# US 2014/0194444 A1 · Aminopyrimidines useful as inhibitors of protein kinases

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2014/0194444 A1
- Document ID: US20140194444A1
- Status: Published application
- Kind: A1
- Application number: 14/155,624
- Filed: 2014-01-15
- Published: 2014-07-10
- Earliest claimed: 2007-03-09
- Applicants: Vertex Pharmaceuticals Incorporated
- Inventors: Juan-Miguel Jimenez; Andrew Miller; Jeremy Green; Huai Gao; Gregory Henkel; Michael Liu; Timothy Neuberger
- Web page: https://patentgrep.com/patent/US20140194444A1

## CPC

- C07D 471/04: Ortho-condensed systems
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/10: for osteoporosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/18: for HIV
- A61P 35/00: Antineoplastic agents
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 403/12: linked by a chain containing hetero atoms as chain links
- C07D 405/14: containing three or more hetero rings
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.

## Claims

### Claim 1

A compound of formula I:
or a pharmaceutically acceptable salt thereof, wherein:
Ht is
wherein any substitutable carbon on Ht is independently and optionally substituted with —R10;
Ring D is a 3-10 membered heterocyclyl; where said heterocyclyl contains 1-2 heteroatoms selected from O, N, or S; and wherein the heterocyclyl is independently and optionally substituted with 1-5-R5; Ring D is bonded to the pyrimidine via a carbon atom;
Z1 is N, CH, or CR10;
RX is H, halo, or C1-6alkyl, wherein the alkyl is independently and optionally substituted with 1-5 groups selected from halo, —CN, and —OR;
RY is H, halo, C2-6alkyl, or a 5-6 membered heterocyclyl ring containing 1-2 heteroatoms selected from O, N, or S; wherein said RY is independently and optionally substituted with 1-4 halo, CN, OR, or C2-6alkyl;
each R10 is independently selected from C1-6alkyl, haloC1-6alkyl, halo, OR, C(═O)R, CO2R, COCOR, NO2, CN, S(O)R, SO2R, SR, N(R4)2, CON(R4)2, SO2N(R4)2, OC(═O)R, N(R4)COR, or N(R4)CO2R;
each R4 is independently selected from H, C1-6alkyl, or haloC1-6alkyl;
each R5 is independently selected from halo, haloC1-6alkyl, or C1-6alkyl; and
each R is independently selected from H, C1-6alkyl, or haloC1-6alkyl.

### Claim 2 (depends on 1)

The compound according to claim 1 wherein Ht is

### Claim 3 (depends on 2)

The compound according to claim 2, wherein R10 is halo.

### Claim 4 (depends on 3)

The compound according to claim 3, wherein R10 is fluoro.

### Claim 5

(canceled)

### Claim 6 (depends on 1)

The compound according to claim 1, wherein Z1 is N.

### Claim 7

(canceled)

### Claim 8

(canceled)

### Claim 9

(canceled)

### Claim 10 (depends on 1)

The compound according to claim 1, wherein RX is H.

### Claim 11 (depends on 1)

The compound according to claim 1, wherein RX is methyl.

### Claim 12 (depends on 4)

The compound according to claim 4, wherein the halo is fluoro.

### Claim 13 (depends on 1)

The compound according to claim 1, wherein RY is halo or C1-6 alkyl.

### Claim 14 (depends on 13)

The compound according to claim 13, wherein RY is methyl.

### Claim 15

(canceled)

### Claim 16

(canceled)

### Claim 17 (depends on 1)

The compound according to claim 1, wherein said heterocyclyl is morpholinyl, piperidinyl, or piperazinyl.

### Claim 18

(canceled)

### Claim 19

(canceled)

### Claim 20

(canceled)

### Claim 21

(canceled)

### Claim 22

(canceled)

### Claim 23

(canceled)

### Claim 24 (depends on 1)

The compound according to claim 1, wherein Ring D is a 6-membered heterocyclyl containing one oxygen atom.

### Claim 25

(canceled)

### Claim 26 (depends on 1)

The compound of claim 1 selected from the following:

### Claim 27 (depends on 1, 26)

A composition comprising a compound according to any one of claim 1 or 26, and a pharmaceutically acceptable carrier, adjuvant, or vehicle.

### Claim at position 28

28-46. (canceled)