Claims for Patent: 5,136,014

Summary for Patent: 5,136,014

Title:	Hyperbranched polyesters
Abstract:	This invention relates to hyperbranched, functional polyesters prepared by self-condensation of AB.sub.n -type monomers wherein n is at least 2 and wherein B moieties contain a terminal carboxylic acid group or derivative thereof, wherein A or B is carboxyl or hydroxyl-terminated moiety which is an aromatic or aliphatic amino. The polyesters have utility as rheology modifiers or drug delivery vehicles.
Inventor(s):	Figuly; Garret D. (Wilmington, DE)
Assignee:	E. I. Du Pont de Nemours and Company (Wilmington, DE)
Application Number:	07/548,681
Patent Claims:	1. A soluble hyperbranched polyester having at least 1 branch per 10 monomer units prepared by conventional polycondensation of one or more monomers of the formula: wherein: R.sup.1 is a divalent C.sub.1-12 hydrocarbyl radical which is linear or branched aliphatic, alicyclic, aromatic or mixed aromatic-aliphatic; R.sup.2 is a C.sub.1-12 hydrocarbyl radical having a valence of (n+1), which radical is linear or branched aliphatic, alicyclic, aromatic or mixed aromatic-aliphatic, or R.sup.2 is R.sup.3 N wherein R.sup.3 is defined as for R.sup.1 ; either of R.sup.1, R.sup.2 or R.sup.3 optionally also containing substituents that are unreactive under processing conditions; X and Y are terminal functions selected from --CO.sub.2 R' and --OR" wherein R' is H or C.sub.1-12 alkyl and R" is H or OC(O)R; m is 0 or 1; and n is an integer and is at least 2; with the provisos that: (i) both X and Y are not --CO.sub.2 R' or --OR"; (ii) no X or Y function is adjacent to another X or Y function; (iii) when R.sup.2 is an aliphatic hydrocarbyl radical, Y is --CO.sub.2 R'; and (iv) when R.sup.2 is R.sup.3 N, m is 1. 2. The polyester of claim 1 wherein the molecular weight is at least 1500. 3. The polyester of claim 1 wherein R.sup.2 is linear or branched aliphatic or mixed aliphatic-aromatic radical and m is 1. 4. The polyester of claim 1 wherein R.sup.2 is R.sup.3 N. 5. The polyester of claim 4 wherein R.sup.3 is a linear or branched aliphatic radical containing 2 to 6 carbon atoms. 6. The polyester of claim 5 wherein R.sup.1 is --CH.sub.2 CH.sub.2 --. 7. The polyester of claim 4 wherein R.sup.3 is a mixed aliphatic-aromatic radical. 8. The polyester of claim 7 wherein R.sup.3 is --C.sub.6 H.sub.4 CH.sub.2 CH.sub.2 --. 9. The polyester of claim 1 wherein R.sup.2 is an aromatic radical and m is 0. 10. The polyester of claim 9 wherein R.sup.2 is 1,3,5-benzenetriyl. 11. The polyester of claim 3 wherein R.sup.2 is a mixed aliphatic-aromatic radical. 12. The polyester of claim 1 wherein R.sup.2 is 3,3-(bis-4-phenylene)-1-butyl. 13. The polyester of claim 12 wherein X is CO.sub.2 R'. 14. The polyester of claims, 8, 10 or 12 wherein the aromatic portion of R.sup.2 contains at least one substituent that is inert under processing conditions. 15. A copolymer consisting essentially of repeat units of one or more of the polyesters of claim 1 and repeat units of a comonomer selected from a polymerizable diol or dicarboxylic acid. 16. The copolymer of claim 15 wherein Y in the one or more polyesters is --OR" and the comonomer is a polymerizable dicarboxylic acid. 17. The copolymer of claim 15 wherein Y in the one or more polyesters is --CO.sub.2 R' and the comonomer is a polymerizable diol. 18. The copolymer of claim 16 wherein the comonomer is 1,1'-ferrocenedicarboxylic acid. 19. The copolymer of claim 16 wherein the comonomer is hemin. 20. A copolymer consisting essentially of repeat units of one or more soluble hyperbranched polyesters having at least 1 branch per 10 monomer units prepared by conventional polycondensation of one or more monomers of the formula wherein: R.sup.1 is a divalent C.sub.1-12 hydrocarbyl radical which is linear or branched aliphatic, alicyclic, aromatic or mixed aromatic-aliphatic; R.sup.2 is a C.sub.1-12 hydrocarbyl radical having a valence of (n+1), which radical is linear or branched aliphatic; either of R.sup.1 or R.sup.2 optionally also containing substituents that are unreactive under processing conditions; X is CO.sub.2 R', Y is OR", wherein R' is H or C.sub.1-12 alkyl and R" is H or OC(O)R'; m is 0 or 1; and n is an integer and is at least 2; with the proviso that no X or Y function is adjacent to another X or Y function, and repeat units of a comonomer selected from a polymerizable diol or dicarboxylic acid. 21. The copolymer of claim 20 wherein the comonomer is a polymerizable dicarboxylic acid. 22. The copolymer of claim 21 wherein in the one or more hyperbranched polyesters m is 1, n is 2, R.sup.1 is --CH.sub.2 --and R.sup.2 is 1,1,1-ethanetriyl. 23. The copolymer of claim 22 wherein the comonomer is 1,1'-ferrocenedicarboxylic acid. 24. The copolymer of claim 22 wherein the comonomer is hemin. 25. The polyester of claim 24 wherein the X and Y functions have been capped with an aliphatic anhydride or acyl chloride. 26. A copolymer consisting essentially of repeat units of one or more of the polyesters of claim 24 and repeat units of a comonomer selected from a polymerizable diol or dicarboxylic acid.

Details for Patent 5,136,014

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Recordati Rare Diseases, Inc.	PANHEMATIN	hemin for injection	For Injection	101246	07/20/1983		2040-01-28