公开(公告)号：DE4404370A1

公开(公告)日：1995-03-09

申请号：DE4404370

申请日：1994-02-11

Applicant: BAYER AG

Inventor： LOCKHOFF OSWALD DR ,  HAYAUCHI YUTAKA DR ,  MIELKE BURKHARD DR ,  BRUNNER HELMUT PROF DR ,  STUENKEL KLAUS DR ,  SPERZEL MICHAEL DR ,  SCHALLER KLAUS DR

IPC: A61K38/00 ,  C07H15/12 ,  C07K9/00 ,  C07H5/06 ,  A61K31/70 ,  A61K38/05 ,  C07K5/00

公开(公告)号：DE4320157A1

公开(公告)日：1994-12-22

申请号：DE4320157

申请日：1993-06-18

Applicant: BAYER AG

Inventor： HEINEMANN ULRICH DR ,  TIEMANN RALF DR ,  STUENKEL KLAUS DR

IPC: A61K31/40 ,  A61K31/41 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61K31/55 ,  A61P9/00 ,  A61P43/00 ,  C07D285/00 ,  C07D285/01 ,  C07D417/04 ,  C07D417/12

公开(公告)号：DE4226373A1

公开(公告)日：1994-02-17

申请号：DE4226373

申请日：1992-08-10

Applicant: BAYER AG

Inventor： PIEL NORBERT DR ,  RODRIGUEZ MARIA-LUISA DR ,  WEICHEL WALTER DR ,  BAUMGARTEN JOERG DR ,  SCHUTT HERMANN DR ,  RAST HANS-GEORG DR ,  BRUNNER HELMUT PROF DR ,  SCHALLER KLAUS DR ,  SCHOENFELD WOLFGANG DR ,  SPERZEL MICHAEL DR ,  STUENKEL KLAUS DR

IPC: A61K38/00 ,  C07K9/00 ,  C07K14/195 ,  C07K7/10 ,  A61K37/02 ,  C07K15/14

Abstract: Glycoproteins including the aminoacid sequence Glu-Glu-Pro-Asp-Gln-Thr-Thr-Val-Asp- Gln-Pro-Glu-Asn-Asn'-Gln-Thr-Met-Thr' -Thr'-Thr'-Met-Thr-Glu in which Asp' and Thr' respectively are bound to an acidic oligosaccharide by an N-glycosidic bonding and by a complete or partial O-glycosidic bonding to a neutral oligosaccharide are new. The glycopeptides may be elongated at (i) their N-terminus by up to 740 aminoacids (AA), and at their (ii) C-terminus by up to 54 AA, possible including N- and O-glycosidically bound oligosaccharides and/or polysaccharides. USE/ADVANTAGE - The glycopeptides are useful in medicaments for therapy and prophylaxis of patients with bacterial, viral, fungal and parasitic infections by boosting the unspecific body defence. The new glycopeptides are more effective in protection against infection and in increasing the colony stimulating factor (CSF). In an example, the 600 bp fragment of H.salinarious DSM668 was cleaved with subtilisin and the glycoproteins of the sequence above were shown to have a very good immunostimulating activity. The activation of tumour necrosis factor (TNF) activity in sera was determined by cytolysis of TNF-sensitive WEHI164/13 cells. NMRI mice together with WEHI-cells in FCS/RPMI medium were incubated overnight at 37 deg.C and 7% CO2. The TNF serum level was increased after treatment with the glycoprotein. To test the prophylaxis for acute infections (peritonitis, sepsis) 24 mice were either treated with the glycoprotein or glycopeptide or with physiological NaCl soln.. After 24 hr they were injected intraperitoneally with 10x LD50 of Staphylococcus aureus ATCC13709. After 7 days, none, 3/24 and 9/24 mice treated with 10 mg/kg of NaCl glycoprotein and glycopeptide respectively survived. 0/24, 6/24 and 12/24 survived when treated with NaCl, glycoprotein and glycopeptides respectively.

公开(公告)号：DE3410238A1

公开(公告)日：1985-10-03

申请号：DE3410238

申请日：1984-03-21

Applicant: BAYER AG

Inventor： SCHLOSSMANN KLAUS DIPL CHEM DR ,  ZEMBROD ALFRED DIPL PHYS DR ,  LOCKHOFF OSWALD DIPL CHEM DR ,  KROLL HEIN-PETER DIPL BIOL DR ,  METZGER KARL-GEORG DR ,  OPITZ HANS-GEORG DR ,  PAESSENS ARNOLD DR ,  SCHALLER KLAUS DR ,  STREISSLE GERT DR ,  STUENKEL KLAUS DR ,  ZEILER HANS-JOACHIM DIPL BIOL

IPC: C07H13/00 ,  A61K9/00 ,  A61K9/127 ,  A61K31/70 ,  A61K31/7024 ,  A61P37/04 ,  C07H13/06 ,  C07H13/12 ,  C07H15/12 ,  C07H5/06

公开(公告)号：DE3812681A1

公开(公告)日：1989-11-02

申请号：DE3812681

申请日：1988-04-16

Applicant: BAYER AG

Inventor： LOCKHOFF OSWALD DR ,  GOOSSENS JOHN DIPL ING ,  BRUNNER HELMUT PROF DR ,  SPERZEL MICHAEL DR ,  STUENKEL KLAUS DR

IPC: A61K31/70 ,  A61K31/7028 ,  A61P37/04 ,  C07H15/12

公开(公告)号：DE3420116A1

公开(公告)日：1985-12-05

申请号：DE3420116

申请日：1984-05-30

Applicant: BAYER AG

Inventor： GROHE KLAUS DR ,  KLIMETZEK VOLKER DR ,  METZGER KARL DR ,  STUENKEL KLAUS DR ,  ZEILER HANS-JOACHIM DR

IPC: A61K31/47 ,  A61K31/495 ,  A61P37/04 ,  C07D215/56

Abstract: 1-Cyclopropylquinolone-3-carboxylic acids of the formula in which R1 is hydrogen, methyl, ethyl or beta -hydroxyethyl, and R2 is hydrogen, chlorine or fluorine or salts thereof stimulate the immune system, especially in conjunction with an antigen.