¿ opioid receptor agonist and use thereof
AssigneeChengdu Aoda Biotechnology Co., Ltd
InventorsShuliang ZHOU, Peng WANG, Lan DENG
Life of this patent
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Abstract
A K opioid receptor agonist and a stereoisomer and pharmaceutically acceptable salt thereof, having the following structural formula and relating to the technical field of biological medicines. The K opioid receptor agonist has high selectivity to a k opioid receptor, the activity of the K opioid receptor agonist is 3-15 times that of Difelikefalin, the drug activity is high, and the k opioid receptor agonist can be used for treating and/or relieving pruritus and/or analgesia. D-Phe-AA1-AA2-D-Lys-4-aminopiperidine-4-carboxamide-AA3-AA4-AA5 (Formula I).
Claims10
A κ-opioid receptor agonist as represented by formula I, a stereisomer thereof, and a pharmaceutically acceptable salt thereof:
- wherein, AA1 is modified or unmodified D-Phe, or modified or unmodified D-Tyr;
- AA2 is D-Leu, or D-cyclopropylalanine;
- AA3 is -(PEGm1(CH2)m2CO)m3—, or (AA6)m4, or is absent, wherein:
- m1 is an integer ranging from 1 to 10;
- m2 is an integer ranging from 1 to 5;
- m3 is an integer ranging from 1 to 5;
- m4 is an integer ranging from 1 to 5;
- AA6 is AEEA, or Gly, or D-Ala, or L-Ala, or D-Leu, or L-Leu, or D-Phe, or L-Phe, or D-Ser, or L-Ser, or D-Thr, or L-Thr, or D-Tyr, or L-Tyr, or D-Asp, or L-Asp, or D-Glu, or L-Glu, or D-Gln, or L-Gln, or D-Lys, or L-Lys, or D-Arg, or L-Arg, or D-His, or L-His;
- AA4 is (AA7)n, or is absent, wherein:
- n is an integer ranging from 1 to 10;
- AA7 is D-Lys, or L-Lys, or D-Dap, or L-Dap, or D-Dab, or L-Dab, or D-Orn, or L-Orn, or D-Dah, or L-Dah, or D-Dao, or L-Dao;
- AA5 is OH, or NH2.
Dependencies are inferred from the claim text.