NEUE BENZOESAEUREDERIVATE, DIESE ENTHALTENDE ARZNEIMITTEL UND VERFAHREN ZUR HERSTELLUNG DIESER VERBINDUNGEN UND ARZNEIMITTEL

• Main Authors: KIESEWETTER,ERWIN,.DR, ZIMMER,OSWALD,.DR, VOLLENBERG,WERNER,.DR, SEIPP,ULRICH,.DR, K.H.,-BIO.LOSCHEN,GERRIET
• Format: Patent
• Language: German
• Published: 30.10.1986
• Edition: 4
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The benzoic acid derivatives according to the invention are specifically acting, adequately stable 5-lipoxygenase inhibitors and can be employed in particular in pharmaceutical preparations for the therapy of pathological conditions in which leukotrienes are involved as mediators. They correspond to the formula in which A and E represent -C IDENTICAL C- and B and D represent -CH2-CH2- or A, B and D in each case represent -C IDENTICAL C- or cis-CH=CH- and E represents trans-CH=CH-, R1 is hydrogen, methyl or ethyl, R2 represents hydrogen, an alkyl or phenyl radical optionally substituted as defined or a cycloalkyl radical, R3 represents hydrogen, acetyl or propionyl and R4 represents a carboxyl group or a functional derivative thereof, such as a salt, an ester, an amide or a hydroxamic acid, or represents a nitrile group. The compounds of the formula I are in particular prepared according to the invention by synthesis of the aliphatic chain starting from suitable acetylene compounds. The radical R4 can then be converted into other desired carboxyl group derivatives. A, B, D and E can be varied within the context of the definition by partial or complete hydrogenation.