Boronate ester compounds and pharmaceutical compositions thereof

Patent metadata

Field	Value
Publication number	US-10604538-B2
Application number	US-201916570065-A
Country	US
Kind code	B2
Filing date	Sep 13, 2019
Priority date	Jun 17, 2008
Publication date	Mar 31, 2020
Grant date	Mar 31, 2020

Abstract

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

First claim

What is claimed is:

1. A compound of formula (II):

or a pharmaceutically acceptable salt thereof, wherein:
A is 0;
P is R c —C(O)—; R c is R D ; R D is 2-pyrazinyl;
R a is isobutyl;
R a1 is CH 2 -phenyl;
each R b1 and R b2 independently is hydrogen;
each R b3 and R b4 independently is —(CH 2 ) p —CO 2 H; p is 0 or 1; and
n is 0 or 1.

Assignees

• Millennium Pharm Inc
• Millenium Pharmaceuticals Inc

Inventors

• Elliott Eric L
• Ferdous Abu J
• Kaufman Michael J
• Komar-Lay Sonja A
• Mazaik Debra L
• Mccubbin Quentin J
• Nguyen Phuong M
• Palaniappan Vaithianathan
• Skwierczynski Raymond D
• Truong Nobel T
• Varga Csanad M
• Zawaneh Peter N

Classifications

• A61P11/06

  Antiasthmatics · CPC title

• A61K31/69 Primary

  Boron compounds · CPC title

• A61K31/198

  Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00) · CPC title

• A61K9/19

  lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)} · CPC title

• C07F5/025

  Boronic and borinic acid compounds · CPC title