The invention relates to novel pyrrolidine derivatives of formula (I):
wherein R
1
, R
2
and R
3
are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
[EN] SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS<br/>[FR] COMPOSÉS PYRAZOLO[1,5-A]PYRIMIDINE SUBSTITUÉS UTILISÉS COMME INHIBITEURS DE MTOR
申请人:ARRAY BIOPHARMA INC
公开号:WO2011029027A1
公开(公告)日:2011-03-10
Compounds of Formula I: and salts thereof in which R1, R2, R2a, R3, n, X and ring B have the meanings given in the specification, are inhibitors of mTOR and are useful in the treatment of diseases which are sensitive to inhibition of mTOR, such as cancers.
[EN] HETEROCYLCIC DERIVATIVES AS INHIBITORS OF GLUTAMINYL CYCLASE<br/>[FR] DÉRIVÉS HÉTÉROCYCLIQUES EN TANT QU'INHIBITEURS DE GLUTAMINYLE CYCLASE
申请人:PROBIODRUG AG
公开号:WO2011029920A1
公开(公告)日:2011-03-17
The invention relates to novel pyrrolidine derivatives of formula (I), wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS
申请人:Andrews Steven W.
公开号:US20120178715A1
公开(公告)日:2012-07-12
Compounds of Formula I: and salts thereof in which R
1
, R
2
, R
2a
, R
3
, n, X and ring B have the meanings given in the specification, are inhibitors of mTOR and are useful in the treatment of diseases which are sensitive to inhibition of mTOR, such as cancers.
2,3,5-Trisubstituted Thiophene Compounds and Uses Thereof
申请人:Barnes David
公开号:US20130123252A1
公开(公告)日:2013-05-16
The present invention provides a compound of formula I:
a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.