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 T07173 Target Info
Target Name Tropomyosin-related kinase A (TrkA)
Synonyms gp140trk; Tyrosine kinase receptor A; Tyrosine kinase receptor; Trk-A; TRKA; TRK1-transforming tyrosine kinase protein; TRK1 transforming tyrosinekinase protein; TRK; P140-TrkA; Neurotrophic tyrosine kinase receptor type 1; NGF-trk receptor type A; MTC; High affinity nerve growth factor receptor
Target Type Successful Target
Gene Name NTRK1
Biochemical Class Kinase
UniProt ID
NTRK1_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2016097869
Title Fused Ring Heteroaryl Compounds and Their Use As Trk Inhibitors.
Abstract The disclosure provides novel chemical compounds represented by Formula (I) or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof. The compounds can be used as an inhibitor of Trk and are useful in the treatment of pain, cancer, inflammation, neurodegenerative disease and certain infectious diseases. In some compounds of Formula I, Q is -CH=CR3C(O)Nr4R5, -C=CC(O)NR4R5,-CCC(0)NR4R5, or (II).
Applicant(s) Cmg Pharmaceutical Co., Ltd
Representative Drug(s) D06NPZ Drug Info IC50 < 10 nM Click to Show More [1]
2 D0D6UF Drug Info IC50 < 10 nM [1]
3 D0U2GJ Drug Info IC50 < 10 nM [1]
Patent ID WO2016054807
Title Trka Kinase Inhibitors, Compositions and Methods Thereof.
Abstract The present invention is directed to substituted indole compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, adisease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0BO1H Drug Info IC50 = 0.5 nM Click to Show More [2]
2 D00EUL Drug Info IC50 = 0.7 nM [2]
3 D08CZY Drug Info IC50 = 4.5 nM [2]
4 D00MGO Drug Info IC50 = 610 nM [2]
5 D0LK8E Drug Info IC50 = 1600 nM [2]
Patent ID WO2016020784
Title N-Acylpyrrolidine Ether Tropomyosin-Related Kinase Inhibitors.
Abstract The present invention relates to compounds of Formula I described herein and their pharmaceutically acceptable salts, and their use in medicine, in particular as Trk antagonists.
Applicant(s) Pfizer Inc
Representative Drug(s) D0X4LA Drug Info IC50 = 12 nM Click to Show More [2]
2 D08BIH Drug Info IC50 = 1300 nM [2]
Patent ID WO2015175788
Title 1-((3S,4R)-4-(3-Fluorophenyl)-1-(2-Methoxyethyl)Pyrrolidin-3-Yl)-3-(4-Methyl-3-(2-Methylpyrimidin-5-Yl)-1-Phenyl-1H-Pyrazol-5-Yl)Urea As A Trka Kinase Inhibitor.
Abstract Provided is Compound (I) or a pharmaceutically acceptable salt thereof, which is an inhibitor of TrkA kinase and is useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation and inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis, pelvic pain syndrome, diseases related to an imbalance of the regulation of bone remodeling, and diseases resulting from Connective Tissue Growth Factor aberrant signaling.
Applicant(s) Array Biopharma Inc
Representative Drug(s) D0P3VK Drug Info IC50 = 1.1 nM Click to Show More [1]
2 D0T5OF Drug Info IC50 = 1.5 nM [1]
3 D0D7EG Drug Info IC50 = 1.7 nM [1]
Patent ID WO2015148373
Title Trka Kinase Inhibitors, Compositions and Methods Thereof.
Abstract The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0N6NG Drug Info IC50 = 0.34 nM Click to Show More [2]
2 D07AJO Drug Info IC50 = 0.79 nM [2]
3 D0DY5R Drug Info IC50 = 0.96 nM [2]
4 D0KC8X Drug Info IC50 = 1.7 nM [2]
5 D07CPL Drug Info IC50 = 1000 nM [2]
Patent ID WO2015148354
Title Trka Kinase Inhibitors, Compositions and Methods Thereof.
Abstract The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0O0GZ Drug Info IC50 = 0.16 nM Click to Show More [2]
2 D0F8BF Drug Info IC50 = 0.25 nM [2]
3 D0HF1A Drug Info IC50 = 0.69 nM [2]
4 D0I9FU Drug Info IC50 = 0.88 nM [2]
Patent ID WO2015148350
Title Trka Kinase Inhibitors, Compositions and Methods Thereof.
Abstract The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0T4CF Drug Info IC50 = 0.37 nM Click to Show More [2]
2 D04BRW Drug Info IC50 = 0.39 nM [2]
3 D0CY3U Drug Info IC50 = 0.76 nM [2]
Patent ID WO2015148344
Title Trka Kinase Inhibitors, Compositions and Methods Thereof.
Abstract The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0UN4M Drug Info IC50 = 0.069 nM Click to Show More [2]
2 D05MRY Drug Info IC50 = 0.083 nM [2]
3 D04JCD Drug Info IC50 = 0.23 nM [2]
Patent ID WO2015143654
Title Trka Kinase Inhibitors,Compositions and Methods Thereof.
Abstract The present invention is directed to six membered heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0EC4Z Drug Info IC50 = 0.6 nM Click to Show More [2]
2 D0ZE6H Drug Info IC50 = 1 nM [2]
3 D07VFQ Drug Info IC50 = 1.3 nM [2]
4 D0H3ZG Drug Info IC50 = 1.5 nM [2]
Patent ID WO2015112445
Title 6-Phenyl- or 6-(Pyridin-3-Yl)Indazole Derivatives and Methods of Use.
Abstract Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R1, R2, R3, R4, R5, R6, and X are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by Tropomysin receptor kinases (Trk). Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
Applicant(s) Abbvie Inc
Representative Drug(s) D0J9ZG Drug Info IC50 = 2.7 nM Click to Show More [1]
2 D0V5AG Drug Info IC50 = 2.7 nM [1]
3 D0T2OX Drug Info IC50 = 3.4 nM [1]
Patent ID WO2015092610
Title N-Acylpiperidine Ether Tropomyosin-Related Kinase Inhibitors.
Abstract The present invention relates to compounds of Formula (I) described herein and their pharmaceutically acceptable salts, and their use in medicine, in particular as Trk antagonists.
Applicant(s) Pfizer Limited
Representative Drug(s) D03BAY Drug Info IC50 = 1.3 nM Click to Show More [2]
2 D04GCC Drug Info IC50 = 1.5 nM [2]
3 D00FJH Drug Info IC50 = 1.7 nM [2]
4 D00XXZ Drug Info IC50 = 6 nM [2]
5 D0X1LP Drug Info IC50 = 12 nM [2]
6 D04RXX Drug Info IC50 = 290 nM [2]
Patent ID WO2015042088
Title Trka Kinase Inhibitors, Compositions and Methods Thereof.
Abstract The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0U5XI Drug Info IC50 = 27 nM Click to Show More [2]
2 D0VD5J Drug Info IC50 = 28 nM [2]
3 D0M8VS Drug Info IC50 = 99 nM [2]
Patent ID WO2014078408
Title Bicyclic Heteroaryl Urea, Thiourea, Guanidine and Cyanoguanidine Compounds As Trka Kinase Inhibitors.
Abstract Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.
Applicant(s) Array Biopharma Inc
Representative Drug(s) D0YN0I Drug Info IC50 = 48 nM Click to Show More [2]
2 D05AQT Drug Info IC50 = 82 nM [2]
Patent ID WO2013176970
Title Trka Kinase Inhibitors, Compositions and Methods Thereof.
Abstract The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0UQ2G Drug Info IC50 = 6.5 nM Click to Show More [2]
2 D0CG8N Drug Info IC50 = 11 nM [2]
Patent ID WO2013009582
Title Trka Kinase Inhibitors, Compositions and Methods Thereof.
Abstract The present invention is directed to compounds of formula I and la: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0Y0XJ Drug Info IC50 = 28 nM Click to Show More [2]
2 D02ZQN Drug Info IC50 = 5400 nM [2]
Patent ID WO2012158413
Title Pyrrolidinyl Urea and Pyrrolidinyl Thiourea Compounds As Trka Kinase Inhibitors.
Abstract Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and Ring C are as defined herein, and wherein the Y-B moiety and the NH-C(=X)-NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
Applicant(s) Array Biopharma Inc
Representative Drug(s) D00ICS Drug Info IC50 = 1 to 100 nM Click to Show More [1]
2 D06YON Drug Info IC50 = 1 to 100 nM [1]
3 D0A4YR Drug Info IC50 = 1 to 100 nM [1]
4 D0I8AY Drug Info IC50 = 1 to 100 nM [1]
5 D0J5OO Drug Info IC50 = 1 to 100 nM [1]
6 D0JJ0T Drug Info IC50 = 1 to 100 nM [1]
7 D0K2GH Drug Info IC50 = 1 to 100 nM [1]
8 D0K3QT Drug Info IC50 = 1 to 100 nM [1]
9 D0LB7Z Drug Info IC50 = 1 to 100 nM [1]
10 D0ME5D Drug Info IC50 = 1 to 100 nM [1]
11 D0X0YJ Drug Info IC50 = 1 to 100 nM [1]
12 D0Z6LB Drug Info IC50 = 1 to 100 nM [1]
Patent ID WO2012137089
Title Pyrrolo [2, 3 -D] Pyrimidine Derivatives As Inhibitors of Tropomyosin- Related Kinases.
Abstract The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
Applicant(s) Pfizer Limited
Representative Drug(s) D0AG2A Drug Info IC50 = 4 nM Click to Show More [2]
2 D0S0II Drug Info IC50 = 48 nM [2]
Patent ID WO2012125668
Title Trka Kinase Inhibitors, Compositions and Methods Thereof.
Abstract The present invention is directed to quinazolinyl and pyridoquinazolinyl compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0U3RD Drug Info IC50 = 0.7 nM Click to Show More [2]
2 D0RR8O Drug Info IC50 = 1.5 nM [2]
Patent ID WO2011146336
Title Macrocyclic Compounds As Trk Kinase Inhibitors.
Abstract Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
Applicant(s) Array Biopharma Inc
Representative Drug(s) D05KHT Drug Info IC50 = 1 to 100 nM Click to Show More [1]
2 D05RKT Drug Info IC50 = 1 to 100 nM [1]
3 D0Z5PA Drug Info IC50 = 1 to 100 nM [1]
Patent ID WO2011006074
Title Substituted Pyrazolo[1,5-A]Pyrimidine Compounds As Trk Kinase Inhibitors.
Abstract Compounds of Formula (I) and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
Applicant(s) Array Biopharma Inc
Representative Drug(s) D00DIZ Drug Info IC50 = 1.7 nM Click to Show More [1]
2 D0BI5I Drug Info IC50 = 6.6 nM [1]
3 D0BZ0T Drug Info IC50 = 16.1 nM [1]
4 D0H8XH Drug Info IC50 = 28.9 nM [1]
Patent ID WO2010106028
Title Use of A Kinase Inhibitor for The Treatment of Thymoma.
Abstract The invention provides a low molecular weight ATP-competitive CDK inhibitor and TRKA inhibitor of formula (I) for use in the treatment of thymoma and thymic carcinoma. The compound can be administered together with one or more cytotoxic or cytostatic agents.
Applicant(s) Nerviano Medical Sciences S.R.L
Representative Drug(s) D0AU4G Drug Info IC50 = 1 nM Click to Show More [2]
2 D0O8SX Drug Info IC50 = 53 nM [2]
Patent ID WO2010048314
Title Substituted Pyrazolo[1,5-A]Pyrimidine Compounds As Trk Kinase Inhibitors.
Abstract Compounds of Formula (I) in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.
Applicant(s) Array Biopharma Inc
Representative Drug(s) D03USW Drug Info IC50 = 6.2 nM Click to Show More [1]
2 D09SYD Drug Info IC50 = 10.2 nM [1]
3 D08IWT Drug Info IC50 = 28.5 nM [1]
4 D04KQB Drug Info IC50 = 77.5 nM [1]
Patent ID WO2010033941
Title Substituted Imidazo[1,2B]Pyridazine Compounds As Trk Kinase Inhibitors.
Abstract Compounds of Formula (I): in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.
Applicant(s) Array Biopharma Inc
Representative Drug(s) D04QHI Drug Info IC50 = 2.1 nM Click to Show More [1]
2 D0FS4S Drug Info IC50 = 3.8 nM [1]
3 D0W0UF Drug Info IC50 = 5.5 nM [1]
4 D0DO4I Drug Info IC50 = 15.5 nM [1]
Patent ID WO2010077680
Title Compositions of Protein Receptor Tyrosine Kinase Inhibitors.
Abstract The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF recptor TrkA.
Applicant(s) WU, Jay Jie-Qiang et al
Representative Drug(s) D0PY0G Drug Info IC50 = 85 nM Click to Show More [2]
2 D07KVL Drug Info N.A. [2]
3 D0F2BF Drug Info N.A. [2]
4 D0FL8A Drug Info N.A. [2]
5 D0J4CA Drug Info N.A. [2]
6 D0K6IM Drug Info N.A. [2]
7 D0T0HM Drug Info N.A. [2]
Patent ID WO2016036796
Title Cyclic Urea Compounds As Tropomyosin-Related Kinase (Trk) Inhibitors.
Abstract Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-receptor kinase B (TrkB), tropomyosin-receptor kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).
Applicant(s) Genzyme Corporation
Representative Drug(s) D02QWP Drug Info N.A. Click to Show More [1]
2 D0I5DM Drug Info N.A. [1]
Patent ID WO2014078331
Title N-(Arylalkyl)-N'-Pyrazolyl-Urea, Thiourea, Guanidine and Cyanoguanidine Compounds As Trka Kinase Inhibitors.
Abstract Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C, X, Ra, Rb, Rc, Rd and n are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
Applicant(s) Array Biopharma Inc
Representative Drug(s) D0W9RH Drug Info N.A. Click to Show More [1]
2 D0YM2S Drug Info N.A. [1]
Patent ID WO2013183578
Title Imidazo[1,2-B]Pyridazine Derivative As Kinase Inhibitor.
Abstract The present invention provides a compound useful in treating tumors by ROS1 kinase enzyme activity inhibitory action and NTRK kinase enzyme inhibitory action, or a pharmacologically acceptable salt thereof. A compound having an imidazo[1,2-b]pyridazine structure represented by general formula (I), a pharmacologically acceptable salt thereof, or pharmaceutical compositions comprising such compounds. (In the formula, R1, G, T, Y1, Y2, Y3, and Y4 are as defined in the present description.).
Applicant(s) Daiichi Sankyo Co., Ltd
Representative Drug(s) D0M8UO Drug Info N.A. Click to Show More [1]
2 D0N1CF Drug Info N.A. [1]
3 D0T8XD Drug Info N.A. [1]
Patent ID WO2010144522
Title Ureidophenyl Substituted Triazine Derivatives and Their Therapeutical Applications.
Abstract The present invention provides Uredophenyl substituted triazine derivatives and provides methods of using these compounds to modulate protein kinases and methods of using these compounds to treat protein kinase mediated diseases and conditions.
Applicant(s) Abraxis Bioscience, Llc
Representative Drug(s) D08SDJ Drug Info N.A. Click to Show More [1]
2 D0V7QU Drug Info N.A. [1]
Patent ID WO2016061228
Title Inhibition of Trk Kinase Mediated Tumor Growth and Disease Progression.
Abstract It has been shown that Compound 1 unexpectedly and potently inhibits TRK kinases, including all three forms of TRK: NTRKl, NTRK2, and NTRK3. Additionally it has been shown that Compound 1 potently inhibits oncogenic mutated forms of TRK kinases, including fusion proteins. By way of exemplification, Compound 1 potently inhibits the NTRKl oncogenic fusion protein TPM3/NTRK1 in cellular assays. Compound 1 inhibits TRK kinase mediated tumor growth in vivo in a TPM3/NTRK1 xenograft model.
Applicant(s) Deciphera Pharmaceuticals, Llc
Representative Drug(s) D0FA6S Drug Info IC50 = 3.8 nM [1]
Patent ID WO2016009296
Title N-Acylpiperidine Ether Tropomyosin-Related Kinase Inhibitors.
Abstract The present invention relates to compounds of Formula (I) described herein and their pharmaceutically acceptable salts, and their use in medicine, in particular as Trkantagonists.
Applicant(s) Pfizer Inc
Representative Drug(s) D02OLJ Drug Info IC50 = 4.9 nM [2]
Patent ID WO2015170218
Title Tropomyosin-Related Kinase Inhibitors.
Abstract The present invention relates to compounds of Formula I and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as TrkA antagonists.
Applicant(s) Pfizer Inc
Patent ID WO2015089139
Title Tropomyosin-Related Kinase (Trk) Inhibitors.
Abstract Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).
Applicant(s) Genzyme Corporation
Representative Drug(s) D07RLB Drug Info IC50 = 0.3 nM [1]
Patent ID WO2014177510
Title Polymer Conjugates of Indolocarbazole Compounds In The Treatment of Pruritus.
Abstract The present invention is directed to the novel use of polymer conjugates of a class of indolocarbazole compounds for the prevention, alleviation or/and treatment of pruritus, particularly of pruritus associated with or caused by dermatological diseases.
Applicant(s) Creabilis Sa
Patent ID WO2014129431
Title Trk-Inhibiting Compound.
Abstract The invention provides a drug having as the active ingredient a compound having Trk-inhibiting activity in the prevention and/or treatment of Trk-associated diseases, for example, pain, pruritus, lowe.
Applicant(s) Ono Pharmaceutical Co., Ltd
Representative Drug(s) D0QT8L Drug Info IC50 = 1 nM [2]
Patent ID WO2014053968
Title Pyrrolo[3,2-C]Pyridine Tropomyosin-Related Kinase Inhibitors.
Abstract The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
Applicant(s) Pfizer Limited
Representative Drug(s) D0DQ5G Drug Info IC50 = 4.4 nM [2]
Patent ID WO2014053965
Title Tropomyosin-Related Kinase Inhibitors.
Abstract The present invention relates to compounds of Formula (IA) and (IB) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
Applicant(s) Pfizer Limited
Representative Drug(s) D0RK6W Drug Info IC50 = 17 nM [2]
Patent ID WO2014016434
Title Derivatives of Azaindazole or Diazaindazole Type for Treating A Cancer Overexpressing Trk.
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 pharmaceutical composition comprising such a compound, for use in the treatment of a cancer associated with the overexpression of at least one Trk protein.
Applicant(s) Pierre Fabre Medicament
Representative Drug(s) D0Y1NH Drug Info IC50 = 45 nM [2]
Patent ID WO2013161919
Title Trk-Inhibiting Compound.
Abstract The purpose of the present invention is to provide is a drug the active ingredient of which is a compound that has Trk-inhibiting activity in the prevention and/or treatment of diseases such as pain, pruritus, lower urinary tract disorder, asthma, allergic rhinitis, inflammatory bowel disease and Chagas disease. A compound represented by general formula (I) (where each symbol has the same definition as the symbol described in the Specification), a salt thereof, an N-oxide thereof, or a solvate thereof, or a prodrug of the same, is useful as a drug ingredient having Trk-inhibiting activity in the prevention and/or treatment of disease such as pain, pruritus, lower urinary tract disorder, asthma, allergic rhinitis, inflammatory bowel disease and Chagas disease.
Applicant(s) Ono Pharmaceutical Co., Ltd
Representative Drug(s) D0I2OO Drug Info IC50 = 2 nM [2]
Patent ID WO2013088256
Title Substituted Pyrazolo[1,5-A] Pyridine As Tropomyosin Receptor Kinase (Trk) Inhibitors.
Abstract The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors., method of making and pharmaceutical compositions comprising such compounds.
Applicant(s) Dr. Reddy'S Laboratories Ltd
Representative Drug(s) D0DN3Q Drug Info IC50 < 50 nM [2]
Patent ID WO2013074518
Title Modulating Certain Tyrosine Kinases.
Abstract The present invention provides therapeutic and diagnostic modalities relevant to treating disorders associated with tyrosine kinase actvity.
Applicant(s) Tesaro, Inc
Representative Drug(s) D0T3TZ Drug Info IC50 < 3 nM [1]
Patent ID WO2013026021
Title Trka As A Target for Inhibiting App Cleavage and/or Progression of Alzheimer'S Disease.
Abstract In various embodiments method are provided for inhibiting (partially or fully) the C-terminal cleavage of APP resulting in the formation of APP-C31 peptide and APPneo (APP664) in a mammal. The methods typically involve administering or causing to be administered to the mammal a TrkA kinase inhibitor in an amount sufficient to reduce C-terminal cleavage of APP and production of a C31 peptide and/or APPneo. In certain embodiments the inhibitor comprises ADDN-1351 or a derivative thereof.
Applicant(s) Buck Institute for Research On Aging
Representative Drug(s) D06STX Drug Info IC50 = 700 nM [1]
Patent ID WO2012125667
Title Trka Kinase Inhibitors, Compositions and Methods Thereof.
Abstract The present invention is directed to pyridotriazole and benztriazole compounds of formula (I) (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0MZ7K Drug Info IC50 = 27 nM [2]
Patent ID WO2007022999
Title Polymer Conjugates of K-252A and Derivatives Thereof.
Abstract The present invention relates to novel polymer conjugates of K-252a and derivatives thereof and to their use for the preparation of a pharmaceutical composition useful for the prevention, alleviation and treatment of kinase-associated pathologies. In particular, the present invention relates to the prevention, alleviation and treatment of HMGB1-associated pathologies. In a particular aspect, the invention relates to the use of the novel polymer conjugates of K-252a and derivatives thereof in the preparation of a pharmaceutical composition useful for the prevention, alleviation and treatment of neurological disorders, neuropathies and neurodegenerative disorders of the central and peripheral nervous system. In a further preferred aspect, the invention relates to the use of the polymer conjugates in the preparation of a pharmaceutical composition useful for the prevention, alleviation and treatment of dermal pathologies, in particular dermal pathologies associated with an excessive keratinocyte proliferation, in particular psoriasis. In a still further aspect, the invention relates to the use of the polymer conjugates in the prevention, alleviation and treatment of NGF-related pain. More specifically, the present invention relates to a polymer conjugate of K-252a and derivatives thereof, wherein the polymer is polyethylene glycol or methoxy-polyethylene glycol formula (I).
Applicant(s) Creabilis Therapeutics Spa Traversa, et al
Patent ID WO2014053967
Title Pyrrolo[2,3-D]Pyrimidine Tropomyosin-Related Kinase Inhibitors.
Patent ID WO2015200341
Title Substituted Imidazo[1,2-A]Pyridine Compounds Useful for The Treatment of Pain.
Abstract The present application relates to a series of substituted imidazo[l,2-a]pyridine compounds of formula (I), pharmaceutically acceptable salts, pharmaceutically acceptable solvates or stereoisomers thereof, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.
Applicant(s) Dr. Reddy'S Laboratories Ltd
Representative Drug(s) D0WI7N Drug Info N.A. [2]
Patent ID WO2014152663
Title Crystalline forms of Tyrosine Kinase Inhibitors and Their Salts.
Abstract The invention relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzate, including the polymorphic form A, mixtures of the polymorphs, process for the preparation thereof and the use thereof in a pharmaceutical composition containing thereof.
Applicant(s) Mundipharma International Corporation Limited
Representative Drug(s) D02ETU Drug Info N.A. [2]
Patent ID WO2014078417
Title Pyrazolyl Urea, Thiourea, Guanidine and Cyanoguanidine Compounds As Trka Kinase Inhibitors.
Abstract Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
Applicant(s) Array Biopharma Inc
Representative Drug(s) D0BP9B Drug Info N.A. [1]
Patent ID WO2014078325
Title N-(Monocyclic Aryl),N'-Pyrazolyl-Urea, Thiourea, Guanidine and Cyanoguanidine Compounds As Trka Kinase Inhibitors.
Abstract Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
Applicant(s) Array Biopharma Inc
Representative Drug(s) D05NBR Drug Info N.A. [1]
Patent ID WO2014078322
Title Thiazolyl and Oxazolyl Urea, Thiourea, Guanidine and Cyanoguanidine Compounds As Trka Kinase Inhibitors.
Abstract Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
Applicant(s) Array Biopharma Inc
Representative Drug(s) D0JU4R Drug Info N.A. [1]
Patent ID WO2013088257
Title Substituted Heterocyclic Compounds As Tropomyosin Receptor Kinase A (Trka) Inhibitors.
Abstract The present application relates to a series of substituted pyrazolo[l,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.
Applicant(s) Dr. Reddy'S Laboratories Ltd
Representative Drug(s) D0V9ZJ Drug Info N.A. [2]
Patent ID WO2000043384
Title Aromatic Heterocyclic Compounds As Antiinflammatory Agents.
Abstract Disclosed are novel aromatic heterocyclic compounds of formula (I) wherein Ar1, Ar2, L, Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.
Applicant(s) Boehringer Ingelheim Pharmaceuticals, Inc
Patent ID WO2012116217
Title Compounds and Compositions As Trk Inhibitors.
Abstract The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity.
Applicant(s) Irm Llc
Patent ID WO2012034095
Title Compounds and Compositions As Trk Inhibitors.
Abstract The invention provides compounds of formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity. wherein: and the rest of the variables are as specified in the claims.
Applicant(s) Irm Llc
Patent ID WO2012034091
Title Imidazo [1, 2] Pyridazin Compounds and Compositions As Trk Inhibitors.
Abstract The invention provides compounds of formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity.
Applicant(s) Irm Llc
United States Patent and Trademark Office (USPTO)
Patent ID US20040002145
Title Crystal Structure of Liganded Cfms Kinase Domain.
Representative Drug(s) D0X9VS Drug Info N.A. [1]
References  Top
REF 1 Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part I.Expert Opin Ther Pat. 2017 Jun;27(6):733-751.
REF 2 Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part II.Expert Opin Ther Pat. 2017 Jul;27(7):831-849.

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