# US 5,703,086 A · Compounds and methods of use to derivatize neighboring lysine residues in proteins under physiological conditions

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- Number: US 5,703,086 A
- Document ID: US5703086A
- Status: Granted
- Kind: A
- Application number: 08/471,797
- Filed: 1995-06-06
- Granted: 1997-12-30
- Earliest claimed: 1995-01-06
- Assignees: The Picower Institute for Medical Research
- Inventors: Michael I. Bukrinsky; Anthony Cerami; Peter Ulrich
- Web page: https://patentgrep.com/patent/US5703086A

## CPC

- C07D 239/48: Two nitrogen atoms
- C07C 279/16: having nitrogen atoms of guanidine groups bound to carbon atoms of rings other than six-membered aromatic rings
- C07C 279/26: X and Y being nitrogen atoms, i.e. biguanides
- C07D 251/48: Two nitrogen atoms
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The present invention concerns compounds that block the movement of viral particles through the nuclear membrane and thereby prevent the productive infection of terminally differentiated cells by virus the life cycle of which includes such an importation step. The invention encompasses methods of use of such compounds. The use of the compounds to detect certain specific protein structures which are present in nuclear localization sequences is also taught.

## Claims

### Claim 1

A pharmaceutical composition comprising a compound according to the formula: ##STR4## wherein A.dbd.CH.sub.3 or CH.sub.2 CH.sub.3 and ##STR5## wherein X.dbd.NH.sub.2, CH.sub.3 or CH.sub.2 CH.sub.3 ; X'.dbd.CH.sub.3 or CH.sub.2 CH.sub.3 ; Y.dbd.NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2 ; and Z.dbd.H, CH.sub.3 or CH.sub.2 CH.sub.3 ; or ##STR6## wherein Y' and Z', independently,.dbd.H, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2 or N.sup.+ (CH.sub.3).sub.3 or a salt thereof; a therapeutically effective amount of AZT; and a pharmaceutically acceptable carrier.

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1 comprising compound according to the formula: ##STR7## or a salt thereof, wherein A.dbd.CH.sub.3, X.dbd.NH.sub.2, CH.sub.3 or CH.sub.2 CH.sub.3 ; X'.dbd.CH.sub.3 or CH.sub.2 CH.sub.3 ; Y.dbd.NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2 ; and Z.dbd.H, CH.sub.3, or CH.sub.2 CH.sub.3.

### Claim 3 (depends on 2)

The pharmaceutical composition of claim 2 wherein Z.dbd.H, Y.dbd.NH.sub.2, X and X'.dbd.CH.sub.3 and salts thereof.

### Claim 4 (depends on 3)

A method of treatment of HIV-1 infection comprising administering to an HIV-1-infected subject the pharmaceutical composition of claim 3.

### Claim 5 (depends on 1)

A method of treatment of HIV-1 infection comprising administering to an HIV-1-infected subject the pharmaceutical composition of claim 1.

### Claim 6 (depends on 2)

A method of treatment of HIV-1 infection comprising administering to an HIV-1-infected subject the pharmaceutical composition of claim 2.