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    • 3. 发明申请
    • PYRROLOPYRIDINEDERIVATIVES AS MODULATORS OF THE CANNABINOID RECEPTOR FOR THE TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS
    • 作为用于治疗免疫和炎症疾病的CANNABINOID受体的调节剂的吡咯烷酮
    • WO2007017264A3
    • 2007-04-12
    • PCT/EP2006007875
    • 2006-08-07
    • GLAXO GROUP LTDEATHERTON ANDREW JOHNGIBLIN GERARD MARTIN PAULJANDU KARAMJIT SINGHJOHNSON MATTHEW RUSSELLMITCHELL WILLIAM LEONARDNAYLOR ALANSWEETING JENNIFER ANNE
    • EATHERTON ANDREW JOHNGIBLIN GERARD MARTIN PAULJANDU KARAMJIT SINGHJOHNSON MATTHEW RUSSELLMITCHELL WILLIAM LEONARDNAYLOR ALANSWEETING JENNIFER ANNE
    • C07D471/04A61K31/437A61P19/02A61P29/00A61P37/02
    • C07D471/04
    • The present invention relates to novel pyrrolopyridine derivatives of formula (I), pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease-in activity of the cannabinoid receptor, wherein: X 1 is NH and X 2 and X 3 together form a -CR 13 =CR 11 -group or X 3 is NR 12 and X 2 and X 1 together form a -CR 13 =CR 11 - group; X 4 is O, SO 2 , S, or a bond, or X 4 is -NHCO or -NHCH 2 such that R 6 X 4 is R 6 CONH or R 6 CH 2 NH; R 1 is selected from hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl and halosubstituted C 1-6 alkyl; R 2 is hydrogen or (CH 2 )mR 3 where m is 0 or 1; or R 1 and R 2 together with N to which they are attached form an optionally substituted 4- to 8- membered non-aromatic heterocyclyl ring; R 3 is a 4- to8- membered non-aromatic heterocyclyl group, a C 3-8 cycloalkyl group, a straight or branched C 1-10 alkyl, a C 2-10 alkenyl, a C 3-8 cycloalkenyl, a C 2-10 alkynyl, a C 3-8 cycloalkynyl or phenyl group, any of which can be unsubstituted or substituted, or R 5 ; wherein p is 0, 1 or 2, and X is CH 2 . O, S, or SO 2 ; R 6 is phenyl, C 3-6 cycloalkyl, a straight or branched C 1-6 alkyl group, -CH 2 -C 3-6 cycloalkyl, -CH 2 -phenyl, 4- to 8- membered non-aromatic heterocyclyl group, or a bicyclic group any of which can be unsubstituted or substituted, however when X 4 is a bond R 6 is substituted phenyl; R 7 is OH, C 1-6 alkoxy, NR 8a R 8b , NHCOR 9 , NHSO 2 R 9 or SOqR 9 ; R 8a is H or C 1-6 alkyl; R 8b is Hor C 1-6 alkyl; R 9 is C 1-6 alkyl; R 10 is hydrogen, substituted or unsubstituted (C 1-6 )alkyl or chloro; R 11 is hydrogen or C 1-6 alkyl; R 12 is hydrogen or C 1-6 alkyl; R 13 is hydrogen or C 1-6 alkyl; q is 0, 1 or 2.
    • 本发明涉及式(I)的新型吡咯并吡啶衍生物,含有这些化合物的药物组合物及其在治疗疾病尤其是疼痛中的用途,所述疾病是由大麻素受体直接或间接引起的活性增加或减少引起的 ,其中:X 1是NH且X 2和X 3一起形成-CR 13 = CR 3, SUP> 11 - 组或X 3是NR 12和X 2和X 1一起 形成一个-CR = CR 11 - 组; X 4是O,SO 2,S或键,或X 4是-NHCO或-NHCH 2, SUB>使得R 6 X 4是R 6 CONH或R 6 CH 2, SUB> NH; R 1选自氢,C 1-6烷基,C 3-6环烷基和卤素取代的C 1-6烷基, SUB>烷基; R 2是氢或(CH 2 CH 2)m R 3,其中m是0或1; 或R 1和R 2与它们所连接的N一起形成任选取代的4-至8-元非芳族杂环基环; R 3是4-至8-元非芳族杂环基,C 3-8环烷基,直链或支链C 1-10烷基, 亚烷基,C 2-10链烯基,C 3-8环烯基,C 2-10炔基,C 3-8环炔基或苯基,其中任何一个可以是未取代的或取代的,或R 5; 其中p是0,1或2,X是CH 2。 O,S或SO 2; R 6是苯基,C 3-6环烷基,直链或支链C 1-6 - 烷基,-CH 2, C 3-6环烷基,-CH 2 - 苯基,4-至8-元非芳族杂环基,或双环基,任何一个可以 未取代或取代的,但是当X 4为键时,R 6为取代的苯基; R 7是OH,C 1-6烷氧基,NR 8a R 8b,NHCOR 9, / SO 2,NHSO 2 R 9或SO 3 R 9; R 8a是H或C 1-6烷基; R 8b是Hor C 1-6烷基; R 9是C 1-6烷基; R 10是氢,取代或未取代的(C 1-6 - )烷基或氯; R 11是氢或C 1-6烷基; R 12是氢或C 1-6烷基; R 13是氢或C 1-6烷基; q是0,1或2。