801303-33-3Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of aryl N-methoxyamide derivatives as GPR119 agonists
Jang, Yoon Kyung,Lee, Kyu Myung,Jung, Kwan-Young,Kang, Seung Kyu,Pagire, Suvarna H.,Lee, Jun Mi,Pagire, Haushabhau S.,Kim, Kwang Rok,Bae, Myung Ae,Lee, Hohjai,Rhee, Sang Dal,Ahn, Jin Hee
supporting information, p. 3909 - 3914 (2017/07/27)
A series of N-methoxyamide derivatives was identified and evaluated as GPR119 agonists. Several N-methoxyamides with thienopyrimidine and pyridine scaffolds showed potent GPR119 agonistic activities. Among them, compound 9c displayed good in vitro activity and potency. Moreover, compound 9c lowered glucose excursion in mice in an oral glucose tolerance test and increased GLP-1 secretion in intestinal cells.
SUBSTITUTED TRICYCLIC 1,4-BENZODIAZEPINONE DERIVATIVES AS ALLOSTERIC MODULATORS OF GROUP II METABOTROPIC GLUTAMATE RECEPTORS
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Page/Page column 229-230, (2017/05/28)
The present invention provides novel tricyclic 1,4-benzodiazepinone derivatives of the general formula (I) and pharmaceutical compositions containing them. Moreover, the compounds of formula (I) and the pharmaceutical compositions containing them are provided for use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. The tricyclic 1,4-benzodiazepinone derivatives of formula (I) can act as modulators of nervous system receptors sensitive to glutamate, in particular as modulators of metabotropic glutamate receptors (mGluRs), which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. The present invention further provides tricyclic 1,4-benzodiazepinone derivatives of formula (I) that are modulators of metabotropic glutamate receptors (mGluRs), particularly positive allosteric modulators of mGluRs, and more specifically positive allosteric modulators of mGluR3. (I)
DIHYDROPYRAZOLOPYRIMIDINONE COMPOUNDS AS PDE2 INHIBITORS
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Page/Page column 55; 62, (2016/12/22)
The present invention is directed to dihydropyrazolopyrimidinonecompounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
5-(3-isopropyl benzisoxazol)pyrazin-2-amine and preparation method thereof
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Paragraph 0032; 0036, (2016/12/22)
The invention discloses 5-(3-isopropyl benzisoxazol)pyrazin-2-amine and a preparation method thereof. The 5-(3-isopropyl benzisoxazol)pyrazin-2-amine has the structural formula represented by the formula (I). The compound is a new benzisoxazole compound, provides a new bactericidal drug for people, and further broadens research fields of benzoisoxazole compounds. Moreover, the reaction total yield for preparation of the compound is high, and the process is simple and is suitable for industrialized production.
ANTIDIABETIC BICYCLIC COMPOUNDS
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Page/Page column 85, (2016/04/26)
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
NITROGENATED HETEROCYCLIC COMPOUND
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Paragraph 0620; 1120, (2015/03/28)
The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.
HETEROCYCLIC COMPOUNDS AS CALCIUM SENSING RECEPTOR MODULATORS FOR THE TREATMENT OF HYPERPARATHYROIDISM, CHRONIC RENAL FAILURE AND CHRONIC KIDNEY DISEASE
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Page/Page column 50, (2015/11/16)
The invention relates to heterocyclic compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their pharmaceutical compositions for use in medicine for the treatment of diseases or disorders associated with the modulation of calcium sensing receptor modulators (CaSR), like e.g. hyperparathyroidism, chronic renal failure and chronic kidney disease and their complications.
ALKYNE-BRIDGED HETERO-AROMATICS AND USES THEREOF
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Paragraph 0291; 0292, (2013/06/28)
This invention relates to novel alkyne-bridged hetero-aromatics as described in the specification which are PDE10A inhibitors and useful for the treatment of neurological, psychiatric disorder, metabolic disorders, such as Schizophrenia, Parkinson's disea
HETEROCYCLIC COMPOUND AND USE THEREOF
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Page/Page column 69, (2012/06/01)
The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and use thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
PHTALAZINE DERIVATIVES AS JAK1 INHIBITORS
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Page/Page column 42, (2012/04/04)
JAK1 inhibitors of structural formula (I), wherein Ar1, Ar2, Q, W, X, Y, and Z are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.
