Abstract: Diseases caused by obesity are treated with endothelin receptor antagonists. Diseases treated include those frequently associated with obesity such as hypertension, type 2 diabetes, hyperlipidemia, chronic kidney failure, arteriosclerosis and gout.

Abstract: Compounds of Formula I including pharmaceutically acceptable salts thereof in the form of individual enantiomers, racemates, or other mixtures of enantiomers, in which Ar is phenyl, naphthyl or benzo[b]thiophenyl, each of which may be optionally substituted; R1 and R2, which may be the same or different, independently are a) H, b) an alkyl group containing 1 to 6 carbon atoms, c) an alkenyl group containing 3 to 6 carbon atoms, d) a cycloalkyl group containing 3 to 7 carbon atoms, e) a cycloalkylmethyl group in which the ring contains 3 to 7 carbon atoms, f) an aryl or heteroaryl group optionally substituted g) an arylalkyl or heteroarylalkyl group each optionally substituted; or R1 and R2 form an alkylene chain optionally substituted by one or more alkyl groups each containing 1 to 3 carbon atoms, such that, together with the atoms to which they are attached, they form a 5 or 6 membered ring; R3 is a) H, b) an aryl or heteroaryl group each optionally substituted c) an optionally

Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1 and R2 are independently H or methyl (for example N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl amine hydrochloride optionally in the form of its monohydrate) is used for lowering lipid levels and/or increasing the HDL: LDL cholesterol ratio in humans, for example in humans having hyperlipidaemia, hypercholesterolaemia or hypertriglyceridaemia.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof in which R1 and R2 are independently H or methyl (for example N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl amine hydrochloride optionally in the form of its monohydrate) is used for reducing Insulin resistance in humans in whom Impaired Glucose Tolerance and Non-Insulin Dependent Diabetes Mellitus have not presented.

Abstract: A compound of formula I ##STR1## or a pharmaceutically acceptable salt thereof in which R.sub.1 and R.sub.2 are independently H or methyl (for example N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl amine hydrochloride optionally in the form of its monohydrate) is used for lowering the uric acid level in humans, for example in humans suffering from or at risk of developing gout, hyperuricaemia or coronary heart disease.

Abstract: The invention relates to the use of mixtures of defined composition of purified enzymes from Clostridium histolyticum for obtaining, in a reproducible, standardized manner, cells or tissue fragments from human or animal tissues, and to these enzymes and mixtures thereof; in addition it relates to the direct or indirect medical use of these enzymes, alone or as ingredient of mixtures, eg. in wound treatment.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof in which A is methylene or --O--; B is methylene or --O--; g is 0, 1, 2, 3 or 4; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents an aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress and spasticity ##STR1##

Abstract: Methods of regulating gene expression in subjects using tetracycline-responsive fusion proteins are disclosed. In one embodiment, the method involves introducing into a cell the subject a nucleic acid molecule encoding a fusion protein which inhibits transcription, the fusion protein comprising a first polypeptide which binds to a tet operator sequence, operatively linked to a heterologous second polypeptide which inhibits transcription in eukaryotic cells; and modulating the concentration of a tetracycline, or analogue thereof, in the subject. The first polypeptide can binds to a tet operator sequence in the absence, but not the presence, of tetracycline. Alternatively, the first polypeptide can binds to a tet operator sequence in the presence, but not the absence, of tetracycline.

Abstract: A compound of formula I ##STR1## or a pharmaceutically acceptable salt thereof in which R.sub.1 and R.sub.2 are independently H or methyl (for example 1,1-dimethyl-2-(2-morpholinophenyl)guanidine fumarate) is used for inhibiting the formation of advanced glycosylation end-products, and for the treatment and/or prophylaxis of long-term complications associated with diabetes, such as atherosclerosis, nephropathy, neuropathy and retinopathy.

Abstract: Substituted piperazine compounds of formula I ##STR1## in which HET is a substituted pyrazole, imidazole or 1,2,4-triazole have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.

Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or --O--; B is methylene or --O--; G.sub.1 --G.sub.2 --G.sub.3 are absent or form a heteroaromatic chain; g is 0,1,2,3 or 4; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO. HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mrellitus, hyperglvcaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.

Abstract: The present invention relates to a novel process for the preparation of nizatidine, N-[2-[[[2-(dimethylamino)methyl-4-thiazolyl]methyl]thio]ethyl]-N'-methyl-2 -nitro-1,1-ethenediamine, and pharmaceutically acceptable salts thereof, comprising reacting a compound of formula II ##STR1## with a compound of formula III ##STR2## or a salt thereof, in which X represents a leaving group, in the presence of methylamine in the presence of an inert diluent.

Abstract: Compounds of formula I ##STR1## where R.sub.1 -R.sub.3, L.sub.1, T, L.sub.2 --N--Q--Y and R.sub.6 are as defined in the specification, and pharmaceutically acceptable salts thereof which are antiinflammatory, antiallergic and immunomodulant agents, compositions containing these compounds and processes to make them.

Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.

Abstract: Improvements to a six stage process for production of sodium l-thyroxine from l-tyrosine ?described in U.S. Pat. No. 2,889,363 and U.S. Pat. No. 2,889,364 (Baxter)! are described, the improvements comprising the oxidative coupling of a diiodo-l-thyrosine to form a biphenyl ether derivative, catalysed by a manganese salt in which the amine and acid functionally of the diiodo-l-thyrosine have been protected by suitable protecting groups, characterised in that the reaction is performed at a pressure of about 20 atmospheres in the presence of an organic amine additive using a gaseous oxidant comprising oxygen and optionally an inert diluent. The process optionally further comprises acid hydrolysis of the biphenyl ether derivative with hydrochloric acid to form a l-thyroxine hydrochloride salt and generation of sodium-l-thyroxine from the l-thyroxine hydrochloride salt.

Abstract: Certain 1,2,4-triazolo(4,3-b)pyridazines of formula ##STR1## including pharmaceutically acceptable salts thereof, wherein R.sub.1 -R.sub.8 are as defined in the disclosure, for the treatment, prophylaxis and/or inhibition of seizures, neurological disorders such as epilepsy and/or conditions in which there is neurological damage such as stroke, brain trauma, cerebral ischemia, head injuries and hemorrhage are disclosed.

Abstract: A method for regulating expression of a tet operator-linked gene in a cell of a subject is disclosed. In one embodiment, the method involves introducing into the cell a nucleic acid molecule encoding a tetracycline-controllable transactivator (tTA), the tTA comprising a Tet repressor operably linked to a polypeptide which directly or indirectly activates transcription in eucaryotic cells; and modulating the concentration of a tetracycline, or analogue thereof, in the subject. Alternatively, in another embodiment, the method involves obtaining the cell from the subject, introducing into the cell a first nucleic acid molecule which operatively links a gene to at least one tet operator sequence, introducing into the cell a second nucleic acid molecule encoding a tTA, to form a modified cell, administering the modified cell to the is subject, and modulating the concentration of a tetracycline, or analogue thereof, in the subject. The first and second nucleic acid molecule can be within a single molecule (e.g.

Abstract: Certain 3-(Pyrimidin-4-yl)-1-phenylpyridazin-4(1H)-ones of formula I ##STR1## including pharmaceutically acceptable salts thereof; in which g is 0,1,2,3,4 or 5;R.sub.1 independently represents halo; andR.sub.2 represents H, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl or optionally substituted phenyl;have utility in the treatment of seizures and/or neurological disorders such as epilepsy and/or conditions in which there is neurological damage such as brain trauma, cerebral ischaemia, haemorrhage, head injuries and stroke.

Abstract: Compounds of formula I ##STR1## in which A is S(O).sub.p or O;p is 0, 1 or 2;g is 0, 1, 2, 3, or 4;n is 2 or 3; andR.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are optional substituents have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, cerebral ischemia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, non-insulin dependent diabetes mellitus, hyperglycemia, and stress.

Abstract: Compounds of formula I ##STR1## including pharmaceutically acceptable salts thereof in which R.sub.1 represents a phenyl C.sub.1-6 alkyl group (in which the phenyl ring is optionally substituted by one or more of the following: halo, a C.sub.1-4 alkyl group, a C.sub.1-4 alkoxy group, hydroxy or trifluoromethyl) and the alkyl chain is optionally substituted by one or more C.sub.1-2 alkyl groups; R.sub.2 represents a C.sub.2-6 alkoxycarbonyl group; and R.sub.3 represents hydrogen or halo are disclosed, which are antirheumatic agents and are useful as modulators of cytokine synthesis, immunomodulatory agents, antiinflammatory agents and anti-allergic agents. Compositions containing these compounds and processes to make these compounds are also disclosed.