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Last Updated: April 20, 2024

Claims for Patent: 10,537,561


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Summary for Patent: 10,537,561
Title:CSF-1R inhibitors for treatment of brain tumors
Abstract: The present invention provides a compound of formula I; ##STR00001## wherein R.sup.1 is an alkyl pyrazole or an alkyl carboxamide, and R.sup.2 is a hydroxycycloalkyl; or a pharmaceutically acceptable salt thereof, and compositions containing these compounds, for use to treat a brain tumor, particularly glioblastoma. The invention provides effective treatment of a brain tumor and can be used by oral administration of a compound of Formula I as further described herein. The invention also provides a method to treat a subject having a brain tumor such as glioblastoma, wherein the method comprises administering to the subject an effective amount of a compound of Formula I. Gene signatures correlated with successful treatment using these methods are also disclosed.
Inventor(s): Daniel; Dylan (San Francisco, CA), Joyce; Johanna (Epalinges, CH), Sutton; James (Pleasanton, CA)
Assignee: Novartis AG (Basel, CH) Sloan-Kettering Institute for Cancer Research (New York, NY)
Application Number:15/996,945
Patent Claims:1. A method of treating glioblastoma multiforme in a human subject having glioblastoma multiforme, said method comprising administering to the subject an effective amount of a CSF-1 R kinase inhibitor compound of formula: ##STR00022## or a pharmaceutically acceptable salt thereof.

2. The method of claim 1, wherein the compound is a pharmaceutically acceptable salt.

3. The method of claim 1, wherein the method further comprises the step of: administering to the subject an effective amount of an additional cancer therapeutic selected from bevacizumab with or without irinotecan, a nitrosourea, a platin, an alkylating agent, a tyrosine kinase inhibitor, Ukrain, and a cannabinoid.

4. The method of claim 1, wherein the compound or pharmaceutically acceptable salt thereof is administered orally.

5. The method of claim 1, wherein the compound or pharmaceutically salt thereof is administered to the subject in an amount between about 10 mg/kg per day to about 500 mg/kg per day.

6. The method of claim 1, wherein the compound or pharmaceutically salt thereof is administered to the subject in one or two oral doses per day.

7. The method of claim 3 wherein the additional cancer therapeutic is an alkylating agent.

8. The method of claim 7 wherein the alkylating agent is temozolomide.

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