# US 8,785,648 B1 · PKC-epsilon inhibitors

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- Number: US 8,785,648 B1
- Document ID: US8785648B1
- Status: Granted
- Kind: B1
- Application number: 13/340,406
- Filed: 2011-12-29
- Granted: 2014-07-22
- Earliest claimed: 2010-08-10
- Assignees: The Regents of the University of California
- Applicants: Robert Owen Messing; Michael A. Pleiss
- Inventors: Robert Owen Messing; Michael A. Pleiss
- Web page: https://patentgrep.com/patent/US8785648B1

## CPC

- C07D 409/12: linked by a chain containing hetero atoms as chain links
- C07D 213/75: Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- C07D 405/14: containing three or more hetero rings
- C07D 409/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- C12N 9/99: Enzyme inactivation by chemical treatment
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula I or II or a stereoisomer, tautomer, racemic, metabolite, pro- or pre-drug, salt, hydrate, or solvate thereof, wherein Ar, Cy, R1, R3, p and n have the meaning defined in the claims. In particular, the present invention relates to more specifically AGC kinases inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.

## Claims

### Claim 1

A compound of Formula I or a salt thereof;
wherein
Ar is pyridyl;
Cy is selected from the group consisting of cyclohexyl, adamantyl, and piperidinyl;
n is 0 or 1;
R1 is selected from:
and
with the proviso that when n is 0, then R1 is
A is oxygen or sulfur;
R5, R6, and R7 are each independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, or heterocylyl, where the cycloalkyl or heterocyclyl group may be fused to one phenyl or pyridyl group, and where each of said alkyl, cycloalkyl, heterocyclyl, phenyl or pyridyl groups is optionally substituted by halo, cycloalkyl, phenyl, or pyridyl.

### Claim 2 (depends on 1)

The compound of claim 1, represented by Formula Ia, Ib, or Ic:
wherein
Ar is pyridyl;
Cy is selected from the group consisting of cyclohexyl, adamantyl, and piperidinyl;
A is oxygen or sulfur; and
R5, R6, and R7 are each independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, or heterocylyl, where the cycloalkyl or heterocyclyl group may be fused to one phenyl or pyridyl group, and where each of said alkyl, cycloalkyl, heterocyclyl, phenyl or pyridyl groups is optionally substituted by halo, cycloalkyl, phenyl, or pyridyl.

### Claim 3 (depends on 2)

The compound of claim 2, represented by Formula IIIa, IIIb or IIIc:
wherein Ar, A, and R7 are as defined therein;
or a salt thereof.

### Claim 4 (depends on 1)

The compound of claim 1,
wherein Cy is selected from the group consisting of adamantyl and piperidinyl;
or a salt thereof.

### Claim 5

A compound is selected from Table 1:
TABLE 1
Compound
or a salt thereof.

### Claim 6

A compound selected from Table 2:
TABLE 2
Compound
or a salt thereof.

### Claim 7

A compound selected from Table 3:
TABLE 3
Compound
or salt thereof.

### Claim 8 (depends on 1)

A pharmaceutical or a veterinary composition comprising a compound of claim 1.

### Claim 9 (depends on 8)

A pharmaceutical or veterinary composition according to claim 8 further comprising at least one carrier, excipient or diluent acceptable for pharmaceutical and/or veterinary purposes.