# US 11,078,220 B2 · High-purity large-scale preparation of stannsoporfin > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,078,220 B2 - Document ID: US11078220B2 - Status: Granted - Kind: B2 - Application number: 16/864,510 - Filed: 2020-05-01 - Published: 2020-08-13 - Granted: 2021-08-03 - Earliest claimed: 2006-10-04 - Assignees: Mallinckrodt Hospital Products IP Limited - Applicants: Mallinckrodt Hospital Products IP Limited - Inventors: George S. Drummond; Robert Caroselli; Keith A. Cooke; Daniel Levin; David G. Roe; Christopher P. Boucher - Web page: https://patentgrep.com/patent/US11078220B2 ## CPC - C07F 7/2284: {Compounds with one or more Sn-N linkages} - A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)} - A61K 31/555: containing heavy metals, e.g. hemin, hematin, melarsoprol - A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics - A61P 7/00: Drugs for disorders of the blood or the extracellular fluid - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - C07D 487/22: in which the condensed system contains four or more hetero rings - C07F 7/003: {without C-Metal linkages} - C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22) - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08) ## Abstract Large scale (bulk) compositions comprising high-purity stannsoporfin are disclosed, as well as methods of synthesizing such compositions. ## Claims ### Claim 1 A composition comprising stannsoporfin, wherein the stannsoporfin is at least about 97% pure, and wherein any individual impurity is present in an amount less than about 0.08%, the stannsoporfin formed by: a) contacting a solution or suspension of tin (II) oxide with a mesoporphyrin IX or salt thereof under conditions suitable to form a crude stannsoporfin; and b) purifying the crude stannsoporfin to form the stannsoporfin. ### Claim 2 (depends on 1) The composition of claim 1, wherein the composition comprises palladium in an amount of less than about 20 ppm. ### Claim 3 (depends on 1) The composition of claim 1, wherein the composition comprises palladium in an amount of less than about 10 ppm. ### Claim 4 (depends on 1) The composition of claim 1, wherein the composition comprises at least about 10 grams of stannsoporfin. ### Claim 5 (depends on 1) The composition of claim 1, wherein the composition comprises at least about 100 grams of stannsoporfin. ### Claim 6 (depends on 1) The composition of claim 1, wherein the stannsoporfin is a single-batch preparation of stannsoporfin. ### Claim 7 (depends on 1) The composition of claim 1, wherein the stannsoporfin is at least about 98.5% pure. ### Claim 8 (depends on 1) The composition of claim 1, wherein any impurity present is present in an amount of about 0.07% or less. ### Claim 9 (depends on 1) The composition of claim 1, wherein the purifying the crude stannsoporfin comprises a hot acid trituration, followed by treatment at high pH at or above pH 9 followed by re-acidification, and subsequent hot acid trituration. ### Claim 10 (depends on 1) The composition of claim 1, wherein the mesoporphyrin IX of salt thereof is formed by contacting hemin with a pre-hydrogenated catalyst. ### Claim 11 (depends on 10) The composition of claim 10, wherein the pre-hydrogenated catalyst is formed by exposing a metallic hydrogenation catalyst to a hydrogen atmosphere. ### Claim 12 (depends on 1) The composition of claim 1, wherein the mesoporphyrin IX or salt thereof comprises mesoporphyrin IX dihydrochloride. ### Claim 13 (depends on 1) The composition of claim 1, wherein the composition further comprises at least one impurity in an amount between about 0.05% and about 0.08%, the at least one impurity having a relative retention time of 0.72-0.73 in an HPLC analysis. ### Claim 14 A composition comprising stannsoporfin, wherein the stannsoporfin is at least about 97% pure, and wherein any individual impurity is present in an amount less than about 0.08%, the stannsoporfin formed by: a) exposing a metallic hydrogenation catalyst to a hydrogen atmosphere to form a pre-hydrogenated catalyst; b) contacting hemin with the pre-hydrogenated catalyst to form a mesoporphyrin IX or salt thereof; c) contacting a solution or suspension of tin (II) oxide with the mesoporphyrin IX or salt thereof under conditions suitable to form a crude stannsoporfin; and d) purifying the crude stannsoporfin via hot acid trituration, followed by treatment at high pH at or above pH 9 followed by re-acidification, and subsequent hot acid trituration to form the stannsoporfin. ### Claim 15 (depends on 14) The composition of claim 14, wherein the metallic hydrogenation catalyst comprises palladium on carbon. ### Claim 16 (depends on 14) The composition of claim 14, wherein the mesoporphyrin IX or salt thereof comprises mesoporphyrin IX dihydrochloride. ### Claim 17 (depends on 14) The composition of claim 14, wherein the composition comprises palladium in an amount of less than about 20 ppm. ### Claim 18 (depends on 14) The composition of claim 14, wherein the composition comprises palladium in an amount of less than about 10 ppm. ### Claim 19 (depends on 14) The composition of claim 14, wherein the composition comprises at least about 10 grams of stannsoporfin. ### Claim 20 (depends on 14) The composition of claim 14, wherein the stannsoporfin is at least about 98.5% pure.