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Showing papers by "Novartis published in 1971"


Journal ArticleDOI
Louis J. Ignarro1
TL;DR: The results of these studies indicate that considerable caution must be exercised in the preparation, handling and incubation of lysosomes in order to reveal the stabilizing capacity in vitro of anti-inflammatory drugs.

129 citations


Journal ArticleDOI
Bruno Kamber1
TL;DR: In this paper, the conversion of S-acetamidomethyl cysteine peptides to by a reaction with iodine is described, and the method is applied in the synthesis of the hitherto unknown cyclo-L-cystine.
Abstract: The conversion of S-acetamidomethyl cysteine peptides to by a reaction with iodine is described. The method is applied in the synthesis of the hitherto unknown cyclo-L-cystine. The structure of this compound was confirmed by molecular weight determination, NMR. and mass spectroscopy.

107 citations


Journal ArticleDOI
TL;DR: It is concluded that recovery from corticosteroid-induced depression of immune reactivity is accelerated in the presence of somatotropic hormone, which can interfere with the effect of increased endogenous corticosterone in hypophysectomized animals.

79 citations


Patent
29 Nov 1971
TL;DR: Compositions for inhibiting corrosion and scale formation in aqueous systems which consist essentially of from 20 to 97.5% by weight of total composition of (a) a combination of zinc and hydrolyzed polymaleic anhydride and (b) 2.5 to 80% of total compositions of a corrosion inhibitor, particularly benzotriazole as discussed by the authors.
Abstract: Compositions for inhibiting corrosion and scale formation in aqueous systems which consist essentially of from 20 to 97.5% by weight of total composition of (a) a combination of zinc and hydrolyzed polymaleic anhydride and (b) 2.5 to 80% by weight of total composition of a corrosion inhibitor, particularly benzotriazole.

72 citations


Journal ArticleDOI
TL;DR: Es wird das physiologische Verhalten von Corticosteron in den einzelnen Zyklusphasen im Plasma and in den Nebennieren normaler weiblicher Ratten untersucht.
Abstract: Es wird das physiologische Verhalten von Corticosteron in den einzelnen Zyklusphasen im Plasma und in den Nebennieren normaler weiblicher Ratten untersucht. Die Corticosteronkonzentrationen in Plasma und Nebennieren sind wahrend der Proostrusphase signifikant hoher als wahrend den anderen Zyklusphasen. Der normale Tag-Nacht-Rhythmus bleibt in allen Zyklusphasen aufrechterhalten.

71 citations


Journal ArticleDOI
M. Staehelin1
TL;DR: Aus einem Vergleich der beschriebenen Sequenzen verschiedener Transferribonukleinsäuren lassen sich Schlüsse über die allgemeine Struktur dieser Moleküle ziehen, dass multiple Species vorliegen, sich aber in der Primärsequenz unterscheiden.
Abstract: Aus einem Vergleich der beschriebenen Sequenzen verschiedener Transferribonukleinsauren lassen sich Schlusse uber die allgemeine Struktur dieser Molekule ziehen. Samtliche Sequenzen lassen Basenpaarungen zu, die sich zweidimensional in einer Kleeblattform darstellen lassen. Die bisher bekannten Transferribonukleinsauren lassen sich in 3 Klassen aufteilen, je nachdem, ob sie 3–4 Basenpaare im DHU- und einen kurzen oder langen Extra-Arm besitzen. Die Verteilung der seltenen Nukleotide weist eine auffallende Regelmassigkeit auf. MethylierteBasen kommen meistens nur an einer bestimmten Stelle des Molekuls vor, nur vier wurden an zwei Stellen beschrieben. Dihydrouridin und Pseudouridin wurden an 6 bzw. 9 Stellen gefunden. Dies durfte darauf hinweisen, dass die Enzyme, die Nukleotide in der Transferribonukleinsaure modifizieren, nicht spezifische Transferribonukleinsauren erkennen, sondern spezifische Stellen in den verschiedensten Molekulen. Anhand der serinspezifischen Transferribonukleinsauren aus Rattenleber wird gezeigt, dass multiple Species vorliegen, die zum Teil das gleiche Codon erkennen konnen, sich aber in der Primarsequenz unterscheiden.

69 citations


Journal ArticleDOI
TL;DR: The results indicate that with the use of both models of AA it was possible to detect compounds which were selectively either AI or IS, whereas the anti-inflammatory agents inhibited the disease in a dose related manner.
Abstract: SummaryVarious methods for inducing AA in rats were examined using different rat strains, adjuvant preparations, and sites of injection. The time course of the development of arthritis in the injected and nonin-jected extremity was determined and methods for inducing a disease with limited variability and a high incidence was demonstrated. Standard compounds were tested in two models of AA with special reference to denning a method for discriminating between inhibition due to immunosuppression (IS) and that due to anti-inflammatory (AI) effects. 12 daily doses of IS agents, started on the day of adjuvant injection, totally prevented the disease in the noninjected extremity when measurements were made on day 21. Standard AI agents were ineffective. This test (nonestablished arthritis) was therefore capable of detecting compounds with immunosuppressive potential. The same standard compounds were administered daily for 12 days after the peak of the disease had been reached (established arthritis). In this te...

67 citations


Journal ArticleDOI
TL;DR: Substantial regeneration of complement‐receptor lymphocytes took place in lymph nodes of adult thymectomized whole‐body X‐irradiated mice reconstituted with semi‐allogeneic bone marrow to establish proof that CRL are of extrathymic, bone marrow origin.
Abstract: Substantial regeneration of complement-receptor lymphocytes (CRL) took place in lymph nodes of adult thymectomized whole-body X-irradiated mice reconstituted with semi-allogeneic (F1) bone marrow. In the presence of complement, alloantisera directed against the transplanted bone marrow killed more than 95% of the lymphoid cells of such chimeras. Moreover, lymph node cell suspensions and lymphoid tissue sections of neonatally thymectomized or adult thymectomized, irradiated and marrow-grafted mice contained an increased proportion of CRL. The results concur to establish proof that CRL are of extrathymic, bone marrow origin.

67 citations


Journal ArticleDOI
TL;DR: Histological examination showed a close relationship between depletion of small lymphocytes in the peripheral areas of the follicles and in the marginal zones of the spleen and diminished immune reactivity of the corresponding cell suspensions in vitro.

64 citations


Patent
Harris M1, Schibler L1
11 Nov 1971
TL;DR: In this paper, the authors describe an encapsulation process where the situations to be executed are dispersed in a DISTRIBUTION MEDIUM in the presence of a reactive tenside.
Abstract: AN ENCAPSULATION PROCESS IS PROVIDED WHEREIN THE SUBSTANCES TO BE ENCAPSULATED ARE DISPERSED IN A DISTRIBUTION MEDIUM IN THE PRESENCE OF A REACTIVE TENSIDE WHICH IS CAPABLE TO FORM A COMPOUND INSOLUBLE IN THE DISTRIBUTION MEDIUM. THE DISPERSED REACTIVE TENSIDE IS CONVERTED TO THE IRREVERSIBLE, INSOLUBLE STATE FORMING A PRIMARY CAPSULE SUSPENSION AND THEN MIXED WITH AN AMINOPLAST PRECONDENSATE SOLUTION TO FORM A SECONDARY SUSPENSION OF CAPSULES HAVING STRENGTHENED WALLS. THE REACTIVE TENSIDE AND THE AMINOPLAST PRECONDENSATE ALSO MAY BE ADDED TOGETHER AND CONVERTED TO THE IRREVERSIBLY INSOLUBLE STATE AT THE SAME TIME. THE CAPSULES ARE USEFUL TO ENCAPSULATE MOST DIVERSE ACTIVE SUBSTANCES, SUCH AS SOLVENTS, DYESTUFFS, PIGMENTS OR PESTICIDES.

62 citations


Journal ArticleDOI
L. Maitre1, M. Staehelin1, H.J. Bein1
TL;DR: Although 34276-Ba caused a concentration dependent inhibition of noradrenaline uptake into isolated bovine splenic nerve granules, it did not alter markedly the endogenous concentration of catecholamines in heart and brain even after repeated daily treatment.

Patent
Wilfried Leitz1
04 Feb 1971
TL;DR: In this paper, a pilferproof closure is applied on a failure line of reduced strength, where the closure member is formed from thermoplastic material and the skirt portion is warm rolled onto an undercut section of the neck of a container without heating the material at the failure line.
Abstract: Method of applying a pilferproof closure which has a capping portion and has joined thereto along a failure line of reduced strength a security ring which has adjacent said failure line an annular portion from which extends a skirt portion having a thickness less than that of the annular portion. The closure member is formed from thermoplastic material and the skirt portion is warm rolled onto an undercut section of the neck of a container without heating the material at the failure line so as to distort it.

Journal ArticleDOI
Louis J. Ignarro1
TL;DR: Chloroquine and glucocorticosteroids were the only anti-inflammatory drugs found to stabilize appreciably the lysosomes obtained from rabbit peritoneal polymorphonuclear leukocytes.

Patent
12 Oct 1971
TL;DR: Alkyl esters derived from alkylthioalkanoic acids and alkane polyols are stabilizers of organic material normally subject to thermal and oxidative deterioration as discussed by the authors.
Abstract: Alkyl esters derived from alkylthioalkanoic acids and alkane polyols are stabilizers of organic material normally subject to thermal and oxidative deterioration. They are prepared by conventional esterification techniques. Typical embodiments are pentearythritol tetrakis (3-n-dodecylthiopropionate) and ethylene bis (3-n-didecylthiopropionate). The esters are used in conjunction with phenolic antioxidants to effectively stabilize organic materials from the deliterious effects of heat and oxygen.

Patent
Peter Kelmchuk1
01 Feb 1971
TL;DR: A typical embodiment includes polyamides which are stabilized with 1,2-bis[3,5-di-t-butyl-4-hydroxyphenyl)-propionamido]ethane and sodium hypophosphite, copper acetate and potassium iodide as mentioned in this paper.
Abstract: Heat stabilized synthetic polyamide compositions are prepared by incorporating therein a mixture of a phenolic antioxidant and metal hypophosphite, a copper compound and metal halide. A typical embodiment includes polyamides which are stabilized with 1,2-bis[3,5-di-t-butyl-4-hydroxyphenyl)-propionamido]ethane and sodium hypophosphite, copper acetate and potassium iodide.

Journal ArticleDOI
H. Fritz1, R. Hess1
TL;DR: It is concluded that embryotoxicity and teratogenicity are largely independent phenomena.
Abstract: Groups of pregnant rabbits were given cyclophasphamide (Endoxan Asta®) in single intravenous doses of 30 mg/kg on different days from the 6th day to the 14th day of gestation. On the 28th day (shortly before term) the foetuses were removed by caesarean section. Administration of cyclophosphamide about the time of implantation led to an increase in the number of early embryonic deaths. Injection of cyclophosphamide at the later stages resulted in an increased number of foetal deaths. About 10% of the foetuses from dams treated on the 7th day of pregnancy exhibited malformations, in particular disturbances of ventral closure. When cyclophosphamide was administered on the 11th day of pregnancy more than 30% of the foetuses were found to have median cleft palates and other malformations of jaws and lips. All the foetuses from dams treated on the 12th day showed oligodactylia and brachydactylia. The latter type of malformation was also present when treatment was given on the 13th day. The embryotoxic effect of cyclophosphamide administration was particularly evident in the early periods of embryonic development. In contrast, the teratogenic action was more confined to the later periods of organogenesis. Teratogenicity occurred in two peaks corresponding to characteristic ‘phaenocritical’ phases of development. The first and lower peak coincided with the period of histiotrophic nutrition and the second and higher peak corresponded to the heamotrophic phase. It is concluded that embryotoxicity and teratogenicity are largely independent phenomena.

Patent
J Wasley1, A Wajngurt1
01 Jul 1971
TL;DR: In this article, the indazolaminoquinolines, acid addition salts thereof as well as Noxides thereof are substituted with 7-chloro-4-(6-indazol amino)-quinoline and ethyl 7- chloro- 4-(6-(6)-indazilamino-quinoline-3-carboxylate.
Abstract: Substituted indazolaminoquinolines, acid addition salts thereof as well as N-oxides thereof are anti-inflammatory, anti-hypertensive and anti-malarial agents. Illustrative embodiments are 7-chloro-4-(6-indazolamino)-quinoline and ethyl 7-chloro-4-(6-indazolamino)-quinoline-3-carboxylate.

Journal ArticleDOI
Bruno Kamber1
TL;DR: In this paper, the disulfide bridge between A20 and B19 was established by oxidation with iodine of two S-trityl cysteine peptides in which the carboxyl and amino groups were protected by the t-butyl and tbutyloxycarbonyl residue.
Abstract: The synthesis of six insulin fragments is described, in which various sequences of the two chains are linked by the disulfide bridge between A20 and B19. The fragments in question are: A20–21–B19–21, A20–21–B18–21, A20–21–B17–21, A19–21–B19–21, A16–21–B18–21 and A20–21–B12–21. In order to build up the simpler fragments the disulfide bridge was established by oxidation with iodine of two S-trityl cysteine peptides in which the carboxyl and amino groups were protected by the t-butyl and t-butyloxycarbonyl residue. From the mixture obtained the unsymmetrical cystine peptide was separated in all cases from the two symmetrical ones by counter-current distribution. In the synthesis of the more complex fragments advantageous use was made of smaller unsymmetrical fragments prepared as above but having one amino group protected by the N-trityl residue. After selective elimination of this group it was possible to lengthen the peptide chain at this position. The free peptides were obtained by removal of the protecting groups with strong acids, in particular concentrated hydrochloric acid. While in this deprotecting step the disulfide bond was stable, conditions are discussed under which disproportionation was observed. None of the six synthetic insulin fragments showed activity in stimulating rat adipose tissue to convert 14C-labelled glucose to CO2in vitro.


Patent
22 Jun 1971
TL;DR: In this paper, the authors define an ARYLENE group, where the members are either hydrogens or chlorine atoms, and N is a whole number larger than 3.
Abstract: WHEREIN R IS AN ARYLENE GROUP, THE BONDS TO WHICH ARE NOT IN THE ORTHO-POSITION, X IS HYDROGEN OR CHLORINE ATOM AND N IS A WHOLE NUMBER GREATER THAN 3, ARE USEFUL FOR COLORING PLASTIC AND LACQUERS, ESPECIALLY SOFT POLYVINYL CHLORIDE IN RED SHADES WITH GOOD LIGHT AND SUBLIMATION FASTNESS PROPERTIES. (1-((2-CL,4-X,5-(-CO-)-PHENYL)-N=N-),2-(HO-),3-(-CO-)- NAPHTHALENE)N (-NH-R-NH-)N POLYAZO PIGMENTS OF THE FORMULA

Patent
Gannon J1
30 Sep 1971
TL;DR: In this paper, the authors compare the performance of a carbo-oxygen-constrained expo-branch with deterministic and deterministic deterministic polynomials.
Abstract: COMPOSITIONS COMPRISING CARBOXYL CONTAINING POLYESTERS AND DI- OR POLYEPOXIDES. THE COMPOSITIONS WHEN CURED EXHIBIT EXCELLENT ADHESION TO UNTREATED AND TREATED SUBSTRATES, EXCELLENT FLEXIBILITY AND GOOD RESISTANCE TO CHEMICAL ATTACK.

Journal ArticleDOI
W. Biedermann1
TL;DR: The saturation values of these modifications in cellulose acetate have been determined at 80°C as mentioned in this paper, and they are important in the disperse dyeing of cellulose and polyester materials because of their influence on colour yield and the stability of the dispersion.
Abstract: Meetings of the Manchester Region held at the Manchester Literary and Philosophical Society, Manchester, on 15 January 1970, Mr H. R. Hadfield in the chair; and of the Leeds Junior Section, held in the Department of Colour Chemistry and Dyeing, University of Leeds, on 19 January 1970, Mr K R. F. Cockett in the chair The dye 2-nitroaniline-4-ethylsulphone, 1-phenyl-3-methyl-5-aminopyrazole (aminopyrazole yellow) has been isolated in five different crystal modifications. The saturation values of these modifications in cellulose acetate have been determined at 80°C. Crystal modifications are important in the disperse dyeing of cellulose acetate and polyester materials because of their influence on colour yield and the stability of the dispersion.

Patent
J Hrach1, F Breitenfellner1
24 Aug 1971
TL;DR: In this article, the authors used a POLYESTERM of an InTRINSIC VISCOSITY of at least 0.7 DL/G and a CRYSTALLISATION TEMPERATURE of at LEAST 150*C.
Abstract: THE PRODUCTION OF TRANSPARENT AMORPHOUS ARTICLES FROM POLYETHYLENE TEREPHTHALATES BY USING A POLYESTER OF AN INTRINSIC VISCOSITY OF AT LEAST 0.7 DL/G. AND A CRYSTALLISATION TEMPERATURE OF AT LEAST 150*C.

Patent
A Staub1
12 Apr 1971
TL;DR: A CATIONIC ANTHRAQUINONE DYESTUFF, the Cationic PORTion of WHICH is free of GROUPS that DISSOCIATE ACIDly in WATER and CORRESPONDS to the formula (1-(R1-CH(-R2)-NH-),4-(X1-N(+)(-X2)(- X3)-Q-NH-)-ANTHRA QUINONE) Y(-) wherein R1 and R2 EACH REPRESENT A LOWER
Abstract: A CATIONIC ANTHRAQUINONE DYESTUFF, THE CATIONIC PORTION OF WHICH IS FREE OF GROUPS THAT DISSOCIATE ACIDLY IN WATER AND CORRESPONDS TO THE FORMULA (1-(R1-CH(-R2)-NH-),4-(X1-N(+)(-X2)(-X3)-Q-NH-)-ANTHRA QUINONE) Y(-) WHEREIN R1 AND R2 EACH REPRESENT A LOWER ALKYL GROUP, Q REPRESENTS A LOWER ALKYLENE GROUP, X1 AND X2 EACH DENOTES AN OPTIONALLY SUBSTITUTED LOWER ALKYL GROUP, OR X1 AND X2 TOGETHER WITH THE NITROGEN ATOM THAT UNITES THEM AND, OPTIONALLY WITH INCLUSION OF A FURTHER HETERO ATOM, REPRESENT A HETEROCYCLIC RADICAL, X3 REPRESENTS AN OPTIONALLY SUBSTITUTED ALKYL, CYCLOALKYL OR ARYLALKYL RADICAL, AND Y REPRESENT THE ANION EQUIVALENT OF AN INORGANIC OR ORGANIC ACID.

Patent
12 Jan 1971
TL;DR: In this article, the authors present a set of non-TEXTile sheets for carrying out transfer printing, which are CHARACTERIZED in that they CARRY A DYESTUFF OF THE FORMULA 1-(NH2-)(N-1),1-(R1-N(-R2)-)(2-N),2-(NC-N)-1,2-(Y-)(2 -N),4-(PHENYL-or CYCLOHEXYL-NH-NH)-NH-N- 1),4-(R''
Abstract: NON-TEXTILE SHEET MATERIALS FOR CARRYING OUT TRANSFER PRINTING, CHARACTERIZED IN THAT THEY CARY A DYESTUFF OF THE FORMULA 1-(NH2-)(N-1),1-(R1-N(-R2)-)(2-N),2-(NC-)(N-1),2-(Y-)(2-N) ,4-(PHENYL- OR CYCLOHEXYL-NH-)(N-1),4-(R''-N(-R2'')-)(2-N) -ANTHRAQUINONE WHEREIN THE RING A IS AROMATIC OR SATURATED, R1 IS A HYDROGEN ATOM OR AN ALKYL RADICAL CONTAINING 1 TO 6 CARBON ATOMS, R2 REPRESENTS A HYDROGEN ATOM OR AN ALKYL RADICAL CONTAINING 1 TO 6 CARBON ATOMS, Y IS A HYDROGEN, A BROMINE OR A CHLORINE ATOM OR A METHOXY GROUP, R1'' DENOTES A HYDROGEN ATOM OR AN ALKYL RADICAL CONTAINING 1 TO 6 CARBON ATOMS, R2'' REPRESENTS AN ALKYL GROUP CONTAINING 1 TO 6 CARBON ATOMS, AND N IS 1 OR 2, WITH THE PROVISO THAT IF Y IS A HYDROGEN ATOM, THE ALKYL GROUPS PRESENT MUST CONTAIN AT LEAST 3 CARBON ATOMS, OR A MIXTURE OF SUCH DYESTUFFS AND OPTIONALLY OTHER SULIMABLE DYESTUFFS AND/OR OPTICAL BRIGHTENERS.

Patent
Kay R Mc1, G Bradley1
06 May 1971
TL;DR: In this article, a diarylide pigment composition is produced by coupling a tetrazotised pigment benzidine with a pigment coupling agent, preferably an acetoacetarylamide, and incorporating in the pigment a water-soluble coupled diary lide dyestuff, preferably prior to the isolation and drying of the pigment.
Abstract: A process in which a diarylide pigment composition is produced by coupling a tetrazotised pigment benzidine with a pigment coupling agent, preferably an acetoacetarylamide, and incorporating in the pigment a water-soluble coupled diarylide dyestuff, preferably prior to the isolation and drying of the pigment, and the diarylide pigment composition having better colour strength and transparency properties than conventional diarylide pigments when incorporated in printing inks.

Journal ArticleDOI
L. Machemer1, R. Hess1
TL;DR: Im Gegensatz zu Thio-TEPA (N, N′, N″-Triaethylen-thiophosphoramid) und MMS (Methansulfonsäuremethylester) führten i.p. dosen von Phenylbutazon bei der Maus zu keinen genetischen Effekten im Sinne der Induktion von dominanten Letalfaktoren.
Abstract: Im Gegensatz zu Thio-TEPA (N, N′, N″-Triaethylen-thiophosphoramid) und MMS (Methansulfonsauremethylester) fuhrten i.p. Dosen von Phenylbutazon (50 und 100 mg/kg) bei der Maus, unter Berucksichtigung von post- und prae-implantativen Gestationsstadien, zu keinen genetischen Effekten im Sinne der Induktion von dominanten Letalfaktoren.

Patent
10 Aug 1971
TL;DR: In this article, a method for the manufacture of devices for emitting vapours of active volatile agents, in particular those which are insecticidal, insect-repellent or condition the air especially in closed spaces.
Abstract: A method for the manufacture of devices for emitting vapours of active volatile agents, in particular those which are insecticidal, insect-repellent or condition the air especially in closed spaces. Liquid containing or constituted by the active agent and a solid mass having as base a macromolecular substance other than natural cellulose are placed in a container, e.g. a sachet, which is then sealed and stored until the liquid is completely absorbed by the mass, forming a solid solution therein. The device is put in operation by opening and/or removing the container.

Patent
D Porret1, Habermeier J1, H Batzer1
01 Nov 1971
TL;DR: In this article, the epoxide adducts are derived from polyepoxide compounds which on an average contain more than one epoxide group in the molecule, and less than one equivalent of NH groups for every epoxide equivalent of the poly-epoxide compound, i.e., a binuclear, five or six-membered, unsubstituted or substituted N-heterocyclic compound with an endocycyclic NH group in each nucleus.
Abstract: New ''''advanced'''' adducts, containing epoxide groups, from (1) polyepoxide compounds which on an average contain more than one epoxide group in the molecule, and (2) less than one equivalent of NH groups for every epoxide equivalent of the polyepoxide compound (1) of a binuclear, five or six-membered, unsubstituted or substituted N-heterocyclic compound with an endocyclic NH group in each nucleus, the heterocyclic rings being linked by a divalent aliphatic, cycloaliphatic or araliphatic radical, preferably an alkylene radical, which may be interrupted by oxygen atoms, e.g. the reaction product of 2 mols of diomethanediglycidyl ether and 1 mol of 1,1''-methylene-bis-(5,5-dimethylhydantoin). The epoxide resins ''''advanced'''' by means of such nitrogen compounds have a good storage stability and excellent electrical properties.

Patent
R Fischer1
11 Jun 1971
TL;DR: A tamperproof container for vials and the like formed from a receptacle base member and a lid which are adapted to be connected to each other by means of an interfitting structure of pins and columns extending from the lid and the base.
Abstract: A tamperproof container for vials and the like formed from a receptacle base member and a lid which are adapted to be connected to each other by means of an interfitting structure of pins and columns extending from the lid and the base. The interfitting structure can be mechanically joined, chemically bonded, or ultrasonically welded, as is adapted to permanently join the lid to the base and to separate the assembled container into several sections. The lid is formed with frangible zones which are positioned to align with each of the sections of the assembled container so that access to each of the sections of the assembled container can be obtained only by removing the frangible zone directly above that section.