Deuterated compounds and uses thereof

Patent metadata

Field	Value
Publication number	US-10675367-B2
Application number	US-201816050453-A
Country	US
Kind code	B2
Filing date	Jul 31, 2018
Priority date	May 13, 2014
Publication date	Jun 9, 2020
Grant date	Jun 9, 2020

Abstract

The present invention relates to deuterated and optionally detectably labeled compounds of formula (I) and formula (V):

and salts thereof, wherein R 1 , R 2 , A, and X 10 -X 19 have any of the values defined in the specification. Also included are pharmaceutical compositions comprising such compounds and salts, and methods of using such compounds and salts as imaging agents.

First claim

We claim:

1. A compound selected from:

wherein X is bromine, hydroxy or a toluenesulfonyl group, and salts thereof.

2. A compound according to claim 1 , wherein X is bromine or hydroxy, and salts thereof.

3. A compound according to claim 1 , wherein X is hydroxy, and salts thereof.

4. A compound according to claim 1 , which is

wherein X is bromine or hydroxy, and salts thereof.

5. A compound according to claim 1 , which is

and salts thereof.

6. A method for preparing a compound of formula (III)

wherein R 3 is a group selected from:

the method comprising the 18 F fluorination of a compound of formula (10)

and optionally converting the compound obtained into a salt thereof.

7. A method according to claim 6 , wherein R 3 is

Assignees

• Genentech Inc

Inventors

• Marik Jan
• Lyssikatos Joseph P
• Williams Simon

Classifications

• C07D487/04 Primary

  Ortho-condensed systems · CPC title

• C07B2200/05

  Isotopically modified compounds, e.g. labelled · CPC title

• C07B59/002

  Heterocyclic compounds · CPC title

• A61K51/0459 Primary

  having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine · CPC title

• A61K31/519

  ortho- or peri-condensed with heterocyclic rings · CPC title