936343-48-5Relevant articles and documents
Selective Bruton's tyrosine kinase inhibitor and application thereof
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Paragraph 0162-0165; 0167, (2018/06/04)
The invention discloses a selective Bruton's tyrosine kinase (BTK) inhibitor compound, a pharmaceutical composition, preparation and application thereof to preparation of medicines for treating diseases, disorders or symptoms obtained from inhibition of Bruton's tyrosine kinase activity. The compound disclosed by the invention has anti-proliferation and inhibition effects on tumor cell lines including A549, MINO, OCI-LY10, TMD-8 and the like, has good anti-tumor activity in tumor models including Mino subcutaneous xenoplastic transplantation and the like and can be applied to medicines for treating solid tumors or leukemia related to human or animal cell proliferation; the compound disclosed by the invention has relatively good pharmacokinetic performance and can be orally taken to treat the solid tumors or the leukemia related to the human or animal cell proliferation or autoimmune diseases; the compound disclosed by the invention has a low hERG channel blocking property.
Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: Identification of candidates for clinical development
Letavic, Michael A.,Aluisio, Leah,Atack, John R.,Bonaventure, Pascal,Carruthers, Nicholas I.,Dugovic, Christine,Everson, Anita,Feinstein, Mark A.,Fraser, Ian C.,Hoey, Kenway,Jiang, Xiaohui,Keith, John M.,Koudriakova, Tatiana,Leung, Perry,Lord, Brian,Lovenberg, Timothy W.,Ly, Kiev S.,Morton, Kirsten L.,Timothy Motley,Nepomuceno, Diane,Rizzolio, Michele,Rynberg, Raymond,Sepassi, Kia,Shelton, Jonathan
scheme or table, p. 4210 - 4214 (2010/09/04)
The pre-clinical characterization of novel aryloxypyridine amides that are histamine H3 receptor antagonists is described. These compounds are high affinity histamine H3 ligands that penetrate the CNS and occupy the histamine H3 receptor in rat brain. Several compounds were extensively profiled pre-clinically leading to the identification of two compounds suitable for nomination as development candidates.