# US 7,465,745 B2 · Cathepsin S inhibitors

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- Number: US 7,465,745 B2
- Document ID: US7465745B2
- Status: Granted
- Kind: B2
- Application number: 11/141,153
- Filed: 2005-05-31
- Published: 2005-10-06
- Granted: 2008-12-16
- Earliest claimed: 2003-03-13
- Assignees: Boehringer Ingelheim Pharmaceuticals, Inc.
- Inventors: Eugene R. Hickey; Wiemen Liu; Sanxing Sun; Yancey David Ward; Erick Richard Roush Young
- Web page: https://patentgrep.com/patent/US7465745B2

## CPC

- C07D 211/66: having a hetero atom as the second substituent in position 4
- C07D 413/12: linked by a chain containing hetero atoms as chain links
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

This invention relates to peptidyl compounds of the formulas (I) and (II) active as cathepsin S, a cysteine protease, inhibitors. The compounds are selective, reversible inhibitors of the cathepsin S are therefore useful in the treatment of autoimmune and other diseases. The invention also relates to processes for preparing such compounds and pharmaceutical compositions comprising them.

## Claims

### Claim 1

A compound of the formula (I) or (II):
wherein X in each case is chosen from
R1 is:
or the pharmaceutically acceptable salts thereof.

### Claim 2 (depends on 1)

The compound according to claim 1 wherein:
in the formula (I)
X is

### Claim 3 (depends on 1, 2)

The compound according to any one of claims 1-2 wherein the compound of the formula (I) is the (S) enantiomer which possesses a natural amino acid configuration at the indicated chiral carbon below

### Claim 4 (depends on 1)

A method of treating a disease or condition chosen from:
rheumatoid arthritis, systemic lupus erythematosus, Crohn's disease, ulcerative colitis, Guillain-Barre syndrome, psoriasis, Grave's disease, myasthenia gravis, seleroderma, glomerulonephritis, dermatitis including contact and atopic dermatitis, insulin-dependent diabetes mellitus, endometriosis, asthma and atherosclerosis;
comprising administering to a patient a pharmaceutically effective amount of a compound according to claim 1.