DERIVATIVES OF 2-AZA-BICYCLE [3.1.0] HEXANE AND ITS USE IN THE PREPARATION OF A MEDICINAL PRODUCT FOR THE TREATMENT OF DISEASES RELATED TO GENERAL DYSFUNCTIONS OF THE OREXINE SYSTEM.
Номер патента: AR064561A1
Опубликовано: 08-04-2009
Автор(ы):
Принадлежит: ACTELION PHARMACEUTICALS LTD
Опубликовано: 08-04-2009
Автор(ы):
Принадлежит: ACTELION PHARMACEUTICALS LTD
Реферат: Derivados 2-aza-biciclo[3.1.0]hexano de formula (1). Uso de dichos compuestos, o de sales farmacéuticamente aceptables de dichos compuestos, como medicamentos, especialmente como antagonistas del receptor orexina. Reivindicacion 1: Un compuesto de formula (1) donde A representa arilo o heterociclilo, donde el arilo o heterociclilo es no sustituido o independientemente mono- o di-sustituido, donde los sustituyentes están independientemente seleccionados del grupo que consiste en alquilo C1-4, cicloalquilo C3-6, alquinilo C2-6, alcoxi C1-4, NR2R3, halogeno y fenilo o piridilo no sustituido o independientemente mono- o di-sustituido, donde los sustituyentes están independientemente seleccionados del grupo que consiste en alquilo C1-4, alcoxi C1-4, trifluormetilo, trifluormetoxi, fluor y cloro; B representa un grupo arilo- o heterociclilo, donde el arilo o heterociclilo es no sustituido o independientemente mono-, di-, o tri-sustituido, donde los sustituyentes están independientemente seleccionados del grupo que consiste en alquilo C1-4, alcoxi C1-4, trifluormetilo, -NR2R3, -NHSO2-alquilo C1-4, -N(R2)C(O)R3 y halogeno; n representa el numero entero 0 o 1; R1 representa arilo o heterociclilo, donde el arilo o heterociclilo es no sustituido o independientemente mono-, di-, o tri-sustituido, donde los sustituyentes están seleccionados independientemente del grupo que consiste en alquilo C1-4, alcoxi C1-4, halogeno, trifluormetilo, ciano, alquiltio C1-4, alquinilo C2-6 y -NR2R3; o R1 representa un grupo 2,3-dihidro-benzofuranilo, benzo[1,3]dioxolilo, 2,3-dihidro-benzo[1,4]dioxinilo, 4H-benzo[1,3]dioxinilo, 2H-cromenilo, cromanilo, 2,3-dihidro-tieno[3,4-b][1,4]dioxinilo, un 34-dihidro-2H- benzo[1,4]oxazinilo, o un grupo 4-morfolino-fenilo, donde dichos grupos están no sustituidos o mono- o di-sustituidos, donde los sustituyentes están seleccionados independientemente del grupo que consiste en alquilo C1-4, alcoxi C1-4 y halogeno; R2 representa hidrogeno o alquilo C1-4 y R3 representa hidrogeno o alquilo C1-4 o una sal de dicho compuesto farmacéuticamente aceptable. 2-aza-bicyclo derivatives [3.1.0] hexane of formula (1). Use of said compounds, or pharmaceutically acceptable salts of said compounds, as medicaments, especially as orexin receptor antagonists. Claim 1: A compound of formula (1) wherein A represents aryl or heterocyclyl, wherein the aryl or heterocyclyl is unsubstituted or independently mono- or di-substituted, wherein the substituents are independently selected from the group consisting of C1-4 alkyl, C3-6 cycloalkyl, C2-6 alkynyl, C1-4 alkoxy, NR2R3, halogen and phenyl or pyridyl unsubstituted or independently mono- or di-substituted, wherein the substituents are independently selected from the group consisting of C1-4 alkyl, alkoxy C1-4, trifluoromethyl, trifluoromethoxy, fluorine and chlorine; B represents an aryl- or heterocyclyl group, where the aryl or heterocyclyl is unsubstituted or independently mono-, di-, or tri-substituted, where the substituents are independently selected from the group consisting of C1-4 alkyl, C1-4 alkoxy , trifluoromethyl, -NR2R3, -NHSO2-C1-4 alkyl, -N (R2) C (O) R3 and halogen; n represents the integer 0 or 1; R1 represents aryl or heterocyclyl, where the aryl or heterocyclyl is unsubstituted or independently mono-, di-, or tri-substituted, where the substituents are independently selected from the group consisting of C1-4 alkyl, C1-4 alkoxy, halogen, trifluoromethyl, cyano, C1-4 alkylthio, C2-6 alkynyl and -NR2R3; or R1 represents a 2,3-dihydro-benzofuranyl, benzo [1,3] dioxolyl, 2,3-dihydro-benzo [1,4] dioxinyl, 4H-benzo [1,3] dioxinyl, 2H-chromenyl, chromanyl group , 2,3-dihydro-thieno [3,4-b] [1,4] dioxinyl, a 34-dihydro-2H-benzo [1,4] oxazinyl, or a 4-morpholino-phenyl group, wherein said groups are unsubstituted or mono- or di-substituted, wherein the substituents are independently selected from the group consisting of C1-4 alkyl, C1-4 alkoxy and halogen; R 2 represents hydrogen or C 1-4 alkyl and R 3 represents hydrogen or C 1-4 alkyl or a pharmaceutically acceptable salt of said compound.
2-aza-bicyclo[3,1,0]hexane derivatives as orexin receptor antagonists
Номер патента: RU2460732C2. Автор: Хамед АЙССОЮИ,Кристоф БОСС,Маркус ГУДЕ,Ральф КОБЕРШТАЙН,Тьерри ЗИФФЕРЛЕН,Даниель ТРАКСЕЛЬ. Владелец: Актелион Фармасьютиклз Лтд. Дата публикации: 2012-09-10.