Abstract: The present invention relates to a novel two cyclic cinnamide compound and a pharmaceutical agent comprising the compound as an active ingredient. The two cyclic cinnamide compound represented by the general formula (I): wherein represents a single bond or a double bond; Ar1 represents a phenyl group or pyridinyl group that may be substituted with 1 to 3 substituents; R1 and R2 each represent a C1-6 alkyl group, a hydroxyl group, or the like; Z1 represents a methylene group or vinylene group, which may be substituted with 1 or 2 substituents selected from Substituent Group A1, an oxygen atom, or an imino group that may be substituted with a substituent selected from Substituent Group A1; and p, q, and r each represent an integer of 0 to 2, which has an effect of reducing A?40 and A?42 production, and thus is particularly useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? such as Alzheimer's disease or Down's syndrome.

Abstract: Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.

Abstract: The invention relates to novel secondary amine derivatives of formula (I) and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.

Abstract: Pharmaceutical compounds, pharmaceutical compositions and methods of treatment are disclosed, wherein a compound comprises a targeting moiety which, in free form, binds a cell receptor with a dissociation constant Kd of less than about 10?7 M, and a pharmaceutically active moiety, wherein the targeting moiety is other than an oligopeptide, a polypeptide, a peptidomimetic, a protein or a protein domain, and wherein the targeting moiety and the pharmaceutically active moiety are covalently attached. In some aspects, the targeting moiety binds a sigma-2 receptor with high affinity and high specificity, and the pharmaceutically active moiety is a pro-apoptotic peptide moiety. Methods of cancer treatment are disclosed comprising administering a disclosed pharmaceutical compound to a subject in need of thereof. The treatments selectively induce apoptosis in cancer cells. These methods can further comprise co-administration of radiation therapy and/or an additional chemotherapeutic agent.

Abstract: The present invention relates to a drug combination capable of conferring therapeutic benefits in the treatment of both AIDS and malaria. In particular, it relates to a drug combination including at least one quinolinic antimalarial compound such as chloroquine or hydroxychloroquine, and at least one inhibitor of the Human Immunodeficiency Virus (HIV) protease enzyme. This drug combination is capable of inhibiting the replication of both HIV and Plasmodium sp. It also relates to the direct antimalarial effects of the HIV PIs.

Abstract: Compounds of formulae I and II: are disclosed as 5-HT3 inhibitors. Those compounds are useful in treating CINV, IBS-D and other diseases and conditions.

Abstract: The invention is directed to a compound of formula I, wherein R, R1, R2, R3 and R4 are as defined herein, or a pharmaceutically acceptable salt thereof, and its pharmaceutically composition, preparation and uses as an inhibitor of FGFs (fibroblast growth factors).

Abstract: Compounds of formula (I) are ligands of the CRTH2 receptor and are useful in the treatment of respiratory disease: Formula (I) wherein R1, R2, R3 and R4 each independently are hydrogen, C1C6alkyl, fully or partially fluorinated C1C6alkyl, halo, —S(O)nR10, —SO2N(R10)2, —N(R10)2, —C(O)N(R10)2, —NR10C(O)R9, —CO2R10, —C(O)R9, —NO2, —CN or —OR11; wherein each R9 is independently C1C6alkyl, aryl, heteroaryl; R10 is independently hydrogen, C1C6alkyl, aryl, or heteroaryl; R11 is hydrogen, C1C6alkyl, fully or partially fluorinated C1C6alkyl or a group —SO2R9; n is 0, 1 or 2; R5 is C1C6alkyl, fully or partially fluorinated C1C6alkyl. C1C6alkenyl, C1C6alkynyl, optionally substituted aryl, or optionally substituted heteroaryl; R6 is hydrogen, C1C6alkyl or fully or partially fluorinated C1C6alkyl; R7 and R5 are independently hydrogen or C1C6alkyl, or R7 and R5 together with the atom to which they are attached form a cycloalkyl group; and X is —CHR6—, —S(O)n—, —NR6SO2— or —SO2NR6— wherein n is 0, 1 or 2.

Abstract: The present invention provides compounds of general formula (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.

Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: The present invention relates to muscarinic receptor modulators, specifically, 7-oxo-2-azabicyclo[2.2.1]heptanes of formula (I) which are useful for the treatment of various diseases and conditions, for example, Alzheimer's disease, glaucoma, psychosis, particularly schizophrenia or schizophreniform conditions, mania, pain, bipolar disorder, depression, sleeping disorders, epilepsy, gastrointestinal motility disorders, urinary incontinence, and cognition enhancement.

Abstract: Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.

Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, m and n are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.

Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.

Abstract: A carboxamide compound represented by the formula (I): [wherein Q represents a nitrogen-containing 6-membered aromatic heterocyclic group optionally fused with a benzene ring, two or more ring constitutional atoms of the heterocyclic group are a nitrogen atom, and the heterocyclic group may be substituted with at least one group selected from the group consisting of a C1-C3 alkyl group etc.], and a plant disease controlling agent comprising this as an active ingredient.

Abstract: The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder.

Abstract: This invention relates to novel 9-aza-bicyclo[3.3.1]nonane derivatives 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: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.

Abstract: Compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R1 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R2 is H; or aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R3 is aryl, heteroaryl, cycloalkyl or heterocycloalkyl, all optionally substituted; X is a bond, —(CH2)m—N(R7)—(CH2)n—, —(CH2)m—O—(CH2)n—, —(CH2)m—S—(CH2)n—, —C(O)—, —CH(OH)—, —C(O)N(R7)—, —C(O)N(R7)-alkylene or —N(R7)C(O)—; R7 is H or alkyl; and m and n are each 0-6, provided that the sum of m and n is 0-6; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions thereof, and the use of said compounds in the treatment of cough, pain, anxiety, asthma, depression, alcohol abuse, urinary incontinence and overactive bladder are disclosed.

Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

Abstract: A combination comprising as components (a) the compound 3-(3-Dimethylamino-1-ethyl-2-methyl-propyl)-phenol, and (b) one or more non-steroidal anti-inflammatory drugs (NSAIDs); a pharmaceutical salt comprising said components; a compound derived from said components; a pharmaceutical formulation and a dosage form comprising said combination, salt, or compound; as well as a method of treating pain, e.g. chronic or acute pain, in a mammal characterized in that components (a) and (b) are administered simultaneously or sequentially to a mammal, wherein component (a) may be administered before or after component (b) and wherein components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.

Abstract: The present invention relates to pharmaceutical preparations in the form of aqueous solutions for the production of propellant-free aerosols.

Abstract: Norphenephrine and its salts are disclosed which have powerful metabolic enhancing effects in humans via oral administration. The metabolic enhancing properties include positive blood sugar regulation, increased thermogenesis and fat loss, increased anticatabolism/anabolism, decreased appetite, improved mental focus and psychological outlook and increased energy production and anti-fatigue actions.

Abstract: Embodiments of the present invention provide compositions for controlling a target pest including a pest control product and at least one active agent, wherein: the active agent can be capable of interacting with a receptor in the target pest; the pest control product can have a first activity against the target pest when applied without the active agent and the compositions can have a second activity against the target pest; and the second activity can be greater than the first activity.

Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

Abstract: This invention relates to Applicant's discovery that Metabolic Syndrome, a cluster of disorders stemming from a resistance to insulin, contributes directly to dementia, particularly Alzheimer's disease. Applicant's invention includes a screening method to determine susceptibility and diagnosis of dementia based on the risk factors for Metabolic Syndrome. Applicant's invention further includes methods for the prevention or treatment of dementia and other neurological conditions based on (1) minimizing insulin resistance, thereby preventing excess biosynthesis of insulin; (2) modulating the activity of IDE such that insulin competes less efficiently with ?-amyloid protein for the IDE; and (3) blocking the consequences of NMDA receptor activation, such as by minimizing the generation of NO and other harmful free radicals.

Abstract: Disclosed are compounds of the Formula III and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 R10, and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract: The invention relates to the use of piperidine derivatives encompassed from the general formula (I) for the control of pests, including arthropods and helminths, and a method for the control of pests.

Abstract: A carboxamide compound represented by the formula (I): [wherein Q represents a nitrogen-containing 5-membered heterocyclic group optionally fused with a benzene ring, R1 represents a C1-C3 alkyl group or the like, R2 represents a hydrogen atom or the like, and R3 represents a hydrogen atom.] has an excellent plant disease controlling effect.

Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

Abstract: Disclosed are compounds of Formula (I) wherein G, R2, A, D and E are as described in the specification, or pharmaceutically-acceptable salts, or in vivo-hydrolysable precursors thereof. Also disclosed herein is at least one method of making, at least one pharmaceutical composition containing, and at least one method for using at least one compound in accordance with Formula I.

Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

Abstract: Compounds from 14 Kenyan plants, including from the root of Dovyalis abyssinica and Clutia robusta have been characterized and isolated, and their uses are disclosed.

Abstract: The present disclosure relates to XIAP inhibitor compounds of the formula I.

Abstract: FGF receptor agonist compounds corresponding to the general formula: M1-L-M2 are disclosed in which M1 and M2, which may be identical or different, each represent, independently of one another, a monomer unit M, and L represents a linker group, wherein the monomer unit is of the general formula I.

Abstract: The present invention relates to compounds useful as modulators of TGR5 and methods for the treatment or prevention of metabolic, cardiovascular, and inflammatory diseases.

Abstract: This invention to antagonists that inhibit transporters and receptors. The invention also relates to partial inhibitors of transporters and receptors that allow partial transport or partial binding of a compound to the transporter or receptor. The invention also relates to compounds that differentially prevent transport or binding through a transporter or to a receptor. The invention also relates to the use of these compounds for treating certain diseases and disorders.

Abstract: The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) wherein Ra and Rb each denote a C1-6 alkyl group or the like; Xa denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.

Abstract: The invention relates to an inhalation device comprising plural of doses of a pharmaceutical composition in powder form, wherein the pharmaceutical composition comprises one or more, preferably one, anticholinergic, optionally in combination with a pharmaceutically acceptable excipient.

Abstract: A novel sleep regulating pharmaceutical formulation is introduced, typically implementing two principal drugs having actions which are reversive to one another, yet incorporated into a unitary solid dosage, and prepared for oral administration before bedtime. Usually, structure is configured to initially release a calmative or other sleep-compatible substance by prompt dissolution. The initial release is followed by a specific period of delay, which in basic formulations entails no release of any drug, and which allows a nominal interval of sleep. At the terminus of the delay, a final agent is released to induce wakeup. Incorporation of agents of opposite action within a unitary dosage form renders utility which is uniquely appropriate to the invention. In a preferred embodiment, delay of release and final delivery of wakeup agent are arranged by a dialysis membrane which eventually bursts as a result of osmotic pressure generated by a hydrophilic core.

Abstract: New quinuclidine amide derivatives having the chemical structure of general formula (I) and pharmaceutically acceptable salts thereof including quaternary salts of formula (II) are disclosed; as well as processes for their preparation, pharmaceutical compositions 10 comprising them and their use in therapy as antagonists of M3 muscarinic receptors.

Abstract: The invention relates to 2-aza-bicyclo[2.2.2]octane compounds and uses thereof. Particularly the invention relates to such compounds and their uses as pharmaceuticals in treating pyshoses such as schizophrenia and other diseases, disorders, or conditions.

Abstract: The present invention thus relates to the use of 1,2,3-substituted indolizine derivatives in the preparation of medicaments of use in the treatment of diseases related to pathological choroidal angiogenesis, which derivatives correspond to the following general formula (I):

Abstract: The present invention relates to improved methods and compositions for treating viral infections and other diseases and conditions that induce a cytokine storm. More particularly, the present invention relates to novel compositions comprising quercitin, and an anti-convulsant, such as phenytoin, in combination with mulivitamins as an anti-viral composition and methods of use thereof.

Abstract: Provided are compounds useful for treating diseases associated with a cerebral accumulation of Alzheimer's amyloid, such as Alzheimer's disease. Also provided are methods of treating or reducing the risk of developing ?-amyloid production, ?-amyloid deposition, ?-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer's amyloid by administering therapeutically effective amounts of the compounds. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer's amyloid in animals or humans by administering diagnostically effective amounts of the compounds.

Abstract: The present invention relates to heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof wherein the heterocycle comprises two double bonds which may be present at several positions, and which are represented by the dashed lines (---); the heterocycle contains two heteroatoms, W is N or NH; Y is CH, O or NH, wherein if Y is O, X1 is CH and X2 is C-Z-R2 or C—R3, wherein Z is NH, O, or S; and if Y is CH or NH, one of X1 and X2 is CH or N, wherein if X1 is CH or N, X2 is C-Z-R2 or C—R3, and if X2 is CH or N, X1 is C-Z-R2 or C—R3, wherein Z is NH or S; R1 is chosen from structures (a), (b) and (c): R2 is chosen from (C1-C10)alkyl, (C2-C10)alkenyl and (C2-C10)alkynyl, optionally independently substituted with one or more substituents chosen from halogen, hydroxy, cyano, oxo, (C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkenyloxy, (C1-C6)alkenylthio, (C1-C4)alkoxy(C1-C4)alkoxy, (C5-C7)cycloalkyl, a 5-membered unsaturated heterocycle (optionally s

Abstract: The present invention relates to a medicine, particularly a medicine comprising a novel cyclohepta[b]pyridine-3-carbonylguanidine derivative having an inhibitory effect on an Na+/H+ exchanger (NHE). There is provided a cyclohepta[b]pyridine-3-carbonylguanidine derivative represented by Formula (1): wherein R1 is a group selected from a sulfo group, a sulfoxy group, —OCONH—(CH2CH2O)n—SO3H and the following formulas: R2 represents a halogen atom, a lower alkyl group or a lower alkoxy group; and n represents an integer from 1 to 10, or a pharmaceutically acceptable salt thereof.

Abstract: A method of forming analogs of CDD-0304, i.e., tetra(ethyleneglycol) (4-methoxy-1,2,5-thiadiazol-3-yl)[3-(1-methyl-1,2,4,5-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl]ether hydrochloride includes one or more of the following steps: a) replacing the tetrahydropyridine moiety with one of the following heterocyclic rings, including quinuclidine, [2.2.1]-exo-azabicy-cloheptane, [2.2.1]-endo-azabicycloheptane and terahydropyrimidine; b) varying the length of the linking group by replacing the tetra(ethylene) glycol moiety with one of: ethylene glycol, di(ethylene) glycol, penta(ethylene) glycol, or diether diol; and/or, c) replacing the 1,2,5-thiadiazole moiety with an ester isostere. Also, a method for an asymmetric analog CCD-0304 includes replacing at least one moiety with an ester isostere and at least a second moiety with an ammonium isostere. Also, such analogs compounds and their uses are disclosed.

Abstract: The subject invention relates to 2-azabicyclo[3.3.1]nonane derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states, disorders and conditions mediated by opioid receptors. The subject invention also particularly relates to using such derivatives to treat certain disorders and conditions, for example irritable bowel syndrome, drug addiction, including alcohol addiction, depression, anxiety, schizophrenia and eating disorders, among others, as are more fully described herein.