- Oxazolyl pyrimidinone amide compound or medicinal salt thereof, preparation method and application of oxazolyl pyrimidinone amide compound or medicinal salt thereof
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The invention discloses an oxazole pyrimidone amide compound or a pharmaceutically acceptable salt thereof, and a preparation method and application thereof. The oxazole pyrimidone amide compound has the following structural general formula (I) shown in the description, wherein R1 and R2 are respectively and independently selected from hydrogen and C1-3 alkyl, R3 is selected from C1-3 alkyl groups, R4 and R5 are independently selected from 5-6-membered aryl groups, the aryl groups are phenyl groups or heteroaryl groups containing 1-3 heteroatoms, the heteroatoms are selected from oxygen atoms or nitrogen atoms, and the heteroatoms are located at any position on the heteroaryl groups; the aryl is unsubstituted or at least substituted by one or more halogens or C1-3 alkyl groups, C1-3 polyhalogenated alkyl groups and C1-3 alkoxy groups. The invention also discloses an application of the compound as a TRPA1 antagonist, and the compound is used for preparing medicines for treating or preventing diseases, symptoms and/or obstacles regulated by TRPA1, such as pain and the like.
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Paragraph 0068-0069
(2021/05/15)
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- HYDROXY FORMAMIDE DERIVATIVES AND THEIR USE
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Disclosed are compounds having the formula: (I) wherein R1, R2 and R3 are as defined herein, and methods of making and using the same, including use as inhibitors of BMP1, TLL1 and/or TLL2 and in treatment of diseases associated with BMP1, TLL1 and/or TLL2 activity.
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Page/Page column 97; 98
(2017/01/26)
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- N-(3-PYRIDYL) BIARYLAMIDES AS KINASE INHIBITORS
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The present invention provides a compound of formula (I): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula (I), and pharmaceutical compositions comprising such compounds.
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Page/Page column 41
(2014/03/25)
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- NOVEL RING-SUBSTITUTED N-PYRIDINYL AMIDES AS KINASE INHIBITORS
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The present invention provides a compound of formula (A): I as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
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Page/Page column 43-44
(2014/01/07)
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- CYCLIC ETHER COMPOUNDS USEFUL AS KINASE INHIBITORS
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The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof, as further described herein. Also provided are formulations comprising compounds of formula I, and a method to use such compounds for treating a disease or condition mediated by Provirus Integration of Maloney Maloney Kinase (PIM Kinase), GSK3, PKC, KDR, PDGFRa, FGFR3, FLT3, or cABL.
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Page/Page column 62-63
(2012/02/01)
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- SUBSTITUTED N-(1H-INDAZOL-4-YL)IMIDAZO[1,2-a]PYRIDINE-3-CARBOXAMIDE COMPOUNDS AS TYPE III RECEPTOR TYROSINE KINASE INHIBITORS
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Compounds of Formula I: and pharmaceutically acceptable salts thereof in which R1, R2, R3, R4, R5 and R6 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of fibrosis, bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, pain and burns in a mammal
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Page/Page column 91-92
(2012/06/30)
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- TETRASUBSTITUTED CYCLOHEXYL COMPOUNDS AS KINASE INHIBITORS
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The present invention provides a compound of formula (I): as further described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
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- NOVEL KINASE INHIBITORS
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The present invention provides compounds of Formula I: and related compounds as further described herein, and pharmaceutical compositions comprising these compounds. The invention further provides methods to use these compounds and compositions for treating disorders associated with undesired levels of Pim kinase activity, including cancers and autoimmune disorders.
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- Kinase inhibitors and methods of their use
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New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
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Page/Page column 46
(2010/04/23)
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