep. Med. Chem., Merck Res. Lab., West Point, PA 19486, USA

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R. M. FREIDINGER

R. M. FREIDINGER

Dep. Med. Chem., Merck Res. Lab., West Point, PA 19486, USA

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M. T. GUIDOTTI

M. T. GUIDOTTI

Dep. Med. Chem., Merck Res. Lab., West Point, PA 19486, USA

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E. V. LIS

E. V. LIS

Dep. Med. Chem., Merck Res. Lab., West Point, PA 19486, USA

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J. M. PAWLUCZYK

J. M. PAWLUCZYK

Dep. Med. Chem., Merck Res. Lab., West Point, PA 19486, USA

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D. J. PETTIBONE

D. J. PETTIBONE

Dep. Med. Chem., Merck Res. Lab., West Point, PA 19486, USA

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D. R. REISS

D. R. REISS

Dep. Med. Chem., Merck Res. Lab., West Point, PA 19486, USA

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D. F. VEBER

D. F. VEBER

Dep. Med. Chem., Merck Res. Lab., West Point, PA 19486, USA

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C. J. WOYDEN

C. J. WOYDEN

Dep. Med. Chem., Merck Res. Lab., West Point, PA 19486, USA

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First published: March 12, 1996

Abstract

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ChemInform Abstract

In comparison with the uterine oxytocin receptor OPC 21268 (Xb) and similarly structured derivatives, compound (Xa) is found to be a more potent antagonist of oxytocin-induced contractions of rat uterus in vitro and in vivo having significant oral bioavailability in rats and suited as potential new therapeutic agent for treating preterm labor.

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