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1. 发明申请

WO1998002431A1 cis-SUBSTITUTED AMINOCYCLOPROPANE DERIVATIVES 审中-公开
标题翻译：顺式取代的氨基羰基衍生物
公开(公告)号：WO1998002431A1
公开(公告)日：1998-01-22
申请号：PCT/JP1997002411
申请日：1997-07-11
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , KIMURA, Youichi , TAKAHASHI, Hisashi , ISHIDA, Yohhei
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D207/26 , A61K31/4375 , A61K31/4709 , C07D207/24 , C07D401/04 , Y02A50/475
摘要： Antibacterial drugs exhibiting potent antibacterial effects against various bacteria and high safety, which comprise compounds of general formula (1), or salts of the compounds or hydrates thereof: wherein R and R are each hydrogen or alkyl; n is an integer of 1 to 3; R is alkyl, alkenyl, halogenoalkyl, cyclic alkyl, aryl, heteroaryl, alkoxyl or alkylamino; R is hydrogen or alkylthio; R is hydrogen, amino, hydroxyl, mercapto, halogenomethyl, alkyl, alkenyl, alkynyl or alkoxyl; X is halogeno or hydrogen; A is nitrogen or (II); X is hydrogen, amino, halogeno, cyano, halogenomethyl, halogenomethoxyl, alkyl, alkenyl, alkynyl or alkoxyl; and Y is hydrogen, phenyl, acetoxymethyl, pivaloyloxymethyl, ethoxycarbonyl, cholyl, dimethylaminoethyl, 5-indanyl, phthalidyl, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl, 3-acetoxy-2-oxobutyl, alkyl, alkoxymethyl or phenylalkyl.
摘要翻译：对各种细菌和高度安全性具有强效抗菌作用的抗菌药物，其包含通式（1）的化合物或其化合物或其水合物的盐：其中R 1和R 2各自为氢或烷基; n为1〜3的整数， R 3是烷基，烯基，卤代烷基，环烷基，芳基，杂芳基，烷氧基或烷基氨基; R 4是氢或烷硫基; R 5是氢，氨基，羟基，巯基，卤代甲基，烷基，烯基，炔基或烷氧基; X 1是卤代或氢; A是氮或（II）; X 2是氢，氨基，卤代，氰基，卤代甲基，卤代甲氧基，烷基，烯基，炔基或烷氧基; 并且Y是氢，苯基，乙酰氧基甲基，新戊酰氧基甲基，乙氧基羰基，取代基，二甲基氨基乙基，5-二氢化茚基，邻苯二甲酰基，5-烷基-2-氧代-1,3-二氧杂环戊烯-4-基甲基，3-乙酰氧基-2-氧代丁基，，烷氧基甲基或苯基烷基。

2. 发明申请

WO1998017625A1 NOVEL REMEDIES FOR INFECTIOUS DISEASES 审中-公开
标题翻译：感染性疾病的新措施
公开(公告)号：WO1998017625A1
公开(公告)日：1998-04-30
申请号：PCT/JP1997003812
申请日：1997-10-22
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , OHTA, Toshiharu , NAKAYAMA, Kiyoshi , OHTSUKA, Masami , INAGAKI, Hiroaki , NISHI, Toshiyuki , ISHIDA, Yohhei
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07C211/34
CPC分类号： C07D207/14 , C07C237/42
摘要： Novel compounds having three substituents in the cyclic partial structure thereof, such as a pyrrolidine or a benzene ring, for example, homophenylalanyl-trans-4-((S)-3-amino-2-hydroxypropionylamino)proline 5-indanylamide and N-(3-phenylpropyl)-3-((S)-2-hydroxy-3-aminopropionylamino)-5-(D-homophenylalanylamino)-benzamide. These compounds act on pathogenic microorganisms which have acquired tolerance to the existing antimicrobials and elevate the sensitivity to the antimicrobials, thus making them nontolerant. When used together with the antimicrobials, these compounds can efficaciously establish the prevention and/or treatment of microbial infectious diseases.
摘要翻译：具有其环状部分结构中的三个取代基的新型化合物，例如吡咯烷或苯环，例如高苯丙氨酰 - 反式-4 - （（S）-3-氨基-2-羟基丙酰基氨基）脯氨酸5-茚满酰胺和N- （3-苯基丙基）-3 - （（S）-2-羟基-3-氨基丙酰氨基）-5-（D-homophenylalanylamino） - 苯甲酰胺。这些化合物对已经获得对现有抗微生物剂的耐受性并提高对抗微生物剂的敏感性的致病微生物起作用，使其不耐受。当与抗微生物剂一起使用时，这些化合物可以有效地建立预防和/或治疗微生物感染性疾病。

3. 发明申请

WO1998014421A1 METHOD FOR ESTERIFYING CARBOXYLIC COMPOUNDS 审中-公开
标题翻译：用于酯化羧酸化合物的方法
公开(公告)号：WO1998014421A1
公开(公告)日：1998-04-09
申请号：PCT/JP1997003508
申请日：1997-10-01
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , NISHI, Toshiyuki , ISHIDA, Yohhei , OHTSUKA, Masami
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07C67/10
CPC分类号： C07D477/08 , C07C67/11
摘要： A method for esterifying carboxylic compounds, characterized by treating either a mixture of a carboxylic compound and a base or a salt of a carboxylic compound with a compound represented by the formula R -X (wherein R represents a group capable of forming a biodegradable ester (COOR ) and X represents a halogen atom) in a solvent in the presence of a phase transfer catalyst. The method can provide ester derivatives of carboxylic compounds at a low cost on a commercial scale.
摘要翻译：一种羧酸化合物的酯化方法，其特征在于用式R 1 -X表示的化合物处理羧酸化合物和羧酸化合物的碱或羧酸盐的混合物（其中R 1表示能够在相转移催化剂存在下，在溶剂中形成可生物降解的酯（COOR 1），X表示卤素原子）。该方法可以商业规模以低成本提供羧酸化合物的酯衍生物。

4. 发明申请

WO1993000344A1 CARBAPENEM DERIVATIVE 审中-公开
公开(公告)号：WO1993000344A1
公开(公告)日：1993-01-07
申请号：PCT/JP1992000790
申请日：1992-06-19
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , NISHI, Toshiyuki; , KODA, Hiroko; , SUGITA, Kazuyuki; , ISHIDA, Yohhei; , TAKEMURA, Makoto; , HAYANO, Takeshi;
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D477/00
CPC分类号： C07D477/20 , Y02P20/55
摘要： Known carbapenem derivatives such as thienamycin have disadvantages that they are physicochemically unstable and readily decomposed by enzymes such as DHP of the kidney to bring about adverse effects such as nephrotoxicity, while 1- beta -methylcarbapenem compounds are stable and have potent antibacterial activities but are yet unsatisfactory as regards the stability and antibacterial activity against DHP. Under these circumstances the invention provides an antibiotic represented by general formula (I) which has a potent antibacterial activity against various bacteria including Pseudomonas aeruginosa and is excellent in safety and stable against hydrolases such as DHP, and a salt thereof (I), wherein R represents lower alkyl or optionally protected hydroxy lower alkyl; R , R and R represent each hydrogen or lower alkyl; R represents optionally esterified carboxyl; R , R , R and R represent each an amino-protective group, hydrogen or lower alkyl; R , R , R and R represent each hydrogen, hydroxyl, lower alkyl, hydroxy lower alkyl or halogen, or alternatively R and R and/or R and R may combine together to form alkylene; R represents hydrogen, lower alkyl, carboxyl, carbamoyl or -CONR R ; R and R represent each hydrogen or lower alkyl; R represents hydrogen, lower alkyl or hydroxy lower alkyl, or alternatively R may combine with R to form alkylene; Z represents a single bond, oxygen, sulfur, -CR R -, -NR CO-, -CONR - or -NR -; and m and n represent each an integer of 0 to 6.
摘要翻译：已知的碳青霉烯类衍生物如噻吩霉素具有缺点，它们在物理化学上不稳定，并易于被诸如肾脏的DHP之类的酶分解以产生不利影响如肾毒性，而1-β-甲基碳青霉烯化合物是稳定的并且具有有效的抗菌活性关于对DHP的稳定性和抗菌活性不令人满意。在这些情况下，本发明提供了一种通式（I）表示的抗生素，其对包括绿脓假单胞菌在内的各种细菌具有有效的抗菌活性，并且对于水解酶例如DHP及其盐（I）的安全性和稳定性优异，其中R 1表示低级烷基或任选保护的羟基低级烷基; R 2，R 13和R 14各自代表氢或低级烷基; R 3表示任选酯化的羧基; R 4，R 9，R 10和R 15各自表示氨基保护基，氢或低级烷基; R 5，R 6，R 11和R 12分别表示氢，羟基，低级烷基，羟基低级烷基或卤素，或者R 5和R 6和/ 11>和R 12可以结合在一起形成亚烷基; R 7表示氢，低级烷基，羧基，氨基甲酰基或-CONR 71 R 72; R 71和R 72表示氢或低级烷基; R 8表示氢，低级烷基或羟基低级烷基，或者R 8可与R 7结合形成亚烷基; Z表示单键，氧，硫，-CR 11 R 12 - ， - NR 13 CO - ， - CONR 14 - 或-NR 15 - 。 m和n表示0〜6的整数。

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