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1. 发明申请

WO2008119663A1 HETEROCYCLIC ANTIVIRAL COMPOUNDS 审中-公开
标题翻译：杂环抗病毒化合物
公开(公告)号：WO2008119663A1
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053238
申请日：2008-03-18
申请人： F. HOFFMANN-LA ROCHE AG , MELVILLE, Chris Richard , ROTSTEIN, David Mark
发明人： MELVILLE, Chris Richard , ROTSTEIN, David Mark
IPC分类号： C07D498/10 , A61K31/537 , A61P31/18
CPC分类号： C07D498/10
摘要： This invention relates to piperidine derivatives of formula (I) wherein R 1 , R 2 , R 3 and R 4 are as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 receptors is implicated. Disorders that may be treated or prevented by the present derivatives include HIV and genetically related retroviral infections (and the resulting acquired immune deficiency syndrome, AIDS), rheumatoid arthritis, solid organ transplant reject (graft vs. host disease), asthma and COPD.
摘要翻译：本发明涉及式（I）的哌啶衍生物，其中R 1，R 2，R 3和R 4，如本文所定义的，可用于治疗多种疾病，包括涉及CCR5受体调节的疾病。本衍生物可能治疗或预防的疾病包括艾滋病病毒和遗传相关的逆转录病毒感染（以及由此获得的获得性免疫缺陷综合征，AIDS），类风湿关节炎，实体器官移植排斥（移植物抗宿主病），哮喘和COPD。

2. 发明申请

WO2007057119A2 AZGP GENE SINGLE NUCLEOTIDE POLYMORPHISMS (SNPs) 审中-公开
标题翻译： AZGP基因单核苷酸多态性（SNPs）
公开(公告)号：WO2007057119A2
公开(公告)日：2007-05-24
申请号：PCT/EP2006/010726
申请日：2006-11-09
申请人： F. HOFFMANN-LA ROCHE AG , CLERC, Roger, G. , DUCHATEAU-NGUYEN, Guillemette , ESSIOUX, Laurent , LAGARDE, Delphine , OSTENSON, Claes-Goran
发明人： CLERC, Roger, G. , DUCHATEAU-NGUYEN, Guillemette , ESSIOUX, Laurent , LAGARDE, Delphine , OSTENSON, Claes-Goran
CPC分类号： C12Q1/6883 , C12Q2600/156 , C12Q2600/158 , C12Q2600/172
摘要： The present invention provides single nucleotide polymorphisms and haplotypes in the AZGPl gene that can be used for determining the predisposition of an individual to obesity.
摘要翻译：本发明提供了AZGP1基因中的单核苷酸多态性和单倍型，其可用于确定个体对肥胖的倾向。

3. 发明申请

WO2007016975A1 KINASE AND PHOSPHATASE ASSAYS BASED ON FRET 审中-公开
标题翻译：基于FRET的激酶和磷酸酶测定
公开(公告)号：WO2007016975A1
公开(公告)日：2007-02-15
申请号：PCT/EP2005/053720
申请日：2005-07-29
申请人： F. HOFFMANN-LA ROCHE AG , ENDERLE, Thilo , ROTH, Doris
发明人： ENDERLE, Thilo , ROTH, Doris
IPC分类号： C12Q1/48 , C12Q1/44
CPC分类号： C12Q1/485 , C12Q1/42 , G01N33/542
摘要： The present invention relates to a method of determining kinase or phosphatase activity based on a three parts system. The method comprises contacting a binding partner which can bind phosphorylated peptides, a detection molecule and a substrate peptide. Determination of activities is achieved by measuring energy transfer between an energy donor and an energy acceptor that are present on the detection molecule and the substrate molecule.
摘要翻译：本发明涉及一种基于三部分系统确定激酶或磷酸酶活性的方法。该方法包括使可结合磷酸化肽的结合配偶体，检测分子和底物肽接触。通过测量存在于检测分子和底物分子上的能量供体和能量受体之间的能量转移来实现活性的测定。

4. 发明申请

WO2006063733A1 CD99 AS TARGET/MARKER FOR INSULIN RESISTANCE 审中-公开
标题翻译： CD99作为目标/胰岛素抵抗标记
公开(公告)号：WO2006063733A1
公开(公告)日：2006-06-22
申请号：PCT/EP2005/013195
申请日：2005-12-09
申请人： F.HOFFMANN-LA ROCHE AG , BERNDT, Peter , EVERS, Stefan , FOSER, Stefan , FOUNTOULAKIS, Michael , MARTIN, Mitchell, Lee , SEBOKOVA, Elena
发明人： BERNDT, Peter , EVERS, Stefan , FOSER, Stefan , FOUNTOULAKIS, Michael , MARTIN, Mitchell, Lee , SEBOKOVA, Elena
IPC分类号： G01N33/566
CPC分类号： G01N33/566 , G01N2333/70596 , G01N2500/04 , G01N2800/52
摘要： The present invention relates to the monitoring of disease progression and diagnosis of Insulin Resistance in diabetes by measuring levels of CD99 in a liquid sample, and to screening for novel compounds for the prevention and/or treatment of diabetes.
摘要翻译：本发明涉及通过测量液体样品中CD99的水平以及筛选用于预防和/或治疗糖尿病的新化合物来监测糖尿病中胰岛素抵抗的疾病进展和诊断。

5. 发明申请

WO2006056340A2 METHOD FOR DETERMINING GENOTOXICITY 审中-公开
标题翻译：确定致病性的方法
公开(公告)号：WO2006056340A2
公开(公告)日：2006-06-01
申请号：PCT/EP2005/012209
申请日：2005-11-15
申请人： F. HOFFMANN-LA ROCHE AG , ALLARD, John, David , AUD, Dee, Marie , LIAO, Guochun , PELTZ, Gary, Allen
发明人： ALLARD, John, David , AUD, Dee, Marie , LIAO, Guochun , PELTZ, Gary, Allen
IPC分类号： C12Q1/68 , C12N15/63
CPC分类号： C12Q1/6897 , A01K2217/05 , A01K2217/075 , C07K14/705 , C12Q1/6876 , C12Q2600/158 , C12Q2527/137 , C12Q2527/125
摘要： Methods and reagents for determining the genotoxicity of a compound based on genomic responses to contact therewith are provided.
摘要翻译：提供了用于基于与其接触的基因组响应来确定化合物的基因毒性的方法和试剂。

6. 发明申请

WO2006010534A1 DICKKOPF HOMOLOG 3 AS TARGET/MARKER OF BETA CELL FAILURE 审中-公开
标题翻译： DICKKOPF HOMOLOG 3作为目标/ BETA细胞失败的标记
公开(公告)号：WO2006010534A1
公开(公告)日：2006-02-02
申请号：PCT/EP2005/007858
申请日：2005-07-19
申请人： F.HOFFMANN-LA ROCHE AG , CHRIST, Andreas , EVERS, Stefan , KRAPFENBAUER, Kurt , SEBOKOVA, Elena
发明人： CHRIST, Andreas , EVERS, Stefan , KRAPFENBAUER, Kurt , SEBOKOVA, Elena
IPC分类号： G01N33/68
CPC分类号： G01N33/6893 , G01N2333/4715 , G01N2800/042 , G01N2800/52
摘要： The present invention relates to the monitoring of disease progression and diagnosis of beta-cell failure in diabetes by measuring levels of DKK-3 in a liquid sample, and to screening for novel compounds for the prevention and/or treatment of diabetes.
摘要翻译：本发明涉及通过测量液体样品中DKK-3的水平，以及筛选用于预防和/或治疗糖尿病的新化合物来监测糖尿病中的β-细胞衰竭的疾病进展和诊断。

7. 发明申请

WO2005014622A2 RA ANTIGENIC PEPTIDES 审中-公开
标题翻译： RA抗原肽
公开(公告)号：WO2005014622A2
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008609
申请日：2004-07-30
申请人： F. HOFFMANN-LA ROCHE AG , BERNTENIS, Nikolaos , BUURMAN, Gerrit , KROPSHOFER, Harald , MUELLER, Bernd, Christian , SPINDELDREHER, Sebastian, Thomas , VOGT, Anne , ZOLG, Werner
发明人： BERNTENIS, Nikolaos , BUURMAN, Gerrit , KROPSHOFER, Harald , MUELLER, Bernd, Christian , SPINDELDREHER, Sebastian, Thomas , VOGT, Anne , ZOLG, Werner
IPC分类号： C07K1/22
CPC分类号： C07K14/4713 , C07K14/70539
摘要： The present invention provides novel naturally-processed MHC class II antigenic peptides; which originate from interferon-γ-inducible lysosomal thiol reductase, integrin beta-2, phosphatitylinositol-4,5-bisphosphate 3-kinase, urokinase-type plasminogen activator, immunoglobulin heavy chain V-III region (V H 26), DJ-1 protein, apolipoprotein B-100, 26S proteasome non-ATPase regulatory subunit 8, interleukin-1 receptor, fibromodulin, GM-CSF/IL-3/IL-5 receptor, sorting nexin 3, inter-α-trypsin inhibitor heavy chain H4, complement C4, complement C3 (α-chain), complement C3 (β-chain), SH3 domain-binding glutamic acid-rich-like protein 3, interleukin-4-induced protein 1, hemopexin, Hsc70-interacting protein,invariant chain (Ii), retinoic acid receptor responder protein 2, fibronectin, cathepsin B, tripeptidyl-peptidase II, legumain, platelet activating factor receptor, poly- alpha-2.8-sialyltransferase, and ras-leated protein Rab-11B. Also provided are these antigenic peptides and the proteins they are derived from as markers for erosive and/or non-erosive RA. Moreover, these antigenic peptides linked to MHC class II molecules, antibodies reactive with said antigenic peptides, nucleic acids encoding said antigenic peptides, and nucleic acid constructs, host cells and methods for expressing said antigenic peptides are provided. The antigenic peptides of the invention can be used as markers in diagnosis of RA and in therapy as anti-RA vaccines.
摘要翻译：本发明提供了新的天然处理的MHC II类抗原肽; 其来源于干扰素-γ-诱导型溶酶体巯基还原酶，整联蛋白β-2，磷酸性肌醇-4,5-二磷酸3-激酶，尿激酶型纤溶酶原激活物，免疫球蛋白重链V-III区（V H 26），DJ-1蛋白，载脂蛋白B-100,26S蛋白酶体非ATP酶调节亚基8，白介素-1受体，纤调蛋白，GM-CSF / IL-3 / IL-5受体，nexin 3分选，α - 胰蛋白酶抑制剂重链H4，补体C4，补体C3（α-链），补体C3（β-链），SH3结构域结合谷氨酸富集样蛋白3，白细胞介素-4诱导蛋白1，血红素结合蛋白，Hsc70 - 相互作用蛋白，不变链（Ii），视黄酸受体响应蛋白2，纤连蛋白，组织蛋白酶B，三肽基肽酶II，legumain，血小板活化因子受体，聚-α-2.8-唾液酸转移酶和ras化的蛋白Rab-11B 。还提供了这些抗原肽和它们来源于作为侵蚀性和/或非侵蚀性RA的标志物的蛋白质。此外，提供了与MHC II类分子连接的这些抗原肽，与所述抗原肽反应的抗体，编码所述抗原肽的核酸，以及表达所述抗原肽的核酸构建体，宿主细胞和方法。本发明的抗原性肽可以用作RA诊断和作为抗RA疫苗治疗的标记。

8. 发明申请

WO2005000362A1 TRITIATED GROWTH HORMONE SECRETAGOGUE MK-0677 审中-公开
公开(公告)号：WO2005000362A1
公开(公告)日：2005-01-06
申请号：PCT/EP2004/006567
申请日：2004-06-18
申请人： F. HOFFMANN-LA ROCHE AG , HERTEL, Cornelia , HUGUENIN, Philipp , JENSEN ZOFFMANN, Sannah , PLANCHER, Jean-Marc
发明人： HERTEL, Cornelia , HUGUENIN, Philipp , JENSEN ZOFFMANN, Sannah , PLANCHER, Jean-Marc
IPC分类号： A61K51/04
CPC分类号： A61K51/0455
摘要： The present invention relates to a tritiated growth hormone secretagogue which can be used for the identification of compounds capable of binding to growth hormone secretagogue receptors, or of compounds having activity as growth hormone secretagogues.
摘要翻译：本发明涉及可用于鉴定能够结合生长激素促分泌素受体的化合物或具有作为生长激素促分泌素的活性的化合物的氚生长激素促分泌素。

9. 发明申请

WO2004090157A1 THE USE OF PDE4D IN THE SCREENING FOR MEDICAMENTS AGAINST ATHEROSCLEROSIS 审中-公开
标题翻译： PDE4D在抗甲状腺激素治疗药物筛选中的应用
公开(公告)号：WO2004090157A1
公开(公告)日：2004-10-21
申请号：PCT/EP2004/003739
申请日：2004-04-07
申请人： F. HOFFMANN-LA ROCHE AG , EVERS, Stefan , FINGERLE, Juergen , HIMBER, Jacques
发明人： EVERS, Stefan , FINGERLE, Juergen , HIMBER, Jacques
IPC分类号： C12Q1/34
CPC分类号： C07K7/08 , C07K16/40 , C12Q1/44 , G01N33/6893 , G01N2800/323
摘要： The present invention provides the use of PDE4, preferably PDE4D, more preferably PDE4D5 or PDE4D7, as a novel target for the identification of compounds that can be used for the treatment of atherosclerosis, preferably of Peripheral Arterial Occlusive Disease (PAOD), or for the treatment of restenosis.
摘要翻译：本发明提供了PDE4，优选PDE4D，更优选PDE4D5或PDE4D7作为鉴定可用于治疗动脉粥样硬化的化合物（优选为外周动脉闭塞性疾病（PAOD））或用于治疗再狭窄。

10. 发明申请

WO2004048335A2 MANDELIC ACID DERIVATIVES 审中-公开
标题翻译：曼德尔酸衍生物
公开(公告)号：WO2004048335A2
公开(公告)日：2004-06-10
申请号：PCT/EP2003/013087
申请日：2003-11-21
申请人： F. HOFFMANN-LA ROCHE AG
发明人： BANNER, David, William , GOBBI, Luca, Claudio , GROEBKE ZBINDEN, Katrin , OBST, Ulrike , STAHL, Christoph, Martin
IPC分类号： C07D213/00
CPC分类号： C07C257/18 , C07C259/18 , C07D211/46 , C07D213/30 , C07D213/38 , C07D213/56 , C07D213/65 , C07D213/73 , C07D231/12 , C07D233/56 , C07D239/42 , C07D249/08 , C07D265/36 , C07D271/06 , C07D295/15 , C07D309/12 , C07D311/04
摘要： The invention is concerned with novel mandelic acid derivatives of formula (I), wherein R 1 to R 10 , X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型扁桃酸衍生物，其中R 1至R 10，X和Y如上所定义在说明书和权利要求书中，以及其生理上可接受的盐。这些化合物抑制因子VIIa和组织因子诱导的凝血因子Xa，IXa和凝血酶的形成，并可用作药物。

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