Abstract: The present invention relates to methods of and compositions for treating and relieving symptoms and disease associated with indications caused by a physiological drive to alleviate a sensation of anxiety. More specifically, the present invention relates to methods of and compositions for treating and relieving symptoms associated with substance abuse and withdrawal. The present invention relates to methods of and compositions for treating and relieving symptoms associated with addiction to antidepressants, opiates, nicotine or marijuana. In one method, a patient is treated with a composition that directly or indirectly modulates GABAA by modulating the expression of the GABAA receptor a4 subunit.

Abstract: The invention provides compositions and methods for the treatment and diagnosis of diseases or disorders amenable to treatment through modulation of expression of a gene encoding a Jun N-terminal kinase 1 (JNK1 protein.

Abstract: The present invention relates to a substance for the treatment of the phantom phenomena of acute tinnitus and/or phantom pain, a method for the diagnosis and for the treatment of these phantom phenomena.

Abstract: The present invention provides a compound of formula (I): wherein all variables are as defined herein, pharmaceutical formulations containing the same, processes for preparing the same and their use therapy.

Abstract: Described are controlled release nanoparticulate formulations comprising a nanoparticulate agent to be administered and a rate-controlling polymer which functions to prolong the release of the agent following administration. The novel compositions release the agent following administration for a time period ranging from about 2 to about 24 hours or longer.

Abstract: The present invention relates to the treatment of compulsive, impulsive and pervasive developmental disorders. More particularly, the methods described herein comprise administration of memantine to an individual suffering from such a disorder in an amount effective to relieve one or more symptoms of said disorder.

Abstract: Disclosed herein are non-nucleoside reverse transcriptase inhibitors having structural Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and the methods of their use thereof.

Abstract: Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer therapeutics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.

Abstract: Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is a psychotherapeutic agent and the second compound is a anticonvulsant. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual with a psychotherapeutic agent and an anticonvulsant.

Abstract: The invention concerns compounds according to general formulae 1, wherein G1 is an amine. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.

Abstract: The present invention relates to a benzamide derivative comprising a head, spacer and cap group wherein the spacer includes a benzene ring substituted with an additional spacer and wherein the additional spacer is an unsaturated group.

Abstract: The present invention relates to a method for reducing infarction comprising administering to a patient ion need thereof a therapeutically effective amount of a composition comprising as an active ingredient a vasopressin antagonist compound and to a composition useful therefor. The present invention also relates to a method for reducing infarction comprising administering to a patient in need thereof a therapeutically effective amount of a combination of a vasopressin antagonist compound and a beta-blocker and to combinations useful therefor. The methods, compositions and combinations of the present invention can be used for reducing infarction in the heart (myocardial infarction) and the brain (stroke).

Abstract: A compound of formula (I); or a salt or solvate thereof, wherein: the dotted line indicates the optional presence of a double bond between C2 and C3; R2 is selected from —H, —OH, =0, ?CH2, —CN, —R, OR, halo, ?CH—R, O—SO2—R, CO2R and COR; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo, where R and R? are independently selected from optionally substituted C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R10 and R11 either together form a double bond, or are selected from H and YRY, where Y is selected from O, S and NH and R is H or C1-7 alkyl or H and SOxM, where x is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; each X is independently a heteroarylene group; n is from 1 to 6; and RE is C1-4 alkyl. The compound is useful for the treatment of proliferative diseases.

Abstract: The invention relates to methods of and treatments for using pharmaceutical compositions from a class of compounds that directly or indirectly selectively modulates GABAA chloride channel activity to treat alcohol and/or stimulant substance abuse. The present invention also relates to methods of, and protocols for, relieving symptoms associated with alcohol and/or stimulant substance abuse in a comprehensive treatment plan. More specifically, the present invention relates to the use of a selective chloride channel modulator, such as flumazenil, to treat alcohol and/or psychostimulant dependency, the withdrawal symptoms associated therewith, and the cravings associated therewith.

Abstract: A process for the preparation of polymorph Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2.3-b][1,5]benzodiazepine, or olanzapine.

Abstract: Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.

Abstract: Compounds of formula (I): formula (I) and salts, solvates, chemically protected forms, and prodrugs thereof, are disclosed wherein R2 is selected from: an optionally substituted napthyl group; an optionally substituted thiophenyl or furanyl group; and a phenyl group substituted by: one or more chloro or fluoro groups; an ethyl or propyl group; a 4-t-butyl group; a 2-methyl group; or two methyl groups in the 2- and 6-positions.

Abstract: A family of imidazole compounds useful for inhibiting the activity of prenyl transferases. The compounds are covered by the following formula: wherein X is (CHR11)n3(CH2)n4Z(CH2)n5 where Z is O, N(R12), S, or a bond; Y is CO, CH2, CS, or a bond; R1 is or N(R24R25); and the remaining substituents are as defined in the disclosure.

Abstract: A rapidly disintegrating dosage form containing magnesium carbonate heavy is described, which disintegrates upon contact with moisture. The dosage forms can be either dispersible or orodispersible tablets and can accommodate widely different active principles. The magnesium carbonate heavy is found to be an excellent dispersant under basic and neutral conditions, and gives the tablets a smooth mouth-feel.

Abstract: Compounds of the formula: (I) or solvate thereof, wherein: R2 is an optionally substituted C5-20 aryl group; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NHRR?, nitro, Me3Sn and halo; R? is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms and/or aromatic rings; X is selected from O, S, or NH; z is 2 or 3; M is a monovalent pharmaceutically acceptable cation; R2?, R6?, R7?, R9?, X? and M? are selected from the same groups as R2, R6, R7, R9, X and M respectively, or M and M? may together represent a divalent pharmaceutically acceptable cation.

Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.

Abstract: The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of treating neoplastic conditions.

Abstract: This disclosure relates to amides, aryl sulphonamides, aryl ureas, and ?,?-diketones derivatives useful as carboxylesterase esterase inhibitors. The disclosure is also directed to the use of these compounds as selective human intestinal carboxylesterase inhibitors and insect carboxylesterase inhibitors. The disclosure is also directed to pharmaceutical compositions and pesticide formulations containing these compounds, and to methods for treating or ameliorating the toxic effects following administration of drugs such as cancer therapy drugs, treating or ameliorating the effects of a drug overdose, and to the use of the compounds for increasing the effectiveness of insecticides and pesticides.

Abstract: A method for treating or preventing symptoms of hormonal variation includes administering an effective amount of a receptor antagonist to a subject having one or more symptoms of hormonal variations, wherein the receptor antagonist binds to at least one selected from the group consisting of a serotonin type 2A (5-HT2A) and a dopamine type 2 (D2) receptors.

Abstract: An olanzapine pharmaceutical composition such as a tablet is made using anhydrous lactose as an excipient.

Abstract: This invention relates to phosphate prodrugs of a farnesylated dibenzodiazepinone, to processes of their manufacture, to pharmaceutical compositions comprising the prodrugs, and to their use in the treatment of neoplasms.

Abstract: Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or —CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, NO2, CN, COR4, C(O)OR4, CONR5R6, NR5R6, SO2NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyly is unsubstituted or substituted with a phenyl; R4 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally

Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.

Abstract: The invention relates to the use of flumazenil in developing a drug used for the sequential administration of small quantities of flumazenil at short intervals, until a therapeutically effective quantity is administered to treat alcohol dependence.

Abstract: The present invention is directed to a method of inhibiting CYP3A4 induction. The method involves administering a compound of the following formula: R1—X—(CH2)n—N?C?S with R1, X, and n defined herein, binds to a Pregnane X Receptor or Steroid and Xenobiotic Receptor (SXR or NR1I2) under conditions effective to inhibit CYP3A4 gene induction. The present invention also include a method of administering a compound, described herein, together with the CYP3A4 inducer to prevent a loss of efficacy in the subject to whom the CYP3A4 inducer is repeatedly administered. In addition, such compounds can be administered to block the interaction between a CYP3A4 inducer and another drug being administered that is a substrate of CYP3A4.

Abstract: A method for treatment of HIV infection includes administering at least one anti-HIV drug, such as a reverse transcriptase inhibitor, to a patient in need of such treatment and administering an extract from inflammatory tissue inoculated with vaccinia virus to the patient following the administration of the at least one anti-HIV drug. The extract maintains suppressive action on HIV replication, even if the administration of the anti-HIV drug is terminated.

Abstract: The present invention provides synergistic combinations for the treatment of conditions associated with pain including acute pain, e.g., postoperative pain, chronic pain, inflammatory pain, neuropathic pain and pain associated with migraine. In particular, the present invention relates to the use of an allosteric adenosine A1 receptor enhancer in conjunction with opioid analgesics or 2-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA)/kainate antagonists for alleviating pain, e.g., postoperative pain.

Abstract: O-(3-piperidino-2-hydroxypropyl)-nicotinic amidoxime or a pharmaceutically suitable acid addition salt thereof (BGP-15) can be used for the prevention or reduction of weight gain or obesity in a patient treated with an antipsychotic drug or an antidepressant drug or an antiepileptic drug.

Abstract: The subject invention pertains to methods of treating mental illnesses or conditions characterized by a decreased function of NMDA receptors and/or excessively enhanced glutamate release and activity of non-NMDA receptors (AMPA and/or kainate). Specifically disclosed are methods utilizing BrPhe, or isomers of analogs thereof, for treating or preventing mental illness or conditions such as schizophrenia.

Abstract: A pyrrolobenzodiazepine dimer compound of Formula (I): or pharmaceutically acceptable salt or solvate thereof is useful as a therapeutic agent for the treatment of leukaemias, especially B-cell leukaemias, that exhibit resistance to other chemotherapeutic drugs, wherein: the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3; R2 and R3 are independently selected from —H, ?O, ?CH2, —CN, —R, OR, halo, ?CH—R, O—SO2—R, CO2R and COR; R6, R7 and R9 are independently selected from II, R, OII, OR, SII, SR, NII2, NIIR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R10 is a carbamate-based nitrogen protecting group and R15 is either O—R11, wherein R is an oxygen protecting group, or OH, or R10 and R15 together form a double bond between N10 and C11; R? is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms and/or aromatic rings, and each X is

Abstract: This invention relates to methods of inhibiting growth and/or proliferation of a neoplastic cell, and methods of treating neoplasms using the farnesylated dibenzodiazepinone compound of Formula I.

Abstract: This invention relates to CCK-A agonists of Formula (I) wherein R1-R4, A, B, X, D, E and G are as defined in the specification, as well as, among other things, pharmaceutical compositions containing the compounds and methods of use of the compounds and compositions. The compounds are useful in treating diabetes.

Abstract: Substituted quinolone carboxylic acids and their derivatives are described. These compounds modulate the effect of ?-aminobutyric acid (GABA) via a novel site on the GABAA receptor complex in a therapeutically relevant fashion and may be used to ameliorate CNS disorders amenable to modulation of the GABAA receptor complex.

Abstract: A new treatment methodology and pharmacological composition for the treatment and remission of Parkinson's Disease and other neurological diseases are provided. The medication and treatment are based on the use of a combination of a phosphodiesterase inhibitor medication, commonly used to treat male erectile dysfunction, and a high-dose of serotonergic synaptic reuptake inhibitor medication, commonly used to treat depression, anxiety disorders, obsessive compulsive disorder and various panic phobias. The treatment regime is based upon the discovery that the primary cause of PD and various other related neurological conditions is dysfunction in the serotonergic pathways involving the brainstem, nucleus of Raphe, and various projecting serotonergic fibers.

Abstract: The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments.

Abstract: The invention relates to the use of flumazenil in developing a drug used for the sequential administration of small quantities of flumazenil at short intervals, until a therapeutically effective quantity is administered to treat alcohol dependence.

Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.

Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.

Abstract: An agent for increasing the sugar-transporting capacity and an agent for preventing and/or treating diabetes, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, impaired glucose tolerance or adiposis, which contains a lactam compound or a pharmaceutically acceptable salt thereof as the active ingredient.

Abstract: The present invention provides tricyclic carboxamide compounds and methods and pharmaceutical compositions for their use in treatment, prevention, or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and/or suppression of preterm labor, suppression of labor at term prior to caesarean deliver, and for the treatment of dysmenorrhea. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

Abstract: The present invention relates to methods of treatment using the compound (+)-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate, as a sole active agent or in combination with other pharmacological agents.

Abstract: The invention is directed to a series of novel crystalline olanzapine forms, in particular hydrated and solvated crystalline forms of olanzapine, methods of use in pharmaceutical compositions, and method of treating psychiatric disorders using the crystalline forms. One series of the crystalline forms are hydrates, i.e. water containing crystals, wherein water may be present in a ratio of about 2:1.5 to a ratio of about 1:3 olanzapine:water, while another includes solvates such as an isobutanol solvate. The olanzapine crystalline forms include Forms H, G, Y, X, K, S, Q, Z, and J.

Abstract: The invention concerns a benzodiazepin derivative of formula (I) and their use for treating dyslipidemia, atherosclerosis, diabetes and its complications.

Abstract: 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system.