Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.

Abstract: The present disclosure provides 2,4-disubstituted thiazoles of the general structure shown below that are agonists of G-protein coupled receptor (IC-GPCR2). Also, provided are compositions comprising these compounds as well as methods for using these compounds in a variety of applications including diabetes and metabolic disorders.

Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives of Formula (I): as disclosed herein, to their preparation and to their therapeutic application.

Abstract: This disclosure concerns a protected cyclopropylboronic acid comprising a substituted cyclopropyl group and a boronic ester group having a protecting group. The protecting group is an N-methyliminodiacetic acid (MIDA) group or MIDA-based group.

Abstract: Provided herein are phosphothiophene and phosphothiazole compounds, for example, of any of Formulae I, IA, IIA, IIIA, IVA, VA, VIA, VIIA, IB, IIB, IIIB, IVB, VB, VIB and VIIB disclosed herein, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host infected with HCV.

Abstract: The present invention relates to the use of compounds which increase extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically to the use of 3-disubstituted phenyl-1-pyrrolidinols for the treatment of central nervous system disorders.

Abstract: The present invention relates to compounds of formula (I), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, X, Y, R1, R2, R3 and R4 are as defined in the description and claims.

Abstract: Process for the preparation of 2,2-difluoroethylamine derivatives of the formula (IV) comprising the steps (i) and (ii): step (i): reaction of N-(2,2-difluoroethyl)prop-2-en-1-amine of the formula (I) with a compound of the formula (II) A-CH2-E??(II) to give a compound of the formula (III) optionally in the presence of an inorganic or organic base, and step (ii): removal of the allyl group from the compound of the formula (III), in which, in the formulae (II), (III) and (IV), A and E have the meanings given in the description.

Abstract: The present invention relates to novel benzamidine derivatives, process for the preparation thereof and pharmaceutical composition comprising the same. The novel benzamidine derivatives of the present invention are useful for the prevention and treatment of osteoporosis, bone fractures and allergic inflammatory diseases.

Abstract: Disclosed are an organic semiconductor material including a thiazole compound represented by the following general formula (1) and an organic thin-film transistor using the organic semiconductor material: A1-B1-C1??(1) wherein A1 and C1 each represent an unsubstituted or substituted thiazole ring, and B1 represents an unsubstituted or substituted benzene ring or an unsubstituted or substituted polycondensed aromatic ring. Accordingly, there are provided an organic semiconductor material having high ON current and excellent storage stability and an organic thin-film transistor using the organic semiconductor material.

Abstract: The present invention relates to compositions and methods for modulating retinol binding to retinol binding protein 4 (RBP4). In particular, the present invention provides compounds having Formula (1) or (2) (Formulae (1), (2)); wherein R1, R2, R3, R4, R5, R6, Y1, Y2, Y3, Y4 and m are as defined above.

Abstract: A process for making epi-epothilone compounds according to formula A.1, by reacting a compound according formula C with at least one halogenating agent followed by treatment with base, where R1, R2, R3, R4, R5, R6, R12, R13, Z1 and Z2 in formulae (A.1) and (C) are as defined herein. The epi-epothilone compounds of formula (A.1) can be converted into aziridinyl epothilone compounds, which are useful for the treatment of cancer.

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.

Abstract: The invention relates to a method for producing onium salts with tetrafluoroborate anion by reacting an onium halide with an oxonium tetrafluoroborate, sulfonium tetrafluoroborate, or triphenylcarbonium tetrafluoroborate.

Abstract: The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders.

Abstract: This disclosure relates to reagents and methods useful in the synthesis of aryl fluorides, for example, in the preparation of 18F labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.

Abstract: An embodiment of the composition contains any of compounds of general formula (I) below:

Abstract: The invention relates to a process for the preparation of 2-chloro-5-chloromethyl-thiazole, which is employed as intermediate in the preparation of compounds having a pesticidal action, which process comprises reacting a compound of formula (II), in free form or in salt form, (III), (IV), (V) or (VI) with a chlorinating agent, where R and M+ are as defined in claim 1; to the compounds of the formulae (III) and (IV), which are used in this process as intermediates; and to the use of, and a process for the preparation of, the compounds of the formulae (III) and (IV).

Abstract: It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner.

Abstract: The invention provides crystalline forms of isopropyl alcohol solvate of dasatinib, methods for their preparation, and pharmaceutical compositions thereof.

Abstract: The invention relates to 1-(thiazolyl)- and 1-(isothiazolyl)pyrazol-4-ylacetic acid derivatives of the general formula (I) and salts thereof in which Het, R1, R2, R3, R4, R5, R6 and n are as defined in claim 1. The compounds (I) or salts thereof are suitable for use as herbicides and plant growth regulators, in particular as herbicides for the selective control of harmful plants in crops of useful plants and can be prepared by processes as described in claim 9.

Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A1, A2, A3 and L are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora and KDR.

Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).

Abstract: The present invention relates to novel IAP inhibitor compounds of formula I:

Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.

Abstract: N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy} benzamidine 2 ethansulfonic acid salt, a process for the preparation thereof, a pharmaceutical composition for preventing and treating osteoporosis, bone fractures or allergic inflammatory diseases, comprising the same, and an oral formulation for preventing and treating osteoporosis, bone fractures or allergic inflammatory diseases, comprising the same are described.

Abstract: The present invention relates to a novel class of histone deacetylase inhibitors with aryl-pyrazolyl motifs. The compounds of this invention can be used to treat cancer. The compounds of this invention are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The present invention further provides pharmaceutical compositions comprising the compounds of this invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the compounds of this invention in vivo.

Abstract: Disclosed herein is a composition containing hetero arylene or arylene showing a p-type semiconductor property in addition to thiophene showing a p-type semiconductor property and thiazole rings showing a n-type semiconductor property at a polymer main chain, an organic semiconductor polymer containing the composition, an organic active layer containing the organic semiconductor polymer, an organic thin film transistor (OTFT) containing the organic active layer, an electronic device containing the OTFT, and a method of preparing the same. The composition of example embodiments, which is used in an organic semiconductor polymer and contains thiazole rings, may exhibit increased solubility to an organic solvent, coplanarity, processibility and an improved thin film property.

Abstract: The present invention relates to a novel chrysene derivative and an organic electronic device using the same. A chrysene according to the present invention may act as a hole injection, hole transport, electron injection and transport, or light emitting material in an organic light emitting device and an organic electronic device, and in particular, may be used alone as a light emitting host or a dopant.

Abstract: The invention relates to novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.

Abstract: Novel carboxamides of the formula (I) The present application is further directed toward a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.

Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.

Abstract: The invention relates to a process for the preparation of 2-chloro-5-chloromethyl-thiazole, which is employed as intermediate in the preparation of compounds having a pesticidal action, which process comprises reacting a compound of formula (II), in free form or in salt form, (III), (IV), (V) or (VI) with a chlorinating agent, where R and M+ are as defined in claim 1; to the compounds of the formulae (III) and (IV), which are used in this process as intermediates; and to the use of, and a process for the preparation of, the compounds of formulae (III) and (IV).

Abstract: The invention relates to novel sulfonamide compounds of the formula (I) and their use as orexin receptor antagonists.

Abstract: A 3,4-dihalogenoisothiazole derivative represented by the general formula [I] (wherein R1 is a halogen atom; A is an oxygen atom or a sulfur atom; and R is a C1-C6 alkyl group, a C2-C5 alkenyl group, a C2-C5 alkynyl group, a C3-C6 cycloalkyl group, a phenyl group or a 5- to 10-membered heterocyclic group containing at least one of oxygen atom, sulfur atom and nitrogen atom), or a salt thereof.

Abstract: This disclosure relates to compounds, reagents, and methods useful in the synthesis of aryl fluorides, for example, in the preparation of 18F labeled radiotracers. For example, this disclosure provides universal “locked” aryl substituents that result in StereoElectronic Control of Unidirectional Reductive Elimination (SECURE) from diaryliodonium salts. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.

Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.

Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula I.

Abstract: A process for producing a thiazole compound of the formula (3): wherein X1 is a hydrogen atom or a halogen atom, which comprises reacting a compound of the formula (1): wherein X1 is as defined above, and X2 represents a halogen atom, with ammonia and formaldehyde to obtain a hexahydrotriazine compound of the formula (2): wherein X1 is as defined above, and reacting the resulting hexahydrotriazine compound with hydroxylamine under acidic conditions. According to this process, the thiazole compound of the formula (3) can be industrially advantageously produced using inexpensive ammonia with suppressing the formation of a byproduct of the formula (4): wherein X1 is as defined above.

Abstract: Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.

Abstract: This invention is directed to indole acetic acid derivatives and their use in pharmaceutical compositions for the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic disease. The invention is also directed to intermediates useful in preparation of indole acetic derivatives and to methods of preparation.

Abstract: Compounds of formula (I) where X1, C1, and D1 are defined herein, are inhibitors of polo-like kinases. The compounds of formula (I) are useful for treatment of diseases of cellular proliferation, such as, for example, cancer.

Abstract: Provided are dyes and compositions which are useful in a number of applications, such as the detection and monitoring protein aggregation, kinetic studies of protein aggregation, neurofibrillary plaques analysis, evaluation of protein formulation stability, protein thermal stability shift assay and analysis of molecular chaperone activity. These dyes and compositions are also useful as probes in nucleic acid and protein detection.

Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: Invented are novel hetero-pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.

Abstract: Novel 18F-labeled thiazole derivatives useful for imaging of metabotropic glutamate subtype 5 receptors (mGluR5) in living mammalian brain are disclosed herein. Also disclosed herein is a synthetic method for making the claimed thiazole derivatives under thermal heating or microwave conditions for aryl thioethers that provides the compounds in high yield. Imaging methods in which the claimed 18F-labeled thiazole derivatives are used as imaging agents are also disclosed. Halogen substituted thiazole derivative disclosed herein are also useful as therapeutic agents. Methods of treating mGluR5 mediated disorders with certain halogen substituted thiazole derivatives are disclosed.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with calcium release-activated calcium channels (CRAC).

Abstract: It is intended to provide a benzoxazole derivative or a pharmaceutically acceptable salt or solvate thereof which is useful in the early diagnosis of a conformation disease; a composition or a kit containing the same for diagnosing a conformation disease; a medical composition for treating and/or preventing a conformation disease; and so on.

Abstract: The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having the following Formula: wherein K is —O—, —S—, or —NR7—; A is —(CR8R9)—(CH2)m—Z—wherein Z is —(CHR10)—, —C(?O)—, —C(?O)—C(?O)—, —OC(?O)—, —N(R11)C(?O)—, —O2—, or —N(R11)SO2—; B1 is hydroxyl or cyano and R1 is hydrogen or B1 and R1 are taken together to form a double bond; R2, R3, and R5 are, independently, hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; or R2 and R3 may be taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl; R4 is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl; R6 is hydrogen, alkyl or substituted alkyl; R7, R8, R9, R10, R11 and R12 are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or substi

Abstract: The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1–R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.