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Showing papers by "Novartis published in 1983"


Patent
Helmut Hauser1
11 Feb 1983
TL;DR: In this paper, a new method for producing unilamellar liposomes in the aqueous phase by transferring a suitable lipid component, e.g. Phosphatidic acid, in the ionic form, by subjecting the lipid dispersion to a change in pH and then neutralizing it.
Abstract: The present invention relates to a new, advantageous method for producing unilamellar liposomes in the aqueous phase by transferring a suitable lipid component, e.g. Phosphatidic acid, in the ionic form, by subjecting the lipid dispersion to a change in pH and then neutralizing it. The formation of the unilamellar liposomes occurs spontaneously, i.e. without additional external energy supply. The liposomes obtainable according to the method can be used therapeutically as carriers of active substances of the most varied types.

440 citations


Journal ArticleDOI
Walter Wehrli1
TL;DR: No strict correlation exists between enzyme sensitivity and MIC values, since inhibition of RNA synthesis does not always show up to the same extent in the two different test systems used for the determination of these values.
Abstract: Rifampin specifically inhibits bacterial RNA polymerase, the enzyme responsible for DNA transcription, by forming a stable drug-enzyme complex with a binding constant of 10(-9) M at 37 C. The corresponding mammalian enzymes are not affected by rifampin. Bacterial resistance to rifampin is caused by mutations leading to a change in the structure of the beta subunit of RNA polymerase. Such resistance is not an all-or-nothing phenomenon; rather, a large number of RNA polymerases with various degrees of sensitivity to rifampin have been found. No strict correlation exists between enzyme sensitivity and MIC values, since inhibition of RNA synthesis does not always show up to the same extent in the two different test systems used for the determination of these values.

345 citations


Patent
Helmut Hauser1
25 Jul 1983
TL;DR: In this article, an advantageous process for preparing unilamellar liposomes in aqueous phase by dispersing a homogeneous mixture of an ionic surfactant and of a lipid was described.
Abstract: The present invention relates to an advantageous process for preparing unilamellar liposomes in aqueous phase by dispersing a homogeneous mixture of an ionic surfactant and of a lipid. The unilamellar liposomes are formed spontaneously, i.e. without input of additional external energy. The liposomes obtained by the process can be used as carriers of a wide variety of active substances for therapy.

296 citations


Patent
Adolf Hubele1
11 Feb 1983
TL;DR: In this paper, a method of protecting cultivated plants from the harmful effects of aggressive agricultural chemicals using compounds of the formula worin Ri, R 2 and R 3 unabhangig voneinander Wasserstoff, Halogen, C 1 -C 3 -Alkyl, C 2 -, CH 2 -CH 2 - oder CH(CH 3 )- and Z Cyan oder Amidoxim, where Z is cyano or amidoxime.
Abstract: Verfahren zum Schutzen von Kulturpflanzen gegen schadigende Wirkungen von aggressiven Agrarchemikalien unter Verwendung von Verbindungen der Formel A method of protecting cultivated plants from the harmful effects of aggressive agricultural chemicals using compounds of the formula worin Ri, R 2 und R 3 unabhangig voneinander Wasserstoff, Halogen, C 1 -C 3 -Alkyl, C 1 -C 3 -Alkoxy, Nitro oder Cyan, R 4 , R 5 und R 6 unabhangig voneinander Wasserstoff, Halogen oder C 1 -C 3 -Alkyl, wherein Ri, R 2 and R 3 are independently hydrogen, halogen, C 1 -C 3 alkyl, C 1 -C 3 alkoxy, nitro or cyano, R 4, R 5 and R 6 are independently hydrogen, halogen or C 1 -C 3 alkyl, A eine der Gruppen -CH 2 -, -CH 2 -CH 2 - oder CH(CH 3 )- und Z Cyan oder Amidoxim, welches am Sauerstoffatom acyliert sein kann, bedeuten, unter Einschluss ihrer Saureadditionssalze und Metallkomplexe. A one of the groups -CH 2 -, -CH 2 -CH 2 - or CH (CH 3) - and Z is cyano or amidoxime, which can be acylated on the oxygen atom, to mean including their acid addition salts and metal complexes.

253 citations


Patent
Edward Dr. Irving1
09 Sep 1983
TL;DR: In this paper, the photoinitiator is a diaryliodosyl salt of formula V where R 9 and R 10 are the same or different and each represents a monovalent aromatic radical, x represents 1, 2, or 3, and Z x- is an anion of a protic acid.
Abstract: Photopolymerizable compositions contain a cationically polymerizable material, such as an epoxide resin, a phenoplast, or an aminoplast, and, as photoinitiator, a diaryliodosyl salt of formula ##STR1## where R 9 and R 10 are the same or different and each represents a monovalent aromatic radical, x represents 1, 2, or 3, and Z x- is an anion of a protic acid. Suitable diaryliodosyl salts of formula V include diphenyliodosyl hexafluorophosphate, hexafluoroantimonate, tetrafluoroborate, toluene-p-sulfonate, and chloride. The compositions may be used as surface coatings and adhesives, and in the preparation of reinforced composites and printed circuits.

198 citations


Journal ArticleDOI
06 Jan 1983-Nature
TL;DR: Only one of six point mutations of the sequence around one end of the larger of the introns of the rabbit β-globin gene seriously affects the normal removal of the intron and splicing of the gene.
Abstract: Only one of six point mutations of the sequence around one end of the larger of the introns of the rabbit beta-globin gene seriously affects the normal removal of the intron and splicing of the gene. That mutation converts a GT sequence, invariably found at the 5' end of introns, into an AT, which is no longer recognized as a signal for intron removal. Instead, three normally unused (cryptic) sites are used, leading to aberrant gene transcripts. One of the cryptic sites is an exception to the invariable GT sequence.

191 citations


Journal ArticleDOI
Jeffrey M. Liebman1
TL;DR: It is concluded that at least six of these methods appear to do a reasonable job of excluding gross performance deficit in ICSS, and self-regulation of current intensity constitutes a powerful tool that has yet to realize its full potential in the pharmacological study of ICSS.

176 citations


Patent
15 Dec 1983
TL;DR: In this paper, a color-photographic recording material comprising, on a support, a blue-sensitive, a green-sensitive and/or a red-sensitive silver-halide emulsion layer, a protection layer above the sensitive layers, and, if desired, separation layers between the sensitive layer, where at least one of said layers includes a UV absorber of the formula.
Abstract: The invention relates to a color-photographic recording material comprising, on a support, a blue-sensitive, a green-sensitive and/or a red-sensitive silver-halide emulsion layer, a protection layer above the sensitive layers, and, if desired, separation layers between the sensitive layers, where at least one of said layers includes a UV absorber of the formula ##STR1## The stabilizers of the formula (1) or (1a) have good inherent stability and high light absorption; the photographic recording material described has excellent stability of the magenta, cyan and yellow layers.

163 citations


Journal ArticleDOI
Jui-Yoa Chang1
TL;DR: It is concluded that this acidic C‐terminal segment of hirUDin is essential for hirudin—thrombin interaction and its implication for the enzymatic specificity of thrombin is discussed.

161 citations


Journal ArticleDOI
TL;DR: Yeast cells were transformed with plasmids containing the synthetic gene under control of a yeast glyceraldehyde-3-phosphate dehydrogenase gene promoter and were shown to synthesize a biologically active human epidermal growth factor.
Abstract: We have chemically synthesized and expressed in yeast a gene coding for human epidermal growth factor (urogastrone), a 53-amino-acid polypeptide that has been shown to promote epithelial cell proliferation and to inhibit gastric acid secretion. The synthetic gene, consisting of 170 base pairs, was designed with yeast-preferred codons and assembled by enzymatic ligation of synthetic fragments produced by phosphoramidite chemistry. The DNA synthesis protocol used allows for facile synthesis of oligonucleotides larger than 50 bases. Yeast cells were transformed with plasmids containing the synthetic gene under control of a yeast glyceraldehyde-3-phosphate dehydrogenase gene promoter and were shown to synthesize a biologically active human epidermal growth factor.

161 citations


Journal ArticleDOI
TL;DR: A global scoring system has been devised to permit statistical comparisons of lesion incidence and severity in different groups of rabbits to test drug efficacy in the rabbit lateral meniscectomy model of osteoarthritis.
Abstract: A partial lateral meniscectomy procedure has been developed for the induction of a predictable and reproducible degenerative joint disease in knees of rabbits. The procedure adopted involves section of the fibular collateral and sesamoid ligaments and removal of 4-5 mm of the anterior lateral meniscus. In most experiments the animals are killed and tissues obtained for histologic examination at 6 weeks. Section of the ligaments alone (with or without penetration of the joint space) did not result in significant pathologic change. Significant degeneration was observed in tibial and femoral cartilage when the meniscus as well as the ligaments were cut, but the most extensive lesions were seen when a piece of the anterolateral meniscus was actually removed. These lesions included fibrillation, ulceration and erosion, "clone" and osteophyte formation, loss of chondrocytes, and loss of safraninophilic staining in the articular cartilage. The incidence and distribution of lesions with time following surgery were also investigated. Lesions were observed as early as 1-2 weeks post-surgery and increased in number and severity up to 12 weeks. A global scoring system has been devised to permit statistical comparisons of lesion incidence and severity in different groups of rabbits. This scoring system has enabled us to test drug efficacy in the rabbit lateral meniscectomy model of osteoarthritis.

Journal ArticleDOI
David J. Dooley1, Helmut Bittiger1, Kathleen Hauser1, Serge Bischoff1, P.C. Waldmeier1 
TL;DR: The alteration of alpha 2- and beta-receptors, as a consequence of DSP-4 treatment, may form the basis of a new animal model of adrenergic receptor supersensitivity, and has clear advantages over other methods of depleting central norepinephrine.

Patent
11 May 1983
TL;DR: In this article, a process for preparing 1,4Diketo-pyrrolo [3,4c] pyrroles of the formula worin R 1 and R 2 isocyclische or heterocyclic aromatic radicals is described.
Abstract: Verfahren zur Herstellung von 1,4Diketo-pyrrolo-[3,4-c]-pyrrolen der Formel A process for preparing 1,4Diketo-pyrrolo [3,4-c] pyrroles of the formula worin R 1 und R 2 isocyclische oder heterocyclische aromatische Reste bedeuten, dadurch gekennzeichnet, dass man 1 Mol eines Bernsteinsaurediesters mit 2 Mol eines Nitrils der Formel wherein R 1 and R 2 are isocyclic or heterocyclic aromatic radicals, characterized in that 1 mol of a succinic diester with 2 mol of a nitrile of formula worin R, und R 2 die oben angegebene Bedeutung haben, oder mit 1 Mol eines Nitrils der Formel 11 und 1 Mol eines Nitrils der Formel III in einem organischen Losungsmittel in Gegenwart einer starken Base bei erhohter Temperatur umsetzt und aus dem entstandenen Reaktionsprodukt durch Hydrolyse die Verbindung der Formel 1 freisetzt. wherein R, and R 2 have the abovementioned meaning, or with 1 mole of a nitrile of the formula reacting 11 and 1 mole of a nitrile of formula III in an organic solvent in the presence of a strong base at elevated temperature, and from the resulting reaction product by hydrolysis releasing compound F1. Die Pyrrolo-[3,4-c]-pyrrole eignen sich zum Pigmentieren von hochmolekularem organischem Material. The pyrrolo [3,4-c] pyrroles suitable for pigmenting high molecular weight organic material.

Journal ArticleDOI
S. Bonelli, F. Conoscente, P.G. Movilia, L. Restelli, B. Francucci1, Enzo Grossi1 
01 Jul 1983-Pain
TL;DR: The results of this study show that regional sympathetic block with guanethidine is a good therapeutic tool in the treatment of reflex dystrophies, especially on account of its negligible risks and contraindications.
Abstract: Regional intravenous guanethidine blocks and stellate ganglion blocks have been compared in a randomized trial Nineteen patients, randomly allocated to two groups of therapy and exhibiting severe reflex sympathetic dystrophy following peripheral nerve lesions, have been treated The performance of the intravenous guanethidine block is of longer duration and superior to stellate ganglion block, as regards some early pharmacological effects (skin temperatures and amplitude of plethysmographic waves recorded before blockade and 15 min, 60 min, 24 h, 48 h after institution of the block) In fact the intravenous guanethidine group shows a persistent and significant increase of the skin temperature and of the plethysmographic traces in the blocked side 24 h and 48 h after blockade in comparison with the patients treated with stellate ganglion block Concerning the therapeutic effects (changes in pain scores and clinical signs — hyperpathia, allodynia, vasomotor disturbances, trophic changes, oedema and limited motion), recorded at the end of treatment and 1 month and 3 months follow-up, an intravenous guanethidine block carried out every 4 days up to a total of 4 blocks is comparable with a stellate ganglion block every day up to a total of 8 blocks The results of this study show that regional sympathetic block with guanethidine is a good therapeutic tool in the treatment of reflex dystrophies, especially on account of its negligible risks and contraindications

Patent
Willy Meyer1, Werner Dr. Föry1
19 Jan 1983
TL;DR: In this paper, the N-phenylsulphonyl-N'-diazinyl- and triazinyl-urea derivates are presented and their salts are new.
Abstract: N-phenylsulphonyl-N'-diazinyl- and triazinyl-urea derivs. and their salts are new. A is 1-6C alkyl or 2-6C alkenyl, both opt. substd. by 1-4C alkoxy, 1-4C alkylthio, 1-4C alkylsulphinyl, 1-4C alkylsulphonyl 1-4C haloalkoxy, 1-4C haloalkylthio, 1-4C haloalkylsulphinyl or 1-4C haloalkylsulphonyl or A is 2-6C haloalkenyl. E is methine or N; X is O, S, sulphinyl or sulphonyl; Z is O or S- m is 1 or 2; R1 is H, halogen, 1-5C alkyl, 2-5C alkenyl, 1-4C haloalkyl, YR5, COOR6, NO2 or CONR7R8; R3 and R4 are each H, 1-4C alkyl, 1-4C alkoxy, 1-4C alkylthio, 1-4C haloalkyl, halogen or up to 4C alkoxyalkyl; R5 and R6 are each 1-5C alkyl, 2-5C alkenyl or 2-6C alkinyl; R7 and R8 are each H, 1-5C alkyl, 2-5C alkenyl or 2-6C alkinyl; Y is O, S, sulphinyl or sulphonyl. The intermediate phenylsulphonamide derivs. of formula (II) are also new. (a) R1, R2, A, M and X are as in (I) or (b) R1 and R2 are as in (I), but M=1, A=H and X is O or S. (I) are stable herbicides and plant growth regulators, which are easy to handle. (I) are highly selective and can be used e.g. in tropical areas to inhibit the growth of cover crops so they do not compete with the crops but without totally killing cover crops so that they still provide protection against soil erosion. (I) are esp. useful as selective herbicides in cereal, cotton, soya, maize and rice crops.

Patent
15 Aug 1983
TL;DR: In this paper, a controlled-release copolymerization product of 50 to 99% by weight of a polyvinyl crosslinking agent and 0 to 45% of total monomers of a water-soluble monoolefinic monomer is defined, where the swelling ratio is 2:1 to 22:1.
Abstract: A controlled-release, drug-delivery composition which comprises (A) a crosslinked copolymer, capable of swelling in ethanol to give a swollen copolymer containing at least 40% by weight of ethanol, and capable of swelling in water to give a swollen copolymer containing no more than 20% by weight of water, where the swelling ratio (% ethanol: % water) is 2:1 to 22:1, which comprises the copolymerization product of (a) 50 to 99% by weight of said copolymer of a water-insoluble monoolefinic monomer or (a) with 0 to 45% by weight of total monomers of a water-soluble monoolefinic monomer, with (b) 50 to 1% by weight, but not more than 20 mol % of a divinyl or polyvinyl crosslinking agent; and (B) an effective amount of a pharmaceutical medicament is useful for the controlled and prolonged release of drugs when taken orally.

Journal ArticleDOI
TL;DR: RNA mapping studies suggest that the transcription of the HBsAg gene is initiated at more than one site, or alternatively, that RNA splicing of transcripts occurs in the pre-surface antigen region.
Abstract: We have constructed two simian virus 40 early replacement recombinants that have the coding sequences for hepatitis B virus surface antigen (HBsAg). One construction, LSV-HBsAg, has the coding region for HBsAg but not the portion encoding the putative pre-surface antigen leader. Transformed monkey kidney cells (COS) infected with this recombinant express large quantities of the characteristic partially glycosylated HBsAg molecule, which are assembled into 22-nm particles that appear similar to those produced by human liver cells infected with hepatitis B virus. This result indicates that the pre-surface antigen sequences are not required for the synthesis of HBsAg or its assembly into particulate structures. The second recombinant, LSV-HBpresAg, has the entire surface antigen gene, including the putative promoter and pre-surface antigen region. COS cells infected with this recombinant plasmid produce 40- to 50-fold less HBsAg than those infected with the LSV-HBsAg recombinant plasmid. RNA mapping studies suggest that the transcription of the HBsAg gene is initiated at more than one site, or alternatively, that RNA splicing of transcripts occurs in the pre-surface antigen region.

Journal ArticleDOI
TL;DR: In this article, a statistical method for incorporating historical control data in the analysis of proportions is proposed and illustrated, which has as its extremes logistic regressions completely pooling and completely ignoring historical controls.
Abstract: A statistical method for incorporating historical control data in the analysis of proportions is proposed and illustrated. The method has as its extremes logistic regressions completely pooling and completely ignoring historical controls. The degree of pooling used is determined by the variability from experiment to experiment in the control incidences. The fit of historical control groups to an assumed normal logistic model is assessed using probability plotting techniques. Monte Carlo studies evaluate the adequacy of the asymptotic approximation used. Sensitivity analyses show that results are insensitive to alternative priors. The method is applied to several sets of tumor data from animal experiments.

Journal ArticleDOI
TL;DR: Plasma and synovial fluid concentrations of diclofenac sodium and its principal hydroxylated metabolites have been measured in sixteen rheumatoid patients on chronic therapy to investigate possible reasons for the drug's extended duration of action despite its apparent short elimination half-life in plasma.
Abstract: Plasma and synovial fluid concentrations of diclofenac sodium and its principal hydroxylated metabolites have been measured in sixteen rheumatoid patients on chronic therapy to investigate possible reasons for the drug's extended duration of action despite its apparent short elimination half-life in plasma. Diclofenac was detected in synovial fluid 2 h after dosing but at a lower level than in plasma. Thereafter synovial fluid concentrations remained relatively constant through to 11 h post-dosing whereas plasma levels in the same period declined rapidly from an initially high peak to near the sensitivity limit of the assay. Hydroxylated metabolites (free + conjugated) were rapidly formed with measurable concentrations of the 4′ and 5 mono and dihydroxy derivatives being detected in plasma 2 h after dosing; levels of the 3′ hydroxy metabolite were negligible at this time. Initially plasma levels of all metabolites were higher than those in synovial fluid but after 4 h synovial fluid levels were equal to or slightly higher than those in plasma. The significance of these findings is discussed in relation to the drug's overall clinical effect.

Journal ArticleDOI
Alwyn Spencer1
TL;DR: The palladium-catalysed arylation of alkenes with aryl bromides or iodides was shown to proceed in high yields at very low palladium concentration when carried out in a suitable strongly polar solvent with a carboxylate anion as base.

Journal ArticleDOI
TL;DR: In this article, the 15 N-NMR spectra of azoles, with natural isotope abundance, have been measured under different experimental conditions, and chemical shifts are reported for imidazoles, pyrazoles, oxazoles and isoxazoles.
Abstract: The 15 N-NMR spectra of azoles, with natural isotope abundance, have been measured under different experimental conditions, and chemical shifts are reported for imidazoles, pyrazoles, oxazoles, isoxazoles, thiazoles, and isothiazoles. General trends of substituent effects in this heterocyclic series are discussed based on the data of 67 substituted azoles, dihydro- and tetrahydroazoles. 15 N, 1 H spin-coupling constants have been determined from spectra obtained by [ 1 H] → 15 N polarizationtransfer experiments, i.e. an application of INEPT and DEPT pulse sequences. Two-bond and three-bond coupling constants are fully assigned and are discussed in terms of the specific pathways in azoles. The potential of structural applications of the new data is illustrated for isomeric nitro-imidazoles and highly-substituted pyrazoles, and in the case of ring-chain tautomerism of 2-substituted tetrahydrooxazoles.

Journal ArticleDOI
TL;DR: Recently, compounds which bind avidly to benzodiazepine binding sites have been shown to possess diazepam antagonist properties, and these properties could be used to reverse effects ofdiazepam overdose and to speed recovery of diazepAM-treated patients after various out-patient procedures.

Journal ArticleDOI
TL;DR: Results obtained in this and other laboratories demonstrate that the firing rate of locus coeruleus neurons is affected by a great number of psychoactive agents such as antidepressants, minor tranquillizers, neuroleptics, psychostimulants and certain psychogeriatric drugs.
Abstract: The locus coeruleus is one of the most thoroughly investigated mammalian brain areas. Its fibers innervate large parts of the neuraxis, in particular, areas involved in cognitive functions such as the cortex and the hippocampus. A role of locus coeruleus has been proposed in such processes as memory, the control of vigilance, blood pressure and others. Results obtained in this and other laboratories demonstrate that the firing rate of locus coeruleus neurons is affected by a great number of psychoactive agents such as antidepressants, minor tranquillizers, neuroleptics, psychostimulants and certain psychogeriatric drugs. We have attempted to correlate the data obtained on the cell bodies of locus coeruleus with studies reporting effects on terminal areas and thereby gain an overall view of the action of the above mentioned drugs on this cell system. The activity of noradrenergic neurons in locus coeruleus is thought to correlate with the level of cortical vigilance. Special emphasis is placed on the finding that a number of drugs which exert a positive effect on cognitive functions in man and animals increase the firing rate of the rat locus coeruleus neurons.

Journal ArticleDOI
TL;DR: In 'ex vivo' studies, the inhibitory activity of CGP 11305 A was not lost by dilution or dialysis of homogenates from pretreated animals and the inhibitor could not be displaced by 5-HT, indicating an irreversible interaction.

Journal ArticleDOI
TL;DR: The DSP-4-treated rat may constitute a new model of functional supersensitivity to adrenergic agonists, and is discussed in terms of the selective action of D SP-4 and the responsiveness of Dsp-4 rats to adren allergic agonists.
Abstract: Rats treated with DSP-4 [N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine], a selective noradrenergic neurotoxin, showed no differences compared to control rats in the number of head dips, a measure of exploratory behavior. Since a previous neurochemical investigation had demonstrated that DSP-4 rats have supersensitive α2 and β-adrenergic receptors in certain regions of the central nervous system, the behavior of these animals was also examined after the injection of clonidine, an α2 agonist, and clenbuterol, a β agonist. These drugs reduced, in a dose-dependent manner, the head-dipping of both control and DSP-4 rats. However, this effect was of greater magnitude in DSP-4 animals. Control experiments suggested that the response to clonidine and clenbuterol was mediated centrally by α2 and β receptors, respectively. Other behavioral experiments with agonists of the dopaminergic and serotoninergic systems indicated that these neurotransmitter systems were unchanged in DSP-4 animals. The results are discussed in terms of the selective action of DSP-4 and the responsiveness of DSP-4 rats to adrenergic agonists. The DSP-4-treated rat may constitute a new model of functional supersensitivity to adrenergic agonists.

Patent
02 Dec 1983
TL;DR: In this article, a light sensitive silver halide emulsion layer that is spectrally sensitised with a monomethinecyanine dye of formula (I) is new.
Abstract: Photographic recording materials with a light sensitive silver halide emulsion layer that is spectrally sensitised with a monomethinecyanine dye of formula (I) is new. In (I), R = a benzthiophene residue bonded to the benzene ring of the benzthiazole group at a 2-, 3-, 4-, 5- 6- or 7- position; R and R = sulphoalkyl, carboxyalkyl, -(CH2)n-SO2-NH-SO2-alkyl, -(CH2)n-SO2-NH-CO-alkyl, -(CH2)n-CO-NH-SO2-alkyl or -(CH2)n-CO-NH-CO-alkyl; n = 1-6; R - R = H, halogen, -CN, -CF3, alkyl, alkoxy, aryl or heterocyclic group, or R together with R or R may complete an optionally substituted, condensed-on benzene or naphthalene ring; and M = a charge-balancing cation.

Journal ArticleDOI
O Lundvall, P E Abom, R. Holm1
TL;DR: The results indicate that certain patients have fewer attacks of restless legs during treatment with carbamazepine, and the patients who did not give any preference also had less pronounced symptoms during treatment.
Abstract: Carbamazepine or placebo were given in random order, during two four-week periods, in a double-blind, cross-over trial in six patients presenting with symptoms of restless legs. On global evaluation after completing the trial three patients and the physician preferred to continue treatment with carbamazepine. In the remaining three cases both the physician and the patients preferred not to continue with either of the treatments. However, the patients who did not give any preference also had less pronounced symptoms during treatment with carbamazepine. No patient felt better during treatment with placebo as compared to carbamazepine. The results indicate that certain patients have fewer attacks of restless legs during treatment with carbamazepine.

Patent
Willy Meyer1, Werner Dr. Föry1
17 Jan 1983
TL;DR: The N-phenylsulfonyl-N'-pyrimidinyl- and -triazinylureas of the general formula ##STR1## have good selective, pre- and post-emergence, herbicidal and growth-regulating properties.
Abstract: N-phenylsulfonyl-N'-pyrimidinyl- and -triazinylureas of the general formula ##STR1## and the salts of these compounds with amines, alkali metal or alkaline-earth metal bases or with quaternary ammonium bases have good selective, pre- and post-emergence, herbicidal and growth-regulating properties. The symbols in this formula have the following meanings: A is a C3 -C6 -alkynyl group, a C1 -C6 -alkyl group which is substituted by halogen, C1 -C4 -alkoxy, C1 -C4 -alkylthio, C1 -C4 - alkylsulfinyl, C1 -C4 -alkylsulfonyl, C1 -C4 -haloalkoxy, C1 -C4 -haloalkylthio, C1 -C4 -haloalkylsulfinyl or C1 -C4 -haloalkylsulfonyl, or it is a C2 -C6 -alkenyl group substituted by one of the above substituents, E is the methine group or nitrogen, X is oxygen, sulfur, or a sulfinyl or sulfonyl bridge, Z is oxygen or sulfur, m is the number one or two, R1 is hydrogen, halogen, C1 -C5 -alkyl, C2 -C5 -alkenyl, or a --Y--R6 group, R2 is hydrogen, halogen, C1 -C5 -alkyl, C2 -C5 -alkenyl or C1 -C4 -haloalkyl, or a group --Y--R6, --COOR7, --NO2 or --CO--NR8 --R9, R3 is hydrogen, C1 -C4 -alkyl, C1 -C4 -alkoxy, C1 -C4 -alkylthio, C1 -C4 -haloalkyl, C1 -C4 -haloalkoxy, halogen or alkoxyalkyl having at most 4 carbon atoms, R4 is hydrogen, methyl or ethyl, R5 is hydrogen, C1 -C4 -alkyl, C1 -C3 -alkoxy, methoxymethyl, cyanomethyl or cyanoethyl, R6 and R7 are each C1 -C5 -alkyl, C2 -C5 -alkenyl or C2 -C6 -alkynyl, R8 and R9 independently of one another are each hydrogen, C1 -C5 -alkyl, C2 -C5 -alkenyl or C2 -C6 -alkynyl, and Y is oxygen, sulfur, or a sulfinyl or sulfonyl bridge, and A can also be C2 -C6 -alkenyl when X is oxygen.

Patent
20 May 1983
TL;DR: Sizing agents as mentioned in this paper are known compounds and some of which are novel aromatic compounds which contain in the aromatic nucleus a single hydrophobic substituent containing at least 5 carbon atoms and at least one anionic group.
Abstract: Sizing agents, some of which are known compounds and some of which are novel aromatic compounds which contain in the aromatic nucleus a single hydrophobic substituent containing at least 5 carbon atoms and at least one anionic group, said hydrophobic substituent being linked to the aromatic nucleus through an ester, amide, urethane or urea bridge, with the CO group of ester and amide bridges being attached to the hydrophobic radical and a methylene group being optionally present between said bridges and the aromatic nucleus, are particularly suitable, together with commercially available retention aids, for use in a process for the mass sizing of paper or cardboard or for the surface sizing of paper.

Patent
Kurt Dr. Meier1, Buhler Niklaus1, Hans Dr. Zweifel1, Berner Godwin1, Friedrich Lohse1 
13 May 1983
TL;DR: In this article, the authors describe a set of curable compositions consisting of a kationisch polymerisierbaren organischen material and a cationically polymerizable organic material and mindestens einer Verbindung der Formel.
Abstract: Die Erfindung betrifft hartbare Zusammensetzungen, die aus The invention relates to curable compositions consisting of A) einem kationisch polymerisierbaren organischen Material und A) a cationically polymerizable organic material and B) mindestens einer Verbindung der Formel B) at least one compound of the formula worin a, m, n, q, R 1 , R 2 , M, L und Q die in Anspruch 1 angegebenen Bedeutungen haben, bestehen. wherein a, m, n, q, R 1, R 2, M, L and Q have the meanings given in claim 1, are made. Diese Zusammensetzungen eignen sich zur Herstellung von Oberflachenbeschichtungen, Druckplatten und insbesondere gedruckten Schaltungen. These compositions are suitable for the preparation of surface coatings, printing plates, and particularly printed circuits. Sie lassen sich direkt heissharten, werden aber vorzugsweise zunachst bestrahlt, was lagerfahige aktivierte Vorstufen ergibt, und dann heissgehartet. They can be hot cured directly, but are preferably first irradiated, resulting storable activated precursors and then hot-cured.