Abstract: An improved process for preparing the R- and S-isomers of 2-hydroxymethyl-2-octadecyloxymethyl-tetrahydrofuran, a critical step of which involves the preparation of the R- and S-isomers of 2-[3-(1-methoxy-1-methylethoxy)]propyl-oxiranemethanol employing metal-catalyzed Sharpless epoxidation. In addition, the invention relates to the use of the R- and S-isomers of 2-hydroxymethyl-2-octadecyloxymethyl-tetrahydrofuran in preparing stereoisomers of pharmacologically active compounds, and to the R- and S-isomers of 2-[3-(1-methoxy-1-methylethoxy)]-propyl-oxiranemethanol as novel compounds.
Type:
Grant
Filed:
April 2, 1992
Date of Patent:
May 4, 1993
Assignee:
Sandoz Ltd.
Inventors:
Chung-Pin Chen, Prasad K. Kapa, William J. Houlihan
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: 6,7-Di(C.sub.1-4 alkoxy)-1-[3,5-di(C.sub.1-4 alkoxy)phenyl]-3,4-dihydro-3-hydroxy-methyl-isoquinolines, their physiologically hydrolyzable and -acceptable esters and acid addition salts thereof are novel. The said compounds and esters and pharmaceutically acceptable acid addition salts thereof are useful as pharmaceuticals, e.g. in the treatment of asthma.
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 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: 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: The invention discloses the use of the R-(+)-isomer of 2-methoxy-3-octadecyloxy-propanol-(1)-phosphoric acid, monocholine ester in treating multiple sclerosis and to pharmaceutical compositions containing said isomer.
Abstract: invention relates to heterocyclic phospholipids of formula III which are useful in treating multiple sclerosis:where R .sub.2 is n-C.sub.14 -C.sub.20 alkyl;each R.sub.1, independently, is methyl or ethyl; Y is --O-- or --S--;n is an integer 2 to 6.
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: An injectable pharmaceutical mixture comprises:(A) a water-oil emulsion vehicle comprising:(a) about 5 to 25% fatty acid triglycerides;(b) sufficient physiologically acceptable emulsifying agent, e.g. from about 0 to 1.2% egg phosphatides, purified; andthe balance water, with sufficient alkali metal hydroxide added to adjust to an alkaline pH: and(B) an active ingredient which is a PAF receptor inhibitor or anti-tumor agent, which is an ether or carbamoyl phospholipid salt.
Type:
Grant
Filed:
July 19, 1988
Date of Patent:
April 23, 1991
Assignee:
Sandoz Pharmaceuticals Corp.
Inventors:
Dean A. Handley, William J. Houlihan, David B. Weinstein
Abstract: The substituted benzoic acid heterocyclic amides and esters are serotonin M antagonists. Included are compounds of the formula Iq ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, Z' and R.sub.8 ' have various definitions.
Type:
Grant
Filed:
November 4, 1988
Date of Patent:
March 19, 1991
Assignee:
Sandoz Ltd.
Inventors:
Brian P. Richardson, Gunter Engel, Rudolf K. A. Giger, Andrea Vasella
Abstract: The invention relates to novel alkylene oxide-containing amphoteric compounds and to their use as surface active agents. The novel amphoteric compounds are especially useful in the cosmetics and toiletries areas, e.g., as surfactants in shampoo compositions.
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: Compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-4 alkyl; R.sub.2 is hydrogen and R.sub.3 is hydrogen or C.sub.1-4 alkyl, or R.sub.2 and R.sub.3 together represent an additional bond as indicated by the dotted line; R.sub.4 is hydrogen, C.sub.1-4 alkyl or phenyl; R.sub.5 is methoxy or ethoxy; R.sub.6 is hydrogen, hydroxy, C.sub.1-4 alkoxy, hydroxy-(C.sub.2-4 alkoxy) or (C.sub.1-4 alkoxy)-(C.sub.2-4 alkoxy); R.sub.7 and R.sub.8 are each independently C.sub.1-4 alkoxy or (C.sub.1-4 alkoxy)-(C.sub.2-4 alkoxy); and R.sub.9 is hydrogen or halogen,in free form or pharmaceutically acceptable salt form, have pharmaceutical utility, in particular as bronchodilators, eosinophil accumulation and/or activation inhibiting agents and in the treatment of prophylactic treatment of obstructive or inflammatory airways diseases.
Abstract: The invention relates to novel ether sulfates based on a mixture of branched 1-decanols and to their use as surface active agents. The novel ether sulfates are especially useful as the essential surfactant component in shampoo compositions, which compositions exhibit good foaming properties with little or no irritation potential.
Abstract: The invention relates to novel carboxyalkylated derivatives of alkyl and alkenyl catechol ethoxylates and to their use as surface active agents. The novel carboxyalkylated derivatives are especially useful as self-sequestering surfactants in detergent compositions.
Abstract: The uses of piperazinecarboxylic acid in the treatment of disorders characterized by reduced drive and/or social withdrawal, sleep disturbances or migraine.