Abstract: The invention relates to topically adminstrable pharmaceutical preparations containing pharmaceutically acceptable methanediphosphonic acid derivatives of formula ##STR1## and their salts, wherein each of R.sub.1 and R.sub.2 is halogen, or wherein R.sub.1 is hydrogen and R.sub.2 is Ar--S-- or Het.sub.1 --NH--, in which Ar is unsubstituted or substituted phenyl and Het.sub.1 is unsubstituted or substituted, monocyclic, 5- or 6-membered monoaza-, diaza- or thiaza-aryl that is bonded via a ring carbon atom, or wherein R.sub.1 is hydrogen or hydroxy and R.sub.2 is --A--R.sub.3, in which A is alkylene and, on the one hand, R.sub.3 is Het.sub.2, which is Het.sub.1 bonded via a ring carbon or ring nitrogen atom, or, on the other hand, R.sub.3 is hydrogen, or amino that is unsubsituted or mono- or di-substituted by identical or different substituents selected from alkyl, cycloalkyl, Ar-alkyl, Ar-O-alkyl, Ar-S-alkyl and Het.sub.
Type:
Grant
Filed:
June 29, 1990
Date of Patent:
July 28, 1992
Assignee:
Ciba-Geigy Corporation
Inventors:
Pier G. Ferrini, Carlo Voellmy, Peter H. Stahl, Jonathan Green
Abstract: Unsaturated aminodicarboxylic acid derivatives of formula I ##STR1## wherein A is a divalent aliphatic hydrocarbon radical containing 2 carbon atoms and R.sub.1 and R.sub.2 are each independently of the other free or esterified carboxyl groups, and salts thereof, have a pronounced and selective antagonistic action against N-methyl-D-aspartic acid (NMDA)-sensitive excitatory amino acid receptors. These compounds are prepared, for example, by converting, in a formula of formula II ##STR2## wherein Z.sub.1 and Z.sub.2 are hydroxy or protected hydroxy and Z.sub.3 is protected amino, Z.sub.3 into amino and, if present, converting protected hydroxyl groups Z.sub.1 and/or Z.sub.2 into hydroxy and, if desired, converting a resultant compound into another compound of formula I, resolving a resultant mixture of isomers into the individual components and separating the desired preferred isomer and/or converting a resultant free compound into a salt or a resultant salt into the corresponding free compound.
Abstract: The present invention relates to improved oral forms of administration, for example syrups, having a delayed release characteristic, of carbamazepine. The delayed release of carbamazepine is achieved by the manufacture of an advantageous cubic crystal form of suitable size of dihydrate crystals contained in the form of administration.
Abstract: Compounds of formula I ##STR1## wherein A, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Y, Z and R.sub.1 to R.sub.6 have the meanings given 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:
August 29, 1990
Date of Patent:
June 2, 1992
Assignee:
Ciba-Geigy Corporation
Inventors:
Erfinders J. Stanek, Giorgio Caravatti, Jorg Frei, Hans-Georg Capraro
Abstract: Novel polypeptides, designated hirullins, have a strong antithrombic activity and can therefore be used for the therapy and prophylaxis of thromboses. Said compounds are isolated from the leech Hirudinaria manillensis or are produced by conventional peptide synthesis or by recombinant DNA techniques.
Type:
Grant
Filed:
June 8, 1989
Date of Patent:
May 19, 1992
Assignees:
Ciba-Geigy Corporation, UCP Gen-Pharma AG
Inventors:
Reinhard Maschler, Verena Steiner, Markus G. Grutter, Fritz Raschdorf
Abstract: The invention relates to novel hydrogenated 1-benzooxacycloalkylpyridinecarboxylic acid compounds of formula ##STR1## in which the variables R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, alk, X, Z, m, n and p, the dotted line and the substituents of the ring A have the meanings indicated in the specification and in the claims, and to their tautomers and/or salts. These compounds can be used as pharmaceutical active ingredients and can be prepared in a manner known per se.
Abstract: The invention relates to novel 9H-purine derivatives, especially to the novel substituted 9-benzyl-9H-purines of the general formula ##STR1## in which Ph is a phenyl radical substituted by halogen, R.sub.1 is hydrogen or a free amino group or an amino group that is substituted aliphatically, cycloaliphatically, cycloaliphatically-aliphatically and/or by acyl, and R.sub.2 is halogen, lower alkoxy, lower alkyl, a free amino group, or an amino group that is substituted aliphatically, cycloaliphatically, cycloaliphatically-aliphatically and/or by acyl, with the proviso that R.sub.2 is other than halogen when Ph is 2-fluorophenyl or 2,5- or 2,6-difluorophenyl and R.sub.1 is a radical of the formula --N(R.sub.11)(R.sub.12) (Ia) in which either R.sub.11 is hydrogen, methyl or ethyl and R.sub.12 is hydrogen, methyl, hydroxymethyl, ethyl, n-propyl, isopropyl, cyclopropyl, cyclopenthyl or cyclopropylmethyl, or R.sub.11 is hydrogen and R.sub.12 is methoxymethyl, and with the further proviso that R.sub.
Abstract: Araliphatylaminoalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is an aromatically substituted aliphatic radical, R.sub.2 is hydrogen or a monovalent aliphatic radical and alk is a divalent aliphatic radical, and their salts, exhibit a pronounced regulatory action on the calcium metabolism and can be used as medicaments for the treatment of diseases that are attributable to calcium metabolism disorders. They are prepared, for example, by reacting a compound of formula ##STR2## wherein X.sub.3 is a carboxy and R.sub.0 is a radical R.sub.2, with phosphorous acid and phosphorous trichloride and hydrolysing the primary product.
Abstract: Insulin-like growth factor I (IGF I) and pharmaceutical compositions comprising IGF I are useful in improving glomerular filtration and renal plasma flow and can be used for the treatment of patients suffering from renal diseases and for the preparation of therapeutic combinations for treatment of renal diseases.
Type:
Grant
Filed:
December 21, 1990
Date of Patent:
April 21, 1992
Assignee:
Ciba-Geigy Corporation
Inventors:
Ernst R. Froesch, Hans-Peter Guler, Christoph Schmid, Jurgen Zapf
Abstract: The invention relates to a preferably continuous process for the preparation of R- or S-2-hydroxy-4-phenylbutyric acid in very high enantiomeric purity, which comprises reducing 2-oxo-4-phenylbutyric acid with the enzyme D-lactate dehydrogenase from Staphylococcus epidermidis or with the enzyme L-lactate dehydrogenase from bovine heart, respectively, in the presence of NAD(H) and formate or ethanol and formate dehydrogenase or alcohol dehydrogenase, respectively. R-2-hydroxy-4-phenylbutyric acid is a valuable intermediate in the preparation of ACE inhibitors or their precursors.
Type:
Grant
Filed:
June 2, 1989
Date of Patent:
March 24, 1992
Assignee:
CIBA-GEIGY Corporation
Inventors:
Oreste Ghisalba, Daniel Gygax, Rente Lattmann, Hans-Peter Schar, Elke Schmidt, Gottfried Sedelmeier
Abstract: The invention relates to a novel crystalline form, containing water of crystallization, of 4-(5,6,7,8-tetrahydroimidazol[1,5-a] pyridin-5-yl)-benzonitrile hydrochloride of formula Ia ##STR1## and to a process for the preparation thereof. The novel crystalline form is distinguished by excellent storage stability.
Abstract: The invention relates to aralkyl-4H-1,2,4-triazole derivatives, especially 5-phenyl-lower alkyl-4H-1,2,4-triazole-3-carboxamides of the formula ##STR1## in which Ph represents phenyl substituted by lower alkyl, halogen and/or by trifluoromethyl, alk represents lower alkylidene, R.sub.1 is hydrogen or lower alkyl, and R.sub.2 represents carbamoyl that is unsubstituted or is substituted by lower alkyl or by lower alkanoyl, and their salts and, as the case may be, their tautomers and the salts thereof. These compounds can be used as pharmaceutical active ingredients.
Abstract: Novel trisubstituted indole compounds of formula ##STR1## wherein R is straight-chain C.sub.2 -C.sub.4 alk-1-en-1-yl, and their salts can be used as pharmaceutical active ingredients and can be manufactured in a manner known per se.
Abstract: The invention relates to an advantageous oral administration from the disodium pamidronate in capsules. These capsules are filled with double-coated granules. The inner coating is hydrophilic and elastic, and the outer coating is gastric juice-resistant and intestinal juice-soluble. The granules are distinguished by good gastric compatibility.
Abstract: The invention relates to a pharmaceutical composition for the application of baclofen, in the form of an adhesive tablet, to the mucosa in the oral cavity, which pharmaceutical composition comprisesa) a hydrophilic tablet core, the top surface of which adheres to the receptor surface of the oral mucosa and which contains the drug baclofen or a pharmaceutically acceptable salt thereof and, as excipients, a swellable vinyl polymer, a galactomannan and/or a pharmaceutically acceptable wax and/or a glyceride or completely or partially hydrogenated glyceride, and further optional excipients, and if, desired,b) a hydrophobic coating which covers the tablet core a), with the exception of the surface provided for the release of baclofen.The invention further relates to a process for the preparation of this adhesive tablet and the therepeutic use thereof as spasmolytic.
Abstract: Described is an isoelectric focusing electrophoretic process for the separation and purification of an amphoteric or neutral chemical compound from one or more electrically charged chemical compound(s). Said process is illustrated below at the example of the purification of a protein from contaminating proteins and salts. It may be carried out in an apparatus especially designed therefor, e.g. an apparatus as depicted in FIG. 1. Said apparatus and various modifications thereof are also claimed. The mixture to be separated is present within a hydraulic flow in chamber 8. Cylinders 5 and 12 contain immobilized pH-gradients or are replaced by amphoteric isoelectric pH-membranes. Each of said pH-gradients and pH-membranes has conductivity and both buffering and titrant capacity in its pH-interval.
Abstract: The invention relates to an aqueous oral pharmaceutical preparation of diclofenac which can be used for treating pain and inflammatory processes, and to the preparation of a preparation of this type.
Abstract: Compositions of zwitterionic drugs for transdermal administration and methods of administering zwitterions transdermally are disclosed. The compositions comprise a zwitterionic drug in a salt form and a solvent therefor.
Abstract: Compounds of formula I, ##STR1## wherein Tetr, R, R.sub.0, R.sub.1 and R.sub.2 are as defined in the description, have valuable pharmaceutical properties and are especially effective against tumors. They are prepared in a manner known per se.
Abstract: Compounds of formula I ##STR1## wherein X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5, X.sub.6, Y, Z and R.sub.1 -R.sub.4 are as defined in the description, have valuable pharmaceutical properties and are especially active against tumors. They are prepared in a manner known per se.
Type:
Grant
Filed:
August 16, 1990
Date of Patent:
November 12, 1991
Assignee:
Ciba-Geigy Corporation
Inventors:
Jaroslav Stanek, Giorgio Caravatti, Jorg Frei, Hans-Georg Capraro