摘要:
The invention relates to an antimicrobial compound of the formula: ##STR1## in which R.sup.1 is carboxy or protected carboxy,R.sup.2 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.3 and R.sup.4 are each hydrogen or lower alkyl, andR.sup.5 is saturated 4 to 6-membered heteromonocyclic group containing 1 to 4 nitrogen atom(s), saturated 5 or 6-membered heteromonocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3 nitrogen atom(s) or saturated 5 or 6-membered heteromonocyclic group containing 1 to 2 sulfur atom(s) and 1 to 3 nitrogen atom(s), wherein said aliphatic heterocyclic group may be substituted by one or more suitable substituent(s) selected from a group consisting of hydroxy, protected hydroxy, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, halogen, lower alkoxy, lower alkyl, lower alkoxy(lower)alkyl, imino, protected imino, lower alkylamino, protected lower alkylamino, mono(or di)-(lower)alkylcarbamoyloxy, lower alkylidene, lower alkanimidoyl and imino-protective group, or pharmaceutically acceptable salts thereof.
摘要:
The invention relates to novel intermediate compounds for preparation of compounds of high antimicrobial activity, said intermediate compounds being of one of the formulas: ##STR1## wherein R.sup.1 is carboxy or protected carboxy,R.sup.2 is hydroxy(lower)alkyl or protected hyroxy(lower)alkyl,R.sup.3 and R.sup.4 are each hydrogen or lower alkyl,R.sup.5 is a saturated heterocyclic group, andR.sup.6 is aryl or lower alkoxy,or pharmaceutically acceptable salts thereof.
摘要:
Preparation of optically active 3-substituted azetidinones of the formula (I) ##STR1## in which R.sup.1 is a hydroxy-protective group wherein an allylic alcohol of the formula (II) ##STR2## is acylated, then subjected to asymmetric enzymatic hydrolysis yielding the R-allylic alcohol. The hydroxyl group is protected and then stereoselectively reacted with an amine which is subsequently cyclized to yield the desired 3-substituted azetidinone. Two new species of microorganisms have been isolated, Pimelobacter sp. No. 1254 and Bacillus megaterium No. 1253 which exhibit stereoselective esterase activity.
摘要:
1-Azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds of the formula: ##STR1## in which R.sup.1 is carboxy, COO.sup.-- or protected carboxy,R.sup.2 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.8 is hydrogen or lower alkyl,Z is a group of the formula: ##STR2## wherein R.sup.3 is hydrogen; lower alkyl or lower alkenyl, each of which is optionally substituted by the group consisting of lower alkoxy, carbamoyl, hydroxy, halogen, mono(or di)(lower)alkylcarbamoyl, mono(or di)(lower)alkenylcarbamoyl, mono(or bis)[hydroxy(lower)alkyl]carbamoyl, optionally substituted cyclic-aminocarbonyl, acylamino, ureido, optionally substituted heterocyclic-carbonylamino, carbamoyloxy, mono(or di)(lower)alkylcarbamoyloxy, lower alkylthio, halo(lower)alkylthio, optionally substituted heterocyclicthio, optionally substituted heterocyclic group, optionally substituted aryl, and acyl;R.sup.9 is hydrogen or lower alkyl, andR.sup.10 is lower alkyl,or pharmaceutically acceptable salts thereof, which is useful as an antimicrobial agent.
摘要:
The invention relates to the preparation of 3,4-disubstituted-2-azetidinone compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or amido-protective group, R.sup.2 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl, R.sup.3 is lower alkyl, and R.sup.4 is 1-(lower)alkyl-1-hydroxy(C.sub.2 -C.sub.6)alkyl, 1-(lower)alkyl-1-(protected hydroxy)-(C.sub.2 -C.sub.6)alkyl or 2-thioxothiazolidin-3-yl, useful as an intermediate for the production of antimicrobial agents by reacting a compound a compound of the formula: ##STR2## in which R.sup.5 is acyl, or salts thereof, with a compound of the formula:R.sup.3 --CH.sub.2 CO--R.sup.4or salts thereof, in the presence of an enolizating agent selected from the group consisting of stannous(lower)alkylsulfonate and stannous perhalo(lower)alkylsulfonate.
摘要:
The invention relates particularly to syn compounds of the formula: ##STR1## wherein R.sup.2 is hydrogen or an aliphatic hydrocarbon which may be substituted with halogen, carboxy or pharmaceutically acceptable esterified carboxy,R.sup.5 is carboxy or pharmaceutically acceptable esterified carboxy,R.sup.6 is amino or protected amino andR.sup.7 is lower alkanesulfonyl or arenesulfonyl and pharmaceutically acceptable salt thereof, processes for making them, pharmaceutical compositions containing them and their use in treating infectious diseases.
摘要:
An antenna is provided to improve the gain and to eliminate various negative effects caused by a surrounding environment in which the antenna is mounted, such as the effects caused by neighboring metal plates and the like, while providing an antenna structure to facilitate its assembly into various communication devices. The antenna emitting radio waves at a center frequency has an antenna main body and a grounding line section connected to the ground-side of the coaxial cable for supplying power to the antenna main body. The grounding line section starts from a reference point and extends in a loop so as to surround the antenna main body, and portions of the conductor line are severed so as to provide a first end terminal and a second end terminal so that the length of the conductor line from the reference point to the first end terminal corresponds to one quarter of a wavelength of the center frequency or its integral multiple.
摘要:
A high gain antenna of a compact external dimensions enables various devices for processing radio signals to include the antenna within the internal circuitry, so that there is no need to extend the antenna and avoid a danger of breaking the antenna, and the external appearance of the device is improved. The antenna is constructed by connecting antenna elements and in series, in which each antenna element has an inductance sections and a capacitance sections connected in parallel in such a way that magnetic fields generated by the inductance sections are oriented to intersect with one another so as to increase the signal gain.
摘要:
The invention relates to novel cephem compounds, of high antimicrobial activity, of the formula ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is lower alkyl substituted with 1 to 3 halogen atoms,R.sup.3 is thiadiazolylthiomethyl which may be substituted with lower alkyl, or tetrazolylthiomethyl which may be substituted with lower alkyl or lower alkenyl, andR.sup.4 is carboxy or protected carboxy, and a pharmaceutically acceptable salt thereof.