公开(公告)号：EP1537099B1

公开(公告)日：2010-08-11

申请号：EP03749133.9

申请日：2003-08-21

申请人： Novartis Vaccines and Diagnostics, Inc.

发明人： DESAI, Manoj ,  NI, Zhi-Jie ,  NG, Simon ,  PFISTER, Keith, B. ,  RAMURTHY, Savithri ,  SUBRAMANIAN, Sharadha ,  WAGMAN, Allan, S.

IPC分类号： C07D401/12 ,  C07D521/00 ,  C07D405/14 ,  C07D401/14 ,  C07D453/02 ,  C07D413/14 ,  C07D487/08 ,  A61K31/4439 ,  A61P3/10

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D453/02 ,  C07D487/08

摘要： New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

公开(公告)号：EP1409468B1

公开(公告)日：2008-11-12

申请号：EP01968352.3

申请日：2001-08-31

申请人： Novartis Vaccines and Diagnostics, Inc.

发明人： RENHOWE, Paul, A. ,  CHU, Daniel ,  BOYCE, Rustum ,  NI, Zhi-Jie ,  DUHL, David ,  TOZZO, Effie ,  JOHNSON, Kirk ,  MYLES, David

IPC分类号： C07D295/20 ,  C07C279/18 ,  A61K31/155 ,  A61K31/495 ,  A61P3/00 ,  C07D309/14 ,  C07D213/40 ,  C07D213/82 ,  C07D233/54 ,  C07D243/08 ,  C07D241/42

CPC分类号： C07D233/64 ,  C07B2200/07 ,  C07B2200/09 ,  C07C279/18 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/10 ,  C07C2602/42 ,  C07C2603/74 ,  C07D209/16 ,  C07D215/12 ,  C07D241/08 ,  C07D241/42 ,  C07D295/215 ,  C07D307/24 ,  C07D309/14 ,  C07D333/20 ,  C07D487/04 ,  C07D487/08

摘要： Compounds of formula (IA) and (IB) are new where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.

摘要翻译： 式IIA和IIB的化合物是新的胍化合物，化学式=“CHEM-US-00001”num =“000

公开(公告)号：EP1409468B9

公开(公告)日：2009-07-29

申请号：EP01968352.3

申请日：2001-08-31

申请人： Novartis Vaccines and Diagnostics, Inc.

发明人： RENHOWE, Paul, A. ,  CHU, Daniel ,  BOYCE, Rustum ,  NI, Zhi-Jie ,  DUHL, David ,  TOZZO, Effie ,  JOHNSON, Kirk ,  MYLES, David

IPC分类号： C07D295/20 ,  C07C279/18 ,  A61K31/155 ,  A61K31/495 ,  A61P3/00 ,  C07D309/14 ,  C07D213/40 ,  C07D213/82 ,  C07D233/54 ,  C07D243/08 ,  C07D241/42

CPC分类号： C07D233/64 ,  C07B2200/07 ,  C07B2200/09 ,  C07C279/18 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/10 ,  C07C2602/42 ,  C07C2603/74 ,  C07D209/16 ,  C07D215/12 ,  C07D241/08 ,  C07D241/42 ,  C07D295/215 ,  C07D307/24 ,  C07D309/14 ,  C07D333/20 ,  C07D487/04 ,  C07D487/08

摘要： Compounds of formula (IA) and (IB) are new where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.

公开(公告)号：EP1868630A2

公开(公告)日：2007-12-26

申请号：EP06721134.2

申请日：2006-02-27

申请人： Novartis Vaccines and Diagnostics, Inc. ,  North China Pharmaceutical Group Corporation

发明人： CHU, Daniel ,  NI, Zhi-Jie ,  WANG, John, Jian-xin ,  LEI, Yaohui ,  BAI, Yu

IPC分类号： A61K38/04 ,  A61K38/14 ,  C07K7/50 ,  C07K7/54

CPC分类号： C07K9/008 ,  A61K38/00

摘要： Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of the desmethyl- vancomycin scaffold, in particular, acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. In addition, compounds of the invention include desmethyl- vancomycin scaffolds on which the acid moiety on the macrocyclic ring is converted to certain substituted amides and the amino substituent on the amino-substituted sugar moiety is alkylated with certain alkyl groups. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

公开(公告)号：EP1858908A2

公开(公告)日：2007-11-28

申请号：EP06736361.4

申请日：2006-02-27

申请人： Novartis Vaccines and Diagnostics, Inc. ,  North China Pharmaceutical Group Corporation

发明人： CHU, Daniel ,  NI, Zhi-Jie ,  WANG, John, Jian-xin ,  LEI, Yaohui ,  BAI, Yu

IPC分类号： C07G11/00

CPC分类号： C07K9/008

摘要： Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of a rearranged vancomycin or desmethyl-vancomycin scaffold, in particular, alkylation or acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.