Abstract: The present invention relates to directly-compressible naproxen or naproxen sodium compositions comprising spray-dried naproxen or naproxen sodium. The present invention further relates the processes for preparing the directly-compressible naproxen or naproxen sodium compositions, to aqueous mixtures containing naproxen or sodium naproxen suitable for spray-drying and useful in the processes for preparing the directly-compressible compositions, to naproxen or naproxen sodium tablets prepared from the directly-compressible compositions, and to the processes for preparing the naproxen or naproxen sodium tablets.
Type:
Grant
Filed:
July 6, 1994
Date of Patent:
November 28, 1995
Assignee:
Syntex Pharmaceuticals International Limited
Inventors:
Roy Kuramoto, Zakauddin T. Chowhan, Ranal O. Pendleton, Hafez Hafezzadeh
Abstract: A unique crystalline polymorphic form of flunisolide is disclosed which is stable in aerosols such as Freon.RTM. mixtures and is valuable in the treatment of respiratory diseases, particularly bronchial asthma and allergic rhinitis.
Type:
Grant
Filed:
September 14, 1981
Date of Patent:
June 12, 1990
Assignee:
Syntex Pharmaceuticals International Limited
Abstract: Pharmaceutically useful optically active .alpha.-arylalkanoic acids or esters, ortho esters, or amides thereof are stereoselectively prepared by contacting an aryl magnesium Grignard reagent with an optically active .alpha.-substituted acyl halide to form the optically active aryl .alpha.-substituted alkyl ketone, which is ketalized and rearranged to the desired optically active .alpha.-arylalkanoic acid or the corresponding ester, ortho ester or amide. In an alternate embodiment, the aryl .alpha.-substituted alkyl ketone is reduced to the corresponding alkanol, which is rearranged to the .alpha.-arylalkanal. The alkanal so produced is converted to the desired optically active .alpha.-arylalkanoic acid by conventional methods.
Type:
Grant
Filed:
May 6, 1988
Date of Patent:
March 27, 1990
Assignee:
Syntex Pharmaceutical International Limited
Abstract: .alpha.-Arylalkanoic acids or esters, orthoesters or amides thereof are prepared by forming an .alpha.-hydroxy ketal or thioketal of an aryl alkyl ketone, activating the .alpha.-hydroxy substituent with an esterifying agent to form the corresponding ketal or thioketal ester substrate, wherein the ester group is sufficiently labile to non-catalytically disassociate from the substrate in a protic or dipolar, aprotic solvent, maintaining the ester substrate in contact with the protic or dipolar, aprotic solvent or mixtures thereof for a time sufficient to form the corresponding .alpha.-arylakanoic acid or ester, orthoester or amide thereof, and optionally concomitantly or sequentially hydrolyzing any ester, orthoester or amide formed to the corresponding .alpha.-arylalkanoic acid.
Type:
Grant
Filed:
June 5, 1985
Date of Patent:
March 31, 1987
Assignee:
Syntex Pharmaceuticals International Limited
Abstract: .alpha.-Arylalkanoic acids or esters, orthoesters or amides thereof are prepared by forming an .alpha.-hydroxy ketal or thioketal of an aryl alkyl ketone, activating the .alpha.-hydroxy substituent with an esterifying agent to form the corresponding ketal or thioketal ester substrate, wherein the ester group is sufficiently labile to non-catalytically disassociate from the substrate in a protic or dipolar, aprotic solvent, maintaining the ester substrate in contact with the protic or dipolar, aprotic solvent or mixtures thereof for a time sufficient to form the corresponding .alpha.-arylakanoic acid or ester, orthoester or amide thereof, and optionally concomitantly or sequentially hydrolyzing any ester, orthoester or amide formed to the corresponding .alpha.-arylalkanoic acid.
Type:
Grant
Filed:
June 7, 1983
Date of Patent:
September 17, 1985
Assignee:
Syntex Pharmaceuticals International Limited
Abstract: A manufacturing method is described for the preparation of optically active 1-aromatic-group-substituted-1-alkanones characterized in that an optically active alkane acid halide is allowed to react with an aromatic compound in the presence of a Lewis acid. The optically active 1-aromatic-group-substituted-1-alkanones are useful intermediates in the preparation of optically active alpha-arylalkanoic acids, which are useful as pharmaceutical, e.g. anti-inflammatory, analgesic and anti-pyretic, agents and as insecticidal agents.
Type:
Grant
Filed:
June 11, 1982
Date of Patent:
September 3, 1985
Assignee:
Syntex Pharmaceuticals International Limited
Inventors:
Gen-Ichi Tsuchihashi, Shuichi Mitamura, Koji Kitajima