Abstract: The use, in sequence, of a cytotoxic, but stem cell sparing, agent and granulocyte-macrophage colony stimulating factor as a means to harvest very high numbers of multipotential haemopoietic precursor cells and in reducing the period of myeloid recovery after high dose chemo- or radiotherapy of cancer.
Type:
Grant
Filed:
May 26, 1995
Date of Patent:
July 22, 1997
Assignees:
Sandoz Ltd., Instituto Nazionale Per Lo Studio E La Cura Dei Tumori
Abstract: Somatostatin peptides bearing a chelating group selected from a bifunctional N.sub.4 -chelating group particularly suitable for Tc, Rh, Cu, Co or Re-labelling, and a bifunctional polyamino-polycarboxylic acid chelating group are complexed with a .alpha.-, .beta.-, .gamma.- or positron-emitting nuclide or a nuclide with Auger-e.sup.- -cascades and are useful as radiopharmaceuticals.
Abstract: Salts of the formulaF.sub.n.Awherein F is an anion of a metal-free anionic dye having m acid groupswhereinm is 1 to 4, inclusive,A is a cation of an amine containing 1 to 6 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: Pipecolic acid-containing peptolides wherein the peptidic backbone is of at least 9 .alpha.-amino acid residues joined together by peptide bonds, particularly the compounds of formula I ##STR1## wherein the substituents have various significances, are disclosed. They can be prepared by isolation or derivation from an appropriate microorganism strain such as S 42508/F (NRRL 15761).They have interesting pharmacological, e.g. antifungal, chemotherapeutic drug resistance reversing and to some extent immunosuppressant and antiinflammatory properties.
Type:
Grant
Filed:
May 22, 1995
Date of Patent:
July 1, 1997
Assignee:
Sandoz Ltd.
Inventors:
Michael Morris Dreyfuss, Gerhard Emmer, Maximilian Grassberger, Klaus Ruedi, Hans Tscherter
Abstract: A cyclosporin of the formula ##STR1## wherein A is a residue of the formula ##STR2## wherein R is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy or C.sub.1-3 alkylthio; halo-substituted-C.sub.1-3 alkyl, -C.sub.1-3 alkoxy or -C.sub.1-3 alkylthio; hydroxy-substituted-C.sub.1-3 alkyl, -C.sub.2-3 alkoxy or -C.sub.2-3 alkylthio; or amino or mono- or di-(C.sub.1-2 alkyl)-amino,X is oxygen or sulphur,--x--y-- is --CH.dbd.CH-- (trans) or --CH.sub.2 --CH.sub.2 --,B is -.alpha.Abu-, -Val-, -Thr- or -Nva- andQ is -(D)Ala-; -(D)Ser-; -[O-(2-hydroxyethyl)(D)Ser]-; or -[O-acyl(D)Ser]- or -[O-(2-acyloxy ethyl)(D)Ser]-in which the acyl residue is physiologically hydrolysable and acceptable, are useful in the topical treatment of asthma.
Type:
Grant
Filed:
February 26, 1993
Date of Patent:
July 1, 1997
Assignee:
Sandoz Ltd.
Inventors:
Johann Jakob Boelsterli, Marcel Karl Eberle, Reto Naef, Trevor Glyn Payne
Abstract: The invention relates to a new economical and simple process, using a new intermediate compound, for the production of 3'-substituted 7-amino-3-propenyl-4-cephem-carboxylic acid derivatives of formula ##STR1## wherein R is hydrogen, a negative charge or a silyl protecting group, R.sub.o is hydrogen or methoxy, R.sub.1 is hydrogen or a silyl protecting group and X is the radical of a nucleophile, and their acid addition salts.
Type:
Grant
Filed:
May 5, 1995
Date of Patent:
July 1, 1997
Assignee:
Biochemie Gesellschaft m.b.H.
Inventors:
Johannes Ludescher, Hubert Sturm, Josef Wieser
Abstract: Novel amidine salts of 7-Amino-3-hydroxymethyl-3-cephem-4-carboxylic acid (=HACA), particular guanidine and diaza-bicyclo-alkylene salts, are useful as intermediates in the synthesis of cephalosporins.
Abstract: Compounds of formula I, ##STR1## wherein R.sub.1 to R.sub.4 possess the significances given in the description, may be used in the treatment of senile dementia, Alzheimer's disease and depression.
Abstract: This invention relates to a hard gelatin capsule containing no more than 5 to 10 milligrams of crystalline temazepam and its use in the treatment of transient insomnia.
Abstract: The invention concerns azole compounds of formula ##STR1## wherein the substituents have various significances, in free form or salt form.They can be prepared e.g. by acylation, or by aziridine or oxazole ring opening.The compounds can be used as pharmaceuticals, especially as selective inhibitors of the 25-hydroxyvitamin D3--hydroxylases in the treatment of disorders of proliferation and differentiation in vitamin D--responsive tissues.
Abstract: Process of depleting 7-amino-3-[(E)-2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-carboxylic acid in Z/E mixtures of 7-amino-3-[2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-carboxylic acida) by subjecting an amine salt of a Z/E mixture of 7-amino-3-[2-(4-methyl-5-thiazolyl)vinyl]-3-cephen-4-carboxylic acid to crystallization and converting this amine salt into 7-amino-3-[2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-carboxylic acid, orb) by subjecting the Z/E mixture to chromatography.
Type:
Grant
Filed:
November 16, 1994
Date of Patent:
April 1, 1997
Assignee:
Biochemie Gesellschaft m.b.H.
Inventors:
Johannes Ludescher, Harald Summer, Siegfried Wolf
Abstract: A new process is described for the production of 7-alpha-aminoacyl-cephalosporin free from halogen-containing solvents by acylating 7-amino-ceph-3-em-4-carboxylic acid or a derivative thereof in a halogen-free solvent.
Abstract: The (S)-N-ethyl-3-[(1-dimethylamino)ethyl]-N-methyl-phenylncarbamate in free base or acid addition salt form is useful as pharmaceutical, particularly for systemic transdermal administration.
Abstract: A method for ameliorating or suppressing the acute phase response in a patient receiving IL-6 treatment comprises co-administering with the IL-6 an effective amount of granulocyte colony stimulating factor.
Abstract: A process for etherifying the hydroxymethyl group in position 3 of a cephalosporin by reaction of a 3-hydroxymethyl cephalosporin with an dioxycarbenium-tetrafluoroborate.
Abstract: Compounds of the formula ##STR1## salts thereof, and mixtures of such compounds and salts, wherein D.sub.1 is ##STR2## wherein R.sub.1 is hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, --SO.sub.3 H or --COOH,R.sub.2 is --COOH, --CONR.sub.6 R.sub.7, --SO.sub.2 NR.sub.6 R.sub.7 or --SO.sub.2 --X, wherein each of R.sub.6 and R.sub.7 is independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 -hydroxyalkyl or C.sub.2-4 sulfatoalkyl, or--NR.sub.6 R.sub.7 is a saturated 5- or 6-membered heterocyclic ring containing no hetero atom in addition to the nitrogen atom to which R.sub.6 and R.sub.7 are attached or containing one hetero atom selected from nitrogen and oxygen in addition to said nitrogen atom, which ring is unsubstituted or substituted by 1 to 3 C.sub.1-4 alkyl groups, andm is 0, 1 or 2, andD.sub.2 is ##STR3## wherein R.sub.3 is hydrogen, --SO.sub.3 H or --COOH,R.sub.4 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkyl monosubstituted by hydroxy, halo, cyano, --SO.sub.3 H, --OSO.sub.
Abstract: A process for alkylating the 2'-OH of N.sup.6 -modified adenosine comprising the reacting of an unprotected N.sup.6 -alkyl adenosine with dimethyl sulfate and tetrabutylammonium hydrogen sulfate in a non-polar solvent, preferably dichloromethane, and 5% sodium hydroxide. The products of the reaction are useful as anti-diabetic, hypolipidemic, and analgesic agents.
Abstract: An inhaler for administering powdered medicaments comprising a one-piece, elongate body that has an elongate magazine in a magazine passage extending through the elongate body. The elongate body also has an air inlet, a mouthpiece, and a capsule cutter. The elongate magazine has a plurality of capsule chambers defined in it and spaced along its length, each capsule chamber having an air inlet alignable with the air inlet to the elongate body and an air outlet alignable with the mouthpiece. The magazine is slidable step-wise along the magazine passage to align a capsule chamber with the air inlet to the elongate body, the mouthpiece and the capsule cutter. The capsule cutter, upon activation, pierces both ends of a capsule in the capsule chamber.
Abstract: The present invention provides a pharmaceutical composition for the transdermal systemic administration of an active agent characterized in that the active agent is bopindolol or methysergide. Also the present invention provides a pharmaceutical composition for the transdermal systemic administration of a pharmacologically active agent characterized in that it contains bopindolol, tizanidine, clemastine, ketotifen or methysergide as active agent in a reservoir comprising a hydrophilic polymer. Furthermore a pharmaceutical composition for the transdermal systemic administration of pharmacologically active agents characterized in that the pharmacologically active agent is in a reservoir comprising a polyacrylate polymer containing cationic ester groups.
Type:
Grant
Filed:
September 28, 1994
Date of Patent:
January 14, 1997
Assignee:
Sandoz Ltd.
Inventors:
Thomas Kissel, Henriette Schrank, Hans-Rainer Hoffmann
Abstract: A cephalosporin intermediate of the formula ##STR1## where R.sub.3 is carboxyl, carboxylate, or a carboxylic acid ester group and,R.sub.8 and R.sub.9 are each independently hydrogen, halogen,(C.sub.1-4) alkyl, hydroxy, carboxamido,(C.sub.1-4) alkoxycarbonyl, amino,mono- (C.sub.1-4) alkylamino, di- (C.sub.1-4) alkylamino, ortogether are a 5 or 6-membered carbocyclic ring or an alkali metal, alkaline earth metal, or acid addition salt thereof. Valuable cephalosporin antibiotics can be produced from the cephalosporin intermediate products of formula I.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
December 17, 1996
Assignee:
Biochemie Gesellschaft m.b.h.
Inventors:
Gerd Ascher, Hubert Sturm, Heinrich Thaler, Werner Veit