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US 6,555,562 B1Granted
Phenylalanine derivatives
AssigneeCelltech R&D Limited
InventorsSarah Catherine Archibald, John Clifford Head, Graham John Warrellow, John Robert Porter
Life of this patent
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Abstract
Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; Ar is an optionally substituted aromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
Claims9
A compound of formula (1b):
- wherein:
- R is a carboxylic acid or a derivative thereof;
- W is —N═;
- —(Alk1)r(L1)s— is a —CON(R4)— group;
- R4 is a hydrogen atom or a straight or branched alkyl group;
- Ra, Rb, R9 and R10, which are the same or ditferent, is each an atom or group —L2(CH2)pL3(Rc))q;
- L2 and L3 is each a covalent bond or a linker atom or group;
- Rc is a hydrogen or halogen atom or a group selected from a straight or branched alkyl, ORd, SRd, NRdRc, —NO2, —CN, —CO2Rd, —N(Rd)CORc, —NR(Rd)CSRc, —SO2NRdRc, —N(Rd)SO2Rc, —N(Rd)CONRdRf, —N(R)CSNRdRf or —N(Rd)SO2NRdRf group;
- Rd, Rc and Rf, which are the same or different, is each a hydrogen atom or an optionally substituted straight or branched alkyl group;
- p is zero or the integer 1;
- q is an integer 1, 2 or 3;
- Ar is an optionally substituted aromatic group;
- and the salts, solvates, hydrates and N-oxides thereof.
10 more elements
A compound which is selected from the group consisting of:
- 2-Carboxybenzoyl-(N′-3,5-dichloroisonicotinoyl)-L-4aminophenylalanine;
- (N-2,6-Dimethoxybenzoyl)-(N′-3,5-dichloroisonicotinoyl)-L-4-aminophenylalanine;
- (N-3-Carboxybenzoyl)-(N′-3,5-dichloroisonicotinoyl)-L-4-aminophenylalanine;
- (N-4-Carboxybenzoyl)-(N′-3,5-dichloroisonicotinoyl)-L-4-aminophenylalanine;
- (N-2-t-Butoxycarbonylbenzoyl)-(N′-3,5-dichloroisonicotinoyl)-L-4-aminophenylalanine;
- (N-3-Cyanobazyl)-(N′-3,5-dichloraisoicotinoyl)-L-4-amiophenylalanine;
- [N-3-(1-H-Tetrazol-5-yl)benzoyl]-(N′-3,5-dichloroisonicotinoyl)-L-4-aminophenylalanine;
- [N-(3-Methoxycarbonylbenzoyl)]-(N′-3,5-dichloroisonicotinoyl)-L-4-aminophenylalanine;
- and the salts, solvates, hydrates and N-oxides thereof.
6 more elements
Dependencies are inferred from the claim text.