公开(公告)号：EP1451856A2

公开(公告)日：2004-09-01

申请号：EP02798432.7

申请日：2002-11-07

申请人： Pharmacia Corporation

发明人： CROWLEY, Kathleen, S. ,  BASHKIN, James, K. ,  SCHWEITZER, Barbara, A. ,  PHILLION, Dennis, P.

IPC分类号： H01L21/00

CPC分类号： C12N15/63 ,  A61K31/275 ,  A61K31/40 ,  A61K31/495

摘要： A method for enhancing cellular uptake and redistributing gene regulating polyamides from the extranuclear areas in eukaryotic cells to the nucleus thereof. The method consists of administering to the eukaryotic cells a molecular trafficking compound. The administered molecular trafficking compound affects cellular pathways and mechanisms that accumulate polyamides in cytoplasmic vessicles and/or efflux polyamides from the intracellular regions of cell. The method also includes modifying polyamides to contain negatively-charged or acidic moieties wherein the moieties inhibit the accumulation of polyamides in cellular lysosomes. By affecting the cellular pathways and mechanisms, the polyamides are redistributed throughout the cell, whereby nuclear accumulation of the polyamides is enhanced.

公开(公告)号：EP1421056A1

公开(公告)日：2004-05-26

申请号：EP02757083.7

申请日：2002-08-13

申请人： Pharmacia Corporation

发明人： PHILLION, Dennis, P.

IPC分类号： C07C211/24 ,  C07C211/27 ,  C07C209/74

CPC分类号： C07D403/14 ,  C07B2200/11 ,  C07C17/16 ,  C07C205/57 ,  C07C209/74 ,  C07C269/06 ,  C07C303/02 ,  C07D207/34 ,  C07D233/90 ,  C07D307/68 ,  C07F9/12 ,  C07F9/1406 ,  C07F9/4015 ,  C07F9/4075 ,  C07F9/42 ,  C07F9/4465 ,  C08F8/30 ,  C07C211/24 ,  C07C271/22 ,  C07C309/86

摘要： The present invention describes immobilized haloenamine reagents, immobilized tertiary amides, methods for their preparation, and methods of use.

公开(公告)号：EP1442022A2

公开(公告)日：2004-08-04

申请号：EP02802875.1

申请日：2002-11-07

申请人： Pharmacia Corporation

发明人： PHILLION, Dennis, P. ,  CROWLEY, Kathleen, S. ,  BASHKIN, James, K. ,  SCHWEITZER, Barbara, A. ,  BURNETTE, Barry, L. ,  WOODARD, Scott, S.

IPC分类号： C07D231/02 ,  C07D403/02 ,  C12N5/02

CPC分类号： C12N15/635 ,  C07K14/575

摘要： Processes and compositions are provided for regulating COX2 gene expression in a cell. The process includes selecting a polyamide composition comprising N-methyl pyrrole (Py) and N-methyl imidazole (Im) to provide specific binding to DNA at a COX2 gene target site in a cell. The polyamide is then combined with the cell containing the COX2 gene, wherein the polyamide binds to the COX2 gene promoter target site and regulates transcription of the COX2 gene.

公开(公告)号：EP1572693A1

公开(公告)日：2005-09-14

申请号：EP03814268.3

申请日：2003-12-19

申请人： Pharmacia Corporation

发明人： ANDERSON, David, R. ,  MAHONEY, Matthew, W. ,  PHILLION, Dennis, P. ,  ROGERS, Thomas, E. ,  MEYERS, Marvin, J. ,  PODA, Gennadiy ,  HEGDE, Shridhar, G. ,  SINGH, Megh ,  REITZ, David, B. ,  WU, Kun, K. ,  BUCHLER, Ingrid, P. ,  XIE, Jin ,  VERNIER, William, F.

IPC分类号： C07D471/06

CPC分类号： C07D471/04 ,  C07D401/04 ,  C07D401/14 ,  C07D471/14 ,  C07D487/04 ,  C07D513/04 ,  C07D519/00

摘要： Compounds are described which inhibit mitogen activated protein kinase-activated protein kinase-2 (MK-2). Methods of using such compounds for the inhibition of MK-2, and for the prevention or treatment of a disease or disorder that is mediated by TNFα, are described, where the method involves administering to the subject an MK-2 inhibiting compound of the present invention. Therapeutic compositions, pharmaceutical compositions and kits which contain the present MK-2 inhibiting compounds are also described.

公开(公告)号：EP1430028A2

公开(公告)日：2004-06-23

申请号：EP02796456.8

申请日：2002-08-30

申请人： Pharmacia Corporation

发明人： PHILLION, Dennis, P.

IPC分类号： C07D207/34

CPC分类号： C07D403/14 ,  C07B2200/11 ,  C07C17/16 ,  C07C205/57 ,  C07C209/74 ,  C07C269/06 ,  C07C303/02 ,  C07D207/34 ,  C07D233/90 ,  C07D307/68 ,  C07F9/12 ,  C07F9/1406 ,  C07F9/4015 ,  C07F9/4075 ,  C07F9/42 ,  C07F9/4465 ,  C08F8/30 ,  C07C211/24 ,  C07C271/22 ,  C07C309/86

摘要： The present invention is directed to protected amino acid halide monomers and oligomers, and to their use in the efficient sythesis of polyamides. The present invention is further directed to the use of -haloenamine reagents, which may optionally be immobilized, for the preparation of the amino acid halides.