Carbapenem derivatives, their preparation and their use as antibiotics
    2.
    发明授权
    Carbapenem derivatives, their preparation and their use as antibiotics 失效
    碳青霉烯类衍生物,其制备及其作为抗生素的用途

    公开(公告)号:US5866564A

    公开(公告)日:1999-02-02

    申请号:US889542

    申请日:1997-07-08

    CPC分类号: C07D477/20

    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。

    Carbapenem derivatives having antibiotic activity, their preparation and
their use
    3.
    发明授权
    Carbapenem derivatives having antibiotic activity, their preparation and their use 失效
    具有抗生素活性的碳青霉烯类衍生物及其制备及其应用

    公开(公告)号:US5420119A

    公开(公告)日:1995-05-30

    申请号:US143996

    申请日:1993-10-27

    CPC分类号: C07D477/20

    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.

    摘要翻译: (I)的碳青霉烯化合物:其中:A是完全饱和的杂环基团,其中至少一个环原子是氮; R1是氢或甲基; R2是氢或烷基; R3是氢或负离子; Q为:(i)-B-N + R8R9R10,其中R8,R9和R10为烯基,炔基或任选取代的烷基,B为亚烷基或亚烷基; (ii)一个环原子是> N + R11R12的杂环基,其中R11和R12是烯基,炔基或任选取代的烷基; (iii)被上述(ii)中定义的杂环基取代的烷基; 或(iv)被芳族杂环基取代的烷基,其中一个环原子是R 1和R 2和Q,并且与它们相连的氮形成式(II)的基团: 其中m和n为1,2或3; R6是任选取代的烷基; 并且R 7是烯基,炔基或任选取代的烷基]及其药学上可接受的盐和酯具有有利于抗脱水肽酶I和β-内酰胺酶的抗菌活性。 还提供了制备和使用化合物的方法。

    1- Methylcarbapenem derivatives
    5.
    发明授权
    1- Methylcarbapenem derivatives 失效
    1-甲基碳青霉烯衍生物

    公开(公告)号:US6090802A

    公开(公告)日:2000-07-18

    申请号:US95925

    申请日:1998-06-12

    IPC分类号: C07D477/20 A61K31/409

    CPC分类号: C07D477/20

    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.

    摘要翻译: 由下式(I)表示的1-甲基碳青霉烯化合物:其中R1表示氢或C1-C4烷基; R2代表氢或酯残基; 并且A表示式(A1)的基团,其中n为0,1或2,P为0,1或2,R3为氢或C1-C4烷基,R4为基团(Q2),其中B为亚苯基,亚苯基 (C1-C3)烷基,亚环己基,亚环己基(C1-C3)烷基或C1-C5亚烷基,R7是氢或C1-C4烷基,R14是基团-C(= NH)R8,其中R8是氢或C1 -C4烷基或-NR9R10基团,其中R9和R10相同或不同,为氢或C1-C4烷基; 或其药理学上可接受的盐。

    Method and treatment using 1-methylcarbapenem derivatives as an anti-helicobacter pylori agent
    6.
    发明授权
    Method and treatment using 1-methylcarbapenem derivatives as an anti-helicobacter pylori agent 失效
    使用1-甲基碳青霉烯类衍生物作为抗幽门螺旋杆菌药物的方法和治疗

    公开(公告)号:US06180621B2

    公开(公告)日:2001-01-30

    申请号:US09187680

    申请日:1998-11-06

    IPC分类号: A01N4300

    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.

    摘要翻译: 一种预防或治疗由幽门螺杆菌引起的感染性疾病的方法,通过施用药理学有效量的式(I)的1-甲基碳代青霉烯聚糖或其药理学上可接受的盐或酯:R1代表下式的基团: R2是氢原子或C1-C6烷基,R3是氢原子或C1-C6烷基。

    1-methylcarbapenem derivatives
    7.
    发明授权
    1-methylcarbapenem derivatives 失效
    1-甲基碳青霉烯衍生物

    公开(公告)号:US5977097A

    公开(公告)日:1999-11-02

    申请号:US176804

    申请日:1998-10-22

    CPC分类号: C07D477/20

    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.

    摘要翻译: 由下式表示的1-甲基碳青霉烯化合物:其中,R 1表示氢原子或低级烷基,R 2表示氢原子或低级烷基,R 3表示氢原子,低级烷基,低级烷基 具有取代基,环烷基或式-C(= NH)R 4(其中R 4表示氢原子,低级烷基或氨基)的基团]。 或其药理学上可接受的盐或其衍生物。 本发明的1-甲基碳青霉烯化合物表现出优异的抗菌活性,因此作为感染的预防或补救是有效的。

    Antibacterial compound
    8.
    发明授权
    Antibacterial compound 有权
    抗菌化合物

    公开(公告)号:US07157442B2

    公开(公告)日:2007-01-02

    申请号:US10080191

    申请日:2002-02-19

    CPC分类号: C07H19/06

    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

    摘要翻译: 本发明涉及式(I)化合物(其中R 1和R 2表示芳基,杂环基,烷基,烯基和 任选被取代的R 3表示氢原子或羟基,X 1和X 2表示氧原子或 硫原子或可被取代的氮原子),其药学上可接受的衍生物或其盐。 本发明还涉及包含上述化合物作为预防或治疗细菌感染的活性成分的药物组合物。 本发明包括使用上述化合物以制备有效预防或治疗细菌感染的药物。 本发明涉及一种预防或治疗温血动物细菌感染的方法,其包括将药理学有效量的上述化合物给予它们

    Strain measurement apparatus, linear expansion coefficient measurement method, and correction coefficient measurement method for temperature distribution detector
    9.
    发明授权
    Strain measurement apparatus, linear expansion coefficient measurement method, and correction coefficient measurement method for temperature distribution detector 有权
    应变测量装置,线性膨胀系数测量方法和温度分布检测器的校正系数测量方法

    公开(公告)号:US09410798B2

    公开(公告)日:2016-08-09

    申请号:US13658424

    申请日:2012-10-23

    IPC分类号: H04N13/02 G01B11/16

    CPC分类号: G01B11/16 H04N13/239

    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.

    摘要翻译: 应变测量装置包括:立体照相机装置,其产生测量对象的第一立体图像和第二立体图像; 实际应变计算部分,被配置为从第一立体图像和第二立体图像中找到测量对象的三维配置,以发现测量对象的实际应变; 温度分布检测器,其检测测量对象的温度分布; 自由热应变计算部分,被配置为根据由温度分布检测器检测的温度分布找到测量对象的自由热应变; 以及约束应变计算部,其被配置为通过从由所述实际应变计算部发现的实际应变中减去由所述自由热应变计算部发现的自由热应变而求出测量对象的约束应变。

    METHOD FOR MANUFACTURING AN INJECTION-MOLDED OBJECT
    10.
    发明申请
    METHOD FOR MANUFACTURING AN INJECTION-MOLDED OBJECT 失效
    注射成型对象的制造方法

    公开(公告)号:US20130075959A1

    公开(公告)日:2013-03-28

    申请号:US13577801

    申请日:2011-02-28

    IPC分类号: B29C35/08

    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.

    摘要翻译: 一种注射成型制品的制造方法,其特征在于,包括以下步骤:在注射模具中放置具有红外线照射时具有不同表面温度的区域A和区域B的热收缩性树脂片; 通过将注塑树脂注射到模具中来将树脂片与注塑树脂整合; 在将树脂片放置在注射模具中之前或者在将树脂片材放置在注射模具中之前的整合步骤之前,将树脂片材照射到红外线,使得区域A和区域B的表面温度不同于 至少区域A的表面温度等于或高于树脂片的取向释放应力拐点温度T,从而在区域A和B之间形成厚度差。