IP Library › Granted Patent US 9,181,161
Granted Patent B2
US 9,181,161 · App. 14/396,635 · Granted Nov 10, 2015

Use of dicyclohexylmethanol derivatives having antimicrobial properties

Inventors: Thomas Rudolph (Darmstadt, DE); Tatjana Best (Hergershausen, DE)
Assignee: Merck Patent GmbH
C07C43/196A01N31/04A01N31/06A01N37/02A01N41/04A61K8/345A61K8/466A61K31/047A61K31/08A61K31/185A61Q5/006A61Q15/00A61Q17/005C07C29/20C07C35/21C07C41/20A61K2800/10A61K2800/40A61Q11/00
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Quick Facts
Patent No.
US 9,181,161
App. No.
14/396,635
Granted
Nov 10, 2015
Kind
B2
Abstract

The present invention relates to the use of at least one dicyclohexylmethanol derivative of the formula (I) as antimicrobial active compound or as anti-acne, antidandruff, deodorant or antiperspirant active compound, to preparations comprising these compounds, and to specific dicyclohexylmethanol derivatives and to a process for the preparation thereof.

Claims (39)

1. A method for achieving an antimicrobial effect, or an anti-acne, antidandruff, deodorant or antiperspirant effect, comprising applying to a subject or to a material on or in which said antimicrobial effect is desired or applying to a subject in need of an anti-acne, antidandruff, deodorant or antiperspirant effect at least one compound of formula I

in which

R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 stand, independently of one another, for H, OH, OCOCH 3 , CH 2 OH, SO 3 H, halogen, or a straight-chain or branched alkyl or alkoxy group having 1 to 20 C atoms.

2. A method according to claim 1 , wherein the material on or in which said antimicrobial effect is desired is selected from the group consisting of cosmetic compositions, pharmaceutical compositions, medicinal products, foods, household products, plastics, paper and paints.

3. A method according to claim 2 , wherein the material on or in which said antimicrobial effect is desired is selected from the group consisting of dental and oral care products.

4. A method according to claim 1 , which is for improving preservation.

5. A method according to claim 1 , which is for achieving an anti-acne, antidandruff, deodorant or antiperspirant effect, comprising applying to a subject in need of an anti-acne, antidandruff, deodorant or antiperspirant effect at least one compound of formula I

in which

R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 stand, independently of one another, for H, OH, OCOCH 3 , CH 2 —OH, SO 3 H, halogen, or a straight-chain or branched alkyl or alkoxy group having 1 to 20 C atoms.

6. A method according to claim 1 , wherein at least one of the radicals R1 to R10 stands for OH or a straight-chain or branched alkoxy group having 1 to 20 C atoms.

7. A method according to claim 1 , wherein the compound of formula I stands for a compound of formula Ia

in which

R2 stands for H or SO 3 H,

R3 stands for H, OH, or a straight-chain or branched alkyl or alkoxy group having 1 to 20 C atoms,

R5 stands for H or OH,

R7 stands for H or SO 3 H,

R8 stands for H, OH, halogen or a straight-chain or branched alkoxy group having 1 to 20 C atoms, and

R10 stands for H, OH or a straight-chain or branched alkoxy group having 1 to 20 C atoms.

8. A method according to claim 1 , wherein the at least one compound of formula I stands for one or more compounds of formulae I-1 to I-17

9. A method according to claim 1 , wherein the antimicrobial effect is the prevention of microbial contamination, or the reduction of the growth of microorganisms or the destruction or deactivation of microorganisms, or the inhibition or suppression of the growth and reproduction of microorganisms.

10. A method according to claim 1 , wherein the antimicrobial effect is the reduction of the growth of microorganisms or the destruction or deactivation of microorganisms, or the inhibition or suppression of the growth and reproduction of microorganisms.

11. A method according to claim 1 , wherein the antimicrobial effect is the prevention of microbial contamination on or in a material where the antimicrobial effect is desired, which is selected from the group consisting of cosmetic compositions, pharmaceutical compositions, medicinal products, foods, household products, plastics, paper and paints.

12. A composition, comprising at least one compound of formula I

in which

R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 stand, independently of one another, for H, OH, OCOCH 3 , CH 2 —OH, SO 3 H, halogen, or a straight-chain or branched alkyl or alkoxy group having 1 to 20 C atoms,

and at least one carrier compound or vehicle.

13. A composition according to claim 12 , wherein the compound of formula I is present in an amount of 0.01 to 20% by weight, based on the total amount of the preparation.

14. A composition according to claim 12 , which is a deodorant, an antiperspirant, an antidandruff or anti-acne composition or an antibacterial composition, or an antibacterial dental or oral care composition.

15. A composition according to claim 12 , which comprises at least one further preservative and/or antimicrobial active compound, which is not a compound of formula I.

16. A process for preparing a composition according to claim 12 , comprising mixing together at least one compound of formula I with at least one carrier compound or vehicle.

17. A composition according to claim 12 , wherein in the compound of formula I, at least one of the radicals R1 to R10 stands for OH or a straight-chain or branched alkoxy group having 1 to 20 C atoms.

18. A compound of formula I

in which

R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 stand, independently of one another, for H, OH, OCOCH 3 , CH 2 —OH, SO 3 H, halogen, or a straight-chain or branched alkyl or alkoxy group having 1 to 20 C atoms,

with the proviso that at least one of the radicals R1 to R10 stands for OH or a straight-chain or branched alkoxy group having 1 to 20 C atoms.

19. A compound according to claim 18 , which is one of the following compounds of formula I-1 to I-17

20. A process for preparing a compound of formula I according to claim 18 , comprising converting a compound of formula II

where R1 to R10 are as defined for formula I,

into a corresponding hydrogenated compound of formula I by hydrogenation.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 23, 2014
From: RUDOLPH, THOMAS; BEST, TATJANA
To: MERCK PATENT GMBH
Reel/Frame 034021/0893 →
Priority Claims (2)
DE 10 2012 008 119 · Apr 25, 2012 · national
DE 10 2012 016 194 · Aug 16, 2012 · national
Continuity (1)
Related Publication 20150118172A1 · Apr 30, 2015