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1. (WO1992009297) HIV PROTEASE INHIBITORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1992/009297 International Application No.: PCT/US1991/008850
Publication Date: 11.06.1992 International Filing Date: 25.11.1991
Chapter 2 Demand Filed: 29.06.1992
IPC:
A61K 38/00 (2006.01) ,C07C 69/757 (2006.01) ,C07D 223/04 (2006.01) ,C07D 223/06 (2006.01) ,C07D 233/54 (2006.01) ,C07D 243/08 (2006.01) ,C07K 5/06 (2006.01) ,C07K 5/078 (2006.01) ,C07K 5/097 (2006.01) ,C07K 7/02 (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
69
Esters of carboxylic acids; Esters of carbonic or haloformic acids
74
Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
757
having any of the groups OH, O-metal, -CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
223
Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
02
not condensed with other rings
04
with only hydrogen atoms, halogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
223
Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
02
not condensed with other rings
06
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
233
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54
having two double bonds between ring members or between ring members and non-ring members
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
243
Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
06
having the nitrogen atoms in positions 1 and 4
08
not condensed with other rings
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
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
097
the first amino acid being heterocyclic, e.g. Pro, His, Trp, e.g. thyroliberin, melanostatin
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
7
Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
02
Linear peptides containing at least one abnormal peptide link
Applicants:
SMITHKLINE BEECHAM CORPORATION [US/US]; 709 Swedeland Road P.O. Box 1539 King of Prussia, PA 19406, US (AllExceptUS)
CALLAHAN, James, Francis [US/US]; US (UsOnly)
HUFFMAN, William, Francis [US/US]; US (UsOnly)
MOORE, Michael, Lee [US/US]; US (UsOnly)
NEWLANDER, Kenneth, Allen [US/US]; US (UsOnly)
Inventors:
CALLAHAN, James, Francis; US
HUFFMAN, William, Francis; US
MOORE, Michael, Lee; US
NEWLANDER, Kenneth, Allen; US
Agent:
KINZIG, Charles, M. ; SmithKline Beecham Corporation Corporate Patents - U.S. (UW2220) 709 Swedeland Road P.O. Box 1539 King of Prussia, PA 19406, US
Priority Data:
620,97830.11.1990US
Title (EN) HIV PROTEASE INHIBITORS
(FR) INHIBITEURS DE LA PROTEASE DU VIH
Abstract:
(EN) Peptide mimics, having a constrained peptide backbone conformation, are HIV protease inhibitors. A compound of this invention is, for example, 3-Benzyl-5(alaninyl-1-aminoethyl)-2,3,6,7-tetrahydro-N-azepinyl-2-propionyl-valinyl-valinyl methyl ester.
(FR) Des imitateurs de peptides possédant une conformation de squelette de peptide contrainte sont des inhibiteurs de la protéase du VIH. Un composé selon cette invention, est, par exemple, l'ester méthylique de 3-benzyl-5(alaninyl-1-aminoéthyl)-2,3,6,7-tétrahydro-N-azépinyl-2-proprionyl-valinyl-valinyle.
Designated States: AU, CA, JP, KR, 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)
Also published as:
MXPA/a/1991/002311EP0559793US5438118JPH06503568PT99653AU1991091223