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    • 1. 发明申请
    • NOVEL AMINOGUANIDINES AS MELANOCORTIN RECEPTOR LIGANDS.
    • 新的氨基葡萄糖作为MELANOCORTIN受体配体。
    • WO2008071980A1
    • 2008-06-19
    • PCT/GB2007/004793
    • 2007-12-13
    • ACURE PHARMA ABPETT, Christopher, PhineasLUNDSTEDT, TorbjörnSEIFERT, ElisabethLEK, PerBOMAN, Arne
    • LUNDSTEDT, TorbjörnSEIFERT, ElisabethLEK, PerBOMAN, Arne
    • C07C281/18C07D339/08A61K31/155A61K31/385A61P29/00
    • C07D339/08C07C281/18C07C323/48
    • There are described compounds of general formula (I) and isomeric forms thereof wherein n is 0,1,2 or 3, saturated or unsaturated; most preferably at least one of R 1 to R 5 represents halogen; at least one of R 1 , R 2 , R 3 , R 4 and R 5 is selected from -S-R or -COOR, or two or more Of R 1 -R 5 comprise a linking group such as -S-(CH2) m S-, where m is 1, 2 or 3 and R is selected from alkyl having 1 to 5 carbon atoms, cycloalkyl having 3-6 carbon atoms, hydroxy, and aryl having 6 to 10 carbon atoms, such groups being optionally substituted, and when R 1 is selected from -S-R, then at least one of R 2 , R 3 and R 5 is most preferably selected from halogen; and R 1 , R 2 , R 3 , R 4 and R 5 are otherwise the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and pharmacologically acceptable salts thereof. Compounds described have activity on the melanocortin receptors and have application in the treatment of a wide range of inflammatory, arthritic or central nerve regeneration conditions.
    • 描述了通式(I)的化合物及其异构体形式,其中n为0,1,2或3,饱和或不饱和; 最优选R 1至R 5中的至少一个表示卤素; R 1,R 2,R 3,R 4和R 5中的至少一个, / SUB>选自-SR或-COOR,或者R 1 -R 5中的两个或更多个包含连接基团,例如-S-(CH 2) 5 <>最优选选自卤素; 和R 1,R 2,R 3,R 4和R 5, 选自氢,卤素,具有1-5个碳原子的烷基,电子给体基团如具有1-5个碳原子的烷氧基或羟基,选自氰基,硝基,三氟烷基或酰胺的电子受体基团; 烷基氨基,苯甲酰氧基,硝酰基,苯基或磺基; 及其药理学上可接受的盐。 所描述的化合物对黑皮质素受体具有活性,并且可用于治疗广泛的炎性,关节炎或中枢神经再生条件。
    • 5. 发明公开
    • NOVEL AMINOGUANIDINES AS MELANOCORTIN RECEPTOR LIGANDS.
    • 新型氨基胍作为黑色素受体配体。
    • EP2121585A1
    • 2009-11-25
    • EP07848535.6
    • 2007-12-13
    • Acure Pharma AB
    • LUNDSTEDT, TorbjörnSEIFERT, ElisabethLEK, PerBOMAN, Arne
    • C07C281/18C07D339/08A61K31/155A61K31/385A61P29/00
    • C07D339/08C07C281/18C07C323/48
    • There are described compounds of general formula (I) and isomeric forms thereof wherein n is 0, 1, 2 or 3, saturated or unsaturated; most preferably at least one of R1 to R5 represents halogen; at least one of R1, R2, R3, R4 and R5 is selected from —S—R or —COOR, or two or more Of R1-R5 comprise a linking group such as —S—(CH2)mS—, where m is 1, 2 or 3 and R is selected from alkyl having 1 to 5 carbon atoms, cycloalkyl having 3-6 carbon atoms, hydroxy, and aryl having 6 to 10 carbon atoms, such groups being optionally substituted, and when R1 is selected from —S—R, then at least one of R2, R3 and R5 is most preferably selected from halogen; and R1, R2, R3, R4 and R5 are otherwise the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and pharmacologically acceptable salts thereof. Compounds described have activity on the melanocortin receptors and have application in the treatment of a wide range of inflammatory, arthritic or central nerve regeneration conditions.
    • 描述了通式(I)的化合物及其异构体形式,其中n是0,1,2或3,饱和或不饱和的; 最优选R1至R5中的至少一个表示卤素; R 1,R 2,R 3,R 4和R 5中的至少一个选自-S-,R或-COOR,或者两个或更多个R 1 -R 5包含连接基团,例如-S-(CH 2)m -S m- 其中m为1,2或3,R选自具有1-5个碳原子的烷基,具有3-6个碳原子的环烷基,羟基和具有6-10个碳原子的芳基,这些基团任选被取代,并且当R1是 选自-S-,R,则R 2,R 3和R 5中的至少一个最优选选自卤素; 并且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,电子给体基团如具有1-5个碳原子的烷氧基或羟基,电子受体基团 选自氰基,硝基,三氟烷基或酰胺; 烷基氨基,苯甲酰氧基,硝酰基,苯基或磺基; 及其药理学上可接受的盐。 所述化合物对黑皮质素受体具有活性,并可用于治疗各种炎症,关节炎或中枢神经再生病症。