Otsuka Pharmaceutical Company, Limited

Hiroyuki Hashizume

Makoto Matsumoto

Hirofumi Sasaki

Hidetsugu Tsubouchi

Yoshikazu Haraguchi

Motohiro Itotani

Masanori Kawasaki

Tatsuo Tomishige

Shin Miyamura

Kuninori Tai

Isao Takemura

Takumi Sumida

Takeshi Hasegawa

Hiroshi Shimizu

Takeshi Kuroda

Hideaki Kuroda

Takayuki Matsuzaki

Makoto Komatsu

Yoshikazu Kawano

Kinue Ohguro

Yukitaka Uematsu

Miki Matsuba

Kazuho Kohashi

Yuji Seike

Kazuho Tanaka

Yoshihiko Shimokawa

Xiuhao Chen

Izuru Nakamura

Mikayo Hayashi

Hiromi Yata

The present invention provides a novel 6,7-dihydroimidazo[2,1-b][1,3]oxazine compound that has excellent bactericidal action against tubercle bacilli, multidrug-resistant tubercle bacilli, and atypical acid-fast bacilli. Specifically, the present invention provides a compound represented by Formula (1): or a salt thereof,

6,7-dihydroimidazo [2,1-b] [1,3]oxazine bactericides

The present invention provides antituberculous therapeutic drugs with a higher potency. The present invention provides also antituberculous therapeutic drugs containing oxazole compounds represented by (I) general formula (1): [wherein Rrepresents a hydrogen atom or C1-6 alkyl group, n represents an integer of 0-6, and Rrepresents general formula (A) or the like, wherein Rrepresents a phenoxy group (at least one group selected from the group consisting of a halogen atom, an optionally halogen-substituted C1-6 alkyl group and an optionally halogen-substituted C1-6 alkoxy group may be substituted on the phenyl ring) or the like], optically active forms thereof or salts thereof, and drugs (II) such as primary antituberculous drugs. 

Antituberculous composition comprising oxazole compounds

The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and &#x2014;(CH2)nR2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30) and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against, multi-drug-resistant, and atypical acid-fast bacteria. 

2,3-dihydro-6-nitroimidazo (2,1-b) oxazole compounds for the treatment of tuberculosis

The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: wherein Rrepresents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, Rrepresents a group &#x2014;ORor the like, and Rrepresents a hydrogen atom, C1-C6 alkyl group or the like, or Rand &#x2014;(CH)Rmay bind to each other together with carbon atoms adjacent thereto through nitrogen atoms so as to form a spiro ring represented by the general formula (H): wherein Ris hydrogen, C1-C6 alkyl group or the like. The present compound has an excellent bactericidal action against, multi-drug-resistant, and atypical acid-fast bacteria.

2,3-dihydro-6-nitroimidazo[2,1-b]oxazoles

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Naruto, Japan

Hiroyuki Hashizume