Abstract: The present invention relates to a novel urea derivative represented by the following formula (I), which is useful as an anti-cancer agent: 1

Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human &agr;2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the &agr;2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: Compounds of formula I 1

Abstract: A compound of the formula: wherein R1 is hydrogen or halogen, R2 is hydroxy, acyl(lower)alkoxy, hydroxy(lower)alkyl, lower alkoxy(lower)alkyl, lower alkylthio(lower)alkyl, mono(or di or tri)halo(lower)alkyl, (ethoxycarbonyl)amino, sulfamoylamino, (dimethylsulfamoyl)amino, N,N-di(lower)alkylamino(lower)alkyl, hydroxyimino(lower)alkyl, lower alkoxyimino(lower)alkyl, acyl, lower alkoxycarbonyl, carbamoyl, di(lower)alkylcarbamoyl, (amino(lower)alkyl)carbamoyl, N,N-di(lower)alkylamino(lower)alkylcarbamoyl, guanidinocarbonyl, morpholinylsulfonyl, sulfamoyl, lower alkylsulfamoyl, (lower alkylsulfonyl)(lower)alkyl, guanidinocarbonyl(lower)alkenyl, lower alkylthio, cyano, acyl(lower)alkyl, acyl(lower)alkenyl, aryl which has one or more substituent(s) or a heterocyclic group which has one or more substituent(s), and X is —O—, or a salt thereof.

Abstract: Benzopyran derivatives and analogs are disclosed as useful for the treatment and/or prophylaxis of degenerative diseases such as Huntingdon's chorea, schizophrenia, neurological deficits associated with AIDS, sleep disorders (including circadian rhythm disorders, insomnia and narcolepsy), tics (e.g. Giles de la Tourette's syndrome), traumatic brain injury, tinnitus, neuralgia, especially trigeminal neuralgia, neuropathic pain, dental pain, cancer pain, inappropriate neuronal activity resulting in neurodysthesias in diseases such as diabetes, MS and motor neurone disease, ataxias, muscular rigidity (spasticity), temporomandibular joint dysfunction.

Abstract: 4,4-difluoro-2,3,4,5-tetrahydro-1H-1-benzoazepine compounds or salts thereof and pharmaceutical compositions containing 4,4-difluoro-2,3,4,5-tetrahydro-1H-1-benzoazepine compounds, or salts thereof, and a pharmaceutically acceptable carrier. The chemical structure of these compounds is characterized by a difluoro group on a ring carbon atom adjacent to an azepine ring carbon atom substituted with a methylidene group. Pharmaceutical compositions containing these compounds are particularly useful as oxytocin antagonists and are effective in inhibiting threatened premature birth or abortion and precesarean birth, and are effective as a remedy for dysmenorrhea and other such conditions.

Abstract: This invention is directed to compounds of the formula 1

Abstract: A benzoheterocyclic derivative of the following formula [1]: and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity, vasopressin agonistic activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist, vasopressin agonist or oxytocin antagonist.

Abstract: Substituted indolinones of general formula having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are: 3-Z-[1-(4-(N-Benzyl-N-methyl-aminomethyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone and 3-Z-[1-(4-(2,3,4,5-Tetrahydro-benzo(d)azepin-3-yl-methyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone.

Abstract: This invention is directed to compounds of the formula 1

Abstract: The present invention relates to compounds of formula (I) 1

Abstract: A method of reducing cravings in a mammal to food or an addictive substance is disclosed. The method comprises administering to the mammal an effective amount of a D1/D5 antagonist or a D1/D5 partial agonist alone or in combination with other specified CNS compounds.

Abstract: Halo-alkoxycarbonyl derivatives are provided as prodrug moieties for pharmaceutical agents containing a basic or polar nitrogen containing functionality. The prodrugs are provided as pharmaceutical compositions as well as in methods of treatment.

Abstract: This invention relates to a compound of the Formula I

Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Abstract: Disclosed are methods for modifying or regulating at least one of glucose or lipid metabolism disorders which comprises administering to a human or vertebrate subject a D1 dopamine agonist in conjunction with a dopamine D2 agonist where the conjoined administration is effective to improve at least one of the following lipid and glucose metabolic indices: body weight, body fat, plasma insulin, plasma glucose and plasma lipid, and plasma lipoprotein. In preferred embodiments, the administration of the D1 dopamine agonist and the D2 dopamine agonist is conducted at a predetermined time.

Abstract: A method of reducing cravings in a mammal to nicotine or tobacco is disclosed. The method comprises administering to the mammal an effective amount of a D1/D5 antagonist or a D1/D5 partial agonist alone or in combination with other specified CNS compounds.

Abstract: A topical composition containing capsazepine and particularly suitable for treating neurogenic skin disorders and diseases, especially painful and/or pruriginous diseases, as well as for treating sensitive skin and eyes, in particular, the composition is useful for preventing and/or controlling skin and/or eye irritation, itching, erythema and dysaesthesia and heating of the skin, eyes and mucosa, as well as for reducing the irritancy of an active substance having an irritant side-effect.

Abstract: The subject matter of the present invention concerns a process for the isolation of the alkaloid galanthamine; the galanthamine itself which has been produced according to this process; the use of the galanthamine thus produced in galenic preparations; and the galanthamine thus produced for treating narrow-angle glaucoma, Alzheimer's disease, as well as alcohol and nicotine dependence.

Abstract: A series of tacrine derivatives has be synthesized and disclosed. These tacrine derivatives were claimed to be new and be useful for the treatment of Alzheimer's disease alone or in combination with other drugs for Alzheimer's disease. These tacrine derivatives may be formulated into suitable pharmaceutical dosage forms for the treatment of Alzheimer's disease.

Abstract: The present invention is directed to the use of a group of ACE inhibitors to stimulate angiogenesis in mammals or in mammalian tissue in vitro. Specifically, the present invention is directed to inducing or enhancing angiogenesis through the administration of a group of ACE inhibitors and to ACE inhibitor-containing compositions for effecting the inducement or enhancement of angiogenesis. The ACE inhibitors may also be useful in the promotion of angiogenesis, such as in the promotion of wound healing, bone healing, and in the treatment of bums, as well as in promoting the formation, maintenance, and repair of tissue. In a preferred embodiment, the ACE inhibitor, quinapril, or quinaprilat, is used to treat, prophalactically or otherwise, mammals in need of angiogenic-treatment.

Abstract: The present invention relates to the pharmaceutical treatment of pain. In particular, the present invention relates to the topical use of kappa opioid receptor agonists and partial agonists for the prevention or alleviation of pain in the eye.

Abstract: Compositions and methods for treating otic pain are disclosed. In particular, the invention discloses compositions and methods of using kappa opioid agonists locally for the prevention or alleviation of otic pain.