412327-07-2Relevant articles and documents
6H-THIENO[2,3-E][1,2,4]TRIAZOLO[3,4-C][1,2,4]TRIAZEPINE DERIVATIVE
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Paragraph 0094-0095, (2020/05/07)
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.
EIF4A-INHIBITING COMPOUNDS AND METHODS RELATED THERETO
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Paragraph 1027; 1028, (2017/08/01)
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.
SUBSTITUTED PYRIDIZINONE DERIVATIVES AS PDE10 INHIBITORS
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Page/Page column 84; 85, (2014/09/29)
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.
SUBSTITUTED PYRIDIZINONE DERIVATIVES AS PDE10 INHIBITORS
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Page/Page column 84; 85, (2014/10/04)
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.
Development and a practical synthesis of the JAK2 inhibitor LY2784544
Mitchell, David,Cole, Kevin P.,Pollock, Patrick M.,Coppert, David M.,Burkholder, Timothy P.,Clayton, Joshua R.
, p. 70 - 81 (2012/05/31)
The route selection and process research and development of a practical synthesis for JAK2 inhibitor LY2784544 is described. The first-generation synthesis route, similar to that used in discovery for derivatization of a benzylic amine moiety, was 14 overall steps and possessed several steps that required extensive development for large-scale production. Route selection considerations led to a modified synthesis that utilized a novel vanadium-catalyzed carbon-carbon bond-forming arylation reaction for incorporation of the key benzylic morpholine moiety. A protecting group used to mask an amino pyrazole unit was modified from PMB to tert-butyl, resulting in a dramatic reduction in the overall length of the route. These two major changes resulted in an eight-step synthesis, which was six steps shorter than the first-generation synthesis. In the pilot plant, the new synthesis was scaled to produce >100 kg of LY2784544 in high yield and purity under GMP conditions. The overall development including the vanadium-catalyzed C-C bond-forming methodology, a ketone reductive deoxygenation, and a palladium-catalyzed amination is described.
HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
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Page/Page column 189-190, (2011/10/05)
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.
AMINO PYRAZOLE COMPOUND
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Page/Page column 2, (2010/06/22)
The present invention provides amino pyrazole compounds useful in the treatment of chronic myeloproliferative disorders and various cancers, e.g., glioblastoma, breast cancer, multiple myeloma, prostate cancer, and leukemias.
HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
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Page/Page column 87, (2010/06/11)
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.
Anti-HIV pyrazole derivatives
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, (2008/06/13)
The present invention comprises novel and known pyrazole derivatives having anti-HIV activity, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors
CYTOKINE PRODUCTION INHIBITORS, TRIAZEPINE COMPOUNDS, AND INTERMEDIATES THEREOF
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, (2008/06/13)
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