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1. (WO1991005555) N-ACYL PEPTIDE METALLOENDOPEPTIDASE INHIBITORS AND METHODS OF USING SAME
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/005555 International Application No.: PCT/US1990/005904
Publication Date: 02.05.1991 International Filing Date: 15.10.1990
Chapter 2 Demand Filed: 10.05.1991
IPC:
A61K 38/00 (2006.01) ,C07C 233/51 (2006.01) ,C07D 207/16 (2006.01) ,C07K 5/06 (2006.01) ,C07K 5/062 (2006.01) ,C07K 5/065 (2006.01) ,C07K 5/078 (2006.01) ,C07K 5/08 (2006.01) ,C07K 5/083 (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
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
233
Carboxylic acid amides
01
having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
45
having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
46
with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
51
having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04
having no double bonds between ring members or between ring members and non-ring members
10
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
16
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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
06
Dipeptides
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
06
Dipeptides
062
the side chain of the first amino acid being acyclic, e.g. Gly, Ala
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
06
Dipeptides
065
the side chain of the first amino acid containing carbocyclic rings, e.g. Phe, Tyr
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
06
Dipeptides
078
the first amino acid being heterocyclic, e.g. Pro, His, Trp
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
08
Tripeptides
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
08
Tripeptides
083
the side chain of the first amino acid being acyclic, e.g. Gly, Ala
Applicants:
THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC. [US/US]; 10280 North Torrey Pines Road LaJolla, CA 92037, US (AllExceptUS)
WAYNE STATE UNIVERSITY [US/US]; 5980 Cass Avenue Detroit, MI 48202, US (AllExceptUS)
GHOSH, Soumitra, Shankar [IN/US]; US (UsOnly)
MOBASHERY, Shahriar [US/US]; US (UsOnly)
Inventors:
GHOSH, Soumitra, Shankar; US
MOBASHERY, Shahriar; US
Agent:
WATT, Phillip, H.; Fitch, Even, Tabin & Flannery Room 900 135 South LaSalle Street Chicago, IL 60603 , US
Priority Data:
421,20313.10.1989US
421,20413.10.1989US
Title (EN) N-ACYL PEPTIDE METALLOENDOPEPTIDASE INHIBITORS AND METHODS OF USING SAME
(FR) INHIBITEURS DE METALLOENDOPEPTIDASES PEPTIDIQUES DE N-ACYLE ET LEURS MODES D'EMPLOI
Abstract:
(EN) Inhibitors of the Zn+2-metalloendopeptidases, enkephalinase, angiotensin-converting enzyme, and collagenase, intermediates for synthesizing the inhibitors, and methods of making and using the inhibitors, are provided. The enkephalinase inhibitors of the invention are useful as analgesics or antihypertensives. The angiotensin-converting enzyme inhibitors of the invention are useful as anti-hypertensives. The collagenase inhibitors of the invention are useful in treating diseases, such as corneal ulceration, periodontal disease, and arthritis, which involve undesirable collagen degradation. The inhibitors of the invention are peptide or peptide ester derivatives of the intermediates of the invention, whichare N-acyl derivatives of amino acids of the formula X10-NH-CHR9-(CO2H), wherein X10 is selected from the group consisting of N=C-CHR20-(C=O)- and X21(CR22R23)(CHR24)(C=O)-, wherein R20 is hydrogen or alkyl of 1 to 3 carbon atoms, R22, R23 and R24 are each independently hydrogen or alkyl of 1 to 3 carbon atoms, and X21 is fluoro, chloro or bromo; and R9 is benzyl, alkyl of 1-5 carbon atoms, or hydrogen.
(FR) Inhibiteurs de Zn+2-métalloendopeptidases, d'encéphalinase, d'enzyme de conversion d'angiotensine, et de collagénase, intermédiaires de synthèses des inhibiteurs, et procédés de fabrication et d'emploi desdits inhibiteurs. Les inhibiteurs d'encéphalinase de l'invention sont utiles en tant qu'analgésiques ou anti-hypertensifs. Les inhibiteurs d'enzyme de conversion d'angiotensine de l'invention sont utiles en tant qu'anti-hypertensifs. Les inhibiteurs de collagénase de l'invention sont utiles dans le traitement de maladies telles que l'ulcération de la cornée, la paradontolyse, et l'arthrite, lesquelles impliquent une dégradation indésirable du collagène. Les inhibiteurs de l'invention sont des dérivés de peptides ou d'esters de peptides des intermédiaires de l'invention, lesquels sont des dérivés de N-acyle d'acides aminés de la formule X10-NH-CHR9-(CO2H), dans laquelle X10 est choisi dans le groupe composé de N=C-CHR20-(C=O)- et X21(CR22R23)(CHR24)(C=O)-, dans lesquels R20 représente hydrogène ou alkyle contenant 1 à 3 atomes de carbone, R22, R23 et R24 représentent chacun indépendamment hydrogène ou alkyle contenant 1 à 3 atomes de carbone et X21 représente fluoro, chloro ou bromo; et R9 représente benzyle, alkyle contenant 1 à 5 atomes de carbone, ou hydrogène.
Designated States: CA, JP, NO, US
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
Publication Language: English (EN)
Filing Language: English (EN)