摘要:
Compounds of formula (I): ##STR1## wherein R.sup.1x is hydrogen or methyl, R.sup.2x is hydrogen optionally substituted aliphatic hydrocarbon or acylimidoyl, R.sup.3x is hydrogen or an ester group, and Q.sup.x is cyclic or acyclic nitrogen-containing group. The compounds are potent antibiotics which are resistant to dehydropeptidase I, and are thus useful for the treatment of many microbial infections.
摘要:
Compound of formula (I): ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or --C(.dbd.NH)R.sup.0 where R.sup.0 is hydrogen or C.sub.1 -C.sub.6 alkyl;A is ##STR2## R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or --C(.dbd.NH)R.sup.6 where R.sup.6 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.7 cycloalkyl; R.sup.3 and R.sup.4 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, carboxy, cyano, --CO.NR.sup.a R.sup.b, --OCO.NR.sup.a R.sup.b or --NR.sup.a R.sup.b, where R.sup.a and R.sup.b are independently hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.20", R.sup.21', and R.sup.22" are independently hydrogen or C.sub.1 -C.sub.6 alkyl or R.sup.20" and R.sup.21" or R.sup.20" and R.sup.22" together form a heterocyclic group; R.sup.23" and R.sup.24" are independently hydrogen, halogen or C.sub.1 -C.sub.6 alkyl; n is 1, 2 or 3; and n.sup.3" is 1, 2 or 3. The compounds are antibiotics which are resistant to dehydropeptidase I, and are useful for the treatment of microbial infections.
摘要翻译:式(I)化合物:其中R 1是氢,C 1 -C 6烷基,C 2 -C 6烯基,C 2 -C 6炔基或-C(= NH)R 0)其中R 0是氢或C 1 -C 6烷基; (C 1 -C 6)烷基,C 2 -C 6烯基,C 2 -C 6炔基或-C(= NH)R 6,其中R 6是氢,C 1 -C6烷基或C3-C7环烷基; R 3和R 4独立地是氢,C 1 -C 6烷基,卤素,羟基,羧基,氰基,-CO.RRRRb,-OCO,NR a R b或-NR a R b,其中R a和R b独立地是氢或C 1 -C 6烷基; R 20“,R 21'和R 22”独立地是氢或C 1 -C 6烷基或R 20“,R 21”或R 20“和R 22”一起形成杂环基; R 23“和R 24”独立地是氢,卤素或C 1 -C 6烷基; n为1,2或3; 和n3“是1,2或3.化合物是抗脱水肽酶I的抗生素,并且可用于治疗微生物感染。
摘要:
Carbapenem compounds of formula (I): ##STR1## [in which: A is a fully saturated heterocyclic group, of which at least one ring atom is nitrogen; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or a negative ion; Q is: (i) --B--N.sup.+ R.sup.8 R.sup.9 R.sup.10, where R.sup.8, R.sup.9 and R.sup.10 are alkenyl, alkynyl or optionally substituted alkyl, and B is alkylene or alkylidene; (ii) a heterocyclic group of which one ring atom is a >N.sup.+ R.sup.11 R.sup.12, where R.sup.11 and R.sup.12 are alkenyl, alkynyl or optionally substituted alkyl; (iii) alkyl substituted by a heterocyclic group as defined in (ii) above; or (iv) alkyl substituted by an aromatic heterocyclic group, of which one ring atom is ##STR2## or R.sup.2 and Q, and the nitrogen to which they are attached, form a group of formula (II): ##STR3## where m and n are 1, 2 or 3; R.sup.6 is optionally substituted alkyl; and R.sup.7 is alkenyl, alkynyl or optionally substituted alkyl] and pharmaceutically acceptable salts and esters thereof have valuable antibacterial activity with enhanced resistance to dehydropeptidase I and .beta.-lactamase. Methods of preparing and using the compounds are also provided.
摘要:
Carbapenem compounds of formula (I): ##STR1## in which: A is a fully saturated heterocyclic group, of which at least one ring atom is nitrogen; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or a negative ion; Q is: (i) --B--N.sup.+ R.sup.8 R.sup.9 R.sup.10, where R.sup.8, R.sup.9 and R.sup.10 are alkenyl, alkynyl or optionally substituted alkyl, and B is alkylene or alkylidene.
摘要:
A 1-methylcarbapenem compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.2 represents hydrogen or an ester residue; and A represents a group of the formula (A1) ##STR2## wherein n is 0, 1 or 2, P is 0, 1 or 2, R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl and R.sup.4 is a group (Q2) ##STR3## wherein B is phenylene, phenylene(C.sub.1 -C.sub.3)alkyl, cyclohexylene, cyclohexylene(C.sub.1 -C.sub.3)alkyl or C.sub.1 -C.sub.5 alkylene, R.sup.7 is hydrogen or C.sub.1 -C.sub.4 alkyl, and R.sup.14 is a group --C(.dbd.NH)R.sup.8, wherein R.sup.8 is hydrogen or C.sub.1 -C.sub.4 alkyl or a group --NR.sup.9 R.sup.10, wherein R.sup.9 and R.sup.10 are the same or different and are hydrogen or C.sub.1 -C.sub.4 alkyl; or a pharmacologically acceptable salt thereof.
摘要:
A method for the prophylaxis or treatment of infectious diseases caused by helicobacter pyloir, by administering a pharmacologically effective amount of a 1-methoylcarbapenem coumpund of formula (I) or a pharmacologically acceptable salt or ester thereof: R1 represents a group of the following formula: R2 is a hydrogen atom or a C1-C6 alkyl group, and R3 is a hydrogen atom or a C1-C6 alkyl group.
摘要:
A 1-methylcarbapenem compound represented by the following formula: ##STR1## [wherein R.sup.1 represents a hydrogen atom or a lower alkyl group, R.sup.2 represents a hydrogen atom or a lower alkyl group, R.sup.3 represents a hydrogen atom, a lower alkyl group, a lower alkyl group which has a substituent, a cycloalkyl group or a group of formula --C(.dbd.NH)R.sup.4 (in which R.sup.4 represents a hydrogen atom, a lower alkyl group or an amino group)]; or a pharmacologically acceptable salt or derivative thereof. The 1-methylcarbapenem compounds of the present invention exhibit excellent antibacterial activity and are therefore effective as a preventive or remedy of infections.
摘要:
The present invention relates to a compound of formula (I) (wherein R1 and R2 represent an aryl group, a heterocyclic group, an alkyl group, an alkenyl group and the like which are optionally substituted, R3 represents a hydrogen atom or a hydroxyl group, and X1 and X2 represent an oxygen atom or a sulfur atom, or a nitrogen atom which may be substituted), a pharmaceutically acceptable derivative thereof or a salt thereof.The present invention also relates to a pharmaceutical composition comprising a compound described above as an active ingredient for the prevention or treatment of bacterial infections.The present invention includes the use of a compound described above in order to prepare a medicament effective in the prevention or treatment of bacterial infections.The present invention is concerned with a method for the prevention or treatment of bacterial infections in warm-blooded animals comprising administering a pharmacologically effective amount of a compound described above to them
摘要:
A strain measurement apparatus includes: a stereo camera device that produces a first stereo image and a second stereo image of a measurement object; an actual strain calculation portion configured to find a three-dimensional configuration of the measurement object from the first stereo image and the second stereo image to find actual strain of the measurement object; a temperature distribution detector that detects a temperature distribution of the measurement object; a free thermal strain calculation portion configured to find free thermal strain of the measurement object from the temperature distribution detected by the temperature distribution detector; and a constraint strain calculation portion configured to find as constraint strain of the measurement object a difference obtained by subtracting the free thermal strain found by the free thermal strain calculation portion from the actual strain found by the actual strain calculation portion.
摘要:
A method for producing an injection-molded product includes steps of placing, in an injection mold, a heat-shrinkable resin sheet having region A and region B which have different surface temperatures when irradiated with infrared rays; integrating the resin sheet with an injection molding resin by injecting the injection molding resin into the mold; and, before the resin sheet is placed in the injection mold or before the integration step after the placing of the resin sheet in the injection mold, irradiating the resin sheet with infrared rays so that the surface temperatures of region A and region B are different from each other and the surface temperature of at least region A is equal to or higher than an orientation release stress inflection point temperature T of the resin sheet, thereby forming a difference in thickness between regions A and B.