Abstract: A method of synthesizing Pyrazoles by means of the oxidative conversion of Enamines with suitable N-containing carboxylic acid derivatives in the presence of copper ions and 2-picolinic acid derivatives is provided.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.

Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1 are suitable for use as microbiocides.

Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.

Abstract: The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.

Abstract: A compound of formula (I): where A, B, C, G, m, n, o, p, R1, R2, R3, R4, R5, R6, X, R7, R8, R9, R10 and R11 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: The present invention provides methods for treating cancer comprising inhibiting the activity of p300/CBP histone acetyltransferase (HAT). Also provided are p300/CBP HAT inhibitors for treating a subject having cancer. In addition, the present invention includes biomarkers for p300/CBP HAT inhibition, which are used to i) monitor the effectiveness of cancer therapy, and ii) identify anti-cancer agents for use in combination therapy.

Abstract: The present invention aims to provide a compound having a PDE inhibitory action and useful as a medicament for the prophylaxis or treatment of schizophrenia and the like. A compound represented by the formula (1x): wherein each symbol is as described in the DESCRIPTION, or the formula (1): W1—W2??(1) wherein each symbol is as described in the DESCRIPTION, or a salt thereof.

Abstract: The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR1—C(O)—, and wherein either NR1 is attached to Ar1 and —C(O)— is attached to Ar2, or —C(O)— is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; a

Abstract: The present invention relates to fungicidal N-[(het)arylethyl)] pyrazolecarboxamide or thiocarboxamide and their heterosubstituted analogues, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.

Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as pro-cymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.

Abstract: The bicyclo-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor are disclosed. The definition of substituents in formula (I) are the same as defined in the description.

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

Abstract: The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use: wherein each symbol is the same as defined in the description.

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

Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.

Abstract: The present invention relates to fungicidal N-[(het)arylalkyl)]pyrazolecarboxamide or thiocarboxamide and their heterosubstituted analogues, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.

Abstract: This invention relates to organic chemistry, in particular to processes for the preparation of pyrazoline carboxamidine derivatives of formula (I), known as potent 5-HT6 antagonists. The invention also relates to novel intermediates of these compounds. wherein the symbols have the meanings given in the description.

Abstract: The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.

Abstract: Copper plating baths containing a leveling agent that is a reaction product of one or more of certain cyclodiaza-compounds with one or more epoxide-containing compounds that deposit copper on the surface of a conductive layer are provided. Such plating baths deposit a copper layer that is substantially planar on a substrate surface across a range of electrolyte concentrations. Methods of depositing copper layers using such copper plating baths are also disclosed.

Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract: The bicyclo-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor are disclosed. The definition of substituents in formula (I) are the same as defined in the description.

Abstract: The present invention provides a method of producing 2-alkyl-3-aminothiophene derivative represented by Formula (4), the method comprising oxidizing a compound represented by the following Formula (1) to produce a compound represented by the following Formula (3) and reducing the compound represented by the following Formula (3): wherein in Formula (1), Formula (3), and Formula (4), R represents an alkyl group, a cycloalkyl group, or a bicycloalkyl group; and X represents a hydroxyl group, a halogen atom acyloxy group, an alkylsulfonyl group, or an arylsulfonyl group.

Abstract: The invention describes a novel process for synthesizing pyrazoles by means of oxidative conversion of enamines with suitable N-containing carboxylic acid derivatives.

Abstract: The present invention relates to a process for preparing a compound of formula (II) wherein R1 is CF3, CF2H or CFH2, and R2 and R3 are both independently C1-C6 alkyl, comprising a) reacting compounds of formula (IV), (V) and (VI) wherein R3 is as defined for the compound of formula (II), R4OM (V) wherein M is a lithium, sodium or potassium ion and R4 is C1-C6 alkyl, and (VI) wherein R1 is as defined for the compound of formula (II) and R5 is CrC6 alkyl, to form an enolate of formula (VII) wherein M is as defined for the compound of formula V and R1 and R3 are defined for the compound of formula (II), b) releasing the compound of formula (VIII) wherein R1 and R3 are as defined for the compound of formula (II), from the enolate of formula (VII) by means of an acid, and c) converting the compound of formula (VIII), in the presence of the salt formed from cation M and the anion of the acid in step b), to a compound of formula (II).

Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.

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: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1, R2, R3, R4, R5 and R6 are as defined herein: and compositions, processes for the preparation, and uses thereof, e.g. in the treatment of endometriosis or uterine fibroids.

Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 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 process and intermediates for preparing such compounds.

Abstract: The invention relates to pyrazoline substituted compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder.

Abstract: The present invention relates to screens for compounds that can induce stem cell differentiation. In addition, isoxazoles and sulfonyl hydrazones are identified as general classes of compounds that can induce differentiation of stem cells into cells of neuronal and cardiac fate, respectively.

Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

Abstract: [Problem]A compound which is useful as a GK activator is provided. [Means for Solution] The present inventors have conducted studies on compounds having a GK activating action, which are promising as active ingredients of pharmaceutical compositions for the treatment of diabetes, type 2 diabetes mellitus, obesity, metabolic syndrome and related diseases caused by the aforementioned diseases, and as a result, they have confirmed that a benzamide compound of the present invention has an excellent GK activating action, thereby completing the present invention. That is, the benzamide compound of the present invention has a GK activating action and can be used as an agent for preventing and/or treating diabetes, type 2 diabetes mellitus, obesity, metabolic syndrome, and related diseases caused by the aforementioned diseases.

Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.

Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

Abstract: 4-(3-Alkylthiobenzoyl)pyrazoles of the formula (I) are described as herbicides. In this formula (I), X, Y, R1, R2, R3 and R4 represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen.

Abstract: The invention relates to aminopyrazole derivatives of formula (I), wherein A, E, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.

Abstract: Substituted phenylureas and phenylamides, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for preparing pharmaceutical compositions.

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

Abstract: Compounds of formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.

Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

Abstract: A process for preparing 1,3-disubstituted pyrazole compounds.

Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.

Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.

Abstract: The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R4, R5, R6 and R7 are as defined in the specification; or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.

Abstract: The invention relates to a compound of formula (I), which is suitable for use as a herbicide wherein G is hydrogen or an agriculturally acceptable metal, sulfonium, ammonium or latentiating group; Q is a unsubstituted or substituted C3-C8 saturated or mono-unsaturated heterocyclyl containing at least one heteroatom selected from O, N and S, or Q is heteroaryl or substituted heteroaryl; m is 1, 2 or 3; and Het is an optionally substituted monocyclic or bicyclic heteroaromatic ring; and wherein the compound is optionally an agronomically acceptable salt thereof.

Abstract: Compounds of formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.