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1. (WO1991009051) SUBSTITUTED CYCLIC PENICILLANIC ACID TETRAPEPTIDES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/009051 International Application No.: PCT/US1990/007443
Publication Date: 27.06.1991 International Filing Date: 12.12.1990
Chapter 2 Demand Filed: 27.06.1991
IPC:
A61K 38/00 (2006.01) ,C07K 5/107 (2006.01) ,C07K 14/70 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
5
Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04
containing only normal peptide links
10
Tetrapeptides
107
the side chain of the first amino acid containing carbocyclic rings, e.g. Phe, Tyr
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
14
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435
from animals; from humans
665
derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
70
Enkephalins
Applicants:
G.D. SEARLE & CO. [US/US]; P.O. Box 5110 Chicago, IL 60680, US
Inventors:
HANSEN, Donald, Willis, Jr.; US
MOSBERG, Henry, I.; US
Agent:
WILLIAMS, Roger, A. ; G.D. Searle & Co. Corporate Patent Department P.O. Box 5110 Chicago, IL 60680-9889, US
Priority Data:
451,49915.12.1989US
Title (EN) SUBSTITUTED CYCLIC PENICILLANIC ACID TETRAPEPTIDES
(FR) TETRAPEPTIDES CYCLIQUES SUBSTITUES D'ACIDE PENICILLANIQUE
Abstract:
(EN) The present invention provides novel compounds, compositions, methods of their use and methods of their manufacture. The compounds of this invention are cyclic tetrapeptide tyrosyl substituted dipenicillanic acid opioid agonists that are selective for the delta-receptor. The compounds of the invention act as neurotransmitters or neuromodulators in the central nervous system central pain-suppressant system, to induce analgesia. The present invention provides new cyclic peptide derivatives which show improved potency and bioavailability as analgesic agents by central routes of administration.
(FR) Nouveaux composés, nouvelles compositions, leurs modes d'emploi et leurs procédés de fabrication. Les composés de l'invention sont des agonistes opioides d'acide dipénicillanique à substitution tyrocyle de tétrapeptides cycliques, lesdits agonistes présentant une sélectivité à l'égard du récepteur delta. Les composés de l'invention ont un rôle de neurotransmetteurs ou de neuromodulateurs dans le système central de suppression de la douleur du système nerveux central, afin d'induire une analgésie. L'invention fournit de nouveaux dérivés de peptides cycliques présentant une puissance et une biodisponibilité améliorées en tant qu'agents analgésiques par les voies centrales d'administration.
Designated States: CA, JP, KR
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
Publication Language: English (EN)
Filing Language: English (EN)