Abstract: The present invention relates to a method of treating alcoholism or alcohol abuse by administering to a subject a pharmaceutically effective amount of an opioid antagonist before imminent drinking. Particularly, the present invention relates to a method of treating alcoholism or alcohol abuse by administering transmucosally to a subject a pharmaceutically effective amount of an opioid antagonist before imminent drinking. Preferably, the opioid antagonist used in the method is nalmefene or a pharmaceutically acceptable salt thereof. The invention also relates to a method of treating alcoholism or alcohol abuse by administering to a subject before imminent drinking a transmucosal preparation comprising a pharmaceutically effective amount of an opioid antagonist, wherein the transmucosal preparation has rapid onset of action. Advantageously, a FAH+ subject is treated.

Abstract: Transdermal preparations containing as active ingredient toremifene or one of its metabolites N-demethyltoremifene or 4-hydroxy-toremifene or their pharmaceutically acceptable non-toxic salts are useful for the treatment of cancers localized in the skin or on a short distance form the skin such as metastatic lesions of breast cancer. They may also be used in adjuvant therapy of breast cancer and in the reversal of multidrug resistance of cancer cells to cytotoxic drugs. Such transdernal preparations are of particular interest in the treatment of melanoma, lymphoma, Kaposi's sarcoma and fungoides mycosis.

Abstract: This invention relates to parenteral preparations of antiestrogens such as toremifene, desmethyl toremifene, tamoxifen or desmethyltamoxifen. The preparations can be emulsions, liposomes or aqueous solutions of cyclodextrin-drug complexes. Particularly the invention relates to a parenteral drug formulation comprising a complex having a 2-hydroxypropyl cyclodextrin component and including an active drug substance selected from the group consisting of toremifene, desmethyl toremifene, tamoxifen and desmethyltamoxifen or a pharmaceutically acceptable non-toxic salt thereof, said complex being present either in an aqueous solution or emulsion or loaded into a liposome.

Abstract: The invention provides novel compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different are H or OH, R.sub.3 is ##STR2## wherein R.sub.4 and R.sub.5, which can be the same or different are H or an alkyl group of 1 to 4 carbon atoms, and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds include metabolites of toremifene and exhibit valuable pharmacological properties as oestrogenic, anti-oestrogenic, and progestanic agents.

Abstract: Imidazole derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2, R'.sub.1 and R'.sub.2 which can be the same or different, are H, CH.sub.3, C.sub.2 H.sub.5, OCH.sub.3, OH, CH.sub.2 OH, NH.sub.2 or halogen; R' if H or ##STR2## where R.sub.3 is H, CH.sub.3, or halogen; R.sub.4 is H and R.sub.5 is H or OH and R.sub.6 is H or OH or one of R.sub.5 and R.sub.6 is H and the other, together with R.sub.4, forms a bond and X and Y, which can be the same or different, are a bond, a straight C.sub.1-2 -alkyl or the corresponding alkenyl, and pharmaceutically acceptable salts thereof exhibit valuable pharmacological properties, especially aromatase inhibiting effects and are useful in the treatment of estrogen dependent diseases, e.g. breast cancer. Anti-mycotic and antifungal properties have also been found.

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: A process for the preparation of a substituted imidazole of the formula ##STR1## wherein X is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --O-- R.sub.1 is H, lower alkyl or lower alkenyl, OCH.sub.3 or OCH.sub.2 CH.sub.3, R.sub.2 is H, CH.sub.3, CH.sub.2 CH.sub.3, OCH.sub.3 or OH, R.sub.3 is H, CH.sub.3, CH.sub.2 CH.sub.3, OCH.sub.3 or Hal, R.sub.4 is H, CH.sub.3, CH.sub.2 CH.sub.3, OCH.sub.3 or Hal, and Hal is halogen and their non-toxic acid addition salts exhibit valuable pharmacological activity and are useful especially as selective .alpha..sub.2 -receptor antagonists.

Abstract: The invention provides compounds of the formula: ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3, which can be the same or different, is 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 or hydroxy) and n is 1-4; and their non-toxic pharmaceutically acceptable acid addition salts. These compounds exhibit valuable pharmacological activity and are useful in the treatment of mammals, especially as anti-hypertensive agents. Furthermore, some of the compounds have proved to possess diuretic, .beta.-blocking activity and/or antithrombotic activity. The compounds may be made by a variety of methods and may be incorporated in pharmaceutical compositions also comprising a compatible pharmaceutically acceptable carrier.

Abstract: 4-[(.alpha.-Methyl)-2,3-dimethyl-benzyl]imidazole is useful as a veterinary sedative-analgetic agent, especially in small mammals.

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 compounds of the formula: ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3, which can be the same or different, is hydrogen, chloro, bromo, fluoro, methyl, ethyl, methoxy, amino, hydroxy or nitro; R.sub.4 is hydrogen or alkyl of 1 to 7 carbons atoms; X is ##STR2## (R.sub.5 is hydrogen or hydroxy) and n is 1-4; and their non-toxic pharmaceutically acceptable acid additions salts. These compounds exhibit valuable pharmacological activity and are useful in the treatment of mammals, especially as anti-hypertensive agents. Furthermore, some of the compounds have proved to possess diuretic, .beta.-blocking activity and/or antithrombotic activity. The compounds may be made by a variety of methods and may be incorporated in pharmaceutical compositions also comprising a compatible pharmaceutically acceptable carrier.

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: Compounds of the formula: ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3, which can be the same or different, is hydrogen, chloro, bromo, fluoro, methyl, ethyl, methoxy, amino, hydroxy or nitro; R.sub.4 is hydrogen or alkyl of 1 to 7 carbon atoms; R.sub.5 is hydrogen or a straight or branched alkyl group of 1 to 5 carbon atoms or a phenyl group; and R.sub.6 is hydrogen or an alkyl group of 1 to 7 carbon atoms or a substituted or unsubstituted benzyl, X is --CH.sub.2 --, --CHOH-- or --CH.dbd.CH-- and n is 0-4; provided that R.sub.5 and R.sub.6 are simultaneously hydrogen only when n is 4 and X is --CH.dbd.CH--; and their non-toxic pharmaceutically acceptable acid addition salts and mixtures thereof exhibit valuable pharmacological activity and are useful in the treatment of mammals, especially as antithrombotic agents. Furthermore, some of the compounds have proved to possess antihypertensive or .beta.-blocking activity. Antimicrobial and antifungal properties have also been found.

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 invention provides compounds of the formula: ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3, which can be the same or different, is hydrogen, chloro, bromo, fluoro, methyl, ethyl, methoxy, amino, hydroxy or nitro; R.sub.4 is hydrogen or alkyl of 1 to 7 carbon atoms; and n is 0-3; and their non-toxic pharmaceutically acceptable acid addition salts. These compounds exhibit valuable pharmacological activity and are useful in the treatment of mammals, e.g. as anti-hypertensive, .beta.-blocking and anti-thrombotic agents. Furthermore the compounds have remarkable antimicrobial activity. The compounds may be made by a variety of methods and may be incorporated in pharmaceutical compositions also comprising a compatible pharmaceutically acceptable carrier.

Abstract: Compounds of the formula: ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3, which can be the same or different, is hydrogen, chloro, bromo, fluoro, methyl, ethyl, methoxy, amino, hydroxy or nitro; R.sub.4 is hydrogen or alkyl or 1 to 7 carbon atoms; R.sub.5 is hydrogen or a straight or branched alkyl group of 1 to 5 carbon atoms or a phenyl group; and R.sub.6 is hydrogen or an alkyl group of 1 to 7 carbon atoms or a substituted or unsubstituted benzyl, X is --CH.sub.2 --, --CHOH-- or --CH.dbd.CH-- and n is 0-4; provided that R.sub.5 and R.sub.6 are simultaneously hydrogen only when n is 4 and X is --CH.dbd.CH--; and their non-toxic pharmaceutically acceptable acid addition salts and mixtures thereof exhibit valuable pharmacological activity and are useful in the treatment of mammals, especially as antithrombotic agents. Furthermore, some of the compounds have proved to possess antihypertensive or .beta.-blocking activity. Antimicrobial and antifungal properties have also been found.