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1. 发明申请

WO2010128163A3 SMALL MOLECULE INHIBITORS OF INFLUENZA A AND B VIRUS AND RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开
标题翻译：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
公开(公告)号：WO2010128163A3
公开(公告)日：2010-11-11
申请号：PCT/EP2010/056304
申请日：2010-05-07
申请人： PIKE PHARMA GMBH , KESSLER, Ulrich , RANADHEERA, Charlène , JOUBERT, Muriel , GIETHLEN, Bruno , GARRIDO, Fabrice
发明人： KESSLER, Ulrich , RANADHEERA, Charlène , JOUBERT, Muriel , GIETHLEN, Bruno , GARRIDO, Fabrice
IPC分类号： C07D333/22 , C07D409/04 , C07D417/04 , C07D417/12 , C07D417/14 , G01N33/68
摘要： 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.
摘要翻译：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。}}}}}}}}}}}}}}}}

2. 发明申请

WO2010127712A1 INFLUENZA A AND B VIRUS REPLICATION-INHIBITING PEPTIDES 审中-公开
标题翻译：流感病毒A和B病毒复制抑制肽
公开(公告)号：WO2010127712A1
公开(公告)日：2010-11-11
申请号：PCT/EP2009/055632
申请日：2009-05-08
申请人： PIKE PHARMA GMBH , KESSLER, Ulrich , MAYER, Daniel , WUNDERLICH, Kerstin , RANADHEERA, Charlene , SCHWEMMLE, Martin
发明人： KESSLER, Ulrich , MAYER, Daniel , WUNDERLICH, Kerstin , RANADHEERA, Charlene , SCHWEMMLE, Martin
IPC分类号： C07K14/11 , A61K38/04
CPC分类号： C07K14/005 , A61K38/00 , C12N2760/16122 , C12N2760/16222
摘要： 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.
摘要翻译：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。

3. 发明申请

WO2010128156A1 2,1,3-BENZOXADIAZOL DERIVATIVES FOR THE INHIBITION OF INFLUENZA A AND B VIRUS AND RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开
标题翻译：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
公开(公告)号：WO2010128156A1
公开(公告)日：2010-11-11
申请号：PCT/EP2010/056294
申请日：2010-05-07
申请人： PIKE PHARMA GMBH , KESSLER, Ulrich , RANADHEERA, Charlene
发明人： KESSLER, Ulrich , RANADHEERA, Charlene
IPC分类号： C07D271/12 , C07D417/04 , A61K31/4245 , A61K31/427 , A61K31/7076 , C07H19/167 , A61P31/16
CPC分类号： C07D271/12 , A61K31/4245 , A61K31/427 , A61K31/7076 , C07D417/04 , C07H19/167
摘要： 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.
摘要翻译：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。

4. 发明申请

WO2009080596A3 INSTANT BEVERAGE PRODUCT 审中-公开
公开(公告)号：WO2009080596A3
公开(公告)日：2009-07-02
申请号：PCT/EP2008/067575
申请日：2008-12-16
申请人： NESTEC S.A. , BOEHM, Robert Thomas , DONHOWE, Daniel Paul , MATHIAS, Patricia Ann , FU, Xiaoping , RECHTIENE, Joseph Bernard , KESSLER, Ulrich , SUDHARSAN, Mathalai Balan
发明人： BOEHM, Robert Thomas , DONHOWE, Daniel Paul , MATHIAS, Patricia Ann , FU, Xiaoping , RECHTIENE, Joseph Bernard , KESSLER, Ulrich , SUDHARSAN, Mathalai Balan
IPC分类号： A23F5/32 , A23F5/38 , A23L2/14 , A23L2/395 , A23C9/16 , A23P1/06
摘要： The present invention relates to a method for the production of instant beverage granules which, upon reconstitution with water, form a foamy upper surface. The method makes use of a porous base powder to which the present invention also relates.

5. 发明申请

WO2010112359A1 INSTANT BEVERAGE PRODUCT 审中-公开
标题翻译：即时饮料产品
公开(公告)号：WO2010112359A1
公开(公告)日：2010-10-07
申请号：PCT/EP2010/053675
申请日：2010-03-22
申请人： NESTEC S.A. , BRIEND, Anne Françoise Violette , SUDHARSAN, Mathalai Balan , KESSLER, Ulrich , LACH, Laurent Josef Henry , MEUNIER, Vincent Daniel Maurice , CHANVRIER, Hélène Michèle Jeanne , CARTIER, Jérémie , KOCH, Dietrich , SUTTER, Guido , DUFFEY, Jean-Louis
发明人： BRIEND, Anne Françoise Violette , SUDHARSAN, Mathalai Balan , KESSLER, Ulrich , LACH, Laurent Josef Henry , MEUNIER, Vincent Daniel Maurice , CHANVRIER, Hélène Michèle Jeanne , CARTIER, Jérémie , KOCH, Dietrich , SUTTER, Guido , DUFFEY, Jean-Louis
IPC分类号： A23F5/32 , A23F5/36 , A23F5/38 , A23L2/395 , A23P1/06
CPC分类号： A23F5/38 , A23F5/40 , A23L2/395 , A23P10/40
摘要： The present invention relates to a method for producing an instant beverage product with good foaming and/or dissolution properties, wherein a layer of porous base powder is sintered while gas is forced through the layer.
摘要翻译：本发明涉及一种具有良好的起泡和/或溶解性质的速溶饮料产品的制造方法，其中在将气体强制通过该层时，多孔基础粉末层被烧结。

6. 发明申请

WO2009059938A1 INSTANT BEVERAGE PRODUCT 审中-公开
标题翻译：即时饮料产品
公开(公告)号：WO2009059938A1
公开(公告)日：2009-05-14
申请号：PCT/EP2008/064834
申请日：2008-10-31
申请人： NESTEC S.A. , BOEHM, Robert Thomas , DONHOWE, Daniel Paul , MATHIAS, Patricia Ann , FU, Xiaoping , RECHTIENE, Joseph Bernard , KESSLER, Ulrich , SUDHARSAN, Mathalai Balan , CHANVRIER, Hélène Michèle Jeanne , BRIEND, Anne Françoise Violette , SCHENKER, Stefan
发明人： BOEHM, Robert Thomas , DONHOWE, Daniel Paul , MATHIAS, Patricia Ann , FU, Xiaoping , RECHTIENE, Joseph Bernard , KESSLER, Ulrich , SUDHARSAN, Mathalai Balan , CHANVRIER, Hélène Michèle Jeanne , BRIEND, Anne Françoise Violette , SCHENKER, Stefan
IPC分类号： A23F5/38
CPC分类号： A23F5/38
摘要： The present invention relates to an instant beverage powder and, more particularly, to an instant soluble beverage powder which forms foam on its upper surface when reconstituted with water. The powder has a foaming porosity of at least 35% an open pore volume of less than 3 ml/g and a closed pore average diameter D50 of less than 80 micrometres.
摘要翻译：本发明涉及速溶饮料粉末，更具体地说，涉及当用水重构时在其上表面上形成泡沫的即时可溶性饮料粉末。粉末具有至少35％的开孔孔隙率，小孔体积小于3ml / g，闭孔平均直径D50小于80微米。

7. 发明申请

WO2009040249A1 INSTANT DRINK POWDER 审中-公开
标题翻译：即食饮料粉
公开(公告)号：WO2009040249A1
公开(公告)日：2009-04-02
申请号：PCT/EP2008/061971
申请日：2008-09-10
申请人： NESTEC S.A. , KESSLER, Ulrich , DUFFEY, Jean-Louis , DREYER, Marc, Georges , KAUTER, Michael, Desmond , SUDHARSAN, Mathalai, Balan , CHANVRIER, Hélène, Michèle, Jeanne , WEHRSPANN, Olaf , FU, Xiaoping
发明人： KESSLER, Ulrich , DUFFEY, Jean-Louis , DREYER, Marc, Georges , KAUTER, Michael, Desmond , SUDHARSAN, Mathalai, Balan , CHANVRIER, Hélène, Michèle, Jeanne , WEHRSPANN, Olaf , FU, Xiaoping
IPC分类号： A23F5/36 , A23F5/34
CPC分类号： A23F5/36 , A23F5/34
摘要： The present invention relates to an instant drink powder, preferably an instant coffee powder, which upon reconstitution provides improved foaming. The powder comprises particles having a porosity of at least 55%. The present invention also relates to the use of such a powder, as well as to the method of manufacturing said powder.
摘要翻译：本发明涉及速溶饮料粉末，优选速溶咖啡粉末，其在重构时提供改进的发泡。粉末包含孔隙率至少为55％的颗粒。本发明还涉及这种粉末的使用以及制造所述粉末的方法。

8. 发明申请

WO2004034798A1 FREEZE-DRIED COFFEE TABLETS 审中-公开
标题翻译：冷冻干咖啡片
公开(公告)号：WO2004034798A1
公开(公告)日：2004-04-29
申请号：PCT/EP2003/011359
申请日：2003-10-14
申请人： NESTEC S.A. , KESSLER, Ulrich
发明人： KESSLER, Ulrich
IPC分类号： A23F5/38
CPC分类号： A23F5/385 , A23F5/32
摘要： 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.
摘要翻译：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。

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