	US 7,608,674 B2
	Pharmaceutical compositions comprising cross-linked small molecule amine polymers
Eric Connor, Los Gatos, Calif. (US); Dominique Charmot, Campbell, Calif. (US); Han-Ting Chang, Livermore, Calif. (US); Florence Roger, Preverenges (Switzerland); Gerrit Klaerner, Los Gatos, Calif. (US); Son Hoai Nguyen, San Jose, Calif. (US); Jonathan Mills, San Jose, Calif. (US); Jerry M. Buysse, Los Altos, Calif. (US); Angela Lee, San Jose, Calif. (US); Deidre Madsen, Sunnyvale, Calif. (US); Jun Shao, Fremont, Calif. (US); Michael J. Cope, Berkeley, Calif. (US); and John Fordtran, Dallas, Tex. (US)
Assigned to Ilypsa, Inc., Thousand Oaks, Calif. (US)
Filed on Nov. 03, 2004, as Appl. No. 10/980,991.
Application 10/980991 is a continuation in part of application No. 10/965044, filed on Oct. 13, 2004.
Application 10/965044 is a continuation in part of application No. 10/806495, filed on Mar. 22, 2004.
Application 10/806495 is a continuation in part of application No. 10/701385, filed on Nov. 03, 2003.
Prior Publication US 2005/0147580 A1, Jul. 07, 2005
Int. Cl. C11D 1/00 (2006.01); C08F 26/06 (2006.01)

U.S. Cl. 526—310 [526/258; 525/334; 424/78.06; 424/78.11; 424/78.12; 424/78.16]

49 Claims

1. A pharmaceutical composition comprising a particulate crosslinked amine polymer as an active ingredient and a pharmaceutically acceptable excipient, the particulate crosslinked amine polymer particles having a chloride content of less than about 20 mol % of the amine group content and a size in the range of 5 to 500 microns, the crosslinked amine polymer comprising repeat units derived from polymerization of a non- polymeric amine and a crosslinking agent such that the polymer has a swelling ratio of less than about 5 as measured in a physiological medium, the non-polymeric amine being selected from the group consisting of

(i) a non-polymeric amine of formula (I)

wherein each n, independently, is equal to or greater than 3; m is equal to or greater than 1; and each R_1,independently, is H or optionally substituted alkyl or aryl or is linked to a neighboring R₁to form an optionally substituted alicyclic, aromatic, or heterocyclic group; provided the non-polymeric amine of formula I is not 1,3-diaminopropane, and

(ii) a non-polymeric amine of formula (IV)

wherein each n, independently, is equal to or greater than 3; each r, independently, is 0, 1, or 2; and each R₁, independently, is H or optionally substituted alkyl or aryl or is linked to a neighboring R₁to form an optionally substituted alicyclic, aromatic, or heterocyclic group.