Crystal form of nitrogen-containing spiro compound, preparation method thereof and use thereof

Novel crystal forms of nitrogen-containing spirocyclic compounds address stability and bioavailability issues, enhancing therapeutic efficacy through improved stability and bioavailability.

HK40134682APending Publication Date: 2026-07-10WUHAN LL SCI & TECH DEV CO LTD
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Patent Information

Authority / Receiving Office
HK · HK
Patent Type
Applications
Current Assignee / Owner
WUHAN LL SCI & TECH DEV CO LTD
Filing Date
2026-04-16
Publication Date
2026-07-10

AI Technical Summary

Technical Problem

Existing nitrogen-containing spirocyclic compounds suffer from poor stability, low in vivo exposure, and inadequate oral bioavailability, limiting their therapeutic efficacy.

Method used

Development of novel crystal forms of nitrogen-containing spirocyclic compounds with specific X-ray diffraction peaks, enhancing stability and bioavailability.

Benefits of technology

The new crystal forms exhibit improved stability and high in vivo exposure, effectively inhibiting complement factor D and demonstrating high oral bioavailability.

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Abstract

The invention discloses a nitrogen-containing spiro compound crystal form and a preparation method and application thereof. The invention provides a crystal form I of a nitrogen-containing spiro compound as shown in a formula A. The crystal form I of the nitrogen-containing spiro compound is radiated by Cu-K alpha, and an X-ray powder diffraction pattern expressed by a 2 theta angle has diffraction peaks at 5.67 + / -0.20 degrees, 11.37 + / -0.20 degrees, 16.69 + / -0.20 degrees, 17.32 + / -0.20 degrees and 19.73 + / -0.20 degrees. The invention provides a crystal form II of a nitrogen-containing spiro compound as shown in a formula A. The crystal form II is radiated by Cu-K alpha, and an X-ray powder diffraction pattern expressed by a 20 angle has diffraction peaks at the positions of 11.32 + / -0.20 degrees, 11.70 + / -0.20 degrees, 11.93 + / -0.20 degrees, 18.03 + / -0.20 degrees, 18.81 + / -0.20 degrees and 19.17 + / -0.20 degrees. The crystal form of the nitrogen-containing spiro compound has good stability and complement factor D inhibitory activity, has a good inhibitory effect on rabbit red blood cell hemolysis, and has high in-vivo exposure and high oral bioavailability.
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Description

(19) State Intellectual Property Office (12) Invention Patent Application (10) Application Publication Number (43) Application Publication Date (21) Application Number 202480018892.X (22) Application Date 2024.03.28 (66) Domestic Priority Data 202310317527.6 2023.03.28 CN 202410227541.1 2024.02.29 CN (85) PCT International Application Entering National Phase Date 2025.09.12 (86) PCT International Application Application Data PCT / CN2024 / 084387 2024.03.28 (87) PCT International Application Publication Data WO2024 / 199350 ZH 2024.10.03 (71) Applicant Wuhan Langlai Technology Development Co., Ltd. Address 430075 No. 666 Gaoxin Avenue, East Lake High-tech Development Zone, Wuhan, Hubei Province, C2-2, R&D Area, Wuhan National Bio-industry Base (72) Inventors: Hu Qinquan, Lou Jun, Wang Liang, Zhang Yihan (74) Patent Agency: Shanghai Bixing Law Firm, 31283 Patent Attorneys: Gao Xiaoli, Xue Qi (51) Int.Cl. C07D 221 / 20 (2006.01) C07D 471 / 10 (2006.01) C07D 209 / 54 (2006.01) C07C 69 / 734 (2006.01) A61P 7 / 00 (2006.01) A61P 9 / 00 (2006.01) A61P 37 / 02 (2006.01) A61P 25 / 28 (2006.01) A61P 11 / 00(2006.01) A61P 13 / 00(2006.01) A61P 13 / 12(2006.01) A61P 27 / 02(2006.01) A61P 29 / 00(2006.01) A61P 19 / 02(2006.01) A61P 17 / 06(2006.01) A61P 21 / 04(2006.01) A61P 31 / 14(2006.01) A61K 31 / 438(2006.01) A61K 31 / 395(2006.01) (54) Title of Invention: A crystal form of a nitrogen-containing spirocyclic compound, its preparation method and its application (57) Abstract: This invention discloses a crystal form of a nitrogen-containing spirocyclic compound, its preparation method and its application.This invention provides a crystal form I of a nitrogen-containing spirocyclic compound as shown in Formula A, whose X-ray powder diffraction pattern, expressed in 2θ angles using Cu-Kα radiation, shows diffraction peaks at 5.67±0.20°, 11.37±0.20°, 16.69±0.20°, 17.32±0.20°, and 19.73±0.20°. This invention also provides a crystal form II of a nitrogen-containing spirocyclic compound as shown in Formula A, whose X-ray powder diffraction pattern, expressed in 2θ angles using Cu-Kα radiation, shows diffraction peaks at 11.32±0.20°, 11.70±0.20°, 11.93±0.20°, 18.03±0.20°, 18.81±0.20°, and 19.17±0.20°. The nitrogen-containing spirocyclic compound of the present invention exhibits good stability and complement factor D inhibitory activity, effectively inhibits rabbit erythrocyte hemolysis, and has high in vivo exposure and high oral bioavailability. CN 120897909 A 2025.11.04 CN 1 20 89 79 09 A.