IP Library › Patent Application 12842990
Patent Application
App. No. 12/842,990

PHARMACEUTICAL DRUG CANDIDATES AND METHODS FOR PREPARATION THEREOF

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Quick Facts
Patent No.
US None
App. No.
12/842,990
Abstract

The present invention is directed to methods of preparation of sulfonate derivatized compounds, e.g., 3-amino-1-propanesulfonic acid and 1,3-propanedisulfonic acid disodium salt with increased purity, with reduced potential for toxic by-products, and that are pharmaceutically useful, e.g., for the treatment of amyloidosis.

Claims (23)

1 - 184 . (canceled)

185 . A purity-enhanced pharmaceutical drug candidate comprising:

1,3-propanedisulfonic acid or a salt thereof, wherein the pharmaceutical drug candidate is free of bromide.

186 . A purity-enhanced pharmaceutical drug candidate comprising:

1,3-propanedisulfonic acid or a salt thereof, wherein the pharmaceutical drug candidate is free of sodium.

187 . A purity-enhanced pharmaceutical drug candidate comprising:

1,3-propanedisulfonic acid or a salt thereof, wherein the sulfate content is less than 1.4%.

188 . The purity-enhanced pharmaceutical drug candidate of claim 187 , wherein the sulfate content is less than 1.0%.

189 . The purity-enhanced pharmaceutical drug candidate of claim 187 , wherein the sulfate content is less than 0.9%.

190 . The purity-enhanced pharmaceutical drug candidate of claim 187 , wherein the sulfate content is less than 0.8%.

191 . The purity-enhanced pharmaceutical drug candidate of claim 187 , wherein the sulfate 5 content is less than 0.7%.

192 . The purity-enhanced pharmaceutical drug candidate of claim 187 , wherein the sulfate content is less than 0.6° A.

193 . The purity-enhanced pharmaceutical drug candidate of claim 187 , wherein the sulfate content is less than 0.5%.

194 . The purity-enhanced pharmaceutical drug candidate of claim 187 , wherein the sulfate content is less than 0.4%.

195 . The purity-enhanced pharmaceutical drug candidate of claim 187 , wherein the sulfate content is less than 0.3%.

196 . The purity-enhanced pharmaceutical drug candidate of claim 187 , wherein the sulfate content is less than 0.2%.

197 . The purity-enhanced pharmaceutical drug candidate of claim 187 , wherein the sulfate content is less than 0.1%.

198 . The purity-enhanced pharmaceutical drug candidate of claim 187 , wherein the sulfate content is less than 0.05%.

199 . A purity-enhanced pharmaceutical drug candidate comprising:

1,3-propanedisulfonic acid or a salt thereof, wherein the pharmaceutical drug candidate is free of at least one of the by-products selected from the group consisting of 1,3-propanediol, 3-bromo-propan-1-ol, 1,3-dibromopropane, and 3-bromo-propanesulfonate.

200 . The purity-enhanced pharmaceutical drug candidate of claim 199 , wherein the pharmaceutical drug candidate is free of at least two of the by-products selected from the group consisting of 1,3-propanediol, 3-bromo-propan-1-ol, 1,3-dibromopropane, and 3-bromo-propanesulfonate.

201 . The purity-enhanced pharmaceutical drug candidate of claim 199 , wherein the pharmaceutical drug candidate is free of at least three of the by-products selected from the group consisting of 1,3-propanediol, 3-bromo-propan-1-ol, 1,3-dibromopropane, and 3-bromo-propanesulfonate.

202 . The purity-enhanced pharmaceutical drug candidate of claim 199 , wherein the pharmaceutical drug candidate is free of the four by-products selected from the group consisting of 1,3-propanediol, 3-bromo-propan-1-ol, 1,3-dibromopropane, and 3-bromo-propanesulfonate.