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US 5,811,553 AGranted
Quinoline derivatives(2)
AssigneeSmithKline Beecham Farmaceutici S.p.A.
InventorsCarlo Farina, Giuseppe Arnaldo Maria Giardina, Mario Grugni, Luca Francesco Raveglia
Life of this patent
Estimating the term…
Abstract
NK.sub.3 receptor antagonists of formula (I): ##STR1## are useful in treating inter alia pulmonary disorders, CNS disorders and neurodegenerative disorders.
Claims2
A process for preparing a compound of formula (I) ##STR244## wherein Ar is phenyl, 2-chlorophenyl, 2-thienyl or cyclohexadienyl;
- R is methyl, ethyl, n-propyl, --COOMe, or --COMe;
- R.sub.1 and R.sub.2 are each hydrogen or methyl;
- R.sub.3 is hydrogen, methoxy, or hydroxy;
- R.sub.4 is hydrogen, methyl, ethyl, methoxy, hydroxy, amino, chlorine, bromine, dimethylaminoethoxy, 2-(1-phthaloyl)ethoxy, aminoethoxy, 2-(1-pyrrolidinyl)ethoxy, dimethylaminopropoxy, dimethylaminoacetylamino, acetylamino, or dimethylaminomethyl;
- R.sub.5 is phenyl, 2-thienyl, 2-furyl, 2-pyrryl, 2-thiazolyl or 3-thienyl;
- and X is oxygen,
- or a solvate or salt thereof which comprises reacting a compound of formula (III) ##STR245## in which R', R'.sub.1, R'.sub.2 and Ar' are R, R.sub.1, R.sub.2 and Ar as defined above or a group or atom convertible to R, R.sub.1, R.sub.2 and Ar, with a compound of formula (II) ##STR246## or an active derivative thereof, in which R'.sub.3, R'.sub.4, R'.sub.5 and X' are R.sub.3, R.sub.4, R.sub.5 and X as defined above or a group convertible to R.sub.3, R.sub.4, R.sub.5 and X, to form a compound of formula (Ic) ##STR247## and optionally thereafter performing one or more of the following steps:
- (a) where R', R'.sub.1 to R'.sub.5, Ar' and X' are other than R, R.sub.1 to R.sub.5, Ar and X, converting any one of R', R'.sub.1 to R'.sub.5, Ar' and X' to R, R.sub.1 to R.sub.5, Ar and X to obtain a compound of formula (I),
- (b) where R', R'.sub.1 to R'.sub.5, Ar' and X' are R, R.sub.1 to R.sup.5, Ar and X, converting any one of R, R.sub.1 to R.sub.5, Ar and X to another R, R.sub.1 to R.sub.5, Ar and X, to obtain a compound of formula (I),
- (c) forming a salt and/or solvate of the obtained compound of formula (Ic).
7 more elements
Dependencies are inferred from the claim text.