Abstract: An orally administrable pharmaceutical composition comprising a solution or dispersion of a staurosporine active ingredient in a solid saturated polyalkylene glycol glyceride, such as a mixture of esters of C.sub.8 -C.sub.18 saturated fatty acids with glycerol and polyethylene glycol, is disclosed that may be administered in capsules or as a dispersion in an aqueous medium.
Type:
Grant
Filed:
November 22, 1994
Date of Patent:
April 7, 1998
Assignee:
Novartis Corporation
Inventors:
Roy Lindsay Allen Henry, Graham Paul Matthews
Abstract: Flowable herbicidal compositions which contain an active component combination of at least one triazine and at least one chloroacetanilide with a surfactant component. This surfactant component, which consists of an anionic compound based on a monosulfuric acid ester of alkyl or alkyphenol polyglycol ethers as well as at least one nonionic alkyl or alkylphenol polyglycol ether, gives stable dispersions of the concentrated composition and forms stable dispersions of dilutions of the compositions suitable for direct use.
Abstract: The present invention relates to a pharmaceutical composition for the intravenous administration of the sparingly soluble staurosporin derivative N-benzoyl-staurosporin. The composition comprises the following preferred components:a) the therpeutic agent N-benzoyl-staurosporin;b) a polyoxyethylene/polyoxypropylene block copolymer;c) ethanol and water as carrier liquids; andd) purified lecithin from soybeans ande) as water-soluble excipients glycerol and sorbitol.
Abstract: A topically administrable pharmaceutical composition comprising (A) zinc phthalocyanine, (B) as carrier for (A), (i) a monoalkyl ether of diethyleneglycol substantially in the absence of a N-alkylpyrrolidone, a N,N-dialkylbenzamide or dimethyl sulphoxide, or (ii) a mixture of a monoalkyl ether of diethyleneglycol with a lipid and (C) a gelling agent.
Abstract: Compounds of the formula I ##STR1## in which R.sub.1 is arylamino, N-aryl-N-(lower alkoxy-lower alkyl)-amino, N-aryl-N-aryl-lower alkyl-amino or heterocyclyl bonded via a ring carbon atom, X is a carbonyl or methylene group, R.sub.2 and R.sub.3 independently of one another are hydrogen or lower alkyl or, together with the carbon atom with which they are bonded, are a cycloalkylidene radical, R.sub.4 is hydrogen, lower alkyl, lower alkanoyl or lower alkoxycarbonyl, R.sub.5 is hydroxyl, lower alkanoyloxy or lower alkoxycarbonyloxy, R.sub.6 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cycloalkyl-lower alkyl, aryl-lower alkyl or heteroaryl-lower alkyl having 5 to 7 ring atoms in the heteroaryl ring and R.sub.7 is hydrogen or lower alkyl, or R.sub.6 and R.sub.7, together with the carbon atom with which they are bonded, are a cydoalkylidene radical and R.sub.
Type:
Grant
Filed:
September 8, 1995
Date of Patent:
February 17, 1998
Assignee:
Novartis Corporation
Inventors:
Vittorio Rasetti, Heinrich Rueger, Jurgen Klaus Maibaum, Robert Mah, Markus Grutter, Nissim Claude Cohen
Abstract: The invention relates to a novel process for stereocontrolled preparation of 1',1'-disubstituted and 1'-spiro-nucleosides of the formula I ##STR1## in which the substituents A, R.sub.8 and R.sub.9 are as defined in claim 1, and to novel intermediates and their use in this process and to processes for the preparation of the novel intermediates. The process is illustrated by the example of biologically active (+)-hydantocidin.
Abstract: A salt of 2-?(2,6-dichlorophenyl)amine!phenylacetoxyacetic acid with an organic basic cation of formula (I); Wherein R.sub.1 and R.sub.2 independently are lower alkyl, or if R.sub.1 is hydrogen H--N(R.sub.1)(R.sub.2) has the meaning of arginine or lysine or if R.sub.1 is methyl H--N(R.sub.1)(R.sub.2) has the meaning of N-methylglucamine. This compound pocesses analgesic activity as well as antiinflammatory activity, suitable in the treatment of conditions such as rheumatoid arthritis, ankylosing spondylitis, lumbar pains, luxations and ocular inflammation. The compound further has an improved stability in aqueous solutions in comparison to the alkali metal salts, e.g. sodium and potassium.
Abstract: The invention relates to a novel advantageous process for the preparation of an oral solid dosage form containing diclofenac or a pharmaceutically acceptable salt thereof. The dosage form is obtainable by direct compression of an inclusion compound consisting of diclofenac, or a salt thereof, with .gamma.-cyclodextrin. The inclusion compound itself is novel and is likewise an object of the invention.
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: Described are 3-hydroxypyridin-4-ones of formula I ##STR1## wherein R.sub.1 -R.sub.4, A and B are as defined in the description. The compounds have valuable pharmaceutical properties and are especially effective as chelators of iron. They can be used to treat excess iron in the bodies of warm-blooded animals.
Abstract: Novel compounds of the formula I ##STR1## in which R.sup.1 and R.sup.2 are hydrogen, C.sub.1 -C.sub.4 alkyl or are linked to form C.sub.3 -C.sub.7 cycloalkyl and R.sup.3, R.sup.4 and R.sup.5 are the same or different and are hydrogen, C.sub.1 -C.sub.4 alkyl, hydroxy, OR.sup.6, SR.sup.6, halogen, NR.sup.7 R.sup.8, NO.sub.2, CN, CONR.sup.7 R.sup.8 or CO.sub.2 R.sup.9 wherein R.sup.6 is C.sub.1 -C.sub.4 alkyl or C.sub.7 -C.sub.10 aralkyl and R.sup.7, R.sup.8 and R.sup.9 are the same or different and are hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.7 -C.sub.10 aralkyl or R.sup.7 and R.sup.8 together with the nitrogen atom to which they are bound form 5 or 6 membered azacycloalkyl or oxazacycloalkyl; Arg is arginine ?NH--CH(CH.sub.2 CH.sub.2 CH.sub.2 NH--C(.dbd.NH)--NH.sub.2)--CO!; X is methine CH or nitrogen; n is an integer from 0 to 7; L is a peptide linker, and H is the carboxy terminal end of hirudin, and salts thereof, are provided.
Type:
Grant
Filed:
October 20, 1994
Date of Patent:
November 11, 1997
Assignee:
Novartis Corporation
Inventors:
Derek Edward Brundish, Hans Rink, Markus Grutter, John Peter Priestle, Albert Schmitz
Abstract: Phthalocyanine-chelate complexes of formula I ##STR1## are described which contain as central atom M aluminium, gallium, indium, tin, ruthenium or preferably germanium and in which the remaining symbols are as defined in claim 1. The complexes can be used inter alia in the photodynamic chemotherapy of tumours.
Abstract: The invention relates to substituted 3-amino-1-arylalkyl-benzazepin-2-ones of the general formula ##STR1## wherein the substituents are defined in the specification; or salts thereof; to processes for the preparation thereof; and to the use thereof as well as to pharmaceutical compositions that comprise compounds of formula (I) or pharmaceutically acceptable salts thereof.
Abstract: A drug delivery device for delivering a drug either intermittently or to a pre-selected region of the gastro-intestinal tract, particularly to the colon, consists of an a solid core comprising an active agent coated with a delay jacket, then coated with a semi-permeable membrane which is optionally drilled to provide a release orifice, and then optionally further coated with an enteric material. The device delivers substantially all of the active agent to the targeted site.
Type:
Grant
Filed:
March 22, 1996
Date of Patent:
October 28, 1997
Assignee:
Ciba-Geigy Corporation
Inventors:
Louis Savastano, James Carr, Elizabeth Quadros, Shailesh Shah, Satish Chaudra Khanna
Abstract: Compounds of the formula ##STR1## in which R.sub.l, R.sub.2, R.sub.3, R.sub.4, Y and Z are as defined in claim 1, and, if appropriate, the tautomers thereof, in each case in free form or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.
Abstract: Aqueous emulsions are described comprising an organic phase of a substantially hydrophobic pesticide or mixture of pesticides which are liquid or dissolved in a hydrophobic solvent, and an aqueous phase comprising surfactants and/or dispersants, whereina) the emulsion is in the form of an aqueous concentrate, andb) an emulsion-stabilizing amount of a polymer or polymer mixture is present which is more soluble in the organic phase than in the aqueous phase.
Abstract: The present invention concerns a novel DNA sequence coding for an Aspergillus aspartic protease, an Aspergillus aspartic protease per se and a method for the preparation thereof. The invention further concerns a novel Aspergillus mutant strain defective in a protease of the aspartic proteinase-type, which is useful for the expression of heterologous protein, and a method for the preparation of such a mutant strain.
Type:
Grant
Filed:
October 24, 1994
Date of Patent:
October 7, 1997
Assignee:
Novartis Corporation
Inventors:
Frank Buxton, Gabor Jarai, Jacob Visser
Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating vital infection.
Type:
Grant
Filed:
January 11, 1996
Date of Patent:
September 23, 1997
Assignee:
Ciba-Geigy Corporation
Inventors:
Guido Bold, Shripad S. Bhagwat, Alexander Fassler, Marc Lang
Abstract: Phthalocyanine chelate complexes of formula I ##STR1## are described which contain as central atom M aluminum; gallium, indium, tin, ruthenium or preferably germanium and in which the remaining symbols are as defined in claim 1. The complexes can be used inter alia in the photodynamic chemotherapy of tumors.
Abstract: A process for the synthesis of 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.