Abstract: The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Abstract: The present invention provides novel compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to a chemokine receptor, and which affect the binding of a natural ligand or chemokine to a receptor, such as CXCR4 of a target cell.

Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.

Abstract: A compound of formula (I): wherein the substituents are as defined in the text for use in inhibiting insulin-like growth factor 1 receptor activity in a warm-blooded animal such as man.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme.

Abstract: The present invention is directed to a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.

Abstract: The invention provides ?-helix mimetic structures of formula (I) with the definitions of A, B, D, E, G, W, R1 and R2 as set out in the description and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of fibrotic diseases, such as pulmonary fibrosis.

Abstract: The invention relates to a method for selecting COX-2 selective NSAIDs which have a salutary therapeutic profile. The invention further relates to the use of these selected COX-2 selective NSAIDs in the treatment of certain diseases. The invention yet further relates to combinations comprising COX-2 selective NSAIDs and the use of these combinations.

Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.

Abstract: Substituted piperidines of formulae (I) and (II) with the substituent definitions as explained in the specification. The compounds are suitable in particular as renin inhibitors and are highly potent.

Abstract: The invention relates to the use of 1-phenyl-1,2-diaminoethane derivatives of formula (I) wherein the groups A, R1, R2 and Ra through Rj have the meanings given in the claims and specification, for the preparation of a medicament for the treatment and/or prevention of a disease, wherein the activity of a CCR3 receptor is involved and to novel compounds of formula (I), wherein A represents —CH2CH2— or —C(?O)—NH—.

Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of modafinil, optionally in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.

Abstract: The invention relates to compounds of the formula I: wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms; R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionally substituted phenyl or 5- or 6-membered heteroaryl; R1a is hydrogen or C1-C4 alkyl; and R2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl; and to the physiologically tolerated acid addition salts of these compounds.

Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1) wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.

Abstract: A compound represented by, e.g. the formula (I): [wherein X, Y, Z, and W each independently represent optionally substituted methine; A, B, and D each independently represent —C(O)—, etc.; Q represents a methine or a nitrogen; and R represents the formula (II-1), optionally substituted with lower alkyl, etc.; (wherein R6 represents a lower alkyl, etc; and R7 and R8 each independently represents a lower alkyl, etc.)] or a pharmaceutically acceptable salt of the compound. The compounds and salt have antagonistic activity against a histamine H3 receptor or inverse agonistic activity against a histamine H3 receptor. They are useful in the prevention or treatment of metabolic diseases, circulatory diseases, or neurotic diseases.

Abstract: The present invention provides certain pyrazoline compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions and methods of using the compositions in the treatment of various diseases.

Abstract: The invention is based on the discovery that compounds of formula (I) possess high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. The invention features a compound of formula (I) and uses thereof: formula (I).

Abstract: The invention described herein relates to certain pyrimidinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Abstract: The invention relates to methods of screening for inhibitors of diseases or biological processes that involve peptide or protein polymerization. Included in the methods of the invention are methods to identify inhibitors of deoxyhemoglobin S polymerization. Also included in the invention are diagnostic and therapeutic methods.

Abstract: (?)-(2S,4S)-1-(2-Hydroxymethyl-1,3-dioxolan-4-yl)cytosine (also referred to as (?)-OddC) or its derivative and its use to treat cancer in animals, including humans.

Abstract: In particular, the present invention is concerned with compounds of the general formula (I) wherein X, Y and R1 to R10 are as described herein. The compounds are V1a receptor antagonists. The invention also relates to the manufacture of compounds of formula I, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases.

Abstract: In particular, the present invention is concerned with compounds of the general formula (I) wherein X, Y and R1 to R10 are as described herein. The compounds are V1a receptor antagonists. The invention also relates to the manufacture of compounds of formula I, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases.

Abstract: The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyrazole, 1H-pyrazolo[3,4-b]pyridine, benzo[b]furan, benzimidazole, benzoxazole, 1,2-benzisoxazole and imidazo[1,2-a]pyridine; R1 and R2 each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; an optionally-substituted C1-C6 alkyl, aryl or heterocyclic group; or a C1-C6 alkyl or C2-C6 alkenyl group having the aryl or heterocyclic group; R3 and R4 each represent a hydrogen atom, a halogen atom, a nitro group, a cyclo-C3-C

Abstract: A method of effectively treating nociceptive pain involves administering to a human or animal in need of relief from nociceptive pain a therapeutically effective amount of naloxone intranasally, intravenously, by inhalation, transdermally, or orally. Pain associated with fibromyalgia, arthritis, surgical procedures, etc. can be effectively treated.

Abstract: A prodrug compound of a rapamycin analog and methods for inhibiting, treating, and preventing mammalian diseases.

Abstract: Methods for preventing, managing and reversing disease caused by inflammation mediated vascular lesions may utilize agents that bind to FKBP 12 and inhibit mTOR cascade.

Abstract: New aniline or phenol N-mustards linked to DNA-affinity carriers (such as 9-anilinoacridines, acridines and quinolines), aminobenzamides or aminophenol ethers by a urea, carbamic acid, carbanic acid ester, hydrazineurea, hydrazinecarbamic acid ester, phenoxyurea, phenoxycarbamic acid ester linkage with improved chemical stability and anti-tumor therapeutic efficacy are provided.

Abstract: A method for the treatment or prophylaxis of an infection in a mammal, said infection caused by an anti-microbial resistant bacteria, comprising, administering, to the mammal a pleuromutilin derivative is disclosed.

Abstract: Compounds of the general formula (I); wherein the substituents are as defined in claim 1, are useful as fungicides.

Abstract: The present invention relates to a pharmaceutical composition comprising at least one first active therapeutic substance selected among carveol, thymol, eugenol, borneol, carvacrol, alpha-ionone, beta-ionone, as well as isomers, derivatives and mixtures thereof, and comprising at least one second active therapeutic substance that is an antiparasitic agent, in particular, an antimalarial agent. The invention is for use in the field of pharmaceutics.

Abstract: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.

Abstract: The present invention relates to new compounds or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.

Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.

Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, o, A, A1, A2, X, Z, R1, R3, R2, p, q and r are as defined in the specification.

Abstract: (R)-5-Methyl-4,5-dihydro-pyrazole-1,5-dicarboxylic acid 1-[(4-chloro-phenyl)-amide] 5-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide} pharmaceutical compositions, methods and methods of using the compound or pharmaceutical compositions thereof to treat diseases characterized by abnormal thrombosis in mammals.

Abstract: The present invention relates to nicotinanilides of the formula I in which: n=0, 1, 2; m=2, 3; X1=F, chlorine; X2=halogen; Y=CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, methoxy or methylthio; p=0, 1; R1=halogen, methyl, C1-C4-haloalkyl, methoxy, methylthio, methylsulfinyl or methylsulfonyl; R2=hydrogen, methyl or ethyl; W=O, S; processes for preparing these compounds, compositions and seed comprising them and also methods for controlling harmful fungi.

Abstract: The present invention relates to a ramipril-amlodipine salt.

Abstract: The present invention comprises compounds and compositions for the treatment of metabolic disorders and more particularly, those insulin-related metabolic disorders of the blood such as hyperlipidemia, diabetes, insulin-resistance and the like comprising acetic acid derivatives with cyclohexylmethoxy substituents and their salts. Known as peroxisome proliferator-activated receptor (PPAR) agonists/antagonists, the invention relates to compounds of formula I wherein R1-R6 are further defined herein.

Abstract: Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.

Abstract: A novel use of compounds and pharmaceutically acceptable salts thereof, which are 5-HT6 antagonists, are disclosed. In one embodiment, the invention relates to the use of these compounds or pharmaceutical compositions comprising these compounds for preventing relapse into addiction, for example, relapse into addiction to substances of abuse, including opiates, hallucinogens, inhalants, phencyclidine, amphetamines, cocaine, cannabis, nicotine, and alcohol, relapse into addiction to certain medicines, including sedatives, hypnotics and anxiolytics, and relapse into certain addictive behaviors, including gambling.

Abstract: The present invention relates to a novel method for obtaining (2S,3aS,6aS)-1-[(S)-2-[[(S)-1-(ethoxycarbonyl)-3-phenylpropyl]-amino]propanoyl]octahydro cyclopenta[b]pyrrole-2-carboxylic acid, viz. Ramipril(I) in high optical purity, free of other stereoisomers, and in high bulk density. The present invention also relates to a novel hydrated form of Ramipril(I) and a process for preparation thereof.

Abstract: Agents which contains a serotonin derivative as an active ingredient are effective for improving hemodynamics and for preventing or improving deterioration of hemodynamics associated with aging and progression of cardiovascular diseases.

Abstract: The present invention relates, in general, to isoprenylcysteine carboxylmethyltransferase (Icmt) and, in particular, to inhibitors of Icmt and to methods of disease treatment using same.

Abstract: The present disclosure provides amide-based, non-nucleoside compounds having an inhibitory activity against endogenous polymerases, such as polymerase alpha and polymerase gamma. This disclosure further provides uses of treating hyperproliferative diseases or disorders, such as benign or malignant neoplasms, and more specifically cancers that are sensitive to inhibition of polymerase alpha and polymerase gamma.

Abstract: Stabilization of the pharmaceutical active solid substance atorvastatin alone or in a mixture with other solid substances embedded in a gaseous mixture is carried out in such a manner that in the surrounding gaseous mixture a partial pressure of oxygen of at most 2 kPa, preferably less than 1 kPa, more preferably less than 0.4 kPa is maintained. The corresponding partial pressure is achieved either by use of oxygen absorbers, by packaging under a pressure of 0.3-10 kPa, or by packaging under a slight overpressure of an inert gas, preferably nitrogen, the gas being introduced, by means of nozzles, into the cavities, optionally also into the space of the press roller and of the wiper station.

Abstract: Dosing regimens, routes of administration and methods for the treatment or prevention of arrhythmias are disclosed. In these methods, arrythmias (e.g. atrial fibrillation, atrial flutter, early after depolarizations and prolongation of QT interval) may be reduced or eliminated by administering ion channel modulating compounds to a subject in need thereof via the dosing regimens disclosed herein.

Abstract: The invention relates to substituted [(phenylethanoyl)amino]benzamides and methods for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of inflammatory disorders such as, for example, cutaneous, respiratory tract and cardiovascular disorders such as, for example, arteriosclerosis and coronary heart disease.

Abstract: Colchicine neoglycosides, method for their synthesis and methods for their use are disclosed. The invention provides analogs of colchicine glycosylated to include a sugar moiety on a colchicine scaffold that is generally unglycosylated in nature. The colchicine neoglycosides disclosed herein are shown to have cytotoxic effects equivalent to at least the known cytotoxins paclitaxel and doxorubicin. Further, the neoglycosides disclosed according to the invention have physiologic effects not previously recognized in the alkaloid family that includes colchicine but recognized in other cytotoxic drug families such as the taxanes which act by stabilizing tubulin formation.

Abstract: The invention relates to a medicament for IBS, which comprises a dual antagonist for 5-HT2B and 5-HT7 receptors having selective binding affinities for 5-HT2B and 5-HT7 receptors. The pharmaceutical composition of the invention is useful as a drug which is excellent in the therapeutic effect on IBS and shows lessened side effects occurring in the existing remedies for IBS, because it showed good pharmacological actions in comparison with the case of independently using a 5-HT2B receptor antagonist having selective binding affinity for 5-HT2B receptor or a 5-HT7 receptor antagonist having selective binding affinity for 5-HT7 receptor.