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    Proton exchange membrane materials based on sulfonated poly (phthalazinones)
    54.
    发明申请
    Proton exchange membrane materials based on sulfonated poly (phthalazinones) 有权
    基于磺化聚（2,3-二氮杂萘酮）的质子交换膜材料

    公开(公告)号：US20060155127A1

    公开(公告)日：2006-07-13

    申请号：US10529020

    申请日：2003-09-25

    申请人： Yan Gao ,  Michael Gulver ,  Gilles Robertson ,  Xigao Jian

    发明人： Yan Gao ,  Michael Gulver ,  Gilles Robertson ,  Xigao Jian

    IPC分类号： H01M2/14 ,  C07D237/30

    CPC分类号： C08J5/2256 ,  C08G65/4037 ,  C08G65/48 ,  C08G73/0694 ,  C08J2379/04 ,  H01M8/1027 ,  H01M8/103 ,  H01M8/1032 ,  H01M2300/0082

    摘要： A novel class of proton exchange membrane materials, sulfonated poly(phthalazinones), were prepared by modification of poly(phthalazinone). Sulfonation reactions were conducted at room temperature using mixtures of 95-98% concentrated sulfuric acid and 27-33% fuming sulfuric acid with different acid ratios in order to get SPPEK with degree of sulfonation (DS) in the range of 0.6 to 1.0. The presence of sulfonic acid groups was confirmed by FT-IR analysis, and the DS and structures were characterized by NMR. The introduction of sulfonic groups into the polymer chains led to an increase in the glass transition temperature and a decrease in the decomposition temperature. Membrane films were cast from solution in N,N-dimethylformamide or N,N-dimethylacetamide. Water uptakes and swelling ratios of the membrane films increased with DS and sulfonated polymers with DS>1.2 were water soluble at 80° C. Proton conductivity increased with DS and temperature up to 95° C., reaching 10−2S/Cm.

    摘要翻译： 通过改性聚（酞嗪酮）制备了一类新颖的质子交换膜材料，磺化聚（2,3-二氮杂萘酮）。 使用95-98％浓硫酸和27-33％发烟硫酸的混合物在室温下进行磺化反应，以使得具有0.6-1.0的磺化度（DS）的SPPEK。 通过FT-IR分析证实磺酸基团的存在，并通过NMR表征DS和结构。 在聚合物链中引入磺基导致玻璃化转变温度的升高和分解温度的降低。 从N，N-二甲基甲酰胺或N，N-二甲基乙酰胺中的溶液中浇铸膜膜。 DS的吸水率和溶胀比随DS增加，DS> 1.2的磺化聚合物在80℃水溶性。质子传导性随着DS而升高，达到95℃，达到10〜 SUP> S / Cm。

    Preparation of prodrugs for selective drug delivery
    56.
    发明申请
    Preparation of prodrugs for selective drug delivery 审中-公开
    用于选择性药物递送的前药的制备

    公开(公告)号：US20050080260A1

    公开(公告)日：2005-04-14

    申请号：US10828558

    申请日：2004-04-21

    申请人： Randell Mills ,  Guo-Zhang Wu

    发明人： Randell Mills ,  Guo-Zhang Wu

    IPC分类号： C07C221/00 ,  C07C225/22 ,  C07D209/48 ,  C07D237/32 ,  C07D405/14 ,  C07D487/04 ,  C07D237/30 ,  C07C211/27

    CPC分类号： C07D209/48 ,  C07C221/00 ,  C07D237/32 ,  C07D405/14 ,  C07D487/04 ,  C07C225/22

    摘要： Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

    摘要翻译： 合成具有式A-B-C的化合物，其可用于例如药物递送的应用，其中A是化学发光部分，B是光致变色部分，C是其中A-B-C可以用作前药的生物活性部分。 形成前药的本发明的新型合成方法包括以下步骤：（1）形成二苯甲酮，（2）形成二芳基乙烯，（3）将邻苯二甲酰亚胺部分连接至乙烯的至少一个芳基以形成 邻苯二甲酰亚胺 - 乙烯共轭物，（4）缩合两个乙烯 - 邻苯二甲酰亚胺共轭物以形成邻苯二甲酰亚胺 - 戊二烯缀合物，（5）通过与肼反应形成本发明的载体化合物，将邻苯二甲酰亚胺转化为邻苯二甲酰肼 ）使载体化合物与药物的亲核部分反应形成相应的前药。 或者，可以通过使用卤素取代的二芳基乙烯以已知方法制备相应的阳离子无色染料样化合物来制备载体。 然后通过与亲核试剂反应保护阳离子化合物，并通过钯催化的胺化与氨基间苯二酰胺偶联以形成受保护的邻苯二甲酰亚胺 - 戊二烯缀合物。 将后者与肼回流以将其邻苯二甲酰亚胺转化为邻苯二甲酰肼并酸化以得到载体。 本发明的另一方面涉及这些化合物作为抗病毒剂用于治疗病毒感染如HIV的用途，以及用作治疗诸如肠，肺和乳腺癌的癌症的抗癌剂。

    Phthalazine derivatives as phosphodiesterase 4-inhibitors
    57.
    发明申请
    Phthalazine derivatives as phosphodiesterase 4-inhibitors 审中-公开
    酞嗪衍生物作为磷酸二酯酶4-抑制剂

    公开(公告)号：US20040043999A1

    公开(公告)日：2004-03-04

    申请号：US10441177

    申请日：2003-05-20

    申请人： Zambon Group S.p.A

    发明人： Mauro Napoletano ,  Gabriele Norcini ,  Daniela Botta ,  Giancarlo Grancini ,  Gabriele Morazzoni ,  Francesco Santangelo ,  Jorge G. Siro Herrero ,  Jose Luis Garcia Navaio ,  Julio G. Alvarez-Builla

    IPC分类号： C07D237/30 ,  A61K031/502

    CPC分类号： C07D401/06 ,  C07D237/30 ,  C07D237/34 ,  C07D401/12 ,  C07D405/12

    摘要： A process for preparing a compound of formula I: 1 wherein G is methylene, ethylene, CONH, amino or a bond; R is H, phenyl or a (C1-4)alkyl group optionally substituted by phenyl; Cy is phenyl or a 5- or 6-membered heterocycle of the group consisting of pyrrole, imidazole, pyrazole, pyrrolidine, pyrroline, imidazoline, imidazolidine, pyrazolidine, pyrazoline, pyridine, pyrazine, pyrimidine, pyridazine, piperazine, piperidine, and triazine, the Cy residue being optionally substituted by one or more substituent(s) selected from the group consisting of keto, nitro, carboxy, fluorine, chlorine, bromine, or iodine; R1 is a (C1-6)alkyl or polyfluoro(C1-6)alkyl group; and R2 is aryl, aryl-(C1-10)-alkyl, (C4-7)cycloalkyl or (C4-7)heterocycle wherein the heteroatom is an oxygen atom.

    摘要翻译： 制备式I化合物的方法：其中G是亚甲基，亚乙基，CONH，氨基或键; R是H，苯基或任选被苯基取代的（C 1-4）烷基; Cy是苯基或由吡咯，咪唑，吡唑，吡咯烷，吡咯啉，咪唑啉，咪唑烷，吡唑烷，吡唑啉，吡啶，吡嗪，嘧啶，哒嗪，哌嗪，哌啶和三嗪组成的组的5-或6-元杂环， Cy残基任选被一个或多个选自酮，硝基，羧基，氟，氯，溴或碘的取代基取代; R1是（C1-6）烷基或多氟（C1-6）烷基; 并且R 2是芳基，芳基 - （C 1-10） - 烷基，（C 4-7）环烷基或（C 4-7）杂环，其中杂原子是氧原子。

    MEDICINAL PREPARATION AND PROCESS FOR MANUFACTURING THEREOF
    58.
    发明申请
    MEDICINAL PREPARATION AND PROCESS FOR MANUFACTURING THEREOF 有权
    药物制剂及其制备方法

    公开(公告)号：US20020198208A1

    公开(公告)日：2002-12-26

    申请号：US09979846

    申请日：2001-11-28

    发明人： Musa Tazhudinovich Abidov ,  Alexandr Petrovich Khokhlov

    IPC分类号： A61K031/502 ,  C07D237/30

    CPC分类号： A61K31/502 ,  C07D237/32

    摘要： The present invention can be used in medical practice specifically in chemical and pharmaceutical production of medicinal agents capable of modulating the immune system. This invention essentially relates to a new medicinal preparation 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt having immunomodulatory, antiinflammatory, and antioxidant properties. The preparation is obtained from 3-nitro-phthalanhydride by consecutive isolation of intermediate and end products. The intermediate products include 5-nitro-2,3-dihydrophthalazine-1,4-dione and 5-amino-2,3-dihydrophthala2ine-1,4-dione. The reaction between 5-amino-2,3-dihydrophthalazine-1,4-dione and sodium hydroxide yields the target product, 5-animo-2,3-dihydrophthalazine-1,4-dione sodium salt. The method allows to produce the medicinal preparation with high pharmaceutical activity. It is provided an example of application of this preparation.

    摘要翻译： 本发明可以用于能够调节免疫系统的药剂的化学和药物生产中的医学实践。 本发明基本上涉及具有免疫调节，抗炎和抗氧化性质的新的药用制剂5-氨基-2,3-二氢酞嗪-1,4-二酮钠盐。 通过连续分离中间产物和最终产物，从3-硝基 - 邻苯二甲酸酐获得制备。 中间产物包括5-硝基-2,3-二氢酞嗪-1,4-二酮和5-氨基-2,3-二氢酞嗪-2,4-二酮。 5-氨基-2,3-二氢酞嗪-1,4-二酮与氢氧化钠的反应得到目标产物5-苯并-2,3-二氢酞嗪-1,4-二酮钠盐。 该方法允许制备具有高药用活性的药物制剂。 提供了该制剂的应用实例。

    Pyridazinone derivatives
    59.
    发明申请
    Pyridazinone derivatives 失效
    哒嗪酮衍生物

    公开(公告)号：US20020026048A1

    公开(公告)日：2002-02-28

    申请号：US09732901

    申请日：2000-12-11

    申请人： Sumitomo Chemical Co. Ltd.

    发明人： Takashi Komori

    IPC分类号： A01N043/58 ,  C07D237/04 ,  C07D237/30

    CPC分类号： C07D237/14 ,  A01N43/58 ,  C07D237/26 ,  C07D237/30

    摘要： This invention provides pyridazinone derivatives encompassed by the following the formula: 1 wherein, R1, R2, R3, R4, R5 and R7 represent a hydrogen atom and the like, and R6 represents a C1-C3 alkyl and the like. The pyridazinone derivatives have excellent herbicidal activity, therefore, they can be used as an active ingredient for herbicidal compositions and can be utilized in herbicidal method, which are also described.

    摘要翻译： 本发明提供下列通式所示的哒嗪酮衍生物：其中R1，R2，R3，R4，R5和R7代表氢原子等，R6表示C1-C3烷基等。 哒嗪酮衍生物具有优异的除草活性，因此它们可以用作除草组合物的活性成分，并且可以用于还描述的除草方法中。

    1-arylphthalazine antagonists of excitatory amino acid receptors
    60.
    发明授权
    1-arylphthalazine antagonists of excitatory amino acid receptors 失效
    兴奋性氨基酸受体的1-芳基酞嗪拮抗剂

    公开(公告)号：US6048853A

    公开(公告)日：2000-04-11

    申请号：US588549

    申请日：1996-01-18

    申请人： Mark A. Collins ,  Jeffrey C. Pelletier

    发明人： Mark A. Collins ,  Jeffrey C. Pelletier

    IPC分类号： A61K31/502 ,  A61K31/5025 ,  A61P9/00 ,  A61P25/08 ,  A61P25/18 ,  A61P43/00 ,  C07D237/30 ,  C07D491/04 ,  C07D491/056 ,  A61K31/50

    CPC分类号： C07D491/04 ,  A61K31/502 ,  C07D237/30

    摘要： Substituted 1-arylphthalazine compositions with the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independentlya) H,b) HO,c) R.sup.11 O--,d) halogen,e) C1-C3-alkyl,f) CF.sub.3,g) R.sup.12 CO.sub.2 --, orh) R.sup.12 CONH--;R.sup.1 and R.sup.2, or R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4 can be taken together to bea) --OCH.sub.2 O--, orb) --OCH.sub.2 CH.sub.2 O--;R.sup.5 isa) H,b) C1-C6-alkyl,c) C3-C6-alkenyl,d) C3-C6-alkynyl,e) C3-C6-cycloalkyl,f) phenyl or substituted phenyl, wherein the phenyl is substituted with one or two substituents selected from the group consisting of C1-C3-alky, halogen, R.sup.12 HN--, R.sup.12 O--, CF.sub.3 --, R.sup.13 SO.sub.2 -- and CO.sub.2 R.sup.12, org) phenyl-C1-C3-alkyl or substituted phenyl-C1-C3-alkyl, wherein the phenyl is substituted with one or two substituents selected from the group consisting of C1-C3-alkyl, halogen, R.sup.12 HN--, R.sup.12 O--, CF.sub.3 --, R.sup.13 SO.sub.2 -- and --CO.sub.2 R.sup.12 ;R.sup.6 isa) R.sup.10 R.sup.11 N--,b) R.sup.10 NHC(NH)--,c) R.sup.12 CONH--,d) 1-pyrrolidino ore) 1-piperidino;R.sup.7 is H;R.sup.8 and R.sup.9 are independentlya) H,b) C1-C3-alkyl,c) halogen,d) R.sup.12 O--,e) CF.sub.3 --, orf) --CO.sub.2 R.sup.12 ;R.sup.10 and R.sup.11 are independentlya) H,b) C1-C10-alkyl,c) C1-C6-perfluoroalkyl,d) C3-C10-alkenyl,e) C3-C10-alkynyl, orf) C3-C6-cycloalkyl;R.sup.12 is H or C1-C3-alkyl; andR.sup.13 is C1-C3-alkyl or CF.sub.3 ;and pharmaceutically acceptable salts thereof,

    摘要翻译： 具有下式的取代的1-芳基酞嗪组合物其中R 1，R 2，R 3和R 4独立地为a）H，b）HO，c）R 11 O-，d）卤素，e）C 1 -C 3 - 烷基，f）CF 3，g）R 12 CO 2 - 或h）R12CONH-; R 1和R 2，或R 2和R 3，或R 3和R 4可以一起为a）-OCH 2 O-或b）-OCH 2 CH 2 O-; R 5是a）H，b）C 1 -C 6 - 烷基，c）C 3 -C 6 - 烯基，d）C 3 -C 6 - 炔基，e）C 3 -C 6 - 环烷基，f）苯基或取代的苯基，其中苯基被取代 具有一个或两个选自C 1 -C 3 - 烷基，卤素，R 12 HN-，R 12 O-，CF 3 - ，R 13 SO 2 - 和CO 2 R 12的取代基，或g）苯基-C 1 -C 3 - 烷基或取代的苯基-C 1 -C 3 - 烷基，其中苯基被一个或两个选自C1-C3-烷基，卤素，R12HN-，R12O-，CF3-，R13SO2-和-CO2R12的取代基取代; R6是a）R10R11N-，b）R10NHC（NH） - ，c）R12CONH-，d）1-吡咯烷子基或e）1-哌啶子基; R7为H; R 8和R 9独立地是a）H，b）C 1 -C 3 - 烷基，c）卤素，d）R 12 O-，e）CF 3 - 或f）-CO 2 R 12; R 10和R 11独立地是a）H，b）C 1 -C 10 - 烷基，c）C 1 -C 6全氟烷基，d）C 3 -C 10 - 烯基，e）C 3 -C 10炔基，或f）C 3 -C 6环烷基; R12是H或C1-C3-烷基; 和R 13是C 1 -C 3 - 烷基或CF 3; 及其药学上可接受的盐，