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Details for Patent: 5,703,188

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Details for Patent: 5,703,188

Title: Process for removing bile salts from a patient and compositions therefor
Abstract:A method for removing bile salts from a patient by ion exchange by administering to the patient a therapeutically effective amount of one or more highly crosslinked polymers characterized by a repeat unit having the formula ##STR1## or copolymer thereof, where n is an integer; R.sup.1 is H or a C.sub.1 -C.sub.8 alkyl group: M is ##STR2## Z is O, NR.sup.3, S, or (CH.sub.2).sub.m ; m=0-10; R.sup.3 is H or a C.sub.1 -C.sub.8 alkyl group; and R.sup.2 is ##STR3## where p=0-10, and each R.sup.4, R.sup.5, and R.sup.6, independently is H, a C.sub.1 -C.sub.8 alkyl group, or an aryl group.
Inventor(s): Mandeville, III; W. Harry (Lynnfield, MA), Holmes-Farley; Stephen Randall (Arlington, MA)
Assignee: GelTex Pharmaceuticals, Inc. (Waltham, MA)
Filing Date:Jun 07, 1995
Application Number:08/482,969
Claims:1. A method of synthesizing a crosslinked polymer having hydrophilic and hydrophobic units comprising: polymerizing a mixture comprising a hydrophilic vinylic monomer, a monoreactive hydrophobic vinylic co-monomer and a multifunctional crosslinking co-monomer in an alcoholic solvent under conditions suitable for free radical polymerization.

2. The claim 1 wherein the hydrophilic monomer has a formula ##STR25## where R.sup.1 is H or a C.sub.1 -C.sub.8 alkyl group; M is ##STR26## or --Z-- R.sup.2 ; Z is O, NR.sup.3, S, or (CH.sub.2).sub.m ; m=0-10; R.sup.3 is H-- or a C.sub.1 -C.sub.8 alkyl group; and R.sup.2 is ##STR27## where p=0-10, and each R.sup.4, R.sup.5, and R.sup.6, independently, is H, a C.sub.1 -C.sub.8 alkyl group, or an group.

3. The method of claim 2 wherein said monoreactive hydrophobic co-monomer is selected from the group consisting of styrene and fluorinated derivatives thereof; vinyl naphthalene and fluorinated derivatives thereof; ethyl vinylbenzene and fluorinated derivatives thereof; N-alkyl and N-aryl derivatives of acrylamide and methacrylamide, and fluorinated derivatives thereof; alkyl and aryl acrylates and fluorinated derivatives thereof; alkyl and aryl methacrylates and fluorinated derivatives thereof; 4-vinylbiphenyl and fluorinated derivatives thereof; 4-vinylanisole and fluorinated derivatives thereof; and 4-aminostyrene and fluorinated derivatives thereof.

4. The method of claim 2 wherein said multifunctional crosslinking co-monomer is present in an amount from about 0.5-25% by weight, based upon total monomer weight.

5. The method of claim 4 wherein said crosslinking co-monomer is present in an amount from about 1-10% by weight, based upon total monomer weight.

6. The method of claim 4 wherein said crosslinking co-monomer is selected from the group consisting of ethylene glycoldimethylacrylate, methylene bis methacrylamide, propylene glycoldimethyl acrylate or divinyl benzene.

7. The method of claim 2 further comprising one or more additional amine co-monomers.

8. The method of claim 7 wherein said amine co-monomer is vinyl pyridine, dimethylaminomethyl styrene, or vinyl imidazole.

9. The method of claim 2 wherein said hydrophilic monomer has a formula ##STR28## thereof wherein R.sup.1 and p are as defined in claim 2.

10. The method of claim 9 wherein said monoreactive hydrophobic co-monomer is n-butylmethacrylamide, hexafluorobutylmethacrylate, heptadecafluorodecylmethacrylate, styrene or a fluorinated derivative thereof, 2-vinyl naphthalene, 4-vinyl imidazole, vinyl pyridine, 4-vinylbiphenyl or a fluorinated derivative thereof, 4-vinylanisole or a fluorinated derivative thereof, or 4-aminostyrene or a fluorinated derivative thereof.

11. The method of claim 9 further comprising a hydrophilic monomer selected from the group consisting of trimethylammoniumethylmethacrylate and trimethylammoniumethylacrylate.

12. The method of claim 2 wherein said hydrophilic monomer has a formula ##STR29## wherein R.sup.1 and p are as defined in claim 2.

13. The method of claim 12 wherein said monoreactive hydrophobic co-monomer is isopropylacrylamide, styrene or a fluorinated derivative thereof or hexafluoroisopropylacrylate.

14. The method of claim 12 further comprising the hydrophilic monomer trimethylammoniumethylmethacrylate.

15. The method of claim 2 wherein said hydrophilic monomer has a formula ##STR30## wherein Z is NR.sup.3 or (CH.sub.2).sub.m, R.sup.2 is ##STR31## R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.6, m and p are as defined in claim 2.

16. The method of claim 15 wherein said monoreactive hydrophobic co-monomer is selected from the group consisting of styrene and fluorinated derivatives thereof; vinyl naphthalene and fluorinated derivatives thereof; ethyl vinylbenzene and fluorinated derivatives thereof; N-alkyl and N-aryl derivatives of acrylamide and methacrylamide, and fluorinated derivatives thereof; alkyl and aryl acrylates and fluorinated derivatives thereof; alkyl and aryl methacrylates and fluorinated derivatives thereof; 4-vinylbiphenyl and fluorinated derivatives thereof; 4-vinylanisole and fluorinated derivatives thereof; and 4-aminostyrene and fluorinated derivatives thereof.

17. A method of synthesizing a crosslinked polymer having hydrophilic and hydrophobic units comprising: polymerizing a mixture comprising a hydrophilic vinylic monomer, a monoreactive hydrophobic vinylic co-monomer and a multifunctional crosslinking co-monomer in an alcoholic solvent, under conditions suitable for free radical polymerization wherein said hydrophilic vinylic monomer has a repeat unit having the formula ##STR32## where R.sup.1 is H or a C.sub.1 -C.sub.8 alkyl group; L is --NH-- or ##STR33## G is ##STR34## and each R.sup.2, R.sup.3, independently, is H, a C.sub.1 -C.sub.8 alkyl group, or an aryl group.

18. The method of claim 17 wherein said multifunctional crosslinking co-monomer is present in an amount from about 0.5-25% by weight, based upon total monomer weight.

19. The method of claim 18 wherein said crosslinking co-monomer is present in an amount from about 1-10% by weight, based upon total monomer weight.

20. The method of claim 17 wherein said monoreactive hydrophobic monomer is selected from the group consisting of styrene and fluorinated derivatives thereof; vinyl naphthalene and fluorinated derivatives thereof; ethyl vinylbenzene and fluorinated derivatives thereof; N-alkyl and N-aryl derivatives of acrylamide and methacrylamide, and fluorinated derivatives thereof; alkyl and aryl acrylates and fluorinated derivatives thereof; alkyl and aryl methacrylates and fluorinated derivatives thereof; 4-vinylbiphenyl and fluorinated derivatives thereof; 4-vinylanisole and fluorinated derivatives thereof; and 4-aminostyrene and fluorinated derivatives thereof.

21. The method of claim 17 wherein said hydrophilic monomer has a formula ##STR35## wherein G is as defined in claim 17.

22. The method of claim 17 wherein said hydrophilic monomer has a formula ##STR36## wherein G is as defined in claim 17.

23. A method of synthesizing a crosslinked polymer having hydrophilic and hydrophobic units comprising: polymerizing a mixture comprising hydrophilic vinylic monomers, monoreactive hydrophobic vinylic co-monomers and a multifunctional crosslinking co-monomer in an alcoholic solvent, under conditions suitable for free radical polymerization wherein the alcoholic solvent is 2-propanol.
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