# US 7,745,441 B1 · Urokinase inhibitors

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- Number: US 7,745,441 B1
- Document ID: US7745441B1
- Status: Granted
- Kind: B1
- Application number: 09/787,647
- Filed: 1998-09-18
- Granted: 2010-06-29
- Earliest claimed: 1998-09-18
- Assignees: Wilex AG
- Inventors: Peter Wikström; Helmut Vieweg; Jörg Stürzebecher
- Web page: https://patentgrep.com/patent/US7745441B1

## CPC

- C07D 295/185: from aliphatic carboxylic acids
- C07C 311/19: to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
- C07D 211/16: with acylated ring nitrogen atom
- C07D 211/60: Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D 211/62: attached in position 4
- C07D 295/205: Radicals derived from carbonic acid
- C07D 409/12: linked by a chain containing hetero atoms as chain links
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

New urokinase inhibitors having a triisopropylphenylsulfonyl residue as an Nα-substituent for 3-amidinophenylalanine are provided. The introduction of the triisopropylphenylsulfonyl residue greatly increases the affinity of the compounds to urokinase and, thereby, increases their inhibitory activity against urokinase. These urokinase inhibitors are useful in determining the role of urokinase and urokinase receptor in various diseases, particularly in tumor propagation and metastasis. Methods of treating tumors and a pharmaceutical composition are also provided.

## Claims

### Claim 1

Purified urokinase inhibitors of general formula
which are present as compounds in L-form, and wherein R1 represents
(a) a group of formula
wherein either p=1 and r=2 and R2 is benzyloxycarbonyl, benzylaminocarbonyl or 2-thienylhydrazinocarbonyl, or p=2 and r=1 and R2 is ethoxycarbonyl, 2-propyloxycarbonyl, 2-propylaminocarbonyl, methylaminocarbonyl or methyl; or
(b) a group of formula
wherein R3 is selected from the group consisting of methoxycarbonyl, ethoxycarbonyl, and benzyloxycarbonyl, and
wherein the compounds occur in the form of their free bases or as salts with inorganic acids, or as salts with organic acids.

### Claim 2 (depends on 1)

A composition comprising the urokinase inhibitor according to claim 1 and a pharmaceutical additive.

### Claim 3 (depends on 2)

The composition according to claim 2, wherein said pharmaceutical additive is suitable for administration orally, subcutaneously and/or intravenously.

### Claim 4 (depends on 2)

The composition according to claim 2, wherein said composition is in the form of tablets, dragées, capsules, suppositories, solutions or transdermal systems.

### Claim 5 (depends on 1)

The purified urokinase inhibitors according to claim 1, wherein said compounds occur in the form of their hydrochlorides.

### Claim 6 (depends on 1)

The purified urokinase inhibitors according to claim 1, wherein R1 is
a group of formula:
and R3 is ethoxycarbonyl.