Abstract: The invention relates to the use of derivatives of 3-guanidinophenylalanine as urokinase inhibitors for treating malignant tumors and metastasis.

Abstract: The invention provides novel compounds, methods for treating or preventing a condition related to ER-stress, e.g. hypercholesterolemia, atherosclerosis and related conditions, and pharmaceutical compositions related thereto.

Abstract: A thiazoline derivative represented by Formula (I): wherein R is a cyclic hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; X is a bond or a divalent chain hydrocarbon group which may be substituted; X? is a bond or —N(R5)—; Y is a divalent hydrocarbon group which may be substituted; Y? is a bond or —C(?O)—; ring A is a nitrogen-containing heterocycle which may be substituted; Z1 and Z3 are each independently a bond or a divalent chain hydrocarbon group which may be substituted; Z2 is a bond or —N(R6)—; and B is a group represented by the formula: which is useful as a therapeutic drug for thrombosis, is provided.

Abstract: The invention relates to 3,4-dihydro-2-naphthamide derivatives of formula (I), pharmaceutical compositions containing them and their therapeutic applications as partial agonists or antagonists of the dopamine D3 receptor for the treatment of neuropsychological disorders.

Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, and q have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.

Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.

Abstract: Disclosed are methods for treating patients suffering from cardiovascular diseases comprising administering an intravenous (IV) infusion of ranolazine. In one embodiment, the IV infusion of ranolazine is followed by an orally administered sustained release ranolazine dosage formulation to maintain human ranolazine plasma levels at therapeutic levels in patients.

Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).

Abstract: The present invention is directed to arylalkyl- and cycloalkylalkyl-piperazine derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Abstract: Amphoteric compounds are described, having a zwitterionic structure of the betainic type having general formula (I) and their use for the control of phytopathogen fungi and/or the mitigation of abiotic and biotic stress.

Abstract: An IR spectroscopic technique provides methods for measuring the irritation potential of a formulation and to assess the ability of molecules to enhance the permeability of substances into and through skin using samples comprising stratum corneum. Molecules are screened for their performance as chemical penetration enhancers using a unique in silico procedure that may be applied iteratively in an attempt to generate molecules showing successively higher performance. Both the irritation potential and the ability of the molecule to enhance penetration are considered in the in silico approach. The invention provides specific molecules that may be used in topical or transdermal formulations to improve the delivery of actives. The structures of compounds of the invention include: Formulas (I), (II), (III), (IV), (V), (IV) and analogs thereof.

Abstract: Provided is a novel isoindoline compound of the formula (I): The compound is useful for anesthesia by inducing sedation in a mammal.

Abstract: The present invention relates to non-steroidal progesterone receptor modulators of the general formula I the use of the progesterone receptor modulators for producing medicaments, and pharmaceutical compositions which comprise these compounds. The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.

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

Abstract: The present invention is directed to compounds of the formula I: I (wherein R1, R2, R3, R4, R5, R6, X, Z and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.

Abstract: The present invention provides new method of treatment of epilepsy with non-imidazole alkylamine derivatives that constitute antagonists of the H3-receptors of histamine.

Abstract: The present application describes deuterium-enriched ranolazine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: A compound selected from those of formula (I): wherein: R1, R2, R3 and R4, which may be the same or different, each represent an atom or group selected from hydrogen, halogen, alkyl, alkoxy, phenyl and cyano, X represents a bond, an oxygen atom or a group selected from —(CH2)m—, —OCH2— and —NR5—, wherein m represents 1 or 2, and R5 is as defined in the description, Y represents an oxygen atom or a group selected from NR7 and CHR8, wherein R7 and R8 are as defined in the description, Z represents a nitrogen atom or a CH group, n represents 1 or 2, Ak represents an alkylene chain, Ar represents an aryl or heteroaryl group, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid. Medical products containing the same which are useful in the treatment of conditions requiring a serotonin reuptake inhibitor and/or NK1 antagonist.

Abstract: The present invention is directed to compounds of formula (I): where X, Y, R1, R2 and R3 are defined therein, which can act as modulators of viral replication and/or virus production, especially of the hepatitis C virus (HCV).

Abstract: The present invention relates generally to novel therapeutic compounds and AXOR 109 agonists, and processes for the manufacture and use of the same.

Abstract: Nitroderivatives of prostaglandin amides having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.

Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or stereoisomers thereof. The compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.

Abstract: The present invention provides an amide derivative represented by the following general formula (1): wherein R1 represents a saturated cyclic amino group, R2 represents alkyl, halogen or haloalkyl, R3 represents hydrogen or halogen, Het 2 represents pyridyl or pyrimidinyl, and Het 1 represents a group of the formula [6], or a salt thereof, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention is useful as a BCR-ABL tyrosine kinase inhibitor.

Abstract: The present invention is directed to alkanoyl and cycloalkanoyl-amine derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Abstract: The present invention refert to the use of compounds active on the sigma receptor for the treatment of mechanical allodynia.

Abstract: Piperazinyl- or piperidinylamine-sulfamic acid amides and their use for the manufacture of a medicament in diseases mediated by the action of steroid sulfatase.

Abstract: Formulations are provided for parenteral administration of (amino substituted (e)-2,6-dialkoxystyryl 4-substituted benzylsulfones and the sodium and potassium salts thereof for the prevention and/or treatment of conditions mediated by abnormal cell proliferation. Composition for parenteral administration are provided which comprise an effective amount of compound of formula I or a compound of formula IIa and at least about 50% by weight of at least one water soluble polymer selected from the group consisting essentially of polyethylene glycol (PEG), poly-oxyethylene, poly-oxyethylene-poly-oxypropylene copolymers, polyglycerol, polyvinylalcohol, polyvinylpyrrolidone (PVP), polyvinylpyridine N-oxide, copolymer of vinylpyridine N-oxide and vinylpyridine.

Abstract: Disclosed are neuroblastoma tumor-initiating cell inhibiting compositions comprising chemical entities capable of affecting neuroblastoma tumor-initiating cells. Pharmaceutical preparations that include these chemical entities are also provided for the treatment of neuroblastoma. These pharmaceutical preparations are suitable for the treatment of humans, and are particularly suited for the treatment of children of 12 years of age or younger having neuroblastoma. The compositions and pharmaceutical preparations posses reduced normal cell cytotoxicity. The compositions and pharmaceutical preparations may be used alone or together with other conventional neuroblastoma preparations as part of a clinical regimen in the treatment and management of neuroblastoma.

Abstract: Compounds and methods are provided for the alleviation or treatment of diseases or conditions in which modification of muscarinic m1 receptor activity has a beneficial effect. In the method, a therapeutically effective amount of a selective muscarinic m1 agonist compound is administered to a patient in need of such treatment.

Abstract: The present invention relates to novel solvate and crystalline forms of carbamoyl-cyclohexane derivatives and, more particularly, to novel solvate and crystalline forms of trans-1{4-[2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl}-3,3-dimethyl-urea hydrochloride. Processes for the preparation of these forms, compositions containing these forms, and methods of use thereof are also described.

Abstract: The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.

Abstract: This invention features a method for modulating human N-type calcium channel ?1B+SFVG subunit activity.

Abstract: This invention relates to a pharmaceutical composition for preventing and curing myocardium ischemia and reducing area of myocardial infarction, its pharmaceutical preparation and applications. The composition includes (a) levocarnitine or its derivatives, and (b) trimetazidine or its medicative salts. The quantity of levocarnitine or its derivatives, and trimetazidine or its medicative salts in the composition is effective amount for treating myocardial ischemia and reducing the area of myocardial infarction.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: This invention relates to the treatment of obesity, the treatment of obesity related disorders, prevention of weight gam, prevention of weight regain or for weight maintenance by the use of a cathepsin K inhibitor as active ingredient, alone or in conjunction with other anti-obesity agents The invention also relates to the pharmaceutical compositions comprising cathepsin K inhibitor as active ingredient, pharmaceutically acceptable carriers or excipients, and optionally one or more anti-obesity agents.

Abstract: This invention relates to novel compounds that partially inhibit fatty acid oxidation and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel compounds that are derivatives of ranolazine. This invention also provides compositions comprising one or more compound of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by partial fatty acid oxidation inhibitors, such as ranolazine.

Abstract: Compounds of the present invention are useful for inhibiting protein tyrosine kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract: Methods for treating angina are described. A method for treating angina includes concurrently administering a compound with a therapeutic cardiovascular compound. A combination therapy employs suitable therapeutic cardiovascular compounds, such as a calcium channel blocker, a ?-adrenergic blocker, nitrates, partial fatty acid oxidation inhibitors, potassium channel activators, or a mixture thereof, in combination with a compound such as pyridoxal-5?phosphate, pyridoxic acid, pyridoxal, pyridoxamine, 3-acylated analogues of pyridoxal, 3-acylated analogues of pyridoxal-4,5-aminal, pyridoxine phosphonate analogues, a pharmaceutically acceptable acid addition salt thereof, or a mixture thereof. The invention also includes a novel composition comprising at least one compound and nitrates, partial fatty acid oxidation inhibitors, potassium channel activators, calcium channel blockers, ?-adrenergic blockers, or a mixture thereof.

Abstract: Disclosed herein are substituted piperazine late Na+ channel modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Sulfonylindoline compounds of formula I, wherein R1 through R4, Y and Z have defined meanings, a process for preparation of such compounds, and the use as pharmaceutically active substances, particularly for the treatment or inhibition of neurodegeneration, cardiovascular disease, inflammatory disease, hypercholesterolemia, dyslipidemia, obesity or diabetes.

Abstract: This invention is directed to the use of ranolazine to reduce the risk of adverse coronary events in a mammalian patient. Typically, the natriuretic peptide is associated with coronary disease, acute coronary syndrome, and/or diastolic dysfunction. Ranolazine may be administered to the patient as an intravenous solution or in an oral dose.

Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.

Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-8)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.

Abstract: Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed.

Abstract: The present invention relates to compounds with ?7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.

Abstract: Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.

Abstract: The present invention relates to piperazine derivatives of formulae Ia, Ib, Ic and Id and their use to treat myocarditis. where R1a, R1b, R2, R3, R4, R5, R6, R9, R10 and Y are as defined herein.

Abstract: The invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula (I).

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract: The invention is directed to methods for enhancing endogenous insulin levels in a patient in need thereof which method comprises administering to the patient an insulin secretion-enhancing amount of racemic ranolazine or the R- or S-enantiomer of ranolazine. It is also directed to methods of treatment comprising racemic ranolazine or the R- or S-enantiomer of ranolazine for enhancing endogenous insulin levels in a patient in need thereof. It is also directed to a composition comprising an insulin secretion-enhancing amount of racemic ranolazine or the R- or S-enantiomer of ranolazine and at least one anti-diabetic agent.