Abstract: A benzothiazol compound having the formula is disclosed and is effective to inhibit the production of leukotriene. It is useful against allergy, asthma, affections of the skin, allergic rhinitis and affection of a cardiovascular system. ##STR1## in which R20 is ester or amide and --NR5R6 is amino in variety.
Abstract: The invention relates to compounds of the general formula I ##STR1## wherein R.sub.1 represents one up to and including four, the same or different substituents selected from alkyl(1-6 C), alkoxy(1-6 C), hydroxy, halogen, NO.sub.2, CF.sub.3 or the group --NR.sub.5 R.sub.6, whereby two substituents taken together may also represent a methylene-dioxy group,X represents nitrogen or the group ##STR2## n has the value 0, 1 or 2, R.sub.3 represents one of the moieties: ##STR3## the latter meaning of R.sub.3 (amide) only under the condition that for X is nitrogen the meaning of R.sub.1 is limited to substituents selected from hydroxy, alkoxy(1-6 C) and methylenedioxy, and R.sub.4, R.sub.5 and R.sub.6 represent hydrogen or alkyl(1-6 C), and pharmaceutically acceptable salts thereof, suitable in the treatment of heart failure.
Type:
Grant
Filed:
April 6, 1989
Date of Patent:
May 29, 1990
Assignee:
Akzo N.V.
Inventors:
James Redpath, Robert T. Logan, David B. McFadzen, Robert G. Roy
Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of ##STR2## R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.6 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, halogen, alkoxycarbonyl of 2 to 5 carbon atoms, cyano, ##STR3## R' and R" are individually alkyl of 1 to 5 carbon atoms, R.sub.2 and R.sub.3 together form a member of the group consisting of ##STR4## m is 1, 2 or 3, X.sub.1 and X.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, alkenyl of 2 to 5 carbon atoms, alkoxy of 1 to 5 carbon atoms, aralkoxy, aryloxy, halogen, azido and nitro or taken together form methylenedioxy and their non-toxic, pharmaceutically acceptable acid additon salts capable of treating memory disorders.
Abstract: Heterocyclic compounds of formulae (I) and (II): ##STR1## where R.sup.1 and R.sup.2 are alkyl, R.sup.3 is H or alkyl, m is 2-5 and Het is a hetercycle such as thiazole, benzothiazole, substituted benzothiazole, pyrazine, triazine, thiadiazole, substituted thiadiazole, pyrimidine or substituted pyrimidine. The compounds are calcium channel blockers useful in the treatment of cardiovascular conditions such as hypertension or angina.
Abstract: The invention relates to a method of treatment of ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--(CHR.sup.5).sub.n --CHR.sup.6 -- (Ia)R represents an optionally substituted aryl or heteroaryl radical,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent and said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur;R.sup.5 and R.sup.
Abstract: 5H-pyrido[2',1':2,3]imidazo[4,5-b]indoles of the formulae ##STR1## their pharmaceutically acceptable acid addition salts and the corresponding compounds bearing one or more halogens and/or lower-alkyl groups on the available ring carbon atoms are administered in cholinomimetic amounts to mammals with low acetylcholine or cholinergic activity to ameliorate the symptoms associated with that condition.
Abstract: The present invention provides new tricyclic benzotriazoles of the general formula: ##STR1## wherein Z is a hydrogen atom or an acyl radical, Y is an oxygen or sulphur atom or two hydrogen atoms and X is an oxygen or sulphur atom or a >CR.sub.1 R.sub.2 or >NR.sub.3 group, R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical, R.sub.2 is a hydrogen atom or an alkyl, alkenyl or cyano group or a carbonyl group substituted by a hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino group or R.sub.2, together with R.sub.1, represents a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical and R.sub.3 is a hydrogen atom or an alkyl radical; the tautomers thereof and the physiologically acceptable acid-addition salts thereof with inorganic and organic acids.
Type:
Grant
Filed:
August 3, 1987
Date of Patent:
May 30, 1989
Assignee:
Boehringer Mannheim GmbH
Inventors:
Wolfgang Von Der Saal, Walter-Gunar Friebe, Alfred Mertens, Bernd Muller-Beckmann, Gisbert Sponer
Abstract: The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.
Type:
Grant
Filed:
July 3, 1986
Date of Patent:
May 16, 1989
Assignee:
Boehringer Mannheim GmbH
Inventors:
Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
Abstract: Compounds of formula ##STR1## (wherein R and R.sub.1 have the meanings reported in the specification) and their preparation are described.The compounds of formula I have anti-allergic, anti-anaphylactic and anti-arthritic activity and are useful in pharmaceutical field.Compositions for pharmaceutical use containing a compound of formula I as active ingredient are described too.
Type:
Grant
Filed:
March 23, 1988
Date of Patent:
May 9, 1989
Assignee:
Zambon Group S.p.A.
Inventors:
Dario Chiarino, Gian C. Grancini, Viviana Frigeni, Angelo Carenzi
Abstract: The invention relates to novel, sulfur-containing 5-substituted benzimidazole derivatives of formula I ##STR1## and acid-addition salts thereof antihyperlipoproteinemic action, a process for preparing the same, pharmaceutical formulations comprising the novel compound as active ingredient and a method for inhibiting atherosclerosis, trombus formation and treating hyperlipoproteinemic diseases.
Type:
Grant
Filed:
March 17, 1986
Date of Patent:
March 21, 1989
Assignee:
Richter Gedeon Vegyeszeti Gyar R.T.
Inventors:
Kalmen Harsanyi, Andrea Maderspach, Andres Javor, Gyorgy Hajos, Gyorgy Fekete, Laslo Szporny, Peter Tetenyi, Katalin Csomor, Egon Karpati, Bela Hegedus, Marta Kapolnas nee Pap, Marta Szollosy, Anna Kallay nee Sohonyai
Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.
Abstract: Microbicidal substituted pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl or dialkylaminocarbonylalkyl, or represent in each case optionally substituted oxiranylalkyl, aralkyl, heterocyclyl or aryl andHet represents an optionally substituted heterocyclic radical.Intermediates therefor of the formula ##STR2## in which R is alkyl, are also disclosed.
Type:
Grant
Filed:
July 24, 1986
Date of Patent:
August 30, 1988
Assignee:
Bayer Aktiengesellschaft
Inventors:
Klaus Jelich, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
Abstract: The present invention provides compounds of the general formula: ##STR1## wherein the various substituents are defined hereinbelow. The compounds are used for the treatment and/or prophylaxis of heart and circulatory diseases.
Type:
Grant
Filed:
September 4, 1986
Date of Patent:
March 8, 1988
Assignee:
Boehringer Mannheim GmbH
Inventors:
Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann
Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.
Abstract: Tricyclic oxindole carboxamides, prepared by (a) reaction of an isocyanate with the basic ring system or (b) ammonolysis of a corresponding alkyl ester, are non-steroidal antiinflammatory agents useful in the treatment of rheumatoid arthritis.
Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of hydroxy and aminothiazolyl-benzodiazinone compounds and pharmaceutical compositions including the same.
Type:
Grant
Filed:
November 22, 1985
Date of Patent:
May 19, 1987
Assignee:
William H. Rorer, Inc.
Inventors:
Donald E. Kubla, Henry F. Campbell, William L. Studt, Bruce F. Molino, Thomas J. Tucker
Abstract: Disclosed are substituted or unsubstituted planar tricyclic fluorene or nuclear analogs thereof, spiro-coupled to a five-membered ring containing a secondary amide, and the pharmaceutically acceptable salts thereof. These compounds are useful, inter alia, in the treatment of diabetes. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when indicated for, inter alia, long term, prophylactic treatment of the diabetes syndrome.