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4812573 Pharmaceutically active compounds
viii
New Patents
Heterocyclic dihydroxyquinoxaline compounds having the formula See Patent for Chemical Structure wherein R I is halogen, CN, CF3, ethynyl, or N3 and R2 is SO2C1-3-alkyl, CF3, NO2, ethynyl, or CN. The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use. The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.
prepared e.g. by reacting a solution in an organic solvent of L-carnitine whose carboxyl group is protected with an N-protected aminoacid in the presence of a condensing agent and then removing the aminoacid and carnitine protecting groups, thus obtaining the desired compound.
4812472
Graham Durant, Andrew D Gribble, Robert A Slater, Plymouth, United Kingdom assigned to SmithKline & French Laboratories Ltd
ISOXAZOLE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM FOR TREATMENT AND PROPHYLAXIS OF RETROVIRUSES DISEASES Dieter Binder, Fran Rovenszky, Vienna, Austria assigned to Chemie Linz Akteingesellschaft Substituted isoxazole derivatives of the formula See Patent for Chemical Structure I in which RI denotes lower alkyl, n denotes the integer 6, 7 or 8, A denotes a group of the formula See Patent for Chemical Structure and R2 denotes hydrogen, methyl, chlorine or bromine. The novel compounds have a pronounced antiviral action and can be employed for the treatment and prophylaxis of virus diseases.
4812478 DERIVATIVES OF L-AMINO ACYL L-CARNITINE, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS HAVING HEPATOPROTECTING ACTIVITY CONTAINING SAME Maria O Tinti, Carlo A Bagolini, Domenic Misiti, Carlo Scolastico, Rome, Italy assigned to Sigma-Tau Industrie Farmaceutiche Riunite S p A L-aminoacyl derivatives of L-carnitine of general formula (I) See Patent for Chemical Structure (I) wherein R is an alkyl radical selected from lmethyl-propyl, isobutyl, isopropyl, mercaptomethyl and 3-guanidino propyl, and their pharmacologically acceptable salts, are
4812573 PHARMACEUTICALLY COMPOUNDS
ACTIVE
The invention relates to a class of tetrahydroisoquinolinylalkanoic acids containing an aryl sulphonamide group which have activity as thromboxane A2 antagonists.
4814184 PHARMACEUTICAL DELIVERY DEVICE HAVING A SILOXANE POLYMER MATRIX Louis M J Aguadisch, Frank S Rankin, Valbonne, France assigned to Dow Corning Ltd Improved pharmaceutical delivery devices which can deliver hydrophilic or polar pharmaceutically active materials, as well as optionally hydrophobic or non-polar materials, have small particles with on average a diameter below 20 microns of a drug component comprising the hydrophilic or polar pharmaceutically active material, dispersed in a silicone matrix. These devices are produced by using certain organopolysiloxane-polyoxyalkylene copolymers. Preferably an emulsion of the drug component in a silicone containing composition is made before curing the composition to an elastomer.
4814326 PHARMACEUTICAL COMPOSITIONS BASED ON DIPHOSPHONATES FOR THE TREATMENT OF ARTHROSIS AND OSTEOARTHRITIS Sergio Rosini, Luciano Fontanelli, Pisa, Italy assigned to Istituto Gentili S p A
New Patents
Heterocyclic dihydroxyquinoxaline compounds having the formula See Patent for Chemical Structure wherein R I is halogen, CN, CF3, ethynyl, or N3 and R2 is SO2C1-3-alkyl, CF3, NO2, ethynyl, or CN. The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use. The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.
prepared e.g. by reacting a solution in an organic solvent of L-carnitine whose carboxyl group is protected with an N-protected aminoacid in the presence of a condensing agent and then removing the aminoacid and carnitine protecting groups, thus obtaining the desired compound.
4812472
Graham Durant, Andrew D Gribble, Robert A Slater, Plymouth, United Kingdom assigned to SmithKline & French Laboratories Ltd
ISOXAZOLE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM FOR TREATMENT AND PROPHYLAXIS OF RETROVIRUSES DISEASES Dieter Binder, Fran Rovenszky, Vienna, Austria assigned to Chemie Linz Akteingesellschaft Substituted isoxazole derivatives of the formula See Patent for Chemical Structure I in which RI denotes lower alkyl, n denotes the integer 6, 7 or 8, A denotes a group of the formula See Patent for Chemical Structure and R2 denotes hydrogen, methyl, chlorine or bromine. The novel compounds have a pronounced antiviral action and can be employed for the treatment and prophylaxis of virus diseases.
4812478 DERIVATIVES OF L-AMINO ACYL L-CARNITINE, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS HAVING HEPATOPROTECTING ACTIVITY CONTAINING SAME Maria O Tinti, Carlo A Bagolini, Domenic Misiti, Carlo Scolastico, Rome, Italy assigned to Sigma-Tau Industrie Farmaceutiche Riunite S p A L-aminoacyl derivatives of L-carnitine of general formula (I) See Patent for Chemical Structure (I) wherein R is an alkyl radical selected from lmethyl-propyl, isobutyl, isopropyl, mercaptomethyl and 3-guanidino propyl, and their pharmacologically acceptable salts, are
4812573 PHARMACEUTICALLY COMPOUNDS
ACTIVE
The invention relates to a class of tetrahydroisoquinolinylalkanoic acids containing an aryl sulphonamide group which have activity as thromboxane A2 antagonists.
4814184 PHARMACEUTICAL DELIVERY DEVICE HAVING A SILOXANE POLYMER MATRIX Louis M J Aguadisch, Frank S Rankin, Valbonne, France assigned to Dow Corning Ltd Improved pharmaceutical delivery devices which can deliver hydrophilic or polar pharmaceutically active materials, as well as optionally hydrophobic or non-polar materials, have small particles with on average a diameter below 20 microns of a drug component comprising the hydrophilic or polar pharmaceutically active material, dispersed in a silicone matrix. These devices are produced by using certain organopolysiloxane-polyoxyalkylene copolymers. Preferably an emulsion of the drug component in a silicone containing composition is made before curing the composition to an elastomer.
4814326 PHARMACEUTICAL COMPOSITIONS BASED ON DIPHOSPHONATES FOR THE TREATMENT OF ARTHROSIS AND OSTEOARTHRITIS Sergio Rosini, Luciano Fontanelli, Pisa, Italy assigned to Istituto Gentili S p A