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Details for Patent: 6,060,517

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Details for Patent: 6,060,517

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 R, 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, 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:Nov 12, 1998
Application Number:09/191,868
Claims:1. A polymer composition effective for removing bile salts by ion exchange comprising a therapeutic amount of the reaction product of:

(a) one or more crosslinked polymers comprising a repeat unit having the formula: ##STR24## where n and m are integer; R.sup.1, R.sup.2 and R.sup.3, independently are H or a C.sub.1 -C.sub.8 alkyl group; and

(b) at least one alkylating agent, said reaction product being non-toxic and stable once ingested.

2. A polymer of claim 1 wherein said polymer is reacted with at least two alkylating agents, one of said alkylating agents having the formula RX where R is a C.sub.4 -C.sub.20 alkyl group and X is one or more electrophilic leaving groups, and the other of said alkylating agents having the formula R.sup.1 X where R.sup.1 is a C.sub.1 -C.sub.20 alkyl ammonium group and X is one or more electrophilic leaving groups.

3. A polymer composition of claim 1 wherein said polymer is reacted at least two alkylating agents, one of said alkylating agents having the formula RX where R is a C.sub.1 -C.sub.20 alkyl group and X is one or more electrophilic leaving groups, and the other of said alkylating agents having the formula R.sup.1 X where R.sup.1 is a C.sub.1 -C.sub.20 hydroxyalkyl group and X is one or more electrophilic leaving groups.

4. A polymer composition of claim 1 wherein said polymer is reacted with at least two alkylating agents, one of said alkylating agents is a C.sub.1 -C.sub.20 dihaloalkane and the other of said alkylating agent is a C.sub.1 -C.sub.20 alkylammonium salt.
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