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    • 1. 发明申请
    • Activation of natural killer cells by adenosine A3 receptor agonists
    • 通过腺苷A3受体激动剂激活天然杀伤细胞
    • US20040204481A1
    • 2004-10-14
    • US09832818
    • 2001-04-12
    • Pnina Fishman
    • A61K031/7076A61K031/695A61K031/52
    • A61K31/52A61K31/00A61K31/70A61K31/7076
    • The present invention is based on the surprising finding that adenosine A3 receptor agonists (A3RAg) are capable of activating natural killer (NK) cells. In particular, methods and pharmaceutical compositions for activating NK cells in an individual comprising administering said individual with an effective amount of one or more A3RAg are provided herein. A further method includes treatment of a disease comprising administering to an individual in need of such treatment NK cells a priori activated with an effective amount of at least one A3RAg. The NK cells may be either autologous cells or cells withdrawn from a donor individual. Further provided are pharmaceutical compositions comprising one or more A3RAg in an amount effective to achieve a therapeutic effect, the therapeutic effect comprising activation of NK cells, the pharmaceutical composition optionally comprising physiologically acceptable additives.
    • 本发明基于令人惊奇的发现,即腺苷A3受体激动剂(A3RAg)能够激活天然杀伤(NK)细胞。 特别地,本文提供了用于激活个体中的NK细胞的方法和药物组合物,其包括给予所述个体有效量的一种或多种A3RAg。 另一种方法包括治疗疾病,其包括向需要这种治疗的个体施用先天用有效量的至少一种A3RAg活化的NK细胞。 NK细胞可以是自体细胞或从供体个体中取出的细胞。 还提供了包含一种或多种有效实现治疗效果的量的一种或多种A3RAg的药物组合物,所述治疗效果包括NK细胞的活化,所述药物组合物任选包含生理上可接受的添加剂。
    • 5. 发明申请
    • Radicicol derivatives
    • 蓝霉素衍生物
    • US20040053990A1
    • 2004-03-18
    • US10629655
    • 2003-07-30
    • KYOWA HAKKO KOGYO CO., LTD
    • Yoji InoNobuyoshi AmishiroMayumi MiyataChikara MurakataHarumi OgawaTadakazu AkiyamaShiro AkinagaShiro SogaYukimasa Shiotsu
    • A61K031/695A61K031/365A61K031/4433A61K031/4025C07D313/20C07D45/02
    • C07D493/04C07D313/00
    • Radicicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: 1 wherein R1 and R2 are the same or different, and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl or tert-butyldimethylsilyl; R3 represents YnullR5 nullwherein Y represents substituted or unsubstituted alkylene; and R5 represents CONR6R7 (wherein R6 represents hydrogen, hydroxyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted higher alkyl, and the like; R7 represents hydroxyl, substituted lower alkyl, and the like), CO2R12 (wherein R12 represents substituted lower alkyl, substituted or unsubstituted higher alkyl, and the like), and the likenull and the like; X represents halogen or is combined together with R4 to represent a single bond; and R4 is combined together with X to represent a single bond, or represents hydrogen, alkanoyl, and the like.
    • 由下式(I)表示的具有酪氨酸激酶抑制活性的衍生物衍生物或其药理学上可接受的盐:其中R 1和R 2相同或不同,各自表示氢,链烷酰基,烯酰基,叔丁基二苯基甲硅烷基或 叔丁基二甲基甲硅烷基; R 3表示Y-R 5 {其中Y表示取代或未取代的亚烷基; 并且R 5表示CONR 6 R 7(其中R 6表示氢,羟基,取代或未取代的低级烷基,取代或未取代的高级烷基等; R 7表示羟基,取代的较低级 烷基等),CO 2 R 12(其中R 12表示取代的低级烷基,取代或未取代的高级烷基等)等}等; X表示卤素或与R 4结合以表示单键; 和R 4与X一起表示单键,或表示氢,烷酰基等。
    • 6. 发明申请
    • Object having a microbicide coating, method for the production thereof and use of the same
    • 具有杀微生物剂涂层的物体,其制造方法及其用途
    • US20040029834A1
    • 2004-02-12
    • US10415396
    • 2003-04-28
    • Thomas SchiestelHermann SchirraHelmut SchmidtDetmar Buxmann
    • A61K031/695A61K009/14
    • C09D183/08C09D4/00C09D5/14C09D183/02C09D183/04C08G77/00C08L2666/52
    • A microbicidally coated article, especially a container, having on at least part of it a coating comprising an organically modified inorganic matrix comprising silver colloids which is obtainable by application of a coating composition comprising a) a hydrolysate or condensate based on at least one hydrolysable silane with at least one non-hydrolysable substituent and b) a silver compound to the surface of the article and treatment with heat and/or radiation to form the silver colloid coating. Articles coated in accordance with the invention are therefore particularly suitable for purposes of disinfection, preservation, cosmetic, pharmaceutical or medical purposes. Articles from the pharmaceutical or medical sector, especially containers for pharmaceuticals or articles or components which come into contact with the human body and are required to be free from germs, are preferred fields of application.
    • 一种杀微生物涂覆的制品,特别是容器,其至少部分具有包含有机改性的无机基质的涂层,其包含银胶体,其可通过施用涂料组合物获得,所述涂料组合物包含:a)基于至少一种可水解硅烷的水解产物或缩合物 与至少一种不可水解的取代基和b)一种银化合物到制品的表面并用热和/或辐射进行处理以形成银胶体涂层。 因此,根据本发明涂覆的制品特别适用于消毒,保存,化妆品,医药或医疗目的。 优选的药物或医疗领域的药物,尤其是与人体接触并被要求不含细菌的药物或制品或成分的容器。
    • 7. 发明申请
    • Novel organosilicon compounds comprising a multifunctional polyorganosiloxane bearing at least one activated imide-type double ethylene bond and method for preparing same
    • 包含具有至少一个活化的酰亚胺型双乙烯键的多官能聚有机硅氧烷的新型有机硅化合物及其制备方法
    • US20040023926A1
    • 2004-02-05
    • US10311545
    • 2003-08-26
    • Nathalie GuennouniJean-Jacques Lebrun
    • A61K031/695A61K007/06A61K007/11
    • C08G77/26C08G77/388
    • The field of the present invention is that of novel organosilicon compounds comprising a multifunctional polyorganosiloxane (abbreviated as POS) comprising, per molecule, and attached to silicon atoms, firstly at least one hydroxyl radical and/or at least one alkoxy radical, and secondly at least one group containing an activated ethylenic double bond consisting of a maleimide group. The present invention also relates to functionalization processes leading to the POSs targeted above, which consist in particular in reacting an organosilane bearing a maleamic acid function and at least two alkoxy functions with a polysilazane. The compounds comprising a multifunctional POS as targeted above are capable of showing advantageous properties, for example of acting as coupling agents (for white filler-elastomer coupling) in rubber compositions based on isoprene elastomer(s) comprising a white filler as reinforcing filler.
    • 本发明的领域是包含每分子包含并连接到硅原子的多官能聚有机硅氧烷(缩写为POS)的新型有机硅化合物,首先至少有一个羟基和/或至少一个烷氧基,其次在 至少一个含有由马来酰亚胺基团组成的活化烯键双键的基团。 本发明还涉及导致上述POS的官能化方法,其特别包括使具有马来酰胺酸官能团和至少两个烷氧基官能团的有机硅烷与聚硅氮烷反应。 包含如上所述的多功能POS的化合物能够显示出有利的性质,例如在基于包含白色填料作为增强填料的异戊二烯弹性体的橡胶组合物中作为偶联剂(用于白色填料 - 弹性体偶联)。
    • 9. 发明申请
    • Tricyclic-bis-enone derivatives and methods of use thereof
    • 三环 - 双烯酮衍生物及其使用方法
    • US20030232786A1
    • 2003-12-18
    • US10345053
    • 2003-01-15
    • Tadashi HondaFrank G. FavaloroGordon W. GribbleMichael B. SpornNanjoo Suh
    • A61K031/695C07D265/30C07D211/06A61K031/537C07D249/08A61K031/497
    • C07C62/38C07C225/12C07C255/47C07C271/18C07C2603/00C07C2603/26C07F7/1804
    • Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.
    • 提供了新的三环双烯衍生物(TBE)以及制备这种TBE的方法。 还提供了用于预防和/或治疗癌症,阿尔茨海默氏病,帕金森病,多发性硬化,肌萎缩性侧索硬化,类风湿性关节炎,炎症性肠病以及其发病机制被认为涉及过量产生一氧化氮的所有其它疾病的方法 NO)或前列腺素或iNOS或COX-2基因或基因产物的过表达。 此外,用于合成本发明的TBE化合物的方法使用便宜的市售试剂,并且是高成本有效的并且适于放大。 还提供了利用新型中间体以及这些中间体的合成的其它高效合成方法。 此外,本发明还提供了设计新型和水溶性TBE的方法。