Abstract: Compounds of the formula ##STR1## WHEREIN Ar.sub.1 and Ar.sub.2 denote an optionally substituted aromatic hydrocarbon radical or a monocyclic, monoazacyclic or diazacyclic radical of aromatic character and Alk represents lower alkylene, or salts thereof, exhibit .beta.-receptor-blocking, blood pressure-lowering and vasodilatory effects and are useful for example in the treatment of arrythmias and angina pectoris, and as blood pressure-lowering agents.
Type:
Grant
Filed:
May 5, 1975
Date of Patent:
May 31, 1977
Assignee:
Ciba-Geigy Corporation
Inventors:
Knut A. Jaeggi, Franz Ostermayer, Herbert Schroter
Abstract: Compounds of the formula ##STR1## in which R.sub.1 represents an aminopyridinium radical and R.sub.2 a heterocyclic radical of aromatic character, bonded to the sulphur atom via a carbon atom, and containing at least 2 nitrogen atoms and additionally a further hetero-atom selected from nitrogen, oxygen and sulphur. They have antimicrobial activity.
Abstract: Novel aminomethyl compounds of the formula ##STR1## wherein X denotes sulphur or oxygen, R denotes hydrogen or an amino protective group, R.sub.1 denotes hydrogen, a free, etherified or esterified hydroxyl group or mercapto group or a substituted ammonium group, R.sub.2 denotes hydroxyl or a carboxyl protective radical which together with the carbonyl grouping of the formula -C(=0)- forms a protected carboxyl group, and their salts, are antibacterial antibiotics or intermediates for the preparation thereof; pharmaceutical preparations containing such active compounds, are useful for combating micro-organisms such as gram-positive or gram-negative bacteria; An illustrative example is 3-acetoxymethyl-7.beta.-[2-(5-aminomethyl-2-thienyl)-acetylamino]-ceph- 3-em-4-carboxylic acid.
Type:
Grant
Filed:
March 24, 1975
Date of Patent:
May 17, 1977
Assignee:
Ciba-Geigy Corporation
Inventors:
Beat Muller, Heinrich Peter, Peter Schneider, Hans Bickel
Abstract: 6-Aryl-1- or 2H,4H-pyrazolo[4,3-d](2)-benzazepines, e.g. those of the formula ##STR1## R = H or alkyl R.degree. = H, alkyl, (HO, alkoxy, amino)-alkyl, aralkyl, aryl or acyl,R' = h, oh or alkylR" = h, alkyl, alkoxy, halo or CF.sub.3N-oxides thereof or therapeutically useful acid addition salts of such compounds exhibit antianxiety and antidepressant effects.
Abstract: 2-Pyrazolyl-benzophenones, e.g. those of the formula ##STR1## CORRESPONDING KETALS, CARBINOLS, ACYL DERIVATIVES OR THERAPEUTICALLY USEFUL ACID ADDITION SALTS THEREOF EXHIBIT ANTIANXIETY AND ANTI-DEPRESSANT EFFECTS.
Abstract: 9-(2-A-3-R-propyl)-9,10-dihydro-9,10-ethanoanthracenes containing the nucleus of the formula ##STR1## wherein R denotes a secondary or tertiary amino group and A denotes a free, etherified or acylated hydroxyl group, their pharmaceutically acceptable salts are useful as psychotropics, especially as anti-depressants.
Type:
Grant
Filed:
April 2, 1975
Date of Patent:
April 12, 1977
Assignee:
Ciba-Geigy Corporation
Inventors:
Max Wilhelm, Raymond Bernasconi, Angelo Storni, Dieter Beck, Karl Schenker
Abstract: The present invention relates to 1,4-dihydropyridines of the formula I ##STR1## and their tautomers, wherein R.sub.1 represents an aryl radical, R.sub.2 and R.sub.3 independently of one another represents hydrogen or a hydrocarbon radical, R.sub.4 represents an alkyl, aryl or aralkyl radical, R.sub.5 denotes an alkoxy radical, which is optionally substituted by an amino group, or denotes an amino group and n is 1 or 2, especially to the 2,6-dimethyl-3-carbomethoxy-5-methylsulphonyl-4-(2-trifluoromethylphenyl)- 1,4-dihydro-pyridine and to the 2,6-dimethyl-3-carbomethoxy-5-methylsulphonyl-4-(2-nitrophenyl)-1,4-dihydr opyridine.They have an antihypertensive activity.
Abstract: Pyrrolyl compounds of the formula I ##STR1## wherein Py is optionally lower-alkylated l-pyrrolyl, Ph is phenylene, R.sub.1 is hydrogen or lower alkyl and R.sub.2 is hydrogen, lower alkyl, aryl-lower alkyl or optionally functionally modified carboxy-lower alkyl or R.sub.1 and R.sub.2 together are loweralkylene, oxa-lower alkylene, thia-lower alkylene or aza-lower alkylene, their antipodes and salts, which are valuable blockers of adrenergic .beta.-receptors and useful in the treatment of heart and circulatory ailments.
Type:
Grant
Filed:
November 24, 1975
Date of Patent:
April 5, 1977
Assignee:
Ciba-Geigy Corporation
Inventors:
Knut A. Jaeggi, Franz Ostermayer, Herbert Schroter
Abstract: 6-Acylamino-penam-3-carboxylic acids and 7-acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula ##STR1## IN WHICH R.sub.1 is hydrogen, R.sub.2 is optionally substituted phenyl, thienyl or furyl or R.sub.1 and R.sub.2 together are optionally substituted cycloalkyl, n and m independently of one another represent 0 or 1 and B represents an optionally substituted 2,6-dioxo- or 2,6-dithioxo-1,2,3,6-tetrahydro-pyrimidyl, 2-thioxo-6-oxo-1,2,3,6-tetrahydropyrimidyl, 2,6-dihydroxy- or 2,6-dimercapto-pyrimidyl, 2-mercapto-6-hydroxy-pyrimidyl, 2,6-diaminopyrimidyl, 2-amino-6-hydroxy-pyrimidyl or 2,6-dihalogenopyrimidyl radical, these radicals being bonded in the 4- or 5-position.
Type:
Grant
Filed:
September 18, 1973
Date of Patent:
March 29, 1977
Assignee:
Ciba-Geigy Corporation
Inventors:
Karoly Kocsis, Bruno Fechtig, Hans Bickel
Abstract: Amines of the formula ##SPC1##Wherein R.sub.1 is lower alkyl, lower alkoxy or amino, R.sub.2 is hydrogen or lower alkyl, R.sub.3 is hydrogen, lower alkyl, carboxyl or lower alkoxycarbonyl, R.sub.4 is hydrogen or lower alkyl, R.sub.5 is lower alkyl, aryl-lower alkyl or optionally functionally modified carboxy-lower alkyl and R.sub.6 denotes halogen, trifluoromethyl, lower alkyl, lower alkenyl, lower alkoxy, lower alkenyloxy, nitro, lower alkoxymethyl, carbamoyl, N-lower alkylcarbamoyl, nitrile, lower alkinyloxy or hydrogen, and their salts block cardiac and vascular .beta.-receptors the are useful in the treatment of arrhythenias and angina pectoris and as intermediates for, especially for pharmaceutically active substances.
Type:
Grant
Filed:
June 4, 1973
Date of Patent:
March 29, 1977
Assignee:
Ciba-Geigy Corporation
Inventors:
Knut Alfred Jaeggi, Franz Ostermayer, Herbert Schroter
Abstract: The invention concerns a new process for the manufacture of 3-substituted thiomethyl-7-amino-3-cephem-4-carboxylic acid compounds which comprises reacting a 3-y-methyl-7-amino-3-cephem-4-carboxylic acid compound, in which Y is hydroxy or esterified hydroxy, with a mercaptane compound, if necessary, in the presence of an optionally protonic Lewis acid, particularly trifluoroacetic acid.
Type:
Grant
Filed:
January 27, 1975
Date of Patent:
March 29, 1977
Assignee:
Ciba-Geigy Corporation
Inventors:
Heinrich Peter, Beat Muller, Walter Sibral, Hans Bickel
Abstract: Compounds of the class of spiro[norbornane-2,3'-piperidines], spiro[bicyclo[2.2.2]octane-2,3'-piperidines], and corresponding spiro-pyrrolidine derivatives which are unsubstituted at the ring nitrogen atom or substituted by neutral or basic radicals, and the pharmaceutically acceptable acid addition salts of these new compounds possess valuable pharmacological properties and are active ingredients for pharmaceutical compositions. In particular, these new compounds have an antiviral activity. Specific embodiments are (1RS,2RS,4SR)-spiro[norbornane-2,3'-piperidine]-hydrochloride and 1'-[2-(2-azaspiro[5.5]undec-2-yl)-ethyl]-spiro[bicyclo[2.2.2]octane-2,3'-p iperidine]-dihydrochloride.
Type:
Grant
Filed:
July 23, 1975
Date of Patent:
March 29, 1977
Assignee:
Ciba-Geigy Corporation
Inventors:
Karl Schaffner, Alex Meisels, Jean Claude Roger, Claus D. Weis
Abstract: Compounds of the formula Ir.sub.1 -- ph -- X -- alk -- R.sub.2 (I)wherein R.sub.1 is adamantyl, Ph is phenylene which is optionally substituted by, nitro, lower alkyl, lower alkoxy, halogen or trifluoromethyl, X is oxy or thio, alk is alkylene with 1 to 20 C atoms or alkenylene with 2 to 20 C atoms and R.sub.2 is free, esterified or amidised carboxyl, sulpho or sulphonamido and therapeutically acceptable salts thereof are useful as anti-allergic and hypolipidaemic agents.
Type:
Grant
Filed:
August 18, 1975
Date of Patent:
March 22, 1977
Assignee:
Ciba-Geigy Corporation
Inventors:
Georges Haas, Roland Jaques, Alberto Rossi, Martin Ruegg
Abstract: New compounds of the general formula Ir.sub.1 -- ph -- X -- CR.sub.2 R.sub.4 -- alk -- R.sub.3 (I)wherein R.sub.1 denotes a cycloalkenyl radical or a monocyclic cycloalkyl radical, Ph denotes an optionally substituted phenylene radical, X denotes the oxy or thio group, R.sub.2 denotes hydrogen or alkyl, R.sub.3 denotes an optionally functionally modified carboxyl group, a sulpho group or a sulphamido group, alk denotes an alkylene or alkenylene radical which separates the groups R.sub.1 --Ph--X--CR.sub.2 R.sub.4 and R.sub.3 by at least 2 carbon atoms and R.sub.4 is hydrogen or, if alk separates the groups R.sub.1 --Ph--X--CR.sub.2 R.sub.4 and R.sub.3 by at least 3 carbon atoms or R.sub.1 denotes a cycloalkenyl radical, R.sub.4 can also denote alkyl, in the free form or in the form of salts are useful as antiallergics.
Type:
Grant
Filed:
September 11, 1974
Date of Patent:
March 22, 1977
Assignee:
Ciba-Geigy Corporation
Inventors:
Georges Haas, Pier Giorgio Ferrini, Alberto Rossi
Abstract: Compounds of the formula ##STR1## wherein R.sub.1.sup.a represents hydrogen or an amino protective group R.sub.1.sup.A and R.sub.1.sup.b represents hydrogen or an acyl group Ac, or R.sub.1.sup.a and R.sub.1.sup.b together represent a bivalent amino protective group, and R.sub.2 represents hydroxyl or a radical R.sub.2.sup.A which together with the carbonyl grouping --C(=O)-- forms a protected carboxyl group, as well as 1-oxides thereof, and salts of such compounds with salt-forming groups, are prepared from compounds of the formula ##STR2## wherein R.sub.1.sup.a and R.sub.1.sup.b have the above mentioned meaning, R denotes an acyloxy group, R.sub.2.sup.a has the meaning of R.sub.2 or R and R.sub.2.sup.o together denote an epoxy group, from a 1-oxide thereof or a salt of such a compound, by reduction with a metal which has a normal potential of -2.4 to -0.40 volt, or an amalgam thereof, at a pH of 1 to 8, in the presence of water.
Abstract: A vehicle comprising: a) a conventional body with at least 3 pairs of rolls mounted on horizontal axles, which are distributed over the periphery of opposite sides of the body and connected thereto; b) a pair of annular, elastically deformable running tires, each of which encircles all of the rolls at one body's side and suspends them above the ground; c) at least one steerable or revolving wheel, ski and/or float resiliently mounted at another side of the body and d) at least one motor operatively connected to the rolls, tires and/or wheel for driving and braking them.
Abstract: The treatment of Osteoarthritis by orally administering a pharmaceutical preparation containing a furanoside of the formula I ##STR1## wherein R.sub.1 is hydrogen or alkyl with up to 7 carbon atoms, and R.sub.3, R.sub.5 and R.sub.6 each independently is hydrogen, alkyl with up to 7 carbon atoms, alkenyl with up to 7 carbon atoms, benzyl, halogeno-benzyl, (C.sub.1 -C.sub.7 -alkyl)-benzyl, (C.sub.1 -C.sub.7 -alkoxy)-benzyl or trifluoromethyl-benzyl.