公开(公告)号：EP1608631A2

公开(公告)日：2005-12-28

申请号：EP04758392.7

申请日：2004-03-26

申请人： SCIOS INC.

发明人： DUGAR, Sundeep ,  CHAKRAVARTY, Sarvajit ,  CONTE, Aurelia ,  AXON, Jonathan ,  MCENROE, Glenn

IPC分类号： C07D239/70 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04

CPC分类号： C07D487/04 ,  A61K31/517 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04

摘要： Compounds in which a pyrimidine nucleus is bridged at the (5) and (6) position and are further substituted at positions (2) and (4) with substituents comprising aromatic moieties are useful in treating subjects with conditions ameliorated by inhibition of TGFβ activity.

摘要翻译： 其中嘧啶核在（5）和（6）位桥接并且在位置（2）和（4）处用包含芳族部分的取代基进一步取代的化合物可用于治疗患有通过抑制TGFβ活性而改善的病症的受试者。

公开(公告)号：EP1589960A1

公开(公告)日：2005-11-02

申请号：EP03813828.5

申请日：2003-12-18

申请人： Scios, Inc.

发明人： MEDICHERLA, Satyanarayana ,  PROTTER, Andrew, A. ,  SCHREINER, George, F.

IPC分类号： A61K31/155 ,  A61K31/415 ,  A61K31/445 ,  A61K31/505

CPC分类号： A61K31/445 ,  A61K31/00 ,  A61K31/155 ,  A61K31/415 ,  A61K31/505

摘要： The invention concerns the treatment obesity and associated conditions with TGF-β inhibitors. More specifically, the invention concerns the use of TGF-β inhibitors in the treatment of obesity, type 2 diabetes, and pathologic conditions associated with obesity or type 2 diabetes.

公开(公告)号：EP1560582A2

公开(公告)日：2005-08-10

申请号：EP03770722.1

申请日：2003-10-09

申请人： SCIOS INC.

发明人： DUGAR, Sundeep

IPC分类号： A61K31/437 ,  A61K31/496 ,  C07D487/04

CPC分类号： C07D471/04 ,  A61K31/496 ,  A61K31/56 ,  A61K39/395 ,  A61K45/06 ,  Y02A50/412 ,  A61K2300/00

摘要： The invention is directed to methods to inhibit p38 kinase, preferably p38-alpha using compounds which are azaindoles wherein the azaindoles are coupled through a piperidine or piperazine type linker to another cyclic moiety.

公开(公告)号：EP1551807A1

公开(公告)日：2005-07-13

申请号：EP03764582.7

申请日：2003-07-11

申请人： SCIOS INC.

发明人： MAVUNKEL, Babu ,  PERUMATTAM, John, Joseph ,  TESTER, Richland, Wayne ,  DUGAR, Sundeep

IPC分类号： C07D215/24

CPC分类号： C07C239/20

摘要： Improved reagents and methods of amination are provided. The reagents are phenyl hydroxylamines containing one nitro and at least one CF3 substituent on the phenyl moiety.

公开(公告)号：EP1539121A2

公开(公告)日：2005-06-15

申请号：EP03791848.9

申请日：2003-08-29

申请人： SCIOS INC.

发明人： PROTTER, Andrew, Asher ,  LIU, David, Y.

IPC分类号： A61K31/00 ,  A61K31/409 ,  A61K31/505

CPC分类号： A61K31/404 ,  A61K31/4164 ,  A61K31/4174 ,  A61K31/4178 ,  A61K31/445 ,  A61K31/454 ,  A61K31/496 ,  A61K31/501 ,  A61K31/517 ,  A61K31/53

摘要： The invention is directed to methods of bone healing by administering a p38 MAP kinase inhibitor. The invention is directed to methods of treating bone fractures, bone diseases, bone grafting, especially enhancing bone healing following facial reconstruction, maxillary reconstruction, mandibular reconstruction or tooth extraction, enhancing long bone extension, enhancing prosthetic ingrowth, and increasing bone synostosis by administering a p38 MAP kinase inhibitor.

公开(公告)号：EP1524524A1

公开(公告)日：2005-04-20

申请号：EP04012655.9

申请日：1999-12-15

申请人： SCIOS INC.

发明人： Joly, Alison ,  Schreiner, George, F. ,  Stanton, Lawrence, W. ,  White, R., Tyler ,  Damm, Deborah, L. ,  Lewicki, John, A.

IPC分类号： G01N33/68 ,  C12Q1/68 ,  C07K14/475

CPC分类号： C07K14/475 ,  C12Q1/6883 ,  C12Q2600/158

摘要： The present invention relates to methods and compositions for the detection, diagnosis, prevention and treatment of a disease, specifically cardiac, kidney or inflammatory disease, and related disorders. The present invention also relates to compositions and methods useful in the diagnosis, prevention and therapeutic treatment of a disease, specifically cardiac, kidney or inflammatory disease. Specifically, methods and compositions are provided for the diagnostic evaluation and prognosis of conditions involving a disease, specifically cardiac, kidney or inflammatory disease, for the identification of subjects exhibiting a predisposition to such conditions, for modulating the effect of these differentially expressed genes, for monitoring patients undergoing clinical evaluation for the prevention and treatment of a disease, specifically cardiac, kidney or inflammatory disease, and its disorders, and for monitoring the efficacy of compounds used in clinical trials.

摘要翻译： 本发明涉及用于检测，诊断，预防和治疗疾病，特别是心脏，肾脏或炎症疾病以及相关疾病的方法和组合物。 本发明还涉及用于诊断，预防和治疗疾病，特别是心脏，肾脏或炎性疾病的组合物和方法。 具体地，提供方法和组合物用于诊断评估和涉及疾病，特别是心脏，肾脏或炎性疾病的病症，用于鉴定表现出对这些病症倾向的受试者，用于调节这些差异表达基因的作用，用于 监测接受临床评估的患者，预防和治疗疾病，特别是心脏，肾脏或炎症疾病及其疾病，并监测临床试验中使用的化合物的功效。

公开(公告)号：EP1453515A2

公开(公告)日：2004-09-08

申请号：EP02778799.3

申请日：2002-11-08

申请人： Scios Inc.

发明人： HIGGINS, Linda, S. ,  LIU, David, Y. ,  PROTTER, Andrew, A.

IPC分类号： A61K31/50 ,  A61K31/445 ,  A61K31/497

CPC分类号： A61K31/496 ,  A61K31/445 ,  A61K31/454 ,  A61K31/497 ,  A61K31/50

摘要： The invention is directed to methods to treat cystic fibrosis by administering certain imidazole derivatives.

公开(公告)号：EP0647268B1

公开(公告)日：2004-03-03

申请号：EP91912653.2

申请日：1991-06-17

申请人： SCIOS INC.

发明人： CORDELL, Barbara

IPC分类号： C12N15/00 ,  A01K67/027 ,  C12N15/18 ,  C12N15/85 ,  C12N15/12

CPC分类号： C12N15/85 ,  A01K67/0278 ,  A01K2207/15 ,  A01K2217/00 ,  A01K2217/05 ,  A01K2227/105 ,  A01K2267/0312 ,  C07K14/4711 ,  C12N15/8509 ,  C12N2830/002 ,  C12N2830/008 ,  C12N2830/15 ,  C12N2830/42 ,  C12N2830/85

摘要： Cloned recombinant or synthetic DNA sequences related to the pathology of Alzheimer's disease are injected into fertilized mammalian eggs (preferably mice eggs). The injected eggs are implanted in pseudo pregnant females and are grown to term to provide transgenic mice whose cells express proteins related to the pathology of Alzheimer's disease. The injected sequences are constructed having promoter sequences connected so as to express the desired protein in specific tissues of the transgenic mammal (most notably in nerve tissue). The proteins which are preferably ubiquitously expressed include (1) β-amyloid core precursor proteins; and (2) β-amyloid related precursor proteins; and (3) serine protease inhibitor. The transgenic mice provide useful models for studying compounds being tested for their usefulness in treating Alzheimer's disease, and for studying the in vivo interrelationships of these proteins to each other.

公开(公告)号：EP1315516A2

公开(公告)日：2003-06-04

申请号：EP01948768.5

申请日：2001-06-27

申请人： Scios Inc.

发明人： CORDELL, Barbara ,  SCHIMMOLLER, Frauke ,  LIU, Yu-Wang ,  QUON, Diana, Hom

IPC分类号： A61K38/48 ,  G01N33/50 ,  A61P25/28

CPC分类号： C12Q1/37 ,  C07K14/4711 ,  C12N9/6421 ,  G01N2500/04

摘要： The present invention is based on the findings that BACE2, a homolog of β-secretase BACE, is able to stimulate processing of APP in a non-amyloidogenic pathway, thereby suppressing the level of Aβ. Accordingly, the present invention provides methods and means for the identification and use of modulators of this unique activity of BACE2 to suppress Aβ production. The compounds identified using the methods and means provided herein may be used as potential candidates for the treatment of Alzheimer's disease and other neurological diseases.

公开(公告)号：EP1305406A2

公开(公告)日：2003-05-02

申请号：EP01935260.8

申请日：2001-05-09

申请人： Scios Inc.

发明人： CORDELL, Barbara ,  HIGAKI, Jeffrey, N. ,  MUTZ, Mitchell

IPC分类号： C12N9/64 ,  C07K14/47 ,  G01N33/68 ,  A61K38/17 ,  A61K38/43

CPC分类号： C12N9/6421 ,  A61K38/00 ,  C07K14/4711

摘要： The present invention provides cell-free η-secretase activity. The method of the invention utilizes a membrane source of APP/η-secretase mixture in the assay to determine factors that may enhance or decrease enzymatic activity affecting β-amyloid peptide production. The cell membranes used in the assay may be from cells expressing an endogenous APP or, preferably, cells expressing a recombinant APP. The APP may be full-length or a fragment capable of being proteolytically cleaved by η-secretase. In addition, the APP expressed in the cells may have one or more mutation, such as a point mutation, small deletion, etc.