Azacyclic compounds, processes for their preparation and pharmac

Details Azacyclic compounds, processes for their preparation and pharmac Azacyclic compounds, processes for their preparation and pharmac

1994-02-16

1995-10-17

Ivy, C. Warren

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546174, 546175, 546176, 546180, 546195, 546200, 546209, 546210, 546212, 546213, 546216, 546219, 546220, 546221, 546281, 548146, C07D20712, C07D21142, C07D70504, C07D40904

Patent

active

054592704

ABSTRACT:
##STR1## Compounds of formula (I), and salts and prodrugs thereof wherein n is 1, 2 or 3; X represents O or S; R.sup.1 represents optionally substituted phenyl; R.sup.2 represents aryl, heteroaryl, benzhydryl, or benzyl; R.sup.4 and R.sup.5 each independently represent H, halo, CH.sub.2 OR.sup.9, C.sub.1-6 alkyl, oxo, CO.sub.2 R.sup.10 or CONR.sup.10 R.sup.11 ; R.sup.8 represents H, COR.sup.9, CO.sub.2 R.sup.10 or optionally substituted C.sub.1-6 alkyl; R.sup.9 represents H, C.sub.1-6 alkyl or phenyl; and R.sup.10 and R.sup.11 each independently represent H or C.sub.1-6 alkyl; are tachykinin antagonists. They and compositions thereof are useful in medicine.

REFERENCES:
The Journal of Organic Chemistry, vol. 56, No. 18, Aug. 30, 1991, 5237-5239.
I. Ojima et al. J. Org. Chem. 1991, 56, 5263-5277.
Chemical Abstracts, vol. 96, 1982, 607-608.
Chemical Abstracts, vol. 112, 1990 p. 599.
Chemical Abstracts, vol. 95, 1981 p. 677.
J. Am. Chem. Soc., 1983, 105, 6339-6342, M. Yamashita et al.
Chemical Abstracts, vol. 102, 1985, p. 609.
Chemical Abstracts, vol. 102, 1985, 569-570.
J. Am. Chem. Soc., 1983, 105, 6339-6342.

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