Abstract: A process for preparing selegiline hydrochloride by reaction of R-(-)-N,.alpha.-dimethylphenylethylamine with 3-bromo-1-propyne is described, which consists in reacting the substances in a molar ratio of approximately 2:1 at 30.degree.-50.degree. C. in a solvent mixture of an aromatic hydrocarbon and water and isolating the selegiline from the organic phase and converting it into the hydrochloride.

Abstract: Iminium ion scavengers are used in the invention to inhibit formation of N-nitrosamines, especially in cosmetics and pharmaceuticals formulations. The iminium ion scavengers may be used in combination with nitrite ion scavengers such as ascorbate.

Abstract: Tetrahydroisoquinoline compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof, in which: R.sub.1 represents one or more substituents selected from H, halo, hydroxy, alkyl (optionally substituted by hydroxy), alkoxy, alkylthio, alkylsulphinyl, alkyl-sulphonyl, nitro, cyano, polyhaloalkyl, polyhaloalkoxy, phenyl (optionally substituted by one or more of halo, alkyl or alkoxy), or R.sub.1 is optionally alkylated carbamoyl;R.sub.2 represents a saturated or unsaturated aliphatic group optionally substituted by hydroxy or alkoxy;E represents an alkylene chain optionally substituted by one or more alkyl groups;and G represents (a) optionally substituted saturated or unsaturated alicyclic group containing 3 to 8 carbon atoms, or (b) optionally substituted saturated or unsaturated aliphatic chain containing 1 to 12 carbon atoms, or (c) optionally substituted 5 or 6 membered heterocyclic ring containing one or more N or O atoms or SO.sub.

Abstract: Tetrahydroisoquinoline compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof, in which: R.sub.1 represents one or more substituents selected from H, halo, hydroxy, alkyl (optionally substituted by hydroxy), alkoxy, alkylthio, alkylsulphinyl, alkyl-sulphonyl, nitro, cyano, polyhaloalkyl, polyhaloalkoxy, phenyl (optionally substituted by one or more of halo, alkyl or alkoxy), or R.sub.1 is optionally alkylated carbamoyl;R.sub.2 represents a saturated or unsaturated aliphatic group optionally substituted by hydroxy or alkoxy;E represents an alkylene chain optionally substituted by one or more alkyl groups;and G represents (a) optionally substituted saturated or unsaturated alicyclic group containing 3 to 8 carbon atoms, or (b) optionally substituted saturated or unsaturated aliphatic chain containing 1 to 12 carbon atoms, or (c) optionally substituted 5 or 6 membered heterocyclic ring containing one or more N or O atoms or SO.sub.

Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which one of A or B represents N and the other represents N or C--R.sub.3 ; R.sub.1 represents hydrogen, halo, alkyl, hydroxy, carboxyalkenyl, alkoxycarbonylalkenyl, hydroxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxy, halogenated alkyl, carboxy, alkoxycarbonyl, alkanoylamino or carbamoylalkenyl; R.sub.2 represents hydrogen, alkyl, halo, alkoxy, hydroxy, alkanoyloxy, or phenoxy; R.sub.3 represents hydrogen or alkyl; R.sub.4 represents hydrogen, halo, alkoxycarbonyl, cyano, benzyloxycarbonyl, alkanoyl, benzoyl, alkyl, carboxy, alkylthio or carbamoyl; R.sub.5 represents hydrogen or alkyl; R.sub.9 represents hydrogen or alkyl; R.sub.10 represents phenyl, pyridyl or pyrimidinyl substituted by OR.sub.6 and optionally further substituted wherein R.sub.6 represents hydrogen, alkyl, alkoxycarbonyl or carbamoyl, alicyclic hydrocarbon, phenyl, cycloalkylalkyl, arylalkyl or pyridyl; or when R.sub.10 represents phenyl, OR.sub.

Abstract: Compounds of the formula I ##STR1## and pharmaceutically acceptable salts thereof in which R.sub.1 represents hydrogen, halo, cyano, cyanoalkyl, alkyl, alkoxy, phenoxy, phenyl, alkoxycarbonyl, --NR.sub.13 R.sub.14, --N(R.sub.15)SO.sub.2 R16, halogenated alkoxy, halogenated alkyl, arylalkoxy, hydroxy, phenylalkyl, alkoxycarbonylvinyl, --S(O).sub.n R.sub.7, alkoxycarbonylalkyl, carboxyalkyl, --CONR.sub.11 R.sub.12 carbamoylvinyl, --OSO.sub.2 R.sub.21, 4,5-dihydrothiazol-2-yl, 4,4-dimethyl-2-oxazolin-2-yl or --NR.sub.60 R.sub.61 ; or R.sub.1 represents a group of formula --(O).sub.z --L.sub.3 G wherein z equals 0 or 1, L.sub.3 represents a C.sub.1-4 alkylene chain, G represents a group of formula a), b), c), or d): a) --NR.sub.22 R.sub.23 ; b) --S(O).sub.m R.sub.26 ; c) CONR.sub.27 R.sub.28 ; d) --OR.sub.29 ; R.sub.2 and R.sub.3 independently represent hydrogen, halo, alkyl, alkoxy, --NR.sub.13 R.sub.14, halogenated alkoxy, halogenated alkyl, hydroxy, --S(O).sub.n R.sub.7 or --NR.sub.60 R.sub.61 ; L.sub.

Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which R.sub.1, R.sub.2 and R.sub.3 independently represent hydrogen, hydroxy, halo, alkyl or alkoxy;ALK.sup.1 represents a C.sub.2-6 alkylene chain optionally substituted by one or more C.sub.1-2 alkyl groups;Y represents a piperidine ring which is attached through nitrogen to ALK.sup.1 ;R.sub.4 represents hydrogen or a C.sub.1-4 alkyl group; the broken line in --- represents a bond, or is absent and the free valency on Y is taken up by hydrogen and the free valency on CR.sub.4 is taken up by hydrogen or a C.sub.1-4 alkyl group;ALK.sup.2 is absent or represents a C.sub.1-4 alkylene chain optionally substituted by one or more C.sub.1-2 alkyl groups; andR.sub.5 and R.sub.6 independently represent hydrogen, alkyl, phenyl, alkyl (optionally substituted) or R.sub.5 and R.sub.

Abstract: Compounds of formula (I) which includes pharmaceutically acceptable salts thereof and stereoisomers thereof: ##STR1## wherein: R.sub.1 represents H or one of the following groups (optionally substituted with one or more of halo, cyano, hydroxy or amino): C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 alkanoyl; R.sub.2 and R.sub.3 independently represent H or one of the following groups (optionally substituted with one or more of halo, cyano, hydroxy or amino): C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 alkanoyl, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphinyl or C.sub.1-6 alkylsulphonyl; R.sub.4 and R.sub.5 combined together with the carbon atom to which they are attached represent C.sub.3-6 cycloalkylidene (each alkyl or cycloalkylidene being optionally substituted with one or more of halo, cyano, hydroxy, amino or C.sub.1-6 alkyl); and R.sub.6, R.sub.7 and R.sub.

Abstract: There is disclosed a solid fast dispersing dosage form of a pharmaceutical composition suitable for oral administration comprising: a therapeutic agent which comprises one or more compound thyroid hormone or hormones; from about 80% to about 99.9% of disintegrating agent by mass; from about 0.01% to about 10% of flavoring agent by mass; and from about 0.1% to about 5% mass of lubricating agent by mass; which has utility in the treatment of disorders associated with the improvement of the thyroid hormone function in animals including human beings.

Abstract: Compounds of the formula I ##STR1## including pharmaceutically acceptable salts thereof are disclosed in which R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently represent hydrogen, hydroxy, halo, halogenated alkyl, halogenated alkoxy, alkyl, alkoxy, cyano, a carbamoyl group, carbonyl group, or R.sub.1 and R.sub.2 together with the phenyl ring represent a naphthalene ring (optionally substituted); L.sub.1 represents C.sub.2-6 alkylene; R.sub.5 represents hydrogen or alkyl, R.sub.6 represents hydrogen or alkyl, phenylalkyl (optionally substituted) or R.sub.5 and R.sub.6 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring; L.sub.2 represents a C.sub.1-6 alkylene chain; and R.sub.7 and R.sub.8 independently represent hydrogen or alkyl or R.sub.7 and R.sub.8 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring.

Abstract: A process for producing solutions of active substances of low solubility, which comprises (1) dissolving the active substance with a phospholipid and a water-soluble lipid in an organic solvent, (2) evaporating the resulting solution to dryness, (3) taking up the residue in a strongly acidic buffer and stirring at elevated temperature until a colloidal solution is produced, (4) cooling the colloidal solution and adjusting to a pH of 6-7 and sterilizing. Particularly suitable for the process are lipids of the formula ##STR1## wherein m, a, b, x and y have the meanings indicated in the description.

Abstract: Compounds of formula (I) including pharmaceutically acceptable salts thereof in which R.sub.1 represents a C.sub.1-6 alkyl group; R.sub.2 represents a group of the formula COOR.sub.4 in which R.sub.4 represents a C.sub.1-5 alkyl group; and R.sub.3 represents a group of formula COOR.sub.5 in which R.sub.5 represents a C.sub.1-5 alkyl group are disclosed, which are anti-rheumatic agents and are useful as modulators of cytokine synthesis, immunomodulatory agents, anti-inflammatory agents and anti-allergic agents. Compositions containing these compounds and processes to make these compounds are also disclosed.

Abstract: Novel bis-1,2-dihydro-3H-dibenzisoquinoline-1,3-diones and their salts, processes for their preparation, pharmaceutical compositions containing them and methods of using them to treat malignancies, mainly human solid tumor carcinomas.

Abstract: A cylindrical delayed release tablet with a convex or flat upper side and lower side is provided, along with a method for its production and a gelatin capsule containing 3-200 tablets of the same having identical or different release rates, wherein the tablet if made of .beta.-phenylpropiophenone derivatives of the formula I as active ingredient ##STR1## where R is n-propyl or 1,1-dimethylpropyl, and their pharmacologically acceptable salts, wherein the tablet has a height and diameter that are both, independently of one another, 1-3 mm, the active ingredient content is in the range from 81-99.

Abstract: Nucleic acid molecules and proteins useful for regulating the expression of genes in eukaryotic cells and organisms in an inducible manner are disclosed. In the regulatory system of the invention, transcription of a tet operator-linked nucleotide sequence is stimulated by a transcriptional activator fusion protein composed of two polypeptides, a first polypeptide which binds to tet operator sequences in the presence of tetracycline or a tetracycline analogue and a second polypeptide which directly or indirectly activates transcription in eukaryotic cells. In one embodiment, the fusion protein comprises a mutated Tet repressor operatively linked to a transcriptional activation polypeptide, such as a portion of herpes simplex virus virion protein 16. In the absence of an inducing agent (tetracycline or a tetracycline analogue), transcription of the tet operator-linked nucleotide sequence remains uninduced.

Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which m is 0, 1 or 2; n is 2, 3, 4 or 5; X is carbonyl or a group of formula II ##STR2## in which R.sub.5 is H or alkyl; Y is an alkylene chain optionally substituted by one or more alkyl groups; Z is an alkylene chain containing 2 to 5 carbon atoms optionally substituted by one or more alkyl groups; R is phenyl optionally substituted by one or more halo substituents or R is naphthyl; and R.sub.1 and R.sub.2, which are the same or different, are H, alkyl, or arylalkyl, provided that when R.sub.1 is benzyl, R.sub.2 is H or methyl;have utility in the treatment of depression, anxiety, Parkinson's disease, obesity, cognitive disorders, seizures, neurological disorders such as epilepsy, and as neuroprotective agents to protect against conditions such as stroke.

Abstract: Transgenic animals carrying two transgenes, the first coding for a transactivator fusion protein comprising a tet repressor and a polypeptide which directly or indirectly activates in eucaryotic cells, and the second comprising a gene operably linked to a minimal promoter operably linked to at least one tet operator sequence, are disclosed. Isolated DNA molecules (e.g., targeting vectors) for integrating a polynucleotide sequence encoding a transactivator of the invention at a predetermined location within a second target DNA molecule by homologous recombination are also disclosed. Transgenic animals having the DNA molecules of the invention integrated at a predetermined location in a chromosome by homologous recombination are also encompassed by the invention. Methods to regulate the expression of a tet operator linked-gene of interest by administering tetracycline or a tetracycline analogue to an animal of the invention are also disclosed.

Abstract: Isolated nucleic acid molecules encoding fusion proteins which regulate transcription in eukaryotic cells are disclosed. The fusion proteins of the invention comprise a Tet repressor having at least one amino acid mutation that confers on the fusion protein an ability to bind a class B tet operator sequence having a nucleotide substitution at position +4 or +6, operatively linked to a polypeptide which regulates transcription in eukaryotic cells. Methods for regulating transcription of a tet operator-linked gene in a cell are also provided.

Abstract: Asymmetrically substituted bisnaphthalimides of the formula I ##STR1## in which A, B, D, R.sup.1, R.sup.2, m and have the meanings stated in the description, and the salts thereof with phsiologically tolerated acids, ale described. The novel compounds are suitable for controlling diseases.

Abstract: A stable active substance emulsion of the oil-in-water type with a phospholipid as emulsifier is described, where the active substance dissolved in the lipid phase has one or more basic groups, is hydrophobic and oil-soluble, and has a pKa of at least 7.5, the aqueous phase is set at an acid pH, and the disperse phase gives a positive zeta potential of at least +15, but preferably +30, mV after dilution of the emulsion ready for administration to a fat content of 0.08% by weight.