Abstract: A pharmaceutical composition with analgesic properties which contains a pharmaceutically acceptable salt of diclofenac and a pharmaceutically acceptable salt of codeine in the weight ratio of about 1:1 to 3:1, and the preparation and use thereof.
Abstract: Novel hydrazones derived from 3-formylrifamycin S or SV as the aldehydo component and a bi- or tri-cyclic N-aminopiperazine as the hydrazino component and having the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6, independently of one another, each represents a hydrogen atom or C.sub.1-4 -alkyl,m and n, independently of one another, each represents an integer from 0 to 5,X represents C.sub.1-5 -alkylidene, benzylidene or C.sub.1-4 -alkoxymethylene,Y represents C.sub.1-5 -alkylidene, C.sub.1-4 -alkoxymethylene, oxy, thio or optionally substituted imino of the formula --N(R)-- wherein R represents hydrogen, C.sub.1-4 -alkyl, C.sub.3-5 -alkenyl, C.sub.3-12 -cycloalkyl or phenyl, orX and Y together represent 1,2-cycloalkylene or o-phenylene each of which can be substituted by from one to three C.sub.
Abstract: Particulate hydroperoxidized poly-N-vinyl lactam containing an average of about 0.5 to 20 hydroperoxy mole equivalents per mole of poly-N-vinyl lactam, the preparation of the same by subjecting particulate poly-N-vinyl lactam to an effective amount of ozone, and the use thereof in the preparation of graft copolymers possessing a low degree of extractibles, finding utility in a wide number of fields, particularly in biomedical devices, semipermeable membranes, and as films or fibers.
Abstract: 1-phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.
Type:
Grant
Filed:
June 20, 1985
Date of Patent:
June 30, 1987
Assignee:
Ciba-Geigy Corporation
Inventors:
Alex Alder, Jaroslav Stanek, Daniel Bellus
Abstract: Organic aprotic solvent soluble polymers which are derivatives of a polyvinyl alcohol, having a weight average molecular weight of at least about 2,000, and containing from about 0.5 to about 90 percent, based on the number of hydroxyl groups in said polyvinyl alcohol, of units of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently alkylene, arylene, cycloaliphatic, aralkylene or aralkarylene, n is 0 or 1, A.sub.1 is a carbamoyloxy or ureido linking group, A is an oxa, imino or ureido group, R.sub.3 is hydrogen or methyl, R.sub.4 is hydrogen, or when R.sub.3 is hydrogen, methyl or also -COOR.sub.5 where B.sub.5 is hydrogen or lower alkyl, and crosslinked hydrogel contact lenses made therefrom and their preparation.
Abstract: 7.alpha.-acylthio-9.alpha.,11.alpha.-epoxy-20-spirox-4-ene-3,21-diones of the formula I ##STR1## in which R represents lower alkanoyl and --A--A-- represents an ethylene or cyclopropylene group, have a high aldosterone-antagonistic activity without significant sexually-specific side-effects and can be used as potassium-protecting diuretics in the treatment of various forms of hyperaldosteronism. The compounds can be obtained by conventional processes of steroid chemistry.
Abstract: Storage stable, quick-disintegrating pressed shapes containing pharmaceutical active substances, which shapes consist substantially of a compressed mixture of(a) an effective amount of a pharmaceutical active substance in granular form, which is coated with a coating material comprising essentially a homogeneous mixture of a poly(H+meth)-acrylic acid-(methyl+ethyl) ester insoluble but dispersible in water and an ethyl cellulose insoluble but dispersible in water, the weight ratio of the acrylic acid ester to ethyl cellulose being 2.5:1 to 5:1;(b) talcum; and(c) colloidal silicon dioxide, and crosslinked polyvinylpolypyrrolidone as the disintegrating agent having a high disintegrating capacity and good binding properties.
Abstract: The invention relates to lipopeptides of the formula I, ##STR1## in which each of R.sub.a.sup.1 and R.sub.b.sup.1, independently of the other, represents an aliphatic or cycloaliphatic-aliphatic hydrocarbon radical having from 7 to 21 carbon atoms that is optionally substituted by oxygen functions, orone of the radicals R.sub.a.sup.1 --CO-- and R.sub.b.sup.1 --CO-- represents hydrogen and the other of the radicals R.sub.a.sup.1 --CO-- and R.sub.b.sup.1 --CO-- represents an acyl radical, wherein R.sub.a.sup.1 and R.sub.b.sup.1 have the meanings given above,R.sup.2 represents an aliphatic or cycloaliphatic-aliphatic hydrocarbon radical having from 1 to 21 carbon atoms that is optionally substituted by oxygen functions,n=0 or 1,As.degree. represents a radical of the formula --O--Kw--CO-- or --NH--Kw--CO-- wherein Kw represents an aliphatic hydrocarbon radical having a maximum of 12 carbon atoms,As.sup.1 represents a D- or L-.alpha.-amino acid,each of Z.sup.1 and Z.sup.
Type:
Grant
Filed:
July 17, 1985
Date of Patent:
May 19, 1987
Assignee:
Ciba-Geigy Corporation
Inventors:
Gerhard Baschang, Albert Hartmann, Oskar Wacker
Abstract: Organic aprotic solvent insoluble polymers which are derivatives of a polyvinyl alcohol, having a weight average molecular weight of at least about 2,000, and containing from about 0.5 to about 90 percent, based on the number of hydroxyl groups in said polyvinyl alcohol, of an addition reaction product of units of the formula ##STR1## with a vinylic monomer, wherein R.sub.1 and R.sub.2 are independently alkylene, arylene, cycloaliphatic, aralkylene or aralkarylene, n is 0 or 1, A.sub.1 is a carbamoyloxy or ureido linking group, A is an oxa, imino or ureido group, R.sub.3 is hydrogen or methyl, R.sub.4 is hydrogen, or when R.sub.3 is hydrogen, methyl or also --COOR.sub.5 where R.sub.5 is hydrogen or lower alkyl, and hydrogel contact lenses made therefrom and their preparation.
Abstract: The invention relates to pharmaceutical preparations containing compounds of formula I ##STR1## in which X.sub.1 and X.sub.2, independently of each other, represent hydrogen, halogen, unsubstituted or substituted amino or a quaternary ammonium salt; etherified or esterified hydroxy; free, etherified, esterified or oxidized mercapto; nitro; functionally modified formyl; free or functionally modified carboxyl; acyl; an unsubstituted or substituted hydrocarbon radical, or an unsubstituted or substituted heterocyclic radical; with the proviso that at least one of the radicals X.sub.1 and X.sub.2 is bonded by a carbon atom to the ring system and with the proviso that X.sub.1 and X.sub.2 cannot be together halogen and formyl; in which Y represents oxygen, sulfur, sulfinyl or sulfonyl but must be sulfur, sulfinyl or sulfonyl, if X.sub.1 is hydrogen and X.sub.
Type:
Grant
Filed:
August 24, 1984
Date of Patent:
May 12, 1987
Assignee:
Zyma SA
Inventors:
Christian G. Rimbault, Philippe M. Narbel
Abstract: Photosensitive compositions of matter which are capable of undergoing condensation or addition reactions and may or may not be crosslinkable, and which contain an anthraquinone of the formula I ##STR1## in which X, X', R' and R" are as defined in patent claim 1 and X or X' is, for example, --OH or --NH.sub.2, at least one monomeric, oligomeric or polymeric compound which can be reacted with this anthraquinone, for example, if X is --OH, a polymer with terminal glycidyl groups, and, where relevant, a crosslinking agent and/or a salt of a metal of group Ib or VIII of the periodic table, are suitable for image formation by means of electroless metal deposition.
Type:
Grant
Filed:
November 4, 1985
Date of Patent:
April 14, 1987
Assignee:
Ciba-Geigy Corporation
Inventors:
Jurgen Finter, Walter Fischer, Friedrich Lohse
Abstract: Compounds of the formula ##STR1## in which R.sub.1 is lower alkyl substituted by hydroxy or by protected hydroxy,R.sub.2 represents carboxy or functionally modified carboxy, andR.sub.3 represents amino, lower alkyl-substituted amino, substituted methyleneamino or protected amino,optical isomers of compounds of the formula I, mixtures of these optical isomers, and salts of such compounds of the formula I that have a salt-forming group have antibiotic activity. The compounds of the formula I are manufactured according to processes that are known per se.
Abstract: The present invention relates to desulfatohirudins, to the preparation thereof, to pharmaceutical compositions containing these compounds, and to the use thereof.The desulfatohirudins of this invention correspond to hirudin in biological activity and are therefore particularly useful for inhibiting blood clotting.
Type:
Grant
Filed:
November 21, 1984
Date of Patent:
March 31, 1987
Assignees:
Ciba-Geigy Corporation, Plantorgan Werk Heinrich G.E. Christensen KG
Inventors:
Hans Fritz, Johannes Dodt, Ursula Seemuller, Ernst Fink
Abstract: The invention concerns compounds of formula I ##STR1## wherein R is a fluorine, bromine or iodine atom or the amino, acetylamino, methyl, cyano, hydroxyl, methoxy or trifluoromethyl group, the tautomeric forms thereof, and acid addition salts of the compounds in which R represents amino. The products have antithrombotic activity. They can be prepared according to methods known per se.
Abstract: Novel asymmetric thioethers of the formula ##STR1## in which R.sup.1 represents a C.sub.1-3 -alkyl radical or a C.sub.1-3 -hydroxyalkyl radical of which the hydroxy group may be in esterified form,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,R.sup.3 represents hydroxy, alkoxy or an optionally substituted amino group, and-X- represents a single bond, a methylene group or an optionally N-acylated primary aminomethylene groupwherein the O-atom of the hydroxy group is in the transconfiguration relative to the S-atom, are effective as leucotriene-antagonists since they eliminate the contractions of smooth muscles caused by leucotrienes and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.
Type:
Grant
Filed:
June 25, 1985
Date of Patent:
March 10, 1987
Assignee:
Ciba-Geigy Corporation
Inventors:
Andreas von Sprecher, Ivan Ernest, Alan J. Main, Andreas Beck
Abstract: Perfluoroalkyl-alkyl-sulfide or sulfonyl-alkylene esters of meta- and para-pyromellitates, partially esterified with 3-chloro-1,2-propane diol, of the formulae: ##STR1## or mixtures thereof, wherein R.sub.f is perfluoroalkyl of 3 to 18 carbon atoms, andm is 0 or 2, are useful for incorporation into organic polymers to render them oil repellent and soil resistant.
Abstract: Pharmaceutical preparations containing (+)-cyanidan-3-ol derivatives of the formula I ##STR1## wherein R' and R" are hydrogen, an unsubstituted or substituted hydrocarbon radical, or heterocyclic radical, halogen, formyl, free or functionally modified carboxyl, free or etherified or esterified hydroxyl, free, etherified or oxidized mercapto, unsubstituted or substituted sulfamoyl, acyl or unsubstituted or substituted amino, where however R' and R" cannot both be hydrogen simultaneously, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each hydrogen or an unsubstituted or substituted hydrocarbon radical, and R.sub.2 and R.sub.3 together can also be an unsubstituted or substituted methylene group, and R.sub.1 also an acyl group or an amidated carboxyl group; and therapeutically applicable salts of these compounds, as well as new compounds of these preparations.These pharmaceutical preparations are particularly valuable for treating liver and venous diseases.
Type:
Grant
Filed:
July 9, 1985
Date of Patent:
February 17, 1987
Assignee:
Zyma SA
Inventors:
Marc E. Ballenegger, Christian G. Rimbault, Alban I. Albert, Andre J. Weith, Pierre Courbat, Robert G. Tyson, Derek R. Palmer, David G. Thompson
Abstract: There are described sugar derivatives of the formula I ##STR1## that have immuno-stimulating action and that contain as inventive element at least one radical A.sup.1 or A.sup.2. These radicals A.sup.1 and A.sup.2, which may be constituents of the radicals R.sup.1, R.sup.2, R.sup.4, R.sup.6, R.sup.9, R.sup.10 or R.sup.12 according to formula I, are defined as follows:A.sup.1 represents lower alkanoyl that is substituted by aryl, heteroaryl or heteroarylthio and that may be additionally substituted by an ethylene radical which, with the above-mentioned aryl or heteroaryl substituent, forms a five-membered ring or represents ortho- or ortho/meta-substituted aroyl. A.sup.2 represents lower alkoxy substituted by aryl heteroaryl or heteroarylthio.Also described are processes for the manufacture of the compounds of the formula I and novel intermediates.
Type:
Grant
Filed:
May 29, 1985
Date of Patent:
February 3, 1987
Assignee:
Ciba-Geigy Corporation
Inventors:
Gerhard Baschang, Albert Hartmann, Oskar Wacker
Abstract: The invention relates to a novel crystal modification, containing water of crystallization, of disodium 3-amino-1-hydroxypropane-1,1-diphosphonate of the formula ##STR1## and to a process for the manufacture thereof. This modification is suitable for the oral treatment of disorders of the calcium and phosphate metabolism and associated diseases in warm-blooded animals.
Type:
Grant
Filed:
July 29, 1985
Date of Patent:
January 27, 1987
Assignees:
Ciba-Geigy Corporation, Henkel Kommanditgesellschaft auf Aktien
Abstract: The invention relates to novel, modified eglins B and C, to the preparation thereof, and to pharmaceutical compositions which contain these compounds. Compared with eglin B and C, the modification consists in a terminal shortening. The compounds of the invention can be prepared e.g. by limited enzymatic proteolysis of elgins or by peptide synthesis.