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1. (WO1991008759) ALKYL SUBSTITUTED CYCLIC PENICILLANIC ACID PENTAPAPTIDES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/008759 International Application No.: PCT/US1990/007444
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 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
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:
HAMMOND, Donna, L.; US
HANSEN, Donald, W.; US
MOSBERG, Henry, I.; US
Agent:
WILLIAMS, Roger, A.; Corporate Patent Department G.D. Searle & Co. P.O. Box 5110 Chicago, IL 60680-9889, US
Priority Data:
451,29015.12.1989US
497,83322.03.1990US
Title (EN) ALKYL SUBSTITUTED CYCLIC PENICILLANIC ACID PENTAPAPTIDES
(FR) PENTAPEPTIDES D'ACIDE PENICILLANIQUE CYCLIQUES SUBSTITUES PAR UN ALKYLE
Abstract:
(EN) The invention relates to novel compounds of general formula (I) and pharmaceutically acceptable salts thereof, wherein X is H, a halogen, nitro, lower alkyl or lower alkyl substituted by halogen or nitro, aralkyl or alkaryl or substituted aralkyl or alkaryl of from one to ten carbon atoms: R1, R2, R3 and R4 are independently H and furthermore, R1, R2, R3, R4, R6 and R7 are independently alkyl of from one to ten carbon atoms; R5 is amino, hydroxy, alkoxy of from one to ten carbon atoms, alkyl amino or dialkylamino of from one to ten carbon atoms; and R8 is independently H, alkyl of from one to ten carbon atoms, carboxyl, alkoxy carbonyl of from one to ten carbon atoms, amino carbonyl, alkylamino carbonyl and dialkylamino carbonyl of from one to ten carbon atoms, or any of these R8 constituents being aryl substituted thereon. The compounds and pharmaceutical compositions thereof are useful in the analgesic methods of the invention.
(FR) L'invention se rapporte à de nouveaux composés de la formule générale (I) et à des sels pharmaceutiquement acceptables, où X est H, un halogène, nitro, alkyle inférieur ou alkyle inférieur substitué par halogène ou nitro, aralkyle ou alcaryle, ou aralkyle ou alcaryle substitués comportant de un à dix atomes de carbone: R1, R2, R3 et R4 sont indépendamment H et, de plus, R1, R2, R3, R4, R6 et R7 sont indépendamment alkyle comportant de un à dix atomes de carbone; R5 est amino, hydroxy, alcoxy comportant de un à dix atomes de carbone, alkylamino ou dialkylamino comportant de un à dix atomes de carbone; et R8 est indépendamment H, alkyle comportant de un à dix atomes de carbone, carboxyle, alcoxycarbonyle comportant de un à dix atomes de carbone, aminocarbonyle, alkylaminocarbonyle et dialkylaminocarbonyle comportant de un à dix atomes de carbone, ou bien n'importe lequel de ces constituants de R8 étant aryle substitué. Les composés et leurs compositions pharmaceutiques sont utiles dans les procédés analgésiques objets de l'invention.
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)