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    • 1. 发明申请
    • CARBAPENEM DERIVATIVE
    • WO1993000344A1
    • 1993-01-07
    • PCT/JP1992000790
    • 1992-06-19
    • DAIICHI PHARMACEUTICAL CO., LTD.NISHI, Toshiyuki;KODA, Hiroko;SUGITA, Kazuyuki;ISHIDA, Yohhei;TAKEMURA, Makoto;HAYANO, Takeshi;
    • DAIICHI PHARMACEUTICAL CO., LTD.
    • C07D477/00
    • C07D477/20Y02P20/55
    • 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.
    • 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。
    • 2. 发明专利
    • ROAD MARKING
    • JP2000120028A
    • 2000-04-25
    • JP15994299
    • 1999-04-28
    • HAYANO TAKESHI
    • HAYANO TAKESHI
    • E01F9/00E01F9/518E01F9/576E01F9/04
    • PROBLEM TO BE SOLVED: To improve the visibility of a driver by coating the centers of a road marking, a center line or a no-passing line with different colors in response to travel-speed control values. SOLUTION: The center of a road is coated with a white center line or no-passing lines 10 while the center of the center line or the no-passing lines 10 is coated with a travel-speed control-value marking line 12 marking travel- speed control values by colors. The travel-speed control value 12 is formed of red at the time of the travel-speed control value of 40 km/h, green at the time of 50 km/h and a sky blue at the time of 60 km/h. The width A of the center line or the no-passing lines 10 is set generally in 0.15 m, but the width B of the travel-speed control-value marking line 12 is set typically in approximately 0.005 m. The travel-speed control-value marking line 12 may be applied simultaneously by adding an each-color coater to an overhead type airless line marker at the time of the application of the center line or the no-passing lines 10. Accordingly, a driver can recognize the travel-speed control values instantaneously by viewing, and the overlooking of the travel-speed control values is prevented.