摘要:
An influenza virus neuraminidase inhibitor, its analogs, its pharmaceutically acceptable salts, derivatives, and mixtures thereof having the following formula: ##STR1## where A is CO.sub.2 H, CO.sub.2 H.sub.3, NO.sub.2, SO.sub.3 H or PO.sub.3 H.sub.2, B is CH, N, O or S, R.sub.1 and R.sub.2 are H, NO.sub.2 or (CH.sub.m).sub.n X.sub.1 where m=1 or 2, n is an integer from 0 to 4 and X.sub.1 is guanidino, OH, NH.sub.2, SH, NO.sub.2, F, Cl, Br, I, CN, CF.sub.3, CO.sub.2 H, SO.sub.3 H or PO.sub.3 H.sub.2, R.sub.3 and R.sub.4 are H, (CH.sub.o).sub.p X.sub.2, (CH.sub.o).sub.p CHX.sub.2 CH.sub.2 X.sub.2, NH(CH.sub.o).sub.p CHX.sub.2 CH.sub.2 X.sub.2, NHCO(CH.sub.o).sub.p CH.sub.2 X.sub.2 or NHCO(CH.sub.o).sub.p CHX.sub.2 CH.sub.2 X.sub.2 where o=1 or 2, p is an integer from 0 to 4 and X.sub.2 is H, guanidino, OH, NH.sub.2, SH, NO.sub.2, CF.sub.3, CO.sub.2 H, SO.sub.3 H or PO.sub.3 H.sub.2 , R.sub.5 =H, OH, NH.sub.2, (CH.sub.k).sub.1 X.sub.3, CO(CH.sub.k).sub.1 X.sub.3, SO(CH.sub.k).sub.1 X.sub.3 or SO.sub.2 (CH.sub.k).sub.1 X.sub.3 where k=1 or 2, 1 is an integer from 0 to 4 and X.sub.3 is guanidino, OH, NH.sub.2, SH, NO.sub.2, CF.sub.3, CO.sub.2 H, SO.sub.3 H or PO.sub.3 H.sub.2, R.sub.6 is H, CH(OH)X.sub.4, CH(NH.sub.2)X.sub.4, COX.sub.4, SOX.sub.4, or SO.sub.2 X.sub.4, where X.sub.4 is H, CH.sub.3, CH.sub.3 CH.sub.2, CH.sub.3 CHCH.sub.3, CH.sub.3 CH.sub.2 CH.sub.2 or halogen substituted analogs of X.sub.4. The inhibitor in a composition with a pharmaceutically acceptable carrier. A method of inhibiting influenza virus neuraminidase where the inhibitor is administered to a subject in a pharmaceutically acceptable amount along with effective amounts of a pharmaceutically acceptable carrier. Methods of marking a pharmaceutical composition of an acceptable carrier and the inhibitor. Methods of treating and preventing a subject infected with influenza virus (type A or B) using the inhibitor.
摘要翻译:流感病毒神经氨酸酶抑制剂,其类似物,其药学上可接受的盐,衍生物及其混合物具有下式:其中A是CO 2 H,CO 2 H 3,NO 2,SO 3 H或PO 3 H 2,B是CH,N,O或S, R 1和R 2是H,NO 2或(CH m)n X 1,其中m = 1或2,n是0至4的整数,X 1是胍基,OH,NH 2,SH,NO 2,F,Cl,Br,I, CF 3,CO 2 H,SO 3 H或PO 3 H 2,R 3和R 4是H,(CHo)pX 2,(CHo)pCHX 2 CH 2 X 2,NH(CHo)pCHX 2 CH 2 X 2,NHCO(CHo)pCH 2 X 2或NHCO(CHo)pCHX 2 CH 2 X 2,其中o = 0〜4的整数,X2为H,胍基,OH,NH2,SH,NO2,CF3,CO2H,SO3H或PO3H2,R5 = H,OH,NH2,(CHK)1X3,CO(CHK) CHK)1X3或SO2(CHK)1X3其中k = 1或2,1为0至4的整数,X3为胍基,OH,NH2,SH,NO2,CF3,CO2H,SO3H或PO3H2,R6为H,CH (OH)X4,CH(NH2)X4,COX4,SOX4或SO2X4,其中X4是H4,CH3,CH3CH2,CH3CHCH3,CH3CH2CH2或X4的卤素取代的类似物。 具有药学上可接受的载体的组合物中的抑制剂。 一种抑制流感病毒神经氨酸酶的方法,其中抑制剂与药学上可接受的量一起施用于受试者以及有效量的药学上可接受的载体。 标记可接受的载体和抑制剂的药物组合物的方法。 使用抑制剂治疗和预防感染流感病毒(A型或B型)的受试者的方法。
摘要:
In the method for operating an interference multiple access communications system, wherein the improvement comprises the steps of employing a distributed scheduler within a Media Access Controller (MAC) for Multiuser Detection (MUD) enabled Mobile Ad-hoc Networks (MANETS) to increase spectral efficiency by increasing spectral use and providing a way to dynamically allocate virtual channels to achieve maximum channel reuse in different network topologies and different link patterns and to ameliorate any hidden or exposed node problems.
摘要:
A method of expressing auxin synthetase gene specifically in cotton seed coat and fiber, which comprises constructing plant expression vector capable of expressing auxin synthetase gene specifically by fusing a tissue-specific promoter with an auxin synthetase gene, and then integrating the construct into a cotton genome. The method can significantly improve the yield and the quality of cotton fiber, thereby providing fiber with high quality for textile industry.
摘要:
An electric reciprocating motion device includes a motor having a rotary shaft for outputting a reciprocating rotational power and a motion head coupling with the rotary shaft and being driven to move in a reciprocating motion along an axis of the rotary shaft and in a predetermined swing angle range. The motor is a spring motor including a motor unit and a torsion spring having two ends affixing at a motor housing and to the rotary shaft respectively. After the rotary shaft outputs a mechanical torque at one rotational direction, the torsion spring applies a spring force against the rotary shaft to drive the rotary shaft to rotate backward for generating the reciprocating rotational power. Using the spring motor in the electric reciprocating motion device, the device achieves the goals of simple mechanical structure, small volume, easy to install, and low in cost.
摘要:
The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. These compounds are based upon N-acetylneuraminic acid glycosides. In particular, this invention provides a novel class of these compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.
摘要:
A method of inhibiting bacterial sialidase comprising administering to a subject an inhibiting effective amount of a compound of formula I: ##STR1## wherein A is CO.sub.2 H, PO.sub.2 H, or SO.sub.2 H; B is N; R.sub.1 and R.sub.2 are H; R.sub.3 and R.sub.4 are, independently, H, OH, NO.sub.2, guanidino, or alkyl or alkenyl of from 1 to 3 carbons where the alkyl or alkenyl is unsubstituted or is substituted, independently, with one or more of OH, NH2, or halide; R.sub.5 is H; and R.sub.6 is COCH.sub.3, or COCI.sub.3 ; or an analog, pharmaceutically acceptable salt, derivative, or mixture thereof. A method of preventing a bacterial or trypanosomal infection using the compounds of formula I. A method of treating a bacterial or trypanosomal infection using the compounds of formula I. A pharmaceutical composition comprising a pharmaceutically acceptable carrier admixed with an inhibiting effective amount of a compound of formula I. A method of making a pharmaceutical composition, comprising admixing a pharmaceutically acceptable carrier with an inhibiting effective amount of a compound of formula I.
摘要:
A sialidase inhibitor of the shown formula I: ##STR1## where dashed lines d.sub.1 and d.sub.2, X.sub.1, R.sub.1, R.sub.2, R.sub.6, R.sub.3, R.sub.4 and R.sub.5 are as described in the specification; or an analog, pharmaceutically acceptable salt, or derivative of the inhibitor, with the proviso that the inhibitor is not HNBA GBA or Neu5Ac2en. The inhibitor in a composition with a pharmaceutically acceptable carrier. Methods of making a pharmaceutical composition of an acceptable carrier and the inhibitor. Methods of inhibiting sialidase and methods of treating and preventing bacterial or trypanosomal infection using the inhibitor.
摘要:
A spring motor, comprising a housing, a stator core, a rotor core, a rotation shaft, a rotor coil, an insulated coil connection wire, a torsion spring, a connection shaft, a cylindrical spiral spring, a round funnel-shaped rubber sealing element, a battery and a spring fixing connection sleeve; the rotor coil of the motor is connected to the terminal of a motor end cover after the insulated coil connection wire winds around the periphery of the rotation shaft continuously several times; the connection shaft is fixed on the rotation shaft, and the cylindrical spiral spring is sleeved on the periphery of the opened end of the connection shaft; the round funnel-shaped waterproof rubber sealing element is sleeved on the rotation shaft; the battery is placed in a rectangular battery holder, three side frames of the battery holder are each a fixed structure, and one side frame of the battery holder is a moveable structure; the spring fixing connection sleeve is sleeved on the rotation shaft, the rear end of the torsion spring is placed on one side of the spring fixing connection sleeve, and the spring fixing connection jacket, the torsion spring and the rotation shaft are fixed and connected with screws.
摘要:
In the method for operating an interference multiple access communications system, wherein the improvement comprises the steps of employing a distributed scheduler within a Media Access Controller (MAC) for Multiuser Detection (MUD) enabled Mobile Ad-hoc Networks (MANETS) to increase spectral efficiency by increasing spectral use and providing a way to dynamically allocate virtual channels to achieve maximum channel reuse in different network topologies and different link patterns and to ameliorate any hidden or exposed node problems.