(3R, 4R)-trans-3, 4-diarylchroman derivatives and a method for the prevention and/or treatment of estrogen dependent diseases

    公开(公告)号:US07427686B2

    公开(公告)日:2008-09-23

    申请号:US10677116

    申请日:2003-09-30

    IPC分类号: C07D311/00

    CPC分类号: C07D311/58

    摘要: The present invention relates to compounds of the formula I in which substituents R2 and R3 are arranged in trans-configuration: wherein: R1 is H or C1-C6 alkyl; C3-C7 cycloalkyl; R2 is phenyl, optionally substituted with 1 to 5 substituents independently selected from the group comprising OH, C1-C6-alkyl, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkoxy and phenyl, wherein R4 is C1-C6 alkyl; R3 is phenyl substituted with OR5 wherein R5 has the formula (II), (III) or (IV) wherein Y is chosen from NHR4, NR42, NHCOR4, NHSO2R4, CONHR4, CONR4, CONR42, COOH, COOR4, SO2R4, SOR4, SONHR4, SONR42, a C3-C7 heterocyclic ring, saturated or unsaturated, containing one or two heteroatoms independently selected from the group consisting of O, S and N, optionally being substituted with 1 to 3 substituents independently selected from the group comprising H, OH, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkyl and C1-C6-alkoxy, preferably NHR4, NR24, or a nitrogen heterocycle, wherein R4 is as defined above, and the esters, ethers, and salts of the compounds of formula I, optionally along pharmaceutically acceptable excipients, a process for the preparation of the same, and a method of preventing and/or treating estrogen-related disease conditions in a subject using compounds of formula 1, or its salts, optionally along with pharmaceutically acceptable excipients.

    (3R, 4R)-trans-3, 4-diarylchroman derivatives and a method for the prevention and/or treatment of estrogen dependent diseases
    4.
    发明申请
    (3R, 4R)-trans-3, 4-diarylchroman derivatives and a method for the prevention and/or treatment of estrogen dependent diseases 失效
    (3R,4R) - 反-3,4-二芳基苯并二氢吡喃衍生物和预防和/或治疗雌激素依赖性疾病的方法

    公开(公告)号:US20050070597A1

    公开(公告)日:2005-03-31

    申请号:US10677116

    申请日:2003-09-30

    CPC分类号: C07D311/58

    摘要: The present invention relates to compounds of the formula I in which substituents R2 and R3 are arranged in trans-configuration: wherein: R1 is H or C1-C6 alkyl; C3-C7 cycloalkyl; R2 is phenyl, optionally substituted with 1 to 5 substituents independently selected from the group comprising OH, C1-C6-alkyl, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkoxy and phenyl, wherein R4 is C1-C6 alkyl; R3 is phenyl substituted with OR5 wherein R5 has the formula (II), (III) or (IV) wherein Y is chosen from NHR4, NR42, NHCOR4, NHSO2R4, CONHR4, CONR4, CONR42, COOH, COOR4, SO2R4, SOR4, SONHR4, SONR42, a C3-C7 heterocyclic ring, saturated or unsaturated, containing one or two heteroatoms independently selected from the group consisting of O, S and N, optionally being substituted with 1 to 3 substituents independently selected from the group comprising H, OH, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkyl and C1-C6-alkoxy, preferably NHR4, NR24, or a nitrogen heterocycle, wherein R4 is as defined above, and the esters, ethers, and salts of the compounds of formula I, optionally along pharmaceutically acceptable excipients, a process for the preparation of the same, and a method of preventing and/or treating estrogen-related disease conditions in a subject using compounds of formula 1, or its salts, optionally along with pharmaceutically acceptable excipients.

    摘要翻译: 本发明涉及式I化合物,其中取代基R 2和R 3以反式构型排列:其中:R 1是H或C 1 -C 6烷基; C3-C7环烷基; R 2是苯基,任选地被1至5个独立地选自OH,C 1 -C 6 - 烷基,卤素,硝基,氰基,SH,SR 4, - 3卤代-C 1 -C 6烷基,C 1 C 1-6 - 烷氧基和苯基,其中R 4是C 1 -C 6烷基; R 3是被OR 5取代的苯基,其中R 5具有式(II),(III)或(IV),其中Y选自NHR 4,NR 4,NHCOR 4 >,NHSO 2 R 4,CONHR 4,CONR 4,CONR 4,COOH,COOR 4,SO 2 R 4,SOR 4,SONHR 4,SONR 4 饱和或不饱和的C3-C7杂环,其含有一个或两个独立地选自O,S和N的杂原子,任选被1至3个独立地选自H,OH,卤素, 硝基,氰基,SH,SR 4,三卤代-C 1 -C 6烷基,C 1 -C 6烷基和C 1 -C 6烷氧基,优选NH 4,NR 2 4或氮杂环, 4>如上所定义,并且式I化合物的酯,醚和盐,任选地沿着药学上可接受的赋形剂,其制备方法,以及预防和/或治疗雌激素相关疾病的方法 使用式1化合物的受试者的条件,或其盐,任选地与药物 lly可接受的赋形剂。

    System for distending body tissue cavities by continuous flow irrigation
    7.
    发明授权
    System for distending body tissue cavities by continuous flow irrigation 有权
    通过连续流动灌溉膨胀身体组织腔的系统

    公开(公告)号:US08652089B2

    公开(公告)日:2014-02-18

    申请号:US10548950

    申请日:2004-07-21

    申请人: Atul Kumar Alka Kumar

    发明人: Atul Kumar Alka Kumar

    IPC分类号: A61M1/00 A61M31/00 A61B1/00

    摘要: The present invention provides a system and a method for distending a body tissue cavity of a subject by continuous flow irrigation such that minimal or negligible fluid turbulence is present inside the cavity, such that any desired cavity pressure can be created and maintained for any desired outflow rate. The present invention also provides a method for accurately determining the rate of fluid loss, into the subject's body system, during any endoscopic procedure without utilizing any deficit weight or fluid volume calculation or flow rate sensor. The system and the methods of the present invention described above can be used in any endoscopic procedure requiring continuous flow irrigation few examples of such endoscopic procedures being hysteroscopic surgery, arthroscopic surgery, trans uretheral surgery, endoscopic surgery of the brain and endoscopic surgery of the spine.

    摘要翻译: 本发明提供一种系统和方法,用于通过连续流动冲洗来膨胀受试者的身体组织腔,使得在腔内存在最小或可忽略的流体湍流,使得可以产生任何期望的腔压力并保持任何期望的流出 率。 本发明还提供了一种用于在任何内窥镜程序期间精确地确定流体损失进入受检者体内系统的方法,而不使用任何赤字重量或流体体积计算或流量传感器。 上述本发明的系统和方法可用于需要连续流动灌洗的任何内窥镜程序中,这种内窥镜手术的例子是宫腔镜手术,关节镜手术,经皮穿刺手术,脑内窥镜手术和脊柱内窥镜手术 。

    EFFICIENT CONTINUOUS FLOW IRRIGATION SYSTEM
    8.
    发明申请
    EFFICIENT CONTINUOUS FLOW IRRIGATION SYSTEM 有权
    高效连续流水灌溉系统

    公开(公告)号:US20080091061A1

    公开(公告)日:2008-04-17

    申请号:US11871051

    申请日:2007-10-11

    申请人: Alka Kumar Atul Kumar

    发明人: Alka Kumar Atul Kumar

    IPC分类号: A61B1/015

    摘要: A continuous flow irrigation endoscope and a continuous flow irrigation fluid management system, both designed to be compatible to each other and meant to function as a single system. The endoscope and the fluid management system are synergistic to each other such that both enhance the efficiency of each other. The system allows a body tissue cavity to be distended by continuous flow irrigation so that the detached tissue pieces and waste fluid present inside a body tissue cavity are continuously automatically evacuated from the tissue cavity without causing the cavity to collapse at any stage and without the need of withdrawing the endoscope or a part of the endoscope from the tissue cavity.

    摘要翻译: 连续流动灌溉内窥镜和连续流动灌溉流体管理系统,其被设计为彼此兼容并且意图用作单个系统。 内窥镜和流体管理系统彼此协同,从而提高彼此的效率。 该系统允许通过连续流动灌洗来扩张身体组织腔,使得存在于身体组织腔内的分离的组织片和废液不断地从组织腔排出,而不会导致腔在任何阶段崩溃,而不需要 从组织腔抽出内窥镜或内窥镜的一部分。

    System of dampening pressure pulsations caused by a positive displacement pump in endoscopic surgery
    10.
    发明申请
    System of dampening pressure pulsations caused by a positive displacement pump in endoscopic surgery 有权
    内镜手术中正位移泵引起的压力波动的抑制系统

    公开(公告)号:US20060129099A1

    公开(公告)日:2006-06-15

    申请号:US11240393

    申请日:2005-10-03

    申请人: Atul Kumar Alka Kumar

    发明人: Atul Kumar Alka Kumar

    IPC分类号: A61M1/00

    CPC分类号: A61M3/0258 A61M3/0216

    摘要: A system for distending body tissue cavities of subjects by continuous flow irrigation during endoscopic procedures, the system including: a fluid source reservoir containing a non viscous physiologic fluid meant for cavity distension; a fluid supply conduit tube connecting the fluid source reservoir to an inlet port of a variable speed positive displacement inflow pump and an outlet port of the said inflow pump being connectable to an inflow port of an endoscope instrument through an inflow tube for pumping the fluid at a controlled flow rate into the cavity, the flow rate of the said inflow pump being termed as the inflow rate; an inflow pressure transducer being located anywhere in the inflow tube between the outlet port of the inflow pump and the inflow port of the endoscope; an outflow port of the endoscope being connectable to a waste fluid collecting container via a waste fluid carrying tube, and characterized in that an active inflow pressure pulsation dampening means is connected to the inflow tube for dampening the pressure pulsations inside the cavity created by the positive displacement inflow pump.

    摘要翻译: 一种用于在内窥镜程序期间通过连续流动灌注来增加受试者的身体组织腔的系统,所述系统包括:含有用于腔膨胀的非粘性生理液的流体源储存器; 将流体源储存器连接到变速正排量流入泵的入口和所述流入泵的出口的流体供应管道,其可通过流入管连接到内窥镜器械的流入口,用于将流体泵送 进入空腔的受控流速,所述流入泵的流量被称为流入速率; 流入压力传感器位于流入管的出口与内窥镜的流入口之间的流入管的任何地方; 所述内窥镜的流出口经由废液输送管可连接到废液收集容器,其特征在于,主动流入压力脉动阻尼装置连接到所述流入管,用于阻尼所述空腔内产生的压力脉动 排量流入泵。