US2006258681A1PendingUtilityA1

3-Z-[1-(4-(N-((4-Methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate and the use thereof as a pharmaceutical composition

Individually held — no corporate assignee on recordPriority: Jul 24, 2002Filed: Jul 28, 2006Published: Nov 16, 2006

Est. expiryJul 24, 2022(expired)· nominal 20-yr term from priority

Inventors:Gerald Juergen Roth Guenter Linz Peter Sieger Werner Rall Frank Hilberg Thomas Bock

A61P 35/04A61P 35/00A61P 43/00C07D 209/34C07D 401/12

PatentIndex Score

Cited by

References

Claims

Abstract

The present invention relates to the compound 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate of formula I and the use thereof as a pharmaceutical composition.

Claims

exact text as granted — not AI-modified

1 . 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate.  
   
   
       2 . 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate in crystalline form, having a melting point of T m.p. =305±5° C. (determined by DSC; evaluation using peak-maximum; heating rate: 10° C./min).  
   
   
       3 . Crystalline 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate according to  claim 2 , the X-ray powder diagram of which includes, inter alia, the characteristic values d=5.43 Å, 5.08 Å, 4.71 Å, 4.50 Å and 4.43 Å with an intensity of more than 40%.  
   
   
       4 . Crystalline 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate according to  claim 2 , characterised by a unit cell determined by X-ray powder diffractometric measurements having the following dimensions: 
 a=16.332 Å,    b=19.199 Å,    c=11.503 Å,    α=95.27°,    β=90.13°,    γ=110.83° and    V=3354.4 Å 3      
   
   
       5 . Crystalline 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate according to one of  claims 2  to  4 , in the form of the hemihydrate.  
   
   
       6 . A pharmaceutical composition comprising 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate and one or more inert carriers and/or diluents.  
   
   
       7 . A metabolite of 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate.  
   
   
       8 . A prodrug of 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate.  
   
   
       9 . A method for treating excessive or abnormal cell proliferation which comprises administering a therapeutically effective amount of 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate.

Join the waitlist — get patent alerts

Track US2006258681A1 — get alerts on status changes and closely related new filings.

We store only your email — no account needed. See our privacy policy.