Abstract: The present invention involves the prevention of ethanol-induced neurodegeneration through the administration to a subject before, during and/or after ethanol consumption an effective amount of dexmedetomidine of a pharmaceutically acceptable salt thereof.

Abstract: The invention provides a method for the preparation of 3,4-dihydroxy-5-nitrobenzaldehyde by reacting 3-ethoxy-4-hydroxy-5-nitrobenzaldehyde with a reagent comprising zinc chloride, water and hydrogen chloride.

Abstract: New compounds of formula (I) wherein R.sub.1 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.sub.2 is a heterocyclyl radical selected from 1-imidazolyl, triazolyl, tetrazolyl, pyrazolyl, pyrimidinyl, oxazolyl, thiazolyl, isoxazolyl and isothiazolyl, R.sub.3 is H or OH, R.sub.4 is H, R.sub.5 is H or OH; or R.sub.4 is H and R.sub.3 and R.sub.5 combined form a bond; or R.sub.3 is H and R.sub.4 and R.sub.5 combined form --(O); R.sub.6 is methylene, ethylene, --CHOH--, --CH.sub.2 --CHOH--, --CHOH--CH.sub.2 --, --CH--CH-- or --C(--O)--; or R.sub.4 is H and R.sub.5 and R.sub.6 combined is --CH-- or --CH--CH.sub.2 --; stereoisomers thereof and non-toxic pharmaceutically acceptable acid addition salts thereof 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: A carboxyterminal propeptide of type I procollagen free from type III procollagen carboxyterminal propeptide can be used to produce an antibody which is specific for carboxyterminal propeptide of type I procollagen and which has no affinity for the type III procollagen carboxyterminal propeptide. This antibody can be used to assay more accurately the propeptide which is a measure of the rate of production of type I procollagen and useful in diagnosing and monitoring e.g. bone diseases.

Abstract: A population of pests, especially a population of rodents, can be controlled hormonally by means of baits that contain an orally active antiestrogen. The hormone present in the baits weakens the reproductive capacity of rodents thereby controls their population.

Abstract: A process is provided for preparing cis-(+)-hydroxy-5-[2-(dimethylamine)ethyl]-2,3-dihydro-2-(4-methoxyphenyl) -benzothiazepin-4(5H)-one that is a useful intermediate in the preparation of diltiazem. It has been found that the requisite N-alkylation reaction proceeds rapidly and with an excellent yield when the solvent is a mixture of toluene and N-methylpyrrolidin-2-one and the base is finely-divided sodium carbonate under anhydrous conditions. Such diltiazem commonly is used in the treatment of angina pectoris.

Abstract: The invention relates to a transfer device for performing a regular, linear transfer movement including a body (1), provided with a threaded bar (2), a stepping motor (3) for driving the threaded bar (2), two guide bars (4, 5), a slide (6), and a follower (7) connected to it. The slide (6) is moved along the guide bars (4, 5) by the follower (7), which transforms the rotational movement of the threaded bar (2) into a linear transfer movement. The object to be transferred with the transfer bar (2) is attachable to the slide (6). The invention is characterized by the fact that the slide (6) includes an opening (8), through which the threaded bar (2) is fitted to pass with some play, and in connection with the opening (8) there is a follower (7), having a tongue (9), which is fitted to follow the threaded groove (10) of the threaded bar (2), so that the rotational movement (A, B) of the threaded bar is transformed into a linear movement of the slide (6) via the follower (7).

Abstract: An ultrasonic processing method by which polymer/drug composites can be quickly and efficiently molded to form matrix-type drug delivery systems is disclosed. The advantages of the method include speed and good control of the process. It also causes less degradation in polymers and/or drugs than most conventional processing methods.

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: The invention relates to an image plate (1) for intraoral dental radiography which can be closed within a cover through which X-rays can pass, where the plate is retained during the X-raying and from where the plate can be removed after the X-raying in order to read the picture. According to the invention the edges of the image plate (1) are equipped with a protective frame (2) projecting from the plane of the plate surface at least on the image side of the plate. The frame may be formed as a continuous cover frame (2) surrounding the edges of the frame, consisting of two opposite frame-like portions (7) pressed together and optionally identical. The purpose of the frame (2) is to protect the image plate (1) against scratches or similar damages as the plate is being handled and read.

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 compound (-)-[[4-(1,4,5,6 tetrahydro-4-methyl-6-oxo-3 pyridazinyl) phenyl]-hydrazono] propane dinitrile and its salts are prepared and used for treating congestive heart failure.

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: The present invention is in the art of eliciting a yohimbine-like alpha-adrenoreceptor antagonistic noradrenergic neurotransmission male sexual activity response in penile erection. The improvement involves a more rapid onset of action and improved effect than that of yohimbine, consisting essentially of the step of administering the compound atipamezole or a pharmaceutically acceptable acid addition salt thereof to a male in need thereof. Atipamezole or pharmaceutically acceptable acid salt thereof may be administered perorally, intravenously, intramuscularly, transmucosally or transdermally.

Abstract: This invention describes a device for peroral administration of a therapeutic agent which is capable of existing in an unionized therapeutically active form. The device comprises a reservoir comprising the therapeutic agent in ionized form, which reservoir has a wall permeable to un-ionized material and impermeable to ionized material; and a solid material which upon uptake of water is converted to a buffer; the solid material having, on uptake of water, a pH which determines the rate of permeation of the therapeutic agent in un-ionized form through the reservoir wall. The device enables the release of the therapeutic agent to be controlled by the pH of the buffer and, if desired, the composition of the reservoir walls. The composition of the surrounding aqueous medium does not affect the rate of release.

Abstract: An enzymatic method for the preparation of (2S,3S)-threo-alkyl-2-hydroxy-3-(4-methoxyphenyl)-3-(2-X-phenylthio)propio nate, where X=NO.sub.2, NH.sub.2, NHCOCH.sub.3, NHCOCF.sub.3, NHCO.sub.2 CH.sub.3, NHCO.sub.2 C(CH.sub.3).sub.3 or NHCHO and R is an alkyl group, e.g., CH.sub.3, or CH.sub.2 CH.sub.3 in an essentially anhydrous organic solvent is described. In this method a lipase which stereospecifically acylates the (2R,3R)-enantiomer of the racemic mixture is used. After enzymatic reaction, the (2S,3S)-enantiomer and the acylated (2R,3R)-compound are separated, e.g., by flash-chromatography or by fraction crystallization of the (2S,3S)-compound from the reaction mixture.

Abstract: A method for preventing or treating myocardial ischemia in a mammalian organism is disclosed. The compound 4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl!hydrazono!prop anedinitrile or its enantiomer or a pharmaceutically acceptable salt there is administered to a mammalian organism in need of such prevention or treatment. The compound may be administered in its racemic form or in a form which is substantially free of the (+)-enantiomer or substantially free of the (-)-enantiomer.

Abstract: Diastereomeric intermediate salts of formulae (IIIa) or (IIIb) ##STR1## are prepared.

Abstract: The invention provides compounds of the formula ##STR1## wherein Y is --CH.sub.2 -- or --CO--;R.sub.1 is F, Cl or OH; R.sub.2 is H, F or Cl; and R.sub.3 is H, CH.sub.3 or CH.sub.2 CH.sub.3, excluding 4-(5-chloro-2,3-dihydro-1H-inden-2-yl)-1H-imidazole and 4-(4-chloro-2,3-dihydro-1H-inden-2-yl)-1H-imidazole; and their non-toxic acid addition salts and mixtures thereof. Processes for the preparation of these compounds are described, as are pharmaceutical compositions comprising at least one of the compounds or its salt. The compounds and their non-toxic salts exhibit valuable pharmacological activity and are highly selective and long acting antagonists at .alpha..sub.2 -adrenoceptors. Their peroral bioavailability is good. The compounds are especially useful in the treatment of cognitive disorders.