Patent number: 8198271
Abstract: A compound having the following formula (1) or a salt thereof: wherein R1 and R2 represent hydrogen, a lower alkyl, a lower alkenyl, a lower alkynyl or a group having the following formula (2): (R6)n—{circle around (A)}—Z—??(2), R3 represents hydroxy, a lower alkoxy, a lower cycloalkyloxy, an aryloxy, carboxy, a lower alkoxycarbonyl, or —NRaRb having the following formula (3): (R7)o—{circle around (B)}—??(3), R4 and R5 represent halogen, a lower alkyl, hydroxy, or a lower alkoxy; R6 represents halogen, a lower alkyl, an aryl group, a heterocyclic, a hydroxy, a lower alkoxy, mercapto, a lower alkylthio, a lower alkylcarbonyl, amino, nitro or cyano; R7 represents a lower alkyl, hydroxy or a lower alkoxy; Ra and Rb represent hydrogen or a lower alkyl; the ring A represents a cyclic hydrocarbon or a heterocyclic ring; the ring B represents a heterocyclic ring having one or more heteroatoms selected from the group consisting of nitrogen and oxygen; X represents a lower alkylene; Y represents a lower alkyle
Type:
Grant
Filed:
May 25, 2009
Date of Patent:
June 12, 2012
Assignee:
Santen Pharmaceutical Co., Ltd.
Inventors:
Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
Publication number: 20120101080
Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.
Type:
Application
Filed:
June 25, 2010
Publication date:
April 26, 2012
Applicant:
BioVersys AG
Inventors:
Ronald Schoenmakers, Wilfried Weber, Marc Gitzinger, Martin Fussenegger, Marcel Tigges, Peter Schneider