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filingDate 2000-05-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2004-09-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-036320-A1
titleOfInvention SUBSTITUTED BENZOLACTAMA COMPOUNDS, THEIR USE IN THE MANUFACTURE OF MEDICINES AND THE COMPOSITIONS OF THE SAME
abstract Claim 1: A method of treating a disorder or condition selected from dysthymia, major depressive disorder, pediatric depression, generalized anxiety disorder, obsessive-compulsive disorder, panic disorder, phobias such as social phobia and agoraphobia; post-traumatic stress disorder, borderline personality disorder, acute pain, chronic, migraine pain, angiogenesis, sunburn, urinary incontinence, inflammatory disorders such as rheumatoid arthritis, osteoarthritis, psoriasis and asthma; emesis, including acute, delayed and anticipated emesis in which the state or the emetic agent is chemotherapy, radiation, surgery, movement, migraine or any other state or emetic agent; disorders caused by Helicobacter pylory, cardiovascular disorders, ophthalmic disorders, urinary tract inflammation, psychosis, schizophrenia, behavior disorder, disruptive behavior disorder, bipolar disorder, movement disorders such as Tourette's syndrome, akinesia-stiffness syndrome, movement disorders associated with Parkinson's disease, tardive dyskinesia and other dyskinesias, cognitive disorders such as dementia (including age-related dementia and senile dementia of the Alzheimer type) and memory disorders; eating disorders such as anorexia nervosa and bulimia nervosa, attention deficit hyperactivity disorder, chronic fatigue syndrome, premature ejaculation, premenstrual syndrome, premenstrual dysphoric disorder, chemical dependencies and addictions, stress-related somatic disorders, neuralgia , peripheral neuropathy, gastroesophageal reflux disease, reflex sympathetic dystrophy, such as shoulder / hand syndrome; hypersensitivity disorders such as hypersensitivity to poison ivy; fibromyalgia, angina, Reynaud's disease, rheumatic diseases such as fibrositis; eczema, rhinitis, allergies, post-herpetic neuralgia, cystitis, inflammatory bowel disease, irritable bowel syndrome, colitis, fibrous and collagen disorders such as scleroderma and eosinophilic fascioliasis; blood circulation disorders due to vasodilation, and disorders related to immune induction or suppression such as systemic lupus erythematosus, in a mammal, including a human being, comprising administering to the mammal in need of such treatment a quantity of a compound of formula chemistry (1), in which W is methylene, ethylene, propylene, vinyl, -CH2-O-, -O-CH2, -CH2-S- or -S-CH2-; R1, R2 and R3 are independently hydrogen, C1-3 alkyl, C1-3 alkoxy-C1-3 alkyl or halo-C1-3 alkyl, with the proviso that when W is methylene, neither R2 nor R3 is hydrogen; or one of R2 or R3 can be hydroxy; X is halo, C1-3 alkoxy, C1-3 alkyl, halo C1-3 alkoxy or C1-3 alkenyl; Y is -NH or -O-; Q is oxygen or sulfur and has a double bond with the carbon to which it is attached, or Q is CH3 and has a single bond with the carbon to which it is attached; and T is (2S, 3S) -2-diphenylmethylquinuclidin-3-yl, (2S, 3S) -2-diphenylmethyl-1-azanorbornan-3-yl; or (2S, 3S) -2-phenylpiperidin-3-yl, the phenyl group of said (2S, 3S) -2-phenylpiperidin-3-yl being optionally substituted with one or more substituents, preferably 0 to 3 substituents, selected independently between halo, C1-6 alkyl optionally substituted with 1 to 7 fluorine atoms, C1-6 alkoxy optionally substituted with 1 to 7 fluorine atoms, amino, cyano, nitro, C1-6-amino alkyl and di [alkyl C1-6] amino; and the dashed line represents an optional double bond; with the proviso that R1 cannot be (C1-3 alkoxy) -CH2- or halo-CH2-; or of a pharmaceutically acceptable salt thereof, which is effective in the treatment of such disorder or condition. Claim 6: A pharmaceutical composition for the treatment of a disorder or condition selected from dysthymia, major depressive disorders, pediatric depression, generalized anxiety disorder, obsessive-compulsive disorder, panic disorder, phobias such as social phobia and agoraphobia; post-traumatic stress disorder and borderline personality disorder in a mammal, comprising an amount of a compound of formula (1), or a pharmaceutically acceptable salt thereof, which is effective in treating such disorder or condition, and a pharmaceutically acceptable vehicle.
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