Method of inhibiting mutant C-KIT
First Claim
1. A method of inhibiting or reducing mutant C-KIT tyrosine kinase activity or expression in a subject suffering from a proliferative disease comprised of identifying the subject having a proliferative disease positive for a constitutively active mutant C-KIT, wherein the C-KIT mutant is at least one of C-KIT D816, D816F, D816H, D816N, D816Y and D816V, and administering to the subject having or suspected to have the proliferative disease, a therapeutically effective amount of the compound of Formula I:
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Abstract
The present invention includes a method of reducing or inhibiting the kinase activity of C-KIT mutant tyrosine kinase activity in a cell or a subject, and the use of such compound for treating mutant C-KIT driven cell proliferative disorder(s) in a subject related to using a compound of the present invention:
or pharmaceutically acceptable salt thereof.
9 Citations
24 Claims
- 1. A method of inhibiting or reducing mutant C-KIT tyrosine kinase activity or expression in a subject suffering from a proliferative disease comprised of identifying the subject having a proliferative disease positive for a constitutively active mutant C-KIT, wherein the C-KIT mutant is at least one of C-KIT D816, D816F, D816H, D816N, D816Y and D816V, and administering to the subject having or suspected to have the proliferative disease, a therapeutically effective amount of the compound of Formula I:
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13. A method for treating a subject suffering from a proliferative disease positive for a mutant C-KIT comprising:
administering to the subject in need of such treatment a therapeutically effective amount of Crenolanib or a salt thereof, wherein the proliferative disease is characterized by mutant C-KIT receptor tyrosine kinase activity, wherein the C-KIT mutant is at least one of C-KIT D816, D816F, D816H, D816N, D816Y and D816V, and wherein the proliferative disease is selected from at least one of a mastocytosis, acute myeloid leukemia, gastrointestinal stromal tumors, sinonasal NK/T-cell lymphoma, seminomas, dysgerminomas, melanomas, and thymic carcinomas. - View Dependent Claims (14, 15, 16, 17, 18, 19, 20, 21, 22)
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23. A method of inhibiting or reducing mutant C-KIT tyrosine kinase activity or expression in a subject having a proliferative disease positive for a constitutively active mutant
C-KIT, which comprises administering to the subject a therapeutically effective amount of the compound of Formula I:
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24. A method for treating a subject suffering from a proliferative disease positive for a constitutively active mutant C-KIT comprising:
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obtaining a sample from a subject suspected of having a proliferative disease selected from at least one of a mastocytosis, acute myeloid leukemia, gastrointestinal stromal tumor, sinonasal NK/T-cell lymphoma, seminoma, dysgerminoma, melanoma, or thymic carcinoma; determining if the proliferative disease is positive for a constitutively active mutant C-KIT, wherein the C-KIT mutant is at least one of C-KIT D816, D816F, D816H, D816N, D816Y, or D816V; and administering to the subject in need of such treatment a therapeutically effective amount of Crenolanib or a salt thereof sufficient to treat the proliferative disease that is positive for the constitutively active mutant C-KIT.
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Specification