公开(公告)号：US07262212B2

公开(公告)日：2007-08-28

申请号：US10530429

申请日：2003-10-10

申请人： Hidetsugu Tsubouchi ,  Hirofumi Sasaki ,  Hideaki Kuroda ,  Motohiro Itotani ,  Takeshi Hasegawa ,  Yoshikazu Haraguchi ,  Takeshi Kuroda ,  Takayuki Matsuzaki ,  Kuninori Tai ,  Makoto Komatsu ,  Makoto Matsumoto ,  Hiroyuki Hashizume ,  Tatsuo Tomishige ,  Yuji Seike ,  Masanori Kawasaki ,  Takumi Sumida ,  Shin Miyamura

发明人： Hidetsugu Tsubouchi ,  Hirofumi Sasaki ,  Hideaki Kuroda ,  Motohiro Itotani ,  Takeshi Hasegawa ,  Yoshikazu Haraguchi ,  Takeshi Kuroda ,  Takayuki Matsuzaki ,  Kuninori Tai ,  Makoto Komatsu ,  Makoto Matsumoto ,  Hiroyuki Hashizume ,  Tatsuo Tomishige ,  Yuji Seike ,  Masanori Kawasaki ,  Takumi Sumida ,  Shin Miyamura

IPC分类号： A61K31/424 ,  A61K31/438 ,  C07D498/04 ,  C07D401/14

CPC分类号： C07D498/04 ,  C07D498/20 ,  C07F7/0812

摘要： The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: wherein R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R2 represents a group —OR3 or the like, and R3 represents a hydrogen atom, C1-C6 alkyl group or the like, or R1 and —(CH2)nR2 may 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 R41 is hydrogen, C1-C6 alkyl group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.

摘要翻译： 本发明提供由下列通式表示的2,3-二氢-6-硝基咪唑并[2,1-b]恶唑化合物：其中R 1表示氢原子或C 1 -C 6烷基 ，n表示0〜6的整数，R 2表示基团-OR 3等，R 3表示氢原子 ，C 1 -C 6烷基等，或R 1和 - （CH 2）n R 2 R 2， 可以通过氮原子与与其相邻的碳原子彼此结合形成由通式（H）表示的螺环：其中R 41是氢，C 1 -C 6烷基或 喜欢。 本发明化合物对结核分枝杆菌，多药耐药结核分枝杆菌和非典型酸性抗菌细菌具有优异的杀菌作用。

公开(公告)号：US20080119478A1

公开(公告)日：2008-05-22

申请号：US10574597

申请日：2004-10-29

申请人： Hidetsugu Tsubouchi ,  Hirofumi Sasaki ,  Motohiro Itotani ,  Yoshikazu Haraguchi ,  Shin Miyamura ,  Makoto Matsumoto ,  Hiroyuki Hashizume ,  Tatsuo Tomishige ,  Masanori Kawasaki ,  Kinue Ohguro ,  Takumi Sumida ,  Takeshi Hasegawa ,  Kazuho Tanaka ,  Isao Takemura

发明人： Hidetsugu Tsubouchi ,  Hirofumi Sasaki ,  Motohiro Itotani ,  Yoshikazu Haraguchi ,  Shin Miyamura ,  Makoto Matsumoto ,  Hiroyuki Hashizume ,  Tatsuo Tomishige ,  Masanori Kawasaki ,  Kinue Ohguro ,  Takumi Sumida ,  Takeshi Hasegawa ,  Kazuho Tanaka ,  Isao Takemura

IPC分类号： A61K31/497 ,  A61K31/41 ,  A61K31/445 ,  C07D211/68 ,  C07D413/00 ,  C07D498/02 ,  C07D215/00 ,  A61P31/00 ,  A61K31/47

CPC分类号： C07D498/04

摘要： 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 —(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 Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.

摘要翻译： 本发明提供由上述通式（1）中的通式（1）表示的2,3-二氢-6-硝基咪唑并[2,1-b]恶唑化合物，R1表示氢原子或C1-C6 烷基，n表示0〜6的整数，R 1和 - （CH 2）n R 2可以与下述式（30）表示的螺环连同相邻的碳原子（在 式中，RRR表示哌啶环上可具有取代基的哌啶基），（30），R 2表示苯并噻唑氧基，喹啉氧基，吡啶氧基等。 本发明化合物对结核分枝杆菌，多药耐药结核分枝杆菌和非典型酸性抗菌细菌具有优异的杀菌作用。

公开(公告)号：US08163753B2

公开(公告)日：2012-04-24

申请号：US10574597

申请日：2004-10-29

申请人： Hidetsugu Tsubouchi ,  Hirofumi Sasaki ,  Motohiro Itotani ,  Yoshikazu Haraguchi ,  Shin Miyamura ,  Makoto Matsumoto ,  Hiroyuki Hashizume ,  Tatsuo Tomishige ,  Masanori Kawasaki ,  Kinue Ohguro ,  Takumi Sumida ,  Takeshi Hasegawa ,  Kazuho Tanaka ,  Isao Takemura

发明人： Hidetsugu Tsubouchi ,  Hirofumi Sasaki ,  Motohiro Itotani ,  Yoshikazu Haraguchi ,  Shin Miyamura ,  Makoto Matsumoto ,  Hiroyuki Hashizume ,  Tatsuo Tomishige ,  Masanori Kawasaki ,  Kinue Ohguro ,  Takumi Sumida ,  Takeshi Hasegawa ,  Kazuho Tanaka ,  Isao Takemura

IPC分类号： A61K31/497 ,  A61K31/47 ,  A61K31/445 ,  A61K31/42 ,  C07D419/06 ,  C07D215/04 ,  C07D213/72 ,  C07D498/04

CPC分类号： C07D498/04

摘要： 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 —(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 Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.

摘要翻译： 本发明提供由上述通式（1）中的通式（1）表示的2,3-二氢-6-硝基咪唑并[2,1-b]恶唑化合物，R1表示氢原子或C1-C6 烷基，n表示0〜6的整数，R1和 - （CH2）nR2可以与相邻的碳原子一起形成由下式（30）表示的螺环（在下式中，RRR表示哌啶基 其可以在哌啶环上具有取代基），（30），R 2表示苯并噻唑氧基，喹啉氧基，吡啶氧基等。 本发明化合物对结核分枝杆菌，多药耐药结核分枝杆菌和非典型酸性抗菌细菌具有优异的杀菌作用。

公开(公告)号：US20060094767A1

公开(公告)日：2006-05-04

申请号：US10530429

申请日：2003-10-10

申请人： Hidetsugu Tsubouchi ,  Hirofumi Sasaki ,  Hideaki Kuroda ,  Motohiro Itotani ,  Takeshi Hasegawa ,  Yoshikazu Haraguchi ,  Takeshi Kuroda ,  Takayuki Matsuzaki

发明人： Hidetsugu Tsubouchi ,  Hirofumi Sasaki ,  Hideaki Kuroda ,  Motohiro Itotani ,  Takeshi Hasegawa ,  Yoshikazu Haraguchi ,  Takeshi Kuroda ,  Takayuki Matsuzaki

IPC分类号： A61K31/424 ,  C07D491/02

CPC分类号： C07D498/04 ,  C07D498/20 ,  C07F7/0812

摘要： The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: wherein R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R2 represents a group —OR3 or the like, and R3 represents a hydrogen atom, C1-C6 alkyl group or the like, or R1 and —(CH2)nR2 may 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 R41 is hydrogen, C1-C6 alkyl group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.

摘要翻译： 本发明提供由以下通式表示的2,3-二氢-6-硝基咪唑并[2,1-b]恶唑化合物：其中R 1表示氢原子或C 1 -C 6烷基 ，n表示0〜6的整数，R 2表示基团-OR 3等，R 3表示氢原子 ，C 1 -C 6烷基等，或R 1和 - （CH 2）n R 2 R 2， 可以通过氮原子与与其相邻的碳原子彼此结合形成由通式（H）表示的螺环：其中R 41是氢，C 1 -C 6烷基或 喜欢。 本发明化合物对结核分枝杆菌，多药耐药结核分枝杆菌和非典型酸性抗菌细菌具有优异的杀菌作用。

公开(公告)号：US09051333B2

公开(公告)日：2015-06-09

申请号：US14111262

申请日：2012-04-13

申请人： Yoshikazu Kawano ,  Yoshikazu Haraguchi ,  Hirofumi Sasaki ,  Yukitaka Uematsu ,  Hidetsugu Tsubouchi ,  Hiromi Yata ,  Hiroshi Shimizu ,  Kazuho Kohashi ,  Motohiro Itotani ,  Kuninori Tai ,  Isao Takemura ,  Mikayo Hayashi ,  Hiroyuki Hashizume ,  Miki Matsuba ,  Izuru Nakamura ,  Xiuhao Chen ,  Makoto Matsumoto

发明人： Yoshikazu Kawano ,  Yoshikazu Haraguchi ,  Hirofumi Sasaki ,  Yukitaka Uematsu ,  Hidetsugu Tsubouchi ,  Hiromi Yata ,  Hiroshi Shimizu ,  Kazuho Kohashi ,  Motohiro Itotani ,  Kuninori Tai ,  Isao Takemura ,  Mikayo Hayashi ,  Hiroyuki Hashizume ,  Miki Matsuba ,  Izuru Nakamura ,  Xiuhao Chen ,  Makoto Matsumoto

IPC分类号： C07D498/04 ,  A61K31/5383

CPC分类号： C07D498/04

摘要： 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, wherein R1 represents tetrahydroisoquinolyl, tetrahydroquinolyl, tetrahydrobenzoazepinyl, benzoxazolyl, benzothiazolyl, indolyl, isoindolinyl, naphthyl, quinolyl, phenyl, biphenylyl, or pyridyl, these groups being optionally substituted, the phenyl, biphenylyl, and pyridyl represented by R1 each being substituted directly or via a linker with at least one group selected from the group consisting of tetrahydropyridyl, diazepanyl, diazabicycloheptanyl, tetrahydrotriazolopyrazinyl, tetrahydroimidazopyrazinyl, azabicyclooctanyl, oxazolyl, piperazinyl, piperidyl, thiazolyl, and the like, each of these groups being optionally substituted; and R2 represents hydrogen or lower alkyl. The present invention further provides a pharmaceutical composition containing the above.

摘要翻译： 本发明提供了对结核杆菌，多重耐药性结核杆菌和非典型抗酸杆菌具有优异的杀菌作用的新型6,7-二氢咪唑并[2,1-b] [1,3]恶嗪化合物。 具体地说，本发明提供由式（1）表示的化合物或其盐，其中R1表示四氢异喹啉基，四氢喹啉基，四氢苯并氮杂基，苯并恶唑基，苯并噻唑基，吲哚基，异吲哚啉基，萘基，喹啉基，苯基，联苯基或吡啶基。 任选被取代的苯基，联苯基和吡啶基，其各自被直接取代或经由具有至少一个选自四氢吡啶基，二氮杂环庚烷基，二氮杂双环庚烷基，四氢三唑并吡嗪基，四氢咪唑并吡嗪基，氮杂双环辛基，恶唑基，哌嗪基，哌啶基 ，噻唑基等，这些基团各自任选被取代; 并且R 2表示氢或低级烷基。 本发明还提供含有上述物质的药物组合物。

公开(公告)号：US20140031342A1

公开(公告)日：2014-01-30

申请号：US14111262

申请日：2012-04-13

申请人： Yoshikazu Kawano ,  Yoshikazu Haraguchi ,  Hirofumi Sasaki ,  Yukitaka Uematsu ,  Hidetsugu Tsubouchi ,  Hiromi Yata ,  Hiroshi Shimizu ,  Kazuho Kohashi ,  Motohiro Itotani ,  Kuninori Tai ,  Isao Takemura ,  Mikayo Hayashi ,  Hiroyuki Hashizume ,  Miki Matsuba ,  Izuru Nakamura ,  Xiuhao Chen ,  Makoto Matsumoto

发明人： Yoshikazu Kawano ,  Yoshikazu Haraguchi ,  Hirofumi Sasaki ,  Yukitaka Uematsu ,  Hidetsugu Tsubouchi ,  Hiromi Yata ,  Hiroshi Shimizu ,  Kazuho Kohashi ,  Motohiro Itotani ,  Kuninori Tai ,  Isao Takemura ,  Mikayo Hayashi ,  Hiroyuki Hashizume ,  Miki Matsuba ,  Izuru Nakamura ,  Xiuhao Chen ,  Makoto Matsumoto

IPC分类号： C07D498/04

CPC分类号： C07D498/04

摘要： 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, wherein R1 represents tetrahydroisoquinolyl, tetrahydroquinolyl, tetrahydrobenzoazepinyl, benzoxazolyl, benzothiazolyl, indolyl, isoindolinyl, naphthyl, quinolyl, phenyl, biphenylyl, or pyridyl, these groups being optionally substituted, the phenyl, biphenylyl, and pyridyl represented by R1 each being substituted directly or via a linker with at least one group selected from the group consisting of tetrahydropyridyl, diazepanyl, diazabicycloheptanyl, tetrahydrotriazolopyrazinyl, tetrahydroimidazopyrazinyl, azabicyclooctanyl, oxazolyl, piperazinyl, piperidyl, thiazolyl, and the like, each of these groups being optionally substituted; and R2 represents hydrogen or lower alkyl. The present invention further provides a pharmaceutical composition containing the above.

摘要翻译： 本发明提供了对结核杆菌，多重耐药性结核杆菌和非典型抗酸杆菌具有优异的杀菌作用的新型6,7-二氢咪唑并[2,1-b] [1,3]恶嗪化合物。 具体地说，本发明提供由式（1）表示的化合物或其盐，其中R1表示四氢异喹啉基，四氢喹啉基，四氢苯并氮杂基，苯并恶唑基，苯并噻唑基，吲哚基，异吲哚啉基，萘基，喹啉基，苯基，联苯基或吡啶基。 任选被取代的苯基，联苯基和吡啶基，其各自被直接取代或经由具有至少一个选自四氢吡啶基，二氮杂环庚烷基，二氮杂双环庚烷基，四氢三唑并吡嗪基，四氢咪唑并吡嗪基，氮杂双环辛基，恶唑基，哌嗪基，哌啶基 ，噻唑基等，这些基团各自任选被取代; 并且R 2表示氢或低级烷基。 本发明还提供含有上述物质的药物组合物。

公开(公告)号：US08129544B2

公开(公告)日：2012-03-06

申请号：US11905446

申请日：2007-10-01

申请人： Fumitaka Goto ,  Noriaki Takemura ,  Tadaaki Otani ,  Takeshi Hasegawa ,  Hidetsugu Tsubouchi ,  Naoto Utsumi ,  Shigekazu Fujita ,  Hideaki Kuroda ,  Takuya Shitsuta ,  Hirofumi Sasaki

发明人： Fumitaka Goto ,  Noriaki Takemura ,  Tadaaki Otani ,  Takeshi Hasegawa ,  Hidetsugu Tsubouchi ,  Naoto Utsumi ,  Shigekazu Fujita ,  Hideaki Kuroda ,  Takuya Shitsuta ,  Hirofumi Sasaki

IPC分类号： C07D407/06

CPC分类号： C07D233/92

摘要： The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH2RA; X is a halogen atom or a group of the formula —S(O)n-R1) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.

摘要翻译： 本发明涉及由通式（1）表示的1-取代-4-硝基咪唑化合物或其盐（其中R是氢原子，低级烷氧基取代的低级烷基，苯基 - 低级烷氧基 取代基的低级烷基，氰基取代的低级烷基，可以具有低级烷氧基作为苯环中的取代基的苯基 - 低级烷基或式-CH2RA的基团; X是卤素原子或 基团-S（O）n -R1）及其制备方法。 式（1）的化合物是用作合成各种药用和农药的中间体的有用化合物，特别是作为抗结核剂的中间体。

公开(公告)号：US07807843B2

公开(公告)日：2010-10-05

申请号：US12007776

申请日：2008-01-15

申请人： Fumitaka Goto ,  Noriaki Takemura ,  Tadaaki Otani ,  Takeshi Hasegawa ,  Hidetsugu Tsubouchi ,  Naoto Utsumi ,  Shigekazu Fujita ,  Hideaki Kuroda ,  Takuya Shitsuta ,  Hirofumi Sasaki

发明人： Fumitaka Goto ,  Noriaki Takemura ,  Tadaaki Otani ,  Takeshi Hasegawa ,  Hidetsugu Tsubouchi ,  Naoto Utsumi ,  Shigekazu Fujita ,  Hideaki Kuroda ,  Takuya Shitsuta ,  Hirofumi Sasaki

IPC分类号： C07D407/06

CPC分类号： C07D233/92

摘要： The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH2RA; X is a halogen atom or a group of the formula —S(O)n-R1) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.

摘要翻译： 本发明涉及由通式（1）表示的1-取代-4-硝基咪唑化合物或其盐（其中R是氢原子，低级烷氧基取代的低级烷基，苯基 - 低级烷氧基 取代基的低级烷基，氰基取代的低级烷基，可以具有低级烷氧基作为苯环中的取代基的苯基 - 低级烷基或式-CH2RA的基团; X是卤素原子或 基团-S（O）n -R1）及其制备方法。 式（1）的化合物是用作合成各种药用和农药的中间体的有用化合物，特别是作为抗结核剂的中间体。

公开(公告)号：US20080097107A1

公开(公告)日：2008-04-24

申请号：US11905446

申请日：2007-10-01

申请人： Fumitaka Goto ,  Noriaki Takemura ,  Tadaaki Otani ,  Takeshi Hasegawa ,  Hidetsugu Tsubouchi ,  Naoto Utsumi ,  Shigekazu Fujita ,  Hideaki Kuroda ,  Takuya Shitsuta ,  Hirofumi Sasaki

发明人： Fumitaka Goto ,  Noriaki Takemura ,  Tadaaki Otani ,  Takeshi Hasegawa ,  Hidetsugu Tsubouchi ,  Naoto Utsumi ,  Shigekazu Fujita ,  Hideaki Kuroda ,  Takuya Shitsuta ,  Hirofumi Sasaki

IPC分类号： C07D233/92

CPC分类号： C07D233/92

摘要： The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH2RA; X is a halogen atom or a group of the formula —S(O)n-R1) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.

摘要翻译： 本发明涉及由通式（1）表示的1-取代-4-硝基咪唑化合物或其盐（其中R是氢原子，低级烷氧基取代的低级烷基，苯基 - 低级烷氧基 取代基的低级烷基，氰基取代的低级烷基，可以具有低级烷氧基作为苯环中的取代基的苯基 - 低级烷基或式-CH 2的基团， X是卤素原子或式-S（O）n R 1）的基团）及其制备方法。 式（1）的化合物是用作合成各种药用和农药的中间体的有用化合物，特别是作为抗结核剂的中间体。

公开(公告)号：US20120130082A1

公开(公告)日：2012-05-24

申请号：US13362646

申请日：2012-01-31

申请人： Fumitaka GOTO ,  Noriaki Takemura ,  Tadaaki Otani ,  Takeshi Hasegawa ,  Hidetsugu Tsubouchi ,  Naoto Utsumi ,  Shigekazu Fujita ,  Hideaki Kuroda ,  Takuya Shitsuta ,  Hirofumi Sasaki

发明人： Fumitaka GOTO ,  Noriaki Takemura ,  Tadaaki Otani ,  Takeshi Hasegawa ,  Hidetsugu Tsubouchi ,  Naoto Utsumi ,  Shigekazu Fujita ,  Hideaki Kuroda ,  Takuya Shitsuta ,  Hirofumi Sasaki

IPC分类号： C07D405/06 ,  C07D233/92 ,  C07D233/84

CPC分类号： C07D233/92

摘要： The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH2RA; X is a halogen atom or a group of the formula —S(O)n-R1) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.

摘要翻译： 本发明涉及由通式（1）表示的1-取代-4-硝基咪唑化合物或其盐（其中R是氢原子，低级烷氧基取代的低级烷基，苯基 - 低级烷氧基 取代基的低级烷基，氰基取代的低级烷基，可以具有低级烷氧基作为苯环中的取代基的苯基 - 低级烷基或式-CH2RA的基团; X是卤素原子或 基团-S（O）n -R1）及其制备方法。 式（1）的化合物是用作合成各种药用和农药的中间体的有用化合物，特别是作为抗结核剂的中间体。