Indirubin derivatives, and uses thereof

US2020247750A1 · US · A1

Patent metadata
FieldValue
Publication numberUS-2020247750-A1
Application numberUS-201916594894-A
CountryUS
Kind codeA1
Filing dateOct 7, 2019
Priority dateFeb 3, 2012
Publication dateAug 6, 2020
Grant date

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  2. Abstract

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Abstract

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Indirubin is the major active anti-tumor component of a traditional Chinese herbal medicine used for treatment of chronic myelogenous leukemia (CML). Indirubin derivatives (IRDs) potently reduce the viabilities of various cancer cells and affect kinase activities. IRDs disclosed herein provide new therapeutics for cancer and conditions regulated by the kinase activities.

First claim

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1 - 21 . (canceled) 22 . A method of treating a cancer or tumor in a subject comprising administering to the subject a therapeutically effective amount of an indirubin derivative (IRD) comprising a structure of Structure A 23 . The method of claim 22 , wherein the cancer or tumor is selected from the group consisting of CML, prostate cancer, melanoma, pancreatic cancer, ovarian cancer, leukemia, and lymphoma. 24 . The method according to claim 22 , wherein the cancer is prostate cancer, and the indirubin derivative is selected from the group consisting of IRD Nos. 10-11, 13, 59, 71, 79, 80, 83, 84, 87, 128 and 176. 25 . The method according to claim 22 , wherein the cancer is melanoma, and the indirubin derivative is selected from the group consisting of IRD Nos. 59, and 176. 26 . The method according to claim 22 , wherein the cancer is pancreatic cancer, and the indirubin derivative is selected from the group consisting of IRD Nos. 9, 11, 13, 59, 61, 68-71, 82-87, 115, and 176. 27 . The method according to claim 22 , wherein the cancer is ovarian cancer, and the indirubin derivative is selected from the group consisting of IRD Nos. 11, 13, 59, 61, 69, 71, 79-82, 84-87, 124, and 176. 28 . The method according to claim 22 , wherein the cancer is leukemia, and the indirubin derivative is selected from the group consisting of IRD Nos. 10-13, 59, 61, 70, 71, 79-80, 83-87, 115, 128, and 176. 29 . The method according to claim 22 , wherein the cancer is lymphoma, and the indirubin derivative is selected from the group consisting of IRD Nos. 10-13, 59, 79-80, 83, 84, 87, 115, 128 and 176. 30 . A method of treating a condition regulated by a protein kinase in a subject comprising administering an indirubin derivative (IRD) comprising a structure of Structure A 31 . The method according to claim 30 , wherein the protein kinase is selected from the group consisting of ABL1, ABL1 (T315I mutant), Aurora A, c-Src, FGR, FLT3, HCK, LYN, JAK2, and TYK2. 32 . The method according to claim 31 , wherein the protein kinase is ABL1, and the indirubin derivative is selected from the group consisting of IRD Nos. 11, 13, 61, 70, 71, 79, 80, 83-87, and 176. 33 . The method according to claim 31 , wherein the protein kinase is ABL1 (T315I mutant), and the indirubin derivative is selected from the group consisting of IRD Nos. 61, 79, 80, 83-85 and 87. 34 . The method according to claim 31 , wherein the protein kinase is Aurora A, and the indirubin derivative is selected from the group consisting of IRD Nos. 61, 70, 79, 80, 83-87, and 176. 35 . The method according to claim 31 , wherein the protein kinase is c-Src, and the indirubin derivative is selected from the group consisting of IRD Nos. 10, 11, 13, 61, 70, 71, 79, 80, 83-87, and 176. 36 . The method according to claim 31 , wherein the protein kinase is FGR, FLT3, HCK, LYN, or TYK2, and the indirubin derivative is IRD No. 176. 37 . The method according to claim 31 , wherein the protein kinase is JAK2, and the indirubin derivative is selected from the group consisting of IRD Nos. 61, 79, 80, 83, 84 and 87.

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Classifications

  • containing three or more hetero rings · CPC title

  • C07D209/40Primary

    Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone · CPC title

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What does patent US2020247750A1 cover?
Indirubin is the major active anti-tumor component of a traditional Chinese herbal medicine used for treatment of chronic myelogenous leukemia (CML). Indirubin derivatives (IRDs) potently reduce the viabilities of various cancer cells and affect kinase activities. IRDs disclosed herein provide new therapeutics for cancer and conditions regulated by the kinase activities.
Who is the assignee on this patent?
Hope City, The National And Kapodistrian Univ Of Athens
What technology area does this patent fall under?
Primary CPC classification C07D209/40. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Thu Aug 06 2020 00:00:00 GMT+0000 (Coordinated Universal Time) (A1). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).