Substituted Prolinamides for Factor Xa Inhibition
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current pharmacological agents lack effective antithrombotic and factor Xa-inhibiting properties, particularly in treating venous and arterial thrombotic diseases, and have limitations in inhibiting related serine proteases.
Innovation Solution
Development of new substituted amides with specific bicyclic ring systems that exhibit antithrombotic activity and factor Xa-inhibiting properties, including the preparation of physiologically acceptable salts for use in pharmaceutical compositions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current pharmacological agents are used, then existing treatment options are available, but effective antithrombotic and factor Xa-inhibiting properties are insufficient
Solution Approach 1:
The patent modifies the chemical structure of amide compounds by changing parameters such as substituting hydrogen atoms with fluorine atoms, introducing bicyclic ring systems, and varying side chain lengths and compositions. These structural parameter changes result in compounds with enhanced antithrombotic activity and improved factor Xa-inhibiting properties, directly resolving the contradiction between reliability of antithrombotic effect and versatility of inhibiting properties.
Solution Approach 2:
The invention creates composite molecular structures by combining bicyclic ring systems with amide core structures and various side chains. This composite approach allows the molecules to simultaneously achieve multiple pharmacological effects (antithrombotic activity and factor Xa inhibition) while maintaining structural integrity, thereby improving both reliability and adaptability.
2Reliability
If existing pharmacological agents are used, then treatment is provided, but inhibition of related serine proteases is limited
Solution Approach 1:
The patent introduces specific local structural features at key positions in the molecule, such as fluorine substitution at specific carbon atoms and particular configurations of the bicyclic ring system. These local quality modifications enhance the molecule's ability to inhibit serine proteases while maintaining factor Xa-inhibiting activity, thereby reducing harmful effects from insufficient protease inhibition.
Solution Approach 2:
The invention creates analogues and derivatives of existing pharmacological agents by copying the basic amide structure while introducing modifications such as bicyclic ring systems and fluorine substitutions. These copied structures retain the essential pharmacological activity while improving serine protease inhibition capabilities.
Data Source
AI summary
The present invention relates to new substituted prolinamides of general formula (I) wherein D, Y, A, B, R3, R4 and R5 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.