公开(公告)号：US4421912A

公开(公告)日：1983-12-20

申请号：US235609

申请日：1981-02-18

申请人： Mitsuo Numata ,  Isao Mimamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

发明人： Mitsuo Numata ,  Isao Mimamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

IPC分类号： C07D277/34 ,  C07D277/36 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36

CPC分类号： C07D501/24 ,  C07D277/34 ,  C07D277/36

摘要： A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula --NR.sup.2 (where R.sup.2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R.sup.1), and Y represents acetoxy group or a group of formula --SR.sup.3 (where R.sup.3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.

公开(公告)号：US4379924A

公开(公告)日：1983-04-12

申请号：US863719

申请日：1977-12-23

申请人： Mitsuo Numata ,  Isao Mimamida ,  Masayoshi Yamaoka ,  Mitsura Shiraishi ,  Toshio Miyawaki

发明人： Mitsuo Numata ,  Isao Mimamida ,  Masayoshi Yamaoka ,  Mitsura Shiraishi ,  Toshio Miyawaki

IPC分类号： C07D277/34 ,  C07D277/36 ,  C07D501/36 ,  A61K31/545

CPC分类号： C07D501/24 ,  C07D277/34 ,  C07D277/36

摘要： A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula --NR.sup.2 (where R.sup.2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R.sup.1), and Y represents acetoxy group or a group of formula --SR.sup.3 (where R.sup.3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.

公开(公告)号：US4080498A

公开(公告)日：1978-03-21

申请号：US534782

申请日：1974-12-20

申请人： Mitsuo Numata ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

发明人： Mitsuo Numata ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

IPC分类号： C07D277/34 ,  C07D277/36 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/60

CPC分类号： C07D501/24 ,  C07D277/34 ,  C07D277/36

摘要： A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula --NR.sup.2 (where R.sup.2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R.sup.1), and Y represents acetoxy group or a group of formula --SR.sup.3 (where R.sup.3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.

摘要翻译： 下式的化合物：其中R 1表示氢或烷基，X表示氧或硫或式-NR 2基团（其中R 2是氢或烷基，在烷基的情况下可以形成 环与R 1连接），Y表示乙酰氧基或式-SR 3（其中R 3为含氮杂环基）基团或其药学上可接受的盐具有宽的抗菌谱，特别是， 对革兰氏阴性菌有效，包括大肠杆菌，肺炎克雷伯杆菌，普通变形杆菌，变形杆菌，以及革兰氏阳性菌。 因此，这些化合物可用于治疗目的的抗微生物剂。

公开(公告)号：US4517361A

公开(公告)日：1985-05-14

申请号：US480791

申请日：1983-03-31

申请人： Mitsuo Numata ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

发明人： Mitsuo Numata ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

IPC分类号： C07D277/34 ,  C07D277/36 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/28

CPC分类号： C07D501/24 ,  C07D277/34 ,  C07D277/36

摘要： A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula -NR.sup.2 (where R.sup.2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R.sup.1), and Y represents acetoxy group or a group of formula -SR.sup.3 (where R.sup.3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.

摘要翻译： 下式的化合物：其中R 1表示氢或烷基，X表示氧或硫或式-NR 2基团（其中R 2是氢或烷基，在烷基的情况下可以形成 环与R 1连接），Y表示乙酰氧基或式-SR 3（其中R 3为含氮杂环基）基团或其药学上可接受的盐具有宽的抗菌谱，特别是， 对革兰氏阴性菌有效，包括大肠杆菌，肺炎克雷伯杆菌，普通变形杆菌，变形杆菌，以及革兰氏阳性菌。 因此，这些化合物可用于治疗目的的抗微生物剂。

公开(公告)号：US3984401A

公开(公告)日：1976-10-05

申请号：US422748

申请日：1973-12-07

申请人： Shinji Terao ,  Mitsuru Shiraishi ,  Toshio Miyawaki ,  Isao Minamida ,  Masayoshi Yamaoka ,  Yoshio Imashiro ,  Mitsuo Numata

发明人： Shinji Terao ,  Mitsuru Shiraishi ,  Toshio Miyawaki ,  Isao Minamida ,  Masayoshi Yamaoka ,  Yoshio Imashiro ,  Mitsuo Numata

IPC分类号： A61K31/545 ,  C07D501/04 ,  C07D501/16 ,  C07D501/26 ,  C07D501/60 ,  C07D513/14 ,  C07D515/14

CPC分类号： C07D501/04 ,  C07D501/26

摘要： A 3-hydroxymethylcephalosporin which is not protected at the carboxyl group can be directly oxidized with a hexavalent chromium compound to give in good yield a lactol type cephalosporin represented by the general formula: ##SPC1##Wherein R.sup.1 is hydrogen or an alkoxy group and R.sup.2 is an acylamino, or imido group. The resulting compounds are very useful and important as intermediates for preparing, e.g. 3-alkoxyiminomethyl cephalosporins.

摘要翻译： 在羧基上未被保护的3-羟甲基头孢菌素可以用六价铬化合物直接氧化，得到良好的产率，由通式表示的乳糖型头孢菌素：

公开(公告)号：US4011214A

公开(公告)日：1977-03-08

申请号：US534787

申请日：1974-12-20

申请人： Shinji Terao ,  Mitsuru Shiraishi ,  Toshio Miyawaki ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuo Numata

发明人： Shinji Terao ,  Mitsuru Shiraishi ,  Toshio Miyawaki ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuo Numata

IPC分类号： C07D501/24 ,  A61K31/43 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/04 ,  C07D501/38 ,  C07D501/50 ,  C07D501/52 ,  C07D501/54 ,  C07D501/60

CPC分类号： C07D501/38

摘要： Novel cephalosporin compounds of the formula ##STR1## wherein R.sup.1 is an acyl group and R.sup.2 is an alkylene group which may be substituted with a lower alkoxyl group, or pharmaceutically acceptable salt thereof, have strong inhibitory actions on broad spectra of gram-positive and gram-negative bacteria and, particularly against Esherichia coli and Klebsiella pneumoniae. Thus, the compounds are useful as therapeutic agent for various bacterial infections of animals including human beings.

公开(公告)号：US4239758A

公开(公告)日：1980-12-16

申请号：US44215

申请日：1979-05-31

申请人： Mitsuo Numata ,  Masayoshi Yamaoka ,  Isao Minamida ,  Mitsuru Shiraishi ,  Tatsuo Nishimura

发明人： Mitsuo Numata ,  Masayoshi Yamaoka ,  Isao Minamida ,  Mitsuru Shiraishi ,  Tatsuo Nishimura

IPC分类号： A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/20 ,  C07D501/22 ,  C07D501/24 ,  C07D501/26 ,  C07D501/28 ,  C07D501/34 ,  C07D501/36 ,  C07D501/38 ,  C07D501/46 ,  C07D501/56 ,  C07D501/60

CPC分类号： C07D501/20 ,  C07D501/24

摘要： A novel cephalosporin derivative of the formula: ##STR1## [wherein X is hydrogen, hydroxyl, acyloxy, alkoxy, carbamoyloxy, quaternary ammonium or a group of the formula --SR.sup.1 (where R.sup.1 is a nitrogen-containing heterocyclic group)] or a pharmaceutically acceptable salt or ester thereof is found to have potent antibiotic activity against various bacteria, particularly against gram-negative bacteria such as Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus mirabilis, Proteus morganii, Proteus rettgeri and Citrobacter freundii.

摘要翻译： 一种下式的新型头孢菌素衍生物：其中X是氢，羟基，酰氧基，烷氧基，氨基甲酰氧基，季铵或式-SR1（其中R1是含氮杂环基）的基团）或药学上 发现其可接受的盐或酯对各种细菌，特别是对革兰氏阴性细菌如大肠杆菌，肺炎克雷伯杆菌，普通变形杆菌，奇异变形杆菌，变形杆菌，变形杆菌和弗氏氟柠檬酸杆菌具有有效的抗生素活性。

公开(公告)号：US4172891A

公开(公告)日：1979-10-30

申请号：US783230

申请日：1977-03-31

申请人： Mitsuo Numata ,  Masayoshi Yamaoka ,  Isao Minamida ,  Mitsuru Shiraishi ,  Tatsuo Nishimura

发明人： Mitsuo Numata ,  Masayoshi Yamaoka ,  Isao Minamida ,  Mitsuru Shiraishi ,  Tatsuo Nishimura

IPC分类号： A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/20 ,  C07D501/22 ,  C07D501/24 ,  C07D501/26 ,  C07D501/28 ,  C07D501/34 ,  C07D501/36 ,  C07D501/38 ,  C07D501/46 ,  C07D501/56 ,  C07D501/60

CPC分类号： C07D501/20 ,  C07D501/24

摘要： A novel cephalosporin derivative of the formula: ##STR1## [wherein X is hydrogen, hydroxyl, acyloxy, alkoxy, carbamoyloxy, quaternary ammonium or a group of the formula --SR.sup.1 (where R.sup.1 is a nitrogen-containing heterocyclic group)] or a pharmaceutically acceptable salt or ester thereof is found to have potent antibiotic activity against various bacteria, particularly against gram-negative bacteria such as Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus mirabilis, Proteus morganii, Proteus rettgeri and Citrobacter freundii.

摘要翻译： 一种下式的新型头孢菌素衍生物：其中X是氢，羟基，酰氧基，烷氧基，氨基甲酰氧基，季铵或式-SR1（其中R1是含氮杂环基）的基团）或药学上 发现其可接受的盐或酯对各种细菌，特别是对革兰氏阴性细菌如大肠杆菌，肺炎克雷伯杆菌，普通变形杆菌，奇异变形杆菌，变形杆菌，变形杆菌和弗氏氟柠檬酸杆菌具有有效的抗生素活性。

公开(公告)号：US4238608A

公开(公告)日：1980-12-09

申请号：US43323

申请日：1979-05-29

申请人： Mitsuo Numata ,  Masayoshi Yamaoka

发明人： Mitsuo Numata ,  Masayoshi Yamaoka

IPC分类号： C07D501/34 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D207/48 ,  C07D501/24 ,  C07D501/36 ,  C07D501/46 ,  C07D501/56

CPC分类号： C07D207/48

摘要： A novel compound of the formula: ##STR1## wherein R is lower alkyl or a group of the formula ##STR2## where R.sup.1 and R.sup.2 are the same or different and each is hydrogen, carboxyl or halogen; Y is acyloxy or a group of the formula --S--Het where Het is a nitrogen-containing heterocyclic group which may optionally be substituted, or a pharmaceutically acceptable salt thereof is found to be effective for treatment of diseases in animals including domestic fowls and human beings, particularly the infectious diseases caused by gram-positive and gram-negative bacteria.

摘要翻译： 下式的新型化合物：其中R是低级烷基或式IMAGE的基团，其中R 1和R 2相同或不同，各自为氢，羧基或卤素; Y是酰氧基或式-S-Het的基团，其中Het是可任选被取代的含氮杂环基，或其药学上可接受的盐对于治疗动物，包括家禽和人类的疾病是有效的 生物，特别是由革兰氏阳性和革兰氏阴性菌引起的传染病。

公开(公告)号：US4725592A

公开(公告)日：1988-02-16

申请号：US637138

申请日：1984-08-03

申请人： Akio Miyake ,  Masayoshi Yamaoka ,  Mitsuo Numata

发明人： Akio Miyake ,  Masayoshi Yamaoka ,  Mitsuo Numata

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/36 ,  C07D501/56

CPC分类号： C07D501/36

摘要： A compound of the formula: ##STR1## wherein R.sub.1 stands for n-propyl or isopropyl; and R.sub.2 stands for n-butyl, isobutyl, n-pentyl, n-hexyl or 2-ethylbutyl, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.

摘要翻译： 下式的化合物：其中R 1代表正丙基或异丙​​基; R2代表正丁基，异丁基，正戊基，正己基或2-乙基丁基，或其药学上可接受的盐，其制备方法及其药物组合物。 该化合物可口服施用，具有改善生物利用度的抗生素。