# US 12,595,253 B2 · Benzamides of pyrazolylamino-pyrimidinyl derivatives, and compositions and methods thereof

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- Number: US 12,595,253 B2
- Document ID: US12595253B2
- Status: Granted
- Kind: B2
- Application number: 17/684,164
- Filed: 2022-03-01
- Published: 2022-09-22
- Granted: 2026-04-07
- Earliest claimed: 2022-03-01
- Assignees: Lynk Pharmaceuticals Co. Ltd.
- Applicants: Lynk Pharmaceuticals Co. Ltd.
- Inventors: Zhaokui Wan; Michael Lawrence Vazquez; Xiaodong Li
- Web page: https://patentgrep.com/patent/US12595253B2

## CPC

- C07D 403/12: linked by a chain containing hetero atoms as chain links
- A61P 25/02: for peripheral neuropathies
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- C07D 401/14: containing three or more hetero rings
- C07D 403/14: containing three or more hetero rings
- C07D 405/14: containing three or more hetero rings
- C07D 451/04: with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
- C07D 471/08: Bridged systems
- C07D 493/08: Bridged systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention provides novel benzamides of pyrazolyl-amino-pyrimidinyl derivatives of Formula (I) as selective and potent JAK inhibitors for treating various diseases and disorders. The invention also provides pharmaceutical composition of these compounds and methods of their preparation and use thereof.

## Claims

### Claim 1

A compound having the structural formula (I):
wherein
X is N;
Z1 is CH;
Z2 is N;
R1 is Cl;
R2 is a C1-C6 alkyl, cycloalkyl or heterocycloalkyl group optionally comprising one or more heteroatoms selected from N, O, S and P, wherein the alkyl, cycloalkyl or heterocycloalkyl group is optionally substituted with one or more of halogen, OR′, NRR′, CN, CONRR′, NRCOR′ and C1-C6 alkyl, which is in turn optionally substituted with F, OR′ or NRR′;
R3 is H;
R4′ is H;
R4 is a CHR″—R5, wherein R″ is H or a C1-C6 alkyl and R5 is CN, CF3 or OR′; and
each R and R′ is independently hydrogen or a C1-C12 unsubstituted or substituted alkyl group,
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The compound of claim 1, wherein R2 is a C1-C6 alkyl.