Otsuka Pharmaceutical Company, Limited

Yoshikazu Haraguchi

Makoto Matsumoto

Hidetsugu Tsubouchi

Motohiro Itotani

Isao Takemura

Hiroshi Shimizu

Hirofumi Sasaki

Hiroyuki Hashizume

Yoshikazu Kawano

Yukitaka Uematsu

Naoto Utsumi

Shin Miyamura

Koichi Shinhama

Kuninori Tai

Satoshi Hayakawa

Shinichi Taira

Takumi Sumida

Yoshihisa Tanada

Norimitsu Hariguchi

Masanori Kawasaki

Takeshi Hasegawa

Nobuhisa Fujita

Kimiyoshi Annaka

Shunpei Ishikawa

Toshio Shinohara

Yuya Nakai

Tatsuo Tomishige

Yohei Hayashi

Takuya Furuta

Takeshi Kuroda

Hideaki Kuroda

Takayuki Matsuzaki

Atsunori Kaneshige

Makoto Komatsu

Kinue Ohguro

Miki Matsuba

Kazuho Tanaka

Yuji Seike

Hiromi Yata

Kazuho Kohashi

Mikayo Hayashi

Izuru Nakamura

Xiuhao Chen

Hiroyuki; Daiaparesu 1401 Hashizume

Takeshi; Daiichiaijitsuhaitsu 607 Hasegawa

Shin; 147-13 Mukaininokoshi Miyamura

It is an object of the present invention to provide a compound having an excellent antibacterial activity against tuberculosis bacteria, multidrug-resistant tuberculosis bacteria and/or non-tuberculous mycobacteria. Disclosed is a compound of the general formula (1): wherein each symbol is defined as described in the attached specification, or a salt thereof.

Heterobicyclic compounds and their use for the treatment of tuberculosis

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 a novel intermediate for manufacturing a 2,3-dihydroimidazo[2,1-b]oxazole compound with a high yield and a high purity, and a manufacturing method of the intermediate. The present invention provides an epoxy compound represented by the general formula (2): wherein, R1 represents a hydrogen or a lower alkyl group; and R2 represents a piperidyl group represented by the general formula (A1): (wherein, R3 represents a phenoxy group having a halogen-substituted lower alkoxy group substituted on a phenyl group, and the like) and the like; and n represents an integer of 1 to 6, a manufacturing method of the epoxy compound, and a manufacturing method of an oxazole compound using the epoxy method.

Epoxy compound and method for manufacturing the same

The present invention provides a novel intermediate for manufacturing a 2,3-dihydroimidazo[2,1-b]oxazole compound with a high yield and a high purity, and a manufacturing method of the intermediate. The present invention provides an epoxy compound represented by the general formula (2): wherein, R1 represents hydrogen or a lower alkyl group; and R2 represents a piperidyl group represented by the general formula (A1): (wherein, R3 represents a phenoxy group having a halogen-substituted lower alkoxy group substituted on a phenyl group, and the like) and the like; and n represents an integer of 1 to 6, a manufacturing method of the epoxy compound, and a manufacturing method of an oxazole compound using the epoxy compound. 

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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Tokushima, Japan

Yoshikazu Haraguchi