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: Substituted imidazoles of the formula ##STR1## wherein R.sub.1 is H, an alkyl of 1 to 4 carbon atoms or --CH.sub.2 OH; R.sub.2 is H or CH.sub.3 ; R.sub.3 is ##STR2## and R.sub.4 is H; R.sub.5, R.sub.6 and R.sub.7 which can be the same or different, are H, --CH.sub.3 , --CH.sub.2 CH.sub.3, halogen, OH or --OCH.sub.3, or R.sub.5 is hydrogen and R.sub.6 and R.sub.7 together form an --O--CH.sub.2 --O--bridge between two adjacent carbon atoms in the phenyl group; provided thatwhen R.sub.1, R.sub.2 and R.sub.4 are all hydrogen, then R.sub.5, R.sub.6, R.sub.7 are not all simultaneously hydrogen;or non-toxic pharmaceutically acceptable acid addition salts thereof. The substituted imidazoles are useful as anti-hypertensives or anti-thrombotic agents or diuretics.

Abstract: The invention provides novel compounds of the formula: ##STR1## wherein n is 0 to 4, R.sub.1 and R.sub.2, which can be the same or different are H, OH, alkoxy of 1 to 4 carbon atoms, benzyloxy or methoxymethoxy; R.sub.3 is H, OH, halogen, alkoxy of 1 to 4 carbon atoms, benzyloxy, methoxymethoxy, 2,3-dihydroxypropoxy or ##STR2## wherein m is 1 or 2, R.sub.6 and R.sub.7, which can be the same or different are H or an alkyl group of 1 to 4 carbon atoms, or ##STR3## can form an N-containing three-, four-, five- or six-membered heterocyclic ring; R.sub.4 is OH, F, Cl, Br, I, mesyloxy, tosyloxy, alkylcarbonyloxy of 1 to 4 C-atoms, formyloxy or CH.sub.2 R.sub.4 is replaced by CHO; R.sub.5 is H or OH; or R.sub.4 and R.sub.5 together form an --O-- bridge between the carbon atoms to which they are attached, and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof. Processes for the preparation of these compounds are described, and also novel pharmaceutical compositions containing them.

Abstract: The invention provides novel compounds of the formula: ##STR1## wherein R.sub.1 is H, an alkyl of 1 to 4 carbon atoms or --CH.sub.2 OH; R.sub.2 is H or CH.sub.3 ; R.sub.3 is --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.3, ##STR2## --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.3, --CH.sub.2 CH.dbd.CH.sub.2, or ##STR3## and R.sub.4 is H or OH; or R.sub.3 and R.sub.4 together represent .dbd.CH.sub.2, .dbd.CH--CH.sub.3, .dbd.CH--CH.sub.2 --CH.sub.3, ##STR4## or .dbd.CH--CH.sub.2 CH.sub.2 CH.sub.3 ; X is ##STR5## R.sub.5, R.sub.6 and R.sub.7, which can be the same or different are H, --CH.sub.3, --CH.sub.2 CH.sub.3, halogen, OH or --OCH.sub.3 or R.sub.5 is hydrogen and R.sub.6 and R.sub.7 together form an --O--CH.sub.2 --O--bridge between two adjacent carbon atoms in the phenyl group; --CHR.sub.8 -- is --CH.sub.2 --, --CH(CH.sub.3)--, --CH(--CH.sub.2 CH.sub.3)--, --CH(--CH.sub.2 CH.sub.2 CH.sub.3)--, ##STR6## --CH(--CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.3)-- or >C.dbd.CH.sub.2, >C.dbd.CH--CH.sub.3, >C.

Abstract: The invention provides novel compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxy, alkoxy of 1 to 4 carbon atoms, benzyloxy, allyloxy, 2,3-epoxypropoxy, methoxymethoxy, ethoxymethoxy, or 2,3-dihydroxypropoxy or ##STR2## wherein one of R.sub.5 and R.sub.6 is hydrogen or R.sub.5 and R.sub.6 are alkyl groups of 1-4 carbon atoms which may be the same or different, or the --NR.sub.5 R.sub.6 group stands for a nitrogen containing 5 to 7 membered heterocyclic radical and m is 1 or 2; R.sub.2 is an alkyl of 1 to 4 carbon atoms or ##STR3## wherein R.sub.7 has the same meanings as R.sub.1 except that R.sub.7 and R.sub.1 cannot simultaneously be the same; R.sub.3 is an alkyl of 2 to 4 carbon atoms, cyclopentyl or hydroxy-cyclopentyl; R.sub.4 is hydrogen or hydroxy; and n is 0 to 3, provided that when R.sub.4 is hydrogen, then R.sub.2 and R.sub.

Abstract: The invention provides novel compounds of the formula: ##STR1## wherein the various substituents are defined herein below. Processes for the preparation of these compounds are described, as are novel pharmaceutical compositions comprising at least one of the compounds of their salts. The compounds and their non-toxic salts exhibit valuable pharmacological activity and are useful in the treatment of mammals, especially as antihypertensive agents. Furthermore, some of the compounds have proved to possess antithrombotic and diuretic activity. Antimycotic and antifungal properties have also been found.

Abstract: The invention provides compounds of the formula: ##STR1## wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are defined hereinbelow. These compounds exhibit valuable pharmacological activity and are useful in the treatment of mammals, e.g. as diuretic agents. Furthermore, they have antithrombotic and anti-hypertensive effects.

Abstract: The invention provides compounds of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3, which can be the same or different, are each hydrogen, chloro, bromo, fluoro, methyl, ethyl, methoxy, amino, hydroxy or nitro; R.sub.4 is hydrogen or alkyl of 1 to 7 carbon atoms; --X-- is ##STR2## R.sub.5 is hydrogen, hydroxy or --OR.sub.6 ; and R.sub.6 is alkyl of 1 to 7 carbon atoms or aryl of 6 to 10 carbon atoms; and their non-toxic pharmaceutically acceptable acid addition salts and mixtures thereof. Processes for the preparation and use of the subject compounds are described, as are novel pharmaceutical compositions comprising at least one of the subject compounds or their salts. The compounds and their non-toxic salts exhibit valuable pharmacological activity and are useful in the treatment of mammals, e.g., as anti-ulcer or anti-hypertensive agents. Furthermore, they are useful as diuretic, sedative, analgesic, anti-inflammatory and tranquilizing agents.

Abstract: The 2,6-dichlorophenyl-substituted amino-imidazole derivatives 1-(2',6'-dichlorophenyl)-2-amino-4-methyl-imidazole, 2-(2',6'-dichloroanilino)-4-methyl-imidazole, their non-toxic, pharmaceutically acceptable, acid addition salts and mixtures thereof, exhibit excellent anti-hypertensive activity which makes the derivatives particularly suitable for treatment of high blood pressure in mammals.The derivatives may be prepared in either of two processes. The first process involves the sequential reaction of a known starting material with ammonia and a halogenated acetone which may be followed by separation of the formed isomers. The second process involves the decarboxylation of the novel intermediates 4-[1-(2',6'-dichlorophenyl)-2-amino)]-imidazoleacetic acid or 4-[2-(2',6'-dichloroanilino)]-imidazoleacetic acid or mixtures thereof. Such intermediates, their lower alkyl esters, their non-toxic, pharmaceutically acceptable acid addition salts or mixtures thereof may also be employed as a diuretic agent.