Title:
クロメン-4-オン誘導体類の使用
Document Type and Number:
Japanese Patent JP4850397
Kind Code:
B2
Abstract:
The use of substituted mono- or polyhydroxy-chromen-4-one derivatives of formula (I) (or (I)-containing preparations) for care, preservation or improvement of general condition of the skin or hair and preventing and/or inhibiting premature skin aging, skin diseases associated with keratinization or benign or malignant growths of the dermis or epidermis is new. The use of chromenones of formula (I) (or (I)-containing preparations) is claimed for: (1) care, preservation or improvement of general condition of the skin or hair; (2) production of preparations for preventing and/or inhibiting premature skin aging; (3) production of preparations for the prophylaxis and/or treatment of skin diseases associated with keratinization; or (4) production of preparations for the prophylaxis and/or treatment of benign or malignant growths of the dermis or epidermis. R 1>, R 2> : H, COR 7>, COOR 7>, 1-20C alkyl, 3-20C alkenyl, 1-20C hydroxyalkyl (where the OH groups are bonded to primary or secondary C-atoms and the chain is optionally interrupted by O); or 3-10C cycloalkyl or 3-10C cycloalkenyl (both optionally over-bridged by (CH 2) n); n : 1-3; R 3> : H or 1-20C alkyl; R 4> : H or OR 8>; R 5>, R 6> : H, OH, 1-20C alkyl, 3-20C alkenyl or 1-20C hydroxyalkyl (where the OH groups are bonded to primary or secondary C-atoms and the chain is optionally interrupted by O); R 7> : H, 1-20C alkyl or the residue of a polyhydroxy compound (preferably an ascorbic acid or glycoside residue); and R 8> : H or 1-20C alkyl. Provided that at either (i) at least two of R 1>, R 2>and R 4>- R 6>are other than H or (ii) at least one of R 1>and R 2>= COR 7>or COOR 7>. Independent claims are included for: (1) preparations containing at least one compound (I), at least one skin-care component (II) and a carrier for topical application; and (2) the production of preparations containing (I), by mixing (I) with a cosmetic, dermatological or foodstuff carrier. [Image] ACTIVITY : Dermatological; antiseborrheic; antiinflammatory; immunosuppressive; antiallergic; antipsoriatic; antirheumatic; cytostatic; virucide; antipruritic; vulnerary; ophthalmological; antialopecia; antiarthritic; cardiant; antiarteriosclerotic; hypotensive; antidiabetic; vasotropic; anorectic. MECHANISM OF ACTION : Protein kinase inhibitor; elastase inhibitor; aldose reductase inhibitor; hyaluronidase inhibitor; catechol-O-methyl transferase inhibitor; AMP phosphodiesterase inhibitor; antioxidant; antiradical. 5,7-Dihydroxy-2-methyl-chromen-2-one (Ia) had IC 5 020 mM for inhibition of hyaluronidase.
Inventors:
Christoph Carora
Sylvia Huber
Ralph Roskopf
Helvic Buchholz
Sylvia Huber
Ralph Roskopf
Helvic Buchholz
Application Number:
JP2004236984A
Publication Date:
January 11, 2012
Filing Date:
August 17, 2004
Export Citation:
Assignee:
Merck Patent Gesellschaft mit beschraenkter Haftung
International Classes:
A61K8/49; C07D311/22; A23L1/30; A61K8/00; A61K8/33; A61K8/35; A61K8/37; A61K8/42; A61K8/67; A61K31/197; A61K31/35; A61K31/352; A61K31/353; A61K31/375; A61K31/4188; A61K31/4406; A61K45/06; A61P1/06; A61P17/00; A61P17/06; A61P17/10; A61P17/12; A61P17/16; A61P29/00; A61P35/00; A61P37/08; A61P43/00; A61Q5/00; A61Q17/00; A61Q17/04; A61Q19/00; A61Q19/08; C07D407/12; A61Q11/00; A61Q19/02
Domestic Patent References:
| JP1096134A | ||||
| JP58062112A | ||||
| JP10194919A | ||||
| JP7188208A | ||||
| JP10114640A | ||||
| JP5301813A | ||||
| JP9188608A | ||||
| JP2002520357A | ||||
| JP2002506807A | ||||
| JP2003128532A |
Foreign References:
| WO2003043595A1 | ||||
| WO2001072287A1 |
Attorney, Agent or Firm:
Akio Miyazaki
Ishibashi Masayuki
Masaaki Ogata
Haruka Oka
Ishibashi Masayuki
Masaaki Ogata
Haruka Oka