SULFONAMIDE DERIVATIVE AND MEDICINAL USE THEREOF

FIELD: chemistry.SUBSTANCE: invention relates to a novel sulfonamide derivative of general formula (1) and a pharmaceutically acceptable salt thereof. Compounds have an inhibitory effect on α4-integrin with high selectivity with a weak effect on α4β1 and a strong effect on α4β7. In general formula (...

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Hauptverfasser: TAKANOKHASI Tosiyuki, YAMAMOTO Takasi, ARISAKA Kharumi, UENO Khirokadzu, SINKAI Kendzi, MIYADZAVA Tomoko
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: chemistry.SUBSTANCE: invention relates to a novel sulfonamide derivative of general formula (1) and a pharmaceutically acceptable salt thereof. Compounds have an inhibitory effect on α4-integrin with high selectivity with a weak effect on α4β1 and a strong effect on α4β7. In general formula (1)A represents a group represented by the general formula (2-1), (2-2) or (2-4),, where Arm is a phenyl group, a pyridyl group or a pyrimidyl group, Ris a lower alkyl group, R, Rand Reach independently represents any of the following fragments: a hydrogen atom, a lower alkoxy group and a lower alkylamino-lower alkyl group, and when A represents a group represented by the general formula (2-1) or (2-4), R, R, R, R, Rand Reach independently represents any of the following fragments: a hydrogen atom, a lower alkyl group and a halo-lower alkyl group, B is any of the following: (a) a hydroxyl group, (b) -O-Rx, wherein Rx is a 6-membered heterocyclic group containing an oxygen atom or a nitrogen atom, optionally substituted with a lower alkyl group, (c) a hydroxyamino group, (d) CCalkoxyamino group or (e) an alkoxy group having from 1 to 10 carbon atoms, optionally substituted with a substituent selected from the group consisting of (e-1) alkyl group having from 1 to 10 carbon atoms, (e-2) halogen atom, (e-3) 6-membered heterocyclic group containing an oxygen atom or a nitrogen atom as a heteroatom, and (e-4) a lower alkoxy group, Rrepresents a hydrogen atom,a, b, c and d are independently C-R, C-R, C-Ror C-Rrespectively, where R, R, Rand Reach independently represents any of the following fragments: a hydrogen atom, a halogen atom, one of g and e is N and the other is CH, or both g and e are CH, f and h are independently C-Ror C-Rrespectively, where Rand Reach independently represents any of the following fragments: a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group and a nitro group, D represents a phenyl group, optionally having a substituent selected from the group consisting of the following substituents: a lower alkyl group, or D is a 6-membered heterocyclic group containing 1 to 2 ring heteroatoms selected from a nitrogen atom, and optionally substituted with a substituent selected from the group consisting of a lower alkyl group, when A represents a group represented by general formula (2-1) or (2-2), E represents a 5- or 6-membered heterocyclic group containing 1 to 3 nitrogen atoms or an oxygen atom, wherein the 5- or 6-membered heter