Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

Abstract: A pharmaceutical composition comprising losartan or a pharmaceutically acceptable salt thereof, which is capable of treating or preventing side effects such as muscle toxicity caused by administering a statin-based lipid-lowering drug, and a pharmaceutical combination composition comprising a statin drug and a losartan drug as active ingredients are provided. The pharmaceutical composition comprising losartan or a pharmaceutically acceptable salt thereof provides an effect on treating or preventing muscle-related side effects caused by administration of a statin drug for treating hyperlipidemia, as well as an intrinsic pharmacological effect for treating or preventing hypertension. When administered along with a statin drug in sequence or co-administered at the same time with the statin drug, the pharmaceutical composition can exhibit an effect of effectively or significantly decreasing or preventing side effects such as muscle toxicity.

Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.

Abstract: A process for preparing a substitute urea of Formula (II) or Formula (I), or a pharmaceutically acceptable salt or ester thereof, Formula (II): Formula (I): the process comprising the reaction of a carbamate of Formula (II?): or formula (I?): with a primary or secondary amine of the formula: R1R2NH, wherein ring A, and R1, R2, R5, V, W, X, Y and Z are as defined herein.

Abstract: The invention relates to a method for diagnosis of multiple sclerosis (MS) wherein, presence or absence of an anti-AT1 receptor antibody is determined in a sample from a patient to be diagnosed and wherein, the presence of an anti-AT1-receptor antibody is indicative of the disease.

Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).

Abstract: Therapeutic compounds, compositions, methods, and medicaments related thereto are disclosed herein.

Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.

Abstract: The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives.

Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Abstract: The present invention relates to compounds of formula (I), as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A, B, R1, R2, R3, R4, R5, n, m and p have the significance defined herein.

Abstract: The invention provides a production method of a biaryltetrazole derivative useful as an intermediate for an angiotensin II receptor antagonist.

Abstract: This invention relates to novel cyclopentyl- and cycloheptylpyrazole derivatives of the formula I wherein A and R1 to R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. The invention relates also to compositions including these compounds and methods of using the compounds.

Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.

Abstract: A process for forming a solid electrolytic capacitor and an electrolytic capacitor formed by the process. The process includes: providing an anode wherein the anode comprises a porous body and an anode wire extending from the porous body; applying a thin polymer layer onto the dielectric, and forming a dielectric on the porous body to form an anodized anode; applying a first slurry to the anodized anode to form a blocking layer wherein the first slurry comprises a first conducting polymer with an median particle size of at least 0.05 ?m forming a layer of crosslinker on the blocking layer; and applying a layer of a second conducting polymer on the layer of crosslinker.

Abstract: The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.

Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.

Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Abstract: Derivatives of selenophene and selenazole heterocycles are disclosed. The compounds are useful as inhibitors of D-amino acid oxidase (DAO) and in the treatment of neurodegenerative and psychiatric diseases and disorders.

Abstract: Compounds exhibiting calcium receptor antagonist activity that are safe and orally administrable having Formula (I) or pharmaceutically acceptable salts thereof:

Abstract: The present invention provides novel compounds that inhibit cell proliferation and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition comprising a compound of the invention and a second therapeutic agent or radiation useful for the treatment or prevention of the mentioned diseases or disorders. In a first aspect the present invention relates to a compound having a structure according to formula (I).

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.

Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.

Abstract: The present invention comprises TGR5 agonists of structural formula I, wherein X, R1, R2, and R5 are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated.

Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.

Abstract: This invention provides a magnetic recording medium excellent in terms of corrosion resistance. The magnetic recording medium comprises a magnetic recording layer, a protective layer and a lubricant layer provided on a nonmagnetic substrate, and the lubricant layer comprises a compound having a heterocyclic ring.

Abstract: The present invention provides a process for preparation of 1-alkyl-5-benzoyl-1H-tetrazole derivative including a step 1 of reacting a ketoamide derivative represented by formula (I) (in formula (I), A represents a halogen atom or the like; n represents an integer of 0 to 5; Y represents an alkyl group) with a halogenating agent to obtain an imidoyl halide derivative represented by formula (II) (in formula (II), A, n and Y are as defined above; X represents a halogen atom); and a step 2 of reacting the imidoyl halide derivative represented by formula (II) with an azide represented by formula (III) (in formula (III), M represents an alkali metal or the like; m represents 1 or 2) to obtain a 1-alkyl-5-benzoyl-1H-tetrazole derivative represented by formula (IV) (in formula (IV), A, n and Y are as defined above).

Abstract: Compounds exhibiting calcium receptor antagonist activity that are safe and orally administrable having Formula (I) or pharmaceutically acceptable salts thereof:

Abstract: substances and the nasal administration thereof, in particular as one of a liquid, as a suspension or solution, or a powder, to the nasal airway of a subject, in particular the posterior region of the nasal airway, and in particular the upper posterior region of the nasal airway, which includes the olfactory bulb, in particular in the treatment of neurological conditions and disorders.

Abstract: The present invention provides a process for the manufacture of the compound 3-{4-methyl-5-[(1R)-1-(2-(3-methylphenyl-2H-tetrazol-5-yl)-ethoxy]-4H-[1,2,4]triazol-3-yl}-pyridine of formula 14 wherein a) the compound 3-(5-methane-sulfonyl-4-methyl-4H-1,2,4-triazol-3-yl)-pyridine of formula 6 and the compound (1R)-[2-(3-methylphenyl)-2H-tetrazol-5-yl]ethanol of formula 13 are dissolved in an aprotic solvent, whereafter an alkoxide base is added, providing the compound of formula 14. The invention also provides methods for manufacturing 3-(5-methanesulfonyl-4-methyl-4H-1,2,4-triazol-3-yl)-pyridine and (1R)-1-[2-(3-methylphenyl)-2H-tetrazol-5-yl]ethanol.

Abstract: It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner.

Abstract: Derivatives of selenophene and selenazole heterocycles are disclosed. The compounds are useful as inhibitors of D-amino acid oxidase (DAO) and in the treatment of neurodegenerative and psychiatric diseases and disorders.

Abstract: The compounds of the formula (I) in which R1 represents hydrogen or in each case optionally substituted alkyl, alkenyl, alkynyl or phenyl are highly suitable as microbicides for protecting plants and materials.

Abstract: The present invention provides a process for the preparation of Olmesartan medoxomil by condensing the ethyl 4-(1-hydroxy-1-methylethyl)-2-propylimidazole-5-carboxylate with 4-[2-(trityl tetrazol-5-yl)phenyl]benzyl bromide to obtain ethyl 4-(1-hydroxy-1-methyl ethyl)-2-propyl-1-{4-[2-(trityl tetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylate and then hydrolyzing ethyl 4-(1-hydroxy-1-methyl ethyl)-2-propyl-1-{4-[2-(trityl tetrazol-5-yl)phenyl]phenyl}methyl imidazole-5-carboxylate to obtain trityl Olmesartan dihydrate followed by reacting trityl Olmesartan dihydrate with 4-chloromethyl-5-methyl-2-oxo-1,3-dioxolene to obtain trityl Olmesartan medoxomil and then deprotecting trityl Olmesartan medoxomil to obtain Olmesartan medoxomil.

Abstract: Biphenyl compounds of Formula (I) and Formula (II), and their pharmaceutically acceptable salts or solvates or prodrugs, their pharmaceutical compositions, their use and process of preparation are provided. Compounds of Formula (I) and Formula (II) are disclosed to exhibit anti-inflammatory properties.

Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.

Abstract: Disclosed herein is a compound of the formula. Therapeutic methods, compositions, and medicaments for the treatment of glaucoma or ocular hypertension related thereto are also disclosed.

Abstract: This invention relates to novel cyclopentyl- and cycloheptylpyrazole derivatives of the formula I wherein A and R1 to R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. The invention relates also to compositions including these compounds and methods of using the compounds.

Abstract: A compound having the structure wherein Y is selected from the group consisting of —C(O)OR2, —C(O)NHR8, —C(CH2)1-2OR3, OH, and or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.

Abstract: Certain chemical entities are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.

Abstract: Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I. The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and Plasmodium falciparum-induced inflammation. In Formula 1, x is 1 or 2: y is O, 1, 2 or 3; and R1 is selected from the group consisting of hydrogen, alkyl having 1 or 2 carbon atoms, hydroxy, alkoxy having 1 or 2 carbon atoms, fluoro, chloro, bromo, and amino.

Abstract: The present invention aims at provision of a method for inhibiting remnant lipoprotein production and a remnant lipoprotein production inhibitor, which includes administering a compound having a CETP inhibitory activity to an administration subject. The remnant lipoprotein production inhibitor of the present invention contains a compound having a CETP inhibitory activity as an active ingredient.

Abstract: The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives.

Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.