发明名称 METHOD FOR IDENTIFYING LIGANDS OF THE AHR RECEPTOR HAVING THERAPEUTIC SEBOSUPPRESSIVE ACTIVITY, AND SAID LIGANDS
摘要 Sorting substances for the purpose of determining their capacity for sebosuppressive activity in topical skin treatment, an in vivo test involves: choosing a substance from ligands of aryl hydrocarbon receptor (AhR); choosing a mammal expressing cytochrome P450, family 1, subfamily A, polypeptide 1 (CYP1A1) gene; treating part of skin of mammal comprising sebaceous glands, with a composition containing substance following a dose/response/response time protocol; examining by immunohistochemical staining expression of CYP1A1 in sebaceous glands of mammal; and selecting substance. Sorting substances for the purpose of determining their capacity for sebosuppressive activity in topical skin treatment, an in vivo test involves: choosing a substance from among the ligands of the aryl hydrocarbon receptor (AhR); choosing a mammal expressing the cytochrome P450, family 1, subfamily A, polypeptide 1 (CYP1A1) gene; treating via topical route part of the skin of the mammal comprising sebaceous glands, with a composition containing the substance following a dose/response/response time protocol; examining by immunohistochemical staining the expression of CYP1A1 in sebaceous glands of the part of the skin of the mammal; and selecting the substance as a function of the sequence of onset of immunohistochemical staining in several different types of cells of the sebaceous glands. Independent claims are included for the following: (1) a composition (C1) for treating and/or preventing skin diseases of a human being, particularly acne, seborrheic dermatitis and rosacea, where the composition is configured to treat and/or prevent hyperseborrhea by means of topical application of the composition on a skin, comprising: an active substance selected from AhR agonist ligands having: an ability to activate the AhR receptor; an ability to modulate a gene regulated by AhR; a short half-life in the human organism of 2-96 hours; a measurable positive effect on a recognized criterion of hyperseborrhea, and where the active substance is positively selected by an in vivo test; (2) a pharmaceutical composition (C2) for topical use intended to reduce sebogenesis, containing 5,6-benzoflavone (5,6-BZF) as active substance; and (3) a pharmaceutical composition (C3) for treating and/or preventing human skin diseases, particularly acne, seborrheic dermatitis and rosacea, where the composition is configured to treat and/or prevent hyperseborrhea by means of topical application of the composition on a skin, comprising 5,6-benzoflavone (5,6-BZF) as active substance; (4) topical use of 5,6 benzoflavone (5,6 BZF) and rutecarpine as active substance in a sebosuppressive composition; (5) treating and/or preventing skin diseases of a human being, such as acne, seborrheic dermatitis and rosacea, comprising providing the composition (C1) and administering topically the composition to the human being; and (6) treating and/or preventing hyperseborrhea in a human being, involving providing a composition configured for topical application of a composition on a skin, where the composition contains 5,6 benzoflavone (5,6 BZF) as active substance, and administering topically the composition to the human being. ACTIVITY : Antiseborrheic; Dermatological. No biological data given. MECHANISM OF ACTION : None given.
申请公布号 SG11201407405V(A) 申请公布日期 2014.12.30
申请号 SG11201407405V 申请日期 2013.05.15
申请人 THESAN PHARMACEUTICALS, INC. 发明人 SAURAT, JEAN, HILAIRE
分类号 G01N33/50;G01N33/68 主分类号 G01N33/50
代理机构 代理人
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