Abstract: The present invention is concerned with 11-aryloestrane and 11-arylpregnane derivatives, characterized in that these derivatives have the following structure: ##STR1## wherein R.sub.1 is an aryl group with an ##STR2## group as substituent,X and Y each being separately H or a (1-4 C) hydrocarbon radical or together a (2-6 C) hydrocarbon radical;R.sub.2 is an alkyl group containing 1-4 carbon atoms;R.sub.3 is H, OH, a saturated or unsaturated hydrocarbon radical containing 1-8 carbon atoms, at least provided with a hydroxyl, oxo, halogen, azido or nitrile group; an acyloxy or an alkoxy group;R.sub.4 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally provided with a hydroxyl, alkoxy, acyloxy or halogen group; or R.sub.3 and R.sub.4 together form a ring system; andR.sub.5 is a hydrocarbon group containing 1-4 carbon atoms, and further with processes for the preparation of these compounds and with pharmaceutical preparations comprising these compounds.
Abstract: The present invention relates to ophthalmic compositions and their preparation and use. More specifically, the invention relates to ophthalmic compositions useful in the treatment of surface disorders of the eye caused by abnormal precorneal tear film, and most specifically to the compositions for treatment of so-called dry eye conditions.
Type:
Grant
Filed:
August 10, 1987
Date of Patent:
September 12, 1989
Assignee:
Spectra Pharmaceutical Services, Inc.
Inventors:
A. Edward Maumenee, Richard L. Giovanoni
Abstract: This invention relates to antiviral organic steroid compositions and derivatives thereof; a process of producing the antiviral compositions; and a method for inhibiting viruses utilizing the compositions. More particularly, the compositions are derived from fireflies of the genus, Photinus.
Abstract: A pharmaceutical composition, having utility as a diuretic or aldosterone antagonist, comprising spironolactone and an aqueous homogenizingly effective amount of a material selected from the group consisting of (i) sodium carboxymethylcellulose, and (ii) a mixture of methylcellulose and a dimethylpolysiloxane polymer.Also disclosed is a method of diuretic or hyperaldosteronism treatment by administration of such composition, e.g., by oral administration.
Abstract: Novel 10-substituted steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 8 carbon atoms, alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 8 carbon atoms, aryl and substituted aryl, aralkyl and substituted aralkyl, protected hydroxy, optionally esterified carboxy, --NH.sub.2, protected amino, mono and di-alkyl amino of 1 to 4 alkyl carbon atoms, halogen and trialkylsilyl, R.sub.2 is methyl or ethyl, R.sub.6 and R.sub.7 together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 6 carbon atoms, acetylthio and alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 6 carbon atoms, X is optionally acylated or etherified hydroxyl and Y is selected from the group consisting of hydrogen, R.sub.4, --CH.sub.2 --CH.sub.2 COOM and --CH.sub.2 --CH.sub.
Abstract: Synergistic compositions for inhibiting the action of androgens comprise the combination in a single topical preparation of a 5.alpha.-reductase enzyme inhibitor and an androgen receptor blocking agent in a pharmaceutically and dermatologically acceptable vehicle. The compositions may be topically applied to affected areas of the skin in the treatment or prevention of sebaceous gland hypertrophy, hirsutism and male-pattern baldness in mammals. The inhibitor and blocking agent are present in the composition in a weight ratio of about 1:20 to 5:1, with the inhibitor comprising up to about 0.1% w/v of the composition and the blocking agent comprising up to about 1% w/v of the composition.
Abstract: Steroid compounds of the 20-spiroxane series and their analogues having an open ring E of the formula, ##STR1## in which --A--A-- represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,R.sup.1 represents hydrogen, andR.sup.2 represents an .alpha.-oriented lower alkoxycarbonyl radical, orR.sup.1 and R.sup.2 together represent an .alpha.- or a .beta.-oriented methylene radical,--B--B-- represents the group --CH.sub.2 --CH.sub.2 -- or an .alpha.- or .beta.-oriented group ##STR2## X represents two hydrogen atoms or oxo, Y.sup.1 and Y.sup.2 together represent the oxygen bridge --O--, orY.sup.1 represents hydroxy, andY.sup.2 represents hydroxy, lower alkoxy or, if X represents H.sub.2, also lower alkanoyloxy,and salts of compounds in which X represents oxo and Y.sup.2 represents hydroxy, are distinguished as effective aldosterone-antagonists with minimal side-effects and, for that reason, are especially suitable for the treatment of all forms of hyperaldosteronism.
Abstract: Topical pharmaceutical compositions containing a corticosteroid component and a penetration-enhancing vehicle are disclosed. The vehicle comprises a binary combination of a C.sub.3 -C.sub.4 diol and a "cell-envelope disordering compound". The vehicle provides marked transepidermal and percutaneous delivery of corticosteroids. A method of treating certain rheumatic and inflammatory conditions, systemically or locally, is also disclosed.
Type:
Grant
Filed:
February 1, 1984
Date of Patent:
November 12, 1985
Assignee:
The Procter & Gamble Company
Inventors:
Eugene R. Cooper, Maurice E. Loomans, Mahdi B. Fawzi
Abstract: (5.alpha.)-20-spirox-1-en-3-ones (I) and 17-hydroxy-5.alpha.,17.alpha.-pregn-1-en-3-ones (II) of the formulae ##STR1## in which X represents O or H.sub.2, R.sub.2 represents O and R.sub.1 represents OH, OMe, OAlk, NH.sub.2, NHR.sub.3, NR.sub.3 R.sub.4, or R.sub.2 represents H.sub.2 and R.sub.1 represents OH, OAlk, OAr, OAralk or OAc,in which R.sub.3, R.sub.4 and Alk represent lower alkyl, Me represents a metal atom or metal equivalent or the cation of an organic base, Ar represents monocyclic aryl, Aralk represents monocyclic aryl-lower alkyl, and Ac represents lower alkanoyl, monocyclic aroyl, lower alkylsulphonyl or monocyclic arylsulphonyl, it being possible for R.sub.3 together with R.sub.4 also to represent a lower alkylene group optionally interrupted by a hetero atom,are manufactured by known analogy processes.
Abstract: A spironolactone containing composition for topical use in the form of a cream active in combatting acne and causing only skin absorption and therefore devoid of any undesired systemic effect.