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374 条记录 (耗时 0.046 秒)

    Process for the preparation of azoxystrobin and analogues thereof
    3.
    发明申请
    Process for the preparation of azoxystrobin and analogues thereof 有权
    嘧菌酯及其类似物的制备方法

    公开(公告)号：US20040242607A1

    公开(公告)日：2004-12-02

    申请号：US10480863

    申请日：2004-06-09

    发明人： David Anthony Jackson ,  James Peter Muxworthy ,  Mark Robert Sykes

    IPC分类号： A61K031/513 ,  C07D239/02

    CPC分类号： C07D239/52

    摘要： A process for the preparation of a compound of the general formula (I): wherein R1 is a 4-pyrimidinyl ring substituted at the 6-position by halo, hydroxy, 2-cyanophenoxy, 2,6-difluorophenoxy, 2-nitrophenoxy or 2-thiocarboxamidophenoxy and R2 is any group which can be transesterified to form a methyl ester, which comprises treating a compound of general formula (II): wherein R1 and R2 have the meanings given above, with a formylating agent and subsequently treating the formylated product with a methylating agent. 1

    摘要翻译： 一种制备通式（I）化合物的方法：其中R 1为6-位被卤素取代的4-嘧啶基环，羟基，2-氰基苯氧基，2,6-二氟苯氧基，2- 硝基苯氧基或2-硫代羧酰氨基苯氧基，R 2是可以酯交换形成甲酯的任何基团，其包括处理通式（II）的化合物：其中R 1和R 2具有上述含义 与甲酰化剂接触，随后用甲基化剂处理甲酰化产物。

    Combination
    4.
    发明申请
    Combination 审中-公开
    组合

    公开(公告)号：US20040242597A1

    公开(公告)日：2004-12-02

    申请号：US10489920

    申请日：2004-03-18

    发明人： Thomas Klein ,  Hans-Peter Kley

    IPC分类号： A61K031/522 ,  A61K031/513 ,  A61K031/4709

    CPC分类号： A61K45/06 ,  A61K31/00 ,  A61K2300/00

    摘要： The invention relates to the combined administration of PDE4-inhibitors and NSAIDs for the treatment of an inflammatory disease and/or an inflammation associated disorder while minimizing gastrointesti-nal side effects, such as gastric erosions and ulcer, which are frequently associated with the use of NSAIDs.

    摘要翻译： 本发明涉及用于治疗炎性疾病和/或炎症相关疾病的PDE4抑制剂和NSAID的组合给药，同时最小化胃肠道侵蚀和溃疡的胃肠道副作用，其通常与使用 NSAIDs。

    Compositions and methods for combination antiviral therapy
    6.
    发明申请
    Compositions and methods for combination antiviral therapy 审中-公开
    用于组合抗病毒治疗的组合物和方法

    公开(公告)号：US20040224917A1

    公开(公告)日：2004-11-11

    申请号：US10757141

    申请日：2004-01-13

    申请人： GILEAD SCIENCES, INC.

    发明人： Terrance C. Dahl ,  Mark M. Menning ,  Reza Oliyai

    IPC分类号： A61K031/7076 ,  A61K031/513

    CPC分类号： A61K31/675 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/513 ,  A61K31/683 ,  A61K31/7076 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to therapeutic combinations of null2-(6-amino-purin-9-yl)-1-methyl-ethoxymethylnull-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Vireadnull) and (2R, 5S, cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtrivanull, (null)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.

    摘要翻译： 本发明涉及[2-（6-氨基 - 嘌呤-9-基）-1-甲基 - 乙氧基甲基] - 膦酸二异丙氧羰基氧基甲酯（富马酸替诺福韦地索普洛尔，Viread）和（2R，5S， 顺式）-4-氨基-5-氟-1-（2-羟甲基-1,3-氧硫杂环戊烷-5-基） - （1H） - 嘧啶-2-酮（恩曲他滨，Emtriva TM，（ - ） - 顺式FTC）及其生理功能衍生物。 这些组合可用于治疗HIV感染，包括具有对核苷和/或非核苷抑制剂的抗性的HIV突变体的感染。 本发明还涉及替诺福韦地索普西富马酸和恩曲他滨的组合的药物组合物和制剂及其生理功能衍生物，以及这些组合物和制剂的使用的治疗方法。

    Compound for the treatment of abnormal cell growth
    7.
    发明申请
    Compound for the treatment of abnormal cell growth 审中-公开
    用于治疗异常细胞生长的化合物

    公开(公告)号：US20040220177A1

    公开(公告)日：2004-11-04

    申请号：US10734039

    申请日：2003-12-11

    申请人： Pfizer Inc

    发明人： John Charles Kath ,  Michael Joseph Luzzio

    IPC分类号： A61K031/55 ,  A61K031/513 ,  A61K031/506 ,  C07D43/02

    CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D513/04

    摘要： The invention relates to compounds of the formula 1 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, R4, R5, n, A and B are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

    摘要翻译： 本发明涉及式1的化合物及其药学上可接受的盐，前药和溶剂合物，其中R 1，R 2，R 3，R 4，R 5，n，A和 B如本文所定义。 本发明还涉及通过施用式1的化合物和用于治疗这些疾病的药物组合物来治疗哺乳动物异常细胞生长的方法，其含有式1的化合物。本发明还涉及制备式1化合物的方法 。

    New derivatives of hydantoins, thiohydantoins, pyrimidinediones and thioxopyrimidinones, their preparation processes and their use as medicaments
    8.
    发明申请
    New derivatives of hydantoins, thiohydantoins, pyrimidinediones and thioxopyrimidinones, their preparation processes and their use as medicaments 失效
    乙内酰脲，硫代乙内酰脲，嘧啶二酮和硫代嘧啶酮的新衍生物，其制备方法及其作为药物的用途

    公开(公告)号：US20040209908A1

    公开(公告)日：2004-10-21

    申请号：US10813139

    申请日：2004-03-30

    申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)

    发明人： Lydie Poitout ,  Valerie Brault ,  Christophe Thurieau

    IPC分类号： A61K031/513 ,  C07D43/02

    CPC分类号： C07D233/86 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14

    摘要： The invention concerns compounds for treating pathological conditions or diseases wherein one (or several) somatostatin receptors is (are) involved, corresponding to general formula (I) wherein: R1 represents in particular a carbocyclic or heterocyclic aryl radical optionally substituted or a non-aromatic heterocyclic radical optionally substituted; R2 represents H, alkyl or aryl optionally substituted; R3 represents H or -(CH2)p-Z3, Z3 representing in particular alkyl, cycloalkyl, bis-arylalkyl or di-aryalkyl, -Y1-(CH2)p-phenyl-(X1)n, carbocyclic or heterocyclic aryl optionally substituted, a non-aromatic heterocyclic radical optionally substituted, X1, every time it is present, being independently selected in particular among the radicals H, Cl, F, Br, I, CF3, NO2, OH, NH2, CN, N3, -OCF3, alkyl, alkoxy, -S-alkyl, -(CH2)p-NH2, -(CH2)p-NH-alkyl, -(CH2)p-N-dialkyl; Y1 represents O, S, NH or is not present; R4 represents -(CH2)p-Z4, Z4 representing in particular amino, alkylamino, N,N-dialkylamino; R5 represents in particular H or alkyl; X represents O or S; p each time it is present is independently 0 or an integer ranging between 1 and 6; q each time it is present is independently an integer between 1 and 5; n represents 0 or 1; provided that when n represents 0, m represents 1, 2 or 3, and when n represents 1, m represents 0 or 1.

    摘要翻译： 本发明涉及用于治疗病理状况或疾病的化合物，其中涉及一种（或几种）促生长抑素受体，对应于通式（I），其中：R 1特别表示任选取代的碳环或杂环芳基或非芳族 任选取代的杂环基团; R2代表H，任选被取代的烷基或芳基; R3表示H或 - （CH2）p-Z3，Z3特别表示烷基，环烷基，双芳基烷基或二 - 芳烷基，-Y1-（CH2）p-苯基 - （X1）n，任选取代的碳环或杂环芳基， 任选取代的非芳族杂环基，每次存在时，独立地选自H，Cl，F，Br，I，CF 3，NO 2，OH，NH 2，CN，N 3，-OCF 3， 烷基，烷氧基，-S-烷基， - （CH 2）p -NH 2， - （CH 2）p-NH-烷基， - （CH 2）p N-二烷基; Y1表示O，S，NH或不存在; R4表示 - （CH2）p-Z4，Z4特别表示氨基，烷基氨基，N，N-二烷基氨基; R5特别表示H或烷基; X表示O或S; 每次存在时，p独立为0或1〜6的整数; 每次存在时，独立地为1和5之间的整数; n表示0或1; 条件是当n表示0时，m表示1,2或3，当n表示1时，m表示0或1。

    Hair growth stimulant compositions
    9.
    发明申请
    Hair growth stimulant compositions 审中-公开
    头发生长刺激剂组合物

    公开(公告)号：US20040204433A1

    公开(公告)日：2004-10-14

    申请号：US10830039

    申请日：2004-04-23

    申请人： TAISHO PHARMACEUTICAL CO., LTD.

    发明人： Koji Imamura ,  Rumi Ochiai ,  Takako Okajima ,  Susumu Morioka ,  Taro Horie

    IPC分类号： A61K031/513

    CPC分类号： A61Q7/00 ,  A61K8/34 ,  A61K8/345 ,  A61K8/4953 ,  A61K31/506

    摘要： Preparations containing minoxidil at a high concentration which scarcely show the precipitation of crystals even at low temperatures and have a high stability. In preparations containing 10 to 50% by mass of water and 3% by mass or more of minoxidil, hair growth stimulant compositions further containing 8 to 30% of one or more polyhydric alcohols and having a pH value of 5.5 to 6.5 scarcely show precipitation of crystals and have a high stability.

    摘要翻译： 含有高浓度米诺地尔的制剂，即使在低温下也几乎不显示晶体析出并具有高稳定性。 在含有10〜50质量％的水和3质量％以上的米诺地尔的制剂中，还含有8〜30％的一种以上的多元醇，pH值为5.5〜6.5的毛发生长刺激剂组合物几乎不显示出 晶体，稳定性高。

    [5-carboxamido or 5-fluoro]-[2',3'-unsaturated or 3'-modified]-pyrimidine nucleosides
    10.
    发明申请
    [5-carboxamido or 5-fluoro]-[2',3'-unsaturated or 3'-modified]-pyrimidine nucleosides 失效
    [5-甲酰氨基或5-氟] - [2'，3'-不饱和或3'-修饰] - 嘧啶核苷

    公开(公告)号：US20040167140A1

    公开(公告)日：2004-08-26

    申请号：US10759985

    申请日：2004-01-16

    申请人： Emory University

    发明人： Raymond F. Schinazi ,  Dennis C. Liotts

    IPC分类号： A61K031/675 ,  A61K031/513 ,  C07D45/02 ,  C07D49/02

    CPC分类号： A61K31/7068 ,  A61K31/70 ,  A61K45/06 ,  C07H19/06 ,  A61K2300/00

    摘要： A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a null5-carboxamido or 5-fluoronull-2null,3null-dideoxy-2null,3null-didehydro-pyrimidine nucleoside or a null5-carboxamido or 5-fluoronull-3null-modified-pyrimidine nucleoside, or a mixture or a pharmaceutically acceptable derivative thereof, including a 5null or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.

    摘要翻译： 公开了用于治疗人和其他宿主动物中的HIV和HBV感染的方法和组合物，其包括给予有效量的[5-甲酰氨基或5-氟] -2'，3'-二脱氧-2' ，3'-二脱氢嘧啶核苷或[5-甲酰氨基或5-氟] -3'-修饰的嘧啶核苷或其混合物或药学上可接受的衍生物，包括5'或N 4烷基化或酰化 衍生物或其药学上可接受的盐在药学上可接受的载体中。