BIPHENYL DERIVATIVES AS AGONISTS OF ß2-ADRENERGIC RECEPTORS AND AS ANTAGONISTS OF MUSCARINAL RECEPTORS
Номер патента: PE20040950A1
Опубликовано: 01-01-2005
Автор(ы): Adam Hughes, Craig Husfeld, Eric Stangeland, Mathai Mammen, Sarah Dunham, Tae Weon Lee, Yan Chen
Принадлежит: Theravance Inc
Опубликовано: 01-01-2005
Автор(ы): Adam Hughes, Craig Husfeld, Eric Stangeland, Mathai Mammen, Sarah Dunham, Tae Weon Lee, Yan Chen
Принадлежит: Theravance Inc
Реферат: SE REFIERE A DERIVADOS DE BIFENILO DE FORMULA I DONDE a Y b SON 0-3; c ES 0-4; R1 ES ALQUILO C1-C4, ALQUENILO C2-C4, ALQUINILO C2-C4, ENTRE OTROS; R2 ES ALQUILO C1-C4, ALQUENILO C2-C4, ENTRE OTROS; W ESTA UNIDO EN LA POSICION 3 o 4 CON RESPECTO AL N EN EL ANILLO DE PIPERIDINA Y ES 0 o Nwa; Wa ES H o ALQUILO C1-C4; R3 ES ALQUILO C1-C4, ALQUENILO C2-C4, ALQUINILO C2-C4, ENTRE OTROS; R4 ES UN GRUPO DIVALENTE DE FORMULA (R4a)d-(A1)e-(R4b)g-(A2)h-(R4d)i, EN DONDE d, e, f, g, h e i 0 o 1; R4a, R4b, R4c Y R4d SON ALQUILENO C1-C10, ALQUENILENO C2-C10 o ALQUINILENO C2-C10, ENTRE OTROS; A1 Y A2 SON CICLOALQUILENO C3-C7, ARILENO C6-C10, O-ARILEN C6-C10, ENTRE OTROS; Q ES UN ENLACE, C(O)O, OC(O), S, ENTRE OTROS; R5 ES H o ALQUILO C1-C4; R6 ES NR6aCR6b(O) o CR6cR6dOR6e; R7 ES H; o R6 y R7 FORMAN JUNTOS NR7aC(O)-CR7b=CR7c; CR7d=CR7e-C(O)-NR7f, ENTRE OTROS; R6a, R6b, R6c, R6d, R6e, R7a, R7b, R7c, R7d, R7e Y R7f SON H o ALQUILO C1-C4. SON COMPUESTOS PREFERIDOS: 1-BIFENIL-2-IL-3-(1-{9-[2-HIDROXI-2-(8-HIDROXI-2-OXO-1,2-DIHIDROQUINOLIN-5-IL)ETILAMINO]NONIL}PIPERIDIN-4-IL)UREA; DITRIFLUOROACETATO DE 1-{9-[2-HIDROXI-2-(8-HIDROXI-2-OXO-1,2-DIHIDROQUINOLIN-5-IL)ETILAMINO]NONIL} PIPERIDIN-4-IL ESTER DE ACIDO BIFENIL-2-ILCARBAMICO; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCESO DE PREPARACION Y COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON AGONISTAS DE LOS RECEPTORES ADRENERGICOS b2 Y ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS Y SON UTILES PARA TRATAR TRASTORNOS PULMONARES REFERS TO BIPHENYL DERIVATIVES OF FORMULA I WHERE a AND b ARE 0-3; c ES 0-4; R1 is C1-C4 ALKYL, C2-C4 ALKENYL, C2-C4 ALKYL, AMONG OTHERS; R2 IS C1-C4 ALKYL, C2-C4 ALKYL, AMONG OTHERS; W IS JOINTED IN THE 3 or 4 POSITION WITH RESPECT TO N IN THE PIPERIDINE RING AND IS 0 or Nwa; Wa IS H or C1-C4 ALKYL; R3 IS C1-C4 ALKYL, C2-C4 ALKYL, C2-C4 ALKYL, AMONG OTHERS; R4 IS A DIVALENT GROUP OF FORMULA (R4a) d- (A1) e- (R4b) g- (A2) h- (R4d) i, WHERE d, e, f, g, h and i 0 or 1; R4a, R4b, R4c AND R4d ARE C1-C10 ALKYLENE, C2-C10 ALKYLENE or C2-C10 ALKYLENE, AMONG OTHERS; A1 AND A2 ARE C3-C7 CYCLOALKYLENE, C6-C10 ARYLENE, C6-C10 O-ARILENE, AMONG OTHERS; Q IS A LINK, C (O) O, OC (O), S, AMONG OTHERS; R5 IS H or C1-C4 ALKYL; R6 IS NR6aCR6b (O) or CR6cR6dOR6e; R7 IS H; or R6 and R7 TOGETHER FORM NR7aC (O) -CR7b = CR7c; CR7d = CR7e-C (O) -NR7f, AMONG OTHERS; R6a, R6b, R6c, R6d, R6e, R7a, R7b, R7c, R7d, R7e AND R7f ARE H or C1-C4 ALKYL. PREFERRED COMPOUNDS ARE: 1-BIPHENYL-2-IL-3- (1- {9- [2-HYDROXY-2- (8-HYDROXY-2-OXO-1,2-DIHYDROQUINOLIN-5-IL) ETHYLAMINE] NONYL} PIPERIDIN-4-IL) UREA; 1- {9- [2-HYDROXY-2- (8-HYDROXY-2-OXO-1,2-DIHYDROQUINOLIN-5-IL) ETHYLAMINE] NONYL} PIPERIDIN-4-IL ESTER OF BIPHENYL-2-ILCARBAMIC ACID ESTER ; AMONG OTHERS. ALSO REFERS TO A PHARMACEUTICAL PREPARATION AND COMPOSITION PROCESS. THESE COMPOUNDS ARE AGONISTS OF ADRENERGIC b2 RECEPTORS AND ANTAGONISTS OF MUSCARINAL RECEPTORS AND ARE USEFUL TO TREAT PULMONARY DISORDERS
Biphenyl derivatives
Номер патента: US7521561B2. Автор: Yan Chen,Mathai Mammen,Adam Hughes. Владелец: Theravance Inc. Дата публикации: 2009-04-21.