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：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：

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：US4160087A

公开(公告)日：1979-07-03

申请号：US795596

申请日：1977-05-10

申请人： Hirotada Yamada ,  Kousaku Okamura ,  Hisao Tobiki ,  Norihiko Tanno ,  Kozo Shimago ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Kenji Irie ,  Yasuko Eda

发明人： Hirotada Yamada ,  Kousaku Okamura ,  Hisao Tobiki ,  Norihiko Tanno ,  Kozo Shimago ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Kenji Irie ,  Yasuko Eda

IPC分类号： A61K31/545 ,  C07D501/34

CPC分类号： C07D501/34 ,  C07D501/24

摘要： A cephalosporin derivative of the formula (I), ##STR1## wherein A is a mono- or polycyclic heteroaromatic ring, which contains at least one nitrogen atom as a hetero atom and which may be substituted with one or more substituents; R is a phenyl group substituted with at least one substituent selected from the group consisting of an amino group, a hydroxy group, a ureido group and a hydroxymethyl group; and X is an --OCOCH.sub.3 group or an --S-Het group in which Het is a 5- or 6-membered heterocyclic ring containing one to four hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur atoms which may be substituted with one or more substituents, and the non-toxic pharmaceutically acceptable salts thereof which are useful as an antimicrobial and prepared by the reaction of a compound of the formula (II),ho--a--cooh (ii)wherein A is as defined above, or a reactive derivative thereof, with a compound of the formula (III), ##STR2## wherein R and X are as defined above, or a derivative thereof.

摘要翻译： 式（I）的头孢菌素衍生物，其中A是单环或多环杂芳环，其含有至少一个氮原子作为杂原子并且可以被一个或多个取代基取代; R是被至少一个选自氨基，羟基，脲基和羟甲基的取代基取代的苯基; 并且X是-OCOCH 3基团或-S-Het基团，其中Het是含有1至4个选自氮，氧和硫原子的杂原子的5或6元杂环，其可以被 一种或多种取代基及其无毒的药学上可接受的盐，其可用作抗微生物剂并通过式（II）化合物，其中A如上定义的HO-A-COOH（II） 或其活性衍生物与式（III）化合物，其中R和X如上所定义的其中，或其衍生物。

公开(公告)号：US4156724A

公开(公告)日：1979-05-29

申请号：US611104

申请日：1975-09-08

申请人： Hirotada Yamada ,  Kousaku Okamura ,  Hisao Tobiki ,  Norihiko Tanno ,  Kozo Shimago ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Kenji Irie ,  Yasuko Eda

发明人： Hirotada Yamada ,  Kousaku Okamura ,  Hisao Tobiki ,  Norihiko Tanno ,  Kozo Shimago ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Kenji Irie ,  Yasuko Eda

IPC分类号： A61K20060101 ,  A61K31/545 ,  C07D20060101 ,  C07D501/04 ,  C07D501/20 ,  C07D501/24 ,  C07D501/26 ,  C07D501/32 ,  C07D501/34 ,  C07D501/36 ,  C07D501/44 ,  C07D501/46 ,  C07D501/54 ,  C07D501/56 ,  C07D501/60 ,  C07D519/00

CPC分类号： C07D501/34 ,  C07D501/24

摘要： A cephalosporin derivative of the formula (I), ##STR1## wherein A is a mono- or polycyclic heteroaromatic ring, which contains at least one nitrogen atom as a hetero atom and which may be substituted with one or more substituents; R is a phenyl group substituted with at least one substituent selected from the group consisting of an amino group, a hydroxy group, a ureido group and a hydroxymethyl group; and X is an --OCOCH.sub.3 group or an --S-Het group in which Het is a 5- or 6-membered heterocyclic ring containing one to four hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur atoms which may be substituted with one or more substituents, and the non-toxic pharmaceutically acceptable salts thereof which are useful as an antimicrobial and prepared by the reaction of a compound of the formula (II),ho--a--cooh (ii)wherein A is as defined above, or a reactive derivative thereof, with a compound of the formula (III), ##STR2## wherein R and X are as defined above, or a derivative thereof.

摘要翻译： 式（I）的头孢菌素衍生物，其中A是单环或多环杂芳环，其含有至少一个氮原子作为杂原子并且可以被一个或多个取代基取代; R是被至少一个选自氨基，羟基，脲基和羟甲基的取代基取代的苯基; 并且X是-OCOCH 3基团或-S-Het基团，其中Het是含有1至4个选自氮，氧和硫原子的杂原子的5或6元杂环，其可以被 一种或多种取代基及其无毒的药学上可接受的盐，其可用作抗微生物剂并通过式（II）化合物，其中A如上定义的HO-A-COOH（II） 或其活性衍生物与式（III）化合物，其中R和X如上所定义的其中，或其衍生物。

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：US4117126A

公开(公告)日：1978-09-26

申请号：US836922

申请日：1977-09-26

申请人： Hirotada Yamada ,  Kosaku Okamura ,  Hisao Tobiki ,  Norihiko Tanno ,  Kozo Shimago ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Kenji Irie ,  Yasuko Eda

发明人： Hirotada Yamada ,  Kosaku Okamura ,  Hisao Tobiki ,  Norihiko Tanno ,  Kozo Shimago ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Kenji Irie ,  Yasuko Eda

IPC分类号： C07D501/24 ,  C07D501/36

CPC分类号： C07D501/24

摘要： A cephalosporin derivative of formula (I): ##STR1## wherein X is an --OCOCH.sub.3 group or an --S--Het group in which Het is a 5- or 6-membered heterocyclic ring containing one to four hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur atoms, which may be substituted with one or more substituents, and the non-toxic pharmaceutically acceptable salts thereof which are useful as an antimicrobial material and which are prepared by the reaction of a compound of formula (II): ##STR2## or a reactive derivative thereof, with a compound of formula (III): ##STR3## wherein X is as defined above, or a derivative thereof.

公开(公告)号：US4008220A

公开(公告)日：1977-02-15

申请号：US495914

申请日：1974-08-08

申请人： Hisao Tobiki ,  Hirotada Yamada ,  Iwao Nakatsuka ,  Kozo Shimago ,  Shigeru Okano ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Yasuko Eda

发明人： Hisao Tobiki ,  Hirotada Yamada ,  Iwao Nakatsuka ,  Kozo Shimago ,  Shigeru Okano ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Yasuko Eda

IPC分类号： C07D499/00 ,  C07D499/68 ,  C07D499/48

CPC分类号： C07D499/00 ,  Y02P20/55

摘要： A penicillin of the formula: ##STR1## wherein ##STR2## is a six-membered heteroaromatic ring containing 1 or 2 nitrogen atoms as the hetero atom, Y is hydrogen, lower alkanoyl or lower alkoxycarbonyl, R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkanoyl, benzoyl, lower alkylmercapto, hydroxyl, mercapto, hydroxy(lower)alkyl, halogen or cyano or R.sub.1 and R.sub.2 may link together to form a lower alkylene chain which may be substituted with an oxo group, and Z is phenyl, hydroxyphenyl, lower alkyl, cyclohexadienyl, thienyl or isothiazolyl, which is prepared by reacting a compound of the formula: ##STR3## wherein Z is as defined above or its derivative with a carboxylic acid of the formula: ##STR4## wherein ##STR5## and R.sub.2 are each as defined above or its reactive derivative, if necessary, followed by hydrolysis or acylation of the resulting product and/or elimination of any protective group and which is useful as an antimicrobial agent against various gram-positive and gram-negative bacteria including Pseudomonas.

摘要翻译： 一种下式的青霉素：其中是含有1或2个氮原子作为杂原子的六元杂芳环，Y是氢，低级烷酰基或低级烷氧基羰基，R 1和R 2各自是氢，低级烷基 ，低级烷酰基，苯甲酰基，低级烷基巯基，羟基，巯基，羟基（低级）烷基，卤素或氰基，或者R 1和R 2可以连接在一起形成可被氧代基取代的低级亚烷基链，Z是苯基， 低级烷基，环己二烯基，噻吩基或异噻唑基，其通过使下式化合物：其中Z如上所定义或其衍生物与下式的羧酸反应制备：其中和R2 各自如上所定义，或其反应性衍生物，如果需要，随后水解或酰化所得产物和/或消除任何保护基团，并且其可用作针对各种革兰氏阳性和革兰氏阴性菌的抗微生物剂，包括 uding假单胞菌

公开(公告)号：US3992371A

公开(公告)日：1976-11-16

申请号：US536181

申请日：1974-12-24

申请人： Hisao Tobiki ,  Hirotada Yamada ,  Iwao Nakatsuka ,  Kozo Shimago ,  Shigeru Okano ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Yasuko Eda

发明人： Hisao Tobiki ,  Hirotada Yamada ,  Iwao Nakatsuka ,  Kozo Shimago ,  Shigeru Okano ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Yasuko Eda

IPC分类号： C07D499/10 ,  C07D471/04 ,  C07D499/00 ,  C07D499/04 ,  C07D499/64 ,  C07D499/68 ,  C07D519/06 ,  C07D499/70

CPC分类号： C07D471/04 ,  C07D499/00

摘要： Novel penicillins of the formula ##SPC1##Wherein ##EQU1## represents a substituted or unsubstituted benzene or nitrogen atom-containing heteroaromatic ring which may be substituted, ##EQU2## represents a pyridine, pyrazine or pyridazine ring, X represents an oxygen or sulfur atom, Y represents a hydrogen atom or a loer alkoxycarbonyl or lower alkanoyl group, and R.sub.1, R.sub.2 and R.sub.3 are each a hydrogen or halogen atom or a nitro, lower alkylamino, di(lower)alkylamino, aine, lower alkoxycarbonylamino, lower alkanoylamino, amino(lower)alkyl, lower alkyl, lower alkoxy, hydroxyl, sulfamoyl, trifluoromethyl, lower alkylthio or lower alkylsulfonyl group, excluding the cases where all of R.sub.1, R.sub.2 and R.sub.3 are hydrogen atoms and where R.sub.1 is a hydroxyl group and R.sub.2 and R.sub.3 are each a hydrogen or halogen atom, and their nontoxic, pharmaceutically acceptable salts, which can be prepared by reacting a carboxylic acid of the formula: ##EQU3## wherein ##EQU4## X and Y are each as defined above or its reactive derivative with a compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2 and R.sub.3 are each as defined above or its reactive derivative, and are ueful as antimicrobial agents against gram-positive and gram-negative bacteria including Pseudomonas.

摘要翻译： 式+ q，10的新型青霉素其中C | A C表示可被取代的取代或未取代的含有苯或含氮原子的杂芳环，C | C | CB表示吡啶，吡嗪或哒嗪环，X表示 氧或硫原子，Y表示氢原子或低级烷氧基羰基或低级烷酰基，R 1，R 2和R 3各自为氢或卤素原子或硝基，低级烷基氨基，二（低级）烷基氨基，亚氨基，低级烷氧基羰基氨基， 低级烷酰基氨基，氨基（低级）烷基，低级烷基，低级烷氧基，羟基，氨磺酰基，三氟甲基，低级烷硫基或低级烷基磺酰基，不包括R1，R2和R3全部为氢原子，其中R1为羟基， R2和R3各自为氢或卤素原子，以及它们的无毒的药学上可接受的盐，其可以通过使下式的羧酸：XY | C | C-COOH A | CB反应而制备，其中CC | | CA | | C，CB，X和Y为ea ch或其反应性衍生物与下式的化合物：+ q，21，其中R1，R2和R3各自如上所定义，或其反应性衍生物，并且作为抗革兰氏阳性和革兰氏阴性细菌的抗微生物剂 包括假单胞菌。

公开(公告)号：US4061748A

公开(公告)日：1977-12-06

申请号：US674205

申请日：1976-04-05

申请人： Hirotada Yamada ,  Kosaku Okamura ,  Hisao Tobiki ,  Norihiko Tanno ,  Kozo Shimago ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Kenji Irie ,  Yasuko Eda

发明人： Hirotada Yamada ,  Kosaku Okamura ,  Hisao Tobiki ,  Norihiko Tanno ,  Kozo Shimago ,  Takenari Nakagome ,  Toshiaki Komatsu ,  Akio Izawa ,  Hiroshi Noguchi ,  Kenji Irie ,  Yasuko Eda

IPC分类号： C07D519/06 ,  A61K31/545 ,  C07D20060101 ,  C07D501/04 ,  C07D501/24 ,  C07D501/32 ,  C07D501/36 ,  C07D501/60 ,  C07D519/00

CPC分类号： C07D501/24

摘要： A cephalosporin derivative of formula (I): ##STR1## wherein X is an --OCOCH.sub.3 group or an -S-Het group in which Het is a 5- or 6-membered heterocyclic ring containing one to four hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur atoms, which may be substituted with one or more substituents, and the non-toxic pharmaceutically acceptable salts thereof which are useful as an antimicrobial material and which are prepared by the reaction of a compound of formula (II): ##STR2## or a reactive derivative thereof, with a compound of formula (III): ##STR3## wherein X is as defined above, or a derivative thereof.

摘要翻译： 式（I）的头孢菌素衍生物：其中X是-OCOCH 3基团或-S-Het基团，其中Het是含有1-4个杂原子的5-或6-元杂环 可以被一个或多个取代基取代的选自氮，氧和硫原子的原子及其无毒的药学上可接受的盐，其可用作抗微生物材料，并且其通过化合物 式（II）化合物或其衍生物与式（III）化合物反应：其中X如上定义，或其衍生物。