30129-53-4Relevant articles and documents
NOVEL CONDENSED HETEROCYCLIC COMPOUND
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Paragraph 0245, (2017/05/12)
PROBLEM TO BE SOLVED: To provide a compound having PDE2A selective inhibitory action, and a pharmaceutical composition comprising the same. SOLUTION: The present invention provides a compound represented by formula (I) or their pharmaceutically acceptable salt, or their solvate, and a pharmaceutical composition comprising them [m is an integer of 1 to 5; Y1 is N or C; Y2 is C-R2a or N-R2b; ring B is a benzene ring or the like; Z is CR5aR5b or O; R1 is a C1-6 alkyl group or the like; R2a is a halogen atom, a C1-6 alkyl group or the like; R2b is a C1-6 alkyl group or the like; R3a and R3b each independently represent H, a C1-6 alkyl group or the like; R4 independently represent a hydroxy group, a halogen atom or the like; R5a and R5b in Z each independently represent H, a C1-6 alkyl group and the like]. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
Substituted annellated pyrimidines and use thereof
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Paragraph 1660; 1661; 1662; 1663, (2014/02/15)
The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating
Structure-based design of a novel series of potent, selective inhibitors of the class i phosphatidylinositol 3-kinases
Smith, Adrian L.,D'Angelo, Noel D.,Bo, Yunxin Y.,Booker, Shon K.,Cee, Victor J.,Herberich, Brad,Hong, Fang-Tsao,Jackson, Claire L. M.,Lanman, Brian A.,Liu, Longbin,Nishimura, Nobuko,Pettus, Liping H.,Reed, Anthony B.,Tadesse, Seifu,Tamayo, Nuria A.,Wurz, Ryan P.,Yang, Kevin,Andrews, Kristin L.,Whittington, Douglas A.,McCarter, John D.,Miguel, Tisha San,Zalameda, Leeanne,Jiang, Jian,Subramanian, Raju,Mullady, Erin L.,Caenepeel, Sean,Freeman, Daniel J.,Wang, Ling,Zhang, Nancy,Wu, Tian,Hughes, Paul E.,Norman, Mark H.
, p. 5188 - 5219 (2012/08/28)
A highly selective series of inhibitors of the class I phosphatidylinositol 3-kinases (PI3Ks) has been designed and synthesized. Starting from the dual PI3K/mTOR inhibitor 5, a structure-based approach was used to improve potency and selectivity, resulting in the identification of 54 as a potent inhibitor of the class I PI3Ks with excellent selectivity over mTOR, related phosphatidylinositol kinases, and a broad panel of protein kinases. Compound 54 demonstrated a robust PD-PK relationship inhibiting the PI3K/Akt pathway in vivo in a mouse model, and it potently inhibited tumor growth in a U-87 MG xenograft model with an activated PI3K/Akt pathway.