Enzyme inhibitors
AssigneeThe Procter & Gamble Company
InventorsScott Edward Osborne, Todd Laurence Underiner
Life of this patent
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Abstract
The present invention relates to compositions which comprise one or more polymer conjugates having the formula: wherein T is a heterocyclic unit which is capable of inhibiting one or more proteolytic enzymes; L is a linking group; [Poly] is a polymeric unit, i indicates the number of said heterocyclic units which comprise said conjugate and has the value of from 1 to 100; z is 0 or 1, said polymer conjugates suitable for use in preventing skin irritation resulting from exposure of the skin to body fluids, inter alia, feces, menstrual fluid. The conjugates of the present invention are useful in diapers, dressings, sanitary napkins, and the like.
Claims41
A composition for inhibiting enzymes comprising:
- a) from about 0.01% by weight, of one or more polymer conjugates capable of inhibiting one or more proteolytic enzymes having the formula:
- wherein T has a formula selected from the group consisting of:
- xi) and mixtures thereof;
- wherein X is selected from the group consisting of —CH2—, —NH—, —O—, —S—, —CF2—, and mixtures thereof;
- and each D, E, F, and G is independently selected from the group consisting of —CH—, —CH2—, —N—, —NH—, —O—, —S—, —CF2—, and mixtures thereof;
- a) hydrogen;
- b) C1-C18 substituted or unsubstituted, linear or branched alkyl;
- c) C3-C18 substituted or unsubstituted, linear or branched cycloalkyl
- d) C2-C18 substituted or unsubstituted, linear or branched alkenyl;
- e) C2-C18 substituted or unsubstituted, linear or branched alkynyl;
- f) C6-C18 substituted or unsubstituted aryl;
- g) C2-C18 substituted or unsubstituted heterocyclic alkyl;
- h) C3-C18 substituted or unsubstituted heterocyclic alkenyl;
- i) alkylenearyl having the formula:
- —(R1)n—R2
- wherein R1 is C1-C12 linear or branched alkylene, C2-C12 linear or branched alkenylene, or mixtures thereof;
- R2 C6-C18 substituted or unsubstituted aryl, or mixtures thereof;
- n is from 1 to 16;
- j) an amino unit having the formula:
- —(CH2)mN(R3)2
- wherein each R3 is independently C1-C18 substituted or unsubstituted, linear or branched alkyl;
- m is from 0 to 10;
- k) a quaternary ammonium unit having the formula:
- wherein each R3 is independently C1-C18 substituted or unsubstituted, linear or branched alkyl;
- Y is an anion of sufficient charge to provide electronic neutrality;
- m is from 0 to 10;
- l) a unit having the formula:
- wherein R4 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R5 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R4 and R5 can be taken together to form a heterocyclic ring comprising from 3 to 5 carbon atoms;
- m) a unit having the formula:
- wherein R6 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R7 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R6 and R7 can be taken together to form a heterocyclic ring comprising from 3 to 5 carbon atoms;
- n) a unit having the formula:
- —R8—R9
- wherein R8 is:
- i) —(CH2)p—, wherein p is from 0 to 12;
- ii) —C(O)—;
- iii) —C(X)NR10—, wherein R10 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- X is oxygen, sulfur, NR10, and mixtures thereof;
- iv) —C(X)R11C(X)—, wherein R11 is C1-C18 alkylene, substituted or unsubstituted phenylene. or mixtures thereof;
- X is oxygen, sulfur, NR10, and mixtures thereof;
- v) —C(X)NR10C(X)—, wherein R10 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- X is oxygen, sulfur, NR10, and mixtures thereof;
- vi) —C(X)NR10R11NR10C(X)—, wherein R10 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- X is oxygen, sulfur, NR10, and mixtures thereof;
- vii) —NR10C(X)—, wherein R10 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- X is oxygen, sulfur, NR10, and mixtures thereof;
- viii) —NR10C(X)NR10—, wherein R10 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- X is oxygen, sulfur, NR10, and mixtures thereof;
- ix) —NR10C(X)R11NR10—, wherein R10 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- X is oxygen, sulfur, NR10, and mixtures thereof;
- x) —NR10R11C(X)NR10—, wherein R10 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- x is oxygen, sulfur, NR10, and mixtures thereof;
- xi) —NR10C(X)R11C(X)O—, wherein R10 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- X is oxygen, sulfur, NR10, and mixtures thereof;
- xii) —OC(X)R11C(X)NR10—, wherein R10 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- X is oxygen, sulfur, NR10, and mixtures thereof;
- xiii) —NR10C(X)NR10R11—, wherein R10 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- X is oxygen, sulfur, NR10, and mixtures thereof;
- xiv) —R11NR10C(X)NR10—, wherein R10 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- wherein X is oxygen, sulfur, NR10, and mixtures thereof;
- xv) —R11NR10C(X)NR10R11—, wherein R10 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- wherein X is oxygen, sulfur, NR10, and mixtures thereof;
- xvi) —NR10, wherein R10 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- xvii) —O—;
- xviii) —(R11)tC(X)(R11)t—;
- wherein R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- t is 0 or 1;
- X is oxygen, sulfur, NR10, and mixtures thereof;
- xix) —(R11)tOC(O)(R11)t—;
- wherein R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- t is 0 or 1;
- xx) —R11)tC(O)O(R11)t—;
- wherein R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- t is 0 or 1;
- xxi) alkyleneoxyalkylene having the formula:
- —(R12O)qR13—
- wherein R12 is C2-C6 linear or branched alkylene, substituted or unsubstituted phenylene;
- R13 is —(CH2)p—, wherein p is from 0 to 12;
- q is from 1 to 4;
- xxii) —S—;
- xxiii) —(R11)tS(R11)t—;
- wherein R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- t is 0 or 1;
- xxiv) —(R11)tS(O)(R11)t—;
- wherein R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- t is 0 or 1;
- xxv) —(R11)tSO2(R11)t—;
- wherein R11 is C1-C12 alkylene, substituted or unsubstituted phenylene, or mixtures thereof;
- t is 0 or 1;
- xxvi) or mixtures thereof;
- R9 is:
- i) hydrogen;
- ii) C1-C18 substituted or unsubstituted, linear or branched alkyl;
- iii) C3-C18 substituted or unsubstituted, linear or branched cycloalkyl
- iv) C2-C18 substituted or unsubstituted, linear or branched alkenyl;
- v) C2-C18 substituted or unsubstituted, linear or branched alkynyl;
- vi) C6-C18 substituted or unsubstituted aryl;
- vii) C2-C18 substituted or unsubstituted heterocyclic alkyl;
- viii) C3-C18 substituted or unsubstituted heterocyclic alkenyl;
- ix) —OH;
- x) —SO3M;
- xi) —OSO3M;
- xii) —NO2;
- xiii) halogen selected from fluorine, chlorine, bromine, iodine, or mixtures thereof;
- xiv) —C(Hal)3, wherein each Hal is fluorine, chlorine, bromine, iodine, or mixtures thereof;
- xv) —COR14;
- wherein R14 is hydrogen, —OH, C1-C12 alkyl, C1-C12 alkoxy, or mixtures thereof;
- —N(R15)2, or mixtures thereof;
- each R15 is independently hydrogen, —OH, C1-C4 alkyl, or mixtures thereof;
- xvi) —CH(OR14)2 wherein R14 is hydrogen, C1-C12 alkyl, or two R14 units can be taken together to form a ring having from 3 to 5 carbon atoms;
- or mixtures thereof;
- xvii) a unit having the formula:
- wherein R4 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R5 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R4 and R5 can be taken together to form a heterocyclic ring comprising from 3 to 5 carbon atoms;
- xviii) a unit having the formula:
- wherein R6 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R7 is hydrogen, C1-C4 alkyl, or mixtures thereof;
- R6 and R7 can be taken together to form a heterocyclic ring comprising from 3 to 5 carbon atoms;
- xix) —NHOR16, wherein R16 is hydrogen;
- C1-C12 linear or branched alkyl;
- acyl having the formula —COR17, wherein R17 is C1-C4 alkyl;
- or mixtures thereof;
- xx) a unit having the formula:
- —CH═NOR16
- wherein R16 is hydrogen;
- C1-C12 linear or branched alkyl;
- C7-C22 linear or branched alkylenearyl;
- acyl having the formula —COR17, R17 is C1-C4 alkyl;
- or mixtures thereof;
- xxi) an amino unit having the formula:
- —(CH2)mN(R3)2
- wherein each R3 is independently C1-C18 substituted or unsubstituted, linear or branched alkyl;
- m is from 0 to 10;
- xxii) a quaternary ammonium unit having the formula:
- wherein each R3 is independently C1-C18 substituted or unsubstituted, linear or branched alkyl;
- Y is an anion of sufficient charge to provide electronic neutrality;
- m is from 0 to 10;
- o) two R units on the same carbon atom can be taken together to form a carbonyl unit or carbonyl unit equivalent;
- and
- p) mixtures thereof;
- L is a linking group;
- [Poly] is a polymeric unit, i indicates the number of said heterocyclic units which comprise said conjugate and has the value of from 1 to 100;
- z is 0 or 1;
- and
- b) the balance carriers and adjunct ingredients.
Dependencies are inferred from the claim text.