Unit dosage composition of AKT inhibitor
A unit dosage composition of an AKT inhibitor, and in particular, relates to a pharmaceutical composition in unit dosage form includes a compound of formula I-0 or a pharmaceutically acceptable salt thereof, wherein the mass of the compound I-0 or the pharmaceutically acceptable salt thereof is 5 mg to 400 mg calculated as free base.
1 . A unit dosage pharmaceutical composition comprising compound I-0 or a pharmaceutically acceptable salt thereof, wherein the mass of the compound I-0 or the pharmaceutically acceptable salt thereof is 5 mg to 400 mg calculated as a free base, and the compound I-0 has the following structure:
wherein, R is selected from the group consisting of C1-C4 alkyl and C3-C6 cycloalkyl; and
X is selected from the group consisting of CH 2 and O.
2 . The unit dosage pharmaceutical composition according to claim 1 , wherein the compound I-0 is selected from the group consisting of:
3 . The unit dosage pharmaceutical composition according to claim 1 , wherein the mass of the compound I-0 or the pharmaceutically acceptable salt of the compound I-0 is 10 mg to 400 mg, or 10 mg to 200 mg, or 10 mg to 150 mg, or 25 mg to 150 mg, or 25 mg to 100 mg, or 10 mg, or 25 mg, or 50 mg, or 75 mg, or 100 mg, or 150 mg, or 200 mg, or 400 mg, calculated as the free base.
4 . The unit dosage pharmaceutical composition according to claim 1 , wherein calculated as the free base, the mass of the compound I-0 or the pharmaceutically acceptable salt thereof is 0.1-99.9% of the total mass of the unit dosage pharmaceutical composition.
5 . The unit dosage pharmaceutical composition according to claim 1 , wherein the compound I-0 is a compound I or a pharmaceutically acceptable salt thereof, wherein the mass of the compound I or the pharmaceutically acceptable salt thereof is 5 mg to 400 mg calculated as a free base, and the compound I has the following structure:
wherein, R is selected from the group consisting of C1-C4 alkyl and C3-C6 cycloalkyl; and
X is selected from the group consisting of CH 2 and O.
6 . The unit dosage pharmaceutical composition according to claim 5 , wherein the compound I is selected from the group consisting of:
7 . The unit dosage pharmaceutical composition according to claim 5 , wherein the mass of the compound I or the pharmaceutically acceptable salt thereof is 10 mg to 400 mg, or 10 mg to 200 mg, or 10 mg to 150 mg, or 25 mg to 150 mg, or 25 mg to 100 mg, or 10 mg, or 25 mg, or 50 mg, or 75 mg, or 100 mg, or 150 mg, or 200 mg, or 400 mg, calculated as the free base.
8 . The unit dosage pharmaceutical composition according to claim 5 , wherein calculated as the free base, the mass of the compound I or the pharmaceutically acceptable salt thereof is 0.1-99.9% of the total mass of the unit dosage pharmaceutical composition.
9 . The unit dosage pharmaceutical composition according to claim 1 , further comprising one or more pharmaceutically acceptable carriers.
10 . The unit dosage pharmaceutical composition according to claim 1 , wherein the unit dosage pharmaceutical composition is a pharmaceutical preparation suitable for an oral administration.
11 . The unit dosage pharmaceutical composition according to claim 1 for use as a medicament.
12 . A method for treating an AKT protein kinase-mediated disease or disease state, wherein the method comprises administering the unit dosage pharmaceutical composition according to claim 1 to a subject in need; wherein, the AKT protein kinase-mediated disease or disease state is a breast cancer, a prostate cancer, or an ovarian cancer.
13 . The method according to claim 12 , wherein the dosage of the unit dosage pharmaceutical composition administered to the subject in need that is calculated based on the compound I-0 is 0.01-50 mg/kg weight/day.
14 . The unit dosage pharmaceutical composition according to claim 1 , wherein R is selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, cyclopropyl, cyclopentyl or cyclohexyl.
15 . The unit dosage pharmaceutical composition according to claim 1 , wherein X is CH 2 .
16 . The unit dosage pharmaceutical composition according to claim 1 , wherein calculated as the free base, the mass of the compound I-0 or the pharmaceutically acceptable salt thereof is 5-90% of the total mass of the unit dosage pharmaceutical composition.
17 . The unit dosage pharmaceutical composition according to claim 1 , wherein calculated as the free base, the mass of the compound I-0 or the pharmaceutically acceptable salt thereof is 25-65% of the total mass of the unit dosage pharmaceutical composition.
18 . The unit dosage pharmaceutical composition according to claim 5 , wherein R is selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, cyclopropyl, cyclopentyl or cyclohexyl.
19 . The unit dosage pharmaceutical composition according to claim 5 , wherein X is CH 2 .
20 . The unit dosage pharmaceutical composition according to claim 5 , wherein calculated as the free base, the mass of the compound I-0 or the pharmaceutically acceptable salt thereof is 5-90% of the total mass of the unit dosage pharmaceutical composition.
21 . The unit dosage pharmaceutical composition according to claim 5 , wherein calculated as the free base, the mass of the compound I-0 or the pharmaceutically acceptable salt thereof is 25-65% of the total mass of the unit dosage pharmaceutical composition.