- OGA INHIBITOR COMPOUNDS
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The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations; or alpha synucleinopathies, in particular Parkinson's disease, dementia due to Parkinson's (or neurocognitive disorder due to Parkinson's disease), dementia with Lewy bodies, multiple system atrophy, or alpha synucleinopathy caused by Gaucher's disease.
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Page/Page column 61-62
(2021/06/26)
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- Heteroaromatic acetamide derivative, preparation and applications thereof
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The present invention provides a heteroaromatic acetamide derivative, a preparation and applications thereof, wherein the derivative comprises a pharmaceutically acceptable salt and/or a solvate thereof. According to the present invention, the experiment results prove that the heteroaromatic acetamide derivative can specifically bind to transient receptor potential ankyrin 1 (TRPA1) and inhibit orreduce the activity of TRPA1, and can be used for treating diseases mediated by TRPA1; and the inhibitor of the present invention further comprises a pharmaceutical composition of the compound, and amethods for preparing the compounds. The derivative has a general formula defined in the specification.
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- Substituted indole compound and method and use thereof
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The invention provides a new indole compound, pharmaceutically acceptable salts and medicinal preparations thereof, and a use of the new indole compound in selective inhibition of 5-hydroxytryptamine reuptake and /or excitation of a 5-HT1A receptor. The invention also relates to medicinal compositions comprising the compounds, and a method for treating the central nervous system dysfunction of mammals, especially humans by using the medicinal compositions.
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Paragraph 0327; 0328; 0409; 04011; 0412
(2018/11/03)
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- Two analogues of fenarimol show curative activity in an experimental model of chagas disease
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Chagas disease, caused by the protozoan parasite Trypanosoma cruzi (T. cruzi), is an increasing threat to global health. Available medicines were introduced over 40 years ago, have undesirable side effects, and give equivocal results of cure in the chronic stage of the disease. We report the development of two compounds, 6 and (S)-7, with PCR-confirmed curative activity in a mouse model of established T. cruzi infection after once daily oral dosing for 20 days at 20 mg/kg 6 and 10 mg/kg (S)-7. Compounds 6 and (S)-7 have potent in vitro activity, are noncytotoxic, show no adverse effects in vivo following repeat dosing, are prepared by a short synthetic route, and have druglike properties suitable for preclinical development.
- Keenan, Martine,Chaplin, Jason H.,Alexander, Paul W.,Abbott, Michael J.,Best, Wayne M.,Khong, Andrea,Botero, Adriana,Perez, Catherine,Cornwall, Scott,Thompson, R. Andrew,White, Karen L.,Shackleford, David M.,Koltun, Maria,Chiu, Francis C. K.,Morizzi, Julia,Ryan, Eileen,Campbell, Michael,Von Geldern, Thomas W.,Scandale, Ivan,Chatelain, Eric,Charman, Susan A.
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p. 10158 - 10170
(2014/01/17)
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- GLYCINE COMPOUND
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[Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.
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Page/Page column 24; 77; 87
(2012/07/28)
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- NOVEL HETEROCYCLES
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Described are novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs th
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Page/Page column 75
(2009/09/05)
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- Novel heterocycles
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The present invention relates to novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prod
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Page/Page column 42
(2010/11/27)
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- NOVEL HETEROCYCLES
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The present invention relates to novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prod
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Page/Page column 68-69
(2010/11/28)
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- INSECTICIDAL 3-(DIHALOALKENYL) PHENYL DERIVATIVES
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Certain novel 3-(dihaloalkenyl)phenyl derivatives have unexpected insecticidal activity. These compounds are represented by formula (I), where R through R5, a, b, D, E, G and U are fully described herein. In addition, compositions comprising an
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Page/Page column 23
(2008/06/13)
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- Parallel synthesis of N-arylpiperazines using polymer-assisted reactions
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A series of N-arylpiperazines were prepared in a parallel fashion using palladium-catalyzed cross-coupling, or nucleophilic aromatic displacement chemistries, and polymer-assisted sequestration and purification techniques as key steps.
- Duncton, Matthew A. J.,Roffey, Jonathan R. A.,Hamlyn, Richard J.,Adams, David R.
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p. 2549 - 2552
(2007/10/03)
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- PROLINE DERIVATIVES AND USE THEREOF AS DRUGS
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The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.
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- IMIDAZO[1,2-A]PYRIDINES FOR THE TREATMENT OF CNS AND CARDIAC DISEASES
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The present invention relates to imidazo[1,2-a]pyridine compounds of formula (1) STR1 which are dopamine D-4 antagonists and useful as anti-psychotic agents.
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- PHARMACEUTICAL COMPOSITION CONTAINING 1-(MONO- OR BIS(TRIFLUOROMETHYL)-2-PYRIDINYL)-PIPERAZINES
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Pharmaceutical composition which is useful as a medicinal product, in particular for the treatment of disorders of the central nervous system, characterized in that it contains customary pharmaceutical excipients, and at least one of the compounds of formula STR1 in which the trifluoromethyl substituent is at the 4-position, at the 5-position, or at 4-and 5-positions of the pyridinyl ring, and the substituent R denotes either hydrogen or a halogen, such as chlorine, at position(s) of the pyridinyl ring not occupied by CF 3, and its pharmaceutically acceptable salts.
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