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1. WO1996039503 - C5a RECEPTOR ANTAGONISTS HAVING SUBSTANTIALLY NO AGONIST ACTIVITY AND METHODS FOR PREPARATION

Publication Number WO/1996/039503
Publication Date 12.12.1996
International Application No. PCT/EP1996/002422
International Filing Date 04.06.1996
Chapter 2 Demand Filed 03.12.1996
IPC
A61K 38/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
C07K 14/47 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
46from vertebrates
47from mammals
C07K 16/18 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
16Immunoglobulins, e.g. monoclonal or polyclonal antibodies
18against material from animals or humans
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 37/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
C07K 14/472
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
46from vertebrates
47from mammals
4701not used
472Complement proteins, e.g. anaphylatoxin, C3a, C5a
C07K 16/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
16Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
18against material from animals or humans
C07K 2319/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
2319Fusion polypeptide
Applicants
  • NOVARTIS AG [CH]/[CH] (AllExceptUS)
  • VAN OOSTRUM, Jan [CH]/[CH] (UsOnly)
  • VAN HEEKE, Gino [BE]/[GB] (UsOnly)
  • SCHMITZ, Albert [DE]/[CH] (UsOnly)
Inventors
  • VAN OOSTRUM, Jan
  • VAN HEEKE, Gino
  • SCHMITZ, Albert
Common Representative
  • NOVARTIS AG
Priority Data
08/462,64805.06.1995US
08/463,22405.06.1995US
08/463,37705.06.1995US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) C5a RECEPTOR ANTAGONISTS HAVING SUBSTANTIALLY NO AGONIST ACTIVITY AND METHODS FOR PREPARATION
(FR) ANTAGONISTES DES RECEPTEURS DE C5a NE PRESENTANT SENSIBLEMENT AUCUNE ACTIVITE AGONISTE ET LEURS PROCEDES DE PREPARATION
Abstract
(EN)
Disclosed are polypeptide analogues or derivatives of human C5a which are C5a receptor antagonists that exhibit substantially no analphylatoxin or agonist activity, and derivatives of the analogues, and dimeric forms of the analogues or derivatives. DNA molecules encoding the polypeptides and methods of making the analogues are also provided. Pharmaceutical formulations containing a C5a analogue or derivative, are used therapeutically in the treatment of C5a-mediated diseases and inflammatory conditions in mammals, and prophylactically to prevent or reduce inflammation caused by an event which causes inflammation or aggravates an existing inflammatory condition, respectively. Further disclosed are antibodies specific to the C5a analogues, derivatives thereof, and dimers of the analogues and derivatives which exhibit substantially no cross-reactivity with human C5a. The antibodies are used to detect or quantify circulating C5a analogue or derivative, as well as to modify, e.g., neutralize, the activity of the C5a receptor antagonist $i(in vivo).
(FR)
Analogues polypeptidiques ou dérivés de C5a humaine, antagonistes des récepteurs de C5a ne présentant sensiblement aucune activité d'anaphylatoxine ou d'agoniste, et dérivés de ces analogues, ainsi que les formes dimères des analogues ou des dérivés. L'invention concerne également des molécules d'ADN codant les polypeptides et des procédés de production des analogues. Des formulations pharmaceutiques contenant un analogue ou un dérivé de C5a sont employées en thérapeutique dans le traitement des maladies à médiation par C5a et des états inflammatoires chez des mammifères, et en prophylaxie pour prévenir ou réduire les inflammations provoquées par un événement causant une inflammation ou aggravant un état inflammatoire préexistant, respectivement. Sont également décrits des anticorps spécifiques aux analogues de C5a, à leurs dérivés, et aux dimères des analogues et dérivés ne présentant sensiblement aucune réactivité croisée avec la C5a humaine. Les anticorps sont utilisés pour détecter ou quantifier la circulation d'analogue ou de dérivé de C5a, ainsi que pour modifier, par exemple neutraliser, l'activité de l'antagoniste du récepteur de C5a $i(in vivo).
Also published as
Latest bibliographic data on file with the International Bureau