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    Diaminopyrazole derivatives and dyes containing said compounds
    2.
    发明授权
    Diaminopyrazole derivatives and dyes containing said compounds 有权
    含有所述化合物的二氨基吡唑衍生物和染料

    公开(公告)号：US06600050B2

    公开(公告)日：2003-07-29

    申请号：US10221295

    申请日：2002-09-09

    申请人： Laurent Chassot ,  Hans-Juergen Braun

    发明人： Laurent Chassot ,  Hans-Juergen Braun

    IPC分类号： C07D48702

    CPC分类号： C07D231/38

    摘要： Diaminopyrazole derivatives of the general Formula (I) or their physiological tolerated, water-soluble salts with inorganic or organic acids, and agents, containing these compounds, for the oxidative dyeing of fibers.

    摘要翻译： 通式（I）的二氨基吡唑衍生物或其与无机或有机酸的生理上可接受的水溶性盐和含有这些化合物的试剂用于纤维的氧化染色。

    Ricin inhibitors and methods for use thereof
    4.
    发明授权
    Ricin inhibitors and methods for use thereof 失效
    蓖麻毒素抑制剂及其使用方法

    公开(公告)号：US06562969B1

    公开(公告)日：2003-05-13

    申请号：US09535460

    申请日：2000-03-24

    申请人： Jon Robertus ,  Sean Kerwin ,  Xinjian Yan

    发明人： Jon Robertus ,  Sean Kerwin ,  Xinjian Yan

    IPC分类号： C07D48702

    CPC分类号： C07D239/47 ,  C07D239/48 ,  C07D239/545 ,  C07D285/22 ,  C07D285/24 ,  C07D473/18 ,  C07D475/04 ,  C07D487/04 ,  C07D513/04 ,  C12Q1/34 ,  G01N33/5308 ,  G01N33/56916

    摘要： Ricin A-chain is an N-glycosidase that attacks ribosomal RNA at a highly conserved adenine residue. Crystallographic studies show that not only adenine and formycin, but also pterin-based rings can bind in the ricin active site. For a better understanding of the recognition mode between ricin, and adenine-like rings, the interaction energies and geometries were calculated for a number of complexes. Shiga toxin, a compound essentially identical to the protein originally isolated from Shigella dysenteniae, has an active protein chain that is a homologue of the ricin active chain, and catalyzes the same depurination reaction. The present invention is drawn to identifying inhibitors of ricin and Shiga toxin, using methods molecular mechanics and ab initio methods and using the identified inhibitors as antidotes to ricin or Shiga toxin, or to facilitate immunotoxin treatment by controlling non-specific cytotoxicity.

    摘要翻译： 蓖麻毒素A链是一种在高度保守的腺嘌呤残基下攻击核糖体RNA的N-糖苷酶。 晶体学研究表明，不仅腺嘌呤和霉素，而且基于蝶呤的环可以在蓖麻毒素活性位点结合。 为了更好地了解蓖麻毒蛋白和腺嘌呤样环之间的识别模式，计算了多种复合物的相互作用能和几何形状。 志贺毒素，一种与最初从志贺氏菌志愿菌中分离的蛋白质基本相同的化合物，具有活性蛋白质链，其是蓖麻毒素活性链的同系物，并催化相同的去血反应。 本发明涉及鉴定蓖麻毒素和志贺毒素的抑制剂，使用分子力学和从头法，并使用鉴定的抑制剂作为蓖麻毒素或志贺毒素的解毒剂，或通过控制非特异性细胞毒性促进免疫毒素治疗。

    Pigmented vitreous material
    6.
    发明授权
    Pigmented vitreous material 失效
    着色玻璃质材料

    公开(公告)号：US06737533B2

    公开(公告)日：2004-05-18

    申请号：US10335727

    申请日：2003-01-02

    申请人： Véronique Hall-Goulle ,  Zhimin Hao

    发明人： Véronique Hall-Goulle ,  Zhimin Hao

    IPC分类号： C07D48702

    CPC分类号： C07D409/12 ,  C03C14/008 ,  C03C17/007 ,  C03C17/009 ,  C03C17/28 ,  C03C2214/17 ,  C03C2214/32 ,  C03C2217/485 ,  C03C2218/113 ,  C07D209/46 ,  C07D487/04 ,  C07D493/04 ,  Y10T428/10 ,  Y10T428/1095 ,  Y10T428/131

    摘要： The present application relates to a process for the manufacture of pigmented vitreous materials, as well as to pigmented vitreous materials, characterized by the use of soluble pigment precursors and preferably the absence of significant amounts of dispersants. These pigmented vitreous materials can be used as coloured materials for any known purposes. Soluble pigment precursors comprising a partial structure: are also claimed, wherein X1 is an aromatic or heteroaromatic ring, B is hydrogen or a group of the formula: but at least one group B is not hydrogen, and L is a solubilizing group.

    摘要翻译： 本申请涉及一种用于制备着色玻璃质材料的方法，以及着色的玻璃质材料，其特征在于使用可溶性颜料前体，优选不存在显着量的分散剂。 这些着色的玻璃质材料可以用作任何已知目的的有色材料。 还要求保护含有部分结构的可溶性颜料前体，其中X1是芳族或杂芳族环，B是氢或下列基团：但至少一个B不是氢，L是增溶基团。

    Macrocyclic compounds having nitrogen-containing linkages
    7.
    发明授权
    Macrocyclic compounds having nitrogen-containing linkages 失效
    具有含氮键的大环化合物

    公开(公告)号：US06207826B1

    公开(公告)日：2001-03-27

    申请号：US08410703

    申请日：1995-03-27

    申请人： Phillip Dan Cook ,  Charles J. Guinosso ,  Pei-Pei Kung ,  Allister S. Fraser

    发明人： Phillip Dan Cook ,  Charles J. Guinosso ,  Pei-Pei Kung ,  Allister S. Fraser

    IPC分类号： C07D48702

    CPC分类号： C07D471/08 ,  B01J2219/0072 ,  C07D515/08

    摘要： Novel macrocyclic compounds are constructed to include a ring or ring system having two bridgehead atoms with a bridge extending between the bridgehead atoms. Located in at least the bridge are two or more nitrogenous moieties that are derivatized with chemical functional groups. The ring or ring systems can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring. These can also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the library.

    摘要翻译： 构建新的大环化合物以包括具有两个桥头原子的环或环体系，桥桥原子之间延伸有桥。 位于至少桥上是两个或更多个用化学官能团衍生的含氮部分。 环或环系统可以包括作为环原子的另外的含氮部分或连接到环上的侧基上。 这些也可以用化学官能团衍生化。 化学官能团的整体赋予化合物某些构象和其他性质。 根据本发明的某些实施方案，利用化学官能团和含氮部分的置换和组合来制备这些化合物的文库，从而构建文库的复杂性。

    Substituted cyclic compounds and mixtures comprising same
    8.
    发明授权
    Substituted cyclic compounds and mixtures comprising same 失效
    取代的环状化合物和包含它们的混合物

    公开(公告)号：US06191273B1

    公开(公告)日：2001-02-20

    申请号：US09148762

    申请日：1998-09-04

    申请人： Phillip Dan Cook ,  Haoyun An ,  Becky Haly ,  Tingmin Wang

    发明人： Phillip Dan Cook ,  Haoyun An ,  Becky Haly ,  Tingmin Wang

    IPC分类号： C07D48702

    CPC分类号： C40B40/04 ,  C07D471/08 ,  C40B50/08

    摘要： Novel chemical compounds and mixtures of same are provided having antibacterial and other utilities. The mixtures preferably are formed by reacting a cyclic scaffold moiety with a set of chemical substituients. Libraries formed in accordance with the invention have utility per se and are articles of commerce. They can be used to screen for pesticides, drugs and other biologically active compounds.

    摘要翻译： 提供新的化合物及其混合物具有抗菌和其他效用。 混合物优选通过使环状支架部分与一组化学取代基反应而形成。 根据本发明形成的图书馆本身具有效用，并且是商品。 它们可用于筛选农药，药物和其他生物活性化合物。

    Substituted pyrazinoquinoxaline derivatives as serotonin receptor agonist and antagonists ligands
    9.
    发明授权
    Substituted pyrazinoquinoxaline derivatives as serotonin receptor agonist and antagonists ligands 有权
    取代的吡嗪喹喔啉衍生物作为血清素受体激动剂和拮抗剂配体

    公开(公告)号：US06638934B2

    公开(公告)日：2003-10-28

    申请号：US10026404

    申请日：2001-12-19

    申请人： Albert Robichaud ,  Ian S. Mitchell ,  Taekyu Lee ,  Wenting Chen

    发明人： Albert Robichaud ,  Ian S. Mitchell ,  Taekyu Lee ,  Wenting Chen

    IPC分类号： C07D48702

    CPC分类号： C07D487/04

    摘要： The present invention is directed to novel compounds represented by structural Formulas (I) and (I-a): or a pharmaceutically acceptable salt thereof, wherein R1, R4a, R4b, R5, R6, R7, R8, R9, n, and X are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep and sexual disorders, migraine and other conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

    摘要翻译： 本发明涉及由结构式（I）和（Ia）表示的新化合物：或其药学上可接受的盐，其中R 1，R 4a，R 4b，R 5， R 6，R 7，R 8，R 9，n和X如本文所述。 本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。 本发明的化合物是血清素激动剂和拮抗剂，可用于控制或预防中枢神经系统疾病，包括肥胖症，焦虑症，抑郁症，精神病，精神分裂症，睡眠和性障碍，偏头痛和与头痛相关的其他病症，社交恐怖症 ，以及胃肠道疾病如胃肠道运动功能障碍。

    Direct preparation of pyrrolo[3,4-C]pyrroles
    10.
    发明授权
    Direct preparation of pyrrolo[3,4-C]pyrroles 有权
    直接制备吡咯并[3,4-C]吡咯

    公开(公告)号：US06361594B1

    公开(公告)日：2002-03-26

    申请号：US09503266

    申请日：2000-02-14

    申请人： Shivakumar B. Hendi

    发明人： Shivakumar B. Hendi

    IPC分类号： C07D48702

    CPC分类号： C07D487/04 ,  C09B57/004 ,  C09B67/0033

    摘要： A process is disclosed for the direct preparation of pigmentary 1,4-diketopyrrolo-[3,4-c]pyrroles of the formula (I) wherein each of R1 and R2 independently of the other is an isocyclic or heterocyclic aromatic radical, which process comprises heating an appropriate molar ratio of a disuccinate with a nitrile of the formula (II) R1—CN  (II) or of the formula (III) R2—CN  (III) or with mixtures of said nitrites, in an organic solvent and in the presence of a strong base and an effective amount of a selected particle growth inhibitor of formula (IV)-(X), and then obtaining the compound of formula (I) from the reaction product by protolysis. The process yields pigmentary 1,4-diketopyrrolo-[3,4-c]pyrroles directly, i.e., without the need for additional particle-size reducing aftertreatments. Also disclosed is a composition comprising a pigmentary 1,4-diketopyrrolo-[3,4-c]pyrrole and the particle growth inhibitor. These pigment compositions are useful for pigmenting high molecular weight organic materials.

    摘要翻译： 公开了用于直接制备式（I）的颜料1,4-二酮吡咯并[3,4-c]吡咯的方法，其中R 1和R 2各自独立地是一个环状或杂环的芳族基团，该方法 包括在有机溶剂中和在强碱和有效量的存在下，将二琥珀酸与式（II）或式（III）的腈或与所述亚硝酸酯的混合物的合适摩尔比加热 选择的式（IV） - （X）的颗粒生长抑制剂，然后通过原溶解从反应产物获得式（I）化合物。 该方法直接产生颜料1,4-二酮吡咯并[3,4-c]吡咯，即不需要额外的粒度减小后处理。 还公开了包含颜料1,4-二酮吡咯并[3,4-c]吡咯和颗粒生长抑制剂的组合物。 这些颜料组合物可用于着色高分子量有机材料。