Pharmaceutical composition containing a mitophagy inducer
AssigneeHangzhou PhecdaMed Co., Ltd.
InventorsDong LIU, Zhen TIAN, Ronghai WU
Life of this patent
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Abstract
A pharmaceutical composition containing a mitophagy inducer as an active substance. The pharmaceutical composition is conducive to being prepared into a pharmaceutical preparation, can avoid incompatibility caused by the interaction between the active substance and an auxiliary material, and thus can be stored for a long period of time.
Claims17
1-7. (canceled)
A pharmaceutical composition, characterized in that the pharmaceutical composition contains a compound of Formula I or a pharmaceutically acceptable salt thereof, a diluent, a disintegrant, a lubricant, and does not contain any of the following ingredients:
- hydroxypropyl cellulose, crospovidone, colloidal silica, magnesium stearate, talc, mannitol, croscarmellose sodium,
- wherein, R2 is hydrogen, C1~4 alkyl, C3~6 cycloalkyl, four to six-membered epoxy alkyl;
- R3 is
- wherein, R3-1 is hydrogen, hydroxyl, C1~4 alkyl, C1~4 alkoxy, C3~6 cycloalkyl, three to six-membered epoxy alkyl, —N(R3-2R3-2a), —CH2C(O)R3-2, —CH2C(O)OR3-2, —CH2C(O)NR3-2 R3-2a,
- R3-2 and R3-2a are independently hydrogen, C1~4 alkyl or three to six-membered cycloalkyl respectively,
- Ar is phenyl, 5 or 6-membered monocyclic heteroaryl, 5 or 6-membered monocyclic heteroaryl substituted by at least one R3-3, said R3-3 is hydrogen, halogen, C1~4 alkyl, three to six-membered cycloalkyl, hydroxyl, C1~4 Alkoxy, three to six-membered epoxy alkyl, C1~4 halogenated alkyl, C2~4 alkenyl, C2~4 alkynyl, —N(R3-3aR3-3b) or phenyl,
- R3-3a and R3-3b are independently hydrogen, C1~4 alkyl or three to six-membered cycloalkyl respectively;
- R4 is
- wherein, R4-1 is phenyl, phenyl substituted by at least one R4-11, 5 or 6-membered monocyclic heteroaryl, 5 or 6-membered monocyclic heteroaryl substituted by at least one R4-11, 8 to 10-membered fused bicyclic heteroaryl, 8 to 10-membered fused bicyclic heteroaryl substituted by at least one R4-11, said R4-11 is halogen, nitro, C1~4 alkyl, C3~6 cycloalkyl, C1~4 alkoxy, —N(R4-1aR4-1b), phenyl, C1~4 halogenated alkyl, C1~4 halogenated alkoxy or
- R4-1a and R4-1b are independently hydrogen, C1~4 alkyl or C3~6 cycloalkyl respectively, and R4-1a and R4-1b may be bonded to each other to form a ring,
- R4-2 is C1~4 alkyl, C3~6 cycloalkyl, or when R2 is C1~4 alkyl, R4-2 is bonded to R2 to form a 4~8-membered ring,
- R4-3 is C1~4 alkyl or C1~4 alkoxy;
- the number of R5 is 0~5, when the number of R5 is not 0, each R5 is independently selected from halogen, nitro, nitrile, —N+(R5-1)3, C1~4 halogenated alkyl, —C(O)OR5-1, —C(O)R5-1, —C(O)N(R5-1R5-1a), —C(O)N(R5-1R5-1a), —S(O)2R5-1, —S(O)R5-1, —N═C(R5-1R5-1a), hydroxyl, C1~4 alkyl, phenyl, phenyl with at least one hydrogen substituted by R5-1, C1~4 alkoxy, —N(R5-1R5-1a), —N(R5-1)C(O)R5-1a, —OC(O)R5-1, —OC(O)N(R5-1R5-1a) or —SR5-1, wherein R5-1, R5-1a and R5-1b are independently hydrogen, C1~4 alkyl, C2~4 alkenyl, C2~4 alkynyl, C1~4 alkyl with at least one hydrogen substituted by halogen, C2~4 alkenyl with at least one hydrogen substituted by halogen or C2~4 alkynyl with at least one hydrogen substituted by halogen respectively.
Dependencies are inferred from the claim text.