# US 12,600,698 B2 · Kinase inhibitors

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- Number: US 12,600,698 B2
- Document ID: US12600698B2
- Status: Granted
- Kind: B2
- Application number: 17/898,274
- Filed: 2022-08-29
- Published: 2023-06-08
- Granted: 2026-04-14
- Earliest claimed: 2021-01-12
- Assignees: Vidya Therapeutics, Inc.
- Applicants: Vidya Therapeutics, Inc.
- Inventors: Craig A. Coburn; Daniel J. Buzard; Dange Vijay Kumar
- Web page: https://patentgrep.com/patent/US12600698B2

## CPC

- C07D 209/30: with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D 209/08: with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
- C07D 209/42: Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07B 2200/07: Optical isomers
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

Disclosed herein, are protein kinase inhibitors, in particular Bruton tyrosine kinase (BTK) inhibitors, pharmaceutical compositions comprising them, processes for preparing them and uses of the inhibitors to treat or prevent diseases, disorders and conditions associated with kinase function. In particular, the present invention relates to CNS penetrable BTK inhibitors.

## Claims

### Claim 1

A compound having the structure of Formula 1-C-(1S,3R) or Formula 1-C-(1R,3R):
or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, racemate or isotope thereof, wherein:
RB is H or Me;
RC is —CH—CH2 or —C≡C—CH3;
RA is
wherein
RA1 is —F or —Cl; and
RA2 is H or F.

### Claim 2 (depends on 1)

A compound of claim 1, having the structure of Formula 1-C-(1S,3R):
or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, racemate or isotope thereof.

### Claim 3 (depends on 1)

A compound of claim 1, having the structure of Formula 1-C-(1R,3R):
or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, racemate or isotope thereof.

### Claim 4 (depends on 1)

A compound of claim 1, wherein RB is H.

### Claim 5 (depends on 1)

A compound of claim 1, wherein RB is Me.

### Claim 6 (depends on 1)

A compound of claim 1, wherein RC is —CH═CH2.

### Claim 7 (depends on 1)

A compound of claim 1, wherein RC is —C≡C—CH3.

### Claim 8 (depends on 1)

A compound of claim 1, wherein RA1 is —F.

### Claim 9 (depends on 1)

A compound of claim 1, wherein RA1 is —Cl.

### Claim 10 (depends on 1)

A compound of claim 1, wherein RA2 is —H.

### Claim 11 (depends on 1)

A compound of claim 1, wherein RA2 is —F.

### Claim 12 (depends on 1)

A compound of claim 1, wherein
RA1 is —Cl;
RA2 is —H; and
RC is —C≡C—CH3.

### Claim 13 (depends on 1)

A compound of claim 1, wherein
RA1 is —Cl;
RA2 is —H or —F;
RB is —H or -Me; and
RC is —C≡C—CH3.

### Claim 14 (depends on 1)

A pharmaceutically acceptable salt of a compound of claim 1.

### Claim 15 (depends on 1)

A pharmaceutical composition comprising the compound of claim 1, or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, racemate, or isotope thereof, and at least one pharmaceutically acceptable excipient.

### Claim 16 (depends on 1)

The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt or solvate thereof.

### Claim 17 (depends on 1)

The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt or solvate thereof.

### Claim 18 (depends on 1)

The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt or solvate thereof.

### Claim 19 (depends on 1)

The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt or solvate thereof.

### Claim 20 (depends on 1)

The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt or solvate thereof.

### Claim 21 (depends on 1)

The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt or solvate thereof.