Abstract: Optically active naphthyl alpha-substituted alkyl ketones, are a class of ketones useful as intermediates in the production of optically active alpha-naphthylalkanoic acids which exhibit anti-inflammatory, analgesic and anti-pyretic activity.
Type:
Grant
Filed:
April 29, 1992
Date of Patent:
May 11, 1993
Assignee:
Syntex Pharmaceuticals International Ltd.
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: A process for preparing compounds represented by the formula ##STR1## wherein: X is hydrogen or lower alkoxy;Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl);n is an integer from 2-4;R.sub.2 is hydrogen or methyl; andR.sub.3 is linear or branched alkyl, ##STR2## --(CH.sub.2).sub.m -phenyl or --CH.sub.2 O-phenyl; in which any phenyl may be optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen, anda is an integer of 0, 1 or 2;b is an integer of 3-7;m is an integer of 0, 1 or 2,as a mixture or separately in a sequence starting from an epoxide represented by the formula ##STR3## and processes for making the novel intermediates.
Abstract: Novel 13,14-dihydroprostaglandin derivatives of the formula ##STR1## wherein: m is 1 or 3;R.sub.1 is hydrogen or alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 and R.sub.4 are independently hydrogen or methyl;R.sub.5 is alkyl, CF.sub.3 (CH.sub.2).sub.n -- in which n is an integer of 3-5, cycloalkyl, or optionally substituted phenyl, benzyl or phenoxy; orR.sub.4 and R.sub.5 taken together with the carbon to which they are attached is cycloalkyl of 4-8 carbon atoms;X is cis --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 -- when m is 3, orX is --CH.sub.2 CH.dbd.C.dbd.CH-- when m is 1;and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta.;or a pharmaceutically acceptable salt thereof,have been prepared. They are useful in particular for their antihypertensive and anti-ulcerogenic properties.
Type:
Grant
Filed:
August 25, 1988
Date of Patent:
December 19, 1989
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Joan Huguet, Joseph M. Muchowski, Maria T. Lara
Abstract: The invention concerns a method of inhibiting thromboxane synthetase with a compound of the formula: ##STR1## or a pharmaceutically acceptable salt or ester thereof, in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclinthromboxane levels.
Abstract: Compounds useful as antiviral agents are depicted in the formula: ##STR1## wherein: X is oxygen or NH, Y is hydrogen, iodo, fluoro, methyl or trifluoromethyl, Z is hydrogen or fluoro and Z' is fluoro; and the wavy line indicates that the group may be above or below the plane of the ring; and the pharmaceutically acceptable acid addition salts thereof.
Type:
Grant
Filed:
April 14, 1986
Date of Patent:
November 3, 1987
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Julien P. H. Verheyden, John C. Martin, G. V. Bindu Madhavan, Daniel P. C. McGee, Ernest J. Prisbe
Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein:n is an integer equal to 0, 1, 2 or 3;R.sup.1 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenyl lower alkyl;each R is independently hydrogen, lower alkyl, optionally substituted phenyl, or optionally substituted phenyl lower alkyl;are .alpha..sub.2 blockers, and, therefore, are useful in treating essential hypertension and depression, and in inhibiting platelet aggregation.
Type:
Grant
Filed:
August 3, 1981
Date of Patent:
March 13, 1984
Inventors:
Arthur F. Kluge, Arthur M. Strosberg, Roger L. Whiting, George A. Christie