# US 11,439,633 B2 · Tetrahydroquinoline derivatives as P2X7 receptor antagonists

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- Number: US 11,439,633 B2
- Document ID: US11439633B2
- Status: Granted
- Kind: B2
- Application number: 17/112,097
- Filed: 2020-12-04
- Published: 2021-03-25
- Granted: 2022-09-13
- Earliest claimed: 2017-03-13
- Assignees: RaQualia Pharma Inc.; Asahi Kasei Pharma Corporation
- Applicants: RaQualia Pharma Inc.; Asahi Kasei Pharma Corporation
- Inventors: Yoshimasa Arano; Kazuki Toyoshima; Toshihiko Sone; Koki Matsubara
- Web page: https://patentgrep.com/patent/US11439633B2

## CPC

- A61K 31/47: Quinolines; Isoquinolines
- A61P 13/12: of the kidneys
- A61P 9/06: Antiarrhythmics
- A61P 19/00: Drugs for skeletal disorders
- A61P 25/00: Drugs for disorders of the nervous system
- 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 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 215/06: having only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to the ring nitrogen atom
- C07D 215/20: Oxygen atoms
- C07D 215/48: Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D 221/04: Ortho- or peri-condensed ring systems
- C07D 401/06: linked by a carbon chain containing only aliphatic carbon atoms
- 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 417/12: linked by a chain containing hetero atoms as chain links
- C07D 417/14: containing three or more hetero rings
- C07D 471/10: Spiro-condensed systems
- C07D 491/08: Bridged systems
- C07D 491/107: with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D 498/10: Spiro-condensed systems
- C07F 7/1804: {Compounds having Si-O-C linkages (Si-O-acyl linkages C07F7/1896)}
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)

## Abstract

The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.

## Claims

### Claim 1

A compound represented by the following formula (L-a) or a pharmaceutically acceptable salt thereof:
wherein:
R3 is independently selected from the group consisting of:
(1) hydrogen, (2) halogen, (3) C1-6 alkyl and (4) —O—C1-6 alkyl;
p is 0, 1, 2 or 3;
when p is 2 or 3, each R3 is the same or different;
R16 is selected from the group consisting of:
(1) CN and (2) —CO2R18;
R17 is selected from the group consisting of:
(1) fluoro and (2) hydroxyl; or,
R16 may form ═O with R17;
R18 is selected from the group consisting of:
(1) hydrogen and (2) C1-6 alkyl.

### Claim 2

A compound represented by the following formula (L-b) or a pharmaceutically acceptable salt thereof:
wherein:
R3 is independently selected from the group consisting of:
(1) hydrogen, (2) halogen, (3) C1-6 alkyl and (4) —O—C1-6 alkyl;
p is 0, 1, 2 or 3;
when p is 2 or 3, each R3 is the same or different;
R4 is selected from the group consisting of:
(1) hydrogen, (2) halogen and (3) hydroxyl.