Crystals of azabicyclic compound
AssigneeTaiho Pharmaceutical Co., Ltd.
InventorTakao Uno
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Abstract
Provided are crystals of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide which are stable and show excellent oral absorbability. The crystals are Form II crystals of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide showing an X-ray powder diffraction spectrum having at least three characteristic diffraction peaks at angles (2θ±0.2°) selected from the group consisting of 7.7°, 8.0°, 11.1°, 12.5°, 12.9°, 15.2°, 15.8°, 17.2°, 19.0°, 22.5°, 26.1°, and 27.4°.
Claims8
A method of treating a tumor, comprising administering, to a subject in need thereof, an effective amount of a Form II crystal of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3.4-b]pyridin-1-yl} benzamide showing an X-ray powder diffraction spectrum having at least three characteristic diffraction peaks at angles (2θ±0.2°) selected from the group consisting of 7.7°, 8.0°, 11.1°, 12.5°, 12.9°, 15.2°, 15.8°, 17.2°, 19.0°, 22.5°, 26.1°, and 27.4°.
A method of treating a tumor which is at least one cancer selected from the group consisting of head and neck carcinoma, gastrointestinal carcinoma including esophageal carcinoma, gastric cancer, gastrointestinal stromal tumor, duodenal carcinoma, hepatocarcinoma, biliary carcinoma such as gallbladder-bile duct cancer, pancreatic cancer, small intestine carcinoma, and large bowel cancer such as colorectal carcinoma, colon cancer, and rectal cancer, lung carcinoma, breast carcinoma, ovarian cancer, uterine carcinoma such as cervical cancer and endometrial cancer, kidney carcinoma, bladder cancer, prostate cancer, urothelial carcinoma, bone and soft tissue sarcoma, blood cancer such as B-cell lymphoma, chronic lymphocytic leukemia, peripheral T-cell lymphoma, myelodysplastic syndrome, acute myeloid leukemia and acute lymphocytic leukemia, multiple myeloma, skin cancer, and mesothelioma, comprising administering, to a subject in need thereof, an effective amount of a Form 11 crystal of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide showing an X-ray powder diffraction spectrum having at least three characteristic diffraction peaks at angles (2θ±0.2°) selected from the group consisting of 7.7°, 8.0°, 11.1°, 12.5°, 12.9°, 15.2°, 15.8°, 17.2°, 19.0°, 22.5°, 26.1°, and 27.4°.
Dependencies are inferred from the claim text.