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    3-SUBSTITUTED-[1,2,3]BENZOTRIAZINONE COMPOUNDS FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES
    4.
    发明申请
    3-SUBSTITUTED-[1,2,3]BENZOTRIAZINONE COMPOUNDS FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES 审中-公开
    3-取代的 - [1,2,3]苯并噻嗪酮化合物，用于增强谷氨酸反应性

    公开(公告)号：WO2008085505A1

    公开(公告)日：2008-07-17

    申请号：PCT/US2007/026415

    申请日：2007-12-28

    申请人： CORTEX PHARMACEUTICALS, INC. ,  MUELLER, Rudolf ,  LEE, Stephen ,  O'HARE, Sean ,  ROGERS, Gary ,  RACHWAL, Stan ,  STREET, Leslie

    发明人： MUELLER, Rudolf ,  LEE, Stephen ,  O'HARE, Sean ,  ROGERS, Gary ,  RACHWAL, Stan ,  STREET, Leslie

    IPC分类号： A01N43/64 ,  A61K31/53

    CPC分类号： C07D498/14 ,  C07D253/08 ,  C07D487/04 ,  C07D498/04

    摘要： This invention relates to the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for higher order behaviors. These brain networks are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias and in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia and affective disorders. In a particular aspect, the present invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.

    摘要翻译： 本发明涉及预防和治疗脑功能不全，包括在负责高阶行为的脑网络突触中增强受体功能。 这些脑网络涉及与记忆障碍相关的认知能力，例如在各种痴呆症中观察到的，以及在不同脑区域之间的神经元活动的不平衡，如在帕金森病，精神分裂症和情感障碍等疾病中所提出的。 在一个特定方面，本发明涉及可用于治疗这些病症的化合物，以及使用这些化合物进行这种治疗的方法。

    METHOD OF MAKING 8-FLUORO-NAPHTHALEN-1-YLAMINE AND RELATED COMPOUNDS
    5.
    发明申请
    METHOD OF MAKING 8-FLUORO-NAPHTHALEN-1-YLAMINE AND RELATED COMPOUNDS 审中-公开
    制备8-氟萘-1-胺及相关化合物的方法

    公开(公告)号：WO2007049124A1

    公开(公告)日：2007-05-03

    申请号：PCT/IB2006/002979

    申请日：2006-10-13

    申请人： PFIZER PRODUCTS INC. ,  ZHU, Zhijian

    发明人： ZHU, Zhijian

    IPC分类号： C07C209/62 ,  C07D241/04 ,  C07C211/59

    CPC分类号： C07D295/067 ,  C07C209/64 ,  C07D253/08 ,  C07C211/59

    摘要： A process is described for preparing 8-flouro-napthalen-l-ylamine comprising reacting lH-naphtlio[l,8-de][l,2,3]triazine with hydrogen fluoride or a complex of hydrogen fluoride and an n-donor base. A process is also set forth for using 8-fluoro- naphthalen-1-ylamine produced as described above in the preparation of l-(8-fluoro- napthalen-l-yl)-piperazine, which can be used as an intermediate in the production of 7- { 4- [4-(8-fluoro-napthalen- 1 -yl)-piperazin- 1 -yl] -butoxy } -3 ,4-dihydro- IH- [l,8]naphthyridin-2-one, a D2 partial agonist indicated for possible use in the treatment of schizophrenia.

    摘要翻译： 描述了一种制备8-三氟萘-1-基胺的方法，其包括使1H-萘并[1,8-de] [1,2,3]三嗪与氟化氢或氟化氢和N-供体碱的配合物 。 还阐述了使用如上所述制备的8-氟萘-1-基胺在1-（8-氟 - 萘-1-基） - 哌嗪的制备方法中的方法，该1-（8-氟 - 萘-1-基） - 哌嗪可用作 制备7- {4- [4-（8-氟 - 萘-1-基） - 哌嗪-1-基] - 丁氧基} -3,4-二氢-1H- [1,8]萘啶-2-酮 ，D2部分激动剂表明可能用于治疗精神分裂症。

    3-HYDROXY-4-OXO-1,2,3-TRIAZINES AND DERIVATIVES THEREOF FOR AMIDE AND ESTER BOND FORMATION
    6.
    发明申请
    3-HYDROXY-4-OXO-1,2,3-TRIAZINES AND DERIVATIVES THEREOF FOR AMIDE AND ESTER BOND FORMATION 审中-公开
    3-羟基-4-氧代-1,2,3-三唑及其衍生物，用于酰胺和酯键形成

    公开(公告)号：WO2005007634A1

    公开(公告)日：2005-01-27

    申请号：PCT/IL2004/000652

    申请日：2004-07-18

    申请人： FRUTAROM LTD. ,  SHPERNAT, Yaacov ,  MIZHIRITSKII, Michael

    发明人： SHPERNAT, Yaacov ,  MIZHIRITSKII, Michael

    IPC分类号： C07D253/04

    CPC分类号： C07D253/08 ,  C07D253/04 ,  C07D471/04 ,  C07D487/04 ,  C07F9/65218 ,  C07F9/65583 ,  C07F9/6561

    摘要： The present invention relates to the use of a compound of formula I as a coupling reagent in forming amide or ester bonds from a reaction between a carboxylic acid and an amine or an alcohol, respectively. The compounds of formula I are especially useful as coupling reagents in the preparation of peptide bonds during peptide synthesis. In particular, the compounds of formula I are useful in promoting the formation of reactive reaction intermediates, inhibiting side reactions and in suppression of racemization. In addition, the present invention provides novel compounds of Formula I, and salts of N-oxides thereof.

    摘要翻译： 本发明涉及分别由羧酸和胺或醇之间的反应形成酰胺或酯键的式I化合物作为偶联剂的用途。 在肽合成期间，式I化合物特别可用作偶联试剂在制备肽键中。 特别地，式I化合物可用于促进反应中间体的形成，抑制副反应和抑制外消旋化。 此外，本发明提供新的式I化合物及其N-氧化物的盐。

    HYDROXAMATE DERIVATIVES OF NON-STEROIDAL ANTI-INFLAMMATORY DRUGS
    7.
    发明申请
    HYDROXAMATE DERIVATIVES OF NON-STEROIDAL ANTI-INFLAMMATORY DRUGS 审中-公开
    非甾体抗炎药物的羟肟酸衍生物

    公开(公告)号：WO2004000215A2

    公开(公告)日：2003-12-31

    申请号：PCT/US2003/019228

    申请日：2003-06-17

    申请人： MEDINOX, INC. ,  WANG, Tingmin ,  LAI, Ching-San

    发明人： WANG, Tingmin ,  LAI, Ching-San

    IPC分类号： A61K

    CPC分类号： C07D253/08 ,  A61K31/425 ,  A61K31/53 ,  C07C259/06 ,  C07C259/10 ,  C07C271/08 ,  C07C311/48 ,  C07C317/44 ,  C07C323/60 ,  C07D209/28 ,  C07D277/36

    摘要： In accordance with the present invention, there are provided novel chemical entities which have multiple utilities, e.g., as prodrugs of NSAIDs; as dual inhibitors of cyclooxygenase (COX) and 5-lipoxygenase (5-LO); as anticancer agents (through promoting apoptosis and/or inhibiting the matrix metalloproteinases (MMPs); as anti-diabetics; and the like. Invention compounds comprise a non-steroidal anti-inflammatory agent (NSAID), covalently linked to a hydroxamate. Invention compouds are useful alone or in combination with one or more additional pharmacologically active agents, and can be used for a variety of applications, such as, for example, treating inflammation and inflammation-related conditions; reducing the side effects associated with administration of anti-inflammatory agents; promoting apoptosis; inhibiting matrix metalloproteinases; as anti-diabetic agents; and the like.

    摘要翻译： 根据本发明，提供了具有多种用途的新型化学实体，例如作为NSAID的前药; 作为环氧合酶（COX）和5-脂氧合酶（5-LO）的双重抑制剂; 作为抗癌剂（通过促进细胞凋亡和/或抑制基质金属蛋白酶（MMPs））;作为抗糖尿病药物等。本发明化合物包含与羟肟酸共价连接的非甾体抗炎药（NSAID）。 可单独使用或与一种或多种另外的药理活性剂组合使用，并且可用于各种应用，例如治疗炎症和炎症相关病症;减少与施用抗炎药相关的副作用 促进细胞凋亡;抑制基质金属蛋白酶;作为抗糖尿病药物等。