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US 6,440,937 B1Granted
Dipeptide benzamidine as a kininogenase inhibitor
AssigneeAbbott Laboratories
InventorsDorit Baucke, Udo Lange, Helmut Mack, Thomas Pfeiffer, Werner Seitz, Thomas Zierke, Hans Wolfgang Höffken, Wilfried Hornberger
Life of this patent
Estimating the term…
Abstract
Compounds of the formula I where R, R1, R2, R3, R4, R5 and R6, and l, m and n have the meanings stated in the description, and their preparation are described. The novel compounds are suitable for controlling diseases.
Claims16
A compound of the formula I
- wherein
- l is 0 or 1,
- m is 0, 1 or 2,
- n is 0, 1 or 2,
- R is hydrogen or C1-4-alkyl,
- R1 is HOOC—, C1-6-alkyl-OOC, benzyl-OOC or hydroxyl,
- R2 is hydrogen, C1-4-alkyl or R1—(CH2)m,
- R3 is hydrogen or C1-4-alkyl which is unsubstituted or substituted by hydroxyl or COOH,
- R4 is hydrogen, C1-4-alkyl, HOOC—C1-4-alkylene,
- R5 is C1-8-alkyl, cycloalkyl-(CR8R9)r (r=0 or 1, R8, R9=hydrogen, cycloalkyl or C1-4-alkyl), wherein up to four CH2 groups of the cycloalkyl radical may be replaced, independently from one another, by CR10R11 (R10=hydrogen or C1-4-alkyl, R11=C1-4-alkyl) and/or the CH group in the cycloalkyl radical which is bonded to CR8R9 may be replaced by CR12 (R12=C1-4-alkyl), and/or one or two C—C single bond(s) of the cycloalkyl ring may be replaced by a C═C double bond,
- R6 is hydrogen, C1-4-alkyl, or
- R4 and R5 are together CH2—CH2—CH(R7), (R7=hydrogen, phenyl or cyclohexyl), or
- R2 and R5 are together CH2—CH2 or CH2—CH2—CH2, in which one hydrogen atom may be replaced by C1-4-alkyl, phenyl or cycloalkyl, or a salt thereof.
10 more elements
A compound of the formula II
- wherein
- l is 0 or 1,
- m is 0, 1 or 2,
- n is 0, 1 or 2,
- R is hydrogen or C1-4-alkyl,
- R1 is HOOC—, C1-6-alkyl-OOC, benzyl-OOC or hydroxyl,
- R2 is hydrogen, C1-4-alkyl or R1—(CH2)m,
- R3 is hydrogen or C1-4-alkyl which is unsubstituted or substituted by hydroxyl or COOH,
- R4 is hydrogen, C1-4-alkyl-, HOOC—C1-4-alkylene-,
- R5 is C1-8-alkyl, cycloalkyl-(CR8R9)r (r=0 or 1, R8, R9=hydrogen, cycloalkyl or C1-4-alkyl), wherein up to four CH2 groups of the cycloalkyl radical may be replaced, independently from one another, by CR10R11 (R10=hydrogen or C1-4-alkyl, R12=C1-4-alkyl) and/or the CH group in the cycloalkyl radical which is bonded to CR8R9 may be replaced by CR12 (R12=C1-4-alkyl), and/or one or two C—C single bond(s) of the cycloalkyl ring may be replaced by a C═C double bond, R6 is hydrogen, C1-4-alkyl, or
- R4 and R5 are together CH2—CH2—CH(R7), (R7=hydrogen, phenyl or cyclohexyl), or
- R2 and R5 are together CH2—CH2 or CH2—CH2—CH2—, in which one hydrogen atom may be replaced by C1-4-alkyl, phenyl or cycloalkyl.
9 more elements
A compound of the formula III
- wherein
- l is 0 or 1,
- R is hydrogen or C1-4-alkyl, and
- Y is an N protective group, an N-terminally protected or unprotected amino acid or hydrogen.
1 more element
Dependencies are inferred from the claim text.