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    • 1. 发明授权
    • Antihypertensive thienopyridines
    • 抗高血压噻吩并吡啶类
    • US4710506A
    • 1987-12-01
    • US874337
    • 1986-06-13
    • Roy V. DaviesJames Fraser
    • Roy V. DaviesJames Fraser
    • A61K31/435A61P9/10A61P9/12C07D333/20C07D333/36C07D333/38C07D495/04A61K31/44
    • C07D495/04C07D333/36
    • Novel thienopyridones with antihypertensive activity have the formula I, ##STR1## wherein the ring A represents an optionally substituted thiophene ring; m is 0 or 1; n is 0, 1 or 2; R is lower alkyl and R.sub.1 is lower alkyl.The fused thieno-ring may carry one or two substituents.Formula I encompasses thieno[3,2-b]pyridones, thieno[3,4-b]pyridones and thieno[2,3-b]pyridones.Processes for preparing the novel thienopyridones and pharmaceutical compositions containing them are described. Pharmaceutically acceptable acid addition salts of the compounds of formula I are also described.The thienopyridones of formula I are antihypertensive agents and are also indicated for use in treating heart failure and ischaemic heart disease.
    • 具有抗高血压活性的新型噻吩并吡啶酮具有式I,其中环A表示任选取代的噻吩环; m为0或1; n为0,1或2; R是低级烷基,R 1是低级烷基。 稠合噻吩环可以携带一个或两个取代基。 式I包括噻吩并[3,2-b]吡啶酮,噻吩并[3,4-b]吡啶酮和噻吩并[2,3-b]吡啶酮。 描述了制备新型噻吩并吡啶酮和含有它们的药物组合物的方法。 还描述了式I化合物的药学上可接受的酸加成盐。 式I的噻吩并吡啶酮是抗高血压药,也用于治疗心力衰竭和缺血性心脏病。
    • 2. 发明授权
    • Quinolone sulphonamides useful as antihypertensive agents
    • 喹诺酮磺酰胺可用作抗高血压药
    • US4772614A
    • 1988-09-20
    • US874217
    • 1986-06-13
    • Roy V. DaviesJames FraserKenneth J. Nichol
    • Roy V. DaviesJames FraserKenneth J. Nichol
    • C07D209/38A61K31/47A61P9/10A61P9/12C07C67/00C07C301/00C07C303/38C07C303/40C07C311/35C07D215/22C07D215/36C07D215/56
    • C07D215/36
    • Quinolones with antihypertensive activity have the general formula I, ##STR1## wherein X is the residue of an optionally substituted benzene ring; R is lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.1 and R.sub.2, which may be the same or different, are hydrogen, lower alkyl, or, together with the nitrogen atom to which they are attached, form a 5 to 7 membered saturated heterocyclic ring optionally containing an additional hetero atom selected from nitrogen, oxygen and sulphur and optionally substituted by 1 or more lower alkyl groups; and the dotted line between positions 2 and 3 of the quinolone nucleus represents an optional bond. The compounds are useful as antihypertensive agents. They are also indicated for use in treating heart failure and ischaemic heart disease.With the exception of the three compounds 1-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, 1,N-dimethyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide and 6,7-dimethoxyl-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, the quinolones of formula I are novel.Pharmaceutical compositions containing the compounds of formula I are described. Processes for preparing the novel quinolones are also described.
    • 具有抗高血压活性的喹诺酮具有通式I,其中X是任选取代的苯环的残基; R为低级烷基; R3是氢或低级烷基; R 1和R 2可以相同或不同,为氢,低级烷基,或与它们相连的氮原子一起形成任选地含有另外的杂原子的5至7元饱和杂环,该杂原子选自氮, 氧和硫,并任选被一个或多个低级烷基取代; 并且喹诺酮核的位置2和3之间的虚线表示任选的键。 该化合物可用作抗高血压药。 它们也被用于治疗心力衰竭和缺血性心脏病。 除了三种化合物之外,1-甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺,1,N-二甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺和6,7-二甲氧基 - 甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺,式I的喹诺酮是新的。 描述含有式I化合物的药物组合物。 还描述了制备新喹诺酮类的方法。
    • 3. 发明授权
    • 4-Quinolinones having antihypertensive activity
    • 具有抗高血压活性的4-喹啉酮
    • US4302460A
    • 1981-11-24
    • US133310
    • 1980-03-24
    • Roy V. DaviesJames FraserKenneth J. NicholRaymond ParkinsonMalcolm F. SimDavid B. Yates
    • Roy V. DaviesJames FraserKenneth J. NicholRaymond ParkinsonMalcolm F. SimDavid B. Yates
    • A61K31/47C07D215/36C07D265/26
    • C07D265/26A61K31/47C07D215/36
    • Compositions which contain a quinolone compound of the general formula ##STR1## wherein n is 0, 1 or 2; R.sub.1 is lower alkyl optionally substituted by hydroxy or C.sub.1-4 alkoxycarbonyl; allyl; propynyl or phenyl- lower alkyl in which the phenyl ring is optionally substituted by 1 or 2 C.sub.1-4 alkoxy groups; R.sub.2 is C.sub.1-4 alkyl with the proviso that when n is 0, R.sub.2 is methyl; and R.sub.3, R.sub.4 and R.sub.5, which may be the same or different, are hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, halo, trifluoromethyl or lower alkylthio show antihypertensive activity.Compounds of general formula ##STR2## in which n, R.sub.1 R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as described above are novel subject to the following provisos (a) when R.sub.3, R.sub.4 and R.sub.4 and R.sub.5 are hydrogen R.sub.2 is methyl and R.sub.1 is lower alkyl, R.sub.1 contains more than one carbon atom, and(b) when R.sub.3 and R.sub.4 are hydrogen, R.sub.5 is hydrogen or 7-methyl, and R.sub.1 is ethyl, R.sub.2 contains more than one carbon atom.The specification describes and claims methods of making the compounds and novel intermediates used in such methods.
    • 含有通式为“IMAGE”的喹诺酮化合物的组合物,其中n为0,1或2; R1是任选被羟基或C 1-4烷氧基羰基取代的低级烷基; 烯丙基 丙炔基或苯基 - 低级烷基,其中苯环任选被1或2个C 1-4烷氧基取代; R2为C1-4烷基,条件是当n为0时,R2为甲基; R 3,R 4和R 5可以相同或不同,为氢,低级烷基,低级烷氧基,低级烷酰基,卤素,三氟甲基或低级烷硫基,表示抗高血压活性。 其中n,R1R2,R3,R4和R5如上所述的通式为“IMAGE”的化合物是新的,具有以下条件(a)当R3,R4和R4和R5为氢时R2为甲基,R1为低级 烷基,R 1含有多于一个碳原子,和(b)当R 3和R 4为氢时,R 5为氢或7-甲基,R 1为乙基,R 2为多于一个碳原子。 该说明书描述并要求制备在这些方法中使用的化合物和新型中间体的方法。
    • 5. 发明申请
    • Frequency locker
    • 频率储物柜
    • US20050225825A1
    • 2005-10-13
    • US10512702
    • 2003-04-25
    • James FraserStephen PopeColin EdgeSteven BorleyLisa DaykinKevin Mullaney
    • James FraserStephen PopeColin EdgeSteven BorleyLisa DaykinKevin Mullaney
    • H01S5/0687H01S3/131H01S5/12H01S5/125G02F1/01G02B26/00
    • H01S5/0687H01S5/0612H01S5/0617
    • A method and assembly for frequency stabilisation of an optical signal especially from a laser, the assembly (11) comprising beam splitter (15), a passive frequency discriminator (16), and a pair of photodiodes (17 & 18). The beam splitter (15) in use receives a collimated optical beam (B) and diverts a sample beam (B1) which is directed towards the discriminator (16) which transmits a portion (B2) of said sample beam to one of the photodiodes (17) and reflects a second portion (B3) of said sample beam to the other photodiode (18). A control signal (S3) is derived from the respective intensities of the transmitted and reflected portions of the sample beam, and utilised to operate the electronic control to adjust the frequency of the laser output signal, if required, to maintain a specified frequency.
    • 一种用于特别是来自激光器的光学信号的频率稳定的方法和组件,包括分束器(15)的组件(11),无源鉴频器(16)和一对光电二极管(17和18)。 使用的分束器(15)接收准直光束(B)并且转向被引导到鉴别器(16)的样本光束(B 1 SUB),该鉴别器(16)透射一部分(B < 将所述样品光束的2π(2π)放大到所述光电二极管(17)中的一个,并将所述样品光束的第二部分(B 3/3)反射到另一个光电二极管(18)。 根据样品光束的透射和反射部分的各自强度导出控制信号(S 3/3),并且如果需要,则利用该电子控制来调节激光输出信号的频率 ,保持指定的频率。
    • 8. 发明授权
    • Frequency locker
    • 频率储物柜
    • US07161725B2
    • 2007-01-09
    • US10512702
    • 2003-04-25
    • James FraserStephen PopeColin EdgeSteven BorleyLisa DaykinKevin Mullaney
    • James FraserStephen PopeColin EdgeSteven BorleyLisa DaykinKevin Mullaney
    • G02B26/00G02B27/10G02B27/30H01S3/10H04J14/02
    • H01S5/0687H01S5/0612H01S5/0617
    • A method and assembly for frequency stabilization of an optical signal especially from a laser, the assembly (11) comprising beam splitter (15), a passive frequency discriminator (16), and a pair of photodiodes (17 & 18). The beam splitter (15) in use receives a collimated optical beam (B) and diverts a sample beam (B1) which is directed towards the discriminator (16) which transmits a portion (B2) of said sample beam to one of the photodiodes (17) and reflects a second portion (B3) of said sample beam to the other photodiode (18). A control signal (S3) is derived from the respective intensities of the transmitted and reflected portions of the sample beam, and utilized to operate the electronic control to adjust the frequency of the laser output signal, if required, to maintain a specified frequency.
    • 一种用于特别是来自激光器的光学信号的频率稳定的方法和组件,包括分束器(15)的组件(11),无源鉴频器(16)和一对光电二极管(17和18)。 使用的分束器(15)接收准直光束(B)并且转向被引导到鉴别器(16)的样本光束(B 1 SUB),该鉴别器(16)透射一部分(B < 将所述样品光束的2π(2π)放大到所述光电二极管(17)中的一个,并将所述样品光束的第二部分(B 3/3)反射到另一个光电二极管(18)。 根据样品光束的透射和反射部分的各自强度导出控制信号(S 3/3),并且如果需要,则利用该电子控制来调节激光输出信号的频率 ,保持指定的频率。
    • 9. 发明授权
    • Screening assay for the identification ov novel immunosuppressives using
cultured T cells
    • 使用培养的T细胞鉴定ov新型免疫抑制剂的筛选试验
    • US5474897A
    • 1995-12-12
    • US152955
    • 1993-11-15
    • Arthur WeissJames Fraser
    • Arthur WeissJames Fraser
    • C12Q1/68
    • C12Q1/6897
    • A method for identifying compounds capable of inducing immunosuppression by inhibiting the CD28 signal transduction pathway and T cell comprises exposing cultured T cells to one or more test compounds. The T cells are obtained from a T cell line which stably incorporates DNA sequence comprising in reading frame an enhancer region responsive to a CD28-regulated nuclear binding protein and a marker gene. The cells are cultured under conditions which result in activation of both the T cell receptor and the CD28 receptor, resulting in enhanced expression of the marker gene. Test compounds which inhibit expression of the marker gene are considered as candidates for immunosuppressive drugs.
    • 通过抑制CD28信号转导途径和T细胞鉴定能够诱导免疫抑制的化合物的方法包括将培养的T细胞暴露于一种或多种测试化合物。 从T细胞系获得T细胞,T细胞系稳定地包含在读框中包含对CD28调节的核结合蛋白和标记基因有响应的增强子区的DNA序列。 在导致T细胞受体和CD28受体活化的条件下培养细胞,导致标记基因的表达增强。 抑制标记基因表达的测试化合物被认为是免疫抑制药物的候选物。