KRAS G12D inhibitors

Abstract

To provide compounds that inhibit KRas G12D, pharmaceutical compositions comprising the compounds, and methods of use therefor.SOLUTION: Provided is a compound of formula (I), or a pharmaceutically acceptable salt thereof.SELECTED DRAWING: None

Claims

1. The following formula for use in a method for treating KRas G12D-associated non-small cell lung cancer: 【Chemistry 1】 A pharmaceutical composition comprising a therapeutically effective amount of a compound having or a pharmaceutically acceptable salt thereof, wherein the method comprises administering the pharmaceutical composition to a patient in need thereof, the administration of which is done by intravenous injection.

2. The following formula for use in a method for treating KRas G12D-associated colorectal cancer: 【Chemistry 2】 A pharmaceutical composition comprising a therapeutically effective amount of a compound having or a pharmaceutically acceptable salt thereof, wherein the method comprises administering the pharmaceutical composition to a patient in need thereof, the administration of which is done by intravenous injection.

3. The following formula for use in a method for treating KRas G12D-associated pancreatic cancer: 【Transformation 3】 A pharmaceutical composition comprising a therapeutically effective amount of a compound having or a pharmaceutically acceptable salt thereof, wherein the method comprises administering the pharmaceutical composition to a patient in need thereof, the administration of which is done by intravenous injection.

4. The following formula for use in a method for treating KRas G12D-associated endometrial cancer: 【Chemistry 4】 A pharmaceutical composition comprising a therapeutically effective amount of a compound having or a pharmaceutically acceptable salt thereof, wherein the method comprises administering the pharmaceutical composition to a patient in need thereof, the administration of which is done by intravenous injection.

5. The following formula for use in a method for treating KRas G12D-associated ovarian cancer: 【Transformation 5】 A pharmaceutical composition comprising a therapeutically effective amount of a compound having or a pharmaceutically acceptable salt thereof, wherein the method comprises administering the pharmaceutical composition to a patient in need thereof, the administration of which is done by intravenous injection.

6. The following formula for use in a method for treating KRas G12D-associated rectal cancer: 【Transformation 6】 A pharmaceutical composition comprising a therapeutically effective amount of a compound having or a pharmaceutically acceptable salt thereof, wherein the method comprises administering the pharmaceutical composition to a patient in need thereof, the administration of which is done by intravenous injection.

7. The following formula for use in a method for treating KRas G12D-associated small cell lung cancer: 【Transformation 7】 A pharmaceutical composition comprising a therapeutically effective amount of a compound having or a pharmaceutically acceptable salt thereof, wherein the method comprises administering the pharmaceutical composition to a patient in need thereof, the administration of which is done by intravenous injection.

8. The pharmaceutical composition according to any one of claims 1 to 7, wherein the therapeutically effective dose of the compound or a pharmaceutically acceptable salt thereof is about 0.01 to 100 mg / kg per day.

9. A pharmaceutical composition according to any one of claims 1 to 7, which is co-administered with different antitumor compounds or used in combination with different treatments.

10. The pharmaceutical composition according to claim 9, wherein the different antitumor compounds include different chemotherapy regimens.

11. The pharmaceutical composition according to claim 9, wherein the different treatments include radiation or surgical intervention.

12. A pharmaceutical composition according to any one of claims 1 to 7, to be administered as an adjuvant before surgery or after surgery.

13. A pharmaceutical composition according to any one of claims 1 to 7, comprising a diluent, a filler, a salt, a buffer, a stabilizer, or a solubilizer.

14. The pharmaceutical composition according to any one of claims 1 to 7, wherein the administration is carried out in multiple doses according to a treatment regimen.

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