Sandoz Gmbh

Sandoz Pharmaceuticals Corp.

Sandoz Pharm. Corp.

Other

William J Houlihan

Jeffrey Nadelson

Goetz E Hardtmann

George A Cooke

Prasad Koteswara Kapa

Jerome Linder

Seung H Cheon

Robert E Manning

Joseph A Smith

Dietmar A Habeck

Paul G Mattner

Russell L Underwood

Heinrich Estermann

John Charles Tomesch

Paul L Anderson

Robert V Coombs

Dean A Handley

Robert C Anderson

Mark L Lee

Robert S Ho

Ronald G Babington

Howard C Smith

F Eugene Harrington

Chung-Pin Chen

David B Weinstein

Rudolf K Giger

Mahavir Prashad

Edwin B Villhauer

A process for preparing the (R) stereoisomer of 2,2-bis(hydroxmethyl)-tetrahydrofuran monobutyrate comprising subjecting the dibutyric ester of the 2,2-bis(hydroxymethyl)-tetrahydrofuran to enzymatic hydrolysis. The invention also relates to the novel (R) stereoisomer prepared by the instant process and to its more stable forms. In addition, the invention relates to the use of the (R) stereoisomer in preparing stereoisomers of pharmacologically active compounds and to certain specific stereoisomers produced thereby.

Use of the (R) isomer of

The invention discloses certain heterocyclic, thioether, keto-ester and alkyl phospholipids, e.g., heterocyclic phospholipids having the formula ##STR1## where R is n-C.sub.14 -C.sub.20 alkyl or O-n-C.sub.14 -C.sub.20 alkyl; each R.sub.1 is methyl or ethyl; n is 2-6; and X is --CH.sub.2 --m, where m is 2-4, CH.sub.2 CH.sub.2 O or CH.sub.2 CH.sub.2 S, or a corresponding hydrate thereof, which compounds are useful in treating multiple sclerosis.

Heterocyclic phospholipids useful in treating multiple sclerosis

Process for the preparation of the (R) stereoisomer of the monobutyric

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.

Process for preparing the R- and S-isomers of

The invention discloses certain thioether, keto-ester and alkyl phospholipids which are useful in treating multiple sclerosis.

Thioether, keto-ester and alkyl phospholipids useful in treating

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.

5-Aryl-substituted-2,3-dihydro-imidazo(1,2-a)furo- and thieno pyridines

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.

Use of the R-(+)-isomer of

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;

An injectable pharmaceutical mixture comprises:

Triglyceride-water emulsion pharmaceutical vehicles

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.

5-aryl-substituted-2,3-dihydro-imidazo[1,2-a]furo- and thieno pyridines

The invention discloses certain 2- or 4-substituted-[2-(1H-imidazol-1-yl)ethyl]piperidines useful as anti-tumor agents, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions in treating tumors.

2- or 4-substituted-[2-(1H-imidazol-1-yl)ethyl]piperidines

The invention discloses certain 6-aryl-substituted-4H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,4]diazepines useful as PAF inhibitors, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-induced blood platelet aggregation, PAF-mediated bronchoconstriction and extravasation, PAF-induced hypotension, PAF-induced ischemic bowel disease and PAF-mediated, endotoxin induced lung injury, for controlling hyperreactive airways and for protecting against endotoxin-induced hypotension and death.

6-aryl-substituted-4H-thieno(2,3-e)(1,2,4)triazolo(3,4-c)(1,4)diazepines

The invention discloses certain 5-hetero or aryl-substituted-imidazo[2,1-a]isoquinolines useful as platelet activating factor (PAF) receptor antagonists, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-mediated bronchoconstriction and extravassation and PAF-mediated, endotoxin-induced lung injury, and for controlling hyperreactive airways induced by PAF or allergin. In addition, the invention discloses the use of a select group of said compounds as anti-tumor agents.

5-hetero-or aryl-substituted-imidazo(2,1-a)isoquinolines and their use

An improved process for preparing monoalkylcarbamate group-containing compounds comprising reacting a hydroxy group-containing compound with an organic halide and an alkali metal cyanate in the conjoint presence of a phase transfer catalyst and a solvent.

Process for the preparation of monoalkylcarbamate group-containing

The invention discloses certain diaryl substituted cyclopentane and cyclopentene derivatives useful as PAF inhibitors, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-induced blood platelet aggregation, PAF-mediated broncho-constriction and extravasation, PAF-induced hypotension, PAF-induced ischemic bowel disease and PAF-mediated, endotoxin induced lug injury.

Growing community of inventors

Mountain Lakes, NJ, United States of America

William J Houlihan