Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula: wherein R1 and R2, which are the same or different are a) H, halogen, OCH3, OH; or  where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, —CH2C≡CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or c) —Y—(CH2)nCH2—O—R6 where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and R3 is H, halogen, OH or —OCH3; stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.

Abstract: This invention relates to the use of an aromatase inhibitor in the treatment of decreased androgen to estrogen ration (DATER) as well as to a method for the treatment of detrusor urethral sphincter dyssnergia (DUSD) in men.

Abstract: The invention relates to a method for the treatment of detrusor urethral sphincter dyssynergia in men, said method comprising administering to the patient an effective amount of an aromatase inhibitor. The invention also concerns a method for the treatment of decreased androgen to estrogen ratio in men, said method comprising administering to the patient an effective amount of an aromatase inhibitor.

Abstract: New 4(5)-imidazole derivatives of formula (Ia) and (Ib) wherein one of R.sub.1 and R.sub.2 is CN and the other one is H, CH.sub.3, OCH.sub.3, NO.sub.2, NH.sub.2, CN, CF.sub.3, CHF.sub.2, CH.sub.2 F or halogen; R' is H or (II) where R.sub.3 is H, CH.sub.3 or halogen; R.sub.4 is H and R.sub.5 is H or R.sub.4 and R.sub.5 together form a bond, n is 1 or 2 and y is 0 to 2, their stereoisomers and their non-toxic pharmaceutically acceptable acid addition salts exhibit selective aromatase inhibiting properties, compared with their desmolase inhibiting properties. The compounds of the invention are valuable in the treatment of estrogen dependent diseases, e.g. breast cancer or benign prostatic hyperplasia (BPH).

Abstract: This invention relates to a transdermal preparation comprising a therapeutically active compound of the formula: ##STR1## where R.sub.1, R.sub.2, and R.sub.3, which can be the same or different are H, CH.sub.3, C.sub.2 H.sub.5 or Cl; X is CH.dbd.CH or (CH.sub.2).sub.n where n is 1 to 3 or X is --C(OR.sub.5)H-- where R.sub.5 is methyl or ethyl; and R.sub.4 is hydrogen or a straight alkyl of 1 to 4 carbon atoms. The transdermal administration of the compounds can be accomplished by preparations in the form of ointments, emulsions, lotions, solutions, creams or transdermal patches.

Abstract: Compounds of formula: ##STR1## where X is --CH.sub.2 --, --CH(CH.sub.3)--, --CHR.sub.3 --CH.sub.2 -- or --CR.sub.3 .dbd.CH-- and R.sub.1, R.sub.2 and R.sub.3, which can be the same or different, are each H or CH.sub.3 or a stereoisomer or pharmaceutically acceptable salt thereof, and pharmaceutical compositions containing them, are useful for lowering intraocular pressure in a mammal, e.g. in the treatment of glaucoma.

Abstract: Transdermal administration of dexmedetomidine, the dextrorotatory isomer of medetomidine, is described. The method involves sedating a patient by administering dexmedetomidine to a predetermined area of skin at an administration rate and for a time period effective to achieve the desired level of sedation. A therapeutic system for transdermally administering the drug is also provided. The therapeutic system is in the form of a skin patch which is a laminated composite of a backing layer, an optional anchor adhesive layer, a contact adhesive layer, and one or more additional layers.

Abstract: Transdermal administration of dexmedetomidine, the dextrorotatory isomer of medetomidine, is described. The method involves sedating a patient by administering dexmedetomidine to a predetermined area of skin at an administration rate and for a time period effective to achieve the desired level of sedation. A therapeutic system for transdermally administering the drug is also provided. The therapeutic system is in the form of a skin patch which is a laminated composite of a backing layer, an optional anchor adhesive layer, a contact adhesive layer, and one or more additional layers.

Abstract: This invention relates to local epidural or intraspinal use of compounds of the formula: ##STR1## where X is H or CH.sub.3 and R.sub.1 and R.sub.2, which can be the same or different, are each H or CH.sub.3 and their stereoisomers and their non-toxic, pharmaceutically acceptable salts. Especially useful are the compounds known under the generic names medetomidine ((.+-.)-4-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole), dexmedetomidine (+)-4-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole and detomidine 4-(2,3-dimethylbenzyl)-1H-imidazole.

Abstract: A method for treating alcoholism. The alcohol-drinking response of alcoholics is extinguished by having them drink alcoholic beverages while nalmefene, an opiate antagonist, blocks the positive reinforcement effect of ethanol in the brain.

Abstract: Medetomidine is useful in the treatment of anxiety disorders.