Abstract: This invention provides novel isatin compounds which are useful as therapeutic agents. The invention isatin compounds and the pharmaceutically acceptable salts thereof exhibit anti-ulcer activities which are applicable for propylaxis and treatment of ulcer diseases in the digestive tract of animals.
Abstract: The invention relates to new nitrogen-arylmethoxy-thiophene derivatives of the formula I ##STR1## wherein the R--CH.sub.2 --O-group is in position 4 or 5 of the thiophene ring, R denotes a 2-pyridinyl- or 2-quinolinyl group and R.sub.1 denotes a --COO-lower alkyl-, --CO--(CH.sub.2)n--CH.sub.3 or --CH(OH)--(CH.sub.2).sub.n --CH.sub.3 group, wherein n represents an integer from 2 to 6, and their hydrates and/or their pharmaceutically acceptable acid addition salts, a process for their preparation and pharmaceutical products containing these compounds. The new compounds and their salts have useful pharmacological properties. They can be used as active compounds for medicaments for the treatment and prevention of diseases, caused by a disturbance in arachidonic acid metabolism.
Type:
Grant
Filed:
December 24, 1986
Date of Patent:
October 18, 1988
Assignee:
Chemie Linz Aktiengesellschaft
Inventors:
Dieter Binder, Franz Rovenszky, Hubert P. Ferber, Karsten Schror
Abstract: 5-Substituted-3-(2-naphthalenyl)-3-[(1H-imidazol-1-ylmethyl or (1H-1,2,4-triazol-1-ylmethyl)]-2-methylisoxazolidines are useful as antifungal agents.
Abstract: Preparation of a 2-benzoxazolone by reacting an ortho-nitrophenol with carbon monoxide in the presence of a catalytic system comprising(a) palladium and/or a palladium compound(b) a ligand having the formula III ##STR1## in which Z and Y are the same or different bridging groups each of which has 3 or 4 atoms in the bridge, of which atoms at least two are carbon atoms and which groups Z and Y may be bound to each other by means of a connection other than that already formed by the carbon atoms shown in formula III and(c) an anion of an acid having a pK of less than 2, except of a hydrohalogenic acid.
Abstract: Oxazole and isoxazole derivatives of the formula ##STR1## wherein A is C.sub.1-6 -alkylene, Het is a 2-R-oxazol-5-yl, 5-R-oxazol-2-yl, 4-R-oxazol-2-yl, 2-R-oxazol-4-yl, 3-R-isoxazol-5-yl or 5-R-isoxazol-3-yl group which is optionally substituted on the heterocyclic ring by a C.sub.1-6 -alkyl group, R is phenyl or thienyl monosubstituted or disubstituted by halogen, trifluoromethyl or C.sub.1-6 -alkylthio, R.sup.1 and R.sup.2 each is a C.sub.1-6 -alkyl group and R.sup.3 is a hydroxy or C.sub.1-6 -alkoxy group or a group of the formula --NR.sup.4 R.sup.5 in which R.sup.4 and R.sup.5 each is a hydrogen atom or a C.sub.1-6 -alkyl group or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached is a 5-membered or 6-membered saturated heteromonocyclic ring which may contain an oxygen or sulphur atom or an additional nitrogen atom, and pharmaceutically acceptable salts of the compounds of formula I in which R.sup.3 is a hydroxy group with bases, have anti-arthritic activity.
Type:
Grant
Filed:
October 10, 1986
Date of Patent:
September 27, 1988
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Peter J. Machin, John M. Osbond, Christopher R. Self, Carey E. Smithen, Brian P. Tong
Abstract: There are disclosed compounds of the formula ##STR1## wherein ##STR2## R.sup.2 is hydrogen, loweralkyl, loweralkoxy, lower alkoxycarbonyl, trifluoromethyl, nitro, cyano or halo;R.sup.3 is hydrogen or loweralkyl;R.sup.4 is hydrogen, lower alkyl, --COOR.sup.3 or ##STR3## R.sup.5 is lower alkyl, monofluoroloweralkyl, difluoroloweralkyl, polyfluoroloweralkyl, perfluoroloweralkyl or ##STR4## and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and as antiinflammatory agents.
Type:
Grant
Filed:
May 15, 1987
Date of Patent:
September 20, 1988
Assignee:
American Home Products Corporation
Inventors:
John H. Musser, Dennis M. Kubrak, Anthony F. Kreft, III, Reinhold H. W. Bender
Abstract: A process for the manufacture of 5-cyano-4-methyl-oxazole which comprises reacting a 5-(lower alkoxycarbonyl)-4-methyl-oxazole with ammonia in the gaseous phase, in the presence of a zirconium oxide or hafnium oxide catalyst.
Abstract: 5-(phenyl or phenoxymethyl)-3-(2-furanyl)-3-(1H-imidazol-1-ylmethyl)-2-methylisoxazolid ine and related derivatives in which one or more hydrogens on the phenyl ring are replaced by halogen, lower alkyl, lower alkoxy, nitro and combinations thereof are useful as antifungal agents.
Abstract: Substituted 3,5-diphenyl-3-[(1H-1,2,4-triazol-1-yl) methyl]-2-methylisoxazolidines in which hydrogens of their phenyl rings may be replaced by halogen, lower alkoxy, lower alkyl or nitro groups are useful as antifungal agents.
Abstract: 5-(Phenyl or phenoxymethyl)-3-(2-thienyl)-3-(1H-imidazol-1-ylmethyl)-2-methylisoxazolid ines and related derivatives in which one or more hydrogens on the 5-phenyl or phenoxy rings are replaced by halogen, lower alkyl, lower alkoxy, nitro and combinations thereof are useful as antifungal agents.
Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is a hydrogen atom or a C.sub.1-6 alkyl group, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are selected from hydrogen, hydroxyl, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy and C.sub.1-4 alkanoyl; G is a hydrogen atom or a hydroxyl group, and m and n are independently integers of from 1 to 3, with the proviso that when G is a hydroxyl grup, m or n is 1;is useful in the treatment of asthma.
Abstract: Alkyl and aryl ester compounds, 5-(acyloxyalkyl)-3-phenyl-3-(1H-imidazol-1-ylmethyl)-2-methylisoxazolidine s in which hydrogens of their phenyl rings may be replaced by halogen, lower alkyl, lower alkoxy or nitro groups are useful as antifungal agents.
Abstract: 3-Phenyl-3-(1H-imidazol-1-ylmethyl)-2-methyl-5-[(phenylamino)methyl]isoxazo lidine and related derivatives in which hydrogens of their phenyl rings may be replaced by one or more halogen, lower alkoxy, lower alkyl and nitro groups are useful as antifungal agents.
Abstract: 3-Phenyl-3-(1H-1,2,4-triazol-1-methyl)-2-methyl-5-alkylisoxazolidines and related derivatives in which hydrogens in the phenyl ring are replaced by halogen, lower alkyl or lower alkoxy groups are useful as antifungal agents.
Abstract: 5-(Hydroxy or alkoxyalkyl)-3-phenyl-3-(1H-imidazol-1-ylmethyl)-2-methylisoxazolidines and related derivatives in which hydrogens of the phenyl ring are replaced by halogen, lower alkyl or lower alkoxy groups are useful as antifungal agents.
Abstract: Analgesic 1,2,3,4-tetrahydroisoquinolines of the formula (1) ##STR1## wherein R.sub.1 and R.sub.2 respectively are hydrogen, hydroxy or alkoxy of 1 to 4 carbon atoms, R.sub.3 and R.sub.4 respectively are hydrogen or alkyl of 1 to 4 carbon atoms, and R.sub.5 is hydroxy, nitro or ##STR2## wherein R.sub.6 and R.sub.7 respectively are hydrogen, alkyl of 1 to 4 carbon atoms or RCO-- wherein R is hydrogen or alkyl of 1 to 4 carbon atoms; pharmaceutically acceptable addition salts thereof with non-toxic acids; analgesic compositions thereof in an inert, pharmaceutical carrier; and methods of preparation from corresponding R.sub.1, R.sub.2, R.sub.3 and R.sub.4 -substituted tetrahydroisoquinolines.
Abstract: The compound (S)(+)-4,4'-(1-methyl-1,2-ethanediyl)-bis(2,6-piperazinedione) is prepared by treating propylenediamine tetraacetic tetraamide in a dipolar aprotic solvent with an alkali metal derivative of dimethyl sulfoxide to form a dialkali metal salt of (S)(+)-4,4'-(1-methyl-1,2-ethanediyl)-bis(2,6-piperazinedione); and neutralizing the dialkali metal salt.