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1. 发明申请

WO1992004342A1 A NOVEL QUINOLONE CARBOXYLIC ACID DERIVATIVE 审中-公开
标题翻译：一种新型的喹啉酮羧酸衍生物
公开(公告)号：WO1992004342A1
公开(公告)日：1992-03-19
申请号：PCT/KR1991000018
申请日：1991-08-14
申请人： DAEWOONG PHARMACEUTICAL CO., LTD. , YOON, Geal, Jung , KIM, Dae, Young , LEE, Jae, Wook , PARK, Nam, Jun , LEE, Kyeu, Sam , KANG, Tae, Choong
发明人： DAEWOONG PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D207/08 , C07D205/04 , C07D211/54 , C07D401/04 , C07D401/12 , C07D401/14
摘要： The present invention relates to a novel quinolone carboxylic acid derivative of structural formula (I) and pharmaceutically acceptable salts thereof. These compounds also have a potent activity against both Gram-positive bacteria and Gram-negative bacteria; wherein R is hydrogen or alkyl group having one to six carbon atoms, R is alkyl group having one to four carbon atoms, haloalkyl group having one to four carbon atoms, cycloalkyl group having three to six carbon atoms, alkenyl group having two to four carbon atoms, or phenyl group which is optionally mono or disubstituted by fluorine atoms, X is hydrogen, amino, or halogen, Y is hydrogen or halogen, Z is (II) (wherein l is 1 or 2, m is 0, 1, or 2, and n is 0 or 1, R is hydrogen, alkyl group having one to four carbon atoms, haloalkyl group having one to three carbon atoms, acyl group, cycloalkyl group having three to six carbon atoms, aryl, or heteroaryl group).
摘要翻译：本发明涉及结构式（I）的新型喹诺酮羧酸衍生物及其药学上可接受的盐。这些化合物对革兰氏阳性菌和革兰氏阴性细菌都具有很强的活性; 其中R 1为氢或具有1至6个碳原子的烷基，R 2为具有1至4个碳原子的烷基，具有1至4个碳原子的卤代烷基，具有3至6个碳原子的环烷基，具有2至4个碳原子的基团，或任选被氟原子单取代或二取代的苯基，X为氢，氨基或卤素，Y为氢或卤素，Z为（II）（其中l为1或2，m 是0,1或2，n为0或1，R 3为氢，具有1至4个碳原子的烷基，具有1至3个碳原子的卤代烷基，酰基，具有3至6个碳原子的环烷基原子，芳基或杂芳基）。

2. 发明申请

WO1992000981A1 NOVEL 3-SUBSTITUTED CEPHEM COMPOUNDS AND PROCESSES FOR PREPARATION THEREOF 审中-公开
标题翻译：新型3-取代的CEPHEM化合物及其制备方法
公开(公告)号：WO1992000981A1
公开(公告)日：1992-01-23
申请号：PCT/KR1991000012
申请日：1991-04-19
申请人： DAE WOONG PHARMACEUTICAL CO., LTD. , MOON, Chi, Jang , PARK, Sae, Choong , KIM, Myoung, Goo , OH, Sea, Han , YIM, Seong, Soo , PARK, Nam, Jun , CHOI, Young, Key , SUNG, Moo, Je
发明人： DAE WOONG PHARMACEUTICAL CO., LTD.
IPC分类号： C07D501/24
CPC分类号： C07D501/00 , Y02P20/55
摘要： The present invention relates to novel cephalosporins of formula (I), wherein R1 represents A C1 SIMILAR C4 alkyl group or ( alpha ), wherein R2 and R3, independently, represent hydrogen or a C1 SIMILAR C3 alkyl group and R4 represents hydrogen or a C1 SIMILAR C4 alkyl group; R1a represents hydrogen or an amino-protecting group; Q represents CH or N; and formula ( beta ) represents a saturated or unsaturated heterocyclic group which contains 1 to 4 nitrogen atoms of which one is substituted with an amino group to form quaternary ammonium, and oxygen or sulfur, or a fused heterocyclic group thereof formed together with a substituted or unsubstituted benzene or an optional heterocyclic group, or a pharmaceutically acceptable salt thereof, to processes for preparing the same and to a pharmaceutical composition containing the same as an active ingredient. The compounds (I) according to the invention exhibit potent antibacterial activity and broad antibacterial spectrum against the Gram-positive strains including Staphylococcus as well as Gram-negative strains including Pseudomonas, and, therefore, are expected to be very useful in treatment of various diseases caused by bacterial infection in human beings and animals.
摘要翻译：本发明涉及式（I）的新型头孢菌素，其中R 1表示C 1 -C 4 C 4烷基或（α），其中R 2和R 3独立地表示氢或C 1 -C 3烷基，R 4表示氢或C 1 类似C4烷基; R 1a表示氢或氨基保护基; Q表示CH或N; 式（β）表示含有1〜4个氮原子的饱和或不饱和杂环基，其中一个被氨基取代形成季铵，并且氧或硫或稠合杂环基与取代或未取代的苯或任选的杂环基，或其药学上可接受的盐，其制备方法和含有该活性成分的药物组合物。根据本发明的化合物（I）对革兰氏阳性菌株（包括葡萄球菌）以及革兰氏阴性菌株（包括假单胞菌属）表现出强大的抗菌活性和广谱抗菌谱，因此预期在治疗各种疾病中非常有用由人类和动物的细菌感染引起。

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