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US 8,263,621 B2Granted
Tartrate derivatives for use as coagulation factor IXa inhibitors
AssigneeSanofi
InventorsHenning Steinhagen, Markus Follmann, Jochen Goerlitzer, Herman Schreuder
Life of this patent
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Abstract
The invention relates to the compounds of formula I having antithrombotic activity which especially inhibits blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.
Claims3
A compound of formula I
- or a stereoisomeric form of a compound of formula I, or a mixture of such forms in any ratio, or a physiologically tolerable salt of a compound of formula I
- where
- R1 is carbamimidoylphenyl, aminomethylphenyl or Het-Z, where Het is selected from the group consisting of benzimidazolyl and isoquinolinyl, and in which Z is amino or amidino,
- R2 and R4 are in each case a hydrogen atom,
- R3 is
- 1) phenyl, in which phenyl is unsubstituted or mono- or disubstituted by T,
- 2)-phenyl-Q-phenyl, in which the two phenyl radicals in each case independently of one another are unsubstituted or mono- or disubstituted by T or
- 3) phenyl-Q-Het-2, in which Het-2 is selected from the group consisting of quinolinyl, quinoxalinyl, furanyl, indolyl, isoquinolinyl, isothiazolyl, isoxazolyl, oxadiazolyl, piperidinyl, pyrazolyl, pyridazinyl, pyrimidinyl, pyridyl, pyrimidinyl, pyrrolyl, thiadiazolyl, thiazolyl, thienyl, thienopyrrolyl or thienothiophenyl, and in which phenyl and Het-2 in each case independently of one another are unsubstituted or mono- or disubstituted by T,
- Q is a covalent bond, —CH2—, —N(CH3)— or —O—,
- T is
- 1) F, Cl or Br,
- 2) —(C1-C4)-alkyl, in which alkyl are unsubstituted or independently mono- or disubstituted by —CF3 or —N—C(O)—CH3, or
- 3) —NO2, and
- R5 and R6 are in each case a hydrogen atom.
11 more elements
Dependencies are inferred from the claim text.