Abstract: Fiber-reactive compounds of the formulaX-O.sub.2 S-W.sub.1 [F.sub.c ]W.sub.2 -NR-Z,and water-soluble salts thereof each cation of which is independently a non-chromophoric cation, and mixtures of such compounds or water-soluble salts,whereinFc is a chromophore-containing radical of a monoazo, disazo, polyazo, formazan, anthraquinone, dioxazine, phenazine or azomethine dye, which is in metal-free or metal complex form,each of W.sub.1 and W.sub.2 is independently a direct bond or a bridging group which is attached to a carbon atom of an aromatic carbocyclic ring or to a carbon or nitrogen atom of an aromatic heterocyclic ring present in F.sub.c,X is --CH.dbd.CH.sub.2 or --C.sub.2-4 alkylene--Y, wherein Y is hydroxy or a group which can be split off under alkaline conditions,R is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkyl monosubstituted by hydroxy, halo, cyano, --SO.sub.3 H, --OSO.sub.3 H or --COOH, andZ is ##STR1## with the provisos as set forth herein.
Type:
Grant
Filed:
June 16, 1992
Date of Patent:
June 18, 1996
Assignee:
Sandoz Ltd.
Inventors:
Gunther Auerbach, Markus Dorr, Paul Doswald, Markus Gisler, Werner Koch, Helmut A. Moser, Roland Wald
Abstract: Cyclosporins wherein the residue at the 1-position (typically -MeBmt- or -dihydro-MeBmt-) is 3'O-acylated or 3'-oxo or -C.sub.1-4 alkoxyimino substituted, or wherein the residue at the 2-position is .beta.-O-acyl or .beta.-oxo substituted, or wherein the residue at the 2-position is -Ile-, or wherein the residue at the 11-position is -MeAls-, -MeIle- or -MealloIle- as well as various naturally occurring cyclosporins/dihydro-derivatives thereof, are useful in reversing resistance to chemotherapy, in particular resistance to cytostatic or anti-neoplastic therapy. Various of these cyclosporins and intermediates for their production are novel. Intermediates wherein the residue (e.g. -MeBmt-, -dihydro-MeBmt- etc.) at the 1-position is 8'-alkoxy or 7'-desmethyl-7'-hydrocarbyl substituted are novel and useful as immunosuppressants, anti-inflammatory and anti-parasitic agents.
Type:
Grant
Filed:
November 10, 1994
Date of Patent:
June 11, 1996
Assignee:
Sandoz Ltd.
Inventors:
Pietro Bollinger, Johann J. Bolsterli, Trevor G. Payne
Abstract: The invention provides use of a 5HT-3 antagonist in the manufacture of a medicament suitable for the prevention or reduction of dependence on a dependence-inducing agent.
Abstract: Compounds of the formula ##STR1## where X.sub.1 and X.sub.2 are independently O or S, andR.sub.1 is as defined in the descriptionR.sub.2, R.sub.3, and R.sub.4 are each independently straight orbranched chain (C.sub.1-4)alkyl, and pharmaceutically acceptable salts, physiological hydrolysable esters, and pro-drug forms thereof are useful as hypoglycemic agents.
Type:
Grant
Filed:
January 17, 1995
Date of Patent:
May 14, 1996
Assignee:
Sandoz Ltd.
Inventors:
Robert C. Anderson, James D. Fraser, Howard C. Smith, Jeffrey W. Hughes, Edwin B. Villhauer, Gregory R. Bebernitz
Abstract: The invention concerns the compounds of formulae ##STR1## wherein the substituents have various significances. They can be prepared by various methods, e.g. acylation, reduction, alkylation, etc. They are indicated for use as pharmaceuticals, in particular as immunosuppressant, antiproliferative and antiinflammatory agents.
Abstract: Salts of the formulaF.sub.n .multidot.A,wherein F is an anion of a metal-free anionic dye having m acid groupswherein m is 1 to 4, inclusive,A is a cation of an amine containing 1 to 4 sterically hindered amine groups, andn is 1 or 2,with the proviso that the salt contains 1 to n.times.m groups selected from ammonium and immonium groups, useful as pigments, particularly for the coloring of solvent-free and solvent-containing plastic materials, lacquers and printing inks.
Abstract: Compounds of formulaA--X--Y--NH--Bwherein A is derived from optionally substituted benzothiophene, indole, 4-aza-and 7-aza-benzothiophene or-indole, A bearing in position 5 hydrogen, halogen, optionally substituted alkyl, hydroxy, nitro, amino, alkylamino, acylamino, alkoxycarbonyl, sulfamoyl, cyano, trimethylsilyl, carboxy, carbamoyl, phosphate, oxycarbamoyl, heterocyclic radical or ether or ester group, X-Y is --CR.sub.8 .dbd.N-- or CH(R.sub.8)--NH-- wherein R.sub.8 is -H or alkyl and attached at position 3 of A, and B is a heterocyclic radical or a residue ##STR1## wherein R.sub.10 is H, optionally substituted alkyl, cycloalkyl, aryl, adamantyl, acyl or carbamoyl and X.sub.2 is alkylthio or NR.sub.3 R.sub.10 wherein R.sub.3 is H or alkyl or R.sub.3 and R.sub.10 together with the nitrogen atom to which they are attached form a heterocyclic radical, in free form or in salt form, have pharmacological activity, e.g. for treating gastrointestinal disorders.
Abstract: A process for preparing carboxylates of polyoxyalkylene siloxanes and -amines, alkylpolyoxyalkylenes, polyoxyalkylene block polymers, alkylamidepolyoxyalkylenes and alkylpolyglucosides comprising subjecting a primary hydroxyl group-containing polyoxyalkylene compound or alkylpolyglucoside to mild oxidiation. The invention also relates to the novel polyoxyalkylene amine and alkylamidepolyoxyalkylene carboxylates prepared by the process.
Type:
Grant
Filed:
June 30, 1994
Date of Patent:
April 2, 1996
Assignee:
Sandoz Ltd.
Inventors:
Parfait J. Likibi, Robert V. Casciani, Gregory L. McCraw
Abstract: The invention concerns the compounds of formula I ##STR1## wherein the substituents have various significances, in free form and, where such forms exist, in salt form.They can be prepared by various processes, e.g. by irradiation; oxidation; elimination; reduction; conversion by e.g. halogenation or acylation; deprotection of protected hydroxy groups; protection of free hydroxy groups; and separation of stereoisomeric mixtures into individual isomers.They are useful as pharmaceuticals, especially as antiinflammatory, and as antiproliferative and antiinflammatory agents.
Abstract: The invention concerns the compounds of formula I ##STR1## wherein the substituents have various significances, in free form and, where such forms exist, in salt form. The compounds have potent antihyperproliferative/antiinflammatory and anticancer activity.
Abstract: Compound of formula IVe ##STR1## where Het is 2-pyridyl or 2-benzothiazolyl, are useful as acylating agents in preparing 7-[2-(2-amino-4-thiazol)-2-oxoacetyl]-cephalosporin intermediates.
Type:
Grant
Filed:
April 30, 1993
Date of Patent:
January 16, 1996
Assignee:
Biochemie Gesellschaft m.b.H.
Inventors:
Hubert Sturm, Heinrich Thaler, Werner Veit
Abstract: Compounds of the formula ##STR1## wherein each R.sub.1 is independently hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or nitro,R.sub.2 is hydrogen or halo,R.sub.3 is halo, andMe is a divalent metal,useful for pigmenting polymeric materials such as polyethylene, polyvinyl chloride, polystyrene, natural rubber and synthetic rubber, for the mass pigmentation of materials such as cellulose acetate and for pigmenting paper, lacquers, paints, printing inks and textile coatings.
Abstract: Somatostatin analogues and derivatives in free form or in pharmaceutically acceptable salt or complex form are useful for preventing or reducing neointimal proleferation following angioplasty.
Abstract: Novel capsaicin derivatives of general formula I ##STR1## wherein R, R.sub.1 to R.sub.7 and X may be a variety of substituents, processes for the production thereof, pharmaceutical compositions containing them and use thereof as pharmaceuticals.
Type:
Grant
Filed:
February 14, 1994
Date of Patent:
April 4, 1995
Assignee:
Sandoz Ltd.
Inventors:
Derek J. Reid, Christopher S. J. Walpole, Roger Wrigglesworth
Abstract: Complexes of the formula ##STR1## which are in free acid or salt form, and mixtures thereof, wherein each ofR.sub.1 and R.sub.3 is independently hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkyl monosubstituted by hydroxy, amino, sulfo or carboxy,each ofR.sub.2 and R.sub.4 is independently hydrogen; C.sub.1-4 alkyl; C.sub.1-4 alkyl monosubstituted by hydroxy, amino, sulfo or carboxy; --COR.sub.5 ; --COOR.sub.6 or --CONHR.sub.7,M is chromium or cobalt, andM.sub.K.sup..sym. is hydrogen or a non-chromophoric cation, useful for dyeing or printing, materials such as natural and synthetic polyamides and particularly artificially produced oxide layers on aluminum and aluminum alloys.
Abstract: The invention relates to a new, economical and simple process for the production of 3-vinylcephalosporin compounds of formula ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and denote hydrogen or an organic radical.
Type:
Grant
Filed:
May 28, 1993
Date of Patent:
March 28, 1995
Assignee:
Sandoz Ltd.
Inventors:
Gerd Ascher, Johannes Ludescher, Hubert Sturm
Abstract: Compounds of the formula ##STR1## wherein D is the residue of a metal-free azo dye free of fiber-reactive groups and containing 2 to 4 sulfo groups,D' is the residue of a metal-free azo dye free of fiber-reactive groups and containing 2 to 4 sulfo groups, with the proviso that D and D' are different,each R.sub.1 is independently hydrogen or C.sub.1-4 alkyl,each of R.sub.2 and R.sub.3 is independently hydrogen, C.sub.1-4 -alkyl or 2-, 3- or 4-hydroxy(C.sub.2-4 alkyl),X is linear or branched C.sub.2-10 alkylene or linear or branched C.sub.3-10 alkylene monosubstituted or disubstituted by hydroxy which optionally contains one or two radicals selected from --O-- and --NRa--, wherein Ra is hydrogen or C.sub.
Abstract: Polypeptide compositions for inter alia SMS are provided containing a monosaccharide/sugar alcohol and/or a polyoxyalkylene ether having enhanced resorption properties for oral or rectal administration.
Type:
Grant
Filed:
January 25, 1993
Date of Patent:
February 28, 1995
Assignee:
Sandoz, Ltd.
Inventors:
Jacky Vonderscher, Joachim Franz, Michel Steiger, Karl Hornung
Abstract: Compounds of the formula ##STR1## wherein R is hydrogen; C.sub.1-8 alkyl; C.sub.2-8 alkenyl; C.sub.3-8 alkadienyl; C.sub.2-8 alkynyl; C.sub.4-8 alkadiynyl; C.sub.2-10 (alkoxyalkyl); C.sub.2.sub.2-10 (alkylthioalkyl); C.sub.3-8 cycloalkyl and C.sub.4-12 (cycloalkylalkyl); optionally substituted by 1 to 6 halos,R.sup.1 is hydrogen or C.sub.1-8 alkyl,R.sup.2 is hydrogen, C.sub.1-8 alkyl or halo,R.sup.3 is ##STR2## wherein each R.sup.5 and R.sup.6, are independently hydrogen, halo, C.sub.1-8 alkyl, optionally substituted by 1 to 6 halos, C.sub.1-8 alkoxy, C.sub.1-8 alkylthio or nitro,W is --O--, --S--, --NR.sup.4 -- or --CO--,W.sup.1 is --O--, --S--, --SO--, --SO.sub.2 --, --NR.sup.4 -- or --CO--,X is --O--, --S--, --NR.sup.4 -- or ##STR3## wherein R.sup.1 is hydrogen or C.sub.1-8 alkyl,Z is hydrogen, C.sub.1-8 alkyl optionally substituted by 1 to 6 halos,m is 0 or 1,m' is 0 or 1, andn is 0, 1 or 2,wherein each R.sup.4 is independently hydrogen or C.sub.1-8 alkyl, said compounds are useful as pesticides, i.e.