Abstract: Compounds of the class of 1-heteroarylsulphonyl-2-imino-imidazolidines which are substituted in the 3-position by an aliphatic or cycloaliphatic hydrocarbon radical, especially a cycloalkyl radical, and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties. In particular, they possess hypoglycaemic activity and can be used for the treatment of hyperglycaemia in mammals. A specific embodiment is 1-[5-(2-butyramido-ethyl)-2-thienylsulphonyl]-2-imino-5-cyclohexyl-imidazo lidine.
Type:
Grant
Filed:
July 15, 1974
Date of Patent:
March 2, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Atso Ilvespaa, Andre Gagneux, Ernst Schweizer, Jorg Frei
Abstract: Compounds of the class of 6-substituted 11b-phenyl-3,11b-oxazirino[2,3-d]-s-triazolo[4,3-a][1,4]benzodiazepines have valuable pharmacological properties and are active ingredients for therapeutic compositions. In particular, these new compounds have an anticonvulsive action and inhibit somatic reflexes. Specific embodiments are 10-chloro-11b-phenyl-3,11bH-oxazirino[2,3-d]-s-triazolo[4,3-a][1,4] benzodiazepine-6-methanol, 10-chloro-11b-phenyl-3,11bH-oxazirino[2,3-d]-s-triazolo[4,3-a][1,4]benzodi azepine-6-carboxaldehyde-diethylacetal and 10-chloro-11b-(o-chlorophenyl)-3,11bH-oxazirino[2,3-d]-s-triazolo[4,3-a][1 ,4]benzodiazepine-6-carboxaldehyde-diethylacetal.
Abstract: A compound of formula ##SPC1##Is produced by reacting 4.alpha.,5.alpha.-epoxy-9,10-dioxatricyclo[4,3,1,0.sup.3,8 ]decane with ammonia or a reaction functional derivative thereof; it is an intermediate for the synthesis of prostaglandins.
Abstract: Benzocycloalkenderivatives substituted in 1-position by carboxyl and carboxyalkyl or two carboxyl groups, and further substituted in the benzene ring by cycloalkyl and optionally other substituents, their esters, amides and pharmaceutically acceptable salts have antiinflammatory and analgesic activity and can be used for the treatment of inflammatory conditions and pain in mammals; a representative embodiment is 1-methoxycarbonyl-5-cyclohexyl-6-chloro-1-indanecarboxylic acid.
Type:
Grant
Filed:
August 16, 1973
Date of Patent:
February 24, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Georges Haas, Erwin F. Jenny, Alberto Rossi
Abstract: Compounds of the formula ##SPC1##Wherein R.sub.1 represents lower alkyl, cycloalkyl or phenyl which is optionally substituted by halogen, lower alkyl or lower alkoxy, and one of the groups R.sub.2 and R.sub.3 represents phenyl which is optionally substituted by halogen, lower alkyl, hydroxy, lower alkoxy, lower alkylthio or lower alkylsulphonyl, and the other represents a 6-membered heteroaromatic radical containing 1 or 2 ring nitrogen atoms, their N-oxides and salts, with anti-inflammatory, antinociceptive and antipyretic activity, they are active ingredients of pharmaceutical compositions and can be used for the relief and removal of pain as well as for the treatment of rheumatic, arthritic and other inflammatory complaints; an illustrative example is 2-isopropyl-4(5)-(p-methoxyphenyl)-5(4)-3-pyridyl-imidazole.
Abstract: 4-Phenylethers of 3-amino-5-sulfamoylbenzoic acids, e.g. those of the formula ##SPC1##R = an aliphatic or araliphatic radicalX = o or SPh.degree. = a phenylene radicalR' = h, alkyl or Ph.degree.--R"One of R.degree. and R" is NH.sub.2 and the other is Halkyl esters or salts thereof are diuretic agents.
Abstract: 2-Pyrazolyl-benzophenones, e.g. those of the formula ##SPC1##R.sup.o = H, alkyl, (HO, alkoxy, amino)- alkyl, aralkyl or arylR = h or alkylR',r" = h, alkyl,alkoxy, halo or CF.sub.3Am = open or cyclic amino groupCorresponding ketals, carbinols, acyl derivatives or therapeutically useful acid addition salts thereof exhibit antianxiety and antidepressant effects.
Abstract: A process for the manufacture of aldehydes of the general formula ##EQU1## in which the symbols R.sub.1, R.sub.2 and R.sub.3 stand for hydrogen or organic radicals and in which at least two of these radicals are linked together by fragmenting a corresponding aziridine compound of the general formula ##EQU2## in which R.sub.1, R.sub.2 and R.sub.3 are as above and R.sub.4 to R.sub.7 each represents hydrogen, an alkoxycarbonyl, cyano, nitro or sulphonyl group or an alkyl, alkenyl, cycloalkenyl or alkyl residue and two or more of these residues may be linked together with simultaneous evolution of nitrogen.
Abstract: The present invention relates to new pharmaceutical compositions comprising an .alpha.-receptor blocker, a .beta.-receptor blocker and a pharmaceutical carrier and to a method of using said compositions in the treatment of high blood pressure and angina pectoris.
Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##SPC1##R.sub.1 = h or alkylR.sub.2 = h, alk(en)yl, cycloalk(en)- yl or cycloalk(en)yl-alkylA = hydroxylated lower alkyleneAnd functional derivatives thereof, are anti-inflammatory agents.
Type:
Grant
Filed:
March 25, 1974
Date of Patent:
February 3, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Richard William James Carney, George DE Stevens
Abstract: Compounds selected from the group consisting of amines of the formula I ##EQU1## in which R.sub.1 and R.sub.2 stand for a member selected from lower alkyl, lower alkenyl, cycloalkyl having 4 to 7 ring members, phenyl-lower alkyl, phenyl-lower alkyl substituted in the phenyl residue by a member selected from lower alkyl, lower alkoxy, halogen and trifluoromethyl, lower alkylene, oxalower alkylene, aza-lower alkylene and thia-lower alkylene, and one of R.sub.1 and R.sub.2 stands for hydrogen and the other has the above meanings, Ph stands for a member selected from meta- and para-phenylene and meta- and para-phenylene substituted by a member selected from lower alkyl, lower alkenyl, lower alkinyl, mercapto-lower alkyl, hydroxy-lower alkyl, phenyl, cyano, hydrogen, halogen, lower alkoxy, lower alkenyloxy, lower alkinyloxy, mono-, di and trihalogeno-lower alkyl, cycloalkyl having 5 to 7 ring members and phenoxy, and R.sub.
Abstract: The new hypocalcaemically active peptides of formula Ih-cys-Gly-Asn-Leu-Ser-Thr-Cys-Met-Leu-Gly-Thr-Tyr-Thr-Gln-Asp-Phe-Asn-Lys-P he-His-Thr-Phe-Pro-Gln-Thr-Ala-Ile-Gly-val-Gly-Ala-Pro-OHand corresponding compounds in which one or more of the asparagine and glutamic acid radicals are replaced by the aspartic acid or glutamic acid radical and/or the aspartic acid radical is replaced by the asparagine radical, their dimers, especially those in which 2 identical peptide sequences (1-32 and 1'-32') are joined in an anti-parallel arrangement via the cysteine radicals 1,7' and 7,1' by means of a disulfide bond, and derivatives are useful as hypocalcaemic agents and are prepared by splitting off groups protecting at least one amino or one carboxyl group or oxidizing the corresponding sulfides to the disulfides or condensing together adequate peptides.
Type:
Grant
Filed:
July 14, 1972
Date of Patent:
January 20, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Werner Rittel, Max Brugger, Bruno Kamber, Bernhard Riniker, Peter Sieber, Hendrik Marie Greven
Abstract: New 2-amino-5-sulphamoylbenzoic acid amide of the general formula ##SPC1##Wherein R.sub.1 denotes lower alkyl, R.sub.2 denotes hydrogen, halogen, trifluoromethyl, lower alkyl or lower alkoxy, R.sub.3 denotes hydrogen, hydroxyl or lower alkyl, R.sub.4 denotes acyl and alk denotes lower 1,2-alkylene or 1,3-alkylene or a therapeutically acceptable acid addition salt thereof are usefull as mild analgesics with an anti-inflammatory component of action.
Type:
Grant
Filed:
May 22, 1974
Date of Patent:
January 20, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Pier Giorgio Ferrini, Georges Haas, Alberto Rossi
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 amino, 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, esterfied or amidised carboxyl, sulpho or sulphonamido and therapeutically acceptable salts thereof are useful as anti-allergic and hypolipidaemic agents.
Type:
Grant
Filed:
October 24, 1973
Date of Patent:
January 20, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Georges Haas, Roland Jaques, Alberto Rossi, Martin Ruegg
Abstract: 3-Amino-4-anilino-5-sulfamoylbenzoic acids, e.g. those of the formula ##SPC1##R = an aliphatic or araliphatic radicalR' = h, alkyl, or aminophenylAlkyl esters or salts thereof are diuretic agents.
Abstract: 3-R-Methyl-7-amino-ceph-2-em-4.xi.-carboxylic acid compounds, in which R is the C-residue of a C-nucleophilic compound are valuable intermediates, for example, in the manufacture of the corresponding 3-R-methyl-7-amino-ceph-3-em-4-carboxylic acid compounds with antibiotic properties.
Type:
Grant
Filed:
July 2, 1971
Date of Patent:
January 13, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Heinrich Peter, Herman Robert Rodriguez, Hans Bickel