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    • 5. 发明申请
    • FREEZE-DRIED COFFEE TABLETS
    • 冷冻干咖啡片
    • WO2004034798A1
    • 2004-04-29
    • PCT/EP2003/011359
    • 2003-10-14
    • NESTEC S.A.KESSLER, Ulrich
    • KESSLER, Ulrich
    • A23F5/38
    • A23F5/385A23F5/32
    • The present invention relates to a coffee tablet which is obtainable by molding and freeze-drying a solution of coffee solids into a desired shape and which has improved dissolution properties and an appealing smooth and/or shiny surface appearance. The coffee tablet also has a closed surface pore structure and an internal pore structure wherein a majority of the pores in the pore structure are interconnected and have a size of between 5 and 50 micrometers. The coffee tablet can also include a coating of a coffee, a flavorant, a colorant or an aroma. The coffee tablet is packaged in an environment of an aroma to form a product that exhibits fresh and strong flavor and aroma characteristics when a beverage is prepared from the tablet even after long term storage of the tablet.
    • 本发明涉及一种咖啡片,其可通过将咖啡固体的溶液成型和冷冻干燥成所需形状并具有改善的溶解性能和吸引光滑的和/或光泽的表面外观而获得。 咖啡片还具有封闭的表面孔结构和内孔结构,其中孔结构中的大部分孔互连并且具有5至50微米的尺寸。 咖啡片还可以包括咖啡,香料,着色剂或香气的涂层。 咖啡片被包装在香气的环境中,以形成当即使在片剂长期储存后也从片剂制备饮料时,其具有新鲜强烈的风味和香味特征的产品。
    • 6. 发明申请
    • SMALL MOLECULE INHIBITORS OF INFLUENZA A AND B VIRUS AND RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    • 小儿甲型和乙型流感病毒与呼吸道合胞病毒复制的小分子抑制剂
    • WO2010128163A3
    • 2010-11-11
    • PCT/EP2010/056304
    • 2010-05-07
    • PIKE PHARMA GMBHKESSLER, UlrichRANADHEERA, CharlèneJOUBERT, MurielGIETHLEN, BrunoGARRIDO, Fabrice
    • KESSLER, UlrichRANADHEERA, CharlèneJOUBERT, MurielGIETHLEN, BrunoGARRIDO, Fabrice
    • C07D333/22C07D409/04C07D417/04C07D417/12C07D417/14G01N33/68
    • Compounds according to the invention are 2-(3-Q 5 -4-Q 4 -5-Q 3 -thien-2-yl)-4-R 3 -5-R 2 -1,3-thiazol, 2-(3-Q 5 -4-Q 4 - 5-Q 3 -fur-2-yl)-4-R 3 -5-R 2 -1,3-thiazol, 2-(3-Q 5 -4-Q 4 -5-Q 3 -thien-2-yl)-5-R 2 -1,3,4-thiadiazol, 2-(3-Q 5 -4-Q 4 -5-Q 3 -fur-2-yl)-5-R 2 -1,3,4-thiadiazol, 2-(2-Q 3 -4-Q 5 -1,3-thiazol-5-yl)4-R 3 -5-R 2 -1,3-thiazol, 2-(2-Q 3 -4-Q 5 -1,3-oxazol-5-yl)4- R 3 -5-R 2 -1,3-thiazol, 2-(4-Q 4 -5-Q 3 -1,3-thiazol-2-yl)4-R 3 -5-R 2 -1,3-thiazol, 2-(4-Q 4 -5-Q 3 -1,3-oxazol-2-yl)4-R 3 -5- R 2 -1,3-thiazol, 2-(4-Q 5 -5-Q 4 -3-Q 2 -thien-3-yl)4-R 3 -5-R 2 -1,3-thiazol, 2-(4-Q 5 -5-Q 4 -3-Q 2 -fur-3-yl)4-R 3 -5-R 2 -1,3-thiazol, 2-benzo[b]thiophen-2-yl4-R 3 -5-R 2 -1,3-thiazol, 2-benzo[b]furan-2-yl4-R 3 -5-R 2 -1,3-thiazol, 2-(3-Q 5 -4- Q 4 -5-Q 3 -thien-2-yl)-6-Z 2 -1,3-benzo[d]thiazol, 2-(3-Q 5 -4-Q 4 -5-Q 3 -thien-2-yl)-6-Z 2 -1,3-benzo[d]oxazol, 2-(2-Z 5 -3- Z 6 -4-Z 7 -phenyl)4-R 3 -5-R 2 -1,3-thiazol, 2-(5-Z 8 -6-Z 7 -3-pyridyl)4-R 3 -5-R 2 -1,3-thiazol, 2-(3-R 3 -4-R 2 -phenyl)-3-Q 5 - 4-Q 4 -5-Q 3 -thiophen, 2-(3-R 3 -4-R 2 -phenyl)-3-Q 5 -4-Q 4 -5-Q 3 -furan, N-Z 9 -N-(4-R 3 -5-R 2 -1,3-thiazol-2-yl)-3-Q 5 -4-Q 4 - 5-Q 3 -thien-2-yl-carboxamid, N-Z 9 -N-(4-R 3 -5-R 2 -1,3-thiazol-2-yl)-3-Q 5 -4-Q 4 -5-Q 3 -fur-2-yl-carboxamid, 5-(3-Q 5 -4- Q 4 -5-Q 3 -thien-2-yl)4-R 4 -2-R 2 -1,3-thiazol, 5-(3-Q 5 -4-Q 4 -5-Q 3 -fur-2-yl)4-R 4 -2-R 2 -1,3-thiazol, 2-(3-Q 5 -4-Q 4 -5-Q 3 - thien-2-yl)-3-R 4 -4-R 3 -5-R 2 -thiophen, 2-(3-Q 5 -4-Q 4 -5-Q 3 -fur-2-yl)-3-R 4 -4-R 3 -5-R 2 -thiophen; wherein R 2 , R 3, R 4 , Q 2 , Q 3 , Q 4 , Q 5 , Z 2 , Z 5 , Z 6 , Z 7 , Z 8 and Z 9 are as defined in the description. Said compounds are particularly advantageous for treating and/or preventing influenza type A and/or influenza type B infections in humans, mammals and/or birds, and for treating and/or preventing respiratory syncytial virus infections in humans, mammals and/or birds.
    • 根据本发明的化合物是2-(3-Q 5 -4-Q 4 -5 -Q 3) -2-噻吩-2-基)-4-R 3 -5-R 2 -1,3-噻唑,2-(3-Q 5) -4-Q 4 -5-Q 3 - 呋喃-2-基)-4-R 3 -5- R 2 -1,3-噻唑,2-(3-Q 5 -4-Q 4 -5 -Q 3) - 噻吩-2-基)-5-R 2 -1,3,4-噻二唑,2-(3-Q 5 -4-Q -5-Q 3 -fur-2-yl)-5-R 2 -1,3,4-噻二唑,2- (2-Q 3 -4-Q 5 -1,3-噻唑-5-基)-4-R 3 -5-R 2-(2-Q 3 -4-Q 5 -1,3-恶唑-5-基)-1,3-噻唑,2-(2-Q 3 -4 -Q 5 -1,3-恶唑-5-基) (4-Q 4 -Q-4-Q-4)-5-R 2 -1,3-噻唑,2-(4-Q 4 -5 -Q -1,3-噻唑-2-基)-4-R 3 -5-R 2 -1,3-噻唑,2 - (4-Q 4 -5-Q 3 -1,3-恶唑-2-基)-4-R 3 -5- R 2 -1,3-噻唑,2-(4-Q 5 -5 -Q 4 -3-Q 2) - 噻吩-3-基)4-R 3 -5-R 2 -1,3-噻唑,2-(4-Q- 5 -5-Q 4 -3-Q 2-呋喃-3-基)-4-R 3 -5-R 2 -1,3-噻唑,2-苯并[b]噻吩-3-基, 2-苯并呋喃-2-基] -4-呋喃-2-基] -4,5-二氢吡啶并[2,3-b]呋喃-2-基] -5-R 2 -1,3-噻唑,2-(3-Q 5 -4 -Q 4 -5) -β-噻吩-2-基)-6-Z 2 -1,3-苯并[d]噻唑,2-(3-Q 5) 功能 -4-Q 4 -5-Q 3 噻吩-2-基)-6-Z 2 -1, 3-苯并[d]恶唑,2-(2-Z5-Z-4-Z7-苯基)4 -R 5 -5-R 2 -1,3-噻唑,2-(5-Z 8 -6 -Z) 3-(3-吡啶基)-4-R 3 -5-R 2 -1,3-噻唑,2-(3-R 3) -4-R 2 - 苯基)-3-Q 5 -4-Q 4 -Q-5-Q- 2-(3-R 3 -4-R 2 - 苯基)-3-Q 5 - 4-Q 4 -5-Q 3 - 呋喃,NZ 9-N-(4-R 3) -5-R 2 -1,3-噻唑-2-基)-3-Q 5 -4-Q 4-5 - N 3 - 噻吩-2-基 - 甲酰胺,NZ 9-N-(4-R 3 -5-R 2) 功能 -1,3-噻唑-2-基)-3- -5-Q-4-Q-5-Q 3 - 呋喃-2-基 - 甲酰胺,5-(3-Q- -5-Q-4-Q-5-Q 3 -thien-2-yl)4-R 4 -s- 2-R 2 -1,3-噻唑,5-(3-Q 5 -4 -Q 4 -5 -Q) 呋喃-2-基)4-R 4 -2-R 2 -1,3-噻唑,2-(3-Q- -5-Q 3 - 噻吩-2-基)-3-R 4 - -4-R 3 -5-R 2 - 噻吩,2-(3-Q 5 -4 -Q 4) / SUP> -5-Q 3 -fur -2-基)-3-R 4 -4-R 3 -5-R 2 - 噻吩; 其中R 2,R 3,R 4,Q 2,Q 3,R 4,R 4, Q 4,Q 5,Z 2,Z 5,Z 6,Z 5,Z 5,Z 5,Z 5,Z 5, ,Z 7,Z 8和Z 9如说明书中所定义。 所述化合物对于治疗和/或预防人类,哺乳动物和/或鸟类中的A型和/或B型流感感染以及治疗和/或预防人类,哺乳动物和/或鸟类中的呼吸道合胞体病毒感染是特别有利的。
    • 7. 发明申请
    • 2,1,3-BENZOXADIAZOL DERIVATIVES FOR THE INHIBITION OF INFLUENZA A AND B VIRUS AND RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    • 用于抑制流感病毒A和B病毒和呼吸道同种病毒复制的2,1,3-苯并恶唑衍生物
    • WO2010128156A1
    • 2010-11-11
    • PCT/EP2010/056294
    • 2010-05-07
    • PIKE PHARMA GMBHKESSLER, UlrichRANADHEERA, Charlene
    • KESSLER, UlrichRANADHEERA, Charlene
    • C07D271/12C07D417/04A61K31/4245A61K31/427A61K31/7076C07H19/167A61P31/16
    • C07D271/12A61K31/4245A61K31/427A61K31/7076C07D417/04C07H19/167
    • A 2,1,3-benzoxadiazole compound as a medicament according to the invention is one of the following compounds: 4-[(4-methoxybenzyl)thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4- yl)thio]ethyl 4-methoxybenzene-1-sulfonate, 4-[(4-methylphenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(2,4-dichlorophenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)thio]ethan-1-ol, 4-[(4-methylbenzyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(4-fluorophenyl)thio]-7-nitro-2,1,3- benzoxadiazole, 4-[(3-chlorophenyl)-thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4- yl)thio]ethyl-4-methoxy-benzoate, 5-[4-(tert-butyl)-1,3-thiazol-2-yl]-2,1,3-benzoxadiazole, N-benzyl-4-nitro-2,1,3-benzoxadiazol-5-amine, 4-nitro-7-(phenylmethylsulfanyl)-2,1,3-benzoxadiazole, 4-nitro-7-(phenylmethylsulfonyl)-2,1,3-benzoxadiazole, 2-(hydroxymethyl)-5-[6-[(4-nitro-2,1,3-benzoxadiazol-7-yl)sulfanyl]purin-9-yl]oxolane-3,4-diole, or 2-[2-amino-6-[(4-nitro-2,1,3-benzoxadiazol-7-yl)sulfanyl]purin-9-yl]-5-(hydroxymethyl) oxolane-3,4-diol; or a physiologically tolerable salt, solvate, or physiologically functional derivative thereof. Said compounds are particularly advantageous for treating and/or preventing influenza type A and/or influenza type B infections in humans, mammals and/or birds, and for treating and/or preventing respiratory syncytial virus infections in humans, mammals and/or birds.
    • 根据本发明的药物的2,1,3-苯并二唑化合物是以下化合物之一:4 - [(4-甲氧基苄基)硫] -7-硝基-2,1,3-苯并恶二唑,2 - [( 4-硝基-2,1,3-苯并恶二唑-4-基)硫基]乙基4-甲氧基苯-1-磺酸酯,4 - [(4-甲基苯基)硫基] -7-硝基-2,1,3-苯并恶二唑, 4 - [(2,4-二氯苯基)硫基] -7-硝基-2,1,3-苯并恶二唑,2 - [(7-硝基-2,1,3-苯并恶唑-4-基)硫]乙-1- - [(4-甲基苄基)硫基] -7-硝基-2,1,3-苯并恶二唑,4 - [(4-氟苯基)硫代] -7-硝基-2,1,3-苯并二恶唑,4 - [(3-氯苯基) - 硫] -7-硝基-2,1,3-苯并恶二唑,2 - [(7-硝基-2,1,3-苯并恶唑-4-基)硫代]乙基-4-甲氧基 - 苯甲酸酯,5- [4-(叔丁基)-1,3-噻唑-2-基] -2,1,3-苯并恶二唑,N-苄基-4-硝基-2,1,3-苯并恶二唑-5 (苯基甲基硫烷基)-2,1,3-苯并恶二唑,4-硝基-7-(苯甲基磺酰基)-2,1,3-苯并恶二唑,2-(羟甲基)-5- [6- [(4-硝基-2,1,3-苯并恶二唑-7-基)硫烷基]嘌呤-9-基]氧杂环戊烷-3,4-二烯或2- [2-氨基-6 - [(4-硝基 - 2,1,3-benzoxad 噻唑-7-基)硫烷基]嘌呤-9-基] -5-(羟甲基)氧杂环戊烷-3,4-二醇; 或其生理上可耐受的盐,溶剂化物或生理功能衍生物。 所述化合物在人,哺乳动物和/或鸟类中治疗和/或预防A型流感和/或B型流感以及用于治疗和/或预防人,哺乳动物和/或鸟类中的呼吸道合胞病毒感染特别有利。
    • 8. 发明申请
    • INFLUENZA A AND B VIRUS REPLICATION-INHIBITING PEPTIDES
    • 流感病毒A和B病毒复制抑制肽
    • WO2010127712A1
    • 2010-11-11
    • PCT/EP2009/055632
    • 2009-05-08
    • PIKE PHARMA GMBHKESSLER, UlrichMAYER, DanielWUNDERLICH, KerstinRANADHEERA, CharleneSCHWEMMLE, Martin
    • KESSLER, UlrichMAYER, DanielWUNDERLICH, KerstinRANADHEERA, CharleneSCHWEMMLE, Martin
    • C07K14/11A61K38/04
    • C07K14/005A61K38/00C12N2760/16122C12N2760/16222
    • A synthesized or isolated influenza virus replication-inhibiting peptide that competitively inhibits protein-protein interaction of the PA and PB1 of both influenza Virus Types A and B and novel in vitro binding screen to identify peptides with antiviral activity against influenza viruses of both type A and B is disclosed. In addition to the well-known pandemic influenza A viruses (such as the 1918 "Spanish" flu or H5N1), both type A and B viruses contribute greatly to the annual recurring epidemics that cause the vast majority of human cases and medical cost. Surprisingly, it was found that the novel virus replication-inhibiting, are able to inhibit protein-protein interaction of the PA and PB1 subunits of the heterotrimeric viral RNA polymerase complex of both influenza virus types A and B. The viral polymerase sub- unit interaction domain turned out as an effective target for the new antivirals, as correct assembly of the three viral polymerase subunits PB1, PB2 and PA is required for viral RNA synthesis and infectivity.
    • 合成或分离的流感病毒复制抑制肽,其竞争性地抑制A型和B型流感病毒的PA和PB1的蛋白质 - 蛋白质相互作用以及新颖的体外结合筛选,以鉴定具有针对A型和A型流感病毒的抗病毒活性的肽 B被公开。 除了着名的大流行性甲型流感病毒(例如1918年“西班牙”流感或H5N1)外,A型和B型病毒对导致绝大多数人类病例和医疗费用的年度流行病学事件有很大贡献。 令人惊讶的是,发现新型病毒复制抑制能够抑制A型和B型流感病毒的异源三聚病毒RNA聚合酶复合物的PA和PB1亚基的蛋白质 - 蛋白质相互作用。病毒聚合酶亚单元相互作用 结构域是新型抗病毒药物的有效靶标,因为病毒RNA合成和感染性需要三种病毒聚合酶亚基PB1,PB2和PA的正确组装。