Novartis Ag

Ciba-geigy Corporation

Isis Pharmaceuticals, Inc.

Bayer Corporation

Ciba-geigy Ag

Novartis Corporation

Adrian Waldner

Steven Mark Barnard

Joseph Berger

David Reinhoudt

Willy Meyer

Marcus Baumann

Marizel Rouilly

Alain De Mesmaeker

Jacques Lebreton

Ren&eacute; Beerli

Phillip Dan Cook

Daniel Bellus

Say-Jong Law

Anand Natrajan

Qingping Jiang

David J Sharpe

Rolf Hilfiker

Alex Alder

Achim Roloff

Dirk Beckelmann

Jun Xi

Paul Senn

Fritz Thommen

Catherine Lesueur

Marc-Olivier Bevierre

Erika Schmidt

Fluoroionophores and their use in optical ion sensors

Fluoroionophores that are functionalised with reactive groups and correspond to the formula I&mdash;R &mdash;F&mdash;R &mdash;G, wherein I is a monovalen residue of an ionophore, wherein F is a divalent residue of a fluorophore, wherein G is a functional group and R and R are each independently of the other a direct bond or a bridging group. The fluoroionophores may be covalently bound to carrier materials and are used as active components in polymer membranes of optical sensors for the detection of ions. The sensors are distinguished by a long usable life and a high degree of sensitivity.

Covalently immobilized fluoroionophores as optical ion sensors

A sensor for the optical determination by fluorescence of carbon dioxide in liquid and gaseous media, which consist essentially of a carrier and a light-sensitive layer applied thereto. In addition to a polymer as a base substance and an anionic fluorescence dye, the light-sensitive layer also contains a quaternary onium phenolate.

Optical carbon dioxide sensors

A water-insoluble copolymer which is composed of (a) from 39.9 to 60% by weight of N,N-dimethylacrylamide or N,N-dimethylmethacrylamide; (b) from 60 to 39.9% by weight of N-alkylated acryl amides or N-alkylated methacryl amides; (c) from 0.1 to 0.7% by weight of a proton-sensitive fluorophore which is covalently bonded to the copolymer; and (d) from 0 to 20% by weight of a diolefinic crosslinking component. The copolymer is used in the form of a membrane on a transparent support material as an optical sensor for ionic strength-independent pH value determination.

Fluorescent N-alkylated acrylamide copolymers and optical pH sensors

Compounds, constructed in modular manner, of formula (I),

Covalently immobilized fluoroionophores for optical ion sensors

Sensors for the qualitative and quantitative determination of K,ions in aqueous systems are described, which consist essentially of a carrier and an active layer applied to this carrier, whereby the active layer contains a polymer in which is dispersed at least one modified valinomycin, in which a radical of a fluorescence dye which emits in long waves, preferably an acridine or fluorescein, with an emission wave length of >550, is covalently bound.

Sensors

Compounds of formula (I) wherein Me is Pd(II) or Pt(II); R is H or C,-C,alkyl, or is C,-C,cycloalkyl, phenyl, pyridyl or phenyl-C,-C,alkylene, each of which is unsubstituted or substituted by C,-C,alkyl, C,-C,alkoxy, R,&mdash;O&mdash;C(O)&mdash;, halogen, &mdash;CN or by &mdash;NO,; R,and R,are each independently of the other H, C,-C,alkyl or C,-C,alkoxy or R,and R,together are &mdash;OCH,O&mdash;, &mdash;OCH,CH,O&mdash;, or &mdash;CH&boxH;CH&mdash;CH&boxH;CH&mdash;, and R,is C,-C,alkyl, C,-C,cycloalkyl, phenyl, benzyl, C,-C,alkylphenyl or C,-C,alkylbenzyl. Compounds of formula (I) are valuable luminophores and/or intermediates for the preparation of palladium (II) or platinum (II) benzoporphyrins, which are likewise luminophores.

Process for the preparation of platinum or palladium benzoporphyrins and platinum or palladium cyclohexenoporphyrins, intermediates, and an oxygen sensor comprising platinum or palladium cyclohexenoporphyrin

A new class of chemiluminescent acridinium or benzacridinium compounds is disclosed by virtue of forming an intramolecular energy transfer conjugate (ETC) between the acridinium or benzacridinium compound and a luminophore. A method of extending the emission wavelengths of acridinium or benzacridinium esters in order to further reduce or eliminate the emission spectral overlap between the parent polysubstituted aryl Acridinium Esters (DMAE) and Benzacridinium Esters (LEAE) is disclosed. The ETC's retain the unique desired properties of acridinium or benzacridinium compounds including complete light emission in very short period of time, monophasic emission spectrum, simplicity of triggering mechanism, ability of labeling the biological molecules of interest to form a tracer, and good stability. Additionally, the range of the emission spectrum of an acridinium or benzacridinium compound can now be shifted at will and at longer leap through the choice of a luminophore as the integral part of an ETC molecule. Disclosed are chemiluminescent labeled conjugates comprising an acridinium or benzacridinium moiety covalently attached to a luminophore via a spacer, said moiety further conjugated to a biological molecule of interest, wherein said spacer is of an appropriate length to allow the excited species generated from said moiety to transfer energy efficiently to said luminophore, resulting in the emission of light in the spectral region of said luminophore. Also disclosed are binding assays using said conjugates, test kits comprising said conjugates and methods of preparing the conjugates.

Chemiluminescent energy transfer conjugates and their uses as labels in

Modified oligonucleotides

Backbone modified oligonucleotide analogs

Compounds of formula I ##STR1## in which R is H, or an aliphatic or aromatic radical, R.sup.1 is alkyl, R.sup.2 is alkyl, alkoxy, aryl, aryloxy, aralkyl, alkaryl, aralkyloxy, alkaryloxy, alkaralkyl or alkaralkyloxy, and one of R.sup.1 and R.sup.2 is H and the other has the meaning given above. These compounds are intermediates for the preparation of herbicidal sulfonylureas.

Preparation of 4-azasaccharines

The process of the invention relates to the reaction of hydrazones of formula II ##STR1## with .alpha.-chloro- or .alpha.-bromoarylonitrile or .alpha.-chloro- or .alpha.-bromoacrylates of formula III ##STR2## to 1-amino-2-cyano-1,4-dihydropyridines or 1-amino-1,4-dihydropyridine-2-carboxylic acid esters of formula IV ##STR3## which are converted into pyridine derivatives of formula I ##STR4## by treatment with an acid, with removal of R.sub.4 R.sub.5 NH. Y is --CN or --COOR.sub.3 and R.sub.1 to R.sub.5 may be alkyl.

Process for the preparation of 2-pyridinecarboxylic acid derivatives and

4-azasaccharines, 4-aza-dihydro- or -tetrahydro-saccharines

A process for producing pyridine-2,3-dicarboxylic acid derivatives of the formula ##STR1## is described. The process is based on the cleavage of HNR.sub.10 R.sub.11 from 1-amino-1,2,3,4-tetrahydropyridine-2,3-dicarboxylic acid derivatives of the formula II ##STR2## to give 1,4-dihydropyridine-2,3-dicarboxylic acid derivatives of the formula III ##STR3## and subsequent oxidation of these compounds to obtain pyridine-2,3-dicarboxylic acid derivatives of the formula I. According to one variant of the process, the 1,4-dihydropyridine-2,3-dicarboxylic acid derivatives of the formula III are obtained directly, without isolation of the intermediately formed 1-amino-1,2,3,4-tetrahydropyridine-2,3-dicarboxylic acid derivatives of the formula II, by reaction of .alpha.,.beta.-unsaturated hydrazones of the formula IV ##STR4## with ethene-1,2-dicarboxylic acid derivatives of the formula V ##STR5## and subsequently oxidized to pyridine-2,3-dicarboxylic acid derivatives of the formula I. In the above formulae, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.10 and R.sub.11 have the meanings defined in claim 1. The pyridine-2,3-dicarboxylic acid derivatives of the formula I are intermediates for producing herbicidal active substances.

Process for producing pyridine-2,3-dicarboxylic acid derivatives; and

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Allschwil, Switzerland

Adrian Waldner