Abstract: The invention relates to the use of known N-phenyl-2-pyrimidine derivatives for inhibiting proteinkinase C in warm-blooded animals as antitumor agents. ##STR1## The substituents in formula I are as defined in claim 1.
Abstract: Compounds of formula I ##STR1## wherein R.sub.1 -R.sub.5, X, Ar and Y are as defined in the description, have valuable pharmaceutical properties and are especially effective as leukotriene antagonists. They are prepared in a manner known per se.
Type:
Grant
Filed:
August 10, 1994
Date of Patent:
April 16, 1996
Assignee:
Ciba-Geigy Corporation
Inventors:
Andreas von Sprecher, Andreas Beck, Marc Gerspacher
Abstract: Compounds of formula I ##STR1## wherein Ar.sub.1, Ar.sub.2, A.sub.1, A.sub.2, R and X are as defined in the description, exhibit valuable pharmaceutical properties and are effective especially against diseases responsive to the inhibition of protein kinases, for example tumors. They are prepared in a manner known per se.
Abstract: The invention relates to novel thiosemicarbazonethiones of formula (I) wherein R.sub.1 is lower alkyl, lower alk-2-en-1-yl or also lower alk-2-yn-1-yl, R.sub.2 and R.sub.3 are each independently of the other hydrogen or lower alkyl or, taken together, are lower alkylidene, R.sub.4 is hydrogen, lower alkyl, lower alkoxy, aryl or aryl-lower alkyl, R.sub.5 is lower alkyl, aryl, aryl-lower alkyl, unsaturated or saturated heterocyclyl-lower alkyl, or is also lower alkyloxycarbonyl-lower alkyl, and the salts thereof, to a process for the preparation of these compounds, to pharmaceutical compositions containing them, and to the use thereof as medicaments.
Abstract: Substituted 2-aminoalk-3-enoic acid derivative of formula I ##STR1## wherein R.sub.1 is an aliphatic hydrocarbon radical that is substituted by hydroxy, and R.sub.2 is free or esterified carboxy, and their salts exhibit NMDA-antagonistic properties and are useful as active ingredients of anticonvulsive medicaments.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
January 30, 1996
Assignee:
Ciba-Geigy Corporation
Inventors:
Christof Angst, Hans Allgeier, Roland Heckendorn, Daniel Wallach
Abstract: New devices and kits for solid-phase immuno-assays comprising a solid porous support, preferably in the form of a sheet, where antigens or immuno-globulins or both of them are bound by direct application in any suitable geometry, e.g. as an assay of dots or lines. Such porous supports are suitable for effecting an unlimited number of antibody-antigen reactions simultaneously and in one operation.
Type:
Grant
Filed:
April 10, 1987
Date of Patent:
January 23, 1996
Assignee:
Ciba-Geigy Corporation
Inventors:
Julian Gordon, Richard Hawkes, Evelyn Niday, Harry Towbin
Abstract: The present invention relates to aqueous depot formulations of hirudin, particularly desulphatohirudin, which are very stable. These formulations contain water, hirudin, and calcium, magnesium, or zinc ions in the form of water insoluble salts, the salts being in a concentration of from 100 mM to 600 mM.
Abstract: The invention relates to color-stable tablets for the therapeutic drug oxcarbazepine, which tablets are provided with a hydrophilic, permeable layer containing white pigments and a hydrophilic, permeable outer layer containing white pigments in combination with iron(II) oxide pigments.
Abstract: The invention relates to pharmaceutical compositions in the form of parenterally, especially intravenously, administrable liposome dispersions or dry preparations, especially lyophilisates, that can be used therefor, comprising the zinc-phthalocyanine complex and synthetic, substantially pure phospholipids.
Type:
Grant
Filed:
October 28, 1994
Date of Patent:
November 14, 1995
Assignee:
Ciba-Geigy Corporation
Inventors:
Peter Schneider, Peter van Hoogevest, Hans G. Capraro, Ute Isele
Abstract: The invention relates to the 3-(1'-hydroxyethyl)-2-azetidinone of formula ##STR1## which can be transformed into 4-acyloxy-3-(1-hydroxyethyl)-2-azetidinone derivatives. The latter can be used as starting materials for the manufacture of a large number of highly active .beta.-lactam antibiotics.
Type:
Grant
Filed:
September 15, 1994
Date of Patent:
October 31, 1995
Assignee:
Ciba-Geigy Corporation
Inventors:
Peter Schneider, Gerardo Ramos, Jacques Bersier
Abstract: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.
Type:
Grant
Filed:
November 30, 1994
Date of Patent:
October 24, 1995
Inventors:
Jaroslav Stanek, Jorg Frei, Giorgio Caravatti
Abstract: P-substituted aminoalkylphosphinic acids of the formula ##STR1## wherein R denotes an optionally fluorinated methyl group, R.sub.1 denotes hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or a fluorinated methyl group and R.sub.2 and R.sub.3 denote hydrogen or R.sub.2 denotes hydroxy, lower alkoxy or halogen and R.sub.3 is hydrogen or R.sub.2 and R.sub.3 together represent an oxo group, and their pharmaceutically acceptable salts are active as GABA.sub.b -agonists and can be used in the treatment of spinal spasticity, multiple sclerosis and cerebral palsy, trigeminus neuralgia, drug withdrawal syndromes and/or conditions of pain. They can be manufactured by methods known per se and suitable such methods are described.
Type:
Grant
Filed:
November 4, 1993
Date of Patent:
October 24, 1995
Assignee:
Ciba-Geigy Corporation
Inventors:
Roger G. Hall, Ludwig Maier, Wolfgang Frostl
Abstract: Compounds of formula I ##STR1## wherein Z, R, R.sub.1, R.sub.2 and X are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.
Type:
Grant
Filed:
September 15, 1994
Date of Patent:
October 10, 1995
Assignee:
Ciba-Geigy Corporation
Inventors:
Marc Lang, Edmond Differding, Jaroslav Stanek
Abstract: Compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and q are as defined in the description, have valuable pharmacological properties and are especially effective as calcium metabolism regulators. They are prepared in a manner known per se.
Abstract: The compounds of the formula ##STR1## in which one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen, C.sub.1-8 -alkyl, C.sub.3-6 -cycloalkyl, phenyl optionally substituted by halogeno, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy and/or trifluoromethyl, or C.sub.7-10 -phenylalkyl optionally substituted in the phenyl moiety by halogeno, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy and/or trifluormethyl, and the other two are hydrogen, or salts thereof.These compounds have valuable pharmaceutical properties.
Type:
Grant
Filed:
June 7, 1994
Date of Patent:
October 10, 1995
Assignee:
Ciba-Geigy Corporation
Inventors:
John G. Dingwall, Josef Ehrenfreund, Roger G. Hall, James Jack
Abstract: N-(tetrahydropyran-4-yloxy-alkanoyl)-staurosporin derivatives of formula I ##STR1## wherein R.sub.1 is hydrogen, hydroxy, lower alkoxy or oxo,R.sub.2 is hydrogen or C.sub.1-4 alkyl andR.sub.3 is hydrogen or C.sub.1-4 alkyl,processes and novel intermediates for the preparation thereof and processes for the preparation of the intermediates are described. The compounds of formula I inhibit the enzyme protein kinase C with a high degree of selectivity and can be used especially as tumour-inhibiting active ingredients.
Abstract: 4-(7-Bromo-5-methoxybenzofuran-2-yl)piperidine (brofarornine) of formula I ##STR1## and its pharmaceutically acceptable salts can be used as active ingredients in medicaments for retarding the degeneration of nerve cells that accompanies degenerative nerve disorders, and as a nootropic agent for treating disorders that are responsive to treatment with nootropic agents.
Abstract: (-)-Galanthamine is obtained in substantially high yield and purity substantially without concomitant production of epigalanthamine by conversion of racemic narwedine to (-)-narwedine and subsequent reduction to (-)-galanthamine using bulky organo-aluminum or organo-boron reducing agents.
Abstract: N-aralkyl- and N-heteroaralkyl-aminoalkanephosphinic acids of formula I ##STR1## wherein R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical having at least 2 carbon atoms, R.sub.1 is hydrogen or hydroxy, R.sub.2 is an araliphatic or heteroarylaliphatic radical substituted by free or functionally modified carboxy that is bonded directly or by way of a spacer, and R.sub.3 is hydrogen, lower alkyl or a group R.sub.2, and the salts thereof have valuable nootropic and anti-epileptic properties and can be used in the preparation of a nootropic or anti-epileptic medicament.
Type:
Grant
Filed:
May 4, 1994
Date of Patent:
June 13, 1995
Assignee:
Ciba-Geigy Corporation
Inventors:
Stuart J. Mickel, Wolfgang Frostl, Pascal Furet
Abstract: The invention relates to a therapeutic system for peroral administration and having systemic action, which system is in the form of a coated and/or laminated mono-compartment system for administering carbamazepine. The therapeutic system comprises(a) a wall made of a material which is permeable to water and impermeable to the components of the drug-containing core,(b) a core containing finely particulate carbamazepine as drug and, as auxiliaries, a protective colloid that inhibits the crystal growth of carbamazepine in the presence of water, a swellable hydrophilic polymer and, optionally, a water-soluble compound for inducing osmosis and/or further pharmaceutically acceptable excipients, and(c) a passageway through the wall (a) for delivering the core components to the environmental body fluid. The therapeutic system can be used as an anticonvulsive for the treatment of convulsive states, especially epileptic states.