# US 9,040,545 B2 · Heterocyclyl pyrazolopyrimidine analogues as selective JAK inhibitors

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- Number: US 9,040,545 B2
- Document ID: US9040545B2
- Status: Granted
- Kind: B2
- Application number: 13/816,555
- Filed: 2011-08-12
- Published: 2013-07-25
- Granted: 2015-05-26
- Earliest claimed: 2010-08-20
- Assignees: Cellzome Limited
- Applicants: Kathryn Bell; Nelly Piton; Claudio Dagostin; Cyrille Boussard; Andrew Ratcliffe; Nigel Ramsden
- Inventors: Kathryn Bell; Nelly Piton; Claudio Dagostin; Cyrille Boussard; Andrew Ratcliffe; Nigel Ramsden
- Web page: https://patentgrep.com/patent/US9040545B2

## CPC

- C07D 487/04: Ortho-condensed systems
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- 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
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 491/107: with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D 498/08: Bridged systems
- C07D 519/00: Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

## Claims

### Claim 1

A compound of the structure:

### Claim 2

A compound of the structure:
or a pharmaceutically acceptable salt thereof.

### Claim 3

A pharmaceutically acceptable salt of a compound of the structure:

### Claim 4 (depends on 1)

A pharmaceutical composition comprising the compound of claim 1, or a pharmaceutically acceptable salt thereof, together with at least one pharmaceutically acceptable carrier.

### Claim 5 (depends on 4)

The pharmaceutical composition according to claim 4 in unit dosage form.