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    • 2. 发明授权
    • Aminomethylpyrrolidine derivatives having aromatic substituents
    • 具有芳香取代基的氨基甲基吡咯烷衍生物
    • US06762181B1
    • 2004-07-13
    • US09936050
    • 2001-09-07
    • Makoto TakemuraHisashi TakahashiKatsuhiro KawakamiToshiyuki TakedaRie Miyauchi
    • Makoto TakemuraHisashi TakahashiKatsuhiro KawakamiToshiyuki TakedaRie Miyauchi
    • A61K314375
    • C07D401/04C07D405/14
    • This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both. In the formula, R2, R3: hydrogen atom, an alkyl group; R4, R5, R6: hydrogen atoms, hydroxyl group, a halogen atom, carbamoyl group, an alkyl group, an alkoxyl group, an alkylthio group; R7, R8: hydrogen atom, an alkyl group; R9: an alkyl group, an alkenyl group, a halogenoalkyl group, a cyclic alkyl group, an aryl group, a heteroaryl group, an alkoxyl group having from 1 to 6 carbon atoms, an alkylamino group; R10: hydrogen atom, an alkylthio group; R11: hydrogen atom, amino group, hydroxyl group, thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; X1: halogen atom, a hydrogen atom; A1: nitrogen atom, C—X2; X2: hydrogen atom, amino group, a halogen atom, cyano group, an halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; A2, A3: >C═C(—A1═)—N(—R9)—, >N—C(—A1═)═C(—R9)—; R10 and R9 or R9 and X2 may be integrated to form a ring structure; and Y: hydrogen atom, ester forming group.
    • 本发明提供了一种喹诺酮衍生物,其具有对各种细菌的抗菌活性,包括耐药菌株,其为下式的化合物,其中R 1为任选取代的芳族基团,其两者的盐或两者的水合物。 式R 2,R 3:氢原子,烷基; R 4,R 5,R 6:氢原子,羟基,卤素原子,氨基甲酰基,烷基,烷氧基,烷硫基; R 7,R 8:氢原子,烷基; R 9:烷基,烯基,卤代烷基,环状烷基,芳基,杂芳基,碳原子数1〜6的烷氧基,烷基氨基, R 10:氢原子,烷硫基; R 11:氢原子,氨基,羟基,硫醇基,卤代甲基,烷基,烯基,炔基,烷氧基; X 1:卤素原子,氢原子; A 1:氮原子,C-X 2; X 2:氢原子,氨基,卤原子,氰基,卤代甲基,卤代甲氧基,烷基,烯基,炔基,烷氧基; A 2,A 3:C = C(-A 1 =)-N(-R 9) - ,> NC(-A 1)= C(-R 9) >) - ; R 10和R 9或R 9和X 2可以一体形成环结构; 和Y:氢原子,酯形成基团。
    • 3. 发明授权
    • Cis-substituted fluoromethylpyrrolidine derivative
    • 顺式取代的氟甲基吡咯烷衍生物
    • US06656952B2
    • 2003-12-02
    • US09446696
    • 1999-12-23
    • Makoto TakemuraHisashi TakahashiHitoshi OhkiKenichi KimuraRie MiyauchiToshiyuki Takeda
    • Makoto TakemuraHisashi TakahashiHitoshi OhkiKenichi KimuraRie MiyauchiToshiyuki Takeda
    • A61K3147
    • C07D401/04
    • An antibacterial drug having potent antibacterial activities upon various bacteria including resistant strains and high safety is disclosed, which comprises as an active ingredient, quinolone derivatives represented by the following formula (I), its salts or hydrates thereof: wherein R1 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, R2 represents a halogenomethoxyl group or an alkoxyl group, R3 represents an alkyl group, an alkenyl group, a halogenoalkyl group, a cyclic alkyl group, a heteroaryl group, an alkoxyl group or an alkylamino group, and R4 represents a hydrogen atom, a phenyl group, an acetoxymethyl group, a pivaloyloxymethyl group, an ethoxycarbonyl group, a choline group, a dimethylaminoethyl group, a 5-indanyl group, a phthalidinyl group, a 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, 3-acetoxy-2-oxobutyl group, an alkyl group, an alkoxylmethyl group or a phenylalkyl group. These substituents may further have additional substituents.
    • 本发明公开了一种对各种细菌(包括耐药菌株)和高度安全性具有有效抗菌活性的抗菌药物,其包含作为活性成分的由下式(I)表示的喹诺酮衍生物,其盐或水合物:其中R 1表示 氢原子或碳原子数1〜6的烷基,R 2表示卤代甲氧基或烷氧基,R 3表示烷基,链烯基,卤代烷基,环状烷基,杂芳基 基团,烷氧基或烷基氨基,R 4表示氢原子,苯基,乙酰氧基甲基,新戊酰氧基甲基,乙氧基羰基,胆碱基,二甲基氨基乙基,5-二氢化茚基, 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,烷基,烷氧基甲基或苯基烷基。 这些取代基还可以具有另外的取代基。
    • 4. 发明授权
    • Cycloalkyl-substituted aminomethylpyrrolidine derivatives
    • 环烷基取代的氨基甲基吡咯烷衍生物
    • US06573260B1
    • 2003-06-03
    • US09856631
    • 2001-05-24
    • Makoto TakemuraHisashi TakahashiRie MiyauchiToshiyuki TakedaIsao Hayakawa
    • Makoto TakemuraHisashi TakahashiRie MiyauchiToshiyuki TakedaIsao Hayakawa
    • A61K314709
    • C07D401/04
    • This invention provides a quinolone derivative which exerts strong antibacterial action upon various bacteria and has high safety, and it relates to a compound having a structure of formula (I), its salts and hydrates thereof: {R1 and R2: hydrogen, alkyl; n: 1 to 4; Q: following structure (Ia): [R3: alkyl, alkenyl, halogenoalkyl, cyclic alkyl, aryl, heteroaryl, alkoxyl, alkylamino; R4: hydrogen, alkylthio; R5: hydrogen, amino, hydroxyl, thiol, halogenomethyl, alkyl, alkenyl, alkynyl, alkoxyl; X1: halogen, hydrogen, A1: nitrogen, structure of formula (II): (X2: hydrogen, amino, halogen, cyano, halogenomethyl, halogenomethyl, alkyl, alkenyl, alkynyl, alkoxyl; R4 and R3 or X2 and R3 may together form a cyclic structure; Y: hydrogen, various ester forming groups]}.
    • 本发明提供了一种喹诺酮衍生物,其对各种细菌具有强烈的抗菌作用并具有高度的安全性,它涉及具有式(I)结构的化合物及其盐和水合物:{R1和R2:氢,烷基; n:1到4; Q:以下结构(Ia):[R3:烷基,烯基,卤代烷基,环烷基,芳基,杂芳基,烷氧基,烷基氨基; R4:氢,烷硫基; R5:氢,氨基,羟基,硫醇,卤代甲基,烷基,烯基,炔基,烷氧基; X1:卤素,氢,A1:氮,式(II)的结构:(X2:氢,氨基,卤素,氰基,卤代甲基,卤代甲基,烷基,烯基,炔基,烷氧基; R4和R3或X2和R3可以一起形成 环状结构; Y:氢,各种酯形成基团]}。
    • 10. 发明授权
    • Electronic circuit capable of stably keeping a frequency during presence
of a burst
    • 能够在存在突发时稳定地保持频率的电子电路
    • US4633510A
    • 1986-12-30
    • US687343
    • 1984-12-28
    • Fumiaki SuzukiToshiyuki TakedaTakeo InoueShigeo Nakajima
    • Fumiaki SuzukiToshiyuki TakedaTakeo InoueShigeo Nakajima
    • H03L7/14H04B1/40H04B7/15H04B7/155H04B1/00
    • H04B1/40H03L7/14
    • In a radio communication system, a transmitting section of a substation comprises a controlling circuit (21) for controlling a carrier frequency of a local oscillator (24) in response to a frequency deviation signal. A burst generating circuit (26) generates a burst in response to the input signal, a burst control signal, and a local oscillation signal of the carrier frequency. The transmitting section further comprises a holding circuit (34) responsive to a frequency control signal and the burst control signal. During presence of the burst control signal, the holding circuit holds the frequency control signal received before a beginning of the burst control signal to keep the carrier frequency of the local oscillation signal invariable until an end of the burst control signal. Otherwise, the frequency control signal passes through the holding circuit as it stands. Consequently, the carrier frequency of the local oscillation signal is controlled only during absence of the input signal and is kept invariable during presence of the input signal.
    • 在无线电通信系统中,变电站的发送部分包括用于响应于频率偏差信号来控制本地振荡器(24)的载波频率的控制电路(21)。 突发发生电路(26)响应于输入信号,脉冲串控制信号和载波频率的本地振荡信号产生脉冲串。 发送部分还包括响应于频率控制信号和突发控制信号的保持电路(34)。 在脉冲串控制信号的存在期间,保持电路保持在突发控制信号开始之前接收到的频率控制信号,以保持本地振荡信号的载波频率不变,直到脉冲串控制信号的结束。 否则,频率控制信号就一直通过保持电路。 因此,本地振荡信号的载波频率仅在没有输入信号的情况下被控制,并且在存在输入信号的过程中保持不变。