NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS
    21.
    发明申请
    NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS 审中-公开
    新型半合成糖苷作为抗菌剂

    公开(公告)号:US20110015119A1

    公开(公告)日:2011-01-20

    申请号:US12552221

    申请日:2009-09-01

    CPC classification number: C07K9/008 A61K38/00 A61K45/06

    Abstract: Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Key reaction is the treatment of properly protected intermediate compound with isocyanate. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

    Abstract translation: 具体描述了具有抗菌活性的半合成糖肽,特别是本文所述的半合成糖肽通过化学修饰糖肽(化合物A,化合物B,化合物H或化合物C)或通过水解二糖部分 在酸性介质中母体糖肽的氨基酸-4得到氨基酸-4单糖; 单糖转化为氨基糖衍生物; 在这些支架上的氨基酸4氨基取代的糖部分上的氨基取代基被某些酰基酰化; 并将这些支架的大环上的酸部分转化为某些取代的酰胺。 关键反应是用异氰酸酯处理适当保护的中间体化合物。 还提供了合成化合物的方法,含有该化合物的药物组合物,以及该化合物用于治疗和/或预防疾病,特别是细菌感染的方法。

    Dual mode negative voltage switching
    23.
    发明授权
    Dual mode negative voltage switching 有权
    双模负压开关

    公开(公告)号:US07570466B2

    公开(公告)日:2009-08-04

    申请号:US11069175

    申请日:2005-03-01

    Applicant: Daniel Chu

    Inventor: Daniel Chu

    CPC classification number: G11C16/30 H03K17/102 Y10T307/74

    Abstract: A negative switch may enable switching of two different negative voltages. The switch may include a negative cascode bias generator which biases the gate of a cascade protection device. When the negative switch is passing a large negative voltage, the bias generator generates a lowered voltage to provide a cascade voltage for snapback protection of a passing transistor. When a relatively low negative voltage is to be switched, the bias generator may produce a positive voltage greater than the threshold voltage of the cascode protection device so that both high and low negative voltages may be switched by the same circuit without exposing the passing device to a voltage in excess of its snapback limit.

    Abstract translation: 负开关可以实现两个不同负电压的切换。 开关可以包括偏置级联保护装置的栅极的负共源共栅偏压发生器。 当负开关通过大的负电压时,偏置发生器产生降低的电压,以提供级联电压以用于通过晶体管的快速保护。 当要切换相对较低的负电压时,偏置发生器可以产生大于共源共栅保护装置的阈值电压的正电压,使得高电压和低负电压都可以由同一电路切换,而不会使经过的装置暴露于 超过其回跳限制的电压。

    Guanidino compounds
    24.
    发明授权
    Guanidino compounds 失效
    胍基化合物

    公开(公告)号:US07456183B2

    公开(公告)日:2008-11-25

    申请号:US10474331

    申请日:2002-04-08

    Abstract: Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH2, N, NR9, C═O, C═S, S═O, SO2, S, O, (CR6R7)n, C(═O)—(CR6R7)n, and C(═S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S═O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.

    Abstract translation: 提供具有一般结构I的化合物。 X和Y独立地选自CH 2,N,NR 9,CO,CS,SO,SO 2,S ,(O) - (CR 6),(O) - (CR 6) C(-S) - (CR 6 R 7)N ,和C(-S) - (CR 6) 其中n为1,2或3.W选自(式I),L选自N,O,SO,SO 2, C(O),NC(O),NC(S),OC(O),OC(S),C(NR 10) ,和共价键。 Z 1,Z 2,Z 3和Z 3独立地选自取代的碳和氮。 式I化合物是黑皮质素-4受体(“MC-4r2”)的激动剂,因此可能具有控制人类MC-4r作用相关疾病如肥胖和II型糖尿病的有用性质。

    Semi-synthetic rearranged vancomycin/desmethyl-vancomycin-based glycopeptides with antibiotic activity
    25.
    发明授权
    Semi-synthetic rearranged vancomycin/desmethyl-vancomycin-based glycopeptides with antibiotic activity 失效
    半合成重组万古霉素/脱甲基万古霉素类糖肽具有抗菌活性

    公开(公告)号:US07368422B2

    公开(公告)日:2008-05-06

    申请号:US11361311

    申请日:2006-02-24

    CPC classification number: C07K9/008

    Abstract: Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of a rearranged vancomycin or desmethyl-vancomycin scaffold, in particular, alkylation or acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

    Abstract translation: 具有抗菌活性的半合成糖肽基于重排的万古霉素或去甲基 - 万古霉素支架的修饰,特别是在该支架上的具有某些酰基的氨基取代的糖部分上的氨基取代基的烷基化或酰化; 和/或将该支架的大环上的酸部分转化为某些取代的酰胺。 还提供了合成化合物的方法,含有化合物的药物组合物,以及用于治疗和/或预防疾病,特别是细菌感染的化合物的使用方法。

    Balancing Means for High-Speed Scanning
    26.
    发明申请
    Balancing Means for High-Speed Scanning 有权
    平衡高速扫描的手段

    公开(公告)号:US20070272878A1

    公开(公告)日:2007-11-29

    申请号:US11694105

    申请日:2007-03-30

    CPC classification number: G01N21/253 B01L7/52 G01N2201/101

    Abstract: Translational motion of a scanning head relative to a planar target, or vice versa, is achieved by a belt and pulley system with a counterweight that is also driven by a belt and pulley system at the same speed but in the opposite direction as the scanning head. The components and belt and pulley system are oriented such that all moving components remain on one side of the target and remain so during their entire range of movement.

    Abstract translation: 扫描头相对于平面目标的平移运动,反之亦然,通过皮带和皮带轮系统来实现,该带和滑轮系统具有配重,该配重也由皮带和滑轮系统以与扫描头相同的速度但与之相反的方向驱动 。 部件和皮带轮系统被定向成使得所有移动部件保持在目标的一侧并且在其整个移动范围内保持。

    Moving coil actuator for reciprocating motion with controlled force distribution

    公开(公告)号:US20070096568A1

    公开(公告)日:2007-05-03

    申请号:US11265000

    申请日:2005-11-01

    CPC classification number: H02K33/18

    Abstract: A moving coil actuator that moves in a rapid back-and-forth motion is constructed with a magnet assembly that concentrates the magnetic flux in a region of limited length and with a coiled electric conductor that includes two separated regions of densely wound coil, the assembly and conductor arranged such that only one of the coil regions resides in a concentrated flux region at either end of the actuator stroke. This is achieved with either a single region of concentrated flux or two spatially separated regions of concentrated flux. In either case, the force constant, i.e., the motor force generated in each coil per unit of current through the coil, is non-linear, with a maximal force at each end of the stroke and a minimal force at the stroke mid-point. The result is an efficient use of the electric current and relatively small amounts of materials of construction, and accordingly less weight for the actuator to carry during its travel and its changes of direction.

    Bias selection
    28.
    发明申请
    Bias selection 有权
    偏见选择

    公开(公告)号:US20060202740A1

    公开(公告)日:2006-09-14

    申请号:US11076970

    申请日:2005-03-11

    CPC classification number: G11C29/12 G05F3/205 G11C5/147 G11C29/12005

    Abstract: One or more MOS devices may be used as a bias selecting circuit to pass a bias voltage from a bias generator to a level shifting circuit.

    Abstract translation: 一个或多个MOS器件可以用作偏置选择电路,以将偏置电压从偏置发生器传递到电平移位电路。

    Stress tolerant high voltage back-to-back switch

    公开(公告)号:US20060001480A1

    公开(公告)日:2006-01-05

    申请号:US10883361

    申请日:2004-06-30

    CPC classification number: H03K19/00315 H03K17/04206 H03K17/102 H03K19/09441

    Abstract: Methods and apparatuses associated with stepping down a high voltage in a high voltage switch. An additional transistor may be coupled to a switching transistor, and the additional transistor biased to a voltage level in between the high voltage to be switched and a switch reference voltage. When the switch is off, the high voltage may thus be spread across multiple devices to prevent a voltage from the gate to the drain to exceed a threshold associated with gate-aided breakdown of the drain-to-substrate channel-side pn-junction.

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