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    • 3. 发明授权
    • Melanocortin 1 receptor selective compounds
    • 黑皮质素1受体选择性化合物
    • US07008925B1
    • 2006-03-07
    • US09674733
    • 1999-05-05
    • Michael SzardeningsRuta MucenieceIlze MutuleFelikss MutulisJarl Wikberg
    • Michael SzardeningsRuta MucenieceIlze MutuleFelikss MutulisJarl Wikberg
    • A61K38/00
    • C07K14/685A61K38/00
    • A compound of general formula (1) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are H or methyl, R13, R14, R15 and R16 are H or alkyl, wherein L1 and L2 are linkers selected from single bond, methyl, ethyl, wherein R19, R20 and R21 are H or —CH2X, NT is selected from H, hydroxyl, alkyl, aminoacid, aminoacid analogue, polypeptide and functional group, CT is selected from hydrogen, hydroxyl, alkyl, aminoacid, aminoacid analogue, polypeptide and functional group shows high selectivity and high affinity for MC1-receptors in combination with effective stimulation or inhibiton of cAMP formation in MC1-receptor expressing cells but low affinity for other subtypes of MC-receptors and may be used to treat a wide range of inflammatory conditions. Also disclosed is a DNA molecule and a corresponding vector encoding the compound, a fusion protein comprising a copy of it, a vector comprising DNA encoding the fusion protein, and a pharmaceutical composition comprising the compound.
    • 通式(1)的化合物,其中R 1,R 2,R 3,R 4,R 5,R 6,R 7,R 8,R 9,R 10,R 11和R 12为H或甲基,R 13,R 14,R 15和R 16为H或烷基, L1和L2是选自单键,甲基,乙基的连接体,其中R 19,R 20和R 21是H或-CH 2 X,NT选自H,羟基,烷基,氨基酸,氨基酸类似物, 多肽和官能团,CT选自氢,羟基,烷基,氨基酸,氨基酸类似物,多肽和官能团对MC1受体具有高选择性和高亲和力,并与MC1受体表达细胞中有效刺激或抑制cAMP形成相结合 但对MC-受体的其它亚型的亲和力低,可用于治疗广泛的炎性病症。 还公开了编码该化合物的DNA分子和相应的载体,包含其拷贝的融合蛋白,包含编码融合蛋白的DNA的载体和包含该化合物的药物组合物。