255374-80-2

Upstream product

• 6553-96-4 2,4,6-triisopropylphenylsulfonyl chloride 
• 57213-48-6 3-cyano-(D,L)-phenylalanine 
• 28188-41-2 m-(bromomethyl)benzonitrile 

Downstream Products

• 255374-81-3 N-TIPPS-3-cyano-(L)-phenylalanine 4-ethoxycarbonylpiperazide 
• 797040-05-2 3-[3-(N-hydroxycarbamimidoyl)-phenyl]-2-(2,4,6-triisopropyl-benzenesulfonylamino)-propionic acid 
• 300579-37-7 3-[(S)-3-[4-(3-Amino-propionyl)-piperazin-1-yl]-3-oxo-2-(2,4,6-triisopropyl-benzenesulfonylamino)-propyl]-benzamidine 
• 797040-25-6 3-[(S)-3-[4-(4-Amino-butyryl)-piperazin-1-yl]-3-oxo-2-(2,4,6-triisopropyl-benzenesulfonylamino)-propyl]-benzamidine 
• 797040-12-1 1-[(S)-3-(3-Carbamimidoyl-phenyl)-2-(2,4,6-triisopropyl-benzenesulfonylamino)-propionyl]-piperidine-4-carboxylic acid (2-amino-ethyl)-amide 
• 901771-96-8 3-[(S)-3-[4-(3-Amino-propionyl)-[1,4]diazepan-1-yl]-3-oxo-2-(2,4,6-triisopropyl-benzenesulfonylamino)-propyl]-benzamidine 
• 797040-69-8 3-[(S)-3-Oxo-3-[4-(piperazine-1-carbonyl)-piperidin-1-yl]-2-(2,4,6-triisopropyl-benzenesulfonylamino)-propyl]-benzamidine 
• 797040-45-0 3-[(S)-3-Oxo-3-[4-(piperidine-4-carbonyl)-piperazin-1-yl]-2-(2,4,6-triisopropyl-benzenesulfonylamino)-propyl]-benzamidine 

Relevant academic research and scientific papers

N-SULPHONYLATED AMINO ACID DERIVATIVES, METHOD FOR THE PRODUCTION AND USE THEREOF

The invention relates to N-sulphonylated amino acid derivatives wherein an aryl radical is bound to an amino acid via the sulphonyl groups in the N-terminal and a radical is bound in the C-terminal via the carbonyl group. Said radical contains at least one imino group and at least one other basic group representing an optionally modified amino-, amidino- or guanidino group. The invention also relates to a method for the production of said compounds and to the use thereof, especially as inhibitors of matriptase.

HYDROXYAMIDINE AND HYDROXYGUANIDINE COMPOUNDS AS UROKINASE INHIBITORS

The invention relates to novel compounds for the inhibition of the urokinase plasminogen activator (uPA) with high bioavailability and which can also be administered orally, and to the use thereof as therapeutic active ingredients for the treatment of urokinase or/and urokinase receptor associated diseases, such as, for example, tumours and metastization. The invention especially relates to compounds (I) and (II) that contain hydroxyamidine or hydroxyguanidine groups, wherein E represents a group consisting of (a).

Novel urokinase inhibitors

The invention relates to the use of derivatives of 3-amidinophenylalanine as urokinase inhibitors for treating malignant tumors and the formation of metastases.

3-Amidinophenylalanine-based inhibitors of urokinase

Synthesis and anti-uPA activity of a series of Nα-triisopropyl-phenylsulfonyl-protected 3-amidino-phenylalanine amides are described. We have explored SAR around the C-terminal amide part for inhibition of uPA, plasmin and trypsin. Modification of the ami