- 6H-THIENO[2,3-E][1,2,4]TRIAZOLO[3,4-C][1,2,4]TRIAZEPINE DERIVATIVE
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The 6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,2,4]triazepine derivatives or salts thereof of the present invention have BRD4 inhibitory activity, and thus, they are useful as medicaments, in particular, as prophylaxis and/or therapeutic agents for diseases associated with BRD4.
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Paragraph 0094-0095
(2020/05/07)
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- EIF4A-INHIBITING COMPOUNDS AND METHODS RELATED THERETO
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The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds X, Y, R1, R2, R3a, R3b, R4a, R4b and R5 are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4A and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
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Paragraph 1027; 1028
(2017/08/01)
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- SUBSTITUTED PYRIDIZINONE DERIVATIVES AS PDE10 INHIBITORS
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The present invention is directed to substituted pyridizinone compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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Page/Page column 84; 85
(2014/09/29)
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- SUBSTITUTED PYRIDIZINONE DERIVATIVES AS PDE10 INHIBITORS
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The present invention is directed to substituted pyridizinone compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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Page/Page column 84; 85
(2014/10/04)
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- HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
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The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
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Page/Page column 189-190
(2011/10/05)
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- HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
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The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
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Page/Page column 87
(2010/06/11)
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- CYTOKINE PRODUCTION INHIBITORS, TRIAZEPINE COMPOUNDS, AND INTERMEDIATES THEREOF
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The present invention relates to a cytokine production inhibitor comprising a compound of the formula [I] wherein R1is aryl or heteroaryl; B is a group of the formula (a) or (b) wherein R2is hydrogen atom, hydroxy, halogen atom and t
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- Therapeutic agent for osteoporosis and triazepine compound
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Therapeutic agents for osteoporosis comprising, as an active ingredient, a triazepine compound of the formula ?I! STR1 wherein R1 is aryl or heteroaryl; R2 is hydrogen atom, hydroxy, halogen atom or lower alkyl; R4 is hydrogen atom or halogen atom, or R2 and R4 form carbonyl combinedly together with the carbon atom to which they bond; R3 is hydrogen atom, lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, --X--Y wherein X is --(CH2)m --, --CO--, --COCH2 --, --NH--, --NHCH2 --, --CH2 NH--, --CH2 NHCO--, --OCH2 --, --(CH2)n O-- or --CH2 S-- and Y is halogen atom, cycloallyl, aryl or heteroaryl; and A is benzene ring or thiophene ring, or a salt thereof, novel triazepine compounds, and intermediate triazepine compounds for producing these triazepine compounds. The triazepine compounds of the formula ?I! have superior bone resorption-inhibitory action and are useful as therapeutic agents for osteoporosis.
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