发明名称 3-aryl-3-hydroxy-2-amino-propionic acid amides, 3-heteroaryl-3-hydroxy-2-aminopropionic acid amides and related compounds having analgesic and/or immuno stimulant activity
摘要 Compounds of Formulas 1 and 2;where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.
申请公布号 US8927589(B2) 申请公布日期 2015.01.06
申请号 US201313834336 申请日期 2013.03.15
申请人 Allergan, Inc. 发明人 Leblond Bertrand;Beausoleil Eric;Taverne Thierry;Donello John E.
分类号 A61K31/40;A61K31/535;C07D409/06;C07D413/06;C07D265/30;A61K31/4025;A61K31/5375;C07D213/64;C07D295/12;C07D319/18;A61K31/4409;A61K31/4439;A61K31/4545;A61K31/4709;A61K31/496;A61K31/5377;A61K31/541 主分类号 A61K31/40
代理机构 代理人 Bass Jonathan Y.
主权项 1. A method for treating chronic pain in a mammal, comprising administering to said mammal at least one compound of the formula: or a pharmaceutically acceptable salt thereof, wherein: R1 is H or alkyl of 1 to 6 carbons;R2 is selected from the group consisting of H, and alkyl of 1 to 6 carbons; or the R1 and R2 groups together with the nitrogen atom to which they are shown attached form a saturated or unsaturated 4, 5, 6 or 7 membered ring that optionally additionally includes one or two heteroatoms independently selected from the group consisting of N, O and S, said 4, 5, 6 or 7 membered ring optionally being substituted with one or two COOH, CH2OH, OH, B(OH)2, halogen groups, cyano groups or with one or two alkyl groups having 1 to 6 carbons;R3 is H, CO—R7 or CO—O—R7 where R7 is H, alkyl of 1 to 20 carbons, cycloalkyl of 3 to 6 carbons, aryl or heteroaryl, aryl-alkyl, aryl(hydroxy)alkyl, heteroaryl-alkyl or heteroalkyl(hydroxy)alkyl where the alkyl moiety has 1 to 4 carbons, said aryl or heteroaryl groups being optionally substituted with 1 to 3 groups independently selected from the group consisting of halogen, alkyl of 1 to 6 carbons, alkoxy of 1 to 6 carbons and thioxy of 1 to 3 carbons;R4 is H, alkyl of 1 to 6 carbons, or CO—R8 where R8 is alkyl of 1 to 6 carbons;R5 and R6 are independently selected from the group consisting of H, halogen, alkyl of 1 to 6 carbons, alkoxy of 1 to 6 carbons and thioxy of 1 to 3 carbons; orR5 and R6 together with the atoms to which they are attached jointly form a carbocyclic or a heterocyclic ring, the carbocyclic ring having 5 or 6 atoms in the ring, the heterocyclic ring having 5 or 6 atoms in the ring and 1 to 3 heteroatoms independently selected from N, O and S;said carbocyclic or heterocyclic ring jointly formed by R5 and R6 being optionally substituted with 1 to 6 R9 groups where R9 is independently selected from halogen, alkyl of 1 to 6 carbons, alkoxy of 1 to 6 carbons, andthe wavy lines represent bonds of the alpha or beta configurationwith the proviso that the formula excludes the compound of the formula below:
地址 Irvine CA US