Methods of treating skin with diphosphonate derivatives
AssigneeIlex Products, Inc.
InventorsStephen Moloney, Albert Jecminek
Life of this patent
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Abstract
The present invention provides for the administration of aryl-substituted 1,1-diphosphonate compounds to increase the dermal collagen content of skin and effect improvement in photoaged skin, chronologically aged skin and in skin of postmenopusal women and patients suffering from osteoporosis.
Claims45
A method for increasing the expression of dermal collagen in skin comprising the administration of an effective amount of a diphosphonate of formula (I):
- wherein X0 is H, an alkyl group having from 1 to 4 carbon atoms;
- X1, X2 and X3 are identical or different and are H, a straight or branched alkyl or alkoxy group having from 1 to 8 carbon atoms,
- R1, R2, R3 and R4 are identical or different and are H, a straight, branched or cyclic alkyl group comprising from 1 to 8 carbon atoms, or R1, R2, R3 and R4 may form an alkylidenedioxy ring comprising from 2 to 8 carbon atoms;
- B is H, or an alkyl group having from 1 to 4 carbon atoms,
- t is 0 or 1,
- when t is 1 then L is —CH═CH—CH2—, —(CH2)n—, —(CH2)n—, —s—, —SO2—, —S(CH2)n—, —SO2 (CH2)n—, where n is an integer from 1 to 7;
- or when t is 0 then L is —(CH═CH)k —(CH2)d —CH═ where k is 0 or 1 and d is an integer from 0 to 4:
A method for increasing skin thickness comprising the administration of an effective amount of a diphosphonate of formula (I):
- wherein X0 is H, an alkyl group having from 1 to 4 carbon atoms;
- X1, X2 and X3 are identical or different and are H, a straight or branched alkyl or alkoxy group having from 1 to 8 carbon atoms,
- R1, R2, R3 and R4 are identical or different and are H, a straight, branched or cyclic alkyl group comprising from 1 to 8 carbon atoms, or R1, R2, R3 and R4 may form an alkylidenedioxy ring comprising from 2 to 8 carbon atoms;
- B is H, or an alkyl group having from 1 to 4 carbon atoms,
- t is 0 or 1,
- when t is 1 then L is —CH═CH—CH2—, —(CH2)n—, —O(CH2)n—, —S—, —SO2—, —S(CH2)n—, —SO2 (CH2)n—, where n is an integer from 1 to 7;
- or when t is 0 then L is —(CH═CH)k —(CH2)d —CH═ where k is 0 or 1 and d is an integer from 0 to 4.
A method for retarding and /or reversing the formation of fine lines and wrinkles in photoaged skin in a human subject requiring such treatment comprising the administration of an effective amount of a diphosphonate of formula (I):
- wherein X0 is H, an alkyl group having from 1 to 4 carbon atoms;
- X1, X2 and X3 are identical or different and are H, a straight or branched alkyl or alkoxy group having from 1 to 8 carbon atoms,
- R1, R2, R3 and R4 are identical or different and are H, a straight, branched or cyclic alkyl group comprising from 1 to 8 carbon atoms, or R1, R2, R3 and R4 may form an alkylidenedioxy ring comprising from 2 to 8 carbon atoms;
- B is H, or an alkyl group having from 1 to 4 carbon atoms,
- t is 0 or 1,
- when t is 1 then L is —CH═CH—CH2—, —(CH2)n—, —O(CH2)n—, —S—, —SO2—, —S(CH2)n—, —SO2 (CH2)n—, where n is an integer from 1 to 7;
- or when t is 0 then L is —(CH═CH)k —(CH2)d —CH═ where k is 0 or 1 and d is an integer from 0 to 4.
A topical pharmaceutical composition comprising a pharmaceutically acceptable topical carrier and a compound of formula (I):
- wherein X0 is H, an alkyl group having from 1 to 4 carbon atoms;
- X, X2 and X3 are identical or different and are H, a straight or branched alkyl or alkoxy group having from 1 to 8 carbon atoms,
- R1, R2, R3 and R4 are identical or different and are H, a straight, branched or cyclic alkyl group comprising from 1 to 8 carbon atoms, or R1, R2, R3 and R4 may form an alkylidenedioxy ring comprising from 2 to 8 carbon atoms;
- B is H, or an alkyl group having from 1 to 4 carbon atoms,
- t is 0 or 1,
- when t is 1 then L is —CH═CH—CH2—, —(CH2)n—, —O(CH2)n—, —S—, —SO2—, —S(CH2)n—, —SO2(CH2)n—, where n is an integer from 1 to 7;
- or when t is 0 then L is —(CH═CH)k —(CH2)d —CH═ where k is 0 or 1 and d is an integer from
- 0 to 4;
- wherein the said compound of formula (I) is in an amount effective to increase the expression of dermal collagen when applied to skin.
Dependencies are inferred from the claim text.