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US 6,645,991 B1Granted
αvβ3 integrin inhibitors
AssigneeMerck Patent GmbH
InventorsAlfred Jonczyk, Oliver Schadt, Simon Goodman
Life of this patent
Estimating the term…
Abstract
The invention describes novel compounds of the formula I which are biologically active as ligands of integrin αvβ3 X—Y—Z—R1—CH2—R2(R4)—CH2—CO—R5 in which X, Y, Z, R1, R2, R4 and R5 are as defined in claim 1, and their physiologically acceptable salts and solvates.
Claims16
A compound of the formula I
- X—Y—Z—R1—CH2—R2(R4)—CH2—CO—R5
- in which
- X is H2N—C(═NH)—, H2N—C(═NH)—NH—, A—C(═NH)—NH—, Het1- or Het1-NH—,
- where the primary amino groups may also be provided with conventional amino-protecting groups,
- Y is
- in which one, two, three or four methylene groups may be replaced by N, O and/or S,
- Z is —O—, —NH—, —NA—, —CH(OH)—, —CH(OA)—, —CHA, —CA2—or —S—,
- R1 is phenylene which is unsubstitued or mono-, di- or trisubstituted by F, Cl, Br, A, OA, OCF3, or CN,
- R2 is N, CH, or CA,
- R3 is H, F, Cl, Br, A, OA or OCF3,
- R4 is phenyl, naphthyl or Het2, each of which is unsubstituted or mono- or polysubstituted by A, aryl, or CF3,
- R5 is OH, OA, NH2, NHA or NA2,
- Het1 is a mono- or bicylic heterocylic radical having from 1 to 4 N atoms, which may be unsubstituted or mono- or disubstituted by NH2,
- Het2 is an aromatic mono- or bicylic heterocylic radical having from 1 to 3 N, O and/or S atoms, which may be unsubstituted or mono- or disubstituted by F, Cl, Br, A, OA, SA, OCF3, —CO—A, CN, COOA, CONH2, CONHA, CONA2, or NO2,
- aryl is phenyl which is unsubstituted or mono-, di-, or trisubstituted by Hal, A or OA,
- A is alkyl having 1-12 carbon atoms,
- n is 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12,
- m, o are each, independently of one another, 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, or 12, or
- a physiologically acceptable salt or solvate thereof.
16 more elements
Dependencies are inferred from the claim text.