Urokinase inhibitors

Details Urokinase inhibitors Urokinase inhibitors

2005-03-01

2005-03-01

Solola, Taofiq (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C514S423000, C544S390000, C548S537000, C562S126000

Reexamination Certificate

active

06861435

ABSTRACT:
The invention relates to the compounds of general formula (I), that are present with respect to R1as racemates as well as L- or D-configured compounds and as E/Z mixtures as well as E or Z isomers and in which the various symbols are defined as in the description and the claims, as well as to the salts thereof, for use as therapeutic agents and for diagnostic purposes. The inventive compounds can be processed to medicaments or to diagnostic agents that are used for the diagnosis, therapy and prevention of urokinase- or urokinase-receptor associated diseases, for example for the treatment of tumors. The compounds are highly efficient in inhibiting growth and/or spread of malign tumors, for example tumor spread of pancreatic cancer, tumor growth of breast cancer and the formation of tumor metastases. The compounds of formula (I) and the salts thereof can be produced by conventional methods.

REFERENCES:
patent: WO 9605189 (1996-02-01), None
patent: WO 0004954 (2000-02-01), None
patent: WO 0017158 (2000-03-01), None
Kim et al.; Rational Design of Selective Thrombin Inhibitors; Bioorganic & Medicinal Chemistry Letters; vol. 7, No. 7; pp 769-774, 1997.
Oh et al.; Discovery of LB30057, A Benzamidrazone-Based Selective Oral Thrombin Inhibitor; Bioorganic & Medicinal Chemistry Letters 8; (1998) pp. 639-634.
Zega et al., Design and Structure-Activity Relationship of Thrombin Inhibitors with an Azaphenylalanine Scaffold; Potency and Selectivity Enhancements Via P2 Optimization; Bioorganic & Medicinal Chemistry 9; (2001), pp. 2745-2756.
Oh et al.; Discovery of LB30057, A Benzamidrazone-Based Selective Oral Thrombin Inhibitor; Bioorganic & Medicinal Chemistry Letters 8; (1998) pp. 631-634.
Sturzebecher et al.; 3-Amidinophenylalanine-based Inhibitors of Urokinase; Bioorganic & Medicinal Chemistry Letters 9; (1999), pp. 3147-3152.
Sturzebecher et al; Synthesis and Structure-Activity Relationships of Potent Thrombin Inhibitors: Piperazides of 3-Amidinophenylalanine; J. Med. Chem; 1997, 40, pp. 3091-3099.
Zega et al; Novel Thrombin Inhibitors with Azaphenylalanine Scaffold; Pharmazie; vol. 56, pp. 683-685; (2001).

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