1293987-69-5Relevant academic research and scientific papers
COMPOUND HAVING γ TURN STRUCTURE AND LSD1 INHIBITOR USING THE SAME
-
Paragraph 0377-0379; 0383-0385, (2017/12/27)
PROBLEM TO BE SOLVED: To provide a compound having LSD1 inhibitory activity and cancer cell growth inhibitory effect. SOLUTION: There is provided a compound represented by the formula (1) and a salt thereof. (1), where R1 is an alkyl group, a cycloalkyl group, an aralkyl group, an aryl group or a heteroaryl group, R2 is H, an alkyl group, a cycloalkyl group, an aryl group or a heteroaryl group, R3 is H, an alkyl group, a cycloalkyl group, an aralkyl group, an aryl group or a heteroaryl group, R4 is an aryl group or a heteroaryl group, each of the above described groups may be substituted, n is an integer of 2 to 10 and *1 and *2 are asymmetric carbons. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPO&INPIT
C-H activation enables a rapid structure-activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors
Miyamura, Shin,Araki, Misaho,Ota, Yosuke,Itoh, Yukihiro,Yasuda, Shusuke,Masuda, Mitsuharu,Taniguchi, Tomoyuki,Sowa, Yoshihiro,Sakai, Toshiyuki,Suzuki, Takayoshi,Itami, Kenichiro,Yamaguchi, Junichiro
, p. 8576 - 8585 (2016/09/28)
We describe the structure-activity relationship of various arylcyclopropylamines (ACPAs), which are potent LSD1 inhibitors. More than 45 ACPAs were synthesized rapidly by an unconventional method that we have recently developed, consisting of a C-H borylation and cross-coupling sequence starting from cyclopropylamine. We also generated NCD38 derivatives, which are known as LSD1 selective inhibitors, and discovered a more effective inhibitor compared to the original NCD38.
2,7-SUBSTITUTED THIENO[3,2-D] PYRIMIDINE COMPOUNDS AS PROTEIN KINASE INHIBITORS
-
Page/Page column 18, (2012/11/08)
Disclosed are a 2,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comp
2,7-SUBSTITUTED THIENO[3,2-D]PYRIMIDINE COMPOUNDS AS PROTEIN KINASE INHIBITORS
-
Page/Page column 38, (2011/05/06)
Disclosed are a 2,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comp
COMPOUNDS AND METHODS
-
Page/Page column 50, (2011/08/04)
Disclosed are compounds having the formula (I): wherein R1, R2, R3, R4, R5, and R6 are as defined herein, and methods of making and using the same.
SPIROPIPERIDINE COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHERMER’S DISEASE
-
Page/Page column 128, (2010/11/08)
The present invention is directed to spiropiperidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. T
