Abstract: Disclosed herein is a method for preventing ovarian hyperstimulation syndrome in a subject by administering an effective amount of a dopamine agonist in a pharmaceutically acceptable carrier. Also disclosed herein is a method for treating ovarian hyperstimulation syndrome by administering an effective amount of a dopamine agonist in a pharmaceutically acceptable carrier.

Abstract: The present invention relates to novel compounds of formula (I): wherein R1, R2, R3, R4, and R5 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.

Abstract: The invention relates to a compound of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and R8 are defined as in the specification and claims and to its use for treating or preventing Alzheimer's disease and other similar diseases.

Abstract: This invention relates to the use of azapaullones, particularly in combination with immunomodulating agents, in the prevention, and/or treatment of pancreatic autoimmune disorders, e.g. type I diabetes or LADA and neurodegenerative disorders.

Abstract: The present invention provides compostions and methods useful for treating and preventing neurodegenerative disease and neurologically related disorders by inhibition of Lp-PLA2. The compositions and methods are useful for treating and preventing diseases and disorders with abnormal blood brain barrier (BBB) function, for example neurodegenerative diseases with a permeable BBB, such as but not limited to, Alzheimer's Disease, Huntington's Disease, Parkinson's Disease and Vascular Dementia.

Abstract: Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.

Abstract: Compounds of formula (I) or a salt thereof are disclosed: wherein, A, m R1, R2, R3, q, W1, W2, R4 and R5 are as defined in the description. Processes for preparation and uses of the compounds in medicine, for example for the treatment of schizophrenia or drug dependency, are also disclosed.

Abstract: The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g. Galanthamine, narwedine and lycoramine, or from metabolites of said compounds.

Abstract: This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ?O, —O(CH2)pO— or —S(CH2)S—; W1 is either O or S; X1 and X2 are both H, or together are ?O or ?S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.

Abstract: Compounds and compositions are provided for treatment or amelioration of one or more symptoms of ?-synuclein toxicity, ?-synuclein mediated diseases or diseases in which ?-synuclein fibrils are a symptom or cause of the disease. In one embodiment, the compounds for use in the compositions and methods are heteroaryl acylguanidines, heteroarylhydrazones, dihy-dropyridones, heteroaryl and aryl styryl ketones, and heteroarylpyrazoles.

Abstract: Controlled-release galantamine formulations, including controlled-release particles, pellets, granules, and spheres are described. Controlled-release particles, pellets, granules, and spheres with immediate release top-coat are also described. Method of preparing such formulations and method of treating a variety of disorders are also disclosed.

Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I

Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.

Abstract: The present invention relates to a method for reducing infarction comprising administering to a patient ion need thereof a therapeutically effective amount of a composition comprising as an active ingredient a vasopressin antagonist compound and to a composition useful therefor. The present invention also relates to a method for reducing infarction comprising administering to a patient in need thereof a therapeutically effective amount of a combination of a vasopressin antagonist compound and a beta-blocker and to combinations useful therefor. The methods, compositions and combinations of the present invention can be used for reducing infarction in the heart (myocardial infarction) and the brain (stroke).

Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I

Abstract: This invention relates to the use of Pax4 stimulating compounds, e.g. Glycogen synthase kinase-3 (GSK-3) inhibitors, particularly in combination with immunomodulating agents, in the prevention, and/or treatment of pancreatic autoimmune disorders, e.g. type I diabetes or LADA. More particularly, this invention relates to the use of compounds selected from paullones, indirubines, substituted ureas, maleimide derivatives and pyrimidine thiones. Further, the present invention relates to a method of identifying and/or characterizing pancreatic beta-cell mitogens by using cells expressing a pancreatic gene or a gene whose function is controlled by a pancreatic gene, particularly the Pax4 gene, and which are transfected with a reporter gene.

Abstract: Film-form, single-layered, cavity-free preparation free of surfactants, effervescent additive and taste masker and comprising one or more film former(s), one or more gel former(s) and one or more active ingredient(s) from the group of neuroleptics.

Abstract: The present invention is directed to a method of simultaneously treating hypertension, hypertriglyceridemia, a pro-inflammatory state, a pro-coagulative state, and insulin resistance (with or without treating obesity or endothelial dysfunction), associated with or independent from Metabolic Syndrome, as well as vascular disease such as cardiovascular, cerebrovascular, or peripheral vascular disease comprising the step of administering to a patient suffering from such disorders a therapeutically effective amount of a central acting dopamine agonist. In one embodiment, the central acting dopamine agonist is bromocriptine, optionally combined with a pharmaceutically acceptable carrier.

Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.

Abstract: Compounds of formula (I): wherein A represents a 5, 6 or 7-membered (hetero)aromatic or non-aromatic ring, n and n? represent 0, 1 or 2 X represents an alkylene chain as defined in the description, R3 represents an aryl or heteroaryl group, one of the groups R1 and R2 represents a hydrogen atom and the other represents a group of formula (II) as defined in the description. Medicinal products containing the same which are useful in treating conditions involving a defect in apoptosis.

Abstract: Macrocyclic benzofused pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions are described herein.

Abstract: Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.

Abstract: The present invention relates to novel pyrazole derivatives of formula I having pharmacological activity as H3 antagonists processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.

Abstract: Methods of treating, mitigating, slowing the progression of, or preventing Alzheimer's Disease and Mild Cognitive Impairment (MCI) include administration of gonadotropin-releasing hormone analogs in combination with acetylcholinesterase inhibitors and/or N-methyl-D-aspartate receptor antagonists.

Abstract: The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.

Abstract: The present invention relates to novel fused thiazole derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.

Abstract: A method of treating infertility disorders by 1) administering an LH-RH antagonist, preferably Cetrorelix, in amounts to selectively suppress endogenous LH but not FSH secretion and 2) inducing follicle growth by administration of exogenous gonadotropin. The selective suppression OF LH allows FSH secretion to be at natural levelS thereby not affecting individual estrogen development. The LH-RH antagonist can be given as a single or dual subcutaneous dose in the range of 1 mg to 10 mg, preferably 2 mg-6 mg. In multiple dosing-posology, LH-RH antagonist can be administered subcutaneously in an amount in the range of 0.1 to 0.5 mg of LH-RH antagonist/day. LH-RH antagonist is applied starting cycle day 1 to 10, preferably on day 4 to 8, and ovulation can be induced between day 9 and 20 of the menstruation cycle by administering rec. LH, native LH-RH, LH-RH agonist or by HCG. In addition rec.

Abstract: The present invention provides a novel fused indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Z11 and Z12 each independently represent a carbonyl group, a methylene group, etc.; represents a double bond or a single bond; R1a represents a hydrogen atom, etc.; the ring A represents a benzene ring, a naphthalene ring or a 5- to 10-membered aromatic heterocyclic ring, etc.; and R2a, R2b and R2c each independently represent (1) a hydrogen atom, (2) a halogen atom, (3) a nitro group, etc.

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

Abstract: The present invention provides a drug delivery system comprising nanoparticles or microparticles of a water poorly soluble drug dispersed in a polymeric bead containing essentially only of hydrophilic polymers (i.e. without hydrophobic polymers). The present invention further provides a method of producing the drug delivery system of the invention.

Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.

Abstract: Amidophenyl-sulfonylamino-quinoxaline compounds of formula (I) are CCK2 modulators useful in the treatment of CCK2 mediated diseases.

Abstract: The present invention is concerned with treatment of sleep disorders by administering a cholinesterase inhibitor, and in particular, by administering galantamine or a pharmaceutically acceptable salt thereof. Also in particular, cholinesterase inhibitors that are active at nicotinic receptors and that are selective for acetylcholinesterase over butylcholinesterase are used in treating sleep disorders.

Abstract: Compounds are provided of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia and dyslipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis wherein A is chosen from B is chosen from wherein the variables R1 to R7, m, n, are as defined herein. A method for treating the above diseases employing the above compounds is also provided.

Abstract: Compounds of formula (I): wherein: R1 represents aryl or heteroaryl, R2 represents hydrogen, halogen or hydroxy, X represents oxygen or sulphur, Y represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with adjacent —CHR3—, forms the ring wherein m represents 1, 2 or 3, R5 represents hydrogen or halogen, their isomers and also their addition salts Medicaments.

Abstract: The invention relates to compounds of formula (I): wherein: R1 represents hydrogen, alkyl or cycloalkyl, R2 represents hydrogen, halogen or hydroxy, A represents CR3R4 or NR3 wherein R3 and R4 are as defined in the description, Y represents an alkylene chain as described in the description, X represents NR5R6, S(O)nR7, OR8, C(O)R9, amidino or a heterocycle, their isomers, and addition salts thereof; and medicinal products containing the same which are useful in the prevention or treatment of diseases associated with AMPA flux.

Abstract: Compounds of formula (I): wherein: R1 represents aryl or heteroaryl, R2 represents hydrogen, halogen or hydroxy, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with adjacent —CHR3—, forms the ring wherein m represents 1, 2 or 3, R5 represents hydrogen or halogen, their isomers and also their addition salts. Medicaments.

Abstract: Compounds of formula (I): wherein: R1 represents a heterocycle, R2 represents hydrogen, a halogen or hydroxy, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with the adjacent —CHR3—, forms the ring wherein m represents 1, 2 or 3, R5 represents hydrogen or a halogen, their isomers, and also addition salts thereof.

Abstract: The present invention relates to a pharmaceutical composition comprising an inhibitor of acetylcholinesterase (AChE inhibitor) and a metabotropic glutamate receptor 2 antagonist (mGluR2 antagonist) and a pharmaceutically acceptable excipient. The invention also relates to a method of treating and/or preventing acute and/or chronic neurological disorders comprising administering to a patient in need of such treatment and/or prevention a therapeutically effective amount of said AChE inhibitor and mGluR2 antagonist as well as a kit comprising said AChE inhibitor and mGluR2 antagonist. In particular, the mGluR2 antagonist relates to the compound of formula I wherein, R1, R2, R3, X and Y are described hereinabove. The combination of the AChE inhibitor and mGluR2 antagonist is useful for treating and/or preventing chronic neurological disorders. These disorders include Alzheimer's disease and mild cognitive impairment.

Abstract: The present invention relates to derivatives of 1-oxa-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory actions, especially to the inhibition of tumour necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

Abstract: The invention concerns the use for producing of GSK-3? inhibiting medicines from paullone derivatives. The invention is useful for treating pathologies involving GSK-3? and CDK5.

Abstract: The present invention provides compounds, which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: Compounds of structural formula (I) are disclosed as useful for modulating the androgen receptor (AR) in a tissue selective manner in a patient in need of such modulation, and in particular for antagonizing AR in the prostate of a male patient or in the uterus of a female patient and agonizing AR in bone and/or muscle tissue. These compounds are useful in the treating conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents.

Abstract: Combinations of diuretics and vasopressin antagonists are useful to slow and reverse the symptoms and process of congestive heart failure, to increase the excretion of water in the urine, and to decrease the excretion of sodium and potassium ions in urine. Preferred vasopressin antagonists have the formula wherein R and R5 are hydrogen or lower alkyl; R1, R2, and R3 are hydrogen, halo, alkyl, alkoxy, and amino; and R4 is hydrogen or phenyl, and a pharmaceutically acceptable salt thereof.

Abstract: Compounds according to general formulae (1 and 2), wherein G1 is an azepine derivative and G2 is a group according to general formulae (9–11) are new. Compounds according to the invention are vasopressin V2 receptor agonists.

Abstract: New compounds of general formula I

Abstract: Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.

Abstract: The invention relates to 2-imidazo-benzothiazoles of general formula wherein R1, R2, R3, R4, R5, R6, R7, R?, R?, X, R?? and n are defined herein, or a pharmaceutically acceptable salt thereof. It has been found that the compound of formula I are adenosine receptor ligands with good affinity to the A1 and A3 receptors. These compounds have useful pharmaceutical activities.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.