Abstract: A new polymer, the feed monomers and molar percents of which, exclusive of a polymerization initiator and crosslinker, are:A. (I) 42 mole % to 58 mole % of a siloxy silane of formula I,(II) 42 mole % to 58 mole % of an unsubstituted alkyl (meth)acrylate of formula II,(III) 0 to 5 mole % of a Group A monomer, and(IV) 0 to 16 mole % of an additional vinylic copolymerizable monomer;B. (I) 42 mole % to 58 mole % of a siloxy silane of formula I,(II) 21 mole % up to less than 42 mole % of an unsubstituted alkyl (meth)acrylate of formula II,(III) 0 to 5 mole % of a Group A monomer, and(IV) 0 to 29 mole % of an additional vinylic copolymerizable monomer; orC. (I) 16 mole % up to less than 42 mole % of a siloxy silane of formula I,(II) 42 mole % to 58 mole % of an unsubstituted alkyl (meth)acrylate of formula II,(III) 0 to 5 mole % of a Group A monomer, and(IV) 0 to 36 mole % of an additional vinylic copolymerizable monomer;where formula I is ##STR1## where formula II is ##STR2## in which R.sub.
Abstract: Novel compounds of formula I ##STR1## wherein R is selected from butyl, diethoxymethyl, cyclohexylmethyl, cyclohex-3-enylmethyl, benzyl, 4-chlorobenzyl, 4-methylbenzyl and 4-methoxybenzyl, R.sub.1 is selected from hydrogen and hydroxy, R.sub.2 is selected from hydrogen, chlorobenzyl, dichlorobenzyl, .alpha.-cyclopropyl-dichloro-benzyl, dichlorophenyl-2-hydroxy-ethyl, dimethylbenzyl, trimethoxybenzyl, methylenedioxybenzyl, chlorophenylethyl, dichlorophenylethyl, chloro-iodo-phenylethyl, dimethoxyphenylethyl, methylenedioxyphenylethyl, trimethoxyphenylethyl, 3-phenylprop-2-yl, 3-phenyl-3-hydroxy-prop-2-yl, dichlorophenylpropyl, dichlorophenyl-3-hydroxyprop-2-yl, dichlorophenylbutyl and quinolin-4-ylmethyl, and R.sub.3 is selected from hydrogen and methyl, and salts thereof, have GABA.sub.B -antagonistic properties and can be used for the treatment of diseases responsive to GABA.sub.B -antagonists.
Abstract: A composition for the transdermal administration of ionic pharmaceutically active agents comprising the active agent along with a suitable counter ion, water, and isopropanol, at an adjusted pH is disclosed. Also disclosed are transdermal systems which employ this composition and methods of transdermally administering such agents therewith. The main advantage achieved is improved flux rates of active agent over other systems.
Abstract: The present invention relates to novel oxazolidines of formula (1) ##STR1## wherein R.sub.1 and R.sub.2 are simultaneously hydrogen or both are the same lower alkyl radical or together are 4- to 7-membered lower alkylene, and to the salts thereof in racemic and chiral form, to the preparation of these novel compounds, to pharmaceutical compositions containing them and to the use thereof as medicaments. The compounds have a stimulating effect on beta-adrenergic receptors and can be used, inter alia, for the treatment of diseases associated with reversible obstruction of the respiratory tract, typically asthma and chronic bronchitis, and also for inflammations of different origin.
Type:
Grant
Filed:
August 17, 1993
Date of Patent:
November 29, 1994
Assignee:
Ciba-Geigy Corporation
Inventors:
Alfred Sallmann, Hans-Peter Gschwind, Eric Francotte
Abstract: Biphenylyl compounds of formula ##STR1## wherein the variables R.sub.1, R.sub.2, R.sub.3, p, q and X and the rings A and B are as defined in claim 1, in free form or in salt form, can be prepared in a manner known per se and can be used, for example, as active ingredients in medicaments.
Type:
Grant
Filed:
July 9, 1993
Date of Patent:
November 29, 1994
Assignee:
Ciba-Geigy Corporation
Inventors:
Tibur Schmidlin, Franz Ostermayer, Peter Buhlmayer
Abstract: The invention relates to a novel process for the preparation of compounds of formula I ##STR1## wherein R is straight-chain C.sub.2 -C.sub.4 alk-1-en-1-yl, and salts thereof, and to a novel starting material and the use thereof.
Abstract: Naphthalocyanine-chelate complexes of formula I ##STR1## are described which contain as central atom M aluminum, gallium, indium, fin, ruthenium or preferably germanium and in which the remaining symbols are as defined in claim 1. The complexes can be used inter alia in the photodynamic chemotherapy of tumors.
Abstract: Compounds of formula I ##STR1## wherein Y, Z, S, S', m, n and R.sub.1 -R.sub.4 are as defined in the description, have valuable pharmaceutical properties and are effective especially against protozoal infections. They are prepared in a manner known per se.
Type:
Grant
Filed:
June 1, 1993
Date of Patent:
October 11, 1994
Assignee:
Ciba-Geigy Corp.
Inventors:
Jaroslav Stanek, Giorgio Caravatti, Hans-Georg Capraro, Jorg Frei
Abstract: Peptides of formula I ##STR1## in which R is hydrogen or acetyl and X is an amino acid sequence of formula -Ser-Leu-Asp-Ser-Pro-Arg-Ser- (Ia) or of formula -Arg-Ile-Ile-Ala-Gln- (Ib), and salts of such compounds, can be used for the treatment of diseases involving bone degeneration.
Abstract: The invention relates to novel thiosemicarbazones of formula I ##STR1## wherein R.sub.1 is lower alkyl, lower alk-2-en-1-yl or lower alk-2-yn-1-yl,R.sub.2 and R.sub.3 independently of one another are hydrogen or lower alkyl, or R.sub.2 and R.sub.3 together are lower alkylidene,R.sub.4 is hydrogen, lower alkyl, lower alkoxy, aryl or aryl-lower alkyl, or the group --C(.dbd.O)--R.sub.6 wherein R.sub.6 is lower alkyl, aryl, heteroaryl, aryloxy, aryl-lower alkoxy or lower alk-2-en-1-yloxy,R.sub.5 is aryl, aryl-lower alkyl, unsaturated or saturated heterocyclyl-lower alkyl, lower alkoxycarbonyl-lower alkyl or the group --C(.dbd.O)--R.sub.7 wherein R.sub.7 is lower alkyl, aryl, aryl-lower alkyl, aryl-lower alkenyl, heteroaryl, aryloxy, aryl-lower alkoxy or lower alk-2-en-1-yloxy, or, when R.sub.4 is other than hydrogen, R.sub.
Abstract: The invention relates to a novel advantageous oral dosage form for methanediphosphonates, especially the active ingredient disodium pamidronate. A preferred dosage form comprises:a) disodium-3-amino-1-hydroxypropane-1,1-diphosphonate (disodium pamidronate),b) a cationic macroporous ion exchange resin based on a styrene/divinylbenzene copolymer having an exchangeable aminophosphonate group and, where appropriate,c) further pharmaceutically acceptable excipients.The ingredients can be processed to form tablets, dragees, capsules etc.
Abstract: Salts of aminosulfonic acid derivatives of formula I ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each independently of the others an aliphatic hydrocarbon radical having from 7 to 21 carbon atoms,n is 0 or 1,As is the amidically bonded residue of a (D)- or (L)-amino acid or of a (D)- or (L)-amino acid derivative from the group consisting of Gly, Ala, Ser, Thr, Asp, Asp(R.sup.5), Glu, Glu(R.sup.5), Gla, Gla(R.sup.5) and Gla(R.sup.5).sub.2, andR.sup.4 and R.sup.5 are each independently of the other the amidically bonded radical of an unsubstituted or carboxy-substituted .omega.-amino-C.sub.2 -C.sub.3 alkanesulfonic acid, are described.Those salts have an immunostimulating action and can be used as medicaments.
Abstract: The invention relates to novel thiosemicarbazonic acid esters of formula I ##STR1## wherein R.sub.1 and R.sub.5 are lower alkyl, lower alk-2-en-1-yl or lower alk-2-yn-l-yl,R.sub.2 and R.sub.3 independently of one another are hydrogen or lower alkyl or together are lower alkylidene, andR.sub.4 is lower alkyl, lower alkoxy, lower alk-2-en-1-yl, lower alk-2-yn-l-yl, aryl-lower alkyl, aryl-lower alkenyl or lower alkoxycarbonyl-lower alkyl, and to the salts and tautomeric compounds and double-bond isomers thereof, to processes for the preparation of the said compounds, to pharmaceutical compositions comprising them and to their use in the treatment of rheumatoid type diseases.
Abstract: The invention relates to a process for the production of cytidine 5'-monophosphosialic acids which comprises reacting a sialic acid with cytidine 5'-triphosphate in the presence of a cell extract of a naturally occurring microorganism having cytidine 5'-monophospho-N-acetylneuraminic acid synthetase activity, the extract optionally having been subjected to one purification step.
Abstract: Described are the use of hexopyranose compounds of the formula I ##STR1## for the prophylaxis and treatment of virus infections, and novel pharmaceutical preparations especially suitable for the use in accordance with the invention.The substituents in formula I have the meanings given in the claims.
Abstract: N-aralkyl- and N-heteroaralkyl-aminoalkanephosphinic acids of formula I ##STR1## wherein R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical having at least 2 carbon atoms,R.sub.1 is hydrogen or hydroxy,R.sub.2 is an araliphatic or heteroarylaliphatic radical substituted by free or functionally modified carboxy that is bonded directly or by way of a spacer, andR.sub.3 is hydrogen, lower alkyl or a group R.sub.2, and the salts thereof have valuable nootropic and anti-epileptic properties and can be used in the preparation of a nootropic or anti-epileptic medicament.
Type:
Grant
Filed:
May 3, 1993
Date of Patent:
July 26, 1994
Assignee:
Ciba-Geigy Corporation
Inventors:
Stuart J. Mickel, Wolfgang Frostl, Pascal Furet
Abstract: Compounds of the formula ##STR1## in which R is alkyl having up to 4 carbon atoms, n has an average value of at least 9, X is a radical of the formula --C(.dbd.O)--(NH--SO.sub.2).sub.m -- in which m is 0 or 1 and, if m is 1, the carhonyl group may be bonded to the oxygen atom or to the nitrogen atom, and each of the radicals A.sub.1, A.sub.2 and A.sub.3, independently of the others, is hydrogen or an acyl radical, and salts of salt-forming compounds of formula I, as well as metal complexes of compounds of formula I, in which A.sub.1, A.sub.2 and A.sub.3 are hydrogen can be used as metal chelators and as auxiliaries in diagnosis.
Abstract: The invention relates to compounds of formula I ##STR1## wherein either R.sub.1 is a radical of formula Ia,--(CH.sub.2).sub.n --O--NH.sub.2 (Ia)in which n is 0 or 1, is hydrogen and R.sub.2 is a radical of formula Ib,--(CH.sub.2).sub.p --O--NH.sub.2 (Ib)in which p is 1 or 2, and wherein R is C.sub.1 -C.sub.2 alkyl which is attached to one carbon atom of the central piperidine ring system, but not to the same carbon atom as R.sub.1 of formula Ia or as R.sub.2 of formula Ib; and m is 1 or 2, and salts thereof. The invention further relates to the preparation of these compounds, to intermediates obtained during their synthesis, to pharmaceutical compositions which contain them, and to the use of said compounds for the therapeutic treatment of the human or animal body and for the preparation of pharmaceutical compositions.The compounds of formula I are inhibitors of ornithin decarboxylase.
Abstract: N-Benzoyl-N'-(2-phenylethyl)-piperazines of formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 have the meanings as defined in the specification, and salts thereof, have analgesic properties and can be used as analgesic active ingredients in medicaments. They are prepared, for example, as follows: a compound of formula II ##STR2## wherein X.sub.1 is carboxy or reactive functionally modified carboxy, or a salt thereof, is reacted with a compound of formula III ##STR3## wherein X.sub.2 is hydrogen.