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 method of controlling the epimeric distribution in the preparation of 16,17-acetals of pregnane derivatives characterized in reaction of a corresponding 16,17-acetonide with an aldehyde or ketone in (a) hydrocarbon solvent wherein the solubility of the pregnane derivative is less than 1 mg/l or in a halogenated hydrocarbon solvent together with a hydrohalogen acid or an organic sulphonic acid as catalyst and in the presence of small grains of an insert material in the reaction medium or (b) a halogenated hydrocarbon solvent together with a hydrohalogen acid an organic sulphonic acid as catalyst and in the presence of an epimeric distribution modifier.
Type:
Grant
Filed:
September 11, 1987
Date of Patent:
May 15, 1990
Assignee:
Astra Pharmaceutical Production Aktiebolag
Inventors:
Edib Jakupovic, Roy T. Sourander, Jan U. Stenhede, Rolf P. Svensson
Abstract: A compound exhibiting anti-inflammatory properties having the formula ##STR1## in which X is H, Hal or CH.sub.3 COO--; R.sub.1 is CH.sub.3 (CH.sub.2).sub.2 CH--; and R.sub.2 and R.sub.3 are separately H or Hal; and a pharmaceutical composition containing the same.
Type:
Grant
Filed:
January 2, 1987
Date of Patent:
May 30, 1989
Assignee:
Sicor Societa' Italiana Corticosteroidi S.p.A.
Abstract: A process for the preparation of 16,17 acetals of pregnane derivatives by trans-ketalization of 16,17-acetonides is described.In the instance of the preparation of 16.alpha.,17.alpha.-butylidenedioxy-11.beta.,21-dihydroxypregna-1,4-diene- 3,20-dione, a compound having useful therapeutic properties, known also as budesonide, it is possible to obtain the more active epimer with high selectivity and remarkable economic advantages in comparison with the known methods.New 16,17 acetals of pregnane derivatives, which can be prepared by the method of the invention, are also described.
Type:
Grant
Filed:
May 30, 1985
Date of Patent:
September 22, 1987
Assignee:
Sicor Societa Italiana Corticosteroidi S.p.A.
Abstract: Pharmaceutical composition for administration primarily to the respiratory tract when treating and controlling anti-inflammatory conditions comprising liposomes in combination with a compound of the formula ##STR1## and R.sup.1 is a saturated or unsaturated, straight or branched alkyl group with 11-19 carbon atoms and R is H, --COCH.sub.3, --COC.sub.2 H.sub.5, --CO(CH.sub.2).sub.2 CH.sub.3 or --CO(CH.sub.2).sub.3 CH.sub.3.The invention also refers to the compounds of the formula I per se processes for preparation of these compounds and to a method for the treatment of inflammatory conditions.
Type:
Grant
Filed:
July 3, 1985
Date of Patent:
September 15, 1987
Assignee:
Aktiebolaget Draco
Inventors:
Bengt I. Axelsson, Ralph L. Brattsand, Carl M. O. Dahlback, Leif A. Kallstrom, Jan W. Trofast