公开(公告)号：US06297248B1

公开(公告)日：2001-10-02

申请号：US09284019

申请日：1999-04-06

申请人： Tetsuo Shimamoto ,  Hidekazu Inoue ,  Yasuhiro Hayashi

发明人： Tetsuo Shimamoto ,  Hidekazu Inoue ,  Yasuhiro Hayashi

IPC分类号： A61K314375

CPC分类号： C07D471/04

摘要： A 1-aryl-1,8-naphthylidin-4-one derivative having the formula (I): wherein R1 indicates a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group, R2, R3, and R4 independently indicate a hydrogen atom, a substituted or unsubstituted lower alkyl group, or a halogen atom, X indicates a group NR5R6 or a group OR7, wherein R5 and R6 independently indicate a hydrogen a atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group, and R7 indicates a hydrogen atom, a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted cycloalkyl group or a salt or solvate thereof and a type IV phosphodiesterase inhibitor containing the same as an effective component.

摘要翻译： 具有式（I）的1-芳基-1,8-二氮杂萘-4-酮衍生物：其中R 1表示取代或未取代的芳基或取代或未取代的杂芳基，R 2，R 3和R 4独立地表示氢原子 取代或未取代的低级烷基或卤素原子，X表示基团NR5R6或基团OR7，其中R5和R6独立地表示氢原子，取代或未取代的低级烷基，取代或未取代的环烷基， 取代或未取代的芳基或取代或未取代的杂芳基，R7表示氢原子，取代或未取代的低级烷基或取代或未取代的环烷基或其盐或溶剂化物，以及含有 与有效成分相同。

公开(公告)号：US6114909A

公开(公告)日：2000-09-05

申请号：US863844

申请日：1997-05-27

申请人： Fukuji Anzai ,  Hidekazu Inoue

发明人： Fukuji Anzai ,  Hidekazu Inoue

IPC分类号： H03F3/45

CPC分类号： H03F3/45479 ,  H03F3/45071

摘要： A differential amplifier (24) includes a pair of transistors (Q2 and Q9); a differential amplifier 25 includes a pair of transistors (Q3 and Q6). A difference in output currents at the differential amplifier (24) is detected by differential amplifier (25). Then, transistors (Q3 and Q6) in differential amplifier (25) supply currents flowing therein into transistors (Q4 and Q5), whose bases are connected to each other via a capacitor (26). With this arrangement, a difference in DC components between a pair of differential currents flowing in the differential amplifier (25) is obtained at both terminals of the capacitor (26). The obtained voltages at the both terminals of the capacitor (26) are fed back to the input of the differential amplifier (24) via transistors (Q1 and Q8), so that offsets at inputs of the differential amplifier (24) are corrected.

摘要翻译： 差分放大器（24）包括一对晶体管（Q2和Q9）; 差分放大器25包括一对晶体管（Q3和Q6）。 差分放大器（24）的输出电流差由差分放大器（25）检测。 然后，差分放大器（25）中的晶体管（Q3和Q6）将流过其中的电流供给到其基极经由电容器彼此连接的晶体管（Q4和Q5）。 通过这种布置，在电容器（26）的两个端子处获得在差分放大器（25）中流动的一对差分电流之间的DC分量的差异。 通过晶体管（Q1和Q8）将电容器（26）的两端的获得的电压反馈到差分放大器（24）的输入，从而校正差分放大器（24）的输入端的偏移。

公开(公告)号：US6051569A

公开(公告)日：2000-04-18

申请号：US911937

申请日：1997-08-15

申请人： Masaji Ishiguro ,  Takashi Nakatsuka ,  Hidekazu Inoue

发明人： Masaji Ishiguro ,  Takashi Nakatsuka ,  Hidekazu Inoue

IPC分类号： C07D477/00 ,  A61K31/397 ,  A61K31/40 ,  A61P31/04 ,  C07D477/08 ,  C07D477/20

CPC分类号： C07D477/08 ,  C07D477/20 ,  Y02P20/55

摘要： A carbapenem derivative represented by the following formula (I), ##STR1## wherein R.sub.1 represents a hydrogen atom, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, R.sub.2 indicates a hydrogen atom or a protective group for a carboxyl group, and R.sub.3 is a methyl group or an ethyl group; or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising this carbapenem derivative or a salt thereof as an active ingredient. The carbapenem derivative exhibits a wide and strong antimicrobial activity, particularly a strong antimicrobial activity against MRSA. An intermediate compound for preparing the carbapenem derivative is also disclosed.

摘要翻译： 由下式（I）表示的碳青霉烯衍生物，其中R1表示氢原子，取代或未取代的芳基或取代或未取代的杂环基，R2表示氢原子或羧基保护基，R3 是甲基或乙基; 或其药学上可接受的盐，以及包含该碳青霉烯衍生物或其盐作为活性成分的药物组合物。 碳青霉烯衍生物具有广泛而强的抗微生物活性，特别是抗MRSA的强抗微生物活性。 还公开了用于制备碳青霉烯衍生物的中间体化合物。