# US 12,595,270 B2 · Benzo nitrogen-containing heteroaromatic ring derivative and use thereof in medicine

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

- Number: US 12,595,270 B2
- Document ID: US12595270B2
- Status: Granted
- Kind: B2
- Application number: 19/352,045
- Filed: 2025-10-07
- Published: 2026-02-05
- Granted: 2026-04-07
- Earliest claimed: 2021-08-18
- Assignees: Xizang Haisco Pharmaceutical Co., Ltd.
- Applicants: Xizang Haisco Pharmaceutical Co., Ltd.
- Inventors: Chen Zhang; Yuting Liao; Guozhi Zhu; Dachao Tang; Yan Yu; Pingming Tang; Xinfan Cheng; Yao Li; Jia Ni; Pangke Yan
- Web page: https://patentgrep.com/patent/US12595270B2

## CPC

- A61P 13/12: of the kidneys
- C07D 498/10: Spiro-condensed systems
- A61K 31/407: condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
- A61K 31/438: The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
- A61K 31/454: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
- A61K 31/4545: containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/5386: spiro-condensed or forming part of bridged ring systems
- C07D 401/06: linked by a carbon chain containing only aliphatic carbon atoms
- C07D 401/14: containing three or more hetero rings
- C07D 403/06: linked by a carbon chain containing only aliphatic carbon atoms
- C07D 403/14: containing three or more hetero rings
- C07D 405/14: 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 495/10: Spiro-condensed systems
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)

## Abstract

Provided are a compound as shown in general formula (I), or a stereoisomer, deuterate, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, an intermediate thereof, a preparation method therefor, and the use thereof in the preparation of a drug for treating a disease associated with the activity or expression quantity of complement factor B.

## Claims

### Claim 1

A compound or a stereoisomer, deuterate, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, wherein the compound is selected from a compound of general formula (Id),
n is 1; X1 and X2 are CR3;
R3 is H; each R6 is H;
one R7 is H, another R7 is selected from cyclopropyl, cyclobutyl, cyclopentyl, wherein the cyclopropyl, cyclobutyl, cyclopentyl is optionally further substituted with 0 to 4 substituents selected from H, D, halogen, C1-4 alkyl;
R1 is selected from methoxy, ethoxy, isopropoxy, wherein the methoxy, ethoxy, isopropoxy is substituted with 1 to 4 substituents selected from D, halogen;
R2 is selected from methyl, ethyl, wherein the methyl, ethyl is optionally further substituted with 0 to 4 substituents selected from H, D, F, Cl, Br, I;
R4 is phenyl, the phenyl is optionally further substituted with 0 to 4 R5;
R5 is independently selected from halogen, OH, cyano, —C(═O)R4e, C1-4 alkyl, C1-4 alkoxy;
R4e is OH.

### Claim 2 (depends on 1)

The compound or the stereoisomer, deuterate, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof according to claim 1, wherein
each R4 is independently selected from
each R5 is —COOH;
is selected from
R1 is independently selected from —OCD3, —OCH2F, —OCHF2, —OCF3; each R2 is methyl, ethyl, CD3, CHD2, or CH2D;
is selected from
the fragments which are connected to R4 at the upper part.

### Claim 3 (depends on 1)

The compound or the stereoisomer, deuterate, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof according to claim 1, wherein the compound is selected from the compound of general formula (Id-5),
is selected from
R1 is selected from —OCD3;
R2 is selected from —CH3 or —CD3;
and n is selected from 1, 2 or 3.

### Claim 4 (depends on 1)

The compound or the stereoisomer, deuterate, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof according to claim 1, wherein the compound is selected from one of the structures shown in following Table

### Claim 5 (depends on 1)

A pharmaceutical composition, comprising the compound or the stereoisomer, deuterate, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof according to claim 1, and a pharmaceutically acceptable carrier.

### Claim 6 (depends on 5)

The pharmaceutical composition according to claim 5, wherein the pharmaceutical composition comprises 1-600 mg of the compound or the stereoisomer, deuterate, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, and a pharmaceutically acceptable excipient.

### Claim 7 (depends on 1)

A method for inhibiting Factor B (FB) activity, comprising administering to the mammal a therapeutically effective amount of the compound or the stereoisomer, deuterate, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof according to claim 1.

### Claim 8 (depends on 7)

The method of claim 7, wherein the therapeutically effective amount is 1-600 mg.