Abstract: The present invention relates to heterocyclic compounds of formula 1, in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, carboxylic acid isosteres and N-oxides. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.

Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof.

Abstract: Provided herein is a pharmaceutical composition or a kit comprising a combination of a non-selective beta-adrenergic receptor blocker and an adenosine A1 receptor agonist. Also provided herein is a method of reducing intraocular pressure (IOP) in a subject using such a combination or kit. In a particular embodiment, provided herein is a combination of timolol marketed under the brand Timoptic™ and Compound A.

Abstract: The present invention relates generally to the field of therapy. The invention particularly relates to insulin sensitizers and methods of regulating glucose homeostasis and to the therapeutic or prophylactic treatment of diseases and associated conditions, in which impaired glucose uptake due to insulin resistance is involved or implicated, such as diabetes, syndrome X, hyperglycaemia, vascular disease and kidney disease. The present invention further relates to compounds and agents and compositions thereof for use in the treatment methods.

Abstract: This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, and or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, Ie, and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, and intermediates useful in the preparation of same.

Abstract: Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.

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

Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, and R4 are as defined in the specification. The invention also comprises pharmaceutical compositions comprising the compounds of formula (I) and methods of preventing, treating or ameliorating a CCR2 mediated syndrome, disorder or disease, for example, type II diabetes, obesity or asthma, by administering the compounds of formula (I).

Abstract: The invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on warm-blooded animals.

Abstract: Described herein are methods for modulation of the activity of the carotid body that afford therapeutic benefit for sleep-related breathing disorders and related conditions.

Abstract: Provided herein is a pharmaceutical composition or a kit comprising a combination of a carbonic anhydrase inhibitor analog and an adenosine A1 receptor agonist. Also provided herein is a method of reducing intraocular pressure (IOP) in a subject using such a combination or kit. In a particular embodiment, provided herein is a combination of dorzolamide marketed under the brand Trusopt™ and Compound A.

Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.

Abstract: Methods for treating a cancer having a mutant isocitrate dehydrogenase (IDH), including, but not limited to, a malignant low-grade glioma, a secondary glioblastoma, a transforming myeloproliferative disorder (tMPD), and an acute myelogenous leukemia (AML), with a glutaminase inhibitor, including, bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide (BPTES), are disclosed.

Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y1, Y2, Z, R1, R2 and R3 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

Abstract: A series of oxazole and thiazole compounds are shown herein to be small molecule inhibitors of the Wnt pathway that specifically target the activity of the stabilized pool of ?-cat oxazole and thiazole compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cancer, and others.

Abstract: Phenylacetamide compounds of the formula having sulfonyl group and cycloalkyl group on the phenyl group and having heteroaryl group on the nitrogen atom in the amide have an excellent glucokinase activation action. The compound of the present invention is useful as an agent for treating diabetes, in particular, type II diabetes, as well as metabolic syndrome and obesity.

Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.

Abstract: Biocompatible polymeric nanoparticles for delivery of bioactive agents, and methods for preparing the particles, are described. Polyoxalate nanoparticles of the subject technology show desired particle sizes suitable for use in drug delivery and a substantially uniform or narrow particle size distribution. The polyoxalate nanoparticles can contain water-soluble, poorly water-soluble, or water-insoluble drugs. The nanoparticles are nontoxic and are generally safe for use in humans. After being administered into the body, the nanoparticles with a high content of a bioactive agent entrapped therein can safely deliver the agent to target sites and stably release the drug at a controlled rate.

Abstract: The present application provides novel imidazole compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.

Abstract: Compositions and methods for inhibiting human gamma-glutamyl transpeptidase (GGT) in vivo or in vitro and for inhibiting and killing neoplastic cancer cells, for example for the treatment, inhibition or prevention of tumors or malignant growths or other neoplasias in mammals, or sensitizing tumor to other therapies including radiation therapy. The GGT inhibitor compounds comprise a class of benzylthiadiazol benzenesulfoniamides. The compounds may also be used to treat a reversible airways obstruction in a mammal or a disease associated with reverse airways obstruction such as asthma, chronic obstructive pulmonary disease (COPD), allergic reaction, respiratory tract infection or upper respiratory tract disease. Other diseases or conditions which may be treated include, for example, degenerative diseases, renal diseases, liver diseases, cardiovascular disease and inner ear conditions or diseases.

Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.

Abstract: The present invention relates to 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9H-carbazole derivatives of the formula (I), wherein R1, R2 and R3 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.

Abstract: Compositions and methods, including novel homogeneous microparticulate suspensions, are described for treating acute wounds, chronic wounds and/or a wound or epithelial tissue surface that contains bacterial biofilm, including unexpected synergy between bismuth-thiol (BT) compounds and certain antibiotics, to provide topical formulations including antiseptic formulations, for management and promotion of wound healing and in particular infected wounds. Previously unpredicted antibacterial properties and anti-biofilm properties of disclosed BT compounds and BT compound-plus-antibiotic combinations are also described, including preferential efficacies of certain such compositions for treating gram-positive bacterial infections, and distinct preferential efficacies of certain such compositions for treating gram-negative bacterial infections.

Abstract: The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

Abstract: Novel imidazo[2,1-b][1,3,4]thiadiazole derivatives of formula (I) wherein R1 and R2 have the meaning according to claim 1, are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumors.

Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Abstract: Compounds for inhibiting hypoxia inducible factor (HIF) prolyl-4-hydroxylases (PHDs) having the general formula (1). Methods of using these and related compounds for treating a patient having a condition that would benefit from inhibiting HIF PHD are also described herein.

Abstract: Disclosed are an assay to identify modulators of the PD-1:PD-L pathway and PD-1:PD-L pathway modulators, e.g., compounds and pharmaceutical compositions thereof. Methods for treating diseases influenced by modulation of the PD-1:PD-L pathway such as, for example, autoimmune diseases, inflammatory disorders, allergies, transplant rejection, cancer, immune deficiency, and other immune system-related disorders, are also disclosed.

Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.

Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.

Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.

Abstract: Compositions and methods for treating cancer are described. Some of the methods include administering to a cancer patient in need thereof a substance, such as a carbonic anhydrase inhibitor, that at a therapeutic dose produces a metabolic acidosis in humans; and administering to the patient at least one of: (a) a monocarboxylate transport inhibitor; (b) a sodium-hydrogen exchange inhibitor; (c) a chloride-bicarbonate exchange inhibitor; or (d) a proton pump inhibitor; wherein the at least one of (a) through (d) is in an amount effective to induce selective cytotoxicity in cancer cells relative to noncancerous cells in humans.

Abstract: The invention relates to the use of compounds having pharmacological activity towards the sigma receptor, and more particularly to 1,2,4-triazole derivatives of formula I to processes of preparation of such compounds and to pharmaceutical compositions comprising them.

Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.

Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising one or more human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.

Abstract: The invention provides agents that target carbonic anhydrase, which can be used as imaging agents or therapeutic agents. The agents can be used to image tumor hypoxia as well as other physiological processes in a subject.

Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.

Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.

Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment of various disorders.

Abstract: A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, —C(?W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents —C(?Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.

Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.

Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.

Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.

Abstract: The present invention relates to substituted benzofused derivatives, which can be used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.