Medicament for treating cancer comprising optically active azabicyclo ring derivative
AssigneeSumitomo Pharma Co., Ltd.
InventorsKen EGUCHI, Akinobu WATANABE, Taeko KUSUDA, Mami INOUE, Takafumi SHIMIZU, Mariko MATSUBARA, Takahiro KUWAKI, Matthew HITRON, Hongliang CAI, Bo XU, Emily BROOKS, Curtis ALLRED, Vishnu PEDDAGALI
Life of this patent
Estimating the term…
Abstract
The present invention relates to suitable usage, dosage, and use of an optically active azabicyclo ring derivative useful as a medicament, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising it.
Claims31
-54. (canceled)
A method for treating or preventing a cancer, comprising:
- orally administrating, to a subject in need thereof, a therapeutically effective amount of an active ingredient comprising 5-fluoro-2-[(4-{7-[(1S,3S,4R)-5-methylidene-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl}pyrimidin-5-yl)oxy]-N,N-di(propan-2-yl)benzamide in free form or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof.
The method of claim 1, wherein the active ingredient is administered once a day or twice a day.
The method of claim 1, wherein the active ingredient is administered twice a day.
The method of claim 1, wherein one dose of the active ingredient is 40 mg, 60 mg, 80 mg, 100 mg, 120 mg, 140 mg, 160 mg, 180 mg, 200 mg, 220 mg, 240 mg, 260 mg, 280 mg, 300 mg, 320 mg, 340 mg, 360 mg, 380 mg, or 400 mg converted to the free form.
The method of claim 1, wherein one dose of the active ingredient is 200 mg, 220 mg, 240 mg, 260 mg, 280 mg, 300 mg, 320 mg, 340 mg, 360 mg, 380 mg, or 400 mg converted to the free form.
The method of claim 2, wherein one dose of the active ingredient is 200 mg or 300 mg converted to the free form.
The method of claim 3, wherein one dose of the active ingredient is 200 mg converted to the free form.
The method of claim 3, wherein one dose of the active ingredient is 300 mg converted to the free form.
The method of claim 1, wherein the cancer is leukemia, polycythemia vera, malignant lymphoma, B-cell lymphoma, myeloma, brain tumor, cancer of the head and neck, esophageal cancer, thyroid cancer, small cell lung cancer, non-small cell lung cancer, breast cancer, gastric cancer, gallbladder and bile duct cancer, liver cancer, hepatocellular cancer, pancreatic cancer, colon cancer, rectal cancer, anal cancer, chorionepithelioma, endometrial cancer, cervical cancer, ovarian cancer, bladder cancer, urothelial cancer, renal cancer, renal cell cancer, prostate cancer, testicular tumor, testicular germ cell tumor, ovarian germ cell tumor, Wilms' tumor, malignant melanoma, neuroblastoma, osteosarcoma, Ewing's sarcoma, chondrosarcoma, soft tissue sarcoma, or skin cancer.
The method of claim 1, wherein the cancer is leukemia, B-cell lymphoma, neuroblastoma, or prostate cancer.
The method of claim 1, wherein the cancer is leukemia.
The method of claim 11, wherein the leukemia is acute leukemia, chronic lymphocytic leukemia, or chronic myeloid leukemia.
The method of claim 12, wherein the acute leukemia is MLL acute leukemia, MLL partial tandem duplicate acute leukemia, or NPM1 mutated acute leukemia.
The method of claim 12, wherein the acute leukemia is MLL acute leukemia or NPM1 mutated acute leukemia.
The method of claim 12, wherein the acute leukemia is acute myeloid leukemia with MLL rearrangement, acute lymphoid leukemia with MLL rearrangement, acute myeloid leukemia with NPM1 mutation, or leukemia accompanied by high expression of HOXa gene cluster or MEIS gene cluster.
The method of claim 12, wherein the acute leukemia is relapsed or refractory acute myeloid leukemia with MLL rearrangement, relapsed or refractory acute lymphoid leukemia with MLL rearrangement, or relapsed or refractory acute myeloid leukemia with NPM1 mutation.
The method of claim 12, wherein the acute leukemia is acute myeloid leukemia with MLL rearrangement, and one dose of the active ingredient is 200 mg or 300 mg converted to the free form.
The method of claim 12, wherein the acute leukemia is relapsed or refractory acute myeloid leukemia with MLL rearrangement, and one dose of the active ingredient is 200 mg or 300 mg converted to the free form.
The method of claim 12, wherein the acute leukemia is acute lymphoid leukemia with MLL rearrangement, and one dose of the active ingredient is 200 mg or 300 mg converted to the free form.
The method of claim 12, wherein the acute leukemia is relapsed or refractory acute lymphoid leukemia with MLL rearrangement, and one dose of the active ingredient is 200 mg or 300 mg converted to the free form.
The method of claim 12, wherein the acute leukemia is acute myeloid leukemia with NPM1 mutation, and one dose of the active ingredient is 200 mg or 300 mg converted to the free form.
The method of claim 12, wherein the acute leukemia is relapsed or refractory acute myeloid leukemia with NPM1 mutation, and one dose of the active ingredient is 200 mg or 300 mg converted to the free form.
The method of claim 12, wherein the acute leukemia is acute myeloid leukemia with MLL rearrangement, one dose of the active ingredient is 300 mg converted to the free form, and the active ingredient is administered twice a day.
The method of claim 12, wherein the acute leukemia is relapsed or refractory acute myeloid leukemia with MLL rearrangement, one dose of the active ingredient is 300 mg converted to the free form, and the active ingredient is administered twice a day.
The method of claim 12, wherein the acute leukemia is acute lymphoid leukemia with MLL rearrangement, one dose of the active ingredient is 300 mg converted to the free form, and the active ingredient is administered twice a day.
The method of claim 12, wherein the acute leukemia is relapsed or refractory acute lymphoid leukemia with MLL rearrangement, one dose of the active ingredient is 300 mg converted to the free form, and the active ingredient is administered twice a day.
The method of claim 12, wherein the acute leukemia is acute myeloid leukemia with NPM1 mutation, one dose of the active ingredient is 300 mg converted to the free form, and the active ingredient is administered twice a day.
The method of claim 12, wherein the acute leukemia is relapsed or refractory acute myeloid leukemia with NPM1 mutation, one dose of the active ingredient is 300 mg converted to the free form, and the active ingredient is administered twice a day.
The method of claim 12, wherein the acute leukemia is leukemia accompanied by high expression of HOXa gene cluster or MEIS gene cluster.
The method of claim 1, wherein the cancer is tumor accompanied by p53 gain-of-function mutation, or the cancer exhibits at least one genetic abnormality selected from NPM1 gene mutation, DNMT3A gene mutation, FLT gene mutation, and MLL translocation.
Dependencies are inferred from the claim text.