`
`Some information about SPM 8224
`
`1. The formation of a salt (with SPM 8224) has been tried with the following acids
`
`Organic acids
`
`aceturic acid
`acclylsalicylic acid
`L-alaninc
`L-(_+)-ascorbic acid
`
`L-aspartic acid
`bcnzoic acid
`citric acid
`B-cyclodcxtrin
`fumaric acid
`rallic acid
`
`glycine hydrochloride
`hippuric acid
`4-hydroxybcnzoic acid
`4-h drox cimiamic acid
`
`isobutyric acid
`malcic acid
`L—(_—)—rnalic acid
`D,L-malic acid
`(+)-mandclic acid
`mclhaiicsulfonic acid
`
`gluconic acid
`D-glucuronic acid
`
`orotic acid
`oxalic acid
`
`palmitic acid
`phlorclinic acid
`phlhalic acid
`roionic acid
`
`_Eyruvic acid
`salicylic acid
`sorbic acid
`stcaric acid
`succinic acid
`sulhanilic acid
`
`(_+)—ta1‘taric acid
`vanillic acid
`
`Inorganic acids
`
`hydrobromic acid (48%)
`hydrochloric acid (in diclhyl clhcr)
`hydrogen sulfate (96%)
`nitric acid (65 %)
`
`Metal complex
`
`magnesium sulfate
`zinc chloride
`
`2. Solubility of SPM 8224
`
`Solublc in acclonc, 2-bulanonc, diclhyl clhcr, mclhylcnc chloridc, cliloroform, tclrahydrofuranc
`insoluble in water
`
`DATE
`
`l111‘or11ia1io11abou1
`SPM 8224 & SPM 8272
`
`Page 1 /2
`
`RESTRICTED CONFIDENTIAL — SUBJECT TO PROTECTIVE ORDER
`
`UCB00O3439i"
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2100 - 0001
`
`
`
`CONFIDENTIAL
`
`Some information about SPM 8272
`
`1. Solubility of SPM 8272
`Soluble in acetone, aeetonitrilc, 2—butanonc, chloroform, water
`
`2. Different solvent—systems for the crystallization of SPM 8272
`
`a)
`
`b)
`
`c)
`
`solved in 2—butanone
`and mixed with butyl acetate, cyclohexane, diethyl ether. ethyl acetate. heptane, isobutyl acetate,
`isopropyl acetate, methyl tcrt.-butyl ether, propyl acetate or toluene
`solved in acetone
`and mixed with butyl acetate, cyelohcxane, diethyl ether. ethyl acetate, isobutyl acetate, isopropyl
`acetate, methyl tert_-butyl ether or propyl acetate
`solved in aeetonitrile
`and mixed with butyl acetate, diethyl ether, ethyl acetate or propyl acetate
`
`no crystallization after
`a)
`solving in acetonitrile
`and mixing with benzene, isobutyl acetate, isopropyl acetate, methyl tert.-butyl ether or toluene
`solving in acetone
`and mixing with benzene or toluene
`
`b)
`
`3. Residual solvents after the crystallization and drying of SPM 8272
`
`Residual solvents 2-butanone
`
`0.34 “o 2-butanone
`0.32 “/0 acetone
`
`0.10 "/0 cyclohcxane
`0.27 % eth 1 acetate
`
`ace-tone
`
`cyclohcxanc
`eth l acetate
`
`acetone
`acetone
`acetone
`
`butyl acetate
`I isopropyl acetate
`Ipropyl acetate
`
`0.36 "a acetone
`l 0.37 % acetone
`l 0.36 % acetone
`
`0.17 % butyl acetate
`l 0.18 "o isopropyl acetate
`l 0.22 % propyl acetate
`
`List of desired salts of SPM 8224 with the followin or anic and inor anic acids
`
`acetic acid
`citric acid
`maleic acid
`
`(+)-tartaric acid
`
`hydrogen sulphate
`ortho phosphoric acid
`
`DATE
`
`lnt‘orniation about
`SPM 8224 & SPM 8272
`
`Page 2 /2
`
`RESTRICTED CONFIDENTIAL — SUBJECT TO PROTECTIVE ORDER
`
`UCB00O34398
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2100 - 0002
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