Abstract: The present invention relates to novel hypoglycemic compounds of formula (1) and pharmaceutically acceptable salts thereof.

Abstract: A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has applicability as a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. wherein R1 is a hydrogen atom; R2 is an aromatic ring group, etc.; R3 is a hydrogen atom, etc; R4 is a hydrogen atom; R5 is an oxepanyl group, etc.; R6 is a hydrogen atom.

Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.

Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.

Abstract: A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.

Abstract: The present invention provides a composition for use as a harmful organism control agent comprising as an active ingredient one or more of compounds represented by formula (I) or salts thereof and an agriculturally or zootechnically acceptable carrier. wherein Het represents pyridyl; X represents an oxygen atom; R1, R2, R3, R7, R10a, R10b, R11, and R12 represent a hydrogen atom; R4, R5, and R6 represent a hydrogen atom, hydroxyl, optionally substituted C1-18 alkylcarbonyloxy, optionally substituted C1-18 alkylsulfonyloxy, optionally substituted arylcarbonyloxy, C1-6 alkyloxy-C1-6 alkyloxy, C1-6 alkyloxy-C1-6 alkyloxy-C1-6 alkyloxy; R8 represents a hydrogen atom; and R13a, R13b, and R13c represent methyl.

Abstract: Provided herein are compounds useful for kinase inhibition.

Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.

Abstract: Novel 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives that are effective for use in treating viral infections are described. Also described are pharmaceutical compositions comprising the 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives and methods for using the compounds or compositions.

Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.

Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.

Abstract: The present invention relates to a method of making pyrimidines of formula (III) wherein X1, X2, R1 and R2 have the meanings as defined herein.

Abstract: The present invention relates to improved processes for the preparation of endolthelin receptor antagonists darusentan and ambrisentan, their salts and intermediates. Processes for the preparation of darusentan and ambrisentan comprise reacting benzophenone with a compound of Formula-3 to provide a compound of Formula-4, which on in-situ treatment with methanol and a suitable acid provides a compound of Formula-5; hydrolyzing the compound of Formula-5 to provide a compound of Formula-6; resolving the compound of Formula-6 to provide a compound of Formula-7; esterifying the compound of Formula-7 to provide a compound of Formula-8; reacting the compound of Formula-8 with a compound of Formula-9 to provide a compound of Formula-10; hydrolyzing the compound of Formula-10 to provide darusentan or ambrisentan; and purifiying darusentan or ambrisentan to provide darusentan or ambrisentan having purity greater than 99.00% by HPLC.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.

Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.

Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.

Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.

Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.

Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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 invention relates to salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical composition for use, e.g., in treatment of airway disorders.

Abstract: A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.

Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, T, U, V, X, Y, Z, G, and Z are defined herein. It also discloses a method of treating an angiogenesis-related disorder, e.g., cancer or age-related macular degeneration, with such a compound.

Abstract: Provided is a cyclic amine compound, represented by the following formula (I) that has superior acaricidal activity, has superior properties and safety, and which can be synthesized industrially advantageously, a salt thereof and an acaricide: (wherein, Cy1 and Cy2 respectively and independently represent, for example, an aryl group, R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b and R5a respectively and independently represent, for example, a hydrogen atom, R1a and R2a or R3a and R4a may together form, for example, an ethylene group, R10, R11, R20 and R21 respectively and independently represent, for example, an alkyl group, R10 or R11 may respectively or mutually, or together with an atom that bonds on Cy1, form a ring, R20 or R21 on Cy2 may respectively or mutually, or with an atom that bonds on Cy2, form a ring, m represents an integer of 0 to 5, n represents an integer of 0 to 5, p represents an integer of 0 to 5, and r represents an integer of 0 to 5).

Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.

Abstract: The present invention provides a novel antimetabolic anticancer agent that has an excellent balance between antitumor effect and toxicity. Specifically, the present invention provides a medicament containing, as an active ingredient, a 5-fluorouracil derivative represented by Formula (I) or a salt thereof: wherein R1 represents a hydrogen atom or a protecting group of a hydroxy group, R2 represents a lower alkoxy-lower alkyl group or a tetrahydrofuranyl group, X represents a carbon atom or a nitrogen atom, and Y represents a halogen atom or a cyano group.

Abstract: Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.

Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

Abstract: A compound having Formula I or II (Formula I) or (Formula II), or a pharmaceutically acceptable salt thereof, wherein X, Z, R1, R2, R11 and R12 are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.

Abstract: There is disclosed the use of a compound of formula (Ia) or (Ib) wherein R1, R2, R3, R4, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of the enzyme myeloperoxidase (MPO) is beneficial. Certain novel compounds of formula (Ia) or (Ib) and pharmaceutically acceptable salts thereof are disclosed, together with processes for their preparation. The compounds of formulae (Ia) and (Ib) are MPO inhibitors and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders.

Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.

Abstract: A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optionally substituted lower alkyl, etc.

Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atherosclerosis.

Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.

Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

Abstract: The present invention relates to a compound comprising an imine bond as an acid-labile trigger group, the use of such an imine bond as an acid-labile trigger group, a process of cleaving the imine bond in said compound, and a pharmaceutical composition comprising said compound.

Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein R1 is a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkoxy and SF5; and n is 1 or 2; their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.

Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, R2?, L, Het, p and p? are as defined herein, compositions containing them, and their use as medicinal products.

Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

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: Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.