Novel compounds inhibiting factor Xa activity

A compound and composition technology, applied in the field of new compounds that inhibit the activity of factor Xa, can solve the problems such as the need to monitor patients, the scope of action of Xa inhibitors and the scope of side effects are not fully investigated, and the dose needs to be adjusted, etc.

Inactive Publication Date: 2007-08-22
莫波化学股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition to the slow onset of action described above, vitamin K antagonists have the drawback of requiring monitoring of the patient and adjustment of the dose...

Method used

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  • Novel compounds inhibiting factor Xa activity
  • Novel compounds inhibiting factor Xa activity
  • Novel compounds inhibiting factor Xa activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094] 0.05M of 2-(3,4,5-trihydroxy-6-hydroxymethyl-tetrahydropyran-2-yloxy)-benzaldehyde in methanol (helicin), 0.05M of 3-amino A solution of benzamidine dihydrochloride in methanol and 0.05 M of 2-isocyano-1-[4-(2-methoxy-phenyl)-piperazin-1-yl]-ethanone in methanol The solution in was reacted at room temperature for 24 hours in a closed vessel. After evaporation of the solvent, the product was subjected to liquid chromatography and mass spectrometry to determine the structure of the final product. The product 2-(3-amidino-phenylamino)-N-{2-[4-(2-methoxy) was purified by liquid chromatography on a reverse phase column using a water / acetonitrile gradient as eluent -Phenyl)-piperazin-1-yl]-2-oxo-ethyl}-2-[2-(3,4,5-trihydroxy-6-hydroxymethyltetrahydropyran-2-yl Oxy)-phenyl]-acetamide.

[0095] C 34 h 42 N 6 o 9 (678.7486)

[0096] ESI-TOF-MS: 679[M+H] +

Embodiment 2

[0098] Analogously to Example 1, and using corresponding suitable starting materials, 2-(3-amidino-phenylamino)-N-{2-[4-(4-methoxy-phenyl)-piperazine is obtained -1-yl]-2-oxo-ethyl}-2-[2-(3,4,5-trihydroxy-6-hydroxymethyltetrahydropyran-2-yloxy)-phenyl] - Acetamide.

[0099] C 34 h 42 N 6 o 9 (678.7486)

[0100] ESI-TOF-MS: 679[M+H] +

Embodiment 3

[0102] Similar to Example 1, and using corresponding suitable starting materials, 2-biphenyl-4-yl 2-(3-amidino-phenylamino)-N-{2-[4-(2-methyl Oxy-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-acetamide.

[0103] C 34 h 36 N 6 o 3 (576.7044)

[0104] ESI-TOF-MS: 577[M+H] +

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Abstract

The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or a pharmaceutically acceptable formulation thereof. Those compounds can be used for inhibiting factor Xa and for the prevention and/or treatment of thromboembolic conditions.

Description

technical field [0001] The present invention relates to novel compounds having an anticoagulant effect (so-called anticoagulants) and their pharmaceutically acceptable salts, solvates and hydrates, pharmaceutical compositions comprising said compounds as active ingredients, preparation of said compounds, salts and Compositions, methods, and uses in the prevention and / or treatment of thromboembolic disorders. The compounds, salts and compositions of the present invention are very potent factor Xa inhibitors. The present invention also relates to prodrugs, optical forms, racemates and diastereomers of said compounds and salts. Background technique [0002] Thromboembolic disorders are the result of an increased propensity for blood to clot in humans, with risk factors such as relatively major surgery, prolonged immobility, broken legs, obesity, dyslipidemia, gram-negative bacterial infection, cancer, and aging . [0003] Venous thrombosis may lead to the formation of edema ...

Claims

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Application Information

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IPC IPC(8): C07C257/18C07C259/18C07D295/16C07D295/18A61K31/495A61K31/165A61P7/02C07D241/04A61K31/496A61P9/10A61P29/00A61P31/04A61P35/00C07D211/32C07D211/52C07D213/38C07D213/74C07D217/06C07D295/185C07D295/24C07D309/12C07D401/12C07D405/12
CPCC07D295/24C07D211/32C07D401/12C07D213/38C07D213/74C07D405/12C07D211/52C07D217/06C07D295/185C07D309/12A61P29/00A61P31/04A61P35/00A61P7/02A61P9/00A61P9/10C07D295/18
Inventor 米夏埃尔·W·卡佩蒂洛·富克斯罗伯特·埃克尔西尔克·沙波特
Owner 莫波化学股份有限公司
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