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Last Updated: November 28, 2020

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Claims for Patent: 7,119,093

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Summary for Patent: 7,119,093
Title:3-Z-[1-(4-(N-((4-Methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-an- ilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulpho- nate and the use thereof as a pharmaceutical composition
Abstract: The present invention relates to the compound 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-a- nilino)-1-phenyl-methylene]-6-methoxycabonyl-2-indolinone-monoethanesulpho- nate of formula I and the use thereof as a pharmaceutical composition ##STR00001##
Inventor(s): Roth; Gerald J. (Biberach, DE), Linz; Guenter (Mittelbiberach, DE), Sieger; Peter (Mittelbiberach, DE), Rall; Werner (Mittelbiberach, DE), Hilberg; Frank (Wien, AT), Bock; Thomas (Biberach, DE)
Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG (Ingelheim, DE)
Application Number:10/623,971
Patent Claims: 1. 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino- )-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesu- lphonate.

2. 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino- )-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesu- lphonate hemihydrate in crystalline form, having a melting point of T.sub.m.p.=305.+-.5.degree. C. (determined by DSC; evaluation using peak-maximum; heating rate: 10.degree. C./min).

3. Crystalline 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-a- nilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulph- onate hemihydrate according to claim 2, the X-ray powder diagram of which includes, inter alia, the characteristic values d=5.43 .ANG., 5.08 .ANG., 4.71 .ANG., 4.50 .ANG. and 4.43 .ANG. with an intensity of more than 40%.

4. Crystalline 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-a- nilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulph- onate hemihydrate according to claim 2, characterised by a unit cell determined by X-ray powder diffractometric measurements having the following dimensions: a=16.332 .ANG., b=19.199 .ANG., c=11.503 .ANG., .alpha.=95.27.degree., .beta.=90.13.degree., .gamma.=110.83.degree. and V=3354.4 .ANG..sup.3.

5. A pharmaceutical composition comprising 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-a- nilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulph- onate and one or more inert carriers and/or diluents.

6. A prodrug of 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-a- nilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulph- onate.

7. 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino- )-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesu- lphonate hemihydrate in crystalline form.

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