CYCLOBUTYL SULFONES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS

Japanese Patent JP2014210787

A

PROBLEM TO BE SOLVED: To provide a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative γ-secretase while sparing the Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal disorders.SOLUTION: A representative of a novel class of cyclobutyl sulfone derivatives useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal disorders is an N-[trans-3-[(4-chlorophenyl)sulfonyl]-3-(2,5-difluorophenyl)cyclobutyl]-1,1,1-trifluoromethanesulfonamide compound.

RICHARD W HEIDEBRECHT
LI CHAOMIN
BENITO MUNOZ
ANDREW ROSENAU
LAURA M SURDI
PAUL TEMPEST
JASON BRUBAKER
PHIENG SILIPHAIVANH

JP2014121533A

November 13, 2014

June 12, 2014

Click for automatic bibliography generation  

MERCK SHARP & DOHME

C07C317/30; A61K31/18; A61K31/351; A61P25/28; A61P43/00; C07D309/12

JP2006501295A	2006-01-12
JP2004533428A	2004-11-04
JP2011518830A	2011-06-30

WO2003055850A1	2003-07-10
US20070203120A1	2007-08-30
WO2005030709A1	2005-04-07
WO2006123184A2	2006-11-23

JPN6015020163; Ｂｅｓｔ，　Ｊｏｎａｔｈａｎ　Ｄ．　ｅｔ　ａｌ．: 'Ｉｎ　ｖｉｖｏ　ｃｈａｒａｃｔｅｒｉｚａｔｉｏｎ　ｏｆ　Ａbeta（４０）　ｃｈａｎｇｅｓ　ｉｎ　ｂｒａｉｎ　ａｎｄ　ｃｅｒｅｂｒｏｓｐｉｎａｌ　　　　　ｆｌｕｉｄ　ｕｓｉｎｇ　ｔｈｅ　ｎｏｖｅｌ　gamma-' Ｊｏｕｒｎａｌ　ｏｆ　Ｐｈａｒｍａｃｏｌｏｇｙ　ａｎｄ　Ｅｘｐｅｒｉｍｅｎｔａｌ　Ｔｈｅｒａｐｅｕｔｉｃｓ ｖｏｌ．３１７　ｎｏ．２, 2006, ｐｐ．７８６-７９０

Makoto Ono
Yoshinori Kanayama
Michiaki Tsubokura
Kazuteru Shigemori
Iwase Yoshiwa
Yasufumi Shiroyama

Previous Patent: NEW COMPOUND CONTAINED IN BLUE ROSE

Next Patent: TERPENE-CONTAINING COMPOSITION AND METHOD OF MAKING AND USING THE SAME