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    • 1. 发明申请
    • N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands
    • N-苯基吡咯胍衍生物作为黑皮质素受体配体
    • US20090018183A1
    • 2009-01-15
    • US12232399
    • 2008-09-17
    • Torbjorn LundstedtAnna SkottnerArne BomanPer AnderssonElisabeth SeifertVictor Andrianov
    • Torbjorn LundstedtAnna SkottnerArne BomanPer AnderssonElisabeth SeifertVictor Andrianov
    • A61K31/40A61P3/00A61P25/00
    • C07D207/335C07D207/34C07D207/36C07D207/38C07D207/42
    • The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.
    • 本发明提供了作为黑皮质素受体配体和/或用于治疗黑皮质素系统中的病症的通式(I)的新化合物:其中X是(CH 2)n,其中n是0,1或2; R 1,R 2,R 3,R 4和R 5可以相同或不同,并且选自氢,卤素,具有1-5个碳原子的烷基,具有1至5个碳原子的烷氧基,羟基,烷基磺酰氧基,氰基,硝基,三卤代烷基,磺基 或方案1中给出的结构之一; 或者R 1,R 2,R 3,R 4和R 5中的两个可以一起形成亚甲二氧基或亚乙二氧基部分; R 6,R 7,R 8和R 9相同或不同,并且选自氢,卤素,具有1至5个碳原子的烷基,具有1至5个碳原子的烷氧基,羟基,具有0,1 或2个碳原子,氰基,硝基,三卤代烷基,酰胺或磺基,z表示残基与苯基或吡咯环的连接点; 及其药理学活性盐。
    • 3. 发明授权
    • N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands
    • N-苯基吡咯胍衍生物作为黑皮质素受体配体
    • US07186748B2
    • 2007-03-06
    • US10484444
    • 2002-08-06
    • Torbjörn LundstedtAnna SkottnerArne BomanPer AnderssonElisabeth SeifertVictor Andrianov
    • Torbjörn LundstedtAnna SkottnerArne BomanPer AnderssonElisabeth SeifertVictor Andrianov
    • A61K31/402C07D207/335
    • C07D207/335C07D207/34C07D207/36C07D207/38C07D207/42
    • The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.
    • 本发明提供了作为黑皮质素受体的配体和/或用于治疗黑皮质素系统中的病症的通式(I)的新化合物:其中X是(CH 2) / SUB>其中n为0,1或2; R 1,R 2,R 3,R 4和R 5可以是 羟基,烷基磺酰氧基,氰基,硝基,三卤代烷基,磺基或方案1中给出的结构之一;其中R 1,R 2, 或R 1,R 2,R 3,R 4和R 5中的两个, 可以一起形成亚甲二氧基或亚乙二氧基部分; R 6,R 7,R 8和R 9相同或不同,并且选自氢, 卤素,具有1至5个碳原子的烷基,具有1至5个碳原子的烷氧基,羟基,具有0,1或2个碳原子的胺(伯,仲或叔),氰基,硝基,三卤代烷基,酰胺或磺基,和z 显示残基与苯基或吡咯环的连接点; 及其药理学活性盐。
    • 4. 发明授权
    • N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands
    • N-苯基吡咯胍衍生物作为黑皮质素受体配体
    • US07442807B2
    • 2008-10-28
    • US11374956
    • 2006-03-15
    • Torbjörn LundstedtAnna SkottnerArne BomanPer AnderssonElisabeth SeifertVictor Andrianov
    • Torbjörn LundstedtAnna SkottnerArne BomanPer AnderssonElisabeth SeifertVictor Andrianov
    • C07D207/325C07D207/335C07D413/10
    • C07D207/335C07D207/34C07D207/36C07D207/38C07D207/42
    • The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.
    • 本发明提供了作为黑皮质素受体的配体和/或用于治疗黑皮质素系统中的病症的通式(I)的新化合物:其中X是(CH 2) / SUB>其中n为0,1或2; R 1,R 2,R 3,R 4和R 5可以是 羟基,烷基磺酰氧基,氰基,硝基,三卤代烷基,磺基或方案1中给出的结构之一;其中R 1,R 2, 或R 1,R 2,R 3,R 4和R 5中的两个, 可以一起形成亚甲二氧基或亚乙二氧基部分; R 6,R 7,R 8和R 9相同或不同,并且选自氢, 卤素,具有1至5个碳原子的烷基,具有1至5个碳原子的烷氧基,羟基,具有0,1或2个碳原子的胺(伯,仲或叔),氰基,硝基,三卤代烷基,酰胺或磺基,和z 显示残基与苯基或吡咯环的连接点; 及其药理学活性盐。