发明名称 NOVEL PYRIDINE DERIVATIVES
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) can be used as a medicament.
申请公布号 US2016137606(A1) 申请公布日期 2016.05.19
申请号 US201615002681 申请日期 2016.01.21
申请人 Hoffmann-La Roche Inc. 发明人 Bissantz Caterina;Grether Uwe;Hebeisen Paul;Kimbara Atsushi;Liu Qingping;Nettekoven Matthias;Prunotto Marco;Roever Stephan;Rogers-Evans Mark;Schulz-Gasch Tanja;Ullmer Christoph;Wang Zhiwei;Yang Wulun
分类号 C07D213/81;C07D213/79;C07D491/107;C07D413/14;C07D417/12;C07D401/04;C07D413/12;C07D405/04 主分类号 C07D213/81
代理机构 代理人
主权项 1. A compound of formula (I) wherein R1 is selected from the group consisting of: cycloalkyl, cycloalkylalkoxy, haloalkoxy, alkoxyalkoxy, phenyl, halophenyl, haloalkylphenyl, phenylalkyl, halophenylalkyl, phenylhydroxyalkyl, phenyloxyalkyl, phenylalkoxy, alkoxyphenyl, halophenyloxy, piperidinylsulfonyl, tetrahydropyranyl, 3-alkoxy-azetidinyl, tetrahydropyranylalkyl, tetrahydropyranylalkoxy, tetrahydrothiopyranyl 1,1-dioxide, 1,1-dioxo-[1,2]thiazinan-4-yl, piperidin-2-onyl, tetrahydrofuranylalkoxy, pyridinylalkoxy, alkyloxetanylalkoxy, hydroxylhaloalkyloxy, halophenylhydroxyalkyl, alkylsulfonyl, alkylsulfanyl and (halo)(haloalkyl)phenyl; R2 is selected from the group consisting of: hydrogen, halogen, alkyl, haloalkyl, hydroxyalkyl, cycloalkyl, hydroxycycloalkyl, alkoxy, haloalkoxy, alkylamino, haloalkylamino, tetrahydropyranyl, 1H-pyrazolyl, pyrrolidinyl, alkylpyrrolidinyl, halopyrrolidinyl, oxopyrrolidinyl, haloazetidinyl, hydroxyazetidinyl, 1,1-dioxido-2-isothioazolidinyl, tetrahydrofuranyl, cycloalkylamino, hydroxyoxetanyl, alkylsulfonyl, oxetanyl, 6oxa-1-aza-spiro[3.3]heptyl, 3,3-difluoro-2-oxo-azetidinyl, oxo-azetidinyl and oxo-pyrrolidinyl; or R1 and R2 together with the ring to which they are attached form tetrahydroquinolinyl or alkyltetrahydroquinolinyl; one of R3 and R4 is hydrogen and the other one is —(CR5R6)m(CR7R8)n—R9; or R3 and R4 together with the nitrogen atom to which they are attached form piperidinyl, 1,1-dioxidotetrahydro-2H-thiopyranyl, thiomorpholinyl, 2-oxa-6-aza-spiro[3.3]heptyl or 1-hydroxyalkylpyrrolidinyl; R5 and R6 are each independently selected from the group consisting of: hydrogen, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, phenyl, pyridazinyl, halophenyl, pyrimidinyl, alkylsulfanylalkyl and alkylsulfonylalkyl; or R5 and R6 together with the carbon atom to which they are attached form cycloalkyl, tetrahydropyranyl or oxetanyl; R7 and R8 are each independently selected from the group consisting of: hydrogen, alkyl and cycloalkyl; R9 is selected from the group consisting of: alkyl, hydroxyl, cyano, carboxyl, alkoxycarbonyl, alkyl[1,2,4]oxadiazolyl, oxazolyl, thiazolyl, [1,3,4]oxadiazolyl, cycloalkyl, phenyl, pyridinyl, tetrahydropyranyl, alkyl[1,2,4]thiadiazolyl, [1,2,4]thiadiazolyl, alkylaminocarbonyl, alkyltetrahydropyranyl, alkylisoxazolyl, aminocarbonyl, morpholinyl, dihydro-oxazolyl, [1,2,4]oxadiazolyl, hydroxycycloalkyl, alkoxycarbonylcycloalkyl, alkoxyalkoxy, hydroxyalkylcycloalkyl, alkoxypyridinyl, piperidinyl, hydroxypiperidinyl, hydroxyalkylpiperidinyl, isoxazolyl, azetidine-carbonyl, alkoxyalkylaminocarbonyl, cycloalkyl-alkylaminocarbonyl, haloazetidinylcarbonyl, alkyloxopyrrolidinyl, 1,1-dioxo-tetrahydro-1λ6-thiophenyl, 1,1-dioxo-tetrahydro-1λ6-thiophenylamino, amino[1,2,4]oxadiazolyl, 4-alkyl-5-oxo-4,5-dihydro-[1,2,4]oxadiazolyl, nitro-benzo[1,2,5]oxadiazolyl, alkylsulfonyl, alkyl[1,2,4]thiazolyl, hydroxyalkylaminocarbonyl, oxotetrahydrofuranyl, (cycloalkylalkyl)(alkoxycarbonyl)amino, 2-oxo-[1,3]oxazinanyl, haloalkyl and hydroxypyrrolidinylaminocarbonyl; m is 0 or 1; and n is 0, 1 or 2; or a pharmaceutically acceptable salt or ester thereof.
地址 Nutley NJ US