公开(公告)号：EP1747220A1

公开(公告)日：2007-01-31

申请号：EP04812567.8

申请日：2004-12-01

申请人： Aventis Pharmaceuticals Inc.

发明人： METZ, William, A. ,  HALLEY, Frank ,  DUTRUC-ROSSET, Gilles ,  CHOI-SLEDESKI, Yong, Mi ,  POLI, Gregory, B. ,  FINK, David, M. ,  DOERFLINGER, Gilles ,  HUANG, Bao-Guo ,  GELORMINI, Ann, Marie ,  GAMBOA, Juan, A. ,  GIOVANNI, Andrew ,  ROEHR, Joachim, E. ,  TSAY, Joseph, T. ,  CAMACHO, Fernando ,  HURST, William, J. ,  HARNISH, Stephen, W. ,  CHIANG, Yulin

IPC分类号： C07D471/04 ,  A61K31/437

CPC分类号： C07D471/04

摘要： The present invention discloses and claims substituted 1H-pyrrolo[3,2-b]pyridine-2-carboxamides, 1H-pyrrolo[3,2-c]pyridine-2-carboxamides and 1H-pyrrolo[2,3-c]pyridine-2-carboxamides (compounds of formula (I)) as inhibitors of human casein kinase I Epsilon, and methods of using said compounds of formula (I) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. Pharmaceutical compositions comprising compounds of formula (I) and methods for the preparation of compounds of formula (I) are also disclosed and claimed.

公开(公告)号：EP1622610B1

公开(公告)日：2006-12-20

申请号：EP04751319.7

申请日：2004-05-05

申请人： Aventis Pharmaceuticals, Inc.

发明人： BORCHERDING, David, R. ,  GROSS, Alexandre ,  SHUM, Patrick, Wai-Kwok ,  WILLARD, Nicole ,  FREED, Brian, S.

IPC分类号： A61K31/4155 ,  C07D401/12 ,  C07D451/02 ,  A61P29/00

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04

摘要： The present invention provides compounds of Formula (I) Wherein ( ) is an optional ethylene bridge; R1 is alkyl, cycloalkyl, aryl or aryl substituted with one or more substituents selected from alkyl, alkoxy and amino, or R1 is pyridyl or pyridyl substituted with one or more substituents selected from alkyl, alkoxy and amino; R2 is optionally substituted alkyl, alkoxyalkyl, optionally substituted cycloalkylalkyl, arylalkyl, or R2 is arylalkyl substituted with one or more substituents selected from alkyl, alkoxy; X is -C(O)-, -C(O)-CH2-, -S(O)2-, or NH-C(O)- ; and A is optionally substituted alkyl or other substituents as defined in claim 1. Pharmaceutical compositions comprising such compounds, their preparation, and their pharmaceutical use in the treatment of disease states capable of being modulated by the inhibition of p38 kinase and/or tumor necrosis factor (TNF), such as asthma or joint inflammation.

公开(公告)号：EP1051176B1

公开(公告)日：2006-11-22

申请号：EP99906684.8

申请日：1999-01-27

申请人： Aventis Pharmaceuticals, Inc.

发明人： EWING, William, R. ,  BECKER, Michael, R. ,  CHOI-SLEDESKI, Yong, Mi ,  PAULS, Heinz, W. ,  HE, Wei ,  CONDON, Stephen, M. ,  DAVIS, Roderick, S. ,  HANNEY, Barbara, A. ,  SPADA, Alfred, P. ,  BURNS, Christopher, J. ,  JIANG, John, Z. ,  LI, Aiwen ,  MYERS, Michael, R. ,  LAU, Wan, F. ,  POLI, Gregory, B.

IPC分类号： C07D241/08 ,  A61K31/495

CPC分类号： C07D471/04 ,  C07D241/08 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D495/04

摘要： This invention is directed to oxoazaheterocyclyl compounds which inhibit factor Xa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds and to a method of inhibiting factor Xa.

公开(公告)号：EP1706422A1

公开(公告)日：2006-10-04

申请号：EP04813202.1

申请日：2004-12-07

申请人： Aventis Pharmaceuticals, Inc.

发明人： PARKAR, Ashfaq ,  AUGUST, Paul ,  KUNTZWEILER, Theresa ,  ARDATI, Mohamad, Ali ,  BASKARAN, Namadev

IPC分类号： C07K14/72

CPC分类号： C07K14/72 ,  C07K14/723 ,  C07K2319/00

摘要： Described herein is a novel member of the prostanoid receptor family, a guinea pig prostaglandin D2 receptor. Described are the receptor, the nucleic acid that encodes it, and various uses for both.

摘要翻译： 本文描述了前列腺素类受体家族的新成员，即豚鼠前列腺素D2受体。 描述了受体，编码它的核酸以及两者的各种用途。

公开(公告)号：EP1687642A2

公开(公告)日：2006-08-09

申请号：EP04790957.7

申请日：2004-10-07

申请人： CENTELION ,  AVENTIS PHARMACEUTICALS INC.

发明人： NESBIT, Mark ,  SPADA, Alfred, P. ,  HE, Wei ,  MYERS, Michael, R.

IPC分类号： G01N33/74 ,  A61K31/498 ,  A61P9/00 ,  A61P35/00

CPC分类号： A61K31/498 ,  G01N33/5011 ,  G01N2333/71

摘要： This invention is directed to potent inhibitors of protein tyrosine kinase alone or in synergistic combination with antiangiogenic or chemotherapeutic agents for the abrogation of mature vasculature within chemotherapeutic refractory tumors, pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cell proliferation, and particularly treatment of brain cancer, ovarian cancer, pancreatic cancer prostate cancer, and human leukemias, such as CML, AML or ALL.

公开(公告)号：EP1680424A2

公开(公告)日：2006-07-19

申请号：EP04788585.0

申请日：2004-09-03

申请人： NEUROGEN CORPORATION ,  Aventis Pharmaceuticals, Inc.

发明人： GE, Ping ,  HORVATH, Raymond, F. ,  ZHANG, Lu, Yan ,  YAMAGUCHI, Yasuchika ,  KAISER, Bernd ,  ZHANG, Xuechun ,  ZHANG, Suoming ,  ZHAO, He ,  JOHN, Stanly ,  MOORCROFT, Neil ,  SHUTSKE, Greg

IPC分类号： C07D487/04

CPC分类号： C07D471/04 ,  C07D487/04

摘要： Substituted heteroaryl fused pyridine, pyrazine, and pyrimidine compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

公开(公告)号：EP1675858A2

公开(公告)日：2006-07-05

申请号：EP04788563.7

申请日：2004-09-03

申请人： NEUROGEN CORPORATION ,  Aventis Pharmaceuticals, Inc.

发明人： HODGETTS, Kevin, J. ,  JOHN, Stanly ,  MOORCROFT, Neil ,  SHUTSKE, Greg ,  KAISER, Bernd ,  YAMAGUCHI, Yasuchika ,  GE, Ping ,  HORVATH, Raymond, F.

IPC分类号： C07D487/04 ,  C07D471/04 ,  C07D519/00 ,  A61K31/519 ,  A61K31/437 ,  A61P25/18 ,  A61P25/22

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D519/00

摘要： 5-aryl-Pyrazolo[4,3-d] pyrimidines, 6-aryl-Pyrazolo[3,4-d]pyrimidines and related compounds, as well as other chemically related compounds, that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRIF receptor binding. Methods of using the compounds in receptor localization studies are given.

公开(公告)号：EP1630709A3

公开(公告)日：2006-06-14

申请号：EP05077415.7

申请日：2000-05-25

申请人： AVENTIS PHARMACEUTICALS INC.

发明人： Theilhaber, Joachim ,  Bushnell, Steven ,  Fuchs, Rainer

IPC分类号： G06F19/00

CPC分类号： G06F19/20

摘要： The present invention relates to a highly accurate and reproducible mathematically-based methodology for quantifying the levels of differential gene expression from microassay protocols. Specifically, the present invention provides a simple deductive approach, grounded in a Bayesian framework, to circumvent the heuristic-based limitation of previous methodologies. Rather than seeking a point-estimate of the fold-change of the level of gene expression, the present invention utilizes the derivation of mathematical formula to determine the a posteriori distribution of all the fold-changes of differential gene expression which may be inferred from the given measurements. From this a posteriori distribution the following information may be obtained: (i) an estimator for the fold-change of the level of gene expression; (ii) confidence limits for the fold-change, at any given confidence level; and (iii) a P-value for assessing the statistical significance of change. The present invention also possesses the advantage that fold-change estimates and confidence limits may even be assigned to signal pairs where both signals are zero or negative, without resorting to heuristic thresholds.

公开(公告)号：EP1644371A1

公开(公告)日：2006-04-12

申请号：EP03742433.0

申请日：2003-07-03

申请人： AVENTIS PHARMACEUTICALS INC.

发明人： MAJID, Tahir, N. ,  HOPKINS, Corey ,  PEDGRIFT, Brian, L. ,  COLLAR, Nicola ,  WIRTZ-BRUGGER, Friederike ,  MERRILL, Jean

IPC分类号： C07D471/04 ,  C07D231/00 ,  C07D221/00

CPC分类号： C07D471/04

摘要： Novel pyrazoloisoquinoline derivatives as kinase inhibitors are disclosed which are suitable for producing pharmaceuticals for the prophylaxis and therapy of diseases whose course involves an increased activity of NIK.

摘要翻译： 公开了作为激酶抑制剂的新型吡唑并异喹啉衍生物，其适于生产用于预防和治疗其病程涉及NIK活性增加的疾病的药物。

公开(公告)号：EP1589991A1

公开(公告)日：2005-11-02

申请号：EP04702167.0

申请日：2004-01-14

申请人： Aventis Pharmaceuticals, Inc.

发明人： ROSSKAMP, Ralf ,  GERSTEIN, Hertzel

IPC分类号： A61K38/28 ,  A61P3/08 ,  A61P3/10 ,  A61P9/10

CPC分类号： A61K38/28

摘要： This invention relates to a method of reducing cardiovascular morbidity and mortality in a prediabetic or Type 2 Diabetes patient population. The method comprises administering an effective dosage of a long acting insulin, preferably insulin glargine, to a prediabetic or Type 2 Diabetes patient.