Abstract: Provided are a tetrahydroisoquinoline derivative, a preparation method therefor and an application thereof in medicine. In particular, provided are a tetrahydroisoquinoline derivative represented by general formula (I), a preparation method therefor and a pharmaceutically acceptable salt thereof as well as use thereof as a therapeutic agent, in particular as an angiotensin II type 2 receptor (AT2R) antagonist, wherein definitions of substituent groups in the general formula (I) are the same as definitions in the description.

Abstract: Methods and pharmaceutical compositions containing gaboxadol or a pharmaceutically acceptable salt thereof for treating 1p36 deletion syndrome are provided.

Abstract: The present invention relates to compounds of general formula (I), wherein the groups R1 and R2 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.

Abstract: A compound represented by formula (I), which is highly effective in controlling harmful arthropods, an intermediate thereof and a production method thereof are described. In formula (I), A1 represents CH or a nitrogen atom; R1 represents a C1-C6 alkyl group optionally having one or more halogen atoms; R5 represents CF3, C2F5, or S(O)mCF3; Q represents NR2C(O)OR3 or N?CR4R6; R2 represents a hydrogen atom or the like; R3 represents a C1-C6 alkyl group optionally having one or more halogen atoms or the like; R4 represents a hydrogen atom or the like; R6 represents a phenyl group optionally having one or more substituents selected from group D, or the like; and n and m each independently are 0, 1, or 2. Group D: a group consisting of C1-C6 alkyl groups optionally having one or more halogen atoms and C1-C6 alkoxy groups optionally having one or more halogen atoms or the like.

Abstract: Methods of treating developmental disorders such as Angelman syndrome, Fragile X syndrome, Fragile X-associated tremor/ataxia syndrome (FXTAS), Autistic Spectrum Disorder, Autism, Asperger's syndrome, pervasive developmental disorder, Childhood Disintegrative Disorder, Rett syndrome, Lanau-Kleffner Syndrome, Prader-Willi Syndrome, Tardive Dyskinesia, and/or Williams Syndrome with gaboxadol or a pharmaceutically acceptable salt thereof are provided. The methods provide therapeutic compositions that may be used to improve one or more symptoms of the developmental disorder.

Abstract: Treatment of Tourette syndrome using gaboxadol or a pharmaceutically acceptable salt thereof is provided. Treatment of tics using gaboxadol or a pharmaceutically acceptable salt thereof is provided. Treatment of stuttering using gaboxadol or a pharmaceutically acceptable salt thereof is provided. Therapeutic compositions that may be used to improve one or more symptoms of Tourette syndrome are provided. Therapeutic compositions that may be used to improve one or more symptoms of tics are provided. Also provided are therapeutic compositions that may be used to improve one or more symptoms of stuttering.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, Y, W, A, X, m and n are as defined herein, compositions including the compounds and methods of using the compounds.

Abstract: The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.

Abstract: Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.

Abstract: The present invention is directed to hydroxymethyl piperidine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

Abstract: Methods of sedating a patient undergoing critical care treatment using intravenous gaboxadol are provided.

Abstract: The present invention relates to compounds of the formulas (IA) and (IB) and pharmaceutically acceptable salts thereof, wherein A and R1-R6, are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract: Methods of increasing tonic inhibition in a subject in need thereof, for example a subject with Fragile X syndrome or Angelman syndrome are disclosed. Methods of treating secondary insomnia in a subject with a neurodegenerative disease or disorder are also disclosed.

Abstract: Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.

Abstract: The present invention in general relates Hemoglobin receptor or its part as a novel vaccine candidate against Leishmaniasis. Specifically, the present invention envisages HbR DNA for eliciting immune response in a mammal against Leishmaniasis. Additional aspect of the present invention is related to a vaccine composition for inducing immune response against Leishmaniasis in mammals. In a preferred aspect, the present invention relates to use of HbR-polypeptide as marker for diagnosis of Leishmania in kala-azar patients.

Abstract: Methods of increasing tonic inhibition in a subject in need thereof, for example a subject with Fragile X syndrome or Angelman syndrome are disclosed. Methods of treating secondary insomnia in a subject with a neurodegenerative disease or disorder are also disclosed.

Abstract: Methods of sedating a patient undergoing critical care treatment using intravenous gaboxadol are provided.

Abstract: The present invention relates compounds according to Formula (I) wherein R1 and R2 are independently H or an optionally substituted group selected from an alkyl, a heteroalkyl, an aryl, a heteroaryl, an arylalkyl, and a heteroarylalkyl, and R3 and R4 taken together form a carbonyl (?O); or wherein R1 and R2 are independently H or an optionally substituted group selected from an alkyl, a heteroalkyl, an aryl, a heteroaryl, an arylalkyl, and a heteroarylalkyl, R3 is H and R4 is H or —OR5, wherein R5 is H or an optionally substituted group selected from an alkyl, a heteroalkyl, an aryl, a heteroaryl, an arylalkyl, and a heteroarylalkyl; or pharmaceutically acceptable salts or esters thereof, for use in the treatment of kidney disease, in particular in the treatment of acute kidney injury. The present invention also relates to methods of treatment of the same and methods of kidney transplant surgery and coronary artery bypass graft surgery using the compounds of Formula (I).

Abstract: Compounds of the formula (I), and the agrochemically acceptable salts and N-oxides of those compounds, including all stereoisomers and tautomeric forms, and wherein the substituents are as defined in claim 1, are useful for controlling animal pests and can be prepared in a manner known per se.

Abstract: Methods and compounds for research and treatment of portal hypertension. The use of racemic or non-racemic mixtures of furopyridine isomers to stimulate eNOS function in sinusoidal endothelial cells and to increase NO production in both normal sinusoidal endothelial cells and injured endothelial cells.

Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.

Abstract: Methods of sedating a patient undergoing critical care treatment using intravenous gaboxadol are provided.

Abstract: This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.

Abstract: A harmful arthropod control composition comprising a compound represented by the following Formula (1) wherein each symbol represents definitions described in the specification, and one or more fungicidal compounds, which are selected from among azoles, strobilurins, phenylamides, rice blast controlling compounds, rice sheath blight disease controlling compounds, and other fungicidal compounds. The composition has an excellent controlling effect against harmful arthropods.

Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.

Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.

Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene) Heterocyclopenta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: Methods are provided herein for treating cardiac arrhythmias, such as for treating an arrhythmia syndrome, for example Brugada syndrome, in a subject. In some embodiments, the methods include selecting a subject with Brugada syndrome and administering to the subject an effective amount of an agent that increases the expression or activity of SIRT1 in the subject. In some embodiments, the agent increases Nav1.5 activation. In some embodiments, the agent increases the expression or activity of SRIT1 and increases Nav1.5 activation.

Abstract: The present invention provides imidazothiadiazole compounds of Formula (I) wherein A, B, D, Rx, R1, R2, R3, X1, X2 and s are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments.

Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).

Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.

Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.

Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.

Abstract: The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.

Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.

Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, and A are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.

Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.

Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis and/or systemic lupus.

Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.

Abstract: The present invention relates to deuterium-enriched pyridinonecarboxamides and their derivatives of the formula 1, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT) receptor subtype 4 (5-HT4), and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, Obsessive compulsive disorder, depression, speech improvement in autistic children, sleep apnea in Alzheimer's patients, Age-related macular degeneration (AMD), irritable bowel syndrome, gastroesophageal reflux disease, Crohn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, a

Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LQ and Ar are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.

Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.

Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.

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

Abstract: Neuropeptide S receptor antagonists are provided that bind in functional assays to neuropeptide S receptors; methods are provided for use of these antagonists in treatment of conditions or disease states that are ameliorated by blocking of the neuropeptide S receptor, including substance abuse and substance abuse relapse; and for use of neuropeptide S receptor antagonists in the manufacture of therapeutics and pro-drugs for therapeutics useful in disease states and conditions sensitive to binding of the neuropeptide S receptor.

Abstract: The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.

Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).