Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1994-03-24
1995-11-07
Tsang, Cecilia
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C07D27300, C07D41300, C07D45100
Patent
active
054647886
ABSTRACT:
Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO.sub.2 --, --(CH.sub.2).sub.p -- or --CO--(CH.sub.2).sub.p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R.sup.5, R.sup.6 or R.sup.7 ; R.sup.1 is hydrogen, cyano, phenyl,--CONHR.sup.2, --CONR.sup.2 R.sup.2, --(CH.sub.2).sub.m --OR.sup.2, --(CH.sub.2).sub.p --S(O).sub.r --R.sup.2, --(CH.sub.2).sub.m --CO.sub.2 R.sup.2, --(CH.sub.2).sub.m --N.sub.3, --(CH.sub.2).sub.m --NH.sub.2 or --(CH.sub.2).sub.m --NR.sup.2 R.sup.2 ; R.sup.2 is hydrogen, C.sub.3-8 cycloalkyl or C.sub.1-5 alkyl; R.sup.5 and R.sup.6 are each independently selected from hydrogen, C.sub.1-5 alkoxy, halogen or --(CH.sub.2).sub.n --N(R.sup.2)--C(O)--R.sup.18 ; R.sup.7 is hydrogen or ##STR2## R.sup.11 is selected from hydrogen, C.sub.1-5 alkylcarbonyl, ##STR3## or substituted C.sub.1-5 alkyl wherein said alkyl substituent is unsubstituted, mono-, di- or tri-substituted pyridyl wherein said substitutents on said pyridyl are independently selected from halogen, C.sub.1-5 alkyl or C.sub.1-5 alkoxyl; R.sup.13 is unsubstituted or substituted C.sub.1-10 alkyl wherein the substituent is selected from --N(R.sup.2).sub.2, --NHR.sup.2 or imidazolyl; R.sup.14 and R.sup.15 are each independently selected from C.sub.1-5 alkyl, C.sub.1-5 alkoxy or halogen; R.sup.16 is hydrogen or oxo; R.sup.18 is C.sub.1-5 alkoxyl, unsubstituted or substituted C.sub.1-5 alkyl where said substituent is Het, unsubstituted or substituted C.sub.2-5 alkenyl where said subsituent is Het or Het; Het is benzimidazolyl, carboxymethyl-substituted benzimidazolyl or indolyl; m is an integer of from 1 to 5; p is an integer of from 1 to 3; and r is an integer of from 0 to 2. Such compounds as useful as oxytocin and vasopressin receptor antagonists.
REFERENCES:
patent: 4087425 (1978-05-01), Garcia et al.
patent: 4147870 (1979-04-01), Garcia et al.
patent: 4894386 (1990-01-01), Brown et al.
patent: 5091387 (1992-02-01), Evans et al.
patent: 5204349 (1993-04-01), Bock et al.
D. J. Pettibone, et al., Drug Dev. Res. (1993) 30, 129-142, entitled L-368,899, A Potent Orally Active Oxytocin Antagonist For Potential Use In Preterm Labor.
B. E. Evans, et al., J. Med. Chem. (1993) 36, 3993-4005, entitled Nanomolar-Affinity, Non-Peptide Oxytocin Receptor Antagonists.
M. G. Bock, et al., Vasopressin (1993), J. Libbey Eurotext, pp. 539-547.
P. D. Williams, et al., J. Med. Chem. (1994) 37, 565-571.
D. J. Pettibone, et al., Reg. Peptides (1993) 45, 289-293, entitled Development and Pharmacological Assessment of Novel Peptide and Nonpeptide Oxytocin Antagonists.
B. E. Evans, et al., J. Med. Chem. (1992) 35, 3919-3927, entitled Orally Active, Nonpeptide Oxytocin Antagonists.
D. J. Pettibone, et al., J. Pharm. Exp. Ther. (1992) 264, 308-314, entitled Identification of an Orally Active, Nonpeptide Oxytocin Antagonist.
Bock Mark G.
Culberson J. Christopher
Evans Ben E.
Gilbert Kevin F.
Rittle Kenneth E.
Appollina Mary A.
Merck & Co. , Inc.
Tsang Cecilia
Winokur Melvin
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