MELANIN PRODUCTION INHIBITOR

WIPO Patent Application WO/2010/074052

A1

Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor comprises a compound represented by general formula (1) (excluding clotrimazole) and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent, wherein at least one of A1, A2 and A3 is selected from the aryl group and the aromatic heterocyclic group, the total number of carbon atoms contained in A1, A2 and A3 is 6 to 50 and, when at least two of A1, A2 and A3 represent the aryl groups or the aromatic heterocyclic groups, the adjacent two aryl or aromatic heterocyclic groups may be bound to each other via an alkyl chain or an alkenyl chain to form a ring; m represents an integer of 0 to 2; X represents a hetero atom, a hydrogen atom, or a carbon atom; R1 and R2 are independently selected from a hydrogen atom and an oxo group, wherein when one of R1 and R2 is an oxo group, the other is not present; and R3 is selected from a hydrogen atom, and a C1-8 hydrocarbon group in which one or some of hydrogen atoms or carbon atoms may be substituted by a hetero atom or hetero atoms, wherein the number of R3’s present in the compound corresponds to the number of X’s and, when two or more R3’s are present, the R3’s are independently present and the adjacent two R3’s may be bound to each other to form, together with X, a ring, and the terminal of R3 may be bound to a carbon atom to which A1, A2 and A3 are bound, thereby forming a ring.

YOKOYAMA KOUJI (JP)
KIMURA MAKOTO (JP)
TAMAI MASASHI (JP)
SAITOH YUKO (JP)
KATO TOMOMI (JP)
IKEDA YU (JP)

PCT/JP2009/071279

July 01, 2010

December 22, 2009

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POLA CHEM IND INC (JP)
YOKOYAMA KOUJI (JP)
KIMURA MAKOTO (JP)
TAMAI MASASHI (JP)
SAITOH YUKO (JP)
KATO TOMOMI (JP)
IKEDA YU (JP)

A61K31/045; A61K8/34; A61K31/065; A61K31/075; A61K31/085; A61K31/135; A61K31/137; A61K31/198; A61K31/40; A61K31/4015; A61K31/4164; A61K31/4409; A61K31/444; A61K31/4453; A61K31/4545; A61K31/495; A61K31/5375; A61P17/16; A61Q19/02; A61K8/40; C07D207/12; C07D207/404; C07D213/30; C07D213/38; C07D233/58; C07D295/02; C07D295/08

WO2002060404A1

2002-08-08

KR20040007044A	2004-01-24
JP2004067515A	2004-03-04
JPH08231367A	1996-09-10
JPH09255634A	1997-09-30
KR20040007044A	2004-01-24
JPS5316879A	1978-02-16

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See also references of EP 2380567A4

KAWAGUCHI, Yoshiyuki et al. (JP)
Yoshiyuki Kawaguchi (JP)

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