Griseofulvin compound and pharmaceutical use thereof
AssigneeDaiichi Sankyo Company, Limited
InventorsKeiji Saito, Katsuyoshi Nakajima, Yasuyuki Ogawa, Mitsuhiro Makino, Kaori Ito, Seiko Nagata, Makoto Hirasawa
Life of this patent
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Abstract
The present invention addresses the problem of providing a compound for prophylaxis and/or treatment of central inflammatory diseases, or a pharmacologically acceptable salt thereof. The present invention addresses a compound of a general formula (I) or a pharmacologically acceptable salt thereof as a means to solve the problem. [R1: a C1-C6 alkyl group or the like, R2: a C1-C6 alkyl group or the like, A: a 5-membered aromatic hetero-ring or the like, R3, R3′: a C1-C6 alkyl group or the like].
Claims13
A method for treating a central inflammatory disease in a subject in need thereof, the method comprising delivering to the subject a compound of a general formula (1) or a pharmacologically acceptable salt thereof:
- wherein
- R1 is a C1-C6 alkyl group optionally substituted with the same or different one to two substituents selected from a substituent group X,
- a C3-C6 cycloalkyl group optionally substituted with the same or different one to two substituents selected from the substituent group X, or
- a 4-7 membered saturated heterocyclic group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- R2 is a C1-C6 alkyl group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- a C3-C6 cycloalkyl group optionally substituted with the same or different one to two substituents selected from the substituent group X, or
- a 4-7 membered saturated heterocyclic group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- A is a 5-membered aromatic heterocyclic ring,
- a 6-membered aromatic heterocyclic ring,
- an 8-10 membered condensed aromatic heterocyclic ring,
- a 5-7 membered unsaturated heterocyclic ring,
- a 4-7 membered saturated heterocyclic ring,
- a benzene ring, —CH═, or a cyano group, wherein when A is a cyano group, R3 and R3′ do not exist,
- R3 and R3′ are each independently a hydrogen atom, a halogen atom, a cyano group, a hydroxy group, an oxo group,
- a C1-C6 alkyl group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- a C1-C6 alkoxy group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- a C2-C6 alkenyl group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- a C2-C6 alkynyl group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- a C3-C6 cycloalkyl group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- an amino group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- a C1-C6 alkoxycarbonyl group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- a carbamoyl group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- a phenyl group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- a 5-membered aromatic heterocyclic group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- a 6-membered aromatic heterocyclic group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- a 5-7 membered unsaturated heterocyclic group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- a 4-7 membered saturated heterocyclic group optionally substituted with the same or different one to two substituents selected from the substituent group X,
- an 8-10 membered condensed aromatic heterocyclic group optionally substituted with the same or different one to two substituents selected from the substituent group X, or
- R3 and R3′ may form a 5-7 membered unsaturated heterocyclic ring, a 4-7 membered saturated heterocyclic ring, or a C3-C6 cycloalkyl ring as a ring that binds to each other and condenses with A, and the ring is optionally substituted with the same or different one to two substituents selected from the substituent group X,
- Substituent group X is a halogen atom, a cyano group, a hydroxy group, an oxo group, a C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C1-C6 haloalkyl group, a C3-C6 cycloalkyl group, a C3-C6 halocycloalkyl group,
- a phenyl group optionally substituted with the same or different one to two substituents selected from a substituent group Y,
- a 5-membered aromatic heterocyclic group optionally substituted with the same or different one to two substituents selected from the substituent group Y,
- a 6-membered aromatic heterocyclic group optionally substituted with the same or different one to two substituents selected from the substituent group Y,
- a 4-7 membered saturated heterocyclic group optionally substituted with the same or different one to two substituents selected from the substituent group Y,
- a C1-C6 alkoxy group, a C1-C6 haloalkoxy group, a C3-C6 cycloalkoxy group, a C3-C6 halocycloalkoxy group,
- a phenoxy group optionally substituted with the same or different one to two substituents selected from the substituent group Y,
- a 5-membered aromatic heterocyclic oxy group optionally substituted with the same or different one to two substituents selected from the substituent group Y,
- a 6-membered aromatic heterocyclic oxy group optionally substituted with the same or different one to two substituents selected from the substituent group Y,
- a 4-7 membered saturated heterocyclic oxy group optionally substituted with the same or different one to two substituents selected from the substituent group Y,
- a C1-C6 alkoxycarbonyl group, a C3-C6 cycloalkoxycarbonyl group, a carboxy group, a C1-C6 alkylcarbonyl group, a C3-C6 cycloalkylcarbonyl group,
- a phenylcarbonyl group optionally substituted with the same or different one to two substituents selected from the substituent group Y,
- a carbamoyl group, a mono (C1-C6 alkyl) aminocarbonyl group, a di (C1-C6 alkyl) aminocarbonyl group, a mono (C1-C6 alkyl) aminosulfonyl group, a di (C1-C6 alkyl) aminosulfonyl group, an amino group, a mono (C1-C6 alkyl) amino group, a di (C1-C6 alkyl) amino group, a C1-C6 alkoxycarbonylamino group, a mono (C1-C6 alkyl) aminocarbonylamino group, a di (C1-C6 alkyl) aminocarbonylamino group, a C1-C6 alkylcarbonylamino group,
- a phenylcarbonylamino group optionally substituted with the same or different one to two substituents selected from the substituent group Y,
- a 5-membered aromatic heterocyclic carbonylamino group optionally substituted with the same or different one to two substituents selected from the substituent group Y,
- a 6-membered aromatic heterocyclic carbonylamino group optionally substituted with the same or different one to two substituents selected from the substituent group Y, or
- a C1-C6 alkylsulfonylamino group,
- Substituent group Y C1-C6 alkyl group, a C1-C6 alkoxy group, a halogen atom, or a hydroxy group,
- wherein a compound or a pharmaceutically acceptable salt thereof of the following general formula (Z) is excluded:
- wherein for the compound of general formula Z:
- R1 is a C1-C6 alkyl group or a hydroxy C1-C6 alkyl group,
- R2 is a C1-C6 alkyl group,
- A is a 5-membered aromatic heterocyclic ring, and
- R3 is a C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, or a C1-C6 alkoxy C1-C6 alkyl group.
Dependencies are inferred from the claim text.