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 T08391 Target Info
Target Name Janus kinase 2 (JAK-2)
Synonyms Tyrosine-protein kinase JAK2
Target Type Successful Target
Gene Name JAK2
Biochemical Class Kinase
UniProt ID
JAK2_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014151871
Title Jak2 and Alk2 Inhibitors and Methods for Their Use.
Abstract Compounds having activity as inhibitors of ALK2 kinase and/or JAK2 kinase are disclosed. The compounds have the following structure (I): [FORMULA SHOULD BE INSERTED HERE] including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, X, z and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Applicant(s) Tolero Pharmaceuticals, Inc
Representative Drug(s) D0AE0M Drug Info IC50 < 10 nM Click to Show More [1]
2 D0A8BV Drug Info IC50 > 1000 nM [1]
Patent ID WO2014128591
Title Pyrrolo [2, 3 -D]Pyrimidine Derivatives As Inhibitors of Janus- Related Kinases (Jak).
Abstract Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.
Applicant(s) Pfizer Inc
Representative Drug(s) D0KL3B Drug Info IC50 = 800 nM Click to Show More [1]
2 D0U5FZ Drug Info IC50 = 1200 nM [1]
3 D0FQ4Z Drug Info IC50 = 7200 nM [1]
Patent ID WO2014101295
Title Isoxazole Derivative That Inhibits Activity of Janus Kinases (Jaks).
Abstract Disclosed is an isoxazole derivative that inhibits the activity of the Janus kinases (JAKs), the structure thereof as presented in formula I, formula II, formula IX, and formula XI. The substituent groups in the formulas are described in the description. Also disclosed are the pharmaceutical composition of the compound and a related use in medicine preparation.
Applicant(s) Zhejiang Dtrm Biopharma
Representative Drug(s) D0TX2G Drug Info IC50 = 13 nM Click to Show More [1]
2 D0G9MM Drug Info IC50 = 350 nM [1]
Patent ID WO2013092854
Title Pyrimidine-2,4-Diamine Derivatives As Kinase Inhibitors.
Abstract The present invention relates to compounds of formula (I) wherein X, R, Y0, T0A, T0B have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immuno logically-mediated diseases. The invention also relates to pharmaceutical compositions including said compoundsand their use as medicaments.
Applicant(s) Cellzome Limited
Representative Drug(s) D0LR6J Drug Info IC50 > 10000 nM Click to Show More [2]
2 D0S6XT Drug Info IC50 > 10000 nM [2]
3 D0SJ1Q Drug Info IC50 > 10000 nM [2]
Patent ID WO2013070606
Title Methods for Treating Inflammatory Diseases and Pharmaceutical Combinations Useful Therefor.
Abstract The present invention provides method of treating or lessening the severity of a disease selected from spondyloarthropathy, systemic lupus erythematosus, rheumatoid arthritis, or any combination thereof comprising the administration of a compound of Formula I and an optional co-therapy (e.g., chemotherapy agent, DMARD, or any combination thereof). The present invention also provides a pharmaceutical composition comprising a compound of Formula I, a method of manufacturing a pharmaceutical composition comprising a compound of Formula I, and a method of administering a pharmaceutical composition comprising a solid form of a compound of Formula I.
Applicant(s) Vertex Pharmaceuticals Incorporated
Representative Drug(s) D0W8DN Drug Info IC50 = 1 nM Click to Show More [1]
2 D0GH8D Drug Info IC50 = 15 nM [1]
Patent ID WO2013028818
Title Pyrimido- Pyridazinone Compounds and Use Thereof.
Abstract The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
Applicant(s) Endo Pharmaceuticals Inc
Representative Drug(s) D0WA1V Drug Info IC50 = 1.7 nM Click to Show More [2]
2 D0CD6Y Drug Info IC50 < 10 nM [2]
Patent ID WO2011101806
Title Bicyclic Compounds and Their Uses As Dual C-Src / Jak Inhibitors.
Abstract The present invention relates to substituted aromatic bicyclic compounds containing pyrimidine and pyridine rings of formula (I) having the structure as well as pharmaceutically acceptable salts thereof. The compounds of the present invention are useful as tyrosine kinase inhibitors, preferably SRC family kinases (SFKs) inhibitors, in particular as multi SFK/JAK. kinases inhibitors and even preferably as dual c-SRC/JAK kinases inhibitors, thereby inhibiting the STAT3 activation and therefore abnormal growth of particular cell types. Notably, the compounds of the present invention are useful for the treatment or inhibition of certain diseases that are the result of deregulation of STAT3.
Applicant(s) Debiopharm Sa
Representative Drug(s) D0M9YZ Drug Info IC50 = 3 nM Click to Show More [3]
2 D0Q5JV Drug Info IC50 = 3 nM [3]
3 D0VI7E Drug Info IC50 = 6 nM [3]
4 D09RTW Drug Info IC50 = 7 nM [3]
5 D0M5AG Drug Info IC50 = 7 nM [3]
6 D0QD5Y Drug Info IC50 = 15 nM [3]
Patent ID WO2015177326
Title 5-Chloro-2-Difluoromethoxyphenyl Pyrazolopyrimidine Compounds Which Are Jak Inhibitors.
Abstract Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein. Claimed uses are the treatment of inflammation and asthma.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D04OCD Drug Info Ki = 0.7 nM [1]
Patent ID WO2015173683
Title Pyrazolopyridines and Pyrazolopyrimidines.
Abstract A compound having the structure: A compound having the structure (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A and A' are independently C or N, where C may be unsubstituted or substituted by halo or C1-C6 alkyl; R and R0 are independently selected from the group consisting of H, C1-C6 alkyl, hydroxy(C1-C6 alkyl), phenyl(C1-C6 alkyl), and -(CH2)n-W, where W is C3-C8 cycloalkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1 -3 N, S and/or 0 atoms, -SO2-R', -NHSO2-R', -NR&quot;SO2-R' and SR', where R' and R&quot; are independently C1-C6 alkyl or C3-C8 cycloalkyl, etc.; wherein each of said alkyl, cycloalkyl, heterocyclic, phenyl, naphthyl or heteroaryl may be unsubstituted or substituted by phenyl, heteroaryl, etc.; or, R and R0 and the N atom to which they are bonded together form a monocyclic or bicyclic heterocyclic ring which may be unsubstituted or substituted by (a) halo, hydroxy, heteroaryl, C1-C6 alkyl, C1-C6 alkoxy, etc., or (b) -(CH2)n-W, where W is C3-C8cycloalkyl, phenyl, etc.; R1 is H, halo or cyano; R2 and R2' are independently H, C1-C6 alkyl, cyano, C1-C6 alkoxy, C1-C6 alkylthio, or C3-C8 cycloalkyl where alkyl, alkoxy, or cycloalkyl is optionally substituted by one or more fluorine atoms; X is a bond, -CO-, -CONH-, -S02-, -SONH-, or -(CH2)m-; R3 is H, C1-C4 alkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1 -3 N atoms, a 5-membered heteroaryl or heterocyclic, etc., or (c) 2 O or S atoms and 0-2 N atoms; wherein each of said phenyl, naphthyl, heteroaryl or heterocyclic is optionally substituted by alkyl, 1 substituent -Y-R4 and/or 1 -4 substituents each independently selected from R5; with the proviso that when X is -CO- or -SO2-, R3 is not H; Y is a bond, -(CH2)m- or -O-; R4 is (a) H, C1-C6 alkyl, C3-C8 cycloalkl, halo, oxo, -OR6, -NR7R8, -SR6, -SOR9, -SO2R9, -COR6, -OCOR6, -COOR6, -NR6COR6, -CONR7R8, etc.; (b) phenyl or naphthyl, said phenyl and naphthyl being optionally substituted with 1 -5 substituents selected from C1-C6 alkyl, C3-C8 cycloalkyl, halo, cyano, -OR6, -NR7R8, etc.; or (c) a 3 to 8-membered saturated or partially unsaturated monocyclic heteroaryl, etc.; R6 is H, C1-C6 alkyl or C3-C8 cycloalkyl, etc.; R7 and R8 are each independently H, C1-C6 alkyl or C3-C8 cycloalkyl or are taken together with the nitrogen atom to which they are attached to form a 4-, 5- or 6-membered saturated heterocyclic ring containing 1 -2 nitrogen atoms or 1 nitrogen and 1 oxygen atom, said C1-C6 alkyl is optionally substituted by C3-C8 cycloalkyl, ha lo, etc., and said heterocyclic ring being optionally substituted by one or more C1-C6 alkyl or C3-C8 cycloalkyli groups; R9 is C1-C6 alkyl or C3-C8 cycloalkyl; and, m and n are independently 0, 1, 2 or 3. The invention also relates to pharmaceutically acceptable salts of these compounds and to pharmaceutically acceptable solvates thereof; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD.
Applicant(s) Pfizer Inc
Representative Drug(s) D03QAY Drug Info IC50 = 2.1 nM [1]
Patent ID WO2015164604
Title Hydrophobically Tagged Janus Kinase Inhibitors and Uses Thereof.
Abstract The present invention provides Janus kinase inhibitors, such as compounds of Formula (I) and Formula (II) wherein RY1 and RY2 comprise a tagged hydrophobic moiety RH. The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). The hydrophobic moiety RH may signal to the intracellular protein homeostasis machinery to induce degradation of the targeted kinase. Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and/or treating and/or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and/or viral infection).
Applicant(s) Dana-Farber Cancer Institute, Inc
Representative Drug(s) D0WZ8N Drug Info IC50 = 3100 nM [2]
Patent ID WO2015148867
Title Substituted Heteroaryl Compounds and Methods of Use.
Abstract The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof useful in preventing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
Applicant(s) Calitor Sciences, Llc
Representative Drug(s) D0GB7G Drug Info IC50 = 18 nM [2]
Patent ID WO2015123453
Title Pyridazine Compounds As Jak Inhibitors.
Abstract In one aspect, the invention provides a compound according to formula I, as well as tautomers, pharmaceutically acceptable salts, and hydrates thereof. Pharmaceutical compositions, methods of inhibiting Janus kinases (JAKs), and methods for treating a condition or disorder mediated at least in part by JAK kinase activity are also described.
Applicant(s) Portola Pharmaceuticals, Inc
Patent ID WO2015118434
Title Pyrazolo[1,5-A]Pyrimidine Derivatives As Kinase Jak-2 Inhibitors.
Abstract A compound of the general formula (I), useful for treating myeloproliferative, cancer,or inflammatory diseases, wherein Q represents a six-membered heteroaromatic ring containing 2 N atoms and R1 is hydrogen atom,or Q represents a five-membered heteroaromatic ring containing 1 or 2 heteroatoms selected from the group consisting of N and S,one substituent R1 is attached at C or N atom of said Q ringand R1 is selected from the group consisting of C1-C4-alkyl and C3-C4-cycloalkyl;R2 represents-NR7aR7bor-CH2-NR8aR8b;R3 represents C1-C4-alkyl;R4 represents phenylora 5-or 6-membered heteroarylcontaining 1 or 2 heteroatoms selected from the group consisting of N and S, and R4 is unsubstituted or substituted with 1 or 2 substituents selected from the group consisting of halogen, trifluoromethyl,hydroxyl and C1-C4-alkoxyl;R5 and R6 independently represent hydrogenatom or C1-C4-alkyl,and at least one of R5 and R6 represents hydrogen atom;and other substituents are as defined in the specification; and pharmaceutically acceptable salts thereof.
Applicant(s) Celon Pharma Sa
Representative Drug(s) D0HS2J Drug Info IC50 < 10 nM [2]
Patent ID WO2015110378
Title Benzimidazole Derivatives and Pharmaceutical Compositions Thereof for The Treatment of Inflammatory Disorders.
Abstract The present invention discloses compounds according to Formula (I) wherein Cy, R1, L1 R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula (I), able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.
Applicant(s) Galapagos Nv
Representative Drug(s) D01CRX Drug Info IC50 > 100 to 500 nM [2]
Patent ID WO2015110092
Title 4-Substituted Pyrrolo[2,3-D]Pyrimidine Compound and Use Thereof.
Abstract The present invention relates to a 4-substituted pyrrolo[2,3-d]pyrimidine compound and the use thereof in preparing medications for treating JAK-targeted diseases such as rheumatoid, immune system dis.
Applicant(s) Jiangsu Carefree Pharmaceutical Co., Ltd
Representative Drug(s) D0M3CB Drug Info IC50 = 0.61 nM [1]
Patent ID WO2015094803
Title Substituted Heteroaryl Compounds and Methods of Use.
Abstract The present invention provides new heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof useful in preventing, treating or lessening the severity of JAK-mediated diseases. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of JAK-mediated diseases.
Applicant(s) Calitor Sciences, Llc
Representative Drug(s) D0F3BK Drug Info IC50 = 8 nM [2]
Patent ID WO2015091531
Title Imidazolopyrimidin-2-Yl Derivatives As Jak Inhibitors.
Abstract New imidazopyridmin-2-yl derivatives are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use as inhibitors of Janus Kinases (JAK) for the treatment of myeloproliferative disorders, leukemia, lymphoid malignancies and solid tumors; bone marrow and organ transplant rejection; immune-mediated diseases and inflammatory diseases.
Applicant(s) Almirall, Sa
Patent ID WO2015089153
Title Treatment of Multiple Sclerosis with A 1,2,4-Triazolo [1,5A] Pyridine Derivative.
Abstract The present disclosure provides methods and compositions for treating chronic autoimmune diseases, such as multiple sclerosis, using [8-(4-methanesulfonyl-phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]-[3-(4-methyl-piperazin-1-yl)-phenyl]-amine or a pharmaceutically acceptable salt thereof.
Applicant(s) Cephalon, Inc
Representative Drug(s) D07XYI Drug Info IC50 = 1.3 nM [2]
Patent ID WO2015086693
Title Pyrazolopyrimidin-2-Yl Derivatives As Jak Inhibitors.
Abstract New pyrazolopyridmiin-2-yl derivatives are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
Applicant(s) Almirall, Sa
Representative Drug(s) D0G0FK Drug Info IC50 < 100 nM [2]
Patent ID WO2015073267
Title Substituted Heteroaryl Compounds and Methods of Use.
Abstract The present invention provides novel heterocyclic compounds, pharmaceutical acceptable salts and formulations thereof useful in preventing, treating or lessening the severity of a JAK-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of JAK-mediated disease.
Applicant(s) Calitor Sciences, Llc
Representative Drug(s) D0PM8K Drug Info IC50 = 47 nM [2]
Patent ID WO2015057695
Title Novel Compositions, Uses and Methods for Their Preparation.
Abstract The present invention relates to novel compunds and pharmaceutical compositions thereof which may be useful in the treatment and/or prevention of various conditions. The present invention also provides methods of prearing such compounds and compositions, and methods of using the same.
Applicant(s) Bohan Jin
Representative Drug(s) D01EYJ Drug Info IC50 < 10 nM [2]
Patent ID WO2015032286
Title Triazolopyridine Compounds, Compositions and Methods of Use Thereof.
Abstract Compounds of Formula 0, Formula I and Formula II and methods of use as Janus kinase inhibitors are described herein.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D00JUI Drug Info IC50 = 0.26 nM [1]
Patent ID WO2015019365
Title N-Cyanomethylamides As Inhibitors of Janus Kinase.
Abstract The present invention relates to compounds of general formula (1) that are inhibitors of Janus Kinase (JAK), a family of tyrosine kinases that are involved in inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. In particular, the compound of the invention inhibits JAK1 and/or JAK2 and/or JAK3 sub families. The present invention also provides methods for the production of the compounds of the invention, pharmaceutical compositions comprising the compounds of the invention, their tautomeric forms, and their pharmaceutically acceptable salts.
Applicant(s) Cadila Healthcare Limited
Representative Drug(s) D0Y2IM Drug Info IC50 = 8 nM [2]
Patent ID WO2014146493
Title Acyclic Cyanoethylpyrazolo Pyridones As Janus Kinase Inhibitors.
Abstract The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D03PBI Drug Info IC50 = 0.18 nM [1]
Patent ID WO2014146492
Title N-(2-Cyano Heterocyclyl)Pyrazolo Pyridones As Janus Kinase Inhibitors.
Abstract Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D06MQB Drug Info IC50 = 0.08 nM [1]
Patent ID WO2014146491
Title Geminally Substituted Cyanoethylpyrazolo Pyridones As Janus Kinase Inhibitors.
Abstract The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0KI5F Drug Info IC50 = 0.05 nM [1]
Patent ID WO2014146490
Title Cycloalkyl Nitrile Pyrazolo Pyridones As Janus Kinase Inhibitors.
Abstract Compounds of formula I are provided, which are JAK inhibitors and are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0PB5X Drug Info IC50 = 0.085 nM [1]
Patent ID WO2014146249
Title Geminally Substituted Cyanoethylpyrazolo Pyridones As Janus Kinase Inhibitors.
Abstract Disclosed are geminally substituted cyanoethylpyrazolo pyridones as Janus Kinase inhibitors, which are useful in the treatment of iJAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0H6XN Drug Info IC50 = 0.09 nM [1]
Patent ID WO2014146246
Title Cycloalkyl Nitrile Pyrazolo Pyridones As Janus Kinase Inhibitors.
Abstract The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0S4TH Drug Info IC50 = 0.54 nM [1]
Patent ID WO2014123167
Title Tricyclic Pyrrolopyridine Compound, and Jak Inhibitor.
Abstract The present invention addresses the problem of providing a novel tricyclic pyrrolopyridine compound which has a JAK inhibitory activity, and is particularly useful for preventing, treating and/or alleviating autoimmune diseases, inflammatory diseases, or allergic diseases. Provided is a novel tricyclic pyrrolopyridine compound represented by formula (I) (the substituents in the formula are defined in detail in the description, however R1 represents a C1-6 alkyl group, or the like, R2 represents a hydrogen atom, or the like, R3 represents a hydrogen atom, or the like, ring A represents a C3-11 cycloalkane, or the like, L1 represents a C1-6 alkylene group, or the like, and R4 represents NRaRb, or the like), a tautomer of said compound or a pharmaceutically acceptable salt thereof, or a solvate of the compound, the tautomer, or the pharmaceutically acceptable salt.
Applicant(s) Nissan Chemical Industries, Ltd
Representative Drug(s) D04BOW Drug Info IC50 = 7 nM [1]
Patent ID WO2014111037
Title Five-and-Six-Membered Heterocyclic Compound, and Preparation Method, Pharmaceutical Composition and Use Thereof.
Abstract A five-and-six-membered heterocyclic compound as represented by general formula I, pharmaceutically acceptable salt, metabolite, metabolic precursors or drug precursors thereof, preparation method, ph.
Applicant(s) Shanghai Yunyi Healthcare Management Co., Ltd
Representative Drug(s) D08WPB Drug Info IC50 < 50 nM [1]
Patent ID WO2014091265
Title Pyrimidine-2,4-Diamine Derivatives As Kinase Inhibitors.
Abstract The present application relates to novel Pyrimidine-2,4-diamine derivatives as kinase inhibitors derivatives of formula (I), as protein kinase inhibitors. Formula (I). The invention particularly relates to compounds of formula (I), preparation of compounds and pharmaceutical compositions thereof. The invention further relates to prodrugs, derivatives, polymorphs, pharmaceutically acceptable salts and compositions comprising the said novel Pyrimidine-2,4-diamine derivatives as kinase inhibitors and their derivatives and their use in the treatment of various disorders.
Applicant(s) Aurigene Discovery Technologies Limited
Patent ID WO2014058921
Title Substituted Pyrimidinyl Kinase Inhibitors.
Abstract Provided are substituted pyrimidinyl compounds for inhibition of JAK and/or Syk kinase, pharmaceutical compositions thereof, methods for inhibiting JAK and/or Syk kinase activity, and methods for treating conditions mediated at least in part by JAK and/or Syk kinase activity.
Applicant(s) Portola Pharmaceuticals, Inc
Patent ID WO2014020531
Title Imidazo[1,2-B]Pyridazin-6-Amine Derivatives As Kinase Jak-2 Inhibitors.
Abstract A compound represented by the general formula (I) wherein R1represents H or C1-C4 alkyl; R2 represents phenyl substituted with one or two substituents selected from the group consisting of halogen atom and OC1-C4 alkyl;R3 represents phenyl or 5 to 10-membered monocyclic or bicyclic heteroaryl having from 1 to 4 ring heteroatoms selected from the group consisting of N, S, and O, which can be unsubstituted or substituted with a substituent selected from halogen atom, C1-C4-alkyl, and -C(O)O-C1-C4 -alkyl; and X represents ...H2-group or carbonyl-C(O)-group;and their acid addition salts;with the exclusion of 3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholinomethyl)-imidazo[1,2-b]pyridazine-6-amine and its salts. The compounds are JAK2 inhibitors and are useful as medicaments, especially for treating proliferative disorders and cancer diseases.
Applicant(s) Celon Pharma Sa
Representative Drug(s) D0KF8H Drug Info IC50 = 1.7 nM [2]
Patent ID WO2014019908
Title Substituted Pyrroles Active As Kinases Inhibitors.
Abstract The present invention relates to substituted pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
Applicant(s) Nerviano Medical Sciences S.R.L
Representative Drug(s) D0YJ4D Drug Info IC50 = 1 nM [1]
Patent ID WO2014000032
Title Phenyl Amino Pyrimidine Bicyclic Compounds and Uses Thereof.
Abstract The present invention relates to phenyl amino pyrimidine bicyclic compounds formula (I) which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
Applicant(s) Ym Biosciences Australia Pty Ltd
Representative Drug(s) D0RJ3W Drug Info IC50 = 30 nM [1]
Patent ID WO2013189771
Title Aminotriazolopyridine for Use In The Treatment of Inflammation, and Pharmaceutical Compositions Thereof.
Abstract The present invention relates to the novel medical use of the compound according to Formula I, in particular in the treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. In particular, the compound inhibits JAK a family of tyrosine kinases, and more particularly JAK1. The present invention also provides pharmaceutical compositions comprising the compound, methods for the prophylaxis and/or treatment of diseases involving inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons by administering the compound.
Applicant(s) Galapagos Nv
Representative Drug(s) D09ALF Drug Info IC50 = 620 nM [2]
Patent ID WO2013188184
Title Inhibitor of Jak1 and Jak2.
Abstract The present invention provides an amino pyrazole compound, which is 3-[(lR)-6-fluoro-2,3-dihydro-1H-inden-l-yl]-N-(3- methyl-IH- pyrazol-5-yl)-3H-imidazo[4,5-b]pyridin-5-amine, or a pharmaceutically acceptable salt thereof, that inhibits JAK1 and JAK2 and, therefore may be useful in treating cancer.
Applicant(s) Eli Lilly and Company
Representative Drug(s) D0WA1V Drug Info IC50 = 1.7 nM [2]
Patent ID WO2013173720
Title Piperidinylcyclobutyl Substituted Pyrrolopyridine and Pyrrolopyrimidine Derivatives As Jak Inhibitors.
Abstract The present invention provides piperidinylcyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I, as defined herein, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Applicant(s) Incyte Corporation
Representative Drug(s) D0VQ7P Drug Info IC50 = 20 to 150 nM [2]
Patent ID WO2013117649
Title Imidazo [4, 5 -C] Pyridine Derivatives Useful for The Treatment of Degenerative and Inflammatory Diseases.
Abstract Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, wherein R1 and Cy are as disclosed herein. These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.
Applicant(s) Galapagos Nv
Representative Drug(s) D0VJ1R Drug Info IC50 = 0.01 to 100 nM [2]
Patent ID WO2013117646
Title Novel Compound Useful for The Treatment of Degenerative and Inflammatory Diseases.
Abstract A novel imidazolopyridine according to Formula I, able to inhibit JAK as disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.
Applicant(s) Galapagos Nv
Representative Drug(s) D0YR8S Drug Info IC50 = 70 nM [2]
Patent ID WO2013116291
Title Imidazo [4, 5 - B] Pyridine Derivatives As Alk and Jak Modulators for The Treatment of Proliferative Disorders.
Abstract This application relates to compounds of the Formula I as defined herein, and/or salts thereof. This application further relates to compositions and methods of using these compounds and/or salts thereof. The compounds of Formula I are useful as ALK and JAK modulators for the treatment of proliferative disorders.
Applicant(s) Cephalon, Inc
Representative Drug(s) D0NP2W Drug Info IC50 < 100 nM [2]
Patent ID WO2013091539
Title Pyrrole Six-Membered Heteroaryl Ring Derivative, Preparation Method Therefor, and Medicinal Uses Thereof.
Abstract The present invention relates to a pyrrole six-membered heteroaryl ring derivative, the preparation method therefor, and the medicinal uses thereof. Specifically, the present invention relates to a new pyrrole six-membered heteroaryl ring derivative as represented in formula (I), the preparation method therefor, a medicinal composition comprising the derivative, and a therapeutic agent using same, and, in particular, the uses as a JAK inhibitor and an immunosuppressor. Substituents in formula (I) have the same definitions as in description.
Applicant(s) Jiangsu Hengrui Medicine Co
Representative Drug(s) D09UBE Drug Info IC50 = 45 nM [1]
Patent ID WO2013055645
Title 5,7-Substituted-Imidazo[1,2-C]Pyrimidines.
Abstract Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
Applicant(s) Array Biopharma Inc
Representative Drug(s) D0U1HA Drug Info IC50 = 10 to 100 nM [2]
Patent ID WO2013052355
Title Azaindoles As Janus Kinase Inhibitors.
Abstract The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0IQ6G Drug Info IC50 > 10 nM [1]
Patent ID WO2013043964
Title Acyclic Cyanoethylpyrazoles As Janus Kinase Inhibitors.
Abstract The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D05GEL Drug Info IC50 = 8 nM [1]
Patent ID WO2013043962
Title Cyanomethylpyrazole Carboxamides As Janus Kinase Inhibitors.
Abstract The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0K2RW Drug Info IC50 = 0.2 nM [1]
Patent ID WO2013041605
Title Pyrazolo[4,3-C]Pyridine Derivatives As Kinase Inhibitors.
Abstract The present invention relates to compounds of formula (I) wherein X1 to X5, Y, ZA, ZB, R and A have the meaning as cited in the description and the claims. Said compounds are useful as kinase inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically- mediated diseases. The invention also relates to pharmaceutical compositions including said compounds as well as the use as medicaments.
Applicant(s) Cellzome Limited
Representative Drug(s) D09PIS Drug Info IC50 > 10000 nM [2]
Patent ID WO2013040863
Title Cycloalkylnitrile Pyrazole Carboxamides As Janus Kinase Inhibitors.
Abstract Cycloalkylnitrile pyrazole carboxamides as JAK inhibitors useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer are provided.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0V0KI Drug Info IC50 = 11 nM [1]
Patent ID WO2013024895
Title Tricyclic Heterocyclic Compounds and Jak Inhibitors.
Abstract Novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities are provided. A tricyclic heterocyclic compound represented by the formula (Ia): wherein the rings Aa and Ba, Xa, Ya, R1a, R2a, R3a, L1a, L2a, L3a and na are as defined in the description.
Applicant(s) Nissan Chemical Industries, Ltd
Representative Drug(s) D0X1FD Drug Info IC50 = 1.6 nM [1]
Patent ID WO2013017480
Title Pyrazolo[4,3-C]Pyridine Derivatives As Jak Inhibitors.
Abstract The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z5, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
Applicant(s) Cellzome Limited
Representative Drug(s) D0D1QH Drug Info IC50 < 100 nM [2]
Patent ID WO2013017479
Title Pyrazolo[4,3-C]Pyridine Derivatives As Jak Inhibitors.
Abstract The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z4, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically- mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
Applicant(s) Cellzome Limited
Representative Drug(s) D02VGC Drug Info IC50 = 1000 to 10000 nM [2]
Patent ID WO2013017461
Title Pyridin-2(1H)-One Derivatives As Jak Inhibitors.
Abstract New pyridin-2(1H)-one derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
Applicant(s) Almirall Sa
Representative Drug(s) D0A6RG Drug Info IC50 < 100 nM [2]
Patent ID WO2013014162
Title Heterocyclyl Pyrimidine Analogues As Jak Inhibitors.
Abstract The present invention relates to compounds of formula (I), wherein X1 to X5, Z1 to Z3, Y0, RY1, RY2 and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically- mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
Applicant(s) Cellzome Limited
Representative Drug(s) D01FVC Drug Info IC50 = 1000 to 10000 nM [2]
Patent ID WO2013014039
Title Alkynyl Substituted Pyrimidinyl-Pyrroles Active As Kinases Inhibitors.
Abstract The present invention relates to alkynyl substituted pyrimidinyl-pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak and/or Src family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
Applicant(s) Nerviano Medical Sciences S.R.L
Representative Drug(s) D0JZ2B Drug Info IC50 = 4 nM [1]
Patent ID WO2013007768
Title Tricyclic Heterocyclic Compounds, Compositions and Methods of Use Thereof As Jak Inhibitors.
Abstract The invention provides novel compounds of formula I having the general formula:(I) wherein Rl s R2, R3, X and Y are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0M2WA Drug Info IC50 = 1 nM [1]
Patent ID WO2013007765
Title Fused Tricyclic Compounds for Use As Inhibitors of Janus Kinases.
Abstract The invention provides novel compounds of formula (I) having the general formula (I) wherein R1, V, W, X, Y and Z are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0LS1O Drug Info IC50 = 36 nM [1]
Patent ID WO2008079521
Title Tricyclic Heteroaryl Compounds Useful As Inhibitors of Janus Kinase.
Abstract The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Applicant(s) Vertex Pharmaceuticals Incorporated
Representative Drug(s) D03TEE Drug Info Ki < 250 nM [2]
Patent ID WO2014157569
Title Heterocyclic Compound.
Abstract Provided is a compound having an excellent JAK-inhibiting effect, the compound being is useful as an agent for the prevention or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, infl.
Applicant(s) Takeda Pharmaceutical Company Limited
Representative Drug(s) D09RUN Drug Info N.A. [1]
Patent ID WO2010141796
Title Preparation and Uses of 1,2,4-Triazolo [1,5A] Pyridine Derivatives.
Abstract This application relates to compounds of the general Formula I and salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of treatment of hyperproliferative diseases or disorders.
Applicant(s) Cephalon, Inc
United States Patent and Trademark Office (USPTO)
Patent ID US20120053208
Title Curcumin Analogs As Dual Jak2/Stat3 Inhibitors and Methods of Making and Using The Same.
Applicant(s) The Ohio State University Research Foundation
Representative Drug(s) D0IC8O Drug Info N.A. Click to Show More [3]
2 D0WD1Z Drug Info N.A. [3]
References  Top
REF 1 Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2.Expert Opin Ther Pat. 2017 Feb;27(2):145-161.
REF 2 Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1.Expert Opin Ther Pat. 2017 Feb;27(2):127-143.
REF 3 A STAT inhibitor patent review: progress since 2011.Expert Opin Ther Pat. 2015;25(12):1397-421.

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