KR920700035A - Topical anti-angiogenic agents as hair growth inhibitors - Google Patents

Abstract

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Description

Topical anti-angiogenic agents as hair growth inhibitors

As this is a public information case, the full text was not included.

Claims (15)

Use of a compound of formula I for the manufacture of a medicament for inhibiting hair growth in a mammal consisting of topically administering a composition consisting of a compound of formula I and an pharmacologically acceptable salt thereof in an amount effective for anti-vessel formation : Wherein a dashed line between positions C-1 and C-2 means that a double bond is present or absent; Binding at C-6 represents α or β; B ₁ is CH ₃ or -C ₂ H ₅ ; R ₂ is H, R ₃ is in the α-position and is —OH, —O-alkyl- (C ₁ -C ₁₂ ), -OC (═O) alkyl (C ₁ -C ₁₂ ) -OC (= 0) Aryl, -OC (= 0) N (R) ₂ or -OC (= 0) R ₇ , wherein aryl is furyl, thienyl, pyrrolyl or pyridyl, wherein each hetero moiety is one or two Optionally substituted with a (C ₁ -C ₄ ) alkyl group or aryl is — (CH ₂ ) _f -phenyl, wherein f is 0-2 and the phenyl ring is chlorine, fluorine, bromine, alkyl (C ₁ -C ₃ ), alkoxy (C ₁ -C ₃ ), thioalkoxy (C ₁ -C ₃ ), Cl ₃ C-, F ₃ C-, -NH ₂ and -NHCOCH ₃ optionally substituted with 1-3 groups selected from wherein R is Hydrogen, alkyl (C ₁ -C ₄ ), or phenyl and each R may be the same or different, wherein R ₇ is aryl or alkyl (C ₁ -C ₁₂ ) as described above; R ₂ is α-Cl and R ₃ is β-Cl; R ₂ and R ₃ taken together are oxygen (—O—) bridging positions C-9 and C-11; R ₂ and R ₃ are taken together to form a double bond between positions C-9 and C-11; R ₄ is H, CH ₃ , Cl or F; R ₅ is H, OH, F, Cl, Br, CH ₃ , phenyl, vinyl or allyl; R ₆ is H or CH ₃ ; R ₉ is H, OH, CH ₃ , F or = CH ₂ ; R ₁₀ is H, OH, CH ₃ or R ₁₀ forms a second bond between positions C-16 and C-17. The use according to claim ₁ , wherein R ₁ , R ₂ , R ₃ , R ₄ and R ₆ are hydrogen, R ₅ is fluorine, R ₉ is methyl, and R ₁₀ is hygisil. Use according to claim 2, wherein R ₉ is α-methyl. Use according to claim 2, wherein R ₉ is β-methyl. Use according to claim 1, wherein the composition comprises at least 1 mg / ml of the compound of general formula (I). 6. Use according to claim 5, wherein the compound of general formula I is present in an amount of about 1- about 10 mg / ml. 2. Use according to claim 1, comprising a pharmaceutical carrier suitable for topical application in said composition. Use according to claim 1, wherein the composition is routinely applied to the therapeutic area. 9. Use according to claim 8, wherein said composition is applied daily or twice daily. A pharmaceutical composition consisting of a compound of Formula I and their pharmaceutically acceptable salts in an effective amount for anti-vessel formation and a pharmaceutical carrier suitable for topical application: Wherein a dashed line between positions C-1 and C-2 means that a double bond is present or absent; Binding at C-6 represents α or β; R ₁ is CH ₃ or —C ₂ H ₃ ; R ₂ is H and R ₃ is in the α- position, -OH, -O- alkyl, _{- (C 1 -C 12),} -OC (= O) alkyl _{(C 1 -C 12), -OC} (= O ) Allyl, -OC (= 0) N (R) ₂ or -OC (= 0) OR ₇ , wherein aryl is furyl, thienyl, pyrrolyl, or pyridyl, wherein each of the hetero moieties is one or Optionally substituted with two (C ₁ -C ₄ ) alkyl groups, or aryl is — (CH ₂ ) _f -phenyl, where f is 0-2 and the phenyl ring is chlorine, fluorine, bromine, alkyl (C ₁ -C ₃₎ ), Alkoxy (C ₁ -C ₃ ) thioalkoxy (C ₁ -C ₃ ), Cl ₃ C-, F ₃ C-, -NH ₂ and -NHCOCH ₃ optionally substituted with 1-3 groups, wherein R is hydrogen, alkyl (C ₁ -C ₄ ), or phenyl and each R may be the same or different, wherein R ₇ is aryl or alkyl (C ₁ -C ₁₂ ) as described above; R ₂ is α-Cl and R ₃ is β-Cl; R ₂ and R ₃ taken together are oxygen (—O—) bridging positions C-9 and C-11; R ₂ and R ₃ are taken together to form a double bond between positions C-9 or C-11, and R ₄ is H, CH ₃ , Cl or F; R ₅ is H, OH, F, Cl, Br, CH 3, phenyl, vinyl or aryl; R ₆ is H or CH ₃ ; R ₉ is H, OH, CH ₃ , F or = CH 2; R ₁₀ is H, OH, CH ₃ or R ₁₀ forms a second bond between positions C-16 and C-17. The composition of claim 10, wherein R ₁ , R ₂ , R ₃ , R ₄ and R ₆ are hydrogen, R ₅ is fluorine, R ₉ is methyl, and R ₁₀ is hydroxyl. The composition of claim 11, wherein R ₉ is α-methyl. 12. The composition of claim 11, wherein R ₉ is β-methyl. The composition of claim 10, wherein said composition comprises at least 1 mg / ml of a compound of Formula I. The composition of claim 14, wherein the compound of Formula I is present in an amount of about 1-about 10 mg / ml. ※ Note: It is to be disclosed by the contents of the original application.