Abstract: The present invention relates to a process for obtaining pure aprepitant substantially free of undesired diastereomeric isomer, namely 5-[2(S)-[1(RS)-[3,5-bis(trifluoromethyl)-phenyl)ethoxy]-3-(S)-(4-fluorophenyl)-morpholin-4-yl-methyl]-3,4-dihydro-2H-1,2,4-triazol-3-one. The present invention further provides an improved process for preparation of aprepitant crystalline form II. The present invention also relates to novel amorphous form of aprepitant, a process for its preparation and to a pharmaceutical composition comprising it. The present invention further relates to aprepitant having a mean particle size of less than about 11.5 microns, a process for its preparation and to a pharmaceutical composition comprising it. Thus, for example, aprepitant having a content of diastereomeric impurity of 1.1% is dissolved in ethyl acetate at 70° C., the solution is concentrated to half the initial volume by distilling off ethyl acetate, and the resulting solid is collected at 0-5° C.

Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.

Abstract: A compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof has an effect of inhibiting binding between S1P and its receptor Edg-1(S1P1), and is useful as a pharmaceutical product. [where A represents a sulfur atom, an oxygen atom, a formula —SO— or a formula —SO2—; R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like; R2 represents an alkyl group having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms or the like; R3 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R4 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a phenyl group or the like; R5 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; and R6 represents an alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group].

Abstract: The present invention provides tetrazole compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the tetrazole compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention.

Abstract: Use of heterobicyclic acrylamides of the formula (I) in which A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description, for controlling pests, novel heterobicyclic acrylamides and processes for preparing these compounds, and also compounds of the formula (IA) in which A2, R1, R2, R5 and R6 are as defined in the description.

Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.

Abstract: Novel oxadiazole derivatives of formula (I) having pharmacological activity, processes for their preparation, compositions containing them and their use in the treatment of neurological, psychiatric disorders and gastrointestinal disorders through modulation of the nicotinic ?7 receptor.

Abstract: The present invention relates to a thrombin receptor antagonist containing a compound represented by the formula (I) wherein R1a, R1b and R2 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted alkoxy, R3 is a group represented by the formula —NHCOR4, —NHSO2R5, —NHCON(R6a)(R6b), —NHCOOR7 or —CONHR8 wherein R4, R5, R6a, R6b, R7 and R8 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group and the like), ring A is monocyclic aromatic ring optionally further having substituent(s), R1a and R1b are optionally bonded to each other to form an optionally substituted nitrogen-containing non-aromatic heterocycle, or a salt thereof or a prodrug thereof.

Abstract: The present invention relates to compounds of Formula I, II, III or IV, or pharmaceutically acceptable salts, esters or prodrugs thereof: which can inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.

Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: wherein the substituent variables are as defined herein, and their use as pharmaceuticals.

Abstract: (1,3,5)-Triazinyl phenyl hydrazones are effective at controlling insects.

Abstract: An implant for insertion into a punctum of a patient comprises a body. The body has a distal end, a proximal end, and an axis therebetween. The distal end of the body is insertable distally through the punctum into the canalicular lumen. The body comprises a therapeutic agent included within an agent matrix drug core. Exposure of the agent matrix to the tear fluid effects an effective therapeutic agent release into the tear fluid over a sustained period. The body has a sheath disposed over the agent matrix to inhibit release of the agent away from the proximal end. The body also has an outer surface configured to engage luminal wall tissues so as to inhibit expulsion when disposed therein. In specific embodiments, the agent matrix comprises a non-bioabsorbable polymer, for example silicone in a non-homogenous mixture with the agent.

Abstract: Novel PDF inhibitors and novel methods for their use are provided.

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

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

Abstract: Methods of treating pulmonary hypertension are disclosed. Particular methods comprise the administration of a tryptophan hydroxylase inhibitor and at least one other active pharmaceutical ingredient to patient in need thereof. Pharmaceutical formulations are also disclosed.

Abstract: The invention provides novel compositions and kits comprising at least one nitric oxide enhancing glutamic acid compound, or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension (n) treating diseases resulting from elevated levels of gamma-glutamyl transpeptidase and (O) the targeted delivery of compounds and nitric oxide to organs, cells or tissues containing the enzyme gamma-glutamyl transpeptidase.

Abstract: New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.

Abstract: The present invention relates to compounds of Formula I, II, III or IV, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.

Abstract: This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, S, T, U, V, and R2 are as defined in the specification. The invention also provides pharmaceutical compositions and methods of treating diseases.

Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one nitric oxide enhancing group, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.

Abstract: The invention relates to the use of substance P antagonists and, in particular, the use of non-peptidic NK1 receptor antagonists for the treatment of cancer and, more specifically, human melanoma, neuroblastoma, glioma, human Hodgkin's lymphoma KM-H2, lymphoblastic leukaemia, human rhabdomyosarcoma, human breast carcinoma, human Burkitt's lymphoma, human lung carcinoma, human Ewing's sarcoma, human glioma and human osteosarcoma.

Abstract: This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production.

Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.

Abstract: Compounds of formula are CRTH2 ligands, useful for treatment of inflammatory, autoimmune, respiratory or allergy disease: wherein R1 is hydrogen or methyl and R2 is optionally substituted cycloalkyl, or optionally substituted non-aromatic heterocyclyl having to 6 ring atoms; or R1 and R2, taken together with the carbon atom to which they are attached form an optionally substituted cycloalkyl, or optionally substituted non-aromatic heterocyclyl having 4 to 6 ring atoms: or R1 and R2, taken together with the carbon atom to which they are attached form an optionally substituted cycloalkyl, or optionally substituted cycloalkyl, or optionally substituted non-aromatic heterocyclyl ring having 4 to 6 ring atoms; R is hydrogen or an optional substitutent by 1, 2 or 3 optional substituents; A is hydrogen or C1-C3 alkyl; and ring Ar is an optionally substituted phenyl or 5- or 6-membered monocyclic heteroaryl ring.

Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.

Abstract: A compound of formula (I), wherein substituents are as given above, useful in the treatment of a disease mediated by the action of CCR3, in particular inflammatory or obstructive airway diseases.

Abstract: The invention describes compositions and kits comprising at least qrie organic nitric oxide enhancing salt of an angiotensin converting enzyme inhibitor, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.

Abstract: The invention provides novel compositions and kits comprising at least one nitric oxide enhancing pyruvate compound, or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension (n) treating reperfusion injury following ischemia; and/or (m) preserving tissues, organs, organ parts and/or limbs. The nitric oxide enhancing pyruvate compounds comprise at least one nitroxide group.

Abstract: Disclosed herein are antifungal triazole derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same. The triazole derivatives of Chemical Formula 1 or pharmaceutically acceptable salts thereof according to the present invention have excellent inhibitory activity against a broad spectrum of fungi, in addition to being safe to the body, and thus are very useful in the treatment and prevention of fungal infection.

Abstract: The present invention comprises phenyl and pyridinyl 1,2,4-oxadiazolone compounds their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) delta agonist activity. Also described and claimed are processes for their preparation and their use as pharmaceuticals. These are compounds of formula I, in which the R-group substituents are defined herein. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and de-myelinating and other neurodegenerative disorders of the central and peripheral nervous system.

Abstract: Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation of S1P family receptor activity, in particular by affording a beneficial immunosuppressive effect are disclosed.

Abstract: The compounds of formula (I) in which R1, R2 and R3 have the meanings as given in the description are novel effective PDE2 inhibitors.

Abstract: Disclosed is a triazole derivative represented by the general formula (1) below or a pharmacologically acceptable salt thereof. Also disclosed are a prodrug of such a triazole derivative and an HSP90 inhibitor containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or amino group or the like.

Abstract: The inventive compounds of the present invention are comprised of phenyl and pyridinyl-1,2,4-oxadiazolone derivatives and their physiologically acceptable salts and functional derivatives that are shown to provide peroxisome proliferator activator receptor (PPARdelta) agonist activity. The compounds of the present invention are comprised of the formula: wherein the substituents R1-R5 and R7-R10 are defined herein. The compounds are therapeutically effective in the regulation and modulation of lipid and carbohydrate metabolism in mammals and are thus suitable for the treatment of diseases such as type-2 diabetes, atherosclerosis, cardiovascular disorders and the like.

Abstract: The present invention provides a triazole compound of the following formula: a prodrug thereof or a pharmaceutically acceptable salt thereof. The above-mentioned triazole compound is useful as a therapeutic drug for the treatment of diabetes, obesity or metabolic syndrome.

Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.

Abstract: The present invention relates to compounds of the Formula wherein R3, R5, R7, U, X, Y and Z are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. This invention also relates to pharmaceutical compositions and methods of treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.

Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.

Abstract: Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:

Abstract: Fungicidal compounds of general formula (1) wherein R, R1, R2, W, X, Y and Z are as defined in the specification

Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

Abstract: A series of S-triazolyl ?-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.

Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.

Abstract: Methods of using thiazolidine derivatives of formula (I) to treat cancer, inflammation, or other disorders related to the activities of protein phosphatases PTPN12 or PTPN2 in a mammal are disclosed.

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: The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.

Abstract: The Wnt signaling pathways are involved in embryo development as well as in tumorigenesis. Dishevelled (Dvl) tranduces Wnt signals from the receptor Frizzled (Fz) to downstream components in canonical and non-canonical Wnt signaling pathways, and the Dvl PDZ domain plays an essential role in both pathways, and the Dvl PDZ domain binds directly to Fz receptors. In the present invention using NMR-assisted virtual ligand screening, several compounds were identified and were found to bind to the Dvl PDZ domain. Molecular dynamics simulation was used to analyze the binding between the PDZ domain and these compounds in detail. These compounds provide a basis for rational design of high-affinity inhibitors of the PDZ domain, which can block Wnt signaling by interrupting the Fz-Dvl interaction.