Anti-tumor effect potentiator using novel biphenyl compound
US-11510915-B2 · Nov 29, 2022 · US
Salt of terphenyl compound
US12419858B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-12419858-B2 |
| Application number | US-202017775795-A |
| Country | US |
| Kind code | B2 |
| Filing date | Nov 13, 2020 |
| Priority date | Nov 13, 2019 |
| Publication date | Sep 23, 2025 |
| Grant date | Sep 23, 2025 |
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Abstract
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A benzoic acid salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile is provided. A sorbic acid salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile is also provided.
First claim
Opening claim text (preview).
The invention claimed is: 1. A crystalline form of a benzoic acid salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, wherein the crystalline form is characterized by a powder X-ray diffraction pattern comprising diffraction peaks at 20 values of 15.3°±0.2°, 16.2°±0.2°, 17.8°±0.2°, 21.4°±0.2°, and 25.5°±0.2°. 2. A crystalline form of a benzoic acid salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, wherein the crystalline form is characterized by a differential scanning calorimetry (DSC) curve with an endothermic peak in the range from 188° C. to 198° C. 3. The crystalline form according to claim 1 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern of FIG. 1 . 4. A crystalline form of a sorbic acid salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, wherein the crystalline form is characterized by a powder X-ray diffraction pattern comprising diffraction peaks at 20 values of 5.5°±0.2°, 10.9°±0.2°, 16.2°±0.2°, 17.2°±0.2°, 20.3°±0.2°, and 24.4°±0.2°. 5. A crystalline form of a sorbic acid salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, wherein the crystalline form is characterized by a differential scanning calorimetry (DSC) curve with an endothermic peak in the range from 142° C. to 152° C. 6. The crystalline form according to claim 4 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern of FIG. 13 . 7. A pharmaceutical composition comprising the crystalline form according to claim 1 . 8. The pharmaceutical composition according to claim 7 , which is an orally administered composition. 9. A method of treating a malignant tumor in a patient in need thereof, the method comprising administering an effective amount of the crystalline form according to claim 1 to the patient. 10. A pharmaceutical composition comprising the crystalline form according to claim 4 . 11. A method of treating a malignant tumor in a patient in need thereof, the method comprising administering an effective amount of the crystalline form according to claim 4 to the patient.
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Classifications
- C07D207/14Primary
Nitrogen atoms not forming part of a nitro radical · CPC title
Crystalline forms, e.g. polymorphs · CPC title
Retinoic acids {; Salts thereof} · CPC title
specific for leukemia · CPC title
Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00 · CPC title
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- What does patent US12419858B2 cover?
- A benzoic acid salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile is provided. A sorbic acid salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile is also provided.
- Who is the assignee on this patent?
- Taiho Pharmaceutical Co Ltd
- What technology area does this patent fall under?
- Primary CPC classification C07D207/14. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Sep 23 2025 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).