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    Carboxamides as fungicides in agriculture
    1.
    发明申请
    Carboxamides as fungicides in agriculture 失效
    甲酰胺作为农业杀菌剂

    公开(公告)号：US20040138265A1

    公开(公告)日：2004-07-15

    申请号：US10470069

    申请日：2004-01-12

    发明人： Harald Walter ,  Stephan Trah

    IPC分类号： A61K031/4433 ,  A61K031/4436 ,  A61K031/416 ,  A61K031/427 ,  A61K031/422

    CPC分类号： C07D207/34 ,  C07D231/14 ,  C07D277/56

    摘要： The invention concerns novel carboxamides of formula (I) wherein A is (A1), (A2), (A3), (A4), (A5); Q is (Q1), (Q2), (Q3), (Q4), (Q5), (Q6); R1 is CH2 R2, CH2CHnullCHR2, CHnullCnullCHR2 or COR3; R2 is hydrogen, C1-C6alkyl, C1-C6haloalkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C7cycloalkyl, COOC1-C4alkyl, COOC3-C6alkenyl, COOC3-C6alkynyl or CN; R3 is C1-C6alkyl, C1-C6alkyl substituted by halogen, C1-C6alkoxy or C1-C6haloalkoxy; or is C1-C6alkylthio, C1-C6haloalkylthio, C1-C6alkoxy, C1-C6haloalkoxy; C3-C6alkenyloxy or C3-C6haloalkenyloxy; C3-C6haloalkenyloxy; C3-C6alkynyloxy or C3-C6haloalkynyloxy; R4 is methyl, CF2Cl, CF3, CF2H, CFH2, Cl or Br, R5 is methyl, CF3, CH2OCH3 or CH2OCF3; R6 is hydrogen, fluoro, CF3 or methyl; R7 is hydrogen, methyl or halogen; and Z is phenyl, halophenyl, C5-C7cycloalkyl, C5-C7acycloalkyl substituted by C1-C3alkyl, C1C3haloalkyl or halogen, or a group of the form nullCHR8nullCH2nullCHR9R10 wherein R8, R9 and R10 are independently of each other C1-C3alkyl. The novel compounds have plant-protective properties and are suitable for protecting plants against infestation by phytopathogenic microorganisms, in particular fungi.

    摘要翻译： 本发明涉及式（I）的新型甲酰胺，其中A为（A1），（A2），（A3），（A4），（A5） Q是（Q1），（Q2），（Q3），（Q4），（Q5），（Q6） R 1是CH 2 R 2，CH 2 CH = CHR 2，CH = C = CHR 2或COR 3; R2是氢，C1-C6烷基，C1-C6卤代烷基，C2-C6链烯基，C2-C6炔基，C3-C7环烷基，COOC1-C4烷基，COOC3-C6链烯基，COOC3-C6炔基或CN; R 3是C 1 -C 6烷基，被卤素，C 1 -C 6烷氧基或C 1 -C 6卤代烷氧基取代的C 1 -C 6烷基; 或是C 1 -C 6烷硫基，C 1 -C 6卤代烷硫基，C 1 -C 6烷氧基，C 1 -C 6卤代烷氧基; C3-C6链烯氧基或C3-C6卤代烯氧基; C3-C6卤代烯氧基; C3-C6炔氧基或C3-C6卤代炔氧基; R4是甲基，CF2Cl，CF3，CF2H，CFH2，Cl或Br，R5是甲基，CF3，CH2OCH3或CH2OCF3; R6是氢，氟，CF3或甲基; R7是氢，甲基或卤素; Z是苯基，卤代苯基，C 5 -C 7环烷基，被C 1 -C 3取代的C 5 -C 7环烷基

    Modulation of anxiety through blockade of anandamide hydrolysis
    2.
    发明申请
    Modulation of anxiety through blockade of anandamide hydrolysis 有权
    通过封闭anandamide水解调节焦虑

    公开(公告)号：US20040127518A1

    公开(公告)日：2004-07-01

    申请号：US10681858

    申请日：2003-10-07

    申请人： The Regents of the University of California

    发明人： Daniele Piomelli ,  Andrea Duranti ,  Andrea Tontini ,  Marco Mor ,  Giorgio Tarzia

    IPC分类号： A61K031/444 ,  A61K031/4436 ,  A61K031/4433 ,  A61K031/4025 ,  C07D49/02 ,  C07D45/02

    CPC分类号： C07C311/29 ,  C07C271/56 ,  C07C275/54 ,  C07C2601/14 ,  C07D209/08 ,  C07D211/06 ,  C07D215/06 ,  C07D307/79 ,  C07D487/04

    摘要： Fatty acid amide hydrolase inhibitors of the Formula: 1 are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.

    摘要翻译： 提供了下式的脂肪酸酰胺水解酶抑制剂：其中X是NH，CH 2，O或S; Q是O或S; Z是O或N; R是选自取代或未取代的芳基的芳族部分; 取代或未取代的联苯基，取代或未取代的萘基和取代或未取代的苯基; 取代或未取代的三联苯基; 取代或未取代的环烷基，杂芳基或烷基; 并且R 1和R 2独立地选自H，取代或未取代的烷基，取代或未取代的杂烷基和取代或未取代的苯基，取代或未取代的联苯基，取代或未取代的芳基和取代或未取代的杂芳基; 条件是如果Z是O，则不存在R 1和R 2之一，并且如果Z是N，则任选地R 1和R 2可以任选地一起形成取代或未取代的N-杂环或具有取代或未取代的杂芳基，其中N 它们各自附着的原子。 提供了包含式I化合物的药物组合物及其用于抑制FAAH和/或治疗食欲障碍，青光眼，疼痛，失眠以及包括焦虑障碍，癫痫和抑郁症在内的神经和心理障碍的方法。

    Epothilone derivatives and their synthesis and use
    5.
    发明申请
    Epothilone derivatives and their synthesis and use 失效
    埃坡霉素衍生物及其合成和用途

    公开(公告)号：US20030203938A1

    公开(公告)日：2003-10-30

    申请号：US10386999

    申请日：2003-03-11

    申请人： The Scripps Research Institute

    发明人： Kyriacos Costa Nicolaou ,  Nigel Paul King ,  Maurice Raymond Verschoyle Finlay ,  Yun He ,  Frank Roschangar ,  Dionisios Vourloumis ,  Hans Vallberg ,  Antony Bigot

    IPC分类号： A61K031/4433 ,  A61K031/427 ,  A61K031/4178 ,  C07D417/02 ,  C07D47/02

    CPC分类号： C07D313/00 ,  C07D417/06 ,  C07D493/04 ,  Y02P20/55

    摘要： The invention relates to epothilone analog represented by the formula I 1 wherein (i) R2 is absent or oxygen; nullanull can be either a single or double bond; nullbnull can be either absent or a single bond; and nullcnull can be either absent or a single bond, with the proviso that if R2 is oxygen then nullbnull and nullcnull are both a single bond and nullanull is a single bond; if R2 is absent then nullbnull and nullcnull are absent and nullanull is a double bond; and if nullanull is a double bond, then R2, nullbnull and nullcnull are absent; R3 is a radical selected from the group consisting of hydrogen; lower alkyl; nullCHnullCH2; nullCnullCH; nullCH2F; nullCH2Cl; nullCH2nullOH; nullCH2nullOnull(C1-C6-alkyl); and nullCH2nullSnull(C1-C6-alkyl); R4 and R5 are independently selected from hydrogen, methyl or a protecting group; and R1 is as defined in the specification, or a salt of a compound of the formula I where a salt-forming group is present. A further aspect of the invention is related to the synthesis of epothilone E. These compounds have inter alia microtubuli depolymerisation inhibiting activity and are e.g. useful against proliferative diseases.

    摘要翻译： 本发明涉及由式I表示的埃坡霉素类似物，其中（i）R2不存在或氧; “a”可以是单键或双键; “b”可以是缺席或单一债券; 和“c”可以不存在或单键，条件是如果R2是氧，则“b”和“c”都是单键，“a”是单键; 如果R2不存在，则“b”和“c”不存在，“a”是双键; 如果“a”是双键，那么R2，“b”和“c”不存在; R3是选自氢的基团; 低级烷基 -CH = CH 2; -C = CH; -CH2F; -CH2Cl; -CH 2 -OH; -CH 2 -O-（C 1 -C 6 - 烷基）; 和-CH 2 -S-（C 1 -C 6 - 烷基）; R 4和R 5独立地选自氢，甲基或保护基; R1如本说明书中所定义，或其中存在成盐基团的式I化合物的盐。 本发明的另一方面涉及埃坡霉素E的合成。这些化合物尤其具有微管解聚抑制活性， 对增殖性疾病有用。

    Cannabinoid derivatives, methods of making, and use thereof
    8.
    发明申请
    Cannabinoid derivatives, methods of making, and use thereof 失效
    大麻素衍生物，制备方法及其用途

    公开(公告)号：US20040242593A1

    公开(公告)日：2004-12-02

    申请号：US10850588

    申请日：2004-05-20

    发明人： Bob M. Moore II ,  Antonio M. Ferreira ,  Mathangi Krishnamurthy

    IPC分类号： A61K031/506 ,  A61K031/4433 ,  A61K031/427 ,  A61K031/4025 ,  A61K031/381 ,  C07D45/02 ,  C07D417/02

    CPC分类号： C07D409/04 ,  C07D311/80

    摘要： 1null-substituted cannabinoid derivatives of delta-8-tetrahydrocannabinol, delta-9-tetrahydrocannabinol, and delta-6a-10a-tetrahydrocannabinol that have affinity for the cannabinoid receptor type-1 (CB-1) and/or cannabinoid receptor type-2 (CB-2). Compounds having activity as either agonists or antagonists of the CB-1 and/or CB-2 receptors can be used for treating CB-1 or CB-2 mediated conditions.

    摘要翻译： 对大麻素受体1型（CB-1）和/或大麻素受体2型具有亲和性的δ-8-四氢大麻酚，δ-9-四氢大麻酚和δ-6a-10a-四氢大麻酚的1'-取代大麻素衍生物 （CB-2）。 具有活性作为CB-1和/或CB-2受体的激动剂或拮抗剂的化合物可用于治疗CB-1或CB-2介导的病症。

    Ascorbic acid salts of organic bases with enhanced bioavailability for synergictic anti-aging and skin protective cosmetic compositions
    9.
    发明申请
    Ascorbic acid salts of organic bases with enhanced bioavailability for synergictic anti-aging and skin protective cosmetic compositions 审中-公开
    有机碱的抗坏血酸盐具有增强的生物利用度用于协同抗衰老和皮肤保护性化妆品组合物

    公开(公告)号：US20040067890A1

    公开(公告)日：2004-04-08

    申请号：US10265000

    申请日：2002-10-04

    发明人： Shyam K. Gupta

    IPC分类号： A61K038/05 ,  A61K031/737 ,  A61K031/7008 ,  A61K031/4433 ,  A61K031/375 ,  C07K005/06

    CPC分类号： A61K31/4433 ,  A61K31/375 ,  A61K31/7008 ,  A61K31/737

    摘要： This invention relates to in-situ preparation, and stable topical delivery systems of ascorbic acid salts of organic bases that provide skin beneficial properties, including reduction in signs of skin aging, anti-wrinkle, anti-oxidant, and photo-protection from UV and sunlight. The formulation avoids the use of oils, minimizes the importance of the pH of the formulation, allows the incorporation of an aqueous solution of ascorbic acid or alkali metal salts of ascorbic acid in the formulation, does not require packaging the formulation in air tight containers, allows the use of large amounts of ascorbic acid, its salts, and its derivatives, and does not require the use of expensive coatings. Moreover, several ascorbic acid derivatives of different chemical composition can be made in a stable topical formulation by the in-situ combination of readily available starting materials in a water solution, despite the understanding well known in the prior art that such compositions in water are inherently unstable. The in-situ method also permits the preparation of novel ascorbic acid derivatives that are not known in the prior art.

    摘要翻译： 本发明涉及提供皮肤有益性质的有机碱的抗坏血酸盐的现场制备和稳定的局部递送系统，包括减少皮肤老化，抗皱，抗氧化和光保护免受UV和 阳光。 该制剂避免使用油，使制剂的pH的重要性最小化，允许将抗坏血酸或抗坏血酸的碱金属盐的水溶液掺入制剂中，不需要将制剂包装在气密容器中， 允许使用大量的抗坏血酸，其盐和其衍生物，并且不需要使用昂贵的涂层。 此外，尽管在现有技术中已知的这种在水中的这些组合物是固有的，但是通过在水溶液中容易获得的原料的现场组合，可以在稳定的局部制剂中制备不同化学组成的几种抗坏血酸衍生物 不稳定 原位法还可以制备现有技术中未知的新型抗坏血酸衍生物。

    Frangible compounds for pathogen inactivation
    10.
    发明申请
    Frangible compounds for pathogen inactivation 审中-公开
    用于病原体灭活的易碎化合物

    公开(公告)号：US20040029897A1

    公开(公告)日：2004-02-12

    申请号：US10341917

    申请日：2003-01-13

    申请人： Cerus Corporation

    发明人： David Cook ,  John E. Merritt ,  Aileen Nerio ,  Henry Rapoport ,  Adonis Stassinopoulos ,  Susan Wollowitz

    IPC分类号： A61K031/497 ,  A61K031/4433 ,  A61K031/4025 ,  A61K031/366 ,  C07D493/02

    CPC分类号： C07D405/12 ,  A61L2/0082 ,  A61M1/0209 ,  B01J20/28 ,  C07D219/10 ,  C07D493/04 ,  C07F9/64

    摘要： Compounds and methods for inactivating pathogens in materials are described, including compositions and methods for inactivating pathogens in biological materials such as red blood cell preparations and plasma. The compounds and methods may be used to treat materials intended for in vitro or in vivo use, such as clinical testing or transfusion. The compounds are designed to specifically bind to and react with nucleic acid, and then to degrade to form breakdown products. The degradation reaction is preferably slower than the reaction with nucleic acid.

    摘要翻译： 描述了用于灭活材料中的病原体的化合物和方法，包括用于灭活生物材料如红细胞制剂和血浆中的病原体的组合物和方法。 化合物和方法可以用于治疗用于体外或体内使用的物质，例如临床试验或输血。 该化合物被设计成与核酸特异性结合并与其反应，然后降解以形成分解产物。 降解反应优选比与核酸的反应更慢。