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filingDate 2016-12-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2018-03-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-107040-A1
titleOfInvention AMINOAZOL DERIVATIVE
abstract A compound or a medically acceptable salt thereof, which has an effect of regulating the activity of an androgen receptor. Claim 1: A compound represented by the formula (1) or a medically acceptable salt thereof, wherein, X represents a sulfur atom or an oxygen atom; Z represents a group selected from the compounds of formula (2) to (4); A represents a C₆₋₁₂ aryl or a 5-12 membered heteroaryl group; R¹¹ to R¹⁴ each independently represent a hydrogen atom, a halogen, a hydroxyl group, a C₁₋₃ alkyl group optionally substituted with a halogen or a hydroxyl group, a C₁₋₃ alkoxy group optionally substituted with a halogen or a hydroxyl group, likewise, two selected from R¹¹ to R¹⁴ can form a ring; n is an integer of 0 or more and 3 or less; Rᵃ are the same or different, and represent a halogen, a hydroxyl group, a C₁₋₆ alkyl group (optionally substituted with a halogen, a hydroxyl group, a phenoxy group or a benzyloxy group), a C₃₋₈ cycloalkyl group optionally substituted with a halogen, a C₁₋₆ alkoxy group (optionally substituted with a halogen, a hydroxyl group, a carboxyl group, a carbamoyl group optionally substituted with a C₁₋₄ alkyl group, a C₁₋₄ alkoxy group or a benzyloxy group), a C₃₋₈ cycloalkoxy group optionally substituted with a halogen, a C₁₋₄alkyl C₁₋₄alkoxy group (optionally substituted with a halogen, a hydroxyl group, a cyano group, a C₁₋₄ alkoxy group or a benzyloxy group), a phenoxy group , a benzyloxy group, a cyano group, a nitro group, a carboxyl group, a C₁₋₆ acyl group, a C₁₋₄ alkoxycarbonyl group, an amino group, a C₁₋₆ monoalkylamino group, a dialkyl group min C, a carbamoyl group optionally substituted with a C₁₋₄ alkyl group, a C₆₋₁₂ aryl group (optionally substituted with a halogen, a cyano group, a C₁₋₄ alkyl group optionally substituted with a halogen, or a group hydroxyl), a 3-12 membered heterocyclic group optionally substituted with a halogen, a sulfanyl group optionally substituted with a C₁₋₆ alkyl group optionally substituted with a halogen, a C₁₋₆ alkylsulfinyl group optionally substituted with a halogen, an alkylsulfonyl group C₁₋₆ optionally substituted with a halogen, or a pentafluorosulfanyl group; R¹ represents a C₁₋₉ alkyl group (optionally substituted with a halogen, a hydroxyl group, a cyano group, a carboxyl group, a C₁₋₄ alkoxycarbonyl group, an amino group, a C₁₋₆ monoalkylamino group, a C₁₋ dialkylamino group ₆ or a C₁₋₆ alkylsulfonyl group), a C₃₋₈ cycloalkyl group (optionally substituted with a halogen, a hydroxyl group or a cyano group), a C₂₋₆ alkenyl group optionally substituted with a halogen or a phenyl group, a group C₂₋₆ alkynyl optionally substituted with a halogen or a phenyl group, a C₁₋₆ alkoxy group (optionally substituted with a halogen, a hydroxyl group, a cyano group or a C₁₋₄ alkoxy group), an aryl group C₆₋₁₂ optionally substituted with 1 to 3 residues of Rᶜ, an aryl group C₆₋₁₂alkyl C₁₋₆ optionally substituted with 1 to 3 residues of Rᵈ, a heterocyclic group of 3-12 members optionally substituted tuido with 1 to 3 R restos moieties, or a 3-12 membered C₁₋₆heterocyclic alkyl group optionally substituted with 1 to 3 Rᶠ moieties; R² represents a hydrogen atom, a halogen, a C₁₋₆ alkyl group (optionally substituted with a halogen, a hydroxyl group or a cyano group), a C₃₋₈ cycloalkyl group (optionally substituted with a halogen, a hydroxyl group or a cyano group) or a phenyl group (optionally substituted with a halogen, a hydroxyl group or a cyano group); R³ represents a hydrogen atom, a halogen, a C₁₋₁₂ alkyl group (optionally substituted with a halogen, a hydroxyl group, a cyano group, a carboxyl group, a C₃₋₈ cycloalkyl group optionally substituted with a halogen or a hydroxyl group , a C₃₋₈ cycloalkoxy group optionally substituted with a halogen or a hydroxyl group, a C₁₋₄ alkoxy group optionally substituted with a phenyl group, a C₁₋₄ alkoxycarbonyl group, an amino group, a C₁₋₆ monoalkylamino group, a group C₁₋₆ dialkylamino, a C₁₋₆ alkylsulfonyl group, a phenoxy group or a silyl group substituted with a C₁₋₄ alkyl group or a phenyl group), a C₃₋₈ cycloalkyl group (optionally substituted with a halogen, a hydroxyl group, a cyano group, a carboxyl group, a C₁₋₄ alkyl group optionally substituted with a halogen or a hydroxyl group, a C₁₋₄ alkoxy group optionally substituted with a halogen eno or a hydroxyl group, a C₁₋₄ alkoxycarbonyl group, an amino group, a C₁₋₆ monoalkylamino group, a C₁₋₆ dialkylamino group or a C₁₋₆ alkylsulfonyl group, a C₁₋₆alkyl C₁₋₆ alkoxy group (optionally substituted with a halogen, a hydroxyl group, a cyano group or a C₁₋₄ alkoxy group), a C₂₋₉ alkenyl group (optionally substituted with a halogen, a hydroxyl group or a cyano group), a C₂₋₉ alkynyl group optionally substituted with a halogen or a cyano group, a C₃₋₈ cycloalkenyl group (optionally substituted with halogen, a hydroxyl group or a cyano group), a C₆₋₁₂ aryl group optionally substituted with 1 to 5 Rᵍ residues, a C₆ aryl group ₋₁₂C₁₋₆ alkyl optionally substituted with 1 to 5 R restos moieties, a 3-12 membered heterocyclic group optionally substituted with 1 to 5 Rⁱ moieties, a 3-12 membered C₁₋₆heterocyclic alkyl group selects It is substituted with 1 to 5 residues of Rʲ, a C₁₋₉ acyl group (optionally substituted with a halogen, a hydroxyl group or a cyano group), a C₃₋₈ cycloalkylcarbonyl group, a benzoyl group, a C₅₋₁₂ spiroalkyl group, an adamantyl group, a silyl group substituted with 1 to 3 residues of C₁₋₄ alkyl group or a phenyl group, or R³⁰, wherein R³ R is a substituent represented by the formula (5); R³¹ and R³² each independently represent a hydrogen atom, a C₁₋₆ alkyl group optionally substituted with a halogen, a C₃₋₈ cycloalkyl group optionally substituted with a halogen, or a phenyl group optionally substituted with a halogen, and R³¹ and R³² can form a ring by connecting directly with each other or through an oxygen atom, a nitrogen atom or a sulfur atom; R⁴ and R⁵ each independently represent a hydrogen atom, a halogen, a C₁₋₆ alkyl group (optionally substituted with a halogen, a hydroxyl group or a cyano group), a phenyl group or a C₃₋ cycloalkyl group ₈ (optionally substituted with a halogen, a hydroxyl group or a cyano group), and R³ and R⁴ can form a ring; Rᶜ, Rᵈ, Rᵉ and Rᶠ represent a halogen, a hydroxyl group, a C₁₋₆ alkyl group optionally substituted with a halogen, a C₃₋₈ cycloalkyl group optionally substituted with a halogen, a C₁₋₆ alkoxy group optionally substituted with a halogen , a C₃₋₈ cycloalkoxy group optionally substituted with a halogen, a C₁₋₄alkyl C₁₋₄alkoxy group (optionally substituted with a halogen, a hydroxyl group, a phenyl group or a C₁₋₄ alkoxy group), a cyano group, a nitro group, an oxo group, a carboxyl group, a C₁₋₆ acyl group, a C₁₋₄ alkoxycarbonyl group, an amino group, a C₁₋₆ monoalkylamino group, a C₁₋₆ dialkylamino group, a sulfanyl group, an alkylsulfanyl group C₁₋₆ optionally substituted with a halogen, a C₁₋₆ alkylsulfinyl group optionally substituted with a halogen or a C₁₋₆ alkylsulfonyl group optionally substituted with a halogen; Rᵍ, Rʰ, Rⁱ and Rʲ represent a halogen, a hydroxyl group, an amino group, a C₁₋₆ monoalkylamino group, a C₁₋₆ dialkylamino group, an acetamido group, a C₁₋₆ alkyl group (optionally substituted with a halogen, a hydroxyl group, a phenoxy group or a benzyloxy group), a C₃₋₈ cycloalkyl group, a C₂₋₆ alkenyl group (optionally substituted with a halogen, a hydroxyl group or a cyano group), an optionally substituted C₂₋₆ alkynyl group with a halogen or a cyano group, a C₁₋₆ alkoxy group (optionally substituted with a halogen, a hydroxyl group, a C₁₋₄ alkoxy group, an amino group, a C₁₋₆ monoalkylamino group, a C₁₋₆ dialkylamino group, a C₆₋₁₀ aryl group or a 3-10 membered heterocyclic group optionally substituted with an oxo group), a C₁₋₆-C₁₋₆ alkoxy group (optionally substituted with a halogen, a phenyl group, a phenoxy group or a group benzyloxy), a C₃₋₈ cycloalkoxy group, a cyano group, a nitro group, an oxo group, a carboxyl group, a sulfanyl group, a C₁₋₆ alkylsulfanyl group optionally substituted with a halogen, an optionally substituted C₁₋₆ alkylsulfinyl group with a halogen, a phenylsulfonyl group optionally substituted with a C₁₋₄ alkyl group, a C₁₋₆ alkylsulfonyl group optionally substituted with a halogen, a C₁₋₆ acyl group, a C₁₋₄ alkoxycarbonyl group, a phenyl group (optionally substituted with a halogen, a cyano group, a trifluoromethyl group or a hydroxyl group), a 3-12 membered heterocyclic group optionally substituted with a halogen or an oxo group, a phenoxy group, a C₆₋₁₂alkoxy C₁₋₆ aryl group, a group 3-12-membered Cícheterocyclic alkoxy or a group represented by the formula R³⁰-CH₂-O-. Claim 15: A compound represented by any of the chemical formulas selected from the group of formulas (6).
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