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11. 发明申请

WO0040547B1 alpha -SUBSTITUTION OF UNPROTECTED beta -AMINO ESTER COMPOUNDS 审中-公开
标题翻译： α - 未受保护的β-亚胺酯化合物的制备
公开(公告)号：WO0040547B1
公开(公告)日：2000-10-19
申请号：PCT/US9930366
申请日：1999-12-17
申请人： AVENTIS PHARM PROD INC , CHANDRAMOULI SITHAMALLI V , BRIEN MICHAEL K O , POWNER TORY H
发明人： CHANDRAMOULI SITHAMALLI V , O'BRIEN MICHAEL K , POWNER TORY H
IPC分类号： C07C227/16 , C07B53/00 , C07B61/00 , C07C227/32 , C07C229/00 , C07C229/30 , C07C253/00 , C07C253/30 , C07C255/57 , C07C255/58 , C07C261/00
CPC分类号： C07C253/00 , C07B2200/07 , C07C227/32 , C07C229/30 , C07C255/57
摘要： Methods for stereoselective substitution in which a (mono or un)- alpha -substituted unprotected beta -amino ester compound or salt thereof is reacted with an aliphatic electrophile in the presence of a base selected from alkyl lithium compounds, lithium hybride, lithium amide, lithium dialkyl amides and alkali hexamethyldisilylamines.
摘要翻译：在选自烷基锂化合物，锂混合物，氨基化锂，锂的碱的存在下，使单（或单）-α-取代的未保护的β-氨基酯化合物或其盐与脂族亲电子试剂反应的立体选择性取代方法二烷基酰胺和碱性六甲基二甲硅烷基胺。

12. 发明申请

WO0013651A3 LUCIFERASE REPORTER BIOASSAY OF PARATHYROID HORMONE COMPOUNDS 审中-公开
标题翻译：杀虫剂报告器生物多样性的杀虫剂化合物
公开(公告)号：WO0013651A3
公开(公告)日：2000-09-08
申请号：PCT/US9919952
申请日：1999-08-31
申请人： AVENTIS PHARM PROD INC , LABAUDINIERE RICHARD F , MORSE CLARENCE C , YU KIN T , CRUMLEY GREGG R
发明人： LABAUDINIERE RICHARD F , MORSE CLARENCE C , YU KIN T , CRUMLEY GREGG R
IPC分类号： G01N33/50 , C12N5/10 , C12N15/09 , C12Q1/66 , C12Q1/68 , G01N33/15 , G01N33/566 , G01N33/68 , G01N33/74 , C12N5/06
CPC分类号： C12Q1/6897
摘要： This invention is directed to a bioassay for determining the functionality of parathyroid hormone compounds. More particularly, this invention is directed to a bioassay wherein the compound to be tested is added to a culture of parathyroid hormone receptor expressing cells bearing a reporter gene under the transcriptional control of multiple c-AMP responsive elements.
摘要翻译：本发明涉及用于测定甲状旁腺激素化合物的功能的生物测定法。更具体地，本发明涉及一种生物测定法，其中将待测化合物加入至多个c-AMP响应元件的转录控制下的带有报告基因的甲状旁腺激素受体表达细胞的培养物中。

13. 发明申请

WO0066737A9 VARIANTS OF TRAF2 WHICH ACT AS AN INHIBITOR OF TNF-ALPHA (TNF alpha ) SIGNALING PATHWAY 审中-公开
标题翻译：作为TNF-ALPHA（TNFα）信号途径抑制剂的TRAF2的变体
公开(公告)号：WO0066737A9
公开(公告)日：2002-08-29
申请号：PCT/US0009178
申请日：2000-04-06
申请人： AVENTIS PHARM PROD INC , SEARFOSS GEORGE H III , PAGNONI MARCO F , IVASHCHENKO YURI D , GUO KUN , CLARK KENNETH L
发明人： SEARFOSS GEORGE H III , PAGNONI MARCO F , IVASHCHENKO YURI D , GUO KUN , CLARK KENNETH L
IPC分类号： C12N15/09 , A61K38/00 , A61K45/00 , A61K48/00 , A61P1/00 , A61P3/10 , A61P9/00 , A61P9/08 , A61P9/10 , A61P17/02 , A61P19/02 , A61P25/28 , A61P29/00 , A61P37/02 , A61P43/00 , C07K14/47 , C07K14/715 , C12N15/12 , C12P21/02 , A61K38/16 , A61K38/17 , C07K14/435 , C12N15/63 , C12N15/64
CPC分类号： C07K14/7151 , A61K38/00 , A61K48/00 , A61K2039/53
摘要： The present invention relates to variants of TRAF2 which demonstrate the ability to inhibit the TNF alpha signaling pathway. In particular, applicants have isolated a splice variant of TRAF2 referred to hereinafter as "TRAF2 truncated" or "TRAF2TR" and a TRAF2 expression construct with enhanced dominant negative properties, hereafter referred to as "TRAF2 truncated-deleted" or "TRAF2TD". Both TRAF2TR and TRAF2TD have the ability to inhibit the TNF alpha signaling pathway and in TRAF2TD, this ability is greatly enhanced, greatly reducing the response to TNF alpha binding.
摘要翻译：本发明涉及TRAF2的变体，其表现出抑制TNFα信号通路的能力。特别地，申请人已经分离了以下称为“TRAF2截短”或“TRAF2TR”的TRAF2和具有增强的显性阴性的TRAF2表达构建体（以下称为“TRAF2截短缺失”或“TRAF2TD”）的剪接变体。 TRAF2TR和TRAF2TD均具有抑制TNFα信号通路的能力，并且在TRAF2TD中，这种能力大大增强，大大降低了对TNFα结合的反应。

14. 发明申请

WO0057837A9 COMPOSITIONS AND METHODS FOR EFFECTING THE LEVELS OF CHOLESTEROL 审中-公开
标题翻译：用于影响胆固醇水平的组合物和方法
公开(公告)号：WO0057837A9
公开(公告)日：2001-10-18
申请号：PCT/US0007870
申请日：2000-03-24
申请人： AVENTIS PHARM PROD INC , UNIV PENNSYLVANIA , JAYE MICHAEL , LYNCH KEVIN J , AMIN DILIP V , DOAN KIM ANH THI , MARCHADIER DAWN , MAUGEAIS CYRILLE , RADER DANIEL J , KRAWIEC JOHN A , SOUTH VICTORIA J
发明人： JAYE MICHAEL , LYNCH KEVIN J , AMIN DILIP V , DOAN KIM-ANH THI , MARCHADIER DAWN , MAUGEAIS CYRILLE , RADER DANIEL J , KRAWIEC JOHN A , SOUTH VICTORIA J
IPC分类号： G01N33/50 , A61K31/7088 , A61K35/76 , A61K38/00 , A61K38/55 , A61K39/395 , A61K45/00 , A61K48/00 , A61P3/06 , A61P43/00 , C07K16/40 , C12N9/20 , C12N15/09 , G01N33/15 , G01N33/53 , G01N33/566 , C07H21/04 , A01N63/00 , C07H21/02 , C12N15/63 , C12Q1/00
CPC分类号： C07K16/40 , A61K38/00 , A61K48/00 , C12N9/20
摘要： Compositions and methods for raising the level of HDL cholesterol and apolipoprotein AI in a patient and for lowering the levels of VLDL cholesterol and LDL cholesterol in a patient, including compositions and methods which effect the expression of a gene, LIPG, which encodes a lipase enzyme that is a member of the tryacylglycerol lipase family or which effect the enzymatic activity of the enzyme.
摘要翻译：用于提高患者中HDL胆固醇和载脂蛋白AI水平并降低患者中VLDL胆固醇和LDL胆固醇水平的组合物和方法，包括影响基因表达的组合物和方法，LIPG编码脂肪酶其是脂肪酰甘油脂肪酶家族的成员或其影响酶的酶活性。

15. 发明申请

WO0174900A2 NUCLEAR FACTOR KB INDUCING FACTOR 审中-公开
标题翻译：核因子KB诱导因子
公开(公告)号：WO0174900A2
公开(公告)日：2001-10-11
申请号：PCT/US0110719
申请日：2001-04-02
申请人： AVENTIS PHARM PROD INC , KAPLOW JUNE , HAWS THOMAS , ROSIER MARIE , DENEFLE PATRICE
发明人： KAPLOW JUNE , HAWS THOMAS , ROSIER MARIE , DENEFLE PATRICE
IPC分类号： C12N15/09 , A61K31/7088 , A61K35/76 , A61K38/00 , A61K39/395 , A61K45/00 , A61K48/00 , A61P9/10 , A61P29/00 , A61P37/02 , A61P43/00 , C07K14/47 , C12Q1/68 , C07K14/475
CPC分类号： C07K14/4705 , A61K38/00 , A61K48/00
摘要： The present invention is directed to nuclear factor kB (NFkB)-inducing factor polypeptides (NFIF polypeptides) which are capable of inducing NKkB. The present invention includes within its scope NFIF polypeptides, including NFIF-14b and NFIF-7a, DNA, including cDNA, encoding these polypeptides, and expression vectors capable of expressing NFIF polypeptides. Also included are methods and compositions for increasing NFkB induction in a patient, methods and compositions for lowering NFkB induction in a patient, methods for inhibiting inflammation, and methods for manufacture of a medicament intended for the treament and/or prevention of an NFkB-regulated inflammatory response. In addition, methods for determining whether a test compound inhibits or enhances the activity of NFIF polypeptides are provided.
摘要翻译：本发明涉及能够诱导NKkB的核因子kB（NFkB）诱导因子多肽（NFIF多肽）。本发明在其范围内包括NFIF多肽，包括NFIF-14b和NFIF-7a，包括编码这些多肽的cDNA，以及能够表达NFIF多肽的表达载体。还包括用于增加患者中NFkB诱导的方法和组合物，用于降低患者中NFkB诱导的方法和组合物，用于抑制炎症的方法和用于制备用于治疗和/或预防NFkB调节的药物的方法炎症反应。此外，提供了用于确定测试化合物是否抑制或增强NFIF多肽的活性的方法。

16. 发明申请

WO0077190A3 INDUCTION OF VASCULAR ENDOTHELIAL GROWTH FACTOR (VEGF) BY THE SERINE/THREONINE PROTEIN KINASE AKT 审中-公开
标题翻译：丝氨酸/蛋白激酶激酶诱导血管内皮生长因子（VEGF）
公开(公告)号：WO0077190A3
公开(公告)日：2001-04-12
申请号：PCT/US0015098
申请日：2000-06-01
申请人： AVENTIS PHARM PROD INC , GUO KUN , IVASHCHENKO YURI , CLARK KENNETH
发明人： GUO KUN , IVASHCHENKO YURI , CLARK KENNETH
IPC分类号： C12N15/09 , A61K31/7088 , A61K33/24 , A61K35/76 , A61K38/00 , A61K38/04 , A61K38/22 , A61K38/45 , A61K38/46 , A61K39/395 , A61K45/06 , A61K48/00 , A61P9/10 , C12N9/12 , A61K35/00
CPC分类号： C12Y207/01037 , A61K38/45 , A61K48/00 , A61K2039/505 , C12N9/1205 , A61K2300/00
摘要： The present invention relates to methods and compositions for therapeutic angiogenesis. More especially, this invention is directed to induction of vascular endothelial growth factor (VEGF) expression by the serine/threonine protein kinase AKT. Preferably, the compositions and methods according to the invention comprise a nucleic acid encoding AKT, and administration thereof.
摘要翻译：本发明涉及用于治疗性血管生成的方法和组合物。更特别地，本发明涉及通过丝氨酸/苏氨酸蛋白激酶AKT诱导血管内皮生长因子（VEGF）表达。优选地，根据本发明的组合物和方法包含编码AKT的核酸和其施用。

17. 发明申请

WO0040584A3 PROCESS FOR PREPARING N6-SUBSTITUTED DEAZA-ADENOSINE DERIVATIVES 审中-公开
标题翻译：制备N6-取代的哒嗪 - 腺苷衍生物的方法
公开(公告)号：WO0040584A3
公开(公告)日：2000-11-02
申请号：PCT/US9929841
申请日：1999-12-15
申请人： AVENTIS PHARM PROD INC , SLEDESKI ADAM W , GRONDARD LUC , POWERS MATTHEW R , POWNER TORY H , BRIEN MICHAEL K O , TSUEI CHING T , LEON PATRICK , KUBIAK GREGORY G , PAILLERES HUBERT LAURENCE , VIGUIER BENOIT
发明人： SLEDESKI ADAM W , GRONDARD LUC , POWERS MATTHEW R , POWNER TORY H , O'BRIEN MICHAEL K , TSUEI CHING T , LEON PATRICK , KUBIAK GREGORY G , PAILLERES-HUBERT LAURENCE , VIGUIER BENOIT
IPC分类号： A61K31/437 , A61P3/06 , A61P9/10 , A61P9/12 , C07D409/12 , C07D409/14 , C07D471/04 , C07H19/23
CPC分类号： C07D409/12 , C07D471/04
摘要： This invention is directed to a process for preparing N6-substituted adenosine derivatives, to intermediates useful therefor and to methods of preparing these intermediates.
摘要翻译：本发明涉及一种制备N6-取代的腺苷衍生物的方法，涉及对其有用的中间体以及制备这些中间体的方法。

18. 发明申请

WO0057837A2 COMPOSITIONS AND METHODS FOR EFFECTING THE LEVELS OF HIGH DENSITY LIPOPROTEIN (HDL) CHOLESTEROL AND APOLIPOPROTEIN AI, VERY LOW DENSITY LIPOPROTEIN (VLDL) CHOLESTEROL AND LOW DENSITY LIPOPROTEIN (LDL) CHOLESTEROL 审中-公开
标题翻译：用于影响高密度脂蛋白（HDL）胆固醇和阿扑普坦AI水平的组合物和方法，非常低密度脂蛋白（VLDL）胆固醇和低密度脂蛋白（LDL）胆固醇
公开(公告)号：WO0057837A2
公开(公告)日：2000-10-05
申请号：PCT/US0007870
申请日：2000-03-24
申请人： AVENTIS PHARM PROD INC , UNIV PENNSYLVANIA , JAYE MICHAEL , LYNCH KEVIN J , AMIN DILIP V , DOAN KIM ANH THI , MARCHADIER DAWN , MAUGEAIS CYRILLE , RADER DANIEL J , KRAWIEC JOHN A , SOUTH VICTORIA J
发明人： JAYE MICHAEL , LYNCH KEVIN J , AMIN DILIP V , DOAN KIM-ANH THI , MARCHADIER DAWN , MAUGEAIS CYRILLE , RADER DANIEL J , KRAWIEC JOHN A , SOUTH VICTORIA J
IPC分类号： G01N33/50 , A61K31/7088 , A61K35/76 , A61K38/00 , A61K38/55 , A61K39/395 , A61K45/00 , A61K48/00 , A61P3/06 , A61P43/00 , C07K16/40 , C12N9/20 , C12N15/09 , G01N33/15 , G01N33/53 , G01N33/566 , A61K
CPC分类号： C07K16/40 , A61K38/00 , A61K48/00 , C12N9/20
摘要： Compositions and methods for raising the level of HDL cholesterol and apolipoprotein AI in a patient and for lowering the levels of VLDL cholesterol and LDL cholesterol in a patient, including compositions and methods which effect the expression of a gene, LIPG, which encodes a lipase enzyme that is a member of the tryacylglycerol lipase family or which effect the enzymatic activity of the enzyme.
摘要翻译：用于提高患者中HDL胆固醇和载脂蛋白AI水平以及降低患者中VLDL胆固醇和LDL胆固醇水平的组合物和方法，包括影响基因表达的组合物和方法，LIPG编码脂肪酶它是脂肪酰甘油脂肪酶家族的成员，或者影响酶的酶活性。

19. 发明申请

WO0039590A2 PREDICTIVE METHODS BASED ON ALPHA-1-ACID GLYCOPROTEIN LEVELS 审中-公开
标题翻译：基于ALPHA-1-ACID GLYCOPROTEIN水平的预测方法
公开(公告)号：WO0039590A2
公开(公告)日：2000-07-06
申请号：PCT/US9931284
申请日：1999-12-30
申请人： AVENTIS PHARM PROD INC , BRUNO RENE
发明人： BRUNO RENE
IPC分类号： G01N33/574 , G01N33/68
CPC分类号： G01N33/68 , G01N33/57407
摘要： A method for determining the dosage of a taxoid to administer to a patient who is being treated for cancer and whose body fluids include alpha-1-acid glycoprotein comprising observing the patient's level of alpha-1-acid glycoprotein, evaluating said level to determine the dosage of the taxoid to administer to the patient by comparing said level to a predetermined alpha-1-acid glycoprotein level derived from a population of patients having said cancer and treated with said taxoid at a common dosage and based on said evaluation, recommending the dosage of the taxoid to administer to the patient. Also, a method for assessing the effect of treatment of a patient who has cancer and who is being treated with a taxoid comprising observing the patient's alpha-1-acid glycoprotein level, comparing said level to a predetermined alpha-1-acid glycoprotein level derived from a population of patients having said cancer and treated with said taxoid at a common dosage and based on said comparison, assessing the effect of continued treatment of the patient with respect to the patient's response to treatment, the length of survival of the patient, or side effects that may be experienced by the patient. Also, a method for reducing the side effects experienced by a patient who has cancer and who is to be treated with a taxoid comprising observing the patient's alpha-1-acid glycoprotein (AAG) level, comparing said level to a predetermined alpha-1-acid glycoprotein level derived from a population of patients having said cancer and treated with said taxoid at a common dosage and based on said comparison recommending the dosage of said taxoid to administer to said patient to reduce the incidence or severity of side effects that the patient may experience during treatment with said taxoid.
摘要翻译：一种确定紫杉烷类药物给予正在接受治疗的患者的剂量的方法，其体液包括α-1-酸糖蛋白，其包括观察患者的α-1-酸性糖蛋白水平，评估所述水平以确定通过将所述水平与来源于患有所述癌症的患者群体并以所述评估用所述紫杉烷类型治疗的预定α-1-酸糖蛋白水平进行比较来评估紫杉烷类药物的剂量，并且基于所述评估，推荐剂量的紫杉醇给予患者。此外，评估治疗患有癌症并且正在用紫杉烷类药物治疗的患者的效果的方法，其包括观察患者的α-1-酸糖蛋白水平，将所述水平与预先确定的α-1-酸糖蛋白水平进行比较从具有所述癌症的患者的群体中并且以所述比较为基础用所述紫杉烷类药物治疗，并且基于所述比较，评估患者对患者对治疗反应的持续治疗的效果，患者的存活时间，或患者可能经历的副作用。另外，一种降低患有癌症并且要用紫杉烷类药物治疗的患者所经历的副作用的方法，包括观察患者的α-1-酸性糖蛋白（AAG）水平，将所述水平与预定的α1- 来自具有所述癌症的患者群体的酸性糖蛋白水平，并以相同的剂量用所述紫杉烷类型治疗，并且基于所述比较，推荐所述紫杉烷类药物的剂量以施用于所述患者以降低患者可能的副作用的发生率或严重程度用紫杉醇治疗期间的经验。

20. 发明申请

WO9935241A9 TRANSGENIC RABBIT THAT EXPRESSES A FUNCTIONAL HUMAN LIPOPROTEIN (A) 审中-公开
标题翻译：表达功能性人类脂蛋白（A）的转基因兔
公开(公告)号：WO9935241A9
公开(公告)日：2000-04-13
申请号：PCT/US9900401
申请日：1999-01-08
申请人： AVENTIS PHARM PROD INC , ROUY DIDIER , DUVERGER NICOLAS , EMMANUEL FLORENCE , DENEFLE PATRICE , HOUDEBINE LOUIS MARIE , VIGLIETTA CELINE , RUBIN EDWARD , HUGHES STEVEN D
发明人： ROUY DIDIER , DUVERGER NICOLAS , EMMANUEL FLORENCE , DENEFLE PATRICE , HOUDEBINE LOUIS-MARIE , VIGLIETTA CELINE , RUBIN EDWARD , HUGHES STEVEN D
IPC分类号： A01K67/027 , A61K49/00 , C07K14/775 , C12N15/09 , C12N15/85 , C12N5/00 , C12N9/00 , C12N11/10 , C12N15/00 , G01N31/00
CPC分类号： C07K14/775 , A01K67/0275 , A01K67/0278 , A01K2207/15 , A01K2217/00 , A01K2217/05 , A01K2227/107 , A01K2267/03 , A01K2267/0375 , A61K49/0008 , C12N15/8509 , Y10S977/924
摘要： A transgenic rabbit which has in its genomic DNA sequences that encode apolipoprotein (a) and apolipoprotein B polypeptides which are capable of combining to produce lipoprotein (a), a process for creating such a rabbit, and the use of the rabbit to identify compounds which are effective in the treatment of human diseases which are associated with, induced and/or exacerbated by Lp(a) expression.
摘要翻译：一种转基因兔，其基因组DNA序列中编码能组合产生脂蛋白（a）的载脂蛋白（a）和载脂蛋白B多肽，一种制备这种兔子的方法，以及使用该兔子鉴定化合物对于与Lp（a）表达相关，诱导和/或恶化的人类疾病的治疗有效。

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