Abstract

The invention relates to a crystalline polymorphic form I, II and III of marimastat, a mixture of the crystalline polymorphic form I and III of marimastat, an amorphous form of marimastat, and processes for their preparation. The invention further relates to a pharmaceutical composition comprising the crystalline polymorphic form I, II or III of marimastat, the mixture of the crystalline polymorphic form I and III of marimastat, the amorphous form of marimastat or a mixture thereof. The invention also relates to the pharmaceutical composition, the crystalline polymorphic form I, II or III of marimastat, the mixture of the crystalline polymorphic form I and III of marimastat, the amorphous form of marimastat or a mixture thereof for use as a medicament, and for use in the prevention and treatment of diseases associated with hyperactivity of extracellular matrix metalloproteinases.

IPC Classes  ?

• C07C 237/12 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups

Abstract

The invention relates to a process for the preparation of marimastat. The invention further relates to marimastat prepared by the process, and a pharmaceutical composition comprising said marimastat. The invention also relates to the pharmaceutical composition for use as a medicament, and said marimastat for use as a medicament. The invention further relates to the pharmaceutical composition for use in the prevention and treatment of diseases associated with hyperactivity of extracellular matrix metalloproteinases, and said marimastat for use in the prevention and treatment of diseases associated with hyperactivity of extracellular matrix metalloproteinases.

IPC Classes  ?

• C07C 235/04 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
• A61K 9/20 - Pills, lozenges or tablets
• A61K 31/16 - Amides, e.g. hydroxamic acids
• C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
• C07C 231/10 - Preparation of carboxylic acid amides from compounds not provided for in groups
• C07C 231/24 - SeparationPurification

Abstract

The invention relates to a process for the preparation of marimastat. The invention further relates to marimastat prepared by the process, and a pharmaceutical composition comprising said marimastat. The invention also relates to the pharmaceutical composition for use as a medicament, and said marimastat for use as a medicament. The invention further relates to the pharmaceutical composition for use in the prevention and treatment of diseases associated with hyperactivity of extracellular matrix metalloproteinases, and said marimastat for use in the prevention and treatment of diseases associated with hyperactivity of extracellular matrix metalloproteinases.

IPC Classes  ?

• C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
• C07D 317/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals