Amino mercaptan compound and preparation method therefor and use thereof in protection against radiation
AssigneeShanghai Kechow Pharma, Inc.
InventorsHongqi Tian, Ying Cheng, Qianru Zhang, Zhimei Zhu, Yueying Wang
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Abstract
The present invention discloses an amino mercaptan compound, preparation method thereof and use thereof in radiation protection. The compound has the structure of formula I, wherein A1, A2, R1, R2, R5, R6, and R3 and R4 are defined herein. The compound has the effects of reducing the biological damage caused by ionizing radiation, extending the survival period and survival rate of the radiated animals, and significantly alleviating the side effects of radiotherapy, and has a low toxicity. The present invention opens up a new way for protection and treatment of ionizing radiation damage.
Claims11
A compound of formula (I):
- wherein
- A1 is selected from:
- —C(O)NR8—, —S(O)2—NR8—, —S(O)NR8—, and —R7—NR8—;
- A2 is selected from:
- carbonyl, sulfonyl, sulfinyl, substituted or unsubstituted C1-6 alkyl;
- R1 is selected from:
- hydrogen, substituted or unsubstituted C1-C5 alkyl or substituted or unsubstituted heteroalkyl;
- R2 is selected from substituted or unsubstituted C1-C5 alkyl or substituted or unsubstituted heteroalkyl;
- R5 is selected from hydrogen, substituted or unsubstituted C1-C5 alkyl or substituted or unsubstituted heteroalkyl;
- R6 is selected from substituted or unsubstituted C1-C5 alkyl or substituted or unsubstituted heteroalkyl;
- n is an integer from 1 to 20,000;
- R3 and R4 are independently selected from:
- hydrogen, X, substituted or unsubstituted C1-6 alkyl;
- X is selected from:
- F, Cl, Br and I;
- and
- R7 is selected from:
- substituted or unsubstituted C1-C6 alkyl;
- R8 is selected from:
- hydrogen, substituted or unsubstituted C1-C6 alkyl;
- or a stereoisomer thereof or a pharmaceutically acceptable salt, a prodrug or a solvate thereof.
A pharmaceutical composition comprising a compound of formula (I):
- wherein
- A1 is selected from:
- —C(O)NR8—, —S(O)2—NR8—, —S(O)NR8—, and —R7—NR8—;
- A2 is selected from:
- carbonyl, sulfonyl, sulfinyl, substituted or unsubstituted C1-6 alkyl;
- R1 is selected from:
- hydrogen, substituted or unsubstituted C1-C5 alkyl or substituted or unsubstituted heteroalkyl;
- R2 is selected from substituted or unsubstituted C1-C5 alkyl or substituted or unsubstituted heteroalkyl;
- R5 is selected from hydrogen, substituted or unsubstituted C1-C5 alkyl or substituted or unsubstituted heteroalkyl;
- R6 is selected from substituted or unsubstituted C1-C5 alkyl or substituted or unsubstituted heteroalkyl;
- n is an integer from 1 to 20,000;
- R3 and R4 are independently selected from:
- hydrogen, X, substituted or unsubstituted C1-6 alkyl;
- X is selected from:
- F, Cl, Br and I;
- and
- R7 is selected from:
- substituted or unsubstituted C1-C6 alkyl;
- R8 is selected from:
- hydrogen, substituted or unsubstituted C1-C6 alkyl;
- or a stereoisomer thereof or a pharmaceutically acceptable salt, a prodrug or a solvate thereof, and
- one or more pharmaceutically acceptable vehicles, carriers, adjuvants, auxiliaries or diluents.
A method for the treatment and/or prevention of radiation damage or chemotherapy damage or a tumor, comprising:
- administrating to a subject in need thereof
- a compound of formula (I):
- wherein
- A1 is selected from:
- —C(O)NR8—, —S(O)2—NR8—, —S(O)NR8—, and —R7—NR8—;
- A2 is selected from:
- carbonyl, sulfonyl, sulfinyl, substituted or unsubstituted C1-6 alkyl;
- R1 is selected from:
- hydrogen, substituted or unsubstituted C1-C5 alkyl or substituted or unsubstituted heteroalkyl;
- R2 is selected from substituted or unsubstituted C1-C5 alkyl or substituted or unsubstituted heteroalkyl;
- R5 is selected from hydrogen, substituted or unsubstituted C1-C5 alkyl or substituted or unsubstituted heteroalkyl;
- R6 is selected from substituted or unsubstituted C1-C5 alkyl or substituted or unsubstituted heteroalkyl;
- n is an integer from 1 to 20,000;
- R3 and R4 are independently selected from:
- hydrogen, X, substituted or unsubstituted C1-6 alkyl;
- X is selected from:
- F, Cl, Br and I;
- and
- R7 is selected from:
- substituted or unsubstituted C1-C6 alkyl;
- R8 is selected from:
- hydrogen, substituted or unsubstituted C1-C6 alkyl;
- or a stereoisomer thereof or a pharmaceutically acceptable salt, a prodrug or a solvate thereof.
Dependencies are inferred from the claim text.