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 T40097 Target Info
Target Name Stress-activated protein kinase JNK1 (JNK1)
Synonyms Stress-activated protein kinase 1c; SAPK1c; PRKM8; Mitogen-activated protein kinase 8; MAPK 8; MAP kinase 8; JNK-46; C-Jun N-terminal kinase 1
Target Type Clinical trial Target
Gene Name MAPK8
Biochemical Class Kinase
UniProt ID
MK08_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2013074986
Title Inhibitors of C-Jun-N-Terminal Kinase (Jnk).
Abstract The present invention provides novel compounds according to Formula (I): where Ring A, Ring B, X, L1, L2, RA, RC, RD, RE, m, n, and p are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of human diseases associated with kinase activity, for example, proliferative diseases, neurodegenerative diseases, metabolic disorders, inflammatory diseases, and cardiovascular diseases.
Applicant(s) Dana-Farber Cancer Institute, Inc
Representative Drug(s) D0ZU8L Drug Info IC50 = 1.3 nM Click to Show More [1]
2 D08JOC Drug Info IC50 = 1.5 nM [1]
3 D0RQ8Q Drug Info IC50 = 4.7 nM [1]
Patent ID WO2013007676
Title Aminomethyl Quinolone Compounds.
Abstract The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula (I): wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0MW7D Drug Info IC50 = 1 to 2700 nM Click to Show More [1]
2 D0Y4HR Drug Info IC50 = 1 nM [1]
3 D06WAW Drug Info IC50 = 26 nM [1]
4 D0XH9K Drug Info IC50 = 100 nM [1]
Patent ID WO2012145569
Title Substituted Diaminocarboxamide and Diaminocarbonitrile Pyrimidines, Compositions Thereof, and Methods of Treatment Therewith.
Abstract Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
Applicant(s) Signal Pharmaceuticals
Representative Drug(s) D00JGN Drug Info IC50 < 200 nM Click to Show More [1]
2 D01GSU Drug Info IC50 < 200 nM [1]
3 D0EA5P Drug Info IC50 < 200 nM [1]
4 D0I3NS Drug Info IC50 < 200 nM [1]
5 D0J8DR Drug Info IC50 < 200 nM [1]
6 D0V0WT Drug Info IC50 < 200 nM [1]
7 D0XB1S Drug Info IC50 < 200 nM [1]
Patent ID WO2012136684
Title Adamantyl Compounds.
Abstract The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula (I): wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0TK0L Drug Info IC50 = 12 nM Click to Show More [1]
2 D09QKG Drug Info IC50 = 44 nM [1]
Patent ID WO2010108155
Title Modulators of Cystic Fibrosis Transmembrane Conductance Regulator.
Abstract This invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R is COOH or CH2OH.
Applicant(s) Vertex Pharmaceuticals Incorporated
Representative Drug(s) D08JIS Drug Info IC50 = 1320 nM Click to Show More [1]
2 D0ID4H Drug Info IC50 = 18000 nM [1]
Patent ID WO2010097335
Title Imidazo [1, 2 -A] Pyridines As Jnk Modulators.
Abstract Compounds of formula (I) modulate JNK wherein X1 and X2 are each simultaneously N or CH; X3 is CH-R2 Or N-SO2R, where R is lower alkyl; R1 is aryl or heteroaryl, substituted with 0-3 lower alkyl radicals; R2 is (II), where R3 is H, lower acyl, or an amino acid, or a pharmaceutically acceptable salt thereof.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0V1CB Drug Info IC50 = 22 nM Click to Show More [1]
2 D04JUD Drug Info IC50 = 24 nM [1]
3 D0S1OV Drug Info IC50 = 49 nM [1]
Patent ID WO2010091310
Title Inhibitors of Jun N-Terminal Kinase.
Abstract The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula (I): or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
Applicant(s) Elan Pharmaceuticals, Inc
Representative Drug(s) D0W8BL Drug Info IC50 = 2 nM Click to Show More [1]
2 D0X2SG Drug Info IC50 = 9 nM [1]
3 D08DNZ Drug Info IC50 = 14 nM [1]
4 D0L2MS Drug Info IC50 = 1600 nM [1]
Patent ID WO2010069833
Title Pyrimidin- 2 -Ylamino Derivatives and Their Use To Treat Inflammation.
Abstract Compounds of formula (I) modulate JNK wherein X1 and X2 are each simultaneously N or CH; X3 is CH-R2 or N-SO2R, where R is lower alkyl; R1 is aryl or heteroaryl, substituted with 0-3 lower alkyl radicals; R2 is formula (II), where R3 is H, lower acyl, or an amino acid, or a pharmaceutically acceptable salt thereof.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0RV2Z Drug Info IC50 = 3 nM Click to Show More [1]
2 D0VE3Y Drug Info IC50 = 5 nM [1]
3 D0H4HD Drug Info IC50 = 24 nM [1]
Patent ID WO2010046273
Title Pyrimidinyl Pyridone Inhibitors of Jnk.
Abstract This application discloses novel pyrimidinyl pyridone derivatives according to Formulae I and II, wherein R1 and R2 are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of Formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of Formula I to a subject in need thereof.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0B4IH Drug Info IC50 = 70 nM Click to Show More [1]
2 D07JQX Drug Info IC50 = 291 nM [1]
Patent ID WO2010015803
Title Diazaindole Derivatives and Their Use In The Inhibition of C-Jun N-Terminal Kinase.
Abstract The invention relates to diazaindole derivatives represented by the general formula (I): where A, E, G, R1, R2, R3 and R4 are defined herein, or pharmaceutically acceptable salts thereof, their use in the inhibition of c-Jun N-terminal kinase (JNK) activity, their use in medicine and particularly in the treatment of neurodegenerative disorders, inflammatory diseases, autoimmune diseases and/or organ failure. The invention also provides processes for the manufacture of said diazaindole derivatives and compositions containing them.
Applicant(s) Eisai R & D Management Co. Ltd
Representative Drug(s) D07KMK Drug Info IC50 = 74 nM Click to Show More [1]
2 D0VR1O Drug Info IC50 = 74 nM [1]
3 D05SJB Drug Info IC50 = 101 nM [1]
4 D0T6IZ Drug Info IC50 = 166 nM [1]
Patent ID WO2008095944
Title 7-Azaindole Derivatives and Their Use In The Inhibition of C-Jun N-Terminal Kinase.
Abstract The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof, the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and the use in medicine and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of said compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them.
Applicant(s) Eisai R & D Management Co. Ltd
Representative Drug(s) D07KMK Drug Info IC50 = 74 nM Click to Show More [1]
2 D0VR1O Drug Info IC50 = 74 nM [1]
3 D05SJB Drug Info IC50 = 101 nM [1]
4 D0T6IZ Drug Info IC50 = 166 nM [1]
Patent ID WO2007125405
Title Substituted 2-Amino-Fused Heterocyclic Compounds.
Abstract The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: R1, R2, Z1, t, and ring A are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of JNK, such as diabetes, the method comprising administering to a mammal an effective amount of a compound of formula (I).
Applicant(s) Pfizer Products Inc
Representative Drug(s) D0EA6L Drug Info Ki = 0.8 nM Click to Show More [1]
2 D0Y7QW Drug Info Ki = 76 nM [1]
Patent ID WO2013091670
Title Novel Jnk Inhibitor Molecules for Treatment of Various Diseases.
Abstract The present invention relates to the use of novel JNK inhibitor molecules and their use in a method of treatment of the human or animal body by therapy.
Applicant(s) COMBETTE, Jean-Marc et al
Representative Drug(s) D0Q4WA Drug Info IC50 = 722 nM [1]
Patent ID WO2012083092
Title Bi-Dentate Compounds As Kinase Inhibitors.
Abstract The present disclosure provides compound having the general structure A or pharmaceutically acceptable salts thereof: Het-L-P (A) wherein Het is an aromatic moiety comprising a heterocyclic structure mimicking ATP, P is a docking site derived peptide or a docking site peptide rnimetic, and L is a linking moiety, wherein L links the ATP mimetic to the docking site peptide moiety. The compounds having the general structure A can serve as inhibitors of kinases, such as the kinases JNK, Erk and p38.
Applicant(s) Sanford-Burnham Medical Research Institute
Representative Drug(s) D0Q8CR Drug Info IC50 = 0.7 nM [1]
Patent ID WO2011071491
Title Isotopologues of 4-[9-(Tetrahydro-Furan-3-Yl)-8-(2, 4, 6- Trifluoro-Phenylamino)-9H-Purin-2-Ylamino]-Cyclohexan-1-Ol.
Abstract Provided herein are isotopologues of Compound 1, which are enriched with isotopes such as, for example, deuterium. Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.
Applicant(s) Signal Pharmaceuticals
Representative Drug(s) D06JRV Drug Info IC50 = 71 nM [1]
Patent ID WO2008028860
Title Benzotriazole Kinase Modulators.
Abstract The invention is concerned with novel benzotriazole derivatives of Formula (I) Wherein R, R1, R2, R3, and m are as defined in the description and the claims, as well as physiologically acceptable salts thereof. These compounds are JNK and CDK modulators.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0H4HD Drug Info IC50 = 24 nM [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20110034470
Title Pyrimidine Derivatives As Jnk Inhibitors and Their Preparation and Use for The Treatment of Jnk-Mediated Diseases.
Representative Drug(s) D0AM2B Drug Info IC50 = 3 nM Click to Show More [1]
2 D03HEK Drug Info IC50 = 4 nM [1]
3 D09YEH Drug Info IC50 = 9 nM [1]
4 D0S3AP Drug Info IC50 = 10 nM [1]
References  Top
REF 1 c-Jun N-terminal kinase inhibitors: a patent review (2010 - 2014).Expert Opin Ther Pat. 2015;25(8):849-72.

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