[EN] (3-HYDROXY-4-AMINO-BUTAN-2-YL) -3- (2-THIAZOL-2-YL-PYRROLIDINE-1-CARBONYL) BENZAMIDE DERIVATIVES AND RELATED COMPOUNDS AS BETA-SECRETASE INHIBITORS FOR TREATING [FR] DÉRIVÉS DE (3-HYDROXY-4-AMINO-BUTAN-2-YL) -3- (2-THIAZOL-2-YL-PYRROLIDINE-1-CARBONYL) BENZAMIDE ET COMPOSÉS ASSOCIÉS UTILISÉS EN TANT QU'INHIBITEURS DE LA BÊTA-SÉCRÉTASE POUR LE TRAITEMENT
The present invention describes 2-methyl-quinazoline compounds of general formula (I), methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions. The 2-methyl substituted quinazoline compounds of general formula(I) effectively and selectively inhibit the Ras-Sos interaction without significantly targeting the EGFR receptor. They are therefore useful for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, such as cancer as a sole agent or in combination with other active ingredients.
[EN] ORAL COMPLEMENT FACTOR D INHIBITORS<br/>[FR] INHIBITEURS DE FACTEUR D DU COMPLÉMENT ORAL
申请人:BIOCRYST PHARM INC
公开号:WO2021072156A1
公开(公告)日:2021-04-15
Disclosed are compounds of formula (I)-(IV), and pharmaceutically acceptable salts thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity.
TETRAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS
申请人:Dillon Michael Patrick
公开号:US20150191487A1
公开(公告)日:2015-07-09
Compounds of the formula I:
or a pharmaceutically acceptable salt thereof, wherein, R
1
is optionally substituted tetrazolyl, R
2
is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R
3
, R
4
, R
5
and R
6
are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X
3
and/or a P2X
2/3
receptor antagonist and methods of making the compounds.
Tetrazole-substituted arylamides as P2X3 and P2X2/3 antagonists
申请人:Dillon Patrick Michael
公开号:US20080004442A1
公开(公告)日:2008-01-03
Compounds of the formula I:
or a pharmaceutically acceptable salt thereof, wherein, R
1
is optionally substituted tetrazolyl, R
2
is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R
3
, R
4
, R
5
and R
6
are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X
3
and/or a P2X
2/3
receptor antagonist and methods of making the compounds.
A compound of formula (I) as detailed in the specification or a pharmaceutically acceptable salt or solvate thereof, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.