Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

Abstract: Compounds of formula (I); wherein R represents various substituent groups, are useful as inhibitors of glucosylceramide synthase.

Abstract: The present invention provides methods of treating cognitive deficits associated with mental retardation. The methods comprise combining cognitive training protocols and a general administration of phosphodiesterase 4 inhibitors.

Abstract: P-glycoprotein transporter (P-gp) acts as a pump at the blood-brain barrier to exclude a wide range of xenobiotics (e.g., toxins, drugs, etc.) from the brain and is also expressed in a tumor in response to exposure to established or prospective chemotherapeutics (a phenomenon known as multidrug resistance). This invention concerns the preparation and use of radiotracers for imaging P-gp function in vitro and in vivo. Radiotracers of the present invention are avid substrates for P-gp and have structures based on N-Desmethyl-loperamide.

Abstract: The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X?. In one embodiment, the present invention provides a prodrug compound of Formula I: where R1-R5 are defined in the written description of the invention.

Abstract: Chemical agents, such as derivatives of hydroxypiperidine moieties, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of enzymes and structural polypeptides present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.

Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.

Abstract: [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder. [Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.

Abstract: Provided are pharmaceutical compositions and methods of treatment or prophylaxis of certain neuropsychiatric conditions, in particular mood disorders. The compounds are of the general Formula I-V as described herein.

Abstract: The film preparation of the present invention includes: a drug-containing intermediate layer containing loperamide hydrochloride, a terpene and a film-forming agent; and coating layers containing a film-forming agent and a plasticizer (but not a terpene) and laminated on both sides of the drug-containing intermediate layer. As a bitter taste derived from loperamide hydrochloride is thereby masked, uncomfortable sensation when taking the film preparation can be reduced. Furthermore, as this film preparation is rapidly dissolved (i.e., has a rapidly dissolving property) only with moisture in the oral cavity, it begins to work quickly and is very convenient when it is carried and taken.

Abstract: Methods of attenuating the toxic or medically undesirable effects of drugs and toxins in a human by administering to a human an injectable formulation comprised of a dispersion of particles comprised of reversed cubic or reversed hexagonal lyotropic liquid crystalline material. The particles absorb or adsorb or otherwise sequester and attenuate the effect of drugs and toxins, and may be used as a rescue or reversal agent, or as a prophylaxis. The invention is especially applicable in reversing adverse effects of local anesthetics inadvertently delivered systemically, and attenuating the therapeutic effects of general anesthetics in the course of treatment.

Abstract: A transdermal patch having a top region containing an antagonist followed by a bottom region containing an agonist, whereby the bottommost end of the bottom region is secured to the skin of the patient for delivering a prescribed dosage of agonist to the patient over a predetermined period of time, the antagonist will be released by migrating or moving from the top region through the bottom region to the patient to prevent overdose. Visual indicators are provided in the patch for changing color to separately indicate the operation of the patch, delivery of prescribed dosage, and/or overdosage.

Abstract: The present invention is concerned with the use of combinations of opioid agonists and antagonists for treating Crohn's disease.

Abstract: The subject invention provides methods for reducing stroke rate, methods for preventing atrial remodeling, and methods for reversing atrial remodeling by administering a multiple ion channel blocker anti-arrhythmic to reduce atrial fibrillation (AF) episode duration and an anticoagulant (AC). According to some methods of the invention, the average AF episode duration can be reduced to less than about 24, 5, 3 or 1 hour(s), and the maximum AF episode duration may be reduced to less than about 20, 10 or 5 hours. According to some methods of the invention, the reduced stroke rate upon administration of multiple ion channel blocker and AC is less than the age-adjusted overall stroke rate. Further, some methods provide that patients who were refractory to one or more anti-arrhythmic drugs prior to administration of the multiple ion channel blocker may also be treated.

Abstract: The present invention provides N-substituted-2(1H) pyridones or the pharmaceutical acceptable salts thereof, and the pharmaceutical preparations containing the compounds. The compounds of the present invention can be used to treat various fibrotic diseases effectively, e.g., hepatic fibrosis.

Abstract: The present specification provides drug delivery platforms useful for the controlled release of a compound over time in an individual.

Abstract: The present invention is directed to novel alkynyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.

Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.

Abstract: The invention relates to oxycarbamoyl compounds of Formula I: The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: This invention relates to novel compounds of the Formula (I), (I*), (Ia), (Ib), (Ic), (Id), (Ie), (If), (If*), (Ig), (Ih), (Ij), (Ik), (ll1-3), (Im1-3), (In1-3), (lo1-2), (Ip1-9), (Iq1-9), (Ir1-9) and (Is1-3) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.

Abstract: The present invention provides methods for treating a flavivirus infection, including hepatitis C virus (HCV) infection, in an individual suffering from a flavivirus infection. In some embodiments, the methods involve administering to an individual in need thereof an effective amount of an agent that inhibits enzymatic activity of a membrane-bound ?-glucosidase inhibitor. In other embodiments, the methods involve administering to an individual in need thereof effective amounts of an ?-glucosidase inhibitor and at least one additional therapeutic agent.

Abstract: The invention relates to crystalline free base forms of biphenyl-2-ylcarbamic acid 1-[2-(4-{[(R)-2-(3-formylamino-4-hydroxyphenyl)-2-hydroxyethylamino]methyl}-2,5-dimethylphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also relates to pharmaceutical compositions containing or prepared from such crystalline forms; processes and intermediates useful for preparing such crystalline forms; and methods of using such crystalline forms to, for example, treat a pulmonary disorder.

Abstract: The present application describes prodrugs of the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.

Abstract: Sulfonamide derivatives act as ion channel antagonists. The compositions are useful for treating or relieving pain-related conditions.

Abstract: This invention relates to novel compounds of the Formula (I), any of the formulas I1-I26 Ia1-3-Ij1-3 or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

Abstract: Novel compounds inhibiting the integrin ?2?1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin ?2?1/GPIa-IIa-mediated activity.

Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.

Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.

Abstract: This invention relates to novel 4-benzhydryloxy-tetraalkyl-piperidine derivatives of Formula (I), any of its stereoisomers or any mixture of its stereoisomers, or an N-oxide thereof, or a pharmaceutically acceptable salt thereof, wherein Ra represents hydrogen or C1-6-alkyl; Rb and Rc independent of each other represent a phenyl group, which phenyl group is optionally substituted with one or more substituents independently selected from the group consisting of halo, trifluoromethyl, trifluoromethoxy, cyano, C1-6-alkoxy and methylenedioxo; R?, R?, R?? and R?? independent of each other represent C1-6-alkyl; and with the proviso that the compound is not 4-benzhydryloxy-1,2,2,6,6-pentamethyl-piperidine, useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: The present invention relates to the field of life needs and more particularly to the therapeutic field. The invention relates more particularly to pharmaceutical compositions for helping the takers of addictive drugs to return to abstinence, in the form of a combination of two medicaments constituted of a partial or complete ligand of dopaminergic receptors—in particular of the D1, D2 and D3 receptors, and having direct prodopaminergic activity, and of an indirect prodopaminergic product, in the form of a pharmaceutical composition for oral, parenteral or transdermal administration. The invention also relates to a method for combating the various forms of addiction to licit or illicit drugs.

Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: The present invention provides a dermatological and/or cosmetic composition which includes a methoxycinnamate, and a cyclic nitroxide. The present invention further provides a method of synthesizing photo absorbing-antioxidant compounds and their use in dermatological and/or cosmetic compositions. In addition, the present invention relates to the use of methoxycinnamate, and nitroxide compounds for the preparation of a composition for the dermatological and/or cosmetic treatment of skin.

Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A1, A2, R1, R2, R3 and R4 have the significance given in claim 1.

Abstract: Low viscosity biodegradable polymer solutions of a liquid biodegradable polymer and biocompatible solvent and methods of using the compositions to form a biodegradable liquid polymer implant are provided.

Abstract: The invention relates to crystalline free base forms of biphenyl-2-ylcarbamic acid 1-[2-(4-{[(R)-2-(3-formylamino-4-hydroxyphenyl)-2-hydroxyethylamino]methyl}-2,5-dimethylphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also relates to pharmaceutical compositions containing or prepared from such crystalline forms; processes and intermediates useful for preparing such crystalline forms; and methods of using such crystalline forms to, for example, treat a pulmonary disorder.

Abstract: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent.

Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or a methyl group, R2 represents a bromine atom, a fluorine atom or a trifluoromethyl group. Medicinal products containing the same which are useful in treating cognitive disorders associated with pathologies of the central nervous system.

Abstract: The present invention relates to the use of sulfonyl-substituted 2-sulfonylaminobenzoic acid N-phenylamides of the formula I, wherein A and R1 to R6 have the meanings indicated in the claims, for treating pain and for manufacturing a medicament for the treatment of pain.

Abstract: Described herein are methods for effectively and accurately measuring a patient response upon administration of one or more drugs to the patient. The methods are more sensitive than current methodologies. Also described herein are compositions comprising an analgesic and a sufficient amount of an antihistamine to enhance the analgesic properties of the analgesic. With respect to these compositions, the methods described herein are useful for evaluating qualities of pain, definite improvement, and one or more bodily functions of a subject afflicted with pain. The compositions described herein are useful in improving the quality of pain in a subject or a bodily function of a subject afflicted with pain or definite improvement of a subject afflicted with pain.

Abstract: The disclosure relates to pharmacotherapy of a psychiatric disorder which is schizophrenia and/or anxiety, wherein schizophrenia includes schizophrenia related disorders such as brief psychotic disorders, delusional disorders, schizoaffective disorders, and schizophreniform disorders, and anxiety includes panic disorders, obsessive-compulsive disorders (OCD), post-traumatic stress disorders (PTSD), social phobia or social anxiety disorders, specific phobia, and generalized anxiety disorders (GAD). The compounds of the disclosure are useful for the treatment of the above psychiatric disorders alone or in combination with other therapeutical agents effective in the treatment of schizophrenia and/or anxiety disorders.

Abstract: The present invention relates to a series of substituted bicyclic[3.1.0]heteroaryl amides of the Formula I, wherein A, Q, X, Y, Z and R1-R5 groups are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

Abstract: [Problems] To provide an antagonist of a melanin-concentrating hormone receptor, which is useful as a medicine for a central nervous system disease, a cardiovascular disease or a metabolic disease. [Means for Solving Problems] The antagonist comprises, as an active ingredient, a compound represented by the formula (I) wherein R1a and R1b independently represent a hydrogen atom or a C1-6 alkyl group; R2a, R2b, R3a and R3b independently represent a hydrogen atom, a C1-6 alkyl group, or the like; Y represents H or —OH; Z represents —OR8, or the like; R8 represents a hydrogen atom, a C1-6 alkyl group which may have a substituent, or the like; R9a and R9b independently represent a hydrogen atom, a C1-6 alkyl group, or the like; Ar1 represents an aromatic carbon ring group, or an aromatic heteroring group; Ar2 represents a group produced by removing two hydrogen atoms from an aromatic carbon ring, or the like; and the ring group A represents an unsaturated heteroring group.

Abstract: The invention relates to a compound of formula (I) wherein A1 and R1 to R5 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: Disclosed herein are compositions and methods for treating a psychiatric disorder or symptoms thereof in a patient. The compositions comprise a compound that modulates KCNQ (Kv7) potassium channel activity and the methods include administering an effective amount of the compound that modulates KCNQ (Kv7) potassium channel activity.

Abstract: Disclosed are compounds that block off-notes in consumables and methods of blocking off-notes in consumables including off-notes provided by sweeteners such as stevioside, swingle extract, glyccerhizin, perillartine, naringin dihydrochalcone, neohesperidine dihydrochalcone, mogroside V, rubusoside, rubus extract, and rebaudioside A, and artificial sweeteners such as aspartame, saccharin, acesulfame K (Acesulfame potassium), sucralose and cyclamate.

Abstract: The present invention is to provide a crystalline form of (2R,4S)-1-{N-(3,5-bistrifluoromethylbenzyl)-N-methyl}aminocarbonyl-2-(4-fluoro-2-methylphenyl)-4-(2-hydroxyethylaminocarbonyloxy)piperidine or a solvate thereof.

Abstract: This invention provides molecular markers that are prognostic and/or diagnostic for a psychiatric disorder. In particular, genes are identified whose expression is altered in schizophrenia and/or bipolar disorder thereby providing prognostic and diagnostic markers for the disorder. In addition genes are identified whose dysregulation provides markers that allow diagnostic distinction between schizophrenia and bipolar disorder.