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 T63505 Target Info
Target Name Tyrosine-protein kinase ABL1 (ABL)
Synonyms p150; Proto-oncogene tyrosine-protein kinase ABL1; Proto-oncogene c-Abl; JTK7; C-ABL; Abl; Abelson tyrosine-protein kinase 1; Abelson murine leukemia viral oncogene homolog 1
Target Type Successful Target
Gene Name ABL1
Biochemical Class Kinase
UniProt ID
ABL1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2012127012
Title Biphenyl Tricyclic Quinazoline Compounds.
Abstract The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are multiple inhibitors of tyrosine kinase activity.
Applicant(s) Universita 'Degli Studi Di Padova
Representative Drug(s) D03JXD Drug Info IC50 < 1000 nM Click to Show More [1]
2 D06LHV Drug Info IC50 < 1000 nM [1]
3 D0KM7V Drug Info IC50 < 1000 nM [1]
Patent ID WO2012101239
Title Derivatives of Azaindazole or Diazaindazole Type As Medicament.
Abstract The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.
Applicant(s) Pf Medicament
Representative Drug(s) D0TX1S Drug Info IC50 = 18 nM Click to Show More [1]
2 D0JD9Z Drug Info IC50 = 38 nM [1]
Patent ID WO2012080284
Title Substituted 6,6-Fused Nitrogenous Heterocyclic Compounds and Uses Thereof.
Abstract The invention provides novel compounds having the general formula (I) wherein X1 is N or N+O-, and one of X2, X3 and X4 is N or N+-O- and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula (I) and methods of use are further described herein.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0O0RB Drug Info Ki = 0.02 nM Click to Show More [1]
2 D0QD6T Drug Info Ki = 0.02 nM [1]
3 D0XL1M Drug Info Ki = 0.02 nM [1]
Patent ID WO2011008788
Title Fluoro-Substituted Compounds As Kinase Inhibitors and Methods of Use Thereof.
Abstract The present invention provides for novel compounds of Formula I and pharmaceutically acceptable salts and solvates thereof which have kinase inhibitor activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating and preventing a Bcr-Abl, c-Kit or PDGF-R mediated disorder for which one or more kinase inhibitor is indicated, including neoplasia such as chronic myelogenous leukemia or gastrointestinal stromal tumors. The present invention also provides for processes of making the compounds of Formula I, including salts and solvates thereof, and pharmaceutical compositions comprising the same.
Applicant(s) Zhang, Dawei
Representative Drug(s) D0RT8M Drug Info IC50 < 100 nM Click to Show More [1]
2 D0X0VH Drug Info IC50 < 100 nM [1]
Patent ID WO2014108021
Title Fluorocyclobutanylimidazole Compounds.
Abstract Provided are fluorocyclobutanylimidazole compounds of formula (I) and N-oxides, pharmaceutically acceptable salt or prodrugs thereof. Also provided are the preparation method thereof and intermediates.
Applicant(s) Terrabay Pharmaceuticals, Inc
Representative Drug(s) D0Y0PE Drug Info IC50 = low nM [1]
Patent ID WO2014102378
Title Azaindole Derivatives As Inhibitors of Protein Kinases.
Abstract The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus also includes the preparation of compounds of formula (I), their uses, in particular in the inhibition of protein kinases which are implicated for example in numerous diseases such as cancers or immune system disorders.
Applicant(s) Oribase Pharma
Representative Drug(s) D05TYI Drug Info Inhibition values higher than 50% = 10000 nM [1]
Patent ID WO2014102376
Title Protein Kinase Inhibitors.
Abstract The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus also includes the preparation of compounds of formula (I), their uses, in particular in the inhibition of protein kinases which are implicated for example in numerous diseases such as cancers or immune system disorders.
Applicant(s) Oribase Pharma
Representative Drug(s) D0X9VH Drug Info Inhibition values higher than 50% = 10000 nM [1]
Patent ID WO2014088519
Title Compounds Including Map Kinase Interacting Kinases 1 and 2 (Mnk1 and Mnk2) Modulators and Abl and Abl (T315I) Inhibitors, and Uses Thereof.
Abstract The present invention relates to certain piperazine-based compounds that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b and/or as ABL or ABL (T315I) inhibitors. The invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of cancer, inflammatory and Alzheimer disease conditions, as well as methods of treatment of these disorders.
Applicant(s) Agency for Science, Technology and Research
Representative Drug(s) D0ZH4I Drug Info IC50 < 1000 nM [1]
Patent ID WO2014071378
Title Substituted Indol-5-Ol Derivatives and Their Therapeutical Applications.
Abstract The present invention relates generally to the use of compounds to treat a variety of disorders, diseases and pathologic conditions and more specifically to the use of substituted indol-5-ol derivatives to modulate protein kinases and for treating protein kinase-mediated diseases.
Applicant(s) Nant Holdings Ip, Llc
Representative Drug(s) D0F4AW Drug Info Complete % enzyme inhibition = 100 nM [1]
Patent ID WO2013068909
Title N-Methyl-2-[3-((E)-2-Pyridin-2-Yl-Vinyl)-1H-Indazol-6-Ylsulfanyl]-Benzamide for The Treatment of Chronic Myelogenous Leukemia.
Abstract The present invention relates to a method of treating chronic myelogenous leukemia in a subject comprising administering to the subject a compound, such as N-methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-benzamide, that inhibits the T315I mutation in BCR-ABL tyrosine kinase, or a pharmaceutically acceptable salt thereof. The present invention also relates to a pharmaceutical composition comprising a compound such as N-methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]- benzamide, that inhibits the T315I mutation in BCR-ABL tyrosine kinase, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.
Applicant(s) Pfizer Inc
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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