Showing papers by "Novartis published in 1982"

Mixtures of quaternary polymeric acrylic ammonium salts, quaternary mono- or oligomeric ammonium salts and surfactants, their preparation and their use in cosmetic compositions

Abstract: 1 An aqueous composition of polymeric, quaternary ammonium salts, of monomeric to oligomeric, quaternary ammonium salts and of monionic or anionic surfactants, which composition has a pH value of 3 to 9 and contains at least (A) one ammonium salt which is soluble or micro-emulsifiable in aqueous surfactant systems and has a molecular weight distribution of 10**4 to 10**9 , the molecular weight of at least 5 per cent by weight of the polymeric salt being 10**7 to 10**9 , said salt containing recurring structural units of the formula see diagramm : EP0080976,P46,F1 and, optionally, in any order, at least one of the recurring structural units of the formulae see diagramm : EP0080976,P46,F2 see diagramm : EP0080976,P46,F3 and see diagramm : EP0080976,P46,F4 wherein A1 , A2 , A3 and A4 are each hydrogen or methyl, G1 and G2 are different from each other and are each -CN, -COOH or see diagramm : EP0080976,P46,F5 D1 and D2 are each oxygen or -NH-, E1 and E2 are each C1 -C4 alkylene which is unsubstituted or substituted by hydroxyl, R1 , R2 , R3 and R4 are each methyl or ethyl, Q is alkyl, C1 -C4 hydroxyalkyl or benzyl and Y1 (cation) is a halide, alkylsulfate or alkylphosphonate anion containing 1 to 4 carbon atoms in the alkyl moiety, (B) an ammonium salt which contains 1 to 3 quaternary nitrogen atoms and has a molecular weight of not more than 9 000, and (C) a nonionic surfactant, a surfactant having a positive and a negative charge in each molecule or an anionic surfactant which may be in zwitterion form, or mixtures thereof, with the proviso that if component (C) is an anionic surfactant, the polymeric ammonium salt used as component (A), in addition to containing structural units of the formula see diagramm : EP0080976,P46,F6 also contains structural units of the formula see diagramm : EP0080976,P47,F1 and the anionic surfactant has been at least partially reacted by ion exchange with components (A) and (B)

New devices and kits for immunological analysis

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.

Elucidation by FAB-MS of the structure of a new cardioactive peptide from Aplysia.

Abstract: The nervous system and gut of Aplysia and other gastropod molluscs contain several classes of cardioactive peptides1 In addition to their excitatory action on the heart, these peptides stimulate contractile activity in the gut1, and modulate neurally induced contractions of somatic muscles2 This report describes the purification and sequence determination by a combination of microprotein chemistry and fast atom bombardment mass spectrometry FAB–MS3,4 of one of these peptides The sequenced peptide is a member of the small class of cardioactive peptides and was termed SCPB A peptide with identical properties to SCPB has been found in several identified central neurones which innervate the gut5 Here we report the structure of SCPB as a C-terminally blocked peptide H-Met-Asn-Tyr-Leu-Ala-Phe-Pro-Arg-Met-NH2 Native and synthetic SCPB have identical actions on molluscan muscle preparations with thresholds at around 10−10 M

A Pilot Newborn Screening for Congenital Adrenal Hyperplasia in Alaska

Abstract: A pilot newborn screening program for 21-hydroxylase deficiency congenital adrenal hyperplasia (CAH) was conducted in Alaska using a 3-mm disc filter paper elution technique of capillary whole blood for 17-hydroxyprogesterone (17-OHP) by RIA. The filter paper specimens were provided via the mandated newborn screening program. The highest values of 17-OHP in a control population of 4569 consecutive normal neonates, aged 2–14 days, was 40 pg/disc, and the range of values for 20 newborns with proven CAH was 57–980 pg/disc. All Alaskan newborns with 17-OHP levels of 57 pg/disc or greater were referred for diagnostic workup, and initially, those with 17-OHP levels of 41–56 pg/disc were recalled for a second specimen. However, the range for recall was changed subsequently to the 17-OHP level greater than 51 pg/disc, since no newborns with 17-OHP level below 50 pg/disc were found to be affected in the initial screening. In a 30-month period, the Alaskan newborns screened on the third day of life consisted of a t...

Strong, silicone containing polymers with high oxygen permeability

Abstract: Clear, strong, crosslinked polymers are described, which are obtained by copolymerization of (A) 8-70% of a linear or branched polysiloxane of 400-100,000 molecular weight (MW) containing at least two terminal or pendant, polymerizable, vinyl groups per each 5000 MW unit of polysiloxane and which are attached to the polysiloxane through at least two urethane, thiourethane, urea or amide linkages and (B) 30-92% of a mono- or divinyl compound or a mixture of such monomers consisting of 85 to 100% of water insoluble monomers. These polymers are useful in the preparation of hard or soft contact lenses.

3-Amino-[1]-benzazepin-2-one-1-alkanoic acids

Abstract: Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzazepin-2-ones and functional derivatives are angiotension converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.

Human pharmacological studies of a new transdermal system containing nitroglycerin

Abstract: A new transdermal therapeutic system (TTS) for the administration of nitroglycerin (NTG) was tested in human pharmacological studies in 26 healthy volunteers. Plasma concentrations and haemodynamic responses were determined after the application of the system in different dosages. The concentrations of NTG reached in the plasma were uniform and dose-related, i.e. dependent on the drug-release area, and showed only minor inter-individual variation. They remained almost constant as long as the system was in contact with the skin. Renewal of the system caused no appreciable change in the plasma concentration. The haemodynamic effects, like those of all nitrates, were not clearly related to the dose administered, and were not always dependent on the plasma concentration. Upon repeated application, NTG-TTS was well tolerated locally and systemically and led to no alteration in blood chemistry or haematological parameters. The typical nitrate headaches disappeared after a few days. The presence of the system on the skin caused no discomfort or inconvenience.

Correlations between different measures of antiserotonin activity of drugs. Study with neuroleptics and serotonin receptor blockers.

Abstract: The antiserotonin properties of a series of neuroleptics, 5-HT-receptor blockers and some adrenoceptor antagonists were investigated in several in vivo test systems (l-5-HTP syndrome and 5-HT-paw edema in the rat) and in an in vitro test (isolated rat uterus preparation). The results were compared to the results obtained with these drugs in an in vivo 3H-spiperone binding assay in the rat. The computations of the relative ED50 (or IC50) values obtained in different test procedures showed that the ability of drugs to bind to 5-HT receptors labelled by 3H-spiperone in the rat frontal cortex correlates fairly well with their potencies to inhibit the l-5-HTP syndrome or 5-HT-induced rat pawedema (Spearman rank correlation coefficient, r=0.80 and 0.79 respectively, n=22). In an in vitro test (rat uterus) the estimated 5-HT-receptor blocking potency of the tested drugs did not, however, correlate with any of the in vivo measures used for this purpose. The results suggest, therefore, that for the determination of central antiserotonin effects of drugs in the rat, functional in vivo tests (l-5-HTP syndrome or 5-HT-induced rat paw-edema) could yield about the same information as the specific, in vivo 3H-spiperone binding assay. The 5-HT-receptor type mediating the behavioral responses to l-5-HTP is tentatively defined as a 5-HT2 receptor.

Reactive dyestuffs, their preparation and their use

Abstract: Reactive dyestuffs with 4-fluoro-6-N-beta-haloethyl- or vinyl-sulphonylalkyl-amino-1,3,5- triazin-2-ylamino substit(s). of formula (I) are new, (in which D is the radical of an organic dyestuff of the mono- or poly-azo, metal complex azo or stilbene series. R is H or (substd.) 1-4C alkyl. A is 2-6C alkylene. Z is beta-haloethyl or vinyl. B is H or a (substd.) hydrocarbyl gp.). In (I), B is H or 1-4C alkyl. A is -C2H4-. R is H, Me or Et. D is derived from a mono- or dis-azo dyestuff or a metal (1:1 Cu) complex azo dyestuff of the benzene or naphthalene series. (I) are prepd. by condensing an organic dyestuff of the formula D-NHR or its precursor with at least one equiv. of 2,4,6-trifluoro-1,3,5-triazine (II); condensing the prod. with at least one equiv. of an amine of the formula BHN-A-SO2-Z; and converting the precursor to the final dyestuff if necessary. (I) are specified for dyeing and printing, esp. of cellulose fibres. They are also useful with natural and synthetic polyamides and polyurethanes. They have high reactivity and good fixing properties, good wet- and light-fastness, high strength of colour and high fibre-dyestuff bond stability under acid and alkaline conditions.

The Use of Inhibitors of GABA-Transaminase for the Determination of GABA Turnover in Mouse Brain Regions: An Evaluation of Aminooxyacetic Acid and Gabaculine

Abstract: The accumulation of γ-aminobutyric acid (GABA) after inhibition of GABA-T (4-aminobutyrate: 2-oxoglutamate aminotransferase, EC 2.6.1.19) by various doses of aminooxyacetic acid (AOAA) and gabaculine was studied in four different regions of the mouse brain. The dose-response curve for GABA accumulation after treatment with AOAA was linear up to 10 mg/kg i.p., and then leveled off. The increase in GABA accumulation after gabaculine treatment was linear up to 100 mg/kg i.p. No further increase was observed with doses up to 300 mg/kg i.p. The selectivity of both GABA-T inhibitors was assessed by measuring their effects on the content of free amino acids in mouse brain. Apart from the substantial increase in the GABA concentration, there were significant decreases in the content of glutamic acid, aspartic acid, alanine and glutamine, and an increase in ornithine content after administration of gabaculine. The same changes in amino acid content were observed after treatment with AOAA, but the level of lysine was also increased and the change in alanine level was biphasic. All these changes, however, were very small compared with the large increase in GABA level. A method for estimating the rate of the GABA turnover in vivo by measuring the initial rate of GABA accumulation after administration of AOAA or gabaculine is proposed, and the validity of the two techniques is discussed. The effect of diazepam on GABA levels and on the gabaculine-induced accumulation of GABA was studied. The results obtained with diazepam show that this method can provide valuable insight into the effects of drugs on GABAergic mechanisms in vivo.

Process for dyeing high-molecular organic material, and novel polycyclic pigments

Abstract: A process for dyeing high-molecular organic material in the bulk characterized by the use of a 1,4-diketo-pyrrolo[3,4-c]-pyrrole of the formula ##STR1## wherein R 1 and R 2 are isocyclic or heterocyclic aromatic radicals, preferably unsubstituted or substituted phenyl or naphthyl radicals. The dyeings obtained, for example in plastics, fibres, lacquers and printings, are distinguished by very high coloring strength, high saturation, good dispersibility, good fastness to cross-lacquering, migration, heat, light and weather, and also by a high gloss and a good IR-remission behavior.

Interaction between oxprenolol and indomethacin on blood pressure in essential hypertensive patients

Abstract: A double-blind, cross-over study in 16 patients with essential hypertension was carried out, to evaluate any possible interference by indomethacin, a known prostaglandin-synthetase inhibitor, with the antihypertensive effect of oxprenolol, a non-selective beta-adrenoceptor blocking agent. Both indomethacin and oxprenolol, as well as the two drugs combined, inhibited plasma renin activity; no change was found in urinary sodium excretion or body weight. Oxprenolol alone caused a highly significant decrease in the systolic (−10.4 mmHg,p<0.001), diastolic (−7.4 mmHg,p<0.001) and mean (−7.7 mmHg,p<0.01) blood pressures, whereas indomethacin did not influence blood pressure. When the two drugs were given in combination, blood pressure decreased (systolic: −5.9 mmHg; diastolic: −4.0 mmHg; mean: −4.6 mmHg), but the changes induced in blood pressure were reduced by about 50% when compared with those in the oxprenolol alone period. The data show that indomethacin seems to interfere with the antihypertensive effect of oxprenolol, by an action which may be due to the inhibition of prostaglandin synthesis.

Tinted contact lenses and a method for their preparation with reactive dyes

Abstract: Contact lenses comprising polymeric lens materials in which reactive dyestuffs have been covalently bonded to monomer units of the polymer backbone, said reactive dyestuffs being reactive dyes capable of forming ether linkages with cellulose and reactive with hydroxyl, amino, amido or mercapto groups present in a hydrogel polymer to form the covalent bond therewith. The invention is of particular interest in the area of so-called hydrophilic or "soft" contact lenses, commonly referred to as hydrogel lenses.

CSF monoamine metabolites in schizophrenic patients.

Abstract: The monoamine metabolites 3-methoxy-4-hydroxyphenylglycol (MHPG), homovanillic acid (HVA) and 5-hydroxyindoleacetic acid (5-HIAA) were measured in the cerebrospinal fluid (CSF) of 16 psychiatrically healthy controls and in 28 schizophrenic patients. There was no difference in CSF MHPG and HVA levels between the group of patients and the controls. CSF levels of 5-HIAA were significantly lower in schizophrenic patients than in controls. Differential analysis of patients with and without neuroleptics revealed that these findings were not due to drug treatment. Positive correlations were found between the level of 5-HIAA and the items: hallucinatory behaviour, grandiosity, and tension as rated on the Brief Psychiatric Rating Scale. As 5-HIAA CSF data are controversial for nosological entities, the search for correlations between 5-HIAA and individual psychopathological variables could provide more specific indices for psychiatric diagnosis, treatment or prophylaxis.

Stable composition for treating textile substrates

Abstract: The invention relates to a stable composition for treating textile substrates which contains at least (a) an organic solvent which is sparingly soluble to insoluble in water and in which component (b) is dissolved and component (c) is dissolved or dispersed, (b) a vehicle for component (c) which is sparingly soluble to insoluble in water, and (c) a finishing agent which is sparingly soluble to insolube in water and which is soluble or dispersible in the vehicle (b). In addition to components (a), (b) and (c), the composition of the invention may also contain (d) a solid carboxylic acid which is sparingly soluble in water, and preferably soluble in the solvent (a), and/or (e) a polar organic solvent as well as further additives or assistants. The novel composition, which preferably contains fluorescent whitening agents as finishing agents, is used in particular for whitening manmade textiles, especially made-up goods such as curtains or underwear.

The Reaction of 3-Formylchromone with ortho-Substituted Anilines. Preparation of a Tetraaza [14]annulene

Abstract: The reactions of 3-formylchromone (1) with 1, 2-phenylenediamine, 2-amino-diphenylamine and 2-aminophenol were reinvestigated and shown to yield 1, 8-dihydro-6, 13-di (2-hydroxybenzoyl)-dibenzo [b, i]-l, 4, 8, 11-tetraazacyclotetradeca- 4, 6, 11,13-tetraene (7), 3-[2-(1-phenyl)benzimidazolyl]chromone (10b) and 3-(2-hydroxyphenyl)iminomethylchromone (4), respectively at variance with earlier reports. Compound 4 reacts with ethanol to give 2-ethoxy-3-[(2-hydroxyphenyl)-aminomethylidene]chroman-4-one (5b). Dehydrogenation of 7 produces 3-(2-benz-imidazolyl)chromone (10a), also at variance with earlier reports. The structures have been elucidated with the aid of NMR. and mass spectra. The reaction mechanism is discussed.

Photopolymerization process employing compounds containing acryloyl groups and maleimide groups

Abstract: In a three stage process, a layer of a liquid composition containing a compound (A) having in the same molecule at least one (meth)acryloyl group and at least one 2,3-disubstituted maleimido group is exposed to actinic radiation so that the layer solidifies due to photopolymerization of (A) through the (meth)acryloyl group(s), remaining, however, further photocrosslinkable. When desired, the solidified layer is exposed, as through a negative, to a substantially greater amount of actinic radiation, the parts so further exposed becoming more highly photocrosslinked through the disubstituted maleimido group(s) and hence insoluble. An image is produced which can be developed by means of suitable solvents. Examples of (A) include N-(2-(acryloyloxy)ethyl)-2,3-dimethylmaleimide and N-(3-(methacryloyloxy)-2-hydroxypropyl)-2,3-dimethylmaleimide.

Effects of low concentrations of antibiotics on Escherichia coli adhesion.

Abstract: Bacterial adhesion to eukaryotic cells is thought to represent an important factor in the pathogenesis of certain infectious diseases [6]. Agents interfering with the process of bacterial adhesion may therefore have beneficial prophylactic or therapeutic effects. Recent evidence indicates that certain antibiotics affect bacterial adhesion at low concentrations that do not significantly influence bacterial growth [3, 7, 9]. We have employed a tissue-culture model system [2, 9, 11] to investigate subinhibitory effects of antibiotics on bacterial adhesion. Since the biological relevance of tissue-culture assays may be criticized, we have compared the effects of low antibiotic concentrations in our adhesion model system with those seen in other systems. The present report demonstrates that some antibiotics change the adhesiveness of Escherichia coli strains in a number of different assays in a strain-specific manner. Although there was no absolute correlation between the different assay systems, one can generalize these effects to a large extent, and they correlate with the observations of other authors [3, 6].

Process for the curing of stoving lacquers

Abstract: Quinolinium sulfonates of the formula I ##STR1## wherein R1 is C1 -C8 -alkyl, C1 -C4 -alkyl substituted by halogen, hydroxyl or C1 -C4 -alkoxy, or it is C2 -C8 -alkenyl, C7 -C9 -phenylalkyl or C5 -C8 -cycloalkyl, R2, R3, R4 and R5 independently of one another are each hydrogen, C1 -C4 -alkyl, halogen, --CN, --COO(C1 -C4 -alkyl), --CHO, hydroxyl, C1 -C4 -alkoxy, an acyloxy group R7 COO--, a group R8 --CH═CH--, C7 -C9 -phenylalkyl or phenyl, R6 is C1 -C12 -alkyl, C6 -C10 -aryl which is unsubstituted or mono- or polysubstituted by C1 -C12 -alkyl, C1 -C4 -alkoxy, halogen or a group R7 CONH--, or it is fluorine, NH2 or CF3, and R7 and R8 independently of one another are each C1 -C4 -alkyl or phenyl, are suitable as latent curing catalysts for acid-curable stoving lacquers. There is formed by irradiation with UV light the actual acid catalyst, which renders possible curing at relatively low stoving temperatures.

Inactivation of a diol epoxide by dihydrodiol dehydrogenase but not by two epoxide hydrolases

Abstract: The mutagenicity of r-8,t-9-dihydroxy-t-10, 11-oxy-8,9,10,11-tetrahydrobenz[a]anthracene (BA-8,9-diol 10, 11-oxide) toward Salmonella typhimurium TA 100 is not decreased by the presence of large amounts of highly purified microsomal or cytosolic epoxide hydrolase. However, highly purified dihydrodiol dehydrogenase inactivates this diol epoxide, which is a major DNA-binding metabolite of benz[a]anthracene. The K-region epoxide, benz[a]anthracene 5,6-oxide (BA 5,6-oxide) is efficiently inactivated by microsomal epoxide hydrolase, is much less readily inactivated by cytosolic epoxide hydrolase, and is not inactivated by dihydrodiol dehydrogenase. This inactivation of a diol epoxide by dihydrodiol dehydrogenase points to a new significance of this enzyme and a new level of control for diol epoxides.