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    • 37. 发明授权
    • Substituted oxadiazole compounds and their use as opioid receptor ligands
    • 取代的恶二唑化合物及其作为阿片受体配体的用途
    • US07589113B2
    • 2009-09-15
    • US12143550
    • 2008-06-20
    • Beatrix MerlaStefan OberboerschBernd SundermannWerner EnglbergerHagen-Heinrich HenniesHeinz Graubaum
    • Beatrix MerlaStefan OberboerschBernd SundermannWerner EnglbergerHagen-Heinrich HenniesHeinz Graubaum
    • A61K31/4245A61P25/00C07D271/06C07D417/02
    • C07D271/06C07D413/04C07D413/06C07D413/08C07D413/14
    • Substituted oxadiazole compounds corresponding to formula I: in which X denotes CH, CH2, CH═CH, CH2CH2, CH2CH═CH or CH2CH2CH2; R1 denotes aryl or heteroaryl, in each case unsubstituted or mono- or polysubstituted; or a C1-3 alkyl group-linked aryl or heteroaryl group, in each case unsubstituted or mono- or polysubstituted; R2 denotes aryl or heteroaryl, in each case unsubstituted or mono- or polysubstituted; a C1-3 alkyl chain-attached aryl group, in each case unsubstituted or mono- or polysubstituted; and R3 and R4 independently denote H; C1-6 alkyl, in each case saturated or unsaturated, branched or unbranched, wherein R3 and R4 do not simultaneously mean H; or R3 and R4 together denote CH2CH2OCH2CH2, or (CH2)3-6. The compounds have an affinity for the μ-opioid receptor and may take the form of the racemate; enantiomers, diastereomers, mixtures of enantiomers or diastereomers, an individual enantiomer or diastereomer, a free base, or a salt with a physiologically acceptable acid.
    • 对应于式I的取代的恶二唑化合物:其中X表示CH,CH 2,CH-CH,CH 2 CH 2,CH 2 CH-CH或CH 2 CH 2 CH 2; R 1表示芳基或杂芳基,在每种情况下是未取代的或单取代或多取代的; 或者C 1-3烷基连接的芳基或杂芳基,在各种情况下是未取代的或单取代或多取代的; R 2表示芳基或杂芳基,在各种情况下为未取代或单取代或多取代; 在各种情况下为未取代或单取代或多取代的C 1-3烷基链连接的芳基; R3和R4独立地表示H; C 1-6烷基,各自为饱和或不饱和的,支链或非支链的,其中R3和R4不同时表示H; 或者R 3和R 4一起表示CH 2 CH 2 OCH 2 CH 2或(CH 2)3-6。 这些化合物对μ-阿片受体具有亲和力,并且可以采取外消旋体的形式; 对映体,非对映异构体,对映异构体或非对映异构体的混合物,单独的对映异构体或非对映体,游离碱或与生理上可接受的酸的盐。
    • 39. 发明申请
    • SUBSTITUTED OXADIAZOLE COMPOUNDS AND THEIR USE AS OPIOID RECEPTOR LIGANDS
    • 取代的奥沙利多化合物及其作为阿片受体配体的用途
    • US20090005427A1
    • 2009-01-01
    • US12143550
    • 2008-06-20
    • Beatrix MERLAStefan OberboerschBernd SundermannWerner EnglbergerHagen-Heinrich HenniesHeinz Graubaum
    • Beatrix MERLAStefan OberboerschBernd SundermannWerner EnglbergerHagen-Heinrich HenniesHeinz Graubaum
    • A61K31/4245A61P25/00C07D271/06C07D417/02
    • C07D271/06C07D413/04C07D413/06C07D413/08C07D413/14
    • Substituted oxadiazole compounds corresponding to formula I: in which X denotes CH, CH2, CH═CH, CH2CH2, CH2CH═CH or CH2CH2CH2; R1 denotes aryl or heteroaryl, in each case unsubstituted or mono- or polysubstituted; or a C1-3 alkyl group-linked aryl or heteroaryl group, in each case unsubstituted or mono- or polysubstituted; R2 denotes aryl or heteroaryl, in each case unsubstituted or mono- or polysubstituted; a C1-3 alkyl chain-attached aryl group, in each case unsubstituted or mono- or polysubstituted; and R3 and R4 independently denote H; C1-6 alkyl, in each case saturated or unsaturated, branched or unbranched, wherein R3 and R4 do not simultaneously mean H; or R3 and R4 together denote CH2CH2OCH2CH2, or (CH2)3-6. The compounds have an affinity for the μ-opioid receptor and may take the form of the racemate; enantiomers, diastereomers, mixtures of enantiomers or diastereomers, an individual enantiomer or diastereomer, a free base, or a salt with a physiologically acceptable acid.
    • 对应于式I的取代的恶二唑化合物:其中X表示CH,CH 2,CH-CH,CH 2 CH 2,CH 2 CH-CH或CH 2 CH 2 CH 2; R 1表示芳基或杂芳基,在每种情况下是未取代的或单取代或多取代的; 或者C 1-3烷基连接的芳基或杂芳基,在各种情况下是未取代的或单取代或多取代的; R 2表示芳基或杂芳基,在各种情况下为未取代或单取代或多取代; 在各种情况下为未取代或单取代或多取代的C 1-3烷基链连接的芳基; R3和R4独立地表示H; C 1-6烷基,各自为饱和或不饱和的,支链或非支链的,其中R3和R4不同时表示H; 或者R 3和R 4一起表示CH 2 CH 2 OCH 2 CH 2或(CH 2)3-6。 这些化合物对μ-阿片受体具有亲和力,并且可以采取外消旋体的形式; 对映体,非对映异构体,对映异构体或非对映异构体的混合物,单独的对映异构体或非对映体,游离碱或与生理上可接受的酸的盐。