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US 2022/0008395 A1Published application
Antimitotic amides for the treatment of cancer and proliferative disorders
AssigneeFrost Biologic, Inc.
InventorAdam SIDDIQUI-JAIN
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Abstract
Novel, antimitotic heteroaryl amides and pharmaceutically acceptable salts of Formula I where Ar, R5, R6, R8, R9, R11, X1, and X2 are as defined herein, as compounds for treatment and prevention of cancer and proliferative diseases and disorders.
Claims20
A compound or salt of formula II
- wherein
- X1 is CR7;
- X2 is selected from N and CR10;
- each of R1, R2, R4, R5, R6, R7, R8, R9 and R10 are —H;
- R3 is selected from substituted or unsubstituted C3-6 cycloalkyl, —ORA, —NRARB, —SRA, —S(O)RA, —S(O)2RA, and substituted or unsubstituted 3- to 10-membered heterocyclyl;
- R11 is selected from —H, halogen, substituted or unsubstituted C1-8 alkyl, —C(O)RA, —CO2RA, —C(O)NRARB, —ORA, and —NRARB;
- each of RA and RB, when present, is independently selected from —H, halogen, substituted or unsubstituted C1-8 alkyl, substituted or unsubstituted C3-6 cycloalkyl, substituted or unsubstituted C2-8 alkenyl, substituted or unsubstituted C2-8 alkynyl, —CN, ═O, —NO2, —OR′, —OC(O)R′, —CO2R′, —C(O)R′, —C(O)NR′R″, —OC(O)NR′R″, —NR′″C(O)R′, —NR′″C(O)NR′R″, —NR′R″, —NR′″CO2R′, —SR′, —S(O)R′, —S(O)2R′, —S(O)2NR′R″, —NR'S(O)2R″, substituted or unsubstituted C6-10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl and substituted or unsubstituted 3- to 10-membered heterocyclyl;
- R′, R″, and R′″ are each independently hydrogen, unsubstituted C1-4 alkyl, and substituted or unsubstituted C3-6 cycloalkyl or R′ and R″ together with the atoms which they substitute form a substituted or unsubstituted 5-, 6-, or 7-membered ring.
5 more elements
A method of treating a proliferative disorder in a patient in need thereof, comprising administering a compound or salt of formula II
- wherein
- X1 is CR7;
- X2 is selected from N and CR10;
- each of R1, R2, R4, R5, R6, R7, R8, R9 and R10 are —H;
- R3 is selected from substituted or unsubstituted C3-6 cycloalkyl, —ORA, —NRARB, —SRA, —S(O)RA, —S(O)2RA, and substituted or unsubstituted 3- to 10-membered heterocyclyl;
- R11 is selected from —H, halogen, substituted or unsubstituted C1-8 alkyl, —C(O)RA, —CO2RA, —C(O)NRARB, —ORA, and —NRARB;
- each of RA and RB, when present, is independently selected from —H, halogen, substituted or unsubstituted C1-8 alkyl, substituted or unsubstituted C3-6 cycloalkyl, substituted or unsubstituted C2-8 alkenyl, substituted or unsubstituted C2-8 alkynyl, —CN, ═O, —NO2, —OR′, —OC(O)R′, —CO2R′, —C(O)R′, —C(O)NR′R″, —OC(O)NR′R″, —NR′″C(O)R′, —NR′″C(O)NR′R″, —NR′R″, —NR′″CO2R′, —SR′, —S(O)R′, —S(O)2R′, —S(O)2NR′R″, —NR'S(O)2R″, substituted or unsubstituted C6-10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl and substituted or unsubstituted 3- to 10-membered heterocyclyl;
- R′, R″, and R′″ are each independently hydrogen, unsubstituted C1-4 alkyl, and substituted or unsubstituted C3-6 cycloalkyl or R′ and R″ together with the atoms which they substitute form a substituted or unsubstituted 5-, 6-, or 7-membered ring.
5 more elements
Dependencies are inferred from the claim text.