公开(公告)号：EP1307216A4

公开(公告)日：2005-01-12

申请号：EP01952656

申请日：2001-07-12

申请人： GRYPHON THERAPEUTICS INC

发明人： KOCHENDOERFER GERD ,  BRADBURNE JAMES A ,  WILKEN JILL G

IPC分类号： A61K47/30 ,  A61K38/00 ,  A61K38/19 ,  A61K45/00 ,  A61K47/34 ,  A61K47/48 ,  A61P9/10 ,  A61P11/06 ,  A61P17/00 ,  A61P27/16 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/08 ,  C07H21/04 ,  C07K14/47 ,  C07K14/52 ,  C07K14/715 ,  C07K19/00 ,  C12P21/02

CPC分类号： C07K14/7158 ,  A61K38/00 ,  A61K47/60 ,  A61K47/62

摘要： The invention relates to polymer-modified bioactive synthetic chemokines and to methods for their production and use. The bioactive synthetic chemokines of the invention comprises a polymer modified polypeptide chemokine backbone. The compounds and methods or the invention are useful for the treatment of disorders involving naturally occurring chemokines, such as for the treatment of HIV and AIDS related disorders and for the treatment of asthma, allergic rhinitis, atopic dermatitis, atheroma/atherosclerosis, organ transplant rejection, and rheumatoid arthritis.

公开(公告)号：EP1318827A1

公开(公告)日：2003-06-18

申请号：EP01952654.0

申请日：2001-07-12

申请人： Gryphon Therapeutics, Inc.

发明人： KOCHENDOERFER, Gerd, G. ,  LOW, Donald, W. ,  BOTTI, Paolo ,  WILKEN, Jill, G. ,  BRADBURNE, James, A. ,  CHEN, Shiah-yun ,  CRESSMAN, Sonya ,  HUNTER, Christie, L. ,  KENT, Stephen, B., H.

IPC分类号： A61K38/02 ,  A61K38/18 ,  A61K38/19 ,  A61K38/20 ,  A61K38/21 ,  C07K1/113 ,  C07K1/13 ,  C07K2/00 ,  C07K14/475

CPC分类号： C07K14/505 ,  A61K38/00

摘要： The present invention relates to methods and compositions for modifying peptides, polypeptides and proteins with polymers, especially glyco-mimetic polymers, so as to improve their biological activity or pharmacokinetic properties. The invention further provides methods and uses for such polymer-modified peptides, polypeptides and proteins. The invention is particularly suitable for use in the synthesis of polymer-modified synthetic bioactive proteins (Figure 1D), and of pharmaceutical compositions that contain such proteins.

公开(公告)号：EP1315738A1

公开(公告)日：2003-06-04

申请号：EP01968707.8

申请日：2001-09-07

申请人： Gryphon Therapeutics, Inc.

发明人： BOTTI, Paolo ,  BRADBURNE, James, A. ,  KENT, Stephen, B.H. ,  LOW, Donald, W.

IPC分类号： C07K1/00

CPC分类号： C07K14/80 ,  C07K5/06026 ,  C07K5/06086 ,  C07K5/06147 ,  C07K5/0812 ,  C07K7/06

摘要： The invention is directed to methods and compositions for chemical ligation of components comprising a first component having a carboxythioester, and preferable an α-carboxythioester, moiety and a second component having an N-substituted, and preferably an Nα-substituted, 2 or 3 carbon chain alkyl or aryl thiol to give a ligation product having an N-substituted amide bond at the ligation site. The reactants of the invention are chemoselective, and the alkyl or aryl thiol moiety is removable from the ligation product. Removal of the alkyl or aryl thiol gives a native amide bond at the ligation site. The methods and compositions of the invention are particularly useful for ligation of peptides and polypeptides. The ligation system of the invention is applicable to a wide variety of molecules, and thus can be exploited to generate peptides, polypeptides and other amino acid containing polymers having a native amide bond at the ligation site.

公开(公告)号：EP1315511A2

公开(公告)日：2003-06-04

申请号：EP01957133.0

申请日：2001-07-12

申请人： Gryphon Therapeutics, Inc.

发明人： KOCHENDOERFER, Gerd ,  BOTTI, Paolo ,  BRADBURNE, James, A. ,  CHEN, Shiah-yun ,  CRESSMAN, Sonya ,  HUNTER, Christie, L. ,  KENT, Stephen, B.H. ,  LOW, Donald, W.

IPC分类号： A61K38/00 ,  C07K1/00 ,  C07K14/505

CPC分类号： C07K14/505 ,  A61K38/00

摘要： Synthetic erythropoiesis stimulating proteins are provided. Also provided are methods for synthesizing the proteins. The invention further relates to derivatives of such synthetic erythropoiesis stimulating proteins that are polymer-modified in a defined manner. Methods and uses for such proteins and derivatized proteins are also provided.

公开(公告)号：EP1299415A1

公开(公告)日：2003-04-09

申请号：EP01984163.4

申请日：2001-07-12

申请人： Gryphon Therapeutics, Inc.

发明人： OFFORD, Robin ,  GAERTNER, Hubert ,  HARTLEY, Oliver

IPC分类号： C07K14/435 ,  C07K14/47 ,  C07K14/52 ,  A61K38/16 ,  A61K38/17 ,  A61K38/19

CPC分类号： C07K14/7158 ,  A61K38/00 ,  A61K47/60 ,  A61K47/62

摘要： Chemokine receptor modulators comprising a chemically modified carboxyl-terminus (C-terminus) and/or amino-terminus (N-terminus) for modulating potency and pharmacokinetic properties, and methods of production and use are disclosed. The compounds and methods of the invention are exemplified by novel N-terminal, C-terminal and N/C-terminal analogs of CC and CXC chemokines. The chemokine receptor modulator analogs of the invention are useful for the treatment of disorders involving the naturally occurring chemokine that the analogs of the invention antagonize, such as for the treatment of HIV and AIDS related disorders and for the treatment of asthma, allergic rhinitis, atopic dermatitis, atheroma/atherosclerosis, organ transplant rejection, and rheumatoid arthritis.