Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T38284 Target Info
Target Name Fusion protein Bcr-Abl (Bcr-Abl)
Synonyms BCR-ABL fusion protein; BCR-ABL
Target Type Successful Target
Gene Name BCR-ABL1
Biochemical Class Kinase
UniProt ID
BCR_HUMAN - ABL1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2013171641
Title Compounds and Compositions for Inhibiting The Activity of Abl1, Abl2 and Bcr-Abl1.
Abstract The present invention relates to compounds of formula I: in which Y, Y1, Y 4, Y5, Y 6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
Applicant(s) Novartis Ag
Representative Drug(s) D0BK6R Drug Info IC50 = 1.2 nM Click to Show More [1]
2 D09WKF Drug Info IC50 = 2 nM [1]
3 D02KNW Drug Info IC50 = 2.1 nM [1]
4 D09ZFM Drug Info IC50 = 2.1 nM [1]
Patent ID WO2013171639
Title Benzamide Derivatives for Inhibiting The Activity of Abl1, Abl2 and Bcr-Abl1.
Abstract The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
Applicant(s) Novartis Ag
Representative Drug(s) D08IUE Drug Info IC50 = 0.8 nM Click to Show More [1]
2 D01KIJ Drug Info IC50 = 1.1 nM [1]
3 D0IA4G Drug Info IC50 = 1.1 nM [1]
Patent ID WO2011093684
Title Thieno[3,2-D]Pyrimidine Derivatives Having Inhibitory Activity On Protein Kinases.
Abstract The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.
Applicant(s) Hanmi Science Co., Ltd
Representative Drug(s) D0I5VG Drug Info IC50 = 1 to 10 nM Click to Show More [1]
2 D0JR7X Drug Info IC50 = 1 to 10 nM [1]
Patent ID WO2010025872
Title Alfa-Carboline Inhibitors of Npm-Alk, Ret, and Bcr-Abl.
Abstract The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in the description, to their pharmaceutical compositions and use thereof for the treatment of cancer expressing oncogenic ALK protein, particularly anaplastic large cell lymphoma (ALCL), diffuse large B cell lymphoma (DLBCL), inflammatory myofibroblastic tumours (IMT) and non-small cell lung cancer (NSCLC).
Applicant(s) Universita' Degli Studi Di Milano-Bicocca
Representative Drug(s) D00AIO Drug Info IC50 = 1600 nM Click to Show More [1]
2 D0AP4V Drug Info IC50 = 1800 nM [1]
3 D0B0BJ Drug Info IC50 = 3100 nM [1]
Patent ID WO2009109867
Title Crystal form of Phenylamino Pyrimidine Derivative.
Abstract The present invention relates to a particular form of the (3,5-bis trifluoromethyl)-N-[4- methyl-3-(4-pyridin-3yl-pyrirnidin-2ylamino)-phenyl]-benzamide (formula I), processes for the preparation thereof, pharmaceutical compositions containing this crystal form, and their use as anti tumor agent in humans. The compound of formula I, also known as AN- 019, is: Formula I (I).
Applicant(s) Natco Pharma Limited
Representative Drug(s) D01OYY Drug Info IC50 = 0.1 to 10 nM Click to Show More [1]
2 D0KR7K Drug Info IC50 = 0.1 to 10 nM [1]
Patent ID WO2009063054
Title Novel Bifunctional Compounds Which Inhibit Protein Kinases and Histone Deacetylases.
Abstract The present invention relates to a bifunctional compound of formula I or its pharmaceutically acceptable salts or solvates A-L-B (I) wherein A is a histone deacetylase (HDAC) inhibitory moiety, L is a single bond or a linker group and B is a protein kinase inhibitory moiety. The bifunctional compound according to formula (I) is useful for the treatment of malignant and non-malignant neoplasia and diseases related to abnormal cell growth.
Applicant(s) 4SC AG
Representative Drug(s) D0E6EP Drug Info IC50 = 2 to 39 nM Click to Show More [1]
2 D0JY1I Drug Info IC50 = 2 to 39 nM [1]
Patent ID WO2008033746
Title Tyrosine Kinase Inhibitors Containing A Zinc Binding Moiety.
Abstract The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
Applicant(s) Curis, Inc
Representative Drug(s) D05YAD Drug Info IC50 < 100 nM Click to Show More [1]
2 D0DC7I Drug Info IC50 < 100 nM [1]
3 D0Y4EU Drug Info IC50 < 100 nM [1]
Patent ID WO2008125691
Title Preparation of Naphthalenecarboxylic Acid and Isoquinolinecarboxylic Acid Amides As Tyrosine Kinase Inhibitors.
Representative Drug(s) D04UXO Drug Info IC50 = 36 to 68 nM Click to Show More [1]
2 D0CJ7F Drug Info IC50 = 36 to 68 nM [1]
3 D0PF2F Drug Info IC50 = 36 to 68 nM [1]
Patent ID WO2004089286
Title Novel Compounds and Compositions As Protein Kinase Inhibitors.
Abstract The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.
Applicant(s) Irm Llc
Representative Drug(s) D05HDJ Drug Info IC50 = 30 nM Click to Show More [1]
2 D0L7XM Drug Info IC50 = 40 nM [1]
3 D0EF5T Drug Info N.A. [1]
Patent ID WO2010045542
Title Fused Ring Heteroaryl Kinase Inhibitors.
Abstract Provided herein are fused ring heteroaryl compounds useful in a variety of methods, including reducing the activity of certain kinases and treating certain disease states.
Applicant(s) The Regents of the University of California
Representative Drug(s) D04ZXR Drug Info IC50 = nM range Click to Show More [1]
2 D0U2LO Drug Info N.A. [1]
3 D0XU3A Drug Info N.A. [1]
Patent ID WO2011104680
Title Oxadiazole Compounds, Their Preparation and Use.
Abstract The present invention relates to oxadiazole compounds in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable prodrugs and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the oxadiazole compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the treatment of cancer, particularly chronic myeloid leukemia (CML). The present invention further provides a method of treatment of cancer by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.
Applicant(s) Piramal Healthcare Limited
Representative Drug(s) D01UBA Drug Info N.A. Click to Show More [1]
2 D0KT5W Drug Info N.A. [1]
Patent ID WO2009109991
Title Novel Hydrazide Containing Tyrosine Kinase Inhibitors.
Abstract The present invention relates to compounds of formula (I), and salts thereof, wherein P represents a 5 or 6-membered heteroaryl ring; R1 is aryl or unsaturated heterocyclyl radical optionally substituted by one or more identical or different radicals R5.
Applicant(s) Sun Pharma Advanced Research Company Ltd
Representative Drug(s) D0D3FB Drug Info N.A. Click to Show More [1]
2 D0XQ5F Drug Info N.A. [1]
Patent ID WO2008115973
Title Aminopyrimidines Useful As Kinase Inhibitors.
Abstract The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
Applicant(s) Vertex Pharmaceuticals Incorporated
Representative Drug(s) D08PXF Drug Info N.A. Click to Show More [1]
2 D0B5DX Drug Info N.A. [1]
3 D0VD5I Drug Info N.A. [1]
Patent ID WO2014086284
Title Deuterated 3-Cyano Quinoline Compound, Pharmaceutical Composition, Preparation Method and Use Thereof.
Abstract Disclosed in the invention are a deuterated 3-cyano quinoline compound or pharmaceutically acceptable salts, solvates, prodrugs, stereoisomers, tautomers, polymorphic substances, metabolites etc., and a pharmaceutical composition containing such compounds, and the use of these compounds or compositions in the preparation of drugs for treating or preventing tumours, especially drugs such as protein kinase inhibitors. Compared with the prior art, the compounds of the present invention have the clear advantages of properties such as plasma drug concentration, half-life, clearance, microsomal stability, bioavailability or enzyme inhibition and the like, and thus can more effectively inhibit the activities of more than one protein kinase and/or inhibit the growth of tumuor cells.
Applicant(s) Shanghai Pharmaceuticals Holding Co., Ltd
Representative Drug(s) D02VDD Drug Info IC50 < 5 nM [1]
Patent ID WO2014082578
Title Heteroaryl Alkyne Compound and Application Thereof.
Abstract The present invention relates to the field of the chemical medicines, and in particular, to a compound with a Heteroaryl alkyne structure shown in formula I or pharmaceutically acceptable salts, isomers, solvate, crystal or prodrug thereof, pharmaceutical compositions containing there compounds and applications of these compounds or compositions in the medicine preparation. The compound of the present invention has a strong inhibiting effect on BCR-ABL kinase, and can be used for treating, for example, neoplastic diseases.
Applicant(s) Nanjing Sanhome Pharmaceutical Co Ltd
Representative Drug(s) D0F5HC Drug Info IC50 = nM range [1]
Patent ID WO2010096395
Title Amides As Kinase Inhibitors.
Abstract The present invention is directed to amides, and pharmaceutical compositions thereof, which are inhibitors of kinases such as BCR AbI, FLT3, c-Kit, KDR, LCK, Epha2 and PDGFR subfamily and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.
Applicant(s) Syntech Solution Llc Chen, Yongsheng
Representative Drug(s) D0BJ6M Drug Info IC50 < 12 nM [1]
Patent ID WO2008128009
Title Aminopyrimidines Useful As Kinase Inhibitors.
Abstract The present invention relates to compounds of formula ( I) useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease/ conditions / and disorders. The invention also provides processes, for preparing compounds of the invention.Compound of formula I: or a pharmaceutically acceptable salt thereof.
Applicant(s) Vertex Pharmaceuticals Incorporated
Representative Drug(s) D0HF0R Drug Info IC50 < 25 nM [1]
Patent ID WO2014019338
Title Protein Kinase Inhibitors.
Abstract Disclosed are compounds of Formula I, as well as pharmaceutically acceptable salts, hydrates, isomers, or solvates thereof. Also disclosed are pharmaceutical compositions which comprise the compounds of Formula I, and methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.
Applicant(s) Astar Biotech Llc
Representative Drug(s) D0KL5M Drug Info N.A. [1]
Patent ID WO2011053938
Title Methods and Compositions for Treating Cancer.
Abstract The invention features methods, kits, and pharmaceutical compositions for treating cancer using 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-y1)-methyl)-3-(trifluoromethyl)phenyl)benzamide.
Applicant(s) Ariad Pharmaceuticals, Inc
Representative Drug(s) D0WL1U Drug Info N.A. [1]
Patent ID WO2008157131
Title Protein Kinase Inhibitors and Methods for Using Thereof.
Abstract The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of Alk, Abl, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, Blk, Bmx, BTK, C-Kit, CSK, C-Src, EphB1, EphB2, EphB4, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFRalpha, PDGFRgama, PKCalpha, SAPK2alpha, Src, SIK, Syk, Tie2 and TrkB kinases.
Applicant(s) Irm Llc
Representative Drug(s) D0Z7DA Drug Info N.A. [1]
Patent ID WO2008144253
Title Protein Kinase Inhibitors and Methods for Using Thereof.
Abstract The invention provides compounds of formula (l) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of AIk, AbI, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, BIk, Bmx, BTK, c-Kit, c-RAF, CSK, c-SRC, EphBl, EphB2, EphB4, FLTl, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFRalpha, PDGFRbeta, PKCalpha, SAPK2alpha, Src, SIK, Syk, Tie2 and TrkB kinases.
Applicant(s) Irm Llc
Representative Drug(s) D03EMY Drug Info N.A. [1]
Patent ID WO2008046003
Title Kinase Inhibitors Useful for The Treatment of Myleoproliferative Diseases and Other Proliferative Diseases.
Abstract The present invention is concerned with novel compounds useful in the treatment of hyperproliferative diseases and mammalian cancers, especially human cancers. The invention also pertains to methods of modulating kinase activities, pharmaceutical compositions, and methods of treating individuals, incorporating or using the compounds. The preferred compounds are active small molecules set forth in formulae Ia-Iww.
Applicant(s) Deciphera Pharmaceuticals, Llc
Representative Drug(s) D0O0YI Drug Info N.A. [1]
Patent ID WO2008042639
Title Compounds and Compositions As Protein Kinase Inhibitors.
Abstract The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases.
Applicant(s) Iron Llc Novartis Ag Albaugh, Pamela Chopiuk, Gregory S. Ding, Qiang Huang, Shenlin Liu, Zuosheng Pan, Shifeng Ren, Pingda Wang, Xia Wang, Xing Xie, Yongping Zhang, Chengzhi Zhang, Qiong Zhang, Guobao Poon, Daniel Renhowe, Paul Sendzik, Martin
Representative Drug(s) D0BE9U Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US2010249108
Title Substituted Dipyrido-Pyrimido-Diazepine and Benzo-Pyrido-Pyrimido Compounds.
Representative Drug(s) D0C9ZW Drug Info Activity inhibition = 80 to 100 % Click to Show More [1]
2 D0K3BR Drug Info Activity inhibition = 80 to 100 % [1]
3 D0OY0U Drug Info Activity inhibition = 80 to 100 % [1]
Patent ID US20080306100
Title Preparation of Phenylaminopyrimidine Derivatives As Inhibitors of Bcr-Abl Kinase for Treating Cancer.
Representative Drug(s) D01OYY Drug Info IC50 = 0.1 to 10 nM Click to Show More [1]
2 D0KR7K Drug Info IC50 = 0.1 to 10 nM [1]
Patent ID US20107790756
Title Kinase Inhibitors Useful for The Treatment of Myeloproliferative Diseases and Other Proliferative Diseases.
Representative Drug(s) D0O2HW Drug Info IC50 = 12 nM [1]
References  Top
REF 1 Bcr-Abl tyrosine kinase inhibitors: a patent review.Expert Opin Ther Pat. 2015 Apr;25(4):397-412.

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