公开(公告)号：US3963736A

公开(公告)日：1976-06-15

申请号：US478118

申请日：1974-06-10

申请人： Takenari Nakagome ,  Hideo Agui ,  Toru Mitani ,  Mitsuo Nakashita

发明人： Takenari Nakagome ,  Hideo Agui ,  Toru Mitani ,  Mitsuo Nakashita

IPC分类号： C07D471/04

摘要： A process for producing a compound of the formula: ##SPC1##Wherein Z is CH or N; R is a lower alkyl group, a lower alkenyl group, a cycloalkyl group or a hydroxyalkyl group; R.sub.1 is a hydrogen atom or lower alkyl group; when Z is N, R.sub.2, R.sub.3 and R.sub.4 are a hydrogen atom, a halogen atom a lower alkyl group, a lower alkoxyl group, a lower hydroxyalkyl group, a lower acyloxyalkyl group, trihalogenoalkyl group, a carboxyl group, a cyano group, or an aralkyl group; when Z is CH, R.sub.2, R.sub.3 and R.sub.4 are a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group, a trihalogenoalkyl group, a cyano group, a nitro group, an alkylmercapto group, a lower alkylenedioxy group, or a lower alkylene bridge attached to the quinoline nucleus, which comprises heating a compound of the formula ##SPC2##Wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and Z are as defined above, followed, if desired, by hydrolyzing the product obtained, is disclosed.The product is useful as an antibacterial agent. An intermediate having the formula: ##SPC3##Wherein A is OR or a halogen atom, and R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and Z are as defined above, and a process for its preparation are also disclosed.

摘要翻译： 一种制备下式化合物的方法：

公开(公告)号：US4216333A

公开(公告)日：1980-08-05

申请号：US7843

申请日：1979-01-30

申请人： Hideo Agui ,  Ikutaro Saji ,  Mitsuo Nakashita

发明人： Hideo Agui ,  Ikutaro Saji ,  Mitsuo Nakashita

IPC分类号： C07D233/62 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： A process for preparing N-tritylimidazole compounds of the formula: ##STR1## by the reaction between a tritylcarbinol derivative of the formula: ##STR2## and an imidazole derivative of the formula: ##STR3## , characterized in that the reaction is effected in the presence of a phosphorus compound of the formula: ##STR4##

摘要翻译： 通过下式的三苯甲基甲醇衍生物与下式的咪唑衍生物反应制备下式的N-三甲基咪唑化合物的方法：[IMAGE] [I] 其特征在于反应在下式的磷化合物存在下进行：[IV]

公开(公告)号：US4054568A

公开(公告)日：1977-10-18

申请号：US661455

申请日：1976-02-25

申请人： Hideo Agui ,  Toru Mitani ,  Mitsuo Nakashita ,  Eiichi Murayama ,  Kousaku Okamura ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Yasuko Eda

发明人： Hideo Agui ,  Toru Mitani ,  Mitsuo Nakashita ,  Eiichi Murayama ,  Kousaku Okamura ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Yasuko Eda

IPC分类号： C07D513/04

CPC分类号： C07D513/04

摘要： Thiazolo[5,4-f]quinoline-8-carboxylic acid derivatives having either the general formula (I): ##STR1## wherein R.sub.1 is a lower alkyl group, a lower alkenyl group or a benzyl group; or the general formula (III-a): ##STR2## WHEREIN R.sub.3 is a lower alkyl group and X is a halogen atom; and methods for the preparation thereof. The compounds of the general formula (I) are useful as antibacterial agents against gram-negative and gram-positive bacteria. The compounds of the general formula (III-a) are useful as antifungal agents against eumycetes and also as an intermediate in a peparation of the compounds of the general formula (I).

摘要翻译： 具有通式（I）的噻唑并[5,4-f]喹啉-8-羧酸衍生物：其中R1是低级烷基，低级烯基或苄基; （III-a）：（III-a）其中R3为低级烷基，X为卤素原子; 及其制备方法。 通式（I）的化合物可用作抗革兰氏阴性细菌和革兰氏阳性细菌的抗菌剂。 通式（III-a）的化合物可用作抗真菌剂的抗真菌剂，也可用作通式（I）化合物的分离中的中间体。

公开(公告)号：US4008237A

公开(公告)日：1977-02-15

申请号：US626001

申请日：1975-10-28

申请人： Hideo Agui ,  Iwao Nakatsuka ,  Toru Mitani ,  Mitsuo Nakashita ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Yasuko Eda

发明人： Hideo Agui ,  Iwao Nakatsuka ,  Toru Mitani ,  Mitsuo Nakashita ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Yasuko Eda

IPC分类号： C07D215/56 ,  C07D491/048

CPC分类号： C07D491/048

摘要： Novel antibacterial agents consisting of a 2,3,5,8-tetrahydro-5-alkoxy-8-oxofuro(2,3-g)quinoline-7-carboxylic acid of the formula: ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl, a process for producing the derivatives and pharmaceutical compositions containing the same. The above-identified derivatives possess antibacterial activity against gram-negative bacteria at test concentration levels of about 0.0001 to 1.0 mg/cc.

摘要翻译： 新型抗菌剂由下列通式的2,3,5,8-四氢-5-烷氧基-8-氧代呋喃（2,3-g）喹啉-7-羧酸组成，其中R是C 1 -C 4烷基 ，制备衍生物的方法和含有该衍生物的药物组合物。 上述衍生物在约0.0001至1.0mg / cc的测试浓度水平下对革兰氏阴性细菌具有抗菌活性。

公开(公告)号：US3954775A

公开(公告)日：1976-05-04

申请号：US515753

申请日：1974-10-17

申请人： Hideo Agui ,  Toru Mitani ,  Mitsuo Nakashita ,  Eiichi Murayama ,  Kousaku Okamura ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Yasuko Eda

发明人： Hideo Agui ,  Toru Mitani ,  Mitsuo Nakashita ,  Eiichi Murayama ,  Kousaku Okamura ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Yasuko Eda

IPC分类号： C07D513/04

CPC分类号： C07D513/04

摘要： Thiazolo[5,4-f]quinoline-8-carboxylic acid derivatives having either the general formula (I): ##SPC1##wherein R.sub.1 is a lower alkyl group, a lower alkenyl group or a benzyl group; or the general formula (III-a): ##SPC2##Wherein R.sub.3 is a lower alkyl group and X is a halogen atom; and methods for the preparation thereof. The compounds of the general formula (I) are useful as antibacterial agents against gram-negative and gram-positive bacteria. The compounds of the general formula (III-a) are useful as antifungal agents against eumycetes and also as an intermediate in a preparation of the compounds of the general formula (I).

摘要翻译： 具有通式（I）的噻唑并[5,4-f]喹啉-8-羧酸衍生物：