Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to 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): or a pharmaceutically acceptable salt thereof, wherein: W is arylene, heteroarylene or formula (a) each L is independently alkylene, alkenylene, alkynylene, a direct bond, arylene, cycloalkylene, alkylene-arylene, alkylene-C?O or —C?O; each X is independently an N-containing heteroarylene, N-containing cycloalkylene or NR; Y is N-containing heteroaryl, N-containing cycloalkyl, NR2, OR1, CN or CO2R; Z1 is formula (b); are useful in therapy, particularly in the therapy of neurodegeneration and cancer.

Abstract: There is disclosed herein a composition for treating gastrointestinal or neurological disorders, constipation, functional constipation, irritable bowel syndrome, diverticulitis, travelers diarrhoea, chronic idiopathic nausea, IBD-associated constipation and diarrhoea, pseudo-obstruction, diabetic gastroparesis, cyclic vomiting, reflux oesophagitis, autism enteropathy, flatulence, halitosis, chronic fatigue, bloating, proctalgia fugax, Parkinsons disease, MS, Alzheimers Disease, Motor Neurone Disease or autism, the composition comprising: (i) at least two anti-clostridial agents selected from the group consisting of: vancomycin, vancomycin derivatives, a multi-valent polymer of vancomycin, aminoglycosides, nitroimidazoles, ansamysins, nifuroxazide, colchicine, prucalopride, prokinetic agent and 5-aminosalicylic acid; or (ii) at least one anti-clostridial agent selected from the above combined with an opioid blocking agent.

Abstract: Compounds of the general formula are disclosed with activity towards treating diseases related to inflammation, such as cancer, neurodegenerative and cardiovascular diseases. Pharmaceutical compositions and methods of use are also described.

Abstract: The present invention relates to new methods for treating and/or preventing vascular events by inhibiting G-coupled Protease Activating Receptor (PAR)-1 and/or PAR-4 with the administration of statins. In one embodiment, individuals who are at risk for vascular events, but have cholesterol levels (e.g., total cholesterol or Low Density Lipoprotein) in normal ranges, are treated with statins.

Abstract: Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.

Abstract: An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.

Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.

Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.

Abstract: Provided is a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action. The 2H-chromene compound or derivative is particularly useful for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells.

Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.

Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (DGAT) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.

Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.

Abstract: The invention concerns the use of azabicycloalkyl derivatives or pyrrolidine-2-one derivatives for the treatment, prevention or delay of progression of ataxia.

Abstract: The invention relates to a process for the manufacture of enantiomerically enriched or pure compounds of formula I wherein R1, R2, R3, R6, R7 and Q are defined as in claim 1 as well as their crystalline forms for the treatment of proliferative diseases such as cancer.

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: The present invention relates to methods and compositions for treating a subject suffering from a sclerosing disorder, comprising administering, to the subject, an effective amount of an estrogen receptor antagonist (“ERANT”), wherein said ERANT has essentially no estrogen receptor agonist activity under physiologic conditions.

Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.

Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.

Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.

Abstract: The application relates to novel substituted piperidines of the general formula (II) in which R1?, R2?, R2?, R4?, X, Z, m and n have the meanings defined in the description, to a process for the preparation thereof and to the use of these compounds as medicines, especially as renin inhibitors.

Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria.

Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).

Abstract: Disclosed are macrocyclic compounds of formulae I-V, which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also disclosed are pharmaceutical compositions comprising an effective kinase-inhibiting amount or an effective HSP90-inhibiting amount of the compounds and methods for the treatment of disorders that are mediated by kinases and HSP90.

Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-piperidine-benzopyrrolone, -benzoxazolone and -benzotriazole derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of formula (I) wherein X, Y and R1 to R10 are as described in the specification.

Abstract: Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.

Abstract: Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.

Abstract: The invention relates to compounds of the formula (I), in which R1, R2, R3, R4, Y and A have the meanings indicated, and to processes for the preparation thereof and to the use thereof for the preparation of medicaments.

Abstract: The present invention relates to compounds of formula I or salts thereof, wherein, R1 is selected from the group consisting of hydrogen and R4; R2 is selected from the group consisting of hydrogen, acetyl and R4; R3 is selected from the group consisting of alkyl, —O-alkyl, —NH-alkyl, aryl and heterocyclyl; R4 represents a moiety (A) wherein, X is selected from the group consisting of a single bond, alkylene, alkenylene, alkynylene, arylene or a heterocyclylene moiety; R5 and R6 are same or different and are independently selected from hydrogen, alkyl, aryl or heterocyclyl; or R5 and R6 may form together with the nitrogen atom to which they are attached a heterocyclyl ring system.

Abstract: The invention relates to piperidine compounds of formula (I): wherein X—R1 represents —N(H)-pyrimidinyl, wherein said pyrimidinyl is unsubstituted or mono-substituted wherein the substituent is selected from (C1-4)alkyl or halogen, or X—R1 represents —NH—C(O)-heterocyclyl, wherein the heterocyclyl is selected from benzofuranyl and imidazo[2,1-b]-thiazolyl, wherein said heterocyclyl is unsubstituted or independently mono-, di- or tri-substituted wherein the substituents are independently selected from (C1-4)alkyl; A represents a phenyl- or thiazolyl-group, wherein the phenyl or thiazolyl is unsubstituted or mono-substituted with (C1-4)alkyl; B represents a phenyl-group, wherein the phenyl is unsubstituted or mono-, or di- substituted, wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, trifluoromethyl, cyano and halogen; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor ant

Abstract: The present invention provides for novel compounds of formula I wherein X is S or S(O); R1 and R2 are each independently selected from the group consisting of —CH2CH3 and phenyl; or R1 and R2 combine to form morpholino; and processes to prepare arzoxifene.

Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, E, T, n and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.

Abstract: The present invention relates generally to the field of hesperetin bioavailability. One embodiment of the present invention is directed at a composition that allows to increase the bioavailability of hesperetin and consequently to maximize the beneficial health effects of hesperetin.

Abstract: The present invention relates to flavanoid compounds of general formula (X1) wherein: R1 is selected from a group consisting of morpholinyl, N-methyl piperizinyl, piperidinyl and N,N?-dimethylamino groups, and n ranges from 3 to 6, and process for preparation thereof. The present invention relates to the demonstration of anti Helicobacter pylori activity and gastric antisecretory activity of semisynthetically designed flavonoid compounds, to be used for the prevention and treatment of gastroduodenal disorders in general and peptic ulcer diseases in particular. The present invention also relates to a hetero-dimeric bi-functional molecule that can be used as monotherapy substituting/replacing/overcoming currently used triple/quadruple therapy, thereby implicating/anticipating/envisaging its commercial applicability.

Abstract: Imidazole-based compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.

Abstract: The invention is directed to a method for alleviating respiratory depression in a subject as a result of disease of pharmacological agents such as opiates, opioids or barbiturates. The invention also discloses pharmaceutical compositions for use with the method, the composition containing in combination, an analgesic, anaesthetic, or a sedative and a positive allosteric AMPA receptor modulator in an amount sufficient to reduce or inhibit respiratory depression caused by the analgesic, anaesthetic, or sedative.

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: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to 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: The present invention relates to a method for enhancing the activity of kinase inhibitors in target cells, and more specifically for enhancing the activity of tyrosine kinase inhibitors (TKIs), said method comprising contacting a cell with a kinase inhibitor and a photosensitizing agent and irradiating said cell with light of a wavelength effective to activate the photosensitizing agent, and to the use of this method for enhancing the effects of kinase inhibitors or kinase inhibitor-based drugs in particular to achieve cell death, for example, in cancer treatment and other diseases or conditions in which kinase inhibitors, such as TKIs, have a beneficial effect.

Abstract: Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.

Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.

Abstract: The present invention is concerned with a novel benzamide derivative and the pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions comprising said novel compound, processes for preparing said compounds and compositions, and the use thereof as a medicine in the treatment of gastrointestinal motility disorders.

Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.

Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.

Abstract: Provided herein are methods and compositions for modulating apoptosis by targeting SKIP (Ski-interacting protein) activity. Methods of increasing DNA damage-induced cell death in cancer cells, and reducing DNA damage-induced cell death in normal cells are provided.

Abstract: A bioluminescence imaging-based high-throughput assay for inhibitors of ABCG2 is described. Compositions of inhibitors of ABCG2 and methods of using ABCG2 inhibitors are also described.

Abstract: A dosing regimen comprising a therapeutically effective amount of flavopiridol or a pharmaceutically acceptable salt thereof optionally in combination with a pharmaceutically acceptable carrier suitable for bolus infusion and subsequently for infusion is disclosed and claimed. Also disclosed and claimed is a method of treating a variety of cancers in a patient comprising administering to said patient the dosing regimen of the invention.

Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.

Abstract: The present application describes substituted piperidinyl modulators of MIP-1? or CCR-1 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 and transplant rejection using said modulators are disclosed.