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    N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-A][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, a dual modulator of chemokine receptor activity, crystalline forms and processes
    1.
    发明授权
    N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-A][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, a dual modulator of chemokine receptor activity, crystalline forms and processes 有权
    N - （（1R，2S，5R）-5-（叔丁基氨基）-2 - （（S）-3-（7-叔丁基吡唑并[1,5-A] 吡啶-4-基氨基）-2-氧代吡咯烷-1-基）环己基）乙酰胺，趋化因子受体活性的双重调节剂，结晶形式和方法

    公开(公告)号：US08383812B2

    公开(公告)日：2013-02-26

    申请号：US12901614

    申请日：2010-10-11

    申请人： Percy H. Carter ,  Robert J. Cherney ,  Victor W. Rosso ,  Jun Li

    发明人： Percy H. Carter ,  Robert J. Cherney ,  Victor W. Rosso ,  Jun Li

    IPC分类号： C07D487/04 ,  A61K31/53 ,  A61P19/02 ,  A61P35/00

    CPC分类号： A61K31/53 ,  C07D487/04

    摘要： The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.

    摘要翻译： 本发明提供新的拮抗剂：N - （（1R，2S，5R）-5-（叔丁基氨基）-2 - （（S）-3-（7-叔丁基吡唑并[1,5-a] 1,3,5]三嗪-4-基氨基）-2-氧代吡咯烷-1-基）环己基）乙酰胺：或其药学上可接受的盐，溶剂合物或前药，具有意想不到的双重CCR-2和CCR-5受体活性。 还公开了结晶形式，代谢物，含有其的药物组合物和使用其作为治疗炎性疾病，过敏性，自身免疫性，代谢性，癌症和/或心血管疾病的药剂的方法。 本公开还提供了制备本文提供的式（I）化合物的方法，包括N - （（1R，2S，5R）-5-（叔丁基氨基）-2 - （（S） 叔丁基吡唑并[1,5-a] [1,3,5]三嗪-4-基氨基）-2-氧代吡咯烷-1-基）环己基）乙酰胺。 本文还提供了该方法有用中间体的化合物。

    Parallel chemistry reactor with interchangeable vessel carrying inserts
    7.
    发明授权
    Parallel chemistry reactor with interchangeable vessel carrying inserts 有权
    具有可更换容器的并联化学反应器

    公开(公告)号：US06893613B2

    公开(公告)日：2005-05-17

    申请号：US10057451

    申请日：2002-01-25

    申请人： Walter Ruediger ,  A. Erik Rubin ,  Alexander Bertok ,  Victor W. Rosso ,  Joseph Nolfo ,  Harold N. Weller

    发明人： Walter Ruediger ,  A. Erik Rubin ,  Alexander Bertok ,  Victor W. Rosso ,  Joseph Nolfo ,  Harold N. Weller

    IPC分类号： B01J19/00 ,  B01L7/00 ,  B01L9/06 ,  C40B60/14 ,  B01L9/00

    CPC分类号： B01J19/0046 ,  B01J2219/00283 ,  B01J2219/0031 ,  B01J2219/00335 ,  B01J2219/00376 ,  B01J2219/00481 ,  B01J2219/00495 ,  B01J2219/00585 ,  B01J2219/00599 ,  B01J2219/0072 ,  B01J2219/00722 ,  B01L7/00 ,  B01L9/06 ,  B01L2200/025 ,  B01L2200/147 ,  B01L2300/1805 ,  C40B60/14

    摘要： The base of the modular reactor includes a frame which defines an opening into which one of a plurality of interchangeable reaction vessel carrying inserts can be removeably received. Each insert has an array of recesses adapted to receive a different number of reaction vessels of different sizes. The recesses are positioned such that all arrays are suitable for use with a standard automated liquid handier. The frame has fluid flow channels for regulating the temperature of the lower portions of the vessels. A temperature control module can be received over the base to regulate the temperature of the upper portions of the vessels for reflux reactions. The corner radii of the insert and frame opening cooperate to permit the insert to be received in the frame in only one orientation. The walls of the insert are inclined to facilitate removal by a friction fit tool. Each vessel receiving recess has a self-centering conical or semi-circular shaped bottom to maximize heat transfer and distribute the load uniformly. The vessels seat as close to the bottom surface of the base as possible to facilitate use with an air driven magnetic stirrer. A thin, electrically heated plate may be received between the base and the stirrer.

    摘要翻译： 模块式反应器的底座包括限定开口的框架，多个可互换的反应容器的插入物中的一个可以被移除到该开口中。 每个插入物具有适于接收不同数量的不同尺寸的反应容器的凹部阵列。 这些凹槽定位成使得所有的阵列都适用于标准的自动化液体洗手液。 框架具有用于调节容器下部的温度的流体流动通道。 温度控制模块可以接收在基座上以调节用于回流反应的容器上部的温度。 插入件和框架开口的拐角半径配合以允许插入件仅在一个方向上被容纳在框架中。 插入件的壁倾斜以便于通过摩擦配合工具移除。 每个容器接收凹槽具有自对中圆锥形或半圆形底部以最大限度地传热并均匀地分布载荷。 船只靠近基座的底面尽可能靠近空气驱动的磁力搅拌器使用。 可以在基座和搅拌器之间容纳薄的电加热板。

    Dynamic resolution of isomers and resolved isomers
    8.
    发明授权
    Dynamic resolution of isomers and resolved isomers 有权
    动态拆分异构体和拆分的异构体

    公开(公告)号：US07388098B2

    公开(公告)日：2008-06-17

    申请号：US09961932

    申请日：2001-09-24

    申请人： John J. Venit ,  Gary D. Madding ,  Victor W. Rosso ,  Francis J. Okuniewicz ,  Robert P. Discordia ,  Susanne Kiau ,  Atul S. Kotnis ,  Michael E. Randazzo ,  D. David Hennings ,  Jingyang Zhu ,  Jason G. Chen

    发明人： John J. Venit ,  Gary D. Madding ,  Victor W. Rosso ,  Francis J. Okuniewicz ,  Robert P. Discordia ,  Susanne Kiau ,  Atul S. Kotnis ,  Michael E. Randazzo ,  D. David Hennings ,  Jingyang Zhu ,  Jason G. Chen

    IPC分类号： C07C53/134 ,  C07D233/00 ,  C07D277/00 ,  C07B55/00

    CPC分类号： C07D233/78 ,  C07C51/412 ,  C07C51/43 ,  C07C213/08 ,  C07C213/10 ,  C07D233/74 ,  C07C57/58

    摘要： Provided is a dynamic resolution method of enriching a desired isomer of an alpha-substituted carboxylic acid relative to an undesired isomer, the method comprising: (a) in a solvent, contacting the alpha-substituted carboxylic acid, wherein the alpha substitution is with a leaving group and wherein the alpha carbon is chiral, with a homochiral amine to form a salt that is partially insoluble under selected reaction conditions, wherein the homochiral amine is selected so that the solubility of the amine salt of the undesired alpha-substituted carboxylic acid is greater than that of the amine salt of the desired alpha-substituted carboxylic acid under the selected reaction conditions; (b) reacting under the selected reaction conditions the salt with a nucleophile, wherein the reacting is effective in producing a net increase in the less soluble amine salt of the alpha-substituted carboxylic acid, and wherein the selected conditions are selected to (i) promote nucleophilic substitution of the nucleophile and the leaving group or (ii) to produce the increase in the less soluble amine salt in the absence of a strong base; and (c) maintaining the reaction for a period of time effective to increase the amount of the desired alpha-substituted carboxylic acid isomer.

    摘要翻译： 提供了相对于不期望的异构体富集α-取代的羧酸的所需异构体的动态拆分方法，该方法包括：（a）在溶剂中使α-取代的羧酸接触，其中α取代为 离去基团，其中所述α碳是手性的，与同基因胺形成在所选择的反应条件下部分不溶的盐，其中选择所述同基因胺，使得不需要的α-取代羧酸的胺盐的溶解度为 在选择的反应条件下大于所需α-取代羧酸的胺盐的浓度; （b）在所选择的反应条件下使所述盐与亲核试剂反应，其中所述反应有效地产生所述α-取代羧酸的较不溶性胺盐的净增加，并且其中所选择的条件选择为：（i） 促进亲核试剂和离去基团的亲核取代，或（ii）在没有强碱的情况下产生较不溶性胺盐的增加; 和（c）保持反应一段时间有效以增加所需的α-取代的羧酸异构体的量。

    High throughput X-ray diffraction filter sample holder
    9.
    发明授权
    High throughput X-ray diffraction filter sample holder 失效
    高通量X射线衍射滤光片样品架

    公开(公告)号：US06968037B2

    公开(公告)日：2005-11-22

    申请号：US10410910

    申请日：2003-04-10

    申请人： Victor W. Rosso ,  Glen Young ,  Joseph Nolfo ,  Imre M. Vit z ,  John J. Venit

    发明人： Victor W. Rosso ,  Glen Young ,  Joseph Nolfo ,  Imre M. Vit z ,  John J. Venit

    IPC分类号： B01L3/00 ,  G01N1/28 ,  G01N23/20

    CPC分类号： G01N1/4077 ,  B01L3/50255 ,  B01L2200/026 ,  B01L2300/0829 ,  B01L2400/049 ,  G01N23/20 ,  G01N23/20025

    摘要： Multiple samples are prepared in slurry form and deposited through a funnel plate by a multiprobe liquid handler into an array of inserts situated in openings in a housing. Each insert has a recess that extends through the insert body and a filter disc situated in the recess to support the sample. The filter is held in place by an annular part which defines a channel providing access to the filter through the lower portion of the recess. A pressure differential is created across each of the filters by attaching a vacuum manifold to the bottom of the housing to simultaneously remove the liquid from each of the samples, leaving the samples in powder form. The housing is then placed in the X-ray diffractometer for sequential analysis of each of the samples, while the samples are situated in the inserts.

    摘要翻译： 多个样品以浆料形式制备并通过漏斗板通过多孔液体处理器沉积到位于壳体中的开口中的插入物阵列中。 每个插入件具有延伸穿过插入体的凹部和位于凹部中以支撑样品的过滤盘。 过滤器通过环形部分保持在适当位置，该环形部分限定了通过凹部的下部进入过滤器的通道。 通过将真空歧管连接到壳体的底部，同时从每个样品中移除液体，使样品成粉末形式，在每个过滤器上形成压差。 然后将壳体放置在X射线衍射仪中，以顺序分析每个样品，而样品位于插入物中。

    Reaction conditions for the cleavage of silyl ethers in the preparation of paclitaxel(taxol®) and paclitaxel analogues
    10.
    发明授权
    Reaction conditions for the cleavage of silyl ethers in the preparation of paclitaxel(taxol®) and paclitaxel analogues 失效
    制备紫杉醇（紫杉醇）和紫杉醇类似物时甲硅烷基醚裂解的反应条件

    公开(公告)号：US06184395B2

    公开(公告)日：2001-02-06

    申请号：US09571234

    申请日：2000-05-16

    申请人： Ambarish K. Singh ,  Raymond E. Weaver ,  Gerald L. Powers ,  Victor W. Rosso

    发明人： Ambarish K. Singh ,  Raymond E. Weaver ,  Gerald L. Powers ,  Victor W. Rosso

    IPC分类号： C07D30514

    CPC分类号： C07D305/14

    摘要： Novel reaction conditions for the cleavage of silyl ethers from silyl protected taxane precursors to afford paclitaxel and paclitaxel analogues in high yield and quality are described. Paclitaxel is prepared from a taxane precursor by treating the taxane precursor with a strong acid such as trifluoroacetic acid in a solvent such as aqueous acetic acid, such that the amount and number of side reactions and taxane impurities are significantly minimized. Also desribed are the crystallization methods for the isolation of paclitaxel in either of the two crystal forms A or B. Paclitaxel and paclitaxel analogues are anti-cancer agents.

    摘要翻译： 描述了从甲硅烷基保护的紫杉烷前体裂解甲硅烷基醚以高产率和高质量得到紫杉醇和紫杉醇类似物的新型反应条件。 通过在溶剂如乙酸水溶液中用强酸例如三氟乙酸处理紫杉烷前体，从紫杉烷前体制备紫杉醇，使得副反应的量和数量和紫杉烷杂质显着减少。 还描述了在两种晶型A或B中的任一种中分离紫杉醇的结晶方法。紫杉醇和紫杉醇类似物是抗癌剂。