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 carbonyl 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: Compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and q are as defined in the description, have valuable pharmacological properties and are especially effective as calcium metabolism regulators. They are prepared in a manner known per se.
Abstract: There are described compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or lower alkyl,R.sub.2 is hydrogen, lower alkyl, lower alkoxycarbonyl, phenyl- or naphthyl-lower alkoxycarbonyl, heterocyclylcarbonyl wherein heterocyclyl contains 5 or 6 ring atoms, is saturated and is bonded to the carbonyl group via a ring nitrogen atom and, in addition to the bonding nitrogen atom, contains as ring member one or more further hetero atoms selected from unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted NH, O, S, S.dbd.O and SO.sub.2, or is lower alkanoyl, phenyl- or naphthyl-lower alkanoyl or lower alkanesulfonyl,R.sub.3 is morpholino, thiomorpholino, S-oxothiomorpholino or S,S-dioxothiomorpholino, the heterocyclyl radical in heterocyclylcarbonyl R.sub.2 having the same definition as R.sub.3 or having a definition other than R.sub.3, andR.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, cyano, trifluoromethyl or fluorine, and salts of those compounds where salt-forming groups are present.
Type:
Grant
Filed:
March 25, 1993
Date of Patent:
April 25, 1995
Assignee:
Ciba-Geigy Corporation
Inventors:
Guido Bold, Alexander Fassler, Marc Lang, Peter Schneider
Abstract: Compounds having GABA.sub.B -antagonistic properties, for example those of formula I ##STR1## wherein one of the radicals R.sub.1, R.sub.2 and R.sub.3 is hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another is hydrogen or, in the case of R.sub.1 or R.sub.2, hydroxy or, in the case of R.sub.1, halogen or, in the case of R.sub.2 together with R.sub.2 ', oxo, and the remaining radical is hydrogen, R.sub.1 ' is hydrogen or halogen, R.sub.2 ' is hydrogen, hydroxy or, together with R.sub.2, is oxo, R.sub.4 and R.sub.5 are hydrogen or R.sub.4 is an araliphatic or heteroarylaliphatic radical and R.sub.5 is hydrogen or an aliphatic radical, and R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical having at least 2 carbon atoms or, when R.sub.1 is hydrogen or hydroxy, R.sub.2 is an aromatic radical and R.sub.1 ', R.sub.2 ' and R.sub.
Type:
Grant
Filed:
May 3, 1993
Date of Patent:
April 18, 1995
Assignee:
Ciba-Geigy Corporation
Inventors:
Christian Marescaux, Raymond Bernasconi, Markus Schmutz, Wolfgang Frostl, Stuart J. Mickel
Abstract: Novel thiazoles of formula I ##STR1## wherein R.sub.1 and R.sub.4 are lower alkyl, lower alk-2-en-1-yl or lower alk-2-yn-1-yl,R.sub.2 and R.sub.3 are each independently of the other hydrogen or lower alkyl or together form lower alkylidene, andR.sub.5 and R.sub.6 are each hydrogen or lower alkyl or together form oxo, andR.sub.5 ' and R.sub.6 ' have the same definitions as R.sub.5 and R.sub.6,with the proviso that at least one of the substituent pairs R.sub.5 and R.sub.6 or R.sub.5 ' and R.sub.6 ' together form oxo, and salts thereof, processes for the preparation of the said compounds, pharmaceutical compositions comprising them and the use thereof as medicinal active ingredients.
Abstract: Compounds of the formula ##STR1## in which R.sub.1 is an aliphatic hydrocarbon radical which is unsubstituted or substituted by halogen or hydroxyl, or a cycloaliphatic or araliphatic hydrocarbon radical; X.sub.1 is CO, SO.sub.2, or --O--C(.dbd.O)-- with the carbon atom of the carbonyl group being attached to the nitrogen atom shown in formula I; X.sub.2 is a divalent aliphatic hydrocarbon radical which is unsubstituted or substituted by hydroxyl, carboxyl, amino, guanidino or a cycloaliphatic or aromatic radical, or is a divalent cycloaliphatic hydrocarbon radical, it being possible for a carbon atom of the aliphatic hydrocarbon radical to be additionally bridged by a divalent aliphatic hydrocarbon radical; R.sub.2 is carboxyl which, if desired, is esterified or amidated, substituted or unsubstituted amino, formyl which, if desired, is acetalized, 1H-tetrazol-5-yl, pyridyl, hydroxyl which, if desired, is etherified, S(O).sub.
Type:
Grant
Filed:
December 29, 1992
Date of Patent:
March 21, 1995
Assignee:
Ciba-Geigy Corp
Inventors:
Peter Buhlmayer, Franz Ostermayer, Tibur Schmidlin
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: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.
Type:
Grant
Filed:
March 28, 1994
Date of Patent:
March 7, 1995
Assignee:
Ciba-Geigy Corporation
Inventors:
Jaroslav Stanek, Jorg Frei, Giorgio Caravatti
Abstract: The invention relates to a pharmaceutical composition in the form of a sterilizable parenteral solution comprising a diclofenac salt and stabilizers, such as ethyl lactate combined with glutathione or N-acetylcysteine.
Abstract: The invention relates to a novel process for the manufacture of (3R,1'R)-4-acyloxy-3-(1'-hydroxyethyl)-2-azetidinones of formula ##STR1## in which R.sup.1 represents lower alkyl or aryl, by enantioselective reduction of the carbonyl group in a suitable .alpha.-acylaminomethyl-acetoacetic acid ester, cyclization of the resulting .alpha.-acylaminomethyl-.beta.-hydroxybutyric acid ester to a 5,6-dihydro-1,3,4H-oxazine with inversion of the carbon atom carrying the hydroxy group, equilibration to form the preferred trans-substituted dihydrooxazine, recleaving to form the configuratively uniform .alpha.-aminomethyl-.beta.-hydroxybutyric acid, ring-closure to form the .beta.-lactam and oxidative acylation at C(4) of the .beta.-lactam. Compounds of formula I can be used as starting materials for the manufacture of .beta.-lactam antibiotics. The invention relates also to novel intermediates.
Abstract: Aminoalkylphenyl derivatives of formula I ##STR1## wherein alk, R.sub.1 -R.sub.6, X and Y are as defined in the description, and salts thereof, exhibit properties inhibiting the biosynthesis of interleukin-1 (IL-1) and analgesic properties and can therefore be used as active ingredients in medicaments. They are prepared in a manner known per se.
Abstract: A tetrahydropyran-4-yloxy-alkanoic acid of formula III ##STR1## wherein R.sub.2 is hydrogen or C.sub.1-4 alkyl and R.sub.3 is hydrogen or C.sub.1-4 alkyl.
Abstract: The invention relates to novel aromatic acids, especially to compounds of formula ##STR1## wherein R.sub.1 is lower alkyl, R.sub.2 is lower alkyl, R.sub.3 is hydrogen, carboxy or sulfo, R.sub.4 is carboxy or sulfo, G is an unsubstituted or substituted 1,4-phenylene group or an unsubstituted or substituted 1,4-naphthylene group, and wherein either R.sub.5 and R.sub.6 together are an additional bond and L is an oxygen or sulfur atom or wherein R.sub.5 is hydrogen, R.sub.6 is halomethyl and L is an oxygen atom, and salts thereof, to the use of compounds I and their salts, to a process for the preparation of compounds I and their salts, to starting materials used in that preparation process, and salts thereof, to a process for the preparation of those starting materials and their salts, to a device in which the compounds I and their salts are used, and to a process in which that device is used.
Abstract: Substituted dialkylthio ethers of formula I ##STR1## wherein R.sub.1 -R.sub.6, alk, X and Y are as defined in the description, and salts thereof, exhibit properties inhibiting the biosynthesis of interleukin-1 (IL-1) and analgesic properties and can therefore be used as active ingredients in medicaments. They are prepared in a manner known per se.
Abstract: Compounds of formula I ##STR1## wherein Z, X, R, R.sub.0, R.sub.1, R.sub.2 and R.sub.3 are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.
Abstract: Compounds of the formula ##STR1## wherein carbon atoms 1 and 2 are linked by a single bond or a double bond, R.sub.1 is hydrogen, methyl or ethyl, and A is a group of the formula --N(--R.sub.2)--X-- wherein R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl and X is C.sub.1 -C.sub.12 alkylene or C.sub.3 -C.sub.6 cycloalkylidene; a group of the formula --N(--R.sub.2)--Y--Phe-- wherein R.sub.2 is as defined above, Y is a direct bond or C.sub.1 -C.sub.6 -alkylene and Phe is an unsubstituted or substituted phenylene radical; a group of the formula --O--X-- wherein X is as defined above, or a group --O--Y--Phe-- wherein Y and Phe are as defined above, are inhibitors of 5.alpha.-reductase and can be used for the therapeutic treatment of the human and animal body.
Abstract: Novel imidazoles of formula I ##STR1## wherein R.sub.1 and R.sub.4 are lower alkyl, lower alk-2-en-1-yl or lower alk-2-yn-1-yl,R.sub.2 and R.sub.3 are each independently of the other hydrogen or lower alkyl or together form lower alkylidene, andR.sub.5 and R.sub.6 are each hydrogen or lower alkyl or together form oxo, andR.sub.5 ' and R.sub.6 ' have the same definitions as R.sub.5 and R.sub.6,with the proviso that at least one of the substituent pairs R.sub.5 and R.sub.6 or R.sub.5 ' and R.sub.6 ' together form oxo, and salts thereof, processes for the preparation of the said compounds, pharmaceutical compositions comprising them and the use thereof as medicinal active ingredients.
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: Compounds of formula I ##STR1## wherein Z, R, R.sub.1, R.sub.2 and X are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.
Type:
Grant
Filed:
March 17, 1993
Date of Patent:
December 27, 1994
Assignee:
Ciba-Geigy Corp.
Inventors:
Marc Lang, Edmond Differding, Jaroslav Stanek
Abstract: Compounds of formula I ##STR1## wherein A, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Y, Z and R.sub.1 to R.sub.6 have the meanings given in the description, have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.
Type:
Grant
Filed:
May 7, 1993
Date of Patent:
December 27, 1994
Assignee:
Ciba-Geigy Corporation
Inventors:
Jaroslav Stanek, Giorgio Caravatti, Jorg Frei, Hans-Georg Capraro