848352-99-8Relevant articles and documents
SUBSTITUTED AMINOBUTYRIC DERIVATIVES AS NEPRILYSIN INHIBITORS
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Page/Page column 179, (2010/12/26)
The present invention provides a compound of formula (I') or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
A facile and efficient multi-gram synthesis of N-protected 5-(guanidinocarbonyl)-1H-pyrrole-2-carboxylic acids
Schmuck, Carsten,Bickert, Volker,Merschky, Michael,Geiger, Lars,Rupprecht, Daniel,Dudaczek, Juergen,Wich, Peter,Rehm, Thomas,Machon, Uwe
, p. 324 - 329 (2008/09/18)
The synthesis of two versatile building blocks for supramolecular anion binding motifs, 5-(N-Boc-guanidinocarbonyl)-1H-pyrrole-2-carboxylic acid (1) and 5-(N-Cbz-guanidinocarbonyl)-1H-pyrrole-2-carboxylic acid (2) is reported. Using these building blocks, a guanidiniocarbonyl-pyrrole anion binding site can easily be introduced into more complex molecules by using standard amide coupling conditions. Both syntheses can be performed on a multi-gram scale. The products are obtained in pure form and can be stored as solids without decomposition. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
Pyrrole-derivatives as factor Xa inhibitors
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Page/Page column 48, (2008/06/13)
The present invention relates to compounds of the formulae I and Ia, wherein R0 ; R1 ; R2 ; R3 ; R4; R22, Q; V, G and M have the meanings indicated in the claims. The compounds of the formulae I and Ia are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formulae I and Ia, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.