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US 6,649,613 B1Granted
Diacylhydrazine derivatives
AssigneeMerck Patent GmbH
InventorsGünter Hölzemann, Simon Goodman, Horst Kessler, Christoph Gibson, Gabór Sulyok
Life of this patent
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Abstract
Diacylhydrazine derivatives of general formula (I) wherein X, Y, Z, R1, 2 and R3 are as defined herein, and their physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be used to combat thromboses, myocardial infarcts, coronary cardiac diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections, and restenosis following angioplasty or during pathological processes that are maintained or propagated by angiogenesis.
Claims35
A compound formula I
- in which
- X is H2N—C(═NH)—NH—, H3C—C(═NH)—NH or Het1—NH—,
- Y is
- Z is is N—R2 or CH—R2,
- R1, R2 are each independently of one another H or A,
- R3 is H, Ar or Het,
- R4 is H, A, Ar, OH, OA, OAr, arylalkyl, Hal, CN, NO2, CF3 or OCF3
- A is alkyl having 1 to 6 carbon atoms,
- Ar is phenyl which is unsubstituted or mono-, di- or trisubstituted by A, OH, OA, CF3, OCF3, CN, NO2 or Hal and which may be substituted by a phenyl which is mono-, di- or trisubstituted by A, OH, OA, CF3, OCF3, CN, NO2 or Hal such that an unsubstituted or substituted biphenyl is formed, or is naphthyl which is unsubstituted or mono-, di- or unsubstituted by A, OH, OA, CF3, OCF3, CN, NO2 or Hal,
- Hal is F, Cl, Br or I,
- Het is a saturated, partially or fully unsaturated mono- or bicyclic heterocyclic radical having 5 to 10 ring members, where 1 or 2 nitrogen and/or 1 or 2 sulfur or oxygen atoms may be present and where the heterocyclic radical may be mono or disubstituted by CN, Hal, OH, OA, CF3, A, NO or OCF3,
- Het1 is a 5- or 6-membered aromatic heterocycle having 1 to 4 nitrogen atoms which may be unsubstituted or mono- or disubstituted by Hal, A, OA, Ar, OAr, arylakyl, CN NO2, CF3 or OCF3,
- n is 2, 3, 4, 5 or 6,
- m, o are 0, 1 or 2;
- or
- a physiologically acceptable salts or solvates.
13 more elements
Dependencies are inferred from the claim text.