Leo Pharmaceutical Products, Ltd.

Leo Pharmaceutical Products Ltd. A/s

Leo Pharmaceutical Products Ltd. A/s (lovens Kemiske Fabrik

Lovens Kemiske Fabrik Produktionsaktieselskab

A/s Lovens Kemiske Fabrik Produktionsakieselskab

A/s Lovens Kemiske Fabrik Produktionsaktieselskab

Ole Bent Nielsen

Peter Werner Feit

Herta Bruun

Ian Ahnfelt-Ronne

Claus Aage Bretting

Erik T Hansen

Schneur Rachlin

Dorte Kirstein

The present invention relates to compounds of formula ##STR1## in which formula I X stands for O, S, ##STR2## R.sub.1 and R.sub.2 which can be the same or different stand for hydrogen, straight or branched, saturated or unsaturated, unsubstituted or substituted C.sub.1- C.sub.8 -alkyl, aryl or for ar-C.sub.1 -C.sub.4 -alkyl, aryl and ar being unsubstituted or substituted phenyl; R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are the same or different and stand for hydrogen, halogen, pseudo halogen, cyano, nitro, amino, carboxy, hydroxy, alkyl, alkoxy; or R.sub.5 and R.sub.6 form an aromatic ring which is fused to the pyridyl ring, and which aromatic ring may substituted; provided that R.sub.1 and R.sub.2 cannot be hydrogen at the same time, and provided that when R.sub.5 and R.sub.6 both are chlorine and R.sub.1 is hydrogen, then R.sub.2 cannot be n-propyl; and salts and bioreversible derivatives thereof. The compounds of formula I are useful in the human and veterinary therapy, as they exert specific 5-lipoxygenase inhibition.

2-quinolinyl methoxy compounds, medical uses and intermediates therefor

Substituted quinolines and medicinal use thereof

The present invention relates to compounds of formula ##STR1## in which formula I X stands for O, S, ##STR2## R.sub.1 and R.sub.2 which can be the same or different stand for hydrogen, straight or branched, saturated or unsaturated, unsubstituted or substituted C.sub.1 -C.sub.8 -alkyl, aryl or for ar-C.sub.1 -C.sub.4 -alkyl, aryl and ar being unsubstituted or substituted phenyl; R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are the same or different and stand for hydrogen, halogen, pseudo halogen, cyano, nitro, amino, carboxy, hydroxy, alkyl, alkoxy; or R.sub.5 and R.sub.6 form an aromatic ring which is fused to the pyridyl ring, and which aromatic ring may substituted; provided that R.sub.1 and R.sub.2 cannot be hydrogen at the same time, and provided that when R.sub.5 and R.sub.6 both are chlorine and R.sub.1 is hydrogen, then R.sub.2 cannot be n-propyl; and salts and bioreversible derivatives thereof. The compounds of formula I are useful in the human and veterinary therapy, as they exert specific 5-lipoxygenase inhibition.

Quinoline and pyridine compounds and inhibition of 5-lipoxygenases

The present invention relates to compounds of formula I ##STR1## in which formula I X stands for O, S, ##STR2## R.sub.1 and R.sub.2 which can be the same or different stand for hydrogen, straight or branched, saturated or unsaturated, unsubstituted or substituted C.sub.1 -C.sub.8 -alkyl, or for ar-C.sub.1 -C.sub.4 -alkyl, aryl and ar being unsubstituted or substituted phenyl; R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are the same or different and stand for hydrogen, halogen, pseudo halogen, cyano, nitro, amino, carboxy, hydroxy, alkyl, alkoxy; or R.sub.5 and R.sub.6 form an aromatic ring which is fused to the pyridyl ring, and which aromatic ring may substituted; provided that R.sub.1 and R.sub.2 cannot be hydrogen at the same time, and provided that when R.sub.5 and R.sub.6 both are chlorine and R.sub.1 is hydrogen, then R.sub.2 cannot be n-propyl; and salts and bioreversible derivatives thereof. The compounds of formula I are useful in the human and veterinary therapy, as they exert specific 5-lipoxygenase inhibition.

Pyridyl and quinoline derivatives

The invention relates to a series of new compounds, salts thereof and to methods for the preparation of the compounds which have the general formula ##STR1## in which R.sub.1 stands for an unsubstituted or substituted phenoxy, phenylthio, benzyl, phenylsulfinyl, or anilino radical;

Compositions and methods for the treatment of hypertension or oedemas

Sulphonamides, compositions containing the same and methods for using

Compounds of the general formulae ##STR1## in which R.sub.1 represents a straight or branched, optionally substituted alkyl, alkenyl or alkynyl radical; R.sub.2 stands for an optionally substituted phenyl radical; Y stands for oxygen, sulphur or a methylene radical; X stands for O or H.sub.2 ; their salts and esters and methods for their preparation. The compounds of the invention possess an outstanding diuretic and saluretic activity with a very low excretion of potassium ions and a low toxicity.

Sulfamylbenzoic acid derivatives

The present invention relates to a series of new compounds, their salts and esters and to methods for the preparation of the compounds having the general formula: ##SPC1## In which R.sub.1 represents a straight or branched C.sub.1 -C.sub.6 alkyl, alkenyl or alkynyl radical, or a C.sub.1 -C.sub.3 alkyl radical substituted with phenyl, halophenyl, trifluoromethylphenyl, (lower alkoxy)phenyl, or with a 5-membered or 6-membered heterocyclic ring containing not more than two heteroatoms selected from the group consisting of oxygen, sulphur and nitrogen; R.sub.2 stands for hydrogen or a straight or branched C.sub.1 -C.sub.6 alkyl, alkenyl, alkynyl or alkoxy radical, optionally being substituted with halogen, a lower alkoxy or di-(lower alkyl) amino radical; Ar stands for a phenyl radical, optionally being substituted with halogen, lower alkyl, or lower alkoxy; Y stands for oxygen, sulphur or a methylene radical. The compounds of the invention which are valuable in the human and veterinary practice, possess a pronounced diuretic and/or saluretic activity.

Benzoyl-benzoic acid derivatives

Compounds of the general formula ##SPC1## In which R.sub.1 represents a straight or branched C.sub.1 -C.sub.6 alkyl, alkenyl or alkynyl radical, or a C.sub.1 -C.sub.3 alkyl radical substituted with phenyl, halophenyl, trifluoromethylphenyl, (lower alkoxy)phenyl, or with a 5-membered or 6-membered heterocyclic ring containing not more than two heteroatoms selected from the group consisting of oxygen, sulphur and nitrogen; R.sub.2 stands for a phenyl radical, optionally being substituted with halogen, lower alkyl, hydroxy, or lower alkoxy; X and Y stand for oxygen or sulphur; their salts and esters and methods for their preparation. The compounds of the invention possess an outstanding diuretic and saluretic activity with a very low excretion of potassium ions and a low toxicity.

Certain 4-phenoxy-3-heteroarylmethyl or ethyl sulfamyl benzoic acid

The present invention relates to a series of new compounds, their salts and esters and to methods for the preparation of the compounds having the general formula: ##SPC1## In which R.sub.1 represents a straight or branched C.sub.1 -C.sub.6 alkyl, alkenyl or alkynyl radical, or a C.sub.1 -C.sub.3 alkyl radical substituted with phenyl, halophenyl, trifluoromethylphenyl, (lower alkoxy)phenyl, or with a 5-membered or 6-membered heterocyclic ring containing not more than two heteroatoms selected from the group consisting of oxygen, sulphur and nitrogen; Ar stands for a phenyl radical, optionally being substituted with halogen, lower alkyl, hydroxy, or lower alkoxy; Y stands for O, S, NH or a CH.sub.2 radical; and YR.sub.1 is placed in the 2- or 3-position. The compounds of the invention which are valuable in the human and veterinary practice, possess a pronounced diuretic and/or saluretic activity.

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Vanlose, Denmark

Ole Bent Nielsen