Substituted pyrroles
AssigneeHoffmann-La Roche Inc.
InventorsPeter D. Davis, Christopher H. Hill, Geoffrey Lawton
Life of this patent
Estimating the term…
Abstract
Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and Y have the signficance given in the description, are useful in the control or prevention of inflammatory, immunological, bronchopulmonary or cardiovascular disorders.
Claims12
A compound of the formula ##STR14## wherein R.sup.1 signifies hydrogen, alkyl, aryl, aralkyl, alkoxyalkyl, hydroxyalkyl, haloalkyl, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, trialkylaminoalkyl, aminoalkylaminoalkyl, azidoalkyl, acylaminoalkyl, acylthioalkyl, alkylsulphonylaminoalkyl, arylsulphonylaminoalkyl, mercaptoalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, alkylsulphonyloxyalkyl, alkylcarbonyloxyalkyl, cyanoalkyl, amidinoalkyl, isothiocyanatoalkyl, glucopyranosyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, hydroxyalkylthioalkyl, mercaptoalkylthioalkyl, arylthioalkyl or carboxyalkylthioalkyl or a group of the formula ##STR15## in which Het signifies a heterocyclyl group.
- W signifies NH, S or a bond,
- T signifies NH or S
- V signifies O, S, NH. NNO.sub.2, NCN or CHNO.sub.2,
- Z signifies alkylthio, amino, monoalkylamino or dialkylamino,
- Im signifies 1-imidazolyl,
- Ar signifies aryl, and
- n stands for 2-6;
- R.sup.2 signifies hydrogen, alkyl, aralkyl, alkoxyalkyl, hydroxyalkyl, haloalkyl, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, acylaminoalkyl, alkylsulphonylaminoalkyl, arylsulphonylaminoalkyl, mercaptoalkyl, alkylthioalkyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylthio or alkylsulphinyl;
- R.sup.3 signifies a carbocyclic or heterocyclic aromatic group;
- R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently signify hydrogen, halogen, alkyl, hydroxy, alkoxy, aryloxy, haloalkyl, nitro, amino, acylamino, monoalkylamino, dialkylamino, alkylthio, alkylsulphinyl or alkylsulphonyl;
- and one of X and Y signifies O and the other signifies O, S, (H,OH) or (H,H);
- with the proviso that R.sup.1 has a significant different from hydrogen when R.sup.2 signifies hydrogen, R.sup.3 signifies 3-indolyl or 6-hydroxy-3-indolyl, R.sup.4, R.sup.5 and R.sup.7 each signify hydrogen, R.sup.6 signifies hydrogen or hydroxy and X and Y both signify O and when R.sup.2 signifies hydrogen, R.sup.3 signifies 3-indolyl, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each signify hydrogen, X signifies (H,H) and Y signifies O;
- or a pharmaceutically acceptable salt of acidic compounds of formula I with bases and of basic compounds of formula I with acids.
A pharmaceutical composition comprising an effective amount of a compound of the formula ##STR17## wherein R.sup.1 signifies hydrogen, alkyl, aryl, aralkyl, alkoxyalkyl, hydroxyalkyl, haloalkyl, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, trialkylaminoalkyl, aminoalkylaminoalkyl, azidoalkyl, acylaminoalkyl, acylthioalkyl, alkylsulphonylaminoalkyl, arylsulphonylaminoalkyl, mercaptoalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, alkylsulphonyloxyalkyl, alkylcarbonyloxyalkyl, cyanoalkyl, amidinoalkyl, isothiocyanatoalkyl, glucopyranosyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, hydroxyalkylthioalkyl, mercaptoalkylthioalkyl, arylthioalkyl or carboxyalkylthioalkyl or a group of the formula ##STR18## in which Het signifies a heterocyclyl group,
- W signifies NH, S or a bond,
- T signifies NH or S,
- V signifies O, S, NH, NNO.sub.2, NCN or CHNO.sub.2,
- Z signifies alkylthio, amino, monoalkylamino or dialkylamino,
- Im signifies 1-imidazolyl,
- Ar signifies aryl, and
- n stands for 2-6;
- R.sup.2 signifies hydrogen, alkyl, aralkyl, alkoxyalkyl, hydroxyalkyl, haloalkyl, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, acylaminoalkyl, alkylsulphonylaminoalkyl, arylsulphonylaminoalkyl, mercaptoalkyl, alkylthioalkyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylthio or alkylsulphinyl;
- R.sup.3 signifies a carbocyclic or heterocyclic aromatic group;
- R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently signify hydrogen, halogen, alkyl, hydroxy, alkoxy, aryloxy, haloalkyl, nitro, amino, acylamino, monoalkylamino, dialkylamino, alkylthio, alkylsulphinyl or alkylsulphonyl;
- and one of X and Y signifies O and the other signifies O, S, (H,OH) or (H,H);
- with the proviso that R.sup.1 has a significance different from hydrogen when R.sup.2 signifies hydrogen, R.sup.3 signifies 3-indolyl or 6-hydroxy-3-indolyl, R.sup.4, R.sup.5 and R.sup.7 each signify hydrogen, R.sup.6 signifies hydrogen or hydroxy and X and Y both signify O and when R.sup.2 signifies hydrogen, R.sup.3 signifies 3-indolyl, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each signify hydrogen, X signifies (H,H) and Y signifies O;
- or a pharmaceutically acceptable salt of acidic compounds of formula I with bases and of basic compounds of formula I with acids, and an inert carrier material.
Dependencies are inferred from the claim text.