Method for removing bile salts from a patient with alkylated amine polymers
AssigneeGelTex Pharmaceuticals, Inc.
InventorsW. Harry Mandeville, III, Stephen Randall Holmes-Farley
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Abstract
A method for removing bile salts from a patient that includes administering to the patient a therapeutically effective amount of product produced by a process comprising alkylating one or more crosslinked amine polymers, salts or copolymers thereof with at least one alkylating agent. The reaction product is characterized in that: (i) at least some of the nitrogen atoms are unreacted with alkylating agent; and (ii) less than 10 mol% of the nitrogen atoms in the polymer react with the alkylating agent to form quaternary ammonium units.
Claims46
A method for removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of a product produced by a process comprising alkylating:
- a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit selected from the group consisting of:
- ##STR3##
- (NR--CH.sub.2 CH.sub.2 --NR--CH.sub.2 CH.sub.2 --NR--CH.sub.2 CHOH--CH.sub.2).sub.n ( 3)
- where n is a positive integer and each R, independently, is H or a C.sub.1 -C.sub.8 alkyl group with
- b) at least one aliphatic alkylating agent, said product characterized in that:
- (i) at least some of the nitrogen atoms in said repeat units are unreacted with said alkylating agent;
- and
- (ii) less than 10 mol% of the nitrogen atoms in said repeat units that react with said alkylating agent form quaternary ammonium units.
A method of removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of a product produced by a process comprising alkylating:
- a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit having the formula ##STR5## where n is a positive integer and each R, independently, is H or a C.sub.1 -C.sub.8 alkyl group with
- b) at least one alkylating agent, said product characterized in that:
- (i) at least some of the nitrogen atoms in said repeat units are unreacted with said alkylating agent;
- and
- (ii) less than 10 mol% of the nitrogen atoms in said repeat units that react with said alkylating agent form quaternary ammonium units.
A method of removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of a product produced by a process comprising alkylating:
- a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit having the formula ##STR6## where n is a positive integer and each R, independently, is H or a Cm-C.sub.s alkyl group with
- b) at least one aliphatic alkylating agent, said product characterized in that:
- (i) at least some of the nitrogen atoms in said repeat units are unreacted with said alkylating agent;
- and
- (ii) less than 10 mol% of the nitrogen atoms in said repeat units that react with said alkylating agent form quaternary ammonium units.
A method for removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of a product produced by a process comprising alkylating:
- a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit selected from the group consisting of:
- ##STR7## where n is a positive integer and each R, independently, is H or a C.sub.1 -C.sub.8 alkyl group with
- b) at least one aliphatic alkylating agent, said product characterized in that:
- (i) at least some of the nitrogen atoms in said repeat units are unreacted with said alkylating agent;
- (ii) less than 10 mol% of the nitrogen atoms in said repeat units that react with said alkylating agent form quaternary ammonium units;
- and
- (iii) said polymer is crosslinked by means of a multifunctional crosslinking agent, said agent being present in an amount from 1-10% by weight based upon the combined weight of monomer and crosslinking agent.
A method for removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of a product produced by a process comprising alkylating:
- a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit selected from the group consisting of:
- ##STR8##
- (NR--CH.sub.2 CH.sub.2 --NR--CH.sub.2 CH.sub.2 --NR--CH.sub.2 CHOH--CH.sub.2).sub.n ( 4)
- where n is a positive integer and each R, independently is H or a C.sub.1 -C.sub.8 alkyl group with
- b) at least one hydrophobic aliphatic alkylating agent, said product characterized in that:
- (i) at least some of the nitrogen atoms in said repeat units are unreacted with said alkylating agent:
- and
- (ii) less than 10 mol% of the nitrogen atoms in said repeat units that react with said alkylating agent form quaternary ammonium units.
A method for removing bile salts from a patient comprising administering to said patient a therapeutically effective amount of a product produced by a process comprising alkylating:
- a) one or more crosslinked polymers, salts or copolymers thereof characterized by a repeat unit selected from the group consisting of:
- ##STR9##
- (NR--CH.sub.2 CH.sub.2 --NR--CH.sub.3 CH.sub.2 --NR--CH.sub.2 CHOH--CH.sub.2).sub.n ( 4)
- where n is a positive integer and each R, independently, is H or a C.sub.1 -C.sub.8 alkyl group with
- b) at least one alkylating agent, having the formula RX wherein R is a C.sub.1 -C.sub.20 alkylammonium group and X is an electrophilic leaving group, said product characterized in that:
- (i) at least some of the nitrogen atoms in said repeat units are unreacted with said alkylating agent;
- and
- (ii) less than 10 mol% of the nitrogen atoms in said repeat units that react with said alkylating agent form quaternary ammonium units.
Dependencies are inferred from the claim text.