Methods of treating LSD1 related diseases and disorders with LSD1 inhibitors
A disease, leukemia technology, applied in the field of treating LSD1-related diseases and diseases with LSD1 inhibitors, can solve problems such as poor prognosis
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
preparation example Construction
[0064] Oral solid dosage forms are prepared as follows. After optionally adding excipients with binders, disintegrants, lubricants, colorants, taste-masking agents or flavoring agents, etc. to Compound A of the present invention, the resulting mixture is formulated by methods known in the art Tablets, coated tablets, granules, powders, capsules, etc.
[0065] Examples of excipients include lactose, sucrose, D-mannitol, glucose, starch, calcium carbonate, kaolin, microcrystalline cellulose, and silicic anhydride. Examples of binders include water, ethanol, 1-propanol, 2-propanol, simple syrup, liquid glucose, liquid alpha-starch, liquid gelatin, D-mannitol, carboxymethylcellulose, hydroxypropylcellulose , hydroxypropyl starch, methyl cellulose, ethyl cellulose, shellac, calcium phosphate, polyvinylpyrrolidone, etc. Examples of disintegrants include dry starch, sodium alginate, powdered agar, sodium bicarbonate, calcium carbonate, sodium lauryl sulfate, monoglyceride stearate,...
Embodiment
[0152] The present invention is described in more detail below with reference to examples. However, the scope of the present invention is not limited to these Examples. The present invention is fully described below by way of examples; however, it should be understood that various changes and modifications may be made by those skilled in the art. Therefore, as long as these changes and modifications do not depart from the scope of the present invention, they are included in the present invention.
[0153] Reference Example 1. Intermittent administration is a more effective treatment for test compound A because compound A does not affect the blood stem cells.
[0154] Using the hydrochloride salt of Compound A (in Reference Example 1, 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy- Continuous administration of 2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile hydrochloride), this compound (referred to as "Test Compound A" for convenience) in Severe...
Embodiment 2
[0162] Reference Example 2. Antitumor effect and body weight change of intermittent dosing regimen in mice (1 week administration + 1 week off The regimen and dosing for 2 weeks + 1 week off is a very useful approach to show anti-tumor effects while avoiding Toxicity due to administration of test compound A)
[0163] (In Reference Example 2, 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl- propyl)phenyl]phenyl]-2-fluoro-benzonitrile benzoate, for convenience this compound is referred to as "Test Compound A".) Human small cell lung cancer (NCI-H1417, American Type Culture Collection) cells were implanted into the right chest of male SCID mice (Charles River Laboratories Japan, Inc.). After tumor implantation, the long axis (mm) and short axis (mm) of the tumor were measured, and the tumor volume (TV) was calculated. Then, the mice were assigned to groups so that the mean TV value of each group was equal. The day on which the grouping (n=5) wa...
PUM
Login to View More Abstract
Description
Claims
Application Information
Login to View More