# US 5,708,002 A · Macrocyclic immunomodulators

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- Number: US 5,708,002 A
- Document ID: US5708002A
- Status: Granted
- Kind: A
- Application number: 08/734,793
- Filed: 1996-10-23
- Granted: 1998-01-13
- Earliest claimed: 1991-09-05
- Assignees: Abbott Laboratories
- Inventors: Jay R. Luly; Megumi Kawai; Yat Sun Or; Paul Wiedeman; Rolf Wagner
- Web page: https://patentgrep.com/patent/US5708002A

## CPC

- C07D 498/18: Bridged systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Immunomodulatory macrocyclic compounds having the formula ##STR1## and pharmaceutically acceptable salts, esters, amides and prodrugs thereof, wherein X is selected from one of the formulae ##STR2## as well as pharmaceutical compositions containing the same.

## Claims

### Claim 1

A compound of the formula: ##STR18## wherein X is ##STR19## and (a) R=ethyl; R'=R2=R3=H; n=1; R.sup.1' =--OCH.sub.3 ; and R.sup.1 =CH.sub.3 C(O)S-- (S Configuration); or
(b) R=ethyl; R'=R2=R3=H; n=1; R.sup.1' =--OCH.sub.3 ; and R.sup.1 =C.sub.6 H.sub.5 S--; or
(c) R=ethyl; R'=R2=R3=H; n=1; R.sup.1' =--OCH.sub.3 ; and R.sup.1 =benzylthio; or
(d) R=ethyl; R'=R2=R3=H; n=1; R.sup.1' =--OCH.sub.3 ; and R.sup.1 =--SH;
or a pharmaceutically acceptable salt, ester, amide or prodrug thereof.

### Claim 2 (depends on 1)

The compound according to claim 1 wherein R=ethyl; R'=R2=R3=H; n=1; R.sup.1' =--OCH.sub.3 ; and R.sup.1 =--SH.

### Claim 3

A compound of the formula: ##STR20## wherein X is ##STR21## and R=ethyl; R'=R2=R3=H; n=1; R.sup.1' =--OCH.sub.3 ; R.sup.1 =N-tetrazole (S-Configuration); or a pharmaceutically acceptable salt, ester, amide or prodrug thereof.

### Claim 4 (depends on 1)

A method for providing immunomodulatory treatment comprising administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1.

### Claim 5 (depends on 3)

A method for providing immunomodulatory treatment comprising administering to a patient in need thereof a therapeutically effective amount of a compound of claim 3.

### Claim 6 (depends on 1)

A pharmaceutical composition for immunomodulatory treatment comprising a therapeutically effective amount of a compound of claim 1 in combination with a pharmaceutically acceptable carrier.

### Claim 7 (depends on 3)

A pharmaceutical composition for immunomodulatory treatment comprising a therapeutically effective amount of a compound of claim 3 in combination with a pharmaceutically acceptable carrier.