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US 12,590,105 B2Granted
KRas G12C inhibitors
AssigneeEli Lilly and Company
InventorsDavid Michael Hyman, Gregory Lawrence Lackner, Sheng-Bin Peng, Bree Leigh Richey, Chong Si
Life of this patent
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Abstract
The present disclosure provides compounds of the formula: where R1, R2, R3, R4, R5, A, and B are as described herein, pharmaceutically acceptable salts thereof, and methods of using these compounds and salts for treating patients for cancer.
Claims24
A compound of the formula:
- wherein:
- A is —OCH2—, —N(R6)CH2—, —OCH2CH2—, —N(R6)CH2CH2—, —CH2OCH2—, or —CH2N(R6)CH2—;
- B is —CH2— or —C(O)—;
- R is —CN, —C(O) C≡CR8, or a group of the formula
- R2 is H, methyl, or —CH2CN;
- R3 and R5 are each independently H, halogen, cyclopropyl, —C1-3 alkyl-cyclopropyl, —C1-6 alkyl optionally substituted 1-3 times with R10, or —O—C1-6 alkyl optionally substituted 1-3 times with R10;
- R4 is a group of the formula
- R is H, halogen, or —C1-6 alkyl optionally substituted 1-3 times with R10;
- R′ is H, or —C1-6 alkyl;
- R6 is H or —C1-6 alkyl optionally substituted 1-3 times with R10;
- R7 is H, halogen, —NR11R12, —CH2NR11R12, —C2-6 alkyl optionally substituted 1-3 times with R10 or —NR13R14, cyclopropyl, —C1-3 alkyl cyclopropyl, or —O—C1-6 alkyl optionally substituted 1-3 times with R10 or —NR13R14;
- R8 is H, —C1-4 alkyl optionally substituted 1-3 times with R10, or —C3-6 cycloalkyl optionally substituted 1-3 times with R10;
- R9 is H, halogen, —CN, C3-6 cycloalkyl, —C1-3 alkyl-C3-6 cycloalkyl, or —C1-6 alkyl optionally substituted 1-3 times with R10;
- R10 is independently at each occurrence halogen, oxygen, hydroxy, —C1-4 alkyl, or —O—C1-4 alkyl;
- R11 and R12 are each independently H, —C1-4 alkyl, or —C1-4 heteroalkyl, wherein R11 and R12 may combine to form a C5-6 heterocycloalkyl;
- and
- R13 and R14 are each independently H or —C1-4 alkyl,
- or a pharmaceutically acceptable salt thereof.
15 more elements
Dependencies are inferred from the claim text.