Abstract: According to the present invention, a compound represented by the following formula (I) having a superior PPAR? agonist action and concurrently showing a hypolipidemic action can be provided, and further, a compound useful as a synthetic intermediate for the compound can be provided.

Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Especially preferred compounds disrupt Nek2/Hec1 binding and are therefore useful as chemotherapeutic agent for neoplastic diseases.

Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating metabolic diseases.

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. An illustrative compound of the invention is shown below.

Abstract: The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.

Abstract: Disclosed is a method for the prevention and/or treatment of a chronic obstructive pulmonary disease by administrating a 5-membered cyclic compound represented by the formula below: or a pharmaceutically acceptable salt of the compound or a prodrug of the compound or salt: wherein X represents an oxygen or sulfur atom; R1 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; R2 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; Y1 represents single bond, a substituted or unsubstituted alkylene or the like; the wavy line means an (E) or (Z) coordination; R3 represents a hydrogen atom, a substituted or unsubstituted aryl or the like; Y2 represents a substituted or unsubstituted alkylene or an alkenylene; R4 represents a hydrogen atom, a substituted or unsubstituted alkanoyl or the like; and R5 represents a hydrogen atom or a substituted or unsubstituted alkyl.

Abstract: The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.

Abstract: The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO—Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.

Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(?O)— or —NR3S(?O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.

Abstract: The present invention relates to pyrrolidinone benzenesulfonamide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of pain.

Abstract: The present invention relates to compounds of formula Ia or Ib below and their tautomers and/or pharmaceutically acceptable salts and compositions and methods of uses thereof.

Abstract: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.

Abstract: An object of the present invention is to provide thiazolidinone derivatives. More specifically, an object of the present invention is to provide novel compounds having a CDC7 inhibitory action. The present invention provides thiazolidinone derivatives represented by the formula (I) The compounds of the present invention inhibit the CDC7 protein kinase activity, and suppress cell proliferation.

Abstract: Isoxazole derivatives, in particular diarylisoxazole derivatives inhibitors of cyclooxygenase (COX), in particular cyclooxygenase-1 (COX-1), their pharmaceutical compositions, the process for their preparation and their use for the chemoprevention and treatment of inflammatory syndromes and in the prevention and treatment of carcinomas, in particular intestinal, ovarian and cutaneous carcinomas, in the treatment of pain syndromes, in particular after surgery, and in the cardiovascular field as antithrombotics/vasoprotectives/cardioprotectives.

Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof. These compounds inhibit serine protease, particularly the hepatitis C virus NS3-NS4A protease.

Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.

Abstract: This invention relates to novel compounds that are substituted oxazolidinones derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel oxazolidinones compounds that are derivatives of rivaroxaban. The invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and condition that are beneficially treated by administering a selective inhibitor of factor Xa, such as rivaroxaban.

Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.

Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed, wherein a dashed line represents the presence or absence of a bond; and, wherein Y, A, R, D, and n are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: This invention describes a series of methods and compositions for prevention and treatment of diseases such as cancer. One aspect of the invention describes small molecule-based drugs that can be used to bind to death receptors TRAIL-R1/DR4 and/or TRAIL-R2/DR5 and induce apoptosis in cancer cells, while sparing normal cells. The invention also describes TRAIL Death Receptor Agonists/Activators (DRAs) and their uses, such as the induction of apoptosis through caspase-8 and caspase-3 activation. The present invention also describes the methods of treating cancers, such as breast, prostate, colon, pancreatic, ovarian, lung, and brain cancers, leukemia, lymphoma, multiple myeloma, and mesothelioma, using DRAs either as single-agent treatments, or in combination with other therapies.

Abstract: The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-3-[2-fluoro-4-(3-oxomorpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.

Abstract: The present invention relates to relates to macrocyclic small molecule inhibitors of the Sonic Hedgehog signaling pathway, syntheses thereof, and intermediates thereto. Such small molecule modulators of the Sonic Hedgehog signaling pathway are useful in the treatment of proliferative diseases (e.g., basal cell carcinoma, Gorlin syndrome, medulloblastoma, or pancreatic cancer), pulmonary diseases (e.g., interstitial pnuemonitis or interstitial pulmonary fibrosis), and developmental disorders (e.g., phocomelia or cyclopia). Novel non-natural macrocycles are provided that inhibit Sonic Hedgehog induced-protein transcription.

Abstract: Compounds of the following general structure for use in compositions and methods for modulating the activity of nuclear receptors are provided: The compounds are useable in compositions and methods for modulating the estrogen related receptors and are agonists, partial agonists, antagonists. or inverse agonists of ERR or ERR?.

Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.

Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.

Abstract: The present invention provides an extended release pharmaceutical composition suitable for once daily dosing comprising Linezolid or pharmaceutically acceptable salt, derivative, prodrug, metabolite and polymorph thereof and one or more pharmaceutically acceptable excipients and a process of preparing the same. The present invention further provides a method of treating bacterial infections in a mammal comprising administering an extended release, pharmaceutical composition suitable for once daily dosing comprising Linezolid capable of maintaining T>MIC for at least 24 hours.

Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).

Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.

Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J, B, Y, and A are as described in claims 1-13. Methods, compositions, and medicaments related thereto are also disclosed, for treating baldness, glaucoma or inflammatory bowel diseases.

Abstract: The present invention relates to a novel cocrystal compound of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide (rivaroxaban) and malonic acid, to processes for its preparation, to medicaments comprising this compound and to their use for controlling diseases.

Abstract: The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) ? (NR1H3) and/or ? (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J1, J2, B, Y, A and D are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

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: A compound having the formula or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. Y, A, U, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.

Abstract: The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, wherein the substitution at the 3-position is an optionally substituted phenyl ring and the substitution at the 2-position is an alkyl or cycloalkyl group; pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators which increase insulin secretion for the treatment of type II diabetes.

Abstract: The present invention relates to novel derivatives of substituted benzylamines, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.

Abstract: Compounds of Formula I: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

Abstract: The invention relates to compounds of formula (I) wherein the groups R and R?, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.

Abstract: Provided herein are novel heteroaryl compounds, compositions comprising the compounds, and methods of treatment or prevention comprising administration of the compounds. The compounds are effective in the targeting of cells defective in the von Hippel-Lindau gene and in inducing autophagic cell death. The methods are directed to treating or preventing diseases such as cancer, and in particular cancers resulting from von Hippel-Lindau disease. The compounds of the invention may be administered in combination with another therapeutic agent.

Abstract: Wherein n is an integer of from 0 to 3; R1A is a 5-membered aromatic heterocyclic group containing at least one oxygen atom; R2A is —COR8 (wherein R8 is aryl); R3A is hydrogen or lower alkyl; and R12 represents cycloalkyl, aryl, aralkyl, alicyclic heterocyclic group, aromatic heterocyclic group, alicyclic hetocyclic-alkyl, or aromatic heterocyclic-alkyl, and R1A, R2A, R3A and R12 are individually optionally substituted.

Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R9, R10, R11, Q and W have the meanings indicated in Claim 1, and precursors thereof are inhibitors of sphingosine kinase and can be employed, inter alia, for the treatment of tumours.

Abstract: This invention relates to novel compounds of the Formula (I) and 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.

Abstract: A compound represented by the formula (1) wherein ring A is aryl optionally having substituent(s) and the like; ring B is arylene optionally having substituent(s) and the like; m=0-2; n=1-5; X is a bond and the like; Y is a bond and the like; and Z is hydrogen atom and the like or a pharmaceutically acceptable salt thereof, and a hydrate or solvate thereof have affinity for CCR3, and can be pharmaceutical products for the treatment and/or prophylaxis of immune or inflammatory diseases.

Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): wherein R1, R2 and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.

Abstract: The present invention provides novel biomarkers, and methods of using said biomarkers, for assessing the efficacy of a treatment regimen for treating cancer in a subject, particularly for treating cancer via Hsp90 inhibition. The present invention also provides methods of identifying test agents capable of treating cancer, particularly in the case of cancers characterized by high levels of IL-8.