Abstract: Novel monoclonal antibodies capable of distinguishing between cyclosporins, e.g. Cyclosporine, and metabolites, e.g. Cyclosporins 17 and 18, are produced, e.g. starting from novel cyclosporins having an activated coupling group, e.g. activated carboxy group, e.g. (i) [(O-succinimidooxysuccinyl)-Thr].sup.2 -Cyclosporine and (ii) [(N-.epsilon.-succinimidooxysuccinyl)-(D)Lys].sup.8 -Cyclosporine. Cyclosporin starting materials required for the production of cyclosporins of type (ii), e.g. [(D)Lys].sup.8 -Cyclosporine are also new and additionally have utility in the preparation of novel labelled cyclosporin derivatives, as well as antibodies and antisera generally. Also claimed are novel antigenic conjugates and hybridoma cell lines used in the production of antibodies and antisera as aforesaid as well as assay kits comprising novel antisera, antibodies and/or labelled cyclosporins as aforesaid.
Type:
Grant
Filed:
October 31, 1988
Date of Patent:
December 8, 1992
Assignee:
Sandoz Ltd.
Inventors:
Joachim Rosenthaler, Roland Wenger, Philipp E. Ball, Max H. Schreier, Valerie Quesniaux
Abstract: Halogenoalkylphenyl-alcohols, ketones and their hydrates of formula I, ##STR1## wherein R.sub.1 to R.sub.8 are as defined in the description, are useful as acetylcholinesterase inhibitors.
Abstract: Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represent hydrogen, alkyl, alkenyl, cycloalkyl, aryl or aralkyl are produced by a new environmentally acceptable process.
Abstract: A polymeric composition which reduces the loss of flowability of a cementitious composition comprises at least one polymer as a salt thereof having the form of a copolymer of(a) a maleic anhydride half-ester with a compound of the formula IRO(AO).sub.m H (I)where R is a C.sub.1-20 alkyl group, A is a C.sub.2-4 alkylene group and m is an integer from 2-16; and(b) a monomer having the formula IICH.sub.2 .dbd.CHCH.sub.2 -(OA).sub.n OR (II)where n is an integer from 1-90.In a preferred embodiment, there is present a polycarboxylate salt which is at least one polymer or copolymer comprising at least one of the monomers acrylic acid, methacrylic acid, maleic anhydride, maleic acid and maleic acid monoester, polymer and polycarboxylate salt being blended in the proportion of 0.1-10 parts of weight of polymer per part of polycarboxylate salt.Cementitious compositions such as concrete in which such polymeric compositions are included maintain their slump properties.
Abstract: The invention discloses certain substituted .alpha.-aminoacids having the formula ##STR1## where m and n are 1 or 2, and R, R.sub.1, R.sub.2, R.sub.3 and Y have various significances, which compounds are useful in treating epilepsy, disorders associated with excess GH or LH secretion, anxiety, schizophrenia, depression, CNS degenerative disorders, cerebral hypoxic conditions and stress-related psychiatric disorders.
Abstract: The invention relates to organic copolymers in free acid or salt form with recurring units of formula I ##STR1## in which R is an alkylene radical with 2 to 6 carbon atoms,R.sub.1 is a C.sub.1-20 alkyl-, cycloalkyl- or phenyl group,x, y and z are numbers from 0.01 to 100,m is a number from 1 to 100 andn is a number from 10 to 100,with the provisos, thati) the ratio of x to (y+z) is from 1:10 to 10:1 inclusive,ii) the ratio of z to y is from 3:1 to 100:1, andiii) m+n=15-100.The products of the invention are excellent superplasticizers and can be used as additives to cementitious mixes.
Abstract: Suppositories comprising a suppository base, a calcitonin and taurocholic acid or a pharmaceutically acceptable salt thereof exhibit improved bioavailability and are well tolerated.
Abstract: Somatostatin analogues and derivatives in free form or in pharmaceutically acceptable salt or complex form are useful for treating degenerative and inflammatory processes in bone or catilage, e.g. arthritic conditions or diseases.
Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is alkyl, alkoxy, alkylthio, alkylamino, aryl, aryloxy, arylthio, arylamino, aralkyl, aralkoxy, aralkylthio or aralkylamino,R.sub.2 and R.sub.3 are each independently hydrogen, halogen, hydroxy, mercapto, nitro or amino or have the meanings given for R.sub.1, andX is --NH.sub.2, --NH--OH, --N(R.sub.4)OH, --NH--NH.sub.2 or --NH--N.dbd.C(R.sub.4)R.sub.5, whereinR.sub.4 and R.sub.5 are each alkyl,in free form or pharmaceutically acceptable salt form, have pharmaceutical utility, in particular in the treatment or prophylaxis of asthma, or in the treatment of inflammation or psoriasis.
Abstract: The invention discloses certain 5-aryl-substituted-2,3-dihydro-imidazo[1,2-a]furo- and thieno pyridines useful as PAF receptor antagonists and for treating tumors, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-mediated bronchoconstriction and extravasation, for controlling hyperreactive airways, for protecting against endotoxin-induced hypotension and death and for treating tumors.
Abstract: The invention relates to a nitrate of (6R,7R)-7-{[2-(2-amino-4-thiazolyl)]-2-oxoacetamido}-3-(1,2,3-thiadizol-5- yl)thiomethyl-3-cephem-4-carboxylic acid, a process for its production and its use.
Abstract: Compounds of the formula ##STR1## wherein R is halo,R.sub.1 is cyano; (C.sub.1-6 alkoxy)carbonyl; (C.sub.3-6 alkenyl)oxycarbonyl; C.sub.1-4 alkylsulfonyl; phenylsulfonyl; (C.sub.1-4 alkyl)carbonyl; benzoyl; carbamoyl; (C.sub.1-4 alkyl)carbamoyl; N,N-di-(C.sub.1-4 alkyl)carbamoyl; phenylcarbamoyl; benzyloxycarbonyl; or (C.sub.1-6 alkoxy)carbonyl, (C.sub.3-6 alkenyl)oxycarbonyl, C.sub.1-4 alkylsulfonyl, phenylsulfonyl or (C.sub.1-4 alkyl)carbamoyl substituted by one or two substituents independently selected from chloro, bromo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, cyano and acyl, andR.sub.2 is formyl, cyano, --CH.dbd.C(R.sub.4).sub.2 or --CH.dbd.N--OH,wherein (1) each R.sub.4 is independently cyano; (C.sub.1-6 alkoxy)carbonyl; (C.sub.3-6 alkenyl)oxycarbonyl; (C.sub.3-6 alkynyl)oxycarbonyl; or (C.sub.1-6 alkoxy)carbonyl, (C.sub.3-6 alkenyl)oxycarbonyl or (C.sub.3-6 alkynyl)oxycarbonyl substituted by one or two substituents independently selected from chloro, bromo, C.sub.1-4 alkyl, C.sub.
Abstract: A cationic polymer composition suitable for use as a flocculating agent and as a retention aid in paper making consists of a mixture ofa) a hydrophilic cationic polymer,b) an anionic surfactant,optionally c) a water-immeriscible oil in which the polymer a) is insoluble,and, if c) is present,optionally d) a lipophilic non-ionic surfactant,optionally e) waterand optionally f) an oil-miscible polar solvent.The compositions may be prepared by water-in-oil emulsion polymerisation and are readily diluted with water.
Abstract: Compounds of the formulae ##STR1## salts thereof, and mixtures of such compounds or salts,wherein Me, Pc, Q.sub.1, R.sub.1, R.sub.2, R.sub.3, Y, a, b, c and d as defined,useful as fiber-reactive dyes for dyeing or printing hydroxy group- and nitrogen-containing organic substrates, for example, textile material comprising cotton, the obtained dyeings and prints having good all-round fastnesses, such as good light fastness.
Abstract: 1:2 metal complexes of the formula ##STR1## wherein each of R.sub.1 and R.sub.3 is independently hydrogen or nitro, with the proviso that when a ring has two nitro groups, they are meta to each other,each of R.sub.2 and R.sub.4 is independently hydrogen, chloro or --SO.sub.3 M,each of R.sub.5 and R.sub.6 is independently hydrogen, --COR.sub.7, --CONHR.sub.8 or --SO.sub.2 R.sub.9,whereinR.sub.7 is C.sub.1-6 alkyl, C.sub.1-6 alkoxy, phenyl(C.sub.1-4 -alkyl) or phenyl (C.sub.1-4 alkyl) the phenyl group of which is substituted by 1 or 2 substituents selected from halo, C.sub.1-4 -alkyl, C.sub.1-4 alkoxy, nitro, amino, --COOM, --SO.sub.3 M and acetamido,R.sub.8 is hydrogen; C.sub.1-6 alkyl; phenyl; phenyl substituted by 1 or 2 substituents selected from halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, amino, --COOM, --SO.sub.3 M and acetamido; naphthyl or naphthyl monosubstituted by chloro, amino, phenylamino, acetamido, benzamido or --SO.sub.3 M, andR.sub.9 is C.sub.
Abstract: Acid addition salt of taurine or glycine, their amino group being amidated with a carboxylic acid residue which contains the structure of a 3.alpha., 7.alpha., 12.alpha.-trihydroxysteroid, their acid group being neutralized with the amino group of an aliphatic amine or neutralized with the amino group of a basic .alpha.-amino carboxylic acid which group is connected over an alkylene bridge with the .alpha.-amino acid group, may be used e.g. as transmucuous resorption promoter of drug compounds.
Abstract: Sulpho group-containing dioxazine compounds corresponding to the formula ##STR1## in which the symbols are as defined in the specification, and salts thereof as well as dyeing preparations thereof are useful for dyeing or printing hydroxy group- or nitrogen-containing organic substrates, optionally combined with a special after-treatment of the dyed or printed textiles thus obtained to improve their wet fastness properties. Most preferred substrates are textile material containing or consisting of cellulose and paper.
Abstract: An apparatus and a process for mixing water from a pressurized source and an additive or admixture for a cementitious composition in a mixing chamber comprising introducing, in the form of a jet, water under a first pressure, which is above atmospheric pressure, and introducing the additive under a second pressure between atmospheric pressure and the first pressure, the amount of the additive that is introduced to the mixing chamber being controlled by means regulated by the pressure of water.
Abstract: Process for the synthesis of compounds of the formula ##STR1## comprising the steps of (i) reacting a compound of the formula ##STR2## with oxalyl chloride or oxalyl bromide to form the corresponding compound of the formula ##STR3## (ii) reacting said compound of the formula ##STR4## with a compound of the formula ##STR5## to form the corresponding compound of the formula ##STR6## (iii) hydrolyzing said compound of the formula ##STR7## to obtain the corresponding compound of the formula ##STR8## the use of the compounds of the formula ##STR9## for the synthesis of the compounds of the formula ##STR10## and the use of the intermediates of Formula VII for the direct synthesis of the compounds of Formula II,whereinR.sub.1 is C.sub.1-3 alkyl, phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C.sub.1-3 alkyl, C.sub.1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups),R.sub.