Abstract: The present invention covers azaquinoline compounds of general formula (I), with A being (A1) or (A2), and in which T, R1, R2, R3, R4, R5, R6 and Q are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.

Abstract: The present invention relates to LSD1 inhibitors and their uses as skeletal muscle hypertrophy inducers as well as to promote skeletal muscle regeneration, to prevent skeletal muscle atrophy, or in the treatment or prevention of a disease or injury resulting in loss of skeletal muscle tissue and/or muscle weakness. It further relates to the non-therapeutic use of such compounds to increase muscle mass, muscle strength and/or muscle performance in a subject.

Abstract: The invention is directed to a method of treatment for pain, the method comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof.

Abstract: Certain embodiments are directed to compositions and methods of inhibiting a pathogenic bacterial infection involving ADAM10, specifically a method for treating pore-forming toxin-inducted pathology caused by exposure to staphylococcus in a subject, comprising administering an effective amount of a ADAM10 inhibitor to a patient. The methods include treating pneumonia or inhibiting disruption to epithelial barrier in a subject, having or at risk of developing staphylococcal infection.

Abstract: Cyclic vinylogous amides of Formula I are disclosed The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.

Abstract: The present invention includes crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide disulfate and crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide monosulfate. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms. In one embodiment, the crystalline compound is (2S,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide.

Abstract: Multitarget inhibitors of the enzymes Fatty Acid Amide Hydrolase (FAAH), Cyclooxygenase-1 (COX-1) and/or Cyclooxygenase-2 (COX-2) having a specific carbamate moiety on the meta or ortho position of the A ring of a substituted biphenyl core and having an halogen in the ortho position of the B ring of the biphenyl core. Also concerns the therapeutical application of the multitarget inhibitors, in particular, in the prevention and treatment of cancer.

Abstract: Disclosed herein are methods of treating a patient suffering from a cognitive disorder using the following compounds:

Abstract: The present invention includes crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and crystalline forms of salts and/or solvates of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms.

Abstract: The present invention provides novel phenylcycloalkylmethylamine derivatives, and methods of preparing phenylcycloalkylmethylamine derivatives. The present invention also provides methods of using phenylcycloalkylmethylamine derivatives and compositions of phenylcycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.

Abstract: Disclosed are compounds of formula: that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.

Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-substituted oleanolic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.

Abstract: Certain embodiments are directed to compositions and methods of inhibiting pathogenic bacterial infection involving ADAMIO comprising administering an effective amount of a metalloprotease inhibitor to a patient. Certain embodiments are directed to method of inhibiting Staphylococcal infection comprising administering an effective amount of a metalloprotease inhibitor to a patient. Other embodiments concern methods of inhibiting infection by a bacteria from the genus Clostridium, Streptococcus, Listeria, Bacillus, or Arcanobacterium.

Abstract: The present invention relates to compounds which activate the p53 response, and find use in, for example, hyperproliferative diseases such as cancer treatment and potentially other diseases/conditions involving sirtuin function.

Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.

Abstract: The present invention relates to new antifungal compositions and their use in the treatment of agricultural products.

Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

Abstract: The present invention relates to the field of cardiology. More specifically, the present invention provides methods and compositions useful for treating cardiac hypertrophy. In a specific embodiment, a method for treating or preventing cardiac hypertrophy in a patient comprises the step of administering a therapeutically effective amount of a glycolipid synthesis inhibitor.

Abstract: Methods and agents are provided for treatment of disorders associated with aberrant adrenocortical cell behavior, including (but not limited to) treatment of adrenocortical carcinoma (ACC) and/or Cushing's syndrome. Such methods involve administration of an agent which exhibits an IC50 value against huACAT1 of less than 10 ?M, and one or more further characteristics including effects on adrenocortical cells, disruption of cholesterol homeostasis, reduction in steroid biosynthesis, reduction of mitochondrial function, and/or preferential binding to by low-density lipoprotein (LDL).

Abstract: The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.

Abstract: The compounds of formula (1) in which R1, R4, A and X have the meanings as given in the description, are novel effective EP2 agonists.

Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as hyperlipidemia and also have a beneficial effect on cholesterol.

Abstract: The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo.

Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives.

Abstract: The present invention relates to compounds having a pipecolate diketoamide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pipecolate diketoamide compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.

Abstract: [Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.

Abstract: Methods and compounds for treating neurodegenerative and other disorders. Included is the administering to a subject in need thereof an effective amount of a compound having binding specificity for a p75NTR receptor molecule. Enhanced survival of neural and other cells has been observed.

Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropiomc acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).

Abstract: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.

Abstract: The invention relates to the use of glutaric acid derivatives of general formula (I), which are disclosed in the invention description, as anti-arrhythmic agents.

Abstract: A method of treating polycystic kidney disease in a subject comprises administering to the subject an effective amount of a compound represented by Structural Formula (1): or a pharmaceutically acceptable salt thereof.

Abstract: Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, reduce biofilms, and/or inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.

Abstract: The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-substituted oleanolic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.

Abstract: The present invention provides compositions and methods useful for treating and preventing neovascular AMD by inhibition of CCR3.

Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.

Abstract: Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP (1-42), PTH (1-34), Glucagon (1-29), GLP-2 (1-33), GLP-1 (7-36), GLP-1 (9-36), oxyntomodulin and exendin variants.

Abstract: The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof; to a composition comprising a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluent; and also to use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, or preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, or preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.

Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.

Abstract: Small compounds that modulate the expression of and/or function of sodium channel, voltage-gated, alpha subunit (SCNxA) are presented. Pharmaceutical compositions containing such small molecules and their use in treating diseases and disorders associated with the expression of SCNxA are also presented.

Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.

Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates 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: Provided herein is a pharmaceutical formulation comprising a GGA derivative in the form of an eye drop. Also provided herein are methods of treating neural diseases or disorders by administering such pharmaceutical formulations.

Abstract: The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors.

Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.

Abstract: The present invention relates to compounds of formula I wherein A, B, X, Y, Ar, R1, R2, R?, m and n are as defined herein and to pharmaceutical active acid addition salts thereof, which have a good affinity to the trace amine associated receptors TAAR1, so that they can be used for the treatment of depression, anxiety disorders and bipolar disorder.

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-19 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I and II: These compounds are useful for the treatment of HIV and AIDS.