Search International and National Patent Collections
Some content of this application is unavailable at the moment.
If this situation persist, please contact us atFeedback&Contact
1. (WO1992009564) PEPTIDYL DERIVATIVES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1992/009564 International Application No.: PCT/GB1991/002142
Publication Date: 11.06.1992 International Filing Date: 03.12.1991
IPC:
A61K 38/00 (2006.01) ,C07C 55/02 (2006.01) ,C07C 237/22 (2006.01) ,C07C 259/06 (2006.01) ,C07C 311/46 (2006.01) ,C07D 209/20 (2006.01) ,C07K 5/06 (2006.01) ,C07K 5/072 (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
55
Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
02
Dicarboxylic acids
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
237
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02
having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
22
having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
259
Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
04
without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
06
having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
311
Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
30
Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
45
at least one of the singly-bound nitrogen atoms being part of any of the groups X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
46
Y being a hydrogen or a carbon atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
10
with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
18
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
20
substituted additionally by nitrogen atoms, e.g. tryptophane
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
072
the side chain of the first amino acid containing more carboxyl groups than amino groups, or derivatives thereof, e.g. Asp, Glu, Asn
Applicants:
CELLTECH LIMITED [GB/GB]; 216 Bath Road Slough Berkshire SL1 4EN, GB (AllExceptUS)
PORTER, John, Robert [GB/GB]; GB (UsOnly)
MORPHY, John, Richard [GB/GB]; GB (UsOnly)
MILLICAN, Thomas, Andrew [GB/GB]; GB (UsOnly)
BEELEY, Nigel, Robert, Arnold [GB/GB]; GB (UsOnly)
Inventors:
PORTER, John, Robert; GB
MORPHY, John, Richard; GB
MILLICAN, Thomas, Andrew; GB
BEELEY, Nigel, Robert, Arnold; GB
Agent:
HALLYBONE, Huw, George; Carpmaels & Ransford 43 Bloomsbury Square London WC1A 2RA, GB
Priority Data:
9026251.003.12.1990GB
9110338.213.05.1991GB
9110339.013.05.1991GB
9112888.414.06.1991GB
9112901.514.06.1991GB
9115038.311.07.1991GB
9115039.111.07.1991GB
9115916.023.07.1991GB
Title (EN) PEPTIDYL DERIVATIVES
(FR) DERIVES DE PEPTIDYLE
Abstract:
(EN) Compounds of formula (I) are described wherein R represents a -CONHOH, carboxyl (-CO2H) or esterified carboxyl group; R1 represents an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R3 represents a hydrogen atom or an alkyl group; R4 represents a hydrogen atom or an alkyl group; R5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R7)-groups [where R7 is a hydrogen atom or a C1-6alkyl group]; X represents an amino (-NH2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular have a selective gelatinase action, and may be of use in the treatment of cancer to control the development of tumour metastases.
(FR) Composés répondant à la formule (I), dans laquelle R représente un groupe -CONHOH, carboxyle (-CO2H) ou carboxyle estérifié; R1 représente un groupe alkyle, alcényle, aryle, aralkyle, hétéroaralkyle ou hétéroarylthioalkyle éventuellement substitué; R2 représente un groupe phényléthyle, phénylpropyle ou phénylbutyle éventuellement substitué; R3 représente un atome d'hydrogène ou un groupe alkyle; R4 représente un atome d'hydrogène ou un groupe alkyle; R5 représente un groupe alkyle ou alcényle éventuellement substitué et éventuellement interrompu par un ou plusieurs atomes -O- ou -S- ou groupes -N(R7)- [où R7 représente un atome d'hydrogène ou un groupe alkyle C1-6]; X représente un groupe amino (-NH2), amino substitué, hydroxyle ou hydroxyle substitué; et leurs sels, solvates et hydrates. Ces composés sont des inhibiteurs de métalloprotéinases, présentent notamment une activité gélatinase sélective, et peuvent être utiles au traitement du cancer en luttant contre le développement des métastases tumorales.
Designated States: AU, CA, FI, GB, HU, JP, KR, NO, US
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
FI923494NO19922967CA2073510KR1019927003520AU1991090233