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Title:
HYDROXAMIC ACID AND ITS DERIVATIVES AS INHIBITORS OF MELANOCYTE TYROSINASE FOR TOPICAL SKIN LIGHTENERS
Document Type and Number:
WIPO Patent Application WO2003057184
Kind Code:
A3
Abstract:
Methods, compounds, and formulations are provided to reduce pigmentation in mammalian skin, comprising hydroxamic acid and its derivatives, and especially benzohydroxamic acid and its derivatives. The compounds preferably inhibit pigment synthesis in melanocytes through inhibition of melanocyte tyrosinase. The methods can be used for lightening skin, and for treating uneven skin complexions, which result from hyperpigmentation-related medical conditions such as melasma, age spots, freckles, ochronosis, and lentigo. The compounds can be used medically or cosmetically, and preferably as topical formulations.

Inventors:
DOOLEY THOMAS P (US)
CHENG LIN (US)
Application Number:
PCT/US2002/041071
Publication Date:
October 09, 2003
Filing Date:
December 23, 2002
Export Citation:
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Assignee:
INTEGRIDERM INC (US)
DOOLEY THOMAS P (US)
CHENG LIN (US)
International Classes:
A61K8/40; A61K8/42; A61K8/49; A61K31/16; A61K31/19; A61K31/44; A61K31/4409; A61K31/455; A61Q19/02; (IPC1-7): A61K7/48; A61K31/16
Domestic Patent References:
WO2000056702A12000-09-28
WO2002024613A22002-03-28
WO1995001157A11995-01-12
WO2001064206A22001-09-07
Foreign References:
US6365137B12002-04-02
DD293958A51991-09-19
US4559328A1985-12-17
EP0199151A21986-10-29
US5514676A1996-05-07
Other References:
DOOLEY T P: "TOPICAL SKIN DEPIGMENTATION AGENTS: CURRENT PRODUCTS AND DISCOVERY OF NOVEL INHIBITORS OF MELANOGENESIS", JOURNAL OF DERMATOLOGICAL TREATMENT, BASINGSTOKE, GB, vol. 8, no. 4, December 1997 (1997-12-01), pages 275 - 279, XP001037520, ISSN: 0954-6634
RICH, PETER R. ET AL., BIOCHIMICA ET BIOPHYSICA ACTA, vol. 525, 1978, pages 325 - 337, XP001091256
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; XP002243063, retrieved from STN Database accession no. 136:58529/DN, HCAPLUS
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; XP002243064, retrieved from STN Database accession no. 96:85266/DN, HCAPLUS
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; XP002243065, retrieved from STN Database accession no. 54:118360/DN, HCAPLUS
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002243066, Database accession no. 2613864
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002243067, Database accession no. 3090687
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002243068, Database accession no. 5664446
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002243069, Database accession no. 2576387
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002243070, Database accession no. 3302271
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002243071, Database accession no. 1941963
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002243072, Database accession no. 4741489
HALL I H ET AL: "THE ANTINEOPLASTIC AND CYTOTOXICITY OF BENZOHYDROXAMIC ACIDS AND RELATED DERIVATIVES IN MURINE AND HUMAN TUMOR CELLS", ANTI-CANCER DRUGS, RAPID COMMUNICATIONS, OXFORD, GB, vol. 3, no. 3, June 1992 (1992-06-01), pages 273 - 280, XP000874908, ISSN: 0959-4973
DINUNZIO, JAMES E. ET AL., JOURNAL OF CHROMATOGRAPHY, vol. 594, 1992, pages 209 - 216, XP002243062
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