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US 6,207,672 B1Granted
Cyclic and heterocyclic N-substituted α-iminohydroxamic and carboxyclic acids
AssigneeAventis Pharma Deutschland GmbH
InventorsWerner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Eckart Bartnik, Klaus-Ulrich Weithmann
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Abstract
Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.
Claims12
A compound of formula I
- or an optionally stereoisomeric form of the compound of the formula I, or a physiologically tolerable salt of the foregoing, where:
- R1 is
- a radical of formula II
- and
- Q as part of the compound of formula I is
- structural moiety X
- R2 is
- (1) phenyl or
- (2) phenyl which is mono-, di-, or trisubstituted by
- 2.1 hydroxyl,
- 2.2 —O—R10, where R10 is
- 2.2.1 (C1-C6)-alkyl,
- 2.2.2 (C3-C6)-cycloalkyl,
- 2.2.3 benzyl, or
- 2.2.4 phenyl,
- 2.3 —COOH,
- 2.4 (C1-C6)-alkyl,
- 2.5 (C3-C6)-cycloalkyl-O-(C1-C4)-alkyl,
- 2.6 halogen,
- 2.7 —CN,
- 2.8 —CF3,
- 2.9 —O—C(O)—R10, where R10 is as defined above,
- 2.10 —O—C(O)-phenyl, mono- or disubstituted by R3,
- 2.11 —C(O)—O—R10, where R10 is as defined above,
- 2.12 —C(O)—NR11R12, where
- R11 and R12 may be identical or different and each is
- 2.12.1 a hydrogen atom,
- 2.12.2 (C1-C4)-alkyl,
- 2.12.3 benzyl, or
- 2.13 —NR13R14, where
- R13 is a hydrogen atom or (C1-C4)-alkyl, and R14 is
- 2.14.1 (C1-C4)-alkyl,
- 2.14.2 benzyl,
- 2.14.3 —C(O)—R10, or
- 2.14.4 —C(O)—O—R10, and R10 is as defined above;
- R6, R7, and R8 are identical or different, and each is
- (1) a hydrogen atom, or
- (2) has the meaning of R2 under items 2.1 to 2.12, and
- n is zero, 1, or 2, and m is zero, 1, or 2, such that the sum of n and m is 1, 2, or 3;
- X is
- (1) a covalent bond,
- (2) —O—,
- (3) —S—,
- (4) —S(O)—,
- (5) —S(O)2—,
- (6) —C(O)—, or
- (7) —C(OH)—;
- Y is
- (1) —O— or
- (2) —S—;
- A is HO—NH—C(O)— or HO—C(O)—;
- and
- B is
- (1) —(CH2)q—, where q is zero, 1, 2, 3 or 4, or
- (2) —CH═CH—.
52 more elements
Dependencies are inferred from the claim text.