公开(公告)号：US4563450A

公开(公告)日：1986-01-07

申请号：US515184

申请日：1983-07-19

申请人： Takao Takaya ,  Yoshikazu Inoue ,  Masayoshi Murata ,  Hisashi Takasugi

发明人： Takao Takaya ,  Yoshikazu Inoue ,  Masayoshi Murata ,  Hisashi Takasugi

IPC分类号： C07D257/04 ,  C07D501/36 ,  A61K31/545

CPC分类号： C07D257/04 ,  Y02P20/55

摘要： This invention relates to a new cephem compound of the formula: ##STR1## wherein R.sup.1 is amino or a substituted amino group;R.sup.2 is carboxy or a protected carboxy group;R.sup.3 is a tetrazolyl group having a lower alkynyl group; andX is --S-- or ##STR2## and pharmaceutically acceptable salts thereof, of high antimicrobial activity.

公开(公告)号：US4427677A

公开(公告)日：1984-01-24

申请号：US332830

申请日：1981-12-21

申请人： Takao Takaya ,  Hisashi Takasugi ,  Masayoshi Murata ,  Akiteru Yoshioka

发明人： Takao Takaya ,  Hisashi Takasugi ,  Masayoshi Murata ,  Akiteru Yoshioka

IPC分类号： C07D277/20 ,  C07D277/40 ,  C07D501/46 ,  A61K31/545

CPC分类号： C07D277/587

摘要： This invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sub.1 is amino, lower alkanoylamino or halo(lower)alkanoylamino,R.sub.2 is lower alkyl, lower alkylthio(lower)alkyl, lower alkenyl, lower alkynyl, carboxy(lower)alkyl or esterified carboxy(lower)alkyl, andX is halogen;and pharmaceutically acceptable salts thereof.

摘要翻译： 本发明涉及具有下式的高抗微生物活性的新型头孢烯化合物：其中R1是氨基，低级烷酰基氨基或卤代（低级）烷酰基氨基，R2是低级烷基，低级烷硫基（低级）烷基，低级烯基，低级炔基， 羧基（低级）烷基或酯化羧基（低级）烷基，X为卤素; 及其药学上可接受的盐。

公开(公告)号：US4393059A

公开(公告)日：1983-07-12

申请号：US302639

申请日：1981-09-15

申请人： Takao Takaya ,  Hisashi Takasugi ,  Kiyoshi Tsuji ,  Toshiyuki Chiba

发明人： Takao Takaya ,  Hisashi Takasugi ,  Kiyoshi Tsuji ,  Toshiyuki Chiba

IPC分类号： C07D277/20 ,  C07D285/06 ,  C07D501/59 ,  C07D501/20 ,  A61K31/545

CPC分类号： C07D277/20 ,  C07D285/06 ,  C07D501/20

摘要： The invention relates particularly to syn compounds of the formula: ##STR1## wherein R.sup.2 is hydrogen or an aliphatic hydrocarbon which may be substituted with halogen, carboxy or pharmaceutically acceptable esterified carboxy,R.sup.5 is carboxy or pharmaceutically acceptable esterified carboxy,R.sup.6 is amino or protected amino andR.sup.7 is lower alkanesulfonyl or arenesulfonyl and pharmaceutically acceptable salt thereof, processes for making them, pharmaceutical compositions containing them and their use in treating infectious diseases.

摘要翻译： 本发明特别涉及下式的顺式化合物：其中R 2为氢或可被卤素，羧基或药学上可接受的酯化羧基取代的脂族烃基，R 5为羧基或药学上可接受的酯化羧基，R6为氨基或保护基 氨基和R7是低级烷基磺酰基或芳烃磺酰基及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗感染性疾病中的用途。

公开(公告)号：US4990507A

公开(公告)日：1991-02-05

申请号：US294743

申请日：1989-01-09

申请人： Takao Takaya ,  Hisashi Takasugi ,  Kimio Esumi ,  Atsushi Kuno ,  Hiroyoshi Sakai ,  Kazuhiro Maeda ,  Yoshie Sakamoto

发明人： Takao Takaya ,  Hisashi Takasugi ,  Kimio Esumi ,  Atsushi Kuno ,  Hiroyoshi Sakai ,  Kazuhiro Maeda ,  Yoshie Sakamoto

IPC分类号： C07D213/26 ,  C07D213/30 ,  C07D213/36 ,  C07D213/75 ,  C07D213/80 ,  C07D213/82 ,  C07D237/08 ,  C07D237/24 ,  C07D413/12 ,  C07D471/04 ,  C07D401/12 ,  A61K31/44

CPC分类号： C07D213/30 ,  C07D213/26 ,  C07D213/36 ,  C07D213/75 ,  C07D213/80 ,  C07D213/82 ,  C07D237/08 ,  C07D237/24 ,  C07D413/12 ,  C07D471/04

摘要： The invention relates to a pharmaceutical composition as a therapeutic agent for ischemic disease comprising a compound of the formula ##STR1## wherein R.sup.1 is carbamoyl substituted with morpholino (lower) alkyl, thiomorpholino(lower)alkyl or lower alkylamino(lower)alkyl; or ureido substituted with lower alkylamino(lower)alkyl; andR.sup.2 is phenyl substituted with nitro, andR.sup.4 is lower alkyl; orR.sup.2 is lower alkyl, andR.sup.4 is phenyl substituted with nitro;with proviso that R.sup.1 is carbamoyl substituted with thiomorpholino(lower)alkyl or lower alkylamino(lower)alkyl; or ureido substituted with lower alkylamino(lower)alkyl when R.sup.4 is lower alkyl; or its salt, as an active ingredient, in association with a pharmaceutically acceptable, substantially nontoxic carrier or excipient.

摘要翻译： 本发明涉及作为缺血性疾病治疗剂的药物组合物，其包含下式化合物其中R 1是被吗啉代（低级）烷基，硫代吗啉代（低级）烷基或低级烷基氨基（低级）烷基取代的氨基甲酰基） 或被低级烷基氨基（低级）烷基取代的脲基; R2是被硝基取代的苯基，R4是低级烷基; 或R 2为低级烷基，R 4为被硝基取代的苯基; 条件是R1是被硫代吗啉代（低级）烷基或低级烷基氨基（低级）烷基取代的氨基甲酰基; 或当R 4为低级烷基时被低级烷基氨基（低级）烷基取代的脲基; 或其盐作为活性成分，与药学上可接受的，基本上无毒的载体或赋形剂结合。

公开(公告)号：US4831030A

公开(公告)日：1989-05-16

申请号：US940923

申请日：1986-12-12

申请人： Hisashi Takasugi ,  Atsushi Kuno ,  Hiroyoshi Sakai ,  Yoshie Sugiyama ,  Takao Takaya

发明人： Hisashi Takasugi ,  Atsushi Kuno ,  Hiroyoshi Sakai ,  Yoshie Sugiyama ,  Takao Takaya

IPC分类号： C07D237/10 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/455 ,  A61K31/495 ,  A61K31/50 ,  A61K31/535 ,  A61K31/54 ,  A61P9/00 ,  A61P25/28 ,  C07D211/78 ,  C07D213/26 ,  C07D213/30 ,  C07D213/36 ,  C07D213/38 ,  C07D213/80 ,  C07D213/82 ,  C07D237/04 ,  C07D237/08 ,  C07D237/24 ,  C07D471/04

CPC分类号： C07D213/30 ,  C07D211/78 ,  C07D213/26 ,  C07D213/36 ,  C07D213/80 ,  C07D213/82 ,  C07D237/04 ,  C07D237/08 ,  C07D237/24 ,  C07D471/04

摘要： The invention relates to compounds for treatment of hypertension, and cardiovascular and cerebrovascular diseases, which compounds are of the formula: ##STR1## wherein R.sup.1 is piperazinyl(lower)alkyl, carbamoyl substituted with piperazinyl(lower)alkyl, or piperazinylcarbonyl, in each of which a piperazinyl group may be substituted with lower alkyl, andR.sup.3 is hydrogen or halogen;R.sup.2 is phenyl substituted with nitro, andR.sup.4 is lower alkyl or halo(lower)alkyl; orR.sup.2 is lower alkyl, andR.sup.4 is phenyl substitured with nitro;and a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及用于治疗高血压和心血管和脑血管疾病的化合物，其化合物具有下式：其中R 1是哌嗪基（低级）烷基，被哌嗪基（低级）烷基或哌嗪基羰基取代的氨基甲酰基， 哌嗪基可以被低级烷基取代，R3是氢或卤素; R2是被硝基取代的苯基，R4是低级烷基或卤代（低级）烷基; 或R2是低级烷基，R4是被硝基取代的苯基; 及其药学上可接受的盐。

公开(公告)号：US4822805A

公开(公告)日：1989-04-18

申请号：US084862

申请日：1987-08-13

申请人： Hisashi Takasugi ,  Kiyotaka Ito ,  Shigetaka Nishino ,  Akito Tanaka ,  Takao Takaya

发明人： Hisashi Takasugi ,  Kiyotaka Ito ,  Shigetaka Nishino ,  Akito Tanaka ,  Takao Takaya

IPC分类号： C07D401/04 ,  A61K31/44

CPC分类号： C07D401/04

摘要： A compound of the formula: ##STR1## wherein R.sup.1 is pyridyl,R.sup.2 is hydrogen, lower alkyl or hydroxy (lower) alkyl,R.sup.3 is hydrogen, hydroxy or lower alkyl, andR.sup.4 is aryl optionally substituted with substituent(s) selected from the group consisting of lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, nitro, amino, substituted amino, hydroxy, lower alkoxy, lower alkynyloxy, substituted or unsubstituted ar(lower)alkoxy, halogen, halo(lower)alkyl, carboxy and esterified carboxy,and a pharmaceutically acceptable salt thereof, processes for the preparation thereof and pharmaceutical composition comprising the same.

公开(公告)号：US4596829A

公开(公告)日：1986-06-24

申请号：US571488

申请日：1984-01-17

申请人： Takao Takaya ,  Hisashi Takasugi ,  Masayoshi Murata ,  Akiteru Yoshioka

发明人： Takao Takaya ,  Hisashi Takasugi ,  Masayoshi Murata ,  Akiteru Yoshioka

IPC分类号： C07D277/20 ,  C07D277/38 ,  C07D277/40 ,  C07D277/46 ,  C07D501/20 ,  C07D501/22 ,  C07D501/36 ,  C07D501/59 ,  A61K31/545

CPC分类号： C07D277/587

摘要： This invention relates to novel 7-acylaminocephalosporanic acid derivatives and pharmaceutically acceptable salts thereof, of high antimicrobial activity, said novel derivatives having the formula ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is carboxy(lower)alkyl, protected carboxy(lower)alkyl, carboxy(lower)alkenyl, protected carboxy(lower)alkenyl, or lower unsaturated aliphatic hydrocarbon,R.sup.3 is hydrogen, halogen, methyl, lower alkoxy, lower alkylthiomethyl, lower alkanoyloxymethyl or a heterocyclicthiomethyl which may have suitable substituents,R.sup.4 is carboxy or protected carboxy,R.sup.5 is hydrogen or lower alkyl, andX is halogen,provided that when R.sup.3 is lower alkanoyloxymethyl, then R.sup.2 is lower unsaturated aliphatic hydrocarbon, and pharmaceutically acceptable salts thereof.

公开(公告)号：US4507293A

公开(公告)日：1985-03-26

申请号：US504428

申请日：1983-06-15

申请人： Takao Takaya ,  Hisashi Takasugi ,  Toshiyuki Chiba ,  Kiyoshi Tsuji

发明人： Takao Takaya ,  Hisashi Takasugi ,  Toshiyuki Chiba ,  Kiyoshi Tsuji

IPC分类号： C07D501/20 ,  C07D501/59

CPC分类号： C07D501/59

摘要： The invention relates to novel cephem compounds, of antimicrobial activity, of the formula ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.3 is lower alkoxy, andR.sup.4 is carboxy or protected carboxy,and a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及抗微生物活性的新颖的头孢烯化合物，其中R1是氨基或被保护的氨基，R2是羧基（低级）烷基或被保护的羧基（低级）烷基，R3是低级烷氧基，R4是羧基 或保护的羧基及其药学上可接受的盐。

公开(公告)号：US4496562A

公开(公告)日：1985-01-29

申请号：US447218

申请日：1982-12-06

申请人： Takao Takaya ,  Hisashi Takasugi ,  Kiyoshi Tsuji ,  Toshiyuki Chiba

发明人： Takao Takaya ,  Hisashi Takasugi ,  Kiyoshi Tsuji ,  Toshiyuki Chiba

IPC分类号： C07D277/20 ,  C07D285/06 ,  C07D501/20 ,  C07D501/22 ,  A61K31/545

CPC分类号： C07D277/20 ,  C07D285/06 ,  C07D501/20

摘要： There are disclosed compounds of the formula: ##STR1## in which R is lower alkoxycarbonyloxy(lower)alkyl or 1-propionyloxyethyl, or a salt thereof, pharmaceutical compositions containing the same and their use to treat infectious diseases.

摘要翻译： 公开了下式的化合物：其中R是低级烷氧基羰氧基（低级）烷基或1-丙酰氧基乙基或其盐，含有它们的药物组合物及其治疗感染性疾病的用途。

公开(公告)号：US4477447A

公开(公告)日：1984-10-16

申请号：US351858

申请日：1982-02-24

申请人： Ikuo Ueda ,  Tsutomu Teraji ,  Takao Takaya ,  Keiji Takai ,  Hisashi Takasugi ,  Fumio Shimojo ,  Shigetaka Nishino

发明人： Ikuo Ueda ,  Tsutomu Teraji ,  Takao Takaya ,  Keiji Takai ,  Hisashi Takasugi ,  Fumio Shimojo ,  Shigetaka Nishino

IPC分类号： A61K20060101 ,  A61K31/545 ,  C07D20060101 ,  C07D501/14 ,  C07D501/16 ,  C07D501/20 ,  C07D501/22 ,  C07D501/46 ,  C07D501/60

CPC分类号： C07D501/20

摘要： This invention relates to novel 7-acylaminocephalosporanic acid derivatives of high antimicrobial activity, to processes for their preparation, and to pharmaceutical compositions comprising said derivatives, said derivatives being of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is dialkanoyloxy(lower)alkyl; alkyl having one or more substituents selected from the group consisting of hydroxy, protected hydroxy, alkoxy, carboxy, protected carboxy, cycloalkylcarbonyloxy and heterocyclic group; lower alkoxycarbonyloxy(lower)alkyl; azido(lower)alkoxycarbonyloxy(lower)alkyl; aroyloxy(lower)alkyl; higher alkanoyloxy(lower)alkyl; phthalidyl; or phthalidylidene(lower)alkyl,R.sup.3 is lower alkyl,Y is thio (--S--) or sulfinyl (--S--), and the dotted line represents 2- or 3-cephem nuclei.

摘要翻译： 本发明涉及高抗微生物活性的新型7-酰基氨基头孢烷酸衍生物及其制备方法，以及包含所述衍生物的药物组合物，所述衍生物具有下式：其中R1是氨基或被保护的氨基，R2是二烷酰氧基 （低级）烷基; 具有一个或多个选自羟基，保护的羟基，烷氧基，羧基，保护的羧基，环烷基羰基氧基和杂环基的取代基的烷基; 低级烷氧基羰氧基（低级）烷基; 叠氮基（低级）烷氧基羰氧基（低级）烷基; 芳氧基（低级）烷基; 高级烷酰氧基（低级）烷基; 苯酞; 或低级烷基，R 3为低级烷基，Y为硫代（-S-）或亚磺酰基（-S-），虚线表示2-或3-头孢烯核。