会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 61. 发明授权
    • 3-aminophenylpentane-1,5-diones
    • 3-氨基戊基-1,5-二酮
    • US5053524A
    • 1991-10-01
    • US515840
    • 1990-04-27
    • Friedrich-Wilhelm RaulfsUdo MayerAndreas Oberlinner
    • Friedrich-Wilhelm RaulfsUdo MayerAndreas Oberlinner
    • C07C211/50C07C215/70C07C225/22C07C251/30C07C255/24C07C255/58C07C255/59C07D209/86C09B55/00
    • C07C251/30C07C211/50C07C215/70C07C225/22C07C255/24C07C255/58C07D209/86C07C2101/08C07C2101/10
    • 3-Aminophenylpentane-1,5-diones of the formula I ##STR1## where R.sup.1 and R.sup.2 are, independently of one another, hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.4 -C.sub.8 -cycloalkyl, cyano-C.sub.2 -C.sub.4 -alkyl, hydroxy-C.sub.2 -C.sub.4 -alkyl, chloro-C.sub.2 -C.sub.4 -alkyl, phenyl-C.sub.1 -C.sub.2 -alkyl which can be substituted by chlorine, or phenyl which can be substituted by clorine or methyl, or R.sup.1 and R.sup.2 form, together with the nitrogen to which they are bonded, a heterocyclic radical which can contain further hetero atoms,R.sup.3 is hydrogen, fluorine, chlorine, C.sub.1 -C.sub.2 -alkyl or C.sub.2 -C.sub.5 -alkoxy or, if R.sup.3 is ortho to --NR.sup. R.sup.2, R.sup.3 and R.sup.2 together form C.sub.2 -C.sub.4 -alkylene, which can be substituted, or 1,2-phenylene andA is naphthyl or a radical of the formula II ##STR2## where X is hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.5 -alkyl, hydroxyl, C.sub.1 -C.sub.5 -alkoxy, phenoxy, phenyl-C.sub.1 -C.sub.2 -alkoxy, cyano or phenyl andn is 1 or 2,with the proviso that R.sup.1 and R.sup.2 are not both methyl when A is phenyl, are described.
    • 式I的3-氨基苯基戊-1,5-二酮其中R 1和R 2彼此独立地为氢,C 1 -C 8 - 烷基,C 4 -C 8 - 环烷基,氰基-C 2 -C 4 - 烷基,羟基-C 2 -C 4 - 烷基,氯代-C 2 - C 4 - 烷基,可被氯取代的苯基-C 1 -C 2 - 烷基,或可被氯取代或甲基取代的苯基,或R 1和R 2一起形成 与其键合的氮原子可以含有其它杂原子的杂环基,R3是氢,氟,氯,C1-C2-烷基或C2-C5-烷氧基,或者如果R3是-NRR2的邻位,R3和 R2一起形成可被取代的C 2 -C 4亚烷基或1,2-亚苯基,A是萘基或式II的基团其中X是氢,氟,氯,溴,C1- C5-烷基,羟基,C1-C5-烷氧基,苯氧基,苯基-C1-C2-烷氧基,氰基或苯基,n为1或2,条件是当A为苯基时,R1和R2不同时为甲基 。
    • 62. 发明授权
    • Guanidino-substituted benzopyrans and their use as pharmaceuticals
    • 甘氨酸取代苯并噻唑及其作为药物的用途
    • US5053427A
    • 1991-10-01
    • US407227
    • 1989-09-14
    • Geoffrey StempGordon BurrellDavid G. Smith
    • Geoffrey StempGordon BurrellDavid G. Smith
    • A61K31/155A61K31/35A61K31/352A61K31/435A61P1/00A61P9/00A61P9/12A61P11/08A61P13/02A61P15/00A61P15/04C07C255/59C07C255/67C07C279/16C07C279/28C07C335/32C07D311/58C07D311/68C07D405/04C07D491/04C07D491/052
    • C07D405/04C07C255/59C07C255/67C07C279/28C07C335/32C07D311/68C07D491/04C07C2102/08
    • Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein a and b together form an --O-- or --CH.sub.2 -- linkage or a bond;either Y is N and R.sub.2 is hydrogen; orY is C-R.sub.1whereineither one of R.sub.1 and R.sub.2 is hydrogen and the other is nitro, cyano, halo, CF.sub.3, formyl, aldoxime, CF.sub.3 O, NO.sub.2 --CH.dbd.CH--, NC--CH.dbd.CH--; a group R.sub.x X-- wherein R.sub.x and C.sub.1-6 alkyl, aryl or heteroaryl either of which may be optionally substituted by one, two or three of C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, halo, CF.sub.3 and cyano; and X is C.dbd.O, O.C.dbd.O, C.dbd.0.0, CHOH, SO, SO.sub.2, 0.SO, 0.SO.sub.2, CONH, 0.CONH, C.dbd.S, 0.C.dbd.S, C.dbd.S.0, CH.SH, SONH, SO.sub.2 NH, 0.SONH, 0.SO.sub.2 NH, CO--CH.dbd.CH, C.dbd.NHOH, C.dbd.NNH.sub.2 ; or a group R.sub.y R.sub.z NZ-- wherein R.sub.y and R.sub.z are independently hydrogen or C.sub.1-6 alkyl and Z is C.dbd.O, SO or SO.sub.2 ; orR.sub.1 is a C.sub.3-8 cycloalkyl group or a C.sub.1-6 alkyl group optionally substituted by a group which is hydroxy, C.sub.1-6 alkoxy, amino optionally substituted by one or two C.sub.1-6 alkyl groups, C.sub.1-7 alkanoylamino, C.sub.3-8 cycloalkyloxy or C.sub.3-8 cycloalkylamino; and R.sub.2 is hydrogen; orone of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl and the other is a different group selected from nitro, cyano, halo, C.sub.1-3 alkylcarbonyl, methoxy or amino optionally substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl;either one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl; orR.sub.3 and R.sub.4 together are C.sub.2-5 polymethylene;either R.sub.5 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy; andR.sub.6 is hydrogen; orR.sub.5 and R.sub.6 together are a bond;either R.sub.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; andR.sub.8 is hydrogen or C.sub.1-6 alkyl; orR.sub.7 and R.sub.8 together are C.sub.2-4 polymethylene;R.sub.9 is CN, NO.sub.2, COR.sub.10 or SO.sub.2 R.sub.10 wherein R.sub.10 is C.sub.1-3 alkyl, NH.sub.2, NH(C.sub.1-3 alkyl), CF.sub.3 or phenyl optionally substituted as defined for R.sub.x ; andthe R.sub.8 N(NR.sub.9)NHR.sub.7 moiety is trans to the R.sub.5 group when R.sub.5 is hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy;having antihypertensive and/or bronchodilator activity, processes for their preparation and their use as pharmaceuticals.
    • 67. 发明授权
    • 9-Amino-3,4-dihydroacridines and related compounds useful for enhancing
memory
    • 9-氨基-3,4-二氢吖啶和有助于增强记忆的相关化合物
    • US4839364A
    • 1989-06-13
    • US7885
    • 1987-01-28
    • Gregory M. ShutskeFrank A. Pierrat
    • Gregory M. ShutskeFrank A. Pierrat
    • C07C255/42A61K31/435A61K31/47C07C20060101C07C67/00C07C253/00C07C255/58C07C255/59C07C255/60C07D219/08C07D219/10C07D219/12C07D221/16C07D409/12
    • C07D409/12C07C255/00C07D219/10C07D219/12C07D221/16
    • There are disclosed compounds having the formula ##STR1## wherein n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, NHCOR.sub.2 where R.sub.2 is loweralkyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl; Y is C.dbd.O or CR.sub.5 OH where R.sub.5 is hydrogen or loweralkyl; Z is CH.sub.2 or C.dbd.CR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are independently hydrogen or loweralkyl; or Y and Z taken together is CR.sub.5 .dbd.Ch where CR.sub.5 and CH correspond to Y and Z respectively; an optical antipode thereof, or a pharmaceutically acceptable acid addition salt thereof, which are useful for enhancing memory, methods for synthesizing them, and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.
    • 公开了具有式“IMAGE”的化合物,其中n为1,2或3; X是氢,低级烷基,低级烷氧基,卤素,羟基,硝基,三氟甲基,NHCOR 2,其中R2是低级烷基,或NR3R4,其中R3和R4独立地是氢或低级烷基; R是氢或低级烷基; R 1是氢,低级烷基,二低级烷基氨基低级烷基,芳基低级烷基,二芳基低级烷基,呋喃基烷基,噻吩基低级烷基,氧桥连的芳基低级烷基,氧桥连的二芳基低级烷基,氧桥连的呋喃基低级烷基或氧桥连的噻吩基低级烷基。 Y是C = O或CR5OH,其中R5是氢或低级烷基; Z是CH 2或C = CR 6 R 7,其中R 6和R 7独立地是氢或低级烷基; 或Y和Z一起为CR5 = Ch,其中CR5和CH分别对应于Y和Z; 可用于增强记忆力的光学对映体或其药学上可接受的酸加成盐,以及合成它们的方法和包含有效记忆增加量的这种化合物的药物组合物。
    • 68. 发明授权
    • Fluorescent indicator dyes for calcium ions
    • 用于钙离子的荧光指示剂染料
    • US4603209A
    • 1986-07-29
    • US648649
    • 1984-09-07
    • Roger Y. TsienGrzegorz Grynkiewicz
    • Roger Y. TsienGrzegorz Grynkiewicz
    • A61K38/00A61K38/22A61P5/00C07C229/18C07C229/52C07C237/30C07C255/59C07C309/49C07C311/39C07C317/32C07D209/08C07D209/14C07D215/40C07D307/79C07D307/82C07D413/04C07K7/23G01N21/78G01N33/84C07C101/447C07D307/87
    • C07D307/79C07D209/08C07D215/40C07D413/04Y10S436/80
    • The present invention discloses a new class of highly fluorescent indicator dyes that are specific for calcium ions. The new fluorescent indicator dyes combine a stilbene-type fluorophore with a tetracarboxylate parent Ca.sup.2+ chelating compound having the octacoordinate pattern of liganding groups characteristic of EGTA and BAPTA. Preferred forms contain extra heterocyclic bridges to reinforce the ethylenic bond of the stilbene and to reduce hydrophobicity. Compared to their widely used predecessor, "quin2", the new dyes offer up to thirty-fold brighter fluorescence, major changes in wavelength (not just intensity) upon Ca.sup.2+ binding, slightly lower affinities for Ca.sup.2+, slightly longer wavelengths of excitation, and considerably improved selectivity for Ca.sup.2+ over other divalent cations. These properties, particularly the wavelength sensitivity to Ca.sup.2+, make the dyes useful indicators for many intracellular applications, especially in single cells, adherent cell layers, or bulk tissues.The present invention also discloses an improved method for synthesizing alpha-acyloxyalkyl bromides wherein the bromides so synthesized are free of contaminating bis(1-bromoalkyl)ether. The improved method is exemplified herein in the synthesis of acetoxymethyl bromide, a compound useful in preparing the acetoxymethyl esters disclosed herein as novel Ca.sup.2+ specific fluorescent indicators.
    • 本发明公开了一类对钙离子具有特异性的高荧光指示剂染料。 新的荧光指示剂染料将二苯乙烯型荧光团与具有EGTA和BAPTA特征的连接组的八配位图案的四羧酸母体Ca 2+螯合化合物结合。 优选的形式包含额外的杂环桥,以加强1,2-二苯乙烯的烯键并降低疏水性。 与其广泛使用的前身“quin2”相比,新型染料提供高达三十倍的荧光,Ca2 +结合时的波长(不仅仅是强度)的主要变化,Ca2 +的亲和力略低,激发波长稍长, 提高Ca2 +对其他二价阳离子的选择性。 这些性质,特别是对Ca2 +的波长敏感性,使得染料对于许多细胞内应用尤其是在单细胞,贴壁细胞层或体组织中是有用的指标。 本发明还公开了一种合成α-酰氧基烷基溴化物的改进方法,其中如此合成的溴化物没有污染的双(1-溴烷基)醚。 改进的方法在本文中示例性地合成乙酰氧甲基溴,其是可用于制备本文公开的乙酰氧基甲酯作为新型Ca 2+特异性荧光指示剂的化合物。