Crystalline form
Patent Information
- Application Number
- HK62026126348
- Authority / Receiving Office
- HK · HK
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2023-03-13
- Filing Date
- 2026-07-20
- Publication Date
- 2026-10-09
- Estimated Expiration
- 2044-03-11
Smart Images
Figure 00000036_0000 
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Abstract
Description
Abstract This specification relates to the crystalline form of (3S)-2-[(5-amino-6-fluoro-1H-pyrrolo[3,2-b]pyridin-2-yl)methyl]-1'-but-2-ynyl-6-fluoro-spiro[isoindoline-3,3'-pyrrolidine]-1,2'-dione, its compositions and uses.
Claims
CLAIMS1. A crystalline form which is a co-crystal of (3S)-2-[(5-amino-6-fluoro-1 H-pyrrolo[3,2- b]pyridin-2-yl)methyl]-1'-but-2-ynyl-6-fluoro-spiro[isoindoline-3,3'-pyrrolidine]-1 ,2'-dione:Compound (I), and adipic acid in a 2:1 ratio (Compound (I) Form A).
2. The crystalline form according to claim 1, wherein the crystalline form has an X-ray powder diffraction pattern containing specific peaks at (±0.2) 8.9, 19.1, 19.7 and 22.9 degrees 2-theta when measured using CuKa radiation.
3. The crystalline form according to claim 1 or 2, wherein the crystalline form has an X-ray powder diffraction pattern containing specific peaks at (±0.2) 8.9, 14.5, 16.9, 17.4, 19.1, 19.7, 21.2, 22.9, 23.7 and 25.8 degrees 2-theta when measured using CuKa radiation.
4. The crystalline form according to any one of claims 1 to 3, wherein the crystalline form has an X-ray powder diffraction substantially as shown in Figure 1 when measured using CuKa radiation.
5. The crystalline form according to any one of claims 1 to 4, wherein the crystalline form has a DSC thermogram substantially as shown in Figure 3.
6. The crystalline form according to claim 1, wherein the crystalline form is a co-crystal of (3S)-2-[(5-amino-6-fluoro-1H-pyrrolo[3,2-b]pyridin-2-yl)methyl]-T-but-2-ynyl-6-fluoro- spiro[isoindoline-3,3'-pyrrolidine]-1 ,2'-dione:Compound (I), and adipic acid in a 2: 1 ratio (Compound (I) Form A), having at least one of the following: a) an X-ray powder diffraction pattern containing specific peaks at (±0.2) 8.9, 19.1 , 19.7 and 22.9 degrees 2-theta when measured using CuKa radiation; b) an X-ray powder diffraction pattern containing specific peaks at (±0.2) 8.9, 14.5, 16.9, 17.4, 19.1 , 19.7, 21.2, 22.9, 23.7 and 25.8 degrees 2-theta when measured using CuKa radiation; c) an X-ray powder diffraction pattern substantially as shown in Figure 1 ; d) a DSC thermogram with an onset melting at 216.6°C plus or minus 5°C and a peak at 217.7°C plus or minus 5°C; e) a DSC thermogram and optionally a TGA thermogram substantially as shown in Figure 3.
7. A pharmaceutical composition comprising the crystalline form according to any one of claims 1 to 6 and at least one pharmaceutically acceptable excipient.
8. The crystalline form according to any one of claims 1 to 6 or the pharmaceutical composition according to claim 7, for use as a medicament, for example in the prophylaxis or treatment of a disorder mediated by PRMT5.
9. Use of the crystalline form according to any one of claims 1 to 6 or the pharmaceutical composition according to claim 7, in the manufacture of a medicament, for example for the prophylaxis or treatment of a disorder mediated by PRMT5.
10. A method of prevention or treatment, for example preventing or treating a disorder mediated by PRMT5, which comprises administering the crystalline form according to any one of claims 1 to 6, or the pharmaceutical composition according to claim 7.
11. The crystalline form for use, pharmaceutical composition for use, use or method according to any one of claims 8 to 10, wherein the disorder is cancer.
12. The crystalline form for use, pharmaceutical composition for use, use or method according to claim 11 , wherein the cancer is a MTAP deleted cancer.
13. The crystalline form for use, pharmaceutical composition for use, use or method according to claim 11 or 12, wherein the cancer is selected from gastric, pancreatic, colorectal, uterine, bile duct, stomach, bladder, cervical, testicular germ cell, lung (e.g. non-small cell lung cancer), multiple myeloma, lymphoma (e.g. diffuse large B cell lymphoma or Hodgkin’s lymphoma), rhabdomyosarcoma and cutaneous squamous cell carcinoma.