发明名称 Pyridine-2-amides useful as CB2 agonists
摘要 The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) is a CB2 agonist and can be used as an active ingredient in a medicament.;
申请公布号 US9409866(B2) 申请公布日期 2016.08.09
申请号 US201314648412 申请日期 2013.12.04
申请人 HOFFMANN-LA ROCHE INC. 发明人 Grether Uwe;Kimbara Atsushi;Nettekoven Matthias;Ricklin Fabienne;Roever Stephan;Rogers-Evans Mark;Rombach Didier;Schulz-Gasch Tanja;Westphal Matthias
分类号 C07D213/81;C07D401/04;A61K31/444;C07D405/12;C07D491/107;C07D413/14;C07D401/06;C07D401/12;C07D405/04;C07D409/12;C07D413/12;C07D417/12;C07D417/14;C07D491/10 主分类号 C07D213/81
代理机构 Genentech, Inc. 代理人 Genentech, Inc. ;Andrus Alex
主权项 1. A compound of formula (I) wherein R1 is halogen, halophenyl, cycloalkylalkoxy, halophenylalkyl, oxetanyloxy, haloalkoxy, halophenylalkoxy or alkyloxetanylalkoxy; R2 is halogen, cycloalkyl, haloazetidinyl, halopyrrolidinyl, cycloalkenyl, halocycloalkyl or halooxetanyl; one of R3 and R4 is hydrogen or alkyl and the other one is —(CR5R6)—(CR7R8)n—R9; or R3 and R4 together with the nitrogen atom to which they are attached form 2-oxo-5-aza-spiro[3.4]octyl, haloazetidinyl or halopyrrolidinyl; R5 and R6 are independently selected from hydrogen, alkyl, cycloalkylalkyl, haloalkyl, cycloalkyl, alkylsulfonylalkyl, phenylalkoxyalkyl, hydroxyalkyl, haloazetidinylalkyl, haloazetidinylcarbonyl, 2-oxa-6-azaspiro[3,3]heptanylcarbonyl, alkylaminocarbonyl, di alkylaminocarbonyl, aminocarbonyl, azetidinylcarbonyl, oxetanyl alkyl and alkyl oxetanyl; or R5 and R6 together with the carbon atom to which they are attached form cycloalkyl, oxetanyl, oxanyl or dioxothietanyl; R7 and R8 are independently selected from hydrogen, alkyl and cycloalkyl; or R7 and R8 together with the carbon atom to which they are attached form cycloalkyl; R9 is alkyl, alkoxycarbonyl, hydroxyl, hydroxyalkyl, aminocarbonyl, cyano, pyridinyl, alkylaminocarbonyl, thiazol-2-yl, oxazol-2-yl, 5-alkyl-[1,2,4]oxadiazol-3-yl, alkyltetrazolyl, alkylthiazol-2-yl, 1H-tetrazolyl, 5-amino-[1,2,4]-oxadiazol-3-yl, 5-alkyl-[1,3,4]-oxadiazol-2-yl, azetidinylcarbonyl, haloazetidinylcarbonyl, 6-oxa-1-azaspiro[3.3]heptanyl, 5-phenyl-[1,3,4]-oxadiazol-2-yl or haloalkylaminocarbonyl; and n is 0 or 1; provided that when R3 and R4 are both alkyl at the same time, then R1 and R2 are not both halogen at the same time; or a pharmaceutically acceptable salt or ester thereof.
地址 Little Falls NJ US