- FUSED TRICYCLIC HETEROCYCLIC COMPOUNDS AS INHIBITORS OF PIKFYVE KINASE USEFUL FOR THE TREATMENT OF NEUROLOGICAL DISEASES
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The present disclosure provides compounds that are inhibitors of PIKfyve and/or PI3 kinases, and are therefore useful for the treatment of neurological diseases that are treatable by inhibition of PIKfyve. Also provided are pharmaceutical compositions containing such compounds, and methods of treatment using such compounds.
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Paragraph 0131; 0132
(2021/06/11)
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- SUBSTITUTED PYRAZOLO-PYRIMIDINES AND USES THEREOF
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The present disclosure provides compounds that are inhibitors of PIKfyve kinases useful for the treatment of neurological diseases treatable by inhibition of PIKfyve. Also provided are pharmaceutical compositions containing such compounds, and methods of
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Paragraph 0160-0162
(2021/07/24)
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- 5- OR 7-AZAINDAZOLES AS BETA-LACTAMASE INHIBITORS
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The present invention relates to β-lactamase inhibitors having the following general formula (I): wherein R1-R4 and X1-X2 are defined in the specification, pharmaceutical composition thereof, and use thereof for the treatment of a bacterial infection, alone or in combination with β-lactam antibiotics and/or other antibiotics and/or other β-lactamase inhibitors.
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Page/Page column 41; 43; 44
(2020/09/19)
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- MULTISUBSTITUTED AROMATIC COMPOUNDS AS INHIBITORS OF THROMBIN
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There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.
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- MULTISUBSTITUTED AROMATIC COMPOUNDS AS SERINE PROTEASE INHIBITORS
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There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of kallikrein, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of kallikrein.
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- NOVEL ANTIPLATELET AGENT
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The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d,Xb1-Xb5 are the same or different, and are nitrogen or carbon,R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino,R2 is an optionally substituted aryl or an optionally substituted heteroaryl,R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.
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Page/Page column 69-70
(2012/10/18)
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- MULTISUBSTITUTED AROMATIC COMPOUNDS AS INHIBITORS OF THROMBIN
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There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.
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- PYRAZOLO-PYRIMIDINE COMPOUNDS
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The present invention has searched for a variety of compounds which show IL-12/IL-23 production-inhibitory activities and herein provides a pharmaceutical composition and an agent for preventing or treating IL-12/IL-23 excess production-related diseases, which comprise the compound.
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Page/Page column 28; 29
(2011/12/13)
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- SYNTHESIS OF PYRAZOLES
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The present invention provides methods of making HCl salts, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other
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Page/Page column 58
(2009/08/16)
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- PYRAZOLE [3, 4-B] PYRIDINE RAF INHIBITORS
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Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
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Page/Page column 111
(2009/10/22)
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- NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS
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The present invention provides compounds of formula (I) and compositions thereof, methods of making them, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.
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Page/Page column 59
(2008/12/07)
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- Synthesis of a new series of ditopic proligands for metal salts: Differing regiochemistry of electrophilic attack at 3{5}-amino-5{3}-(pyrid-2-yl)-1H- pyrazole
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An improved synthesis of 3{5}-amino-5{3}-(pyrid-2-yl)-1H-pyrazole (I) is described, which affords the compound on a multi-gram scale. Reaction of I with acid chloride and isothiocyanate electrophiles in MeCN cleanly results in attack at its amino group, y
- Pask, Christopher M.,Camm, Kenneth D.,Kilner, Colin A.,Halcrow, Malcolm A.
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p. 2531 - 2534
(2007/10/03)
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