459-00-7Relevant academic research and scientific papers
Method for producing hematopoietic stem cells using pyrazole compounds
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, (2016/01/10)
An expanding agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful as a therapy for various hematopoietic diseases and useful for improvement in the efficiency of gene transfer into hematopoietic stem cells for gene therapy is provided. A method of producing hematopoietic stem cells and/or hematopoietic progenitor cells, which comprises expanding hematopoietic stem cells by culturing hematopoietic stem cells ex vivo in the presence of a compound represented by the formula following (I), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof (wherein R1 to R8 are as defined in the description).
PYRAZOLE COMPOUNDS HAVING THERAPEUTIC EFFECT ON MULTIPLE MYELOMA
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, (2013/10/07)
Novel therapeutic agents for myeloma are provided. A therapeutic agent for multiple myeloma containing a pyrazole compound represented by the formula (1): wherein R1 is C1-C6 alkyl, C1-C6 alkyl substituted with R17, C1-C6 haloalkyl, phenyl, phenyl substituted with a R11's or the like, R2 is a hydrogen atom, C1-C6 alkyl, phenyl or phenyl optionally substituted with e R21's or the like, R3 is a hydrogen atom or the like, X is a single bond or —(CR6, R7)n—, each of R4 and R5 is independently C1-C6 alkyl or the like, R6 and R7 are hydrogen atoms or C1-C6 alkyl, R8 is phenyl, phenyl optionally substituted with k R81's or the like, a tautomer of the compound or a pharmaceutically acceptable salt or solvate thereof, as an active ingredient.
Use of 5-hydroxy-4H-benzo[1,4]oxazin-3-ones as β2-adrenoceptor agonists
Hoenke, Christoph,Bouyssou, Thierry,Tautermann, Christofer S.,Rudolf, Klaus,Schnapp, Andreas,Konetzki, Ingo
scheme or table, p. 6640 - 6644 (2010/06/12)
Novel β2-agonists with a 5-hydroxy-4H-benzo[1,4]oxazin-3-one moiety as head group are described. Systematic chemical variations at the phenethylamine residue of these compounds lead to the discovery of compound 6m as potent, full agonist of the β2-adrenoceptor with a high β1/β2-selectivity. Molecular modeling revealed an interaction between the carboxylic acid group of 6m and a lysine residue (K305) of the β2-receptor as putative explanation for the high observed selectivity. Further, compound 6m displayed in a guinea pig in vivo model a complete reversal of acetylcholine induced bronchoconstriction which lasted over the complete study time of 5 h.
novel benzoxazinone derivatives as slow-acting betamimetics and use thereof in treatment of respiratory tract diseases
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Page/Page column 6, (2010/02/14)
Benzoxazinone derivatives (I) are new. Benzoxazinone derivatives of formula (I) and their isomers and acid addition salts are new. n : 1 or 2; A : O or a bond; R : 1-6C alkyl or haloalkyl; R 1>-R 3>H, Q 1>, 1-6C haloalkyl, OH, Q 2>OH, OQ 1>, 6-10C aryl, (6-10C)aryl(1-4C)alkyl, (6-10C)aryl(1-6C)alkoxy, COOH, COOQ 1>, OQ 2>COOH, OQ 2>COOQ 1>, NHSO 3H, NHSO 2Q 1>, NH 2, NHQ 1>, N(Q 1>) 2, NO 2, SQ 1>, SO 2Q 1>, SOQ 1>, OCOQ 1>, COQ 1>, NHCOQ 1> or halo; Q 1>1-6C alkyl; Q 2>1-6C alkylene. [Image] ACTIVITY : Antiinflammatory; Antiasthmatic. No biological data given. MECHANISM OF ACTION : Beta mimetic.
