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 T25005 Target Info
Target Name Tyrosine-protein kinase BTK (ATK)
Synonyms Bruton's tyrosine kinase; Bruton tyrosine kinase; BPK; B-cell progenitor kinase; B cell progenitor kinase; Agammaglobulinemia tyrosine kinase; Agammaglobulinaemia tyrosine kinase; AGMX1
Target Type Successful Target
Gene Name BTK
Biochemical Class Kinase
UniProt ID
BTK_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014022569
Title Treatment of Dry Eye.
Abstract The present disclosure provides a method of treating dry eye by inhibition of Bruton's tyrosine kinase (hereinafter "BTK") inhibitors, pharmaceutical formulations comprising the same, and processes for preparing such compounds.
Applicant(s) Principia Biopharma Inc
Representative Drug(s) D0V8JZ Drug Info IC50 = 1 nM Click to Show More [1]
2 D06ZNU Drug Info IC50 = 2 nM [1]
Patent ID WO2013191965
Title Reversible Covalent Pyrrolo- or Pyrazolopyrimidines Useful for The Treatment Cancer and Autoimmune Diseases.
Abstract Oral pharmaceutical formulations comprising reversible covalent compounds having a Michael acceptor moiety, a process of their production, and use of these formulations for the treatment of diseases treatable by such compounds such as cancer and autoimmune diseases.
Applicant(s) Principia Biopharma Inc
Representative Drug(s) D0V8JZ Drug Info IC50 = 1 nM Click to Show More [1]
2 D06ZNU Drug Info IC50 = 2 nM [1]
Patent ID WO2013157022
Title Substituted Hetero-Bicyclic Compounds, Compositions and Medicinal Applications Thereof.
Abstract The present disclosure provides hetero-biclyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by Bruton's tyrosine kinase (Btk) activity, The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.
Applicant(s) Advinus Therapeutics Limited
Representative Drug(s) D00KPQ Drug Info IC50 = 2 nM Click to Show More [1]
2 D0Q1BE Drug Info IC50 = 6 nM [1]
Patent ID WO2013102059
Title Pyrazolo [3, 4-D] Pyrimidine and Pyrrolo [2, 3-D] Pyrimidine Compounds As Kinase Inhibitors.
Abstract Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Applicant(s) PHARMACYCLICS, INC.
Representative Drug(s) D00KEX Drug Info IC50 < 100 nM Click to Show More [1]
2 D09TKO Drug Info IC50 < 100 nM [1]
Patent ID WO2012158764
Title Tyrosine Kinase Inhibitors.
Abstract The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
Applicant(s) Principia Biopharma Inc
Representative Drug(s) D0V8JZ Drug Info IC50 = 1 nM Click to Show More [1]
2 D06ZNU Drug Info IC50 = 2 nM [1]
Patent ID WO2013010136
Title Inhibitors of Bruton'S Tyrosine Kinase.
Abstract Described herein are kinase inhibitor compounds, methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase.
Applicant(s) PHARMACYCLICS, INC. CHEN, Wei LOURY, David, J. MODY, Tarak, D. WANG, Longcheng
Representative Drug(s) D0QW4H Drug Info IC50 < 100 nM Click to Show More [1]
2 D03ULH Drug Info N.A. [1]
Patent ID WO2015077866
Title Protein Kinase Inhibitors.
Abstract The present invention relates to a novel family of protein kinase inhibitors, more specifically the present invention is directed to inhibitors of the members of the Tec or Src protein kinase families. The present invention also relates to processes for the preparation of these compounds, to the pharmaceutical composition comprising them, and to their use in the treatment of proliferative, inflammatory, infectious or autoimmune diseases, disorder or condition in which protein kinase activity is implicated. More particularly, the present invention relates to a compound of Formula I.
Applicant(s) Pharmascience Inc
Representative Drug(s) D0IX7O Drug Info EC50 < 100 nM [1]
Patent ID WO2015058084
Title Heterocyclic Compounds and Methods of Use.
Abstract The present application discloses compounds that are inhibitors of Btk, compounds that are inhibitors of , and compounds that are dual inhibitors of both Btk and PI3K. Also described are methods for synthesizing such inhibitors and methods for using such inhibitors for the treatment of diseases wherein inhibition of Btk and PI3K provides a therapeutic benefit to a patient having the disease.
Applicant(s) Medivation Technologies, Inc
Representative Drug(s) D00GTY Drug Info IC50 = 4.2 nM [1]
Patent ID WO2015039613
Title Compound Inhibiting Kinase Activities of Btk and/or Jak3.
Abstract A compound capable of inhibiting kinase activities of BTK and/or JAK3, a pharmaceutical composition, and applications in preparing a medicament. The compound is as represented by structural formula I,.
Applicant(s) Beijing Hanmi Pharmaceutical Co., Ltd
Representative Drug(s) D0UH8J Drug Info IC50 < 50 nM [2]
Patent ID WO2015039612
Title Compound Inhibiting Kinase Activities of Btk and/or Jak3.
Abstract The present invention relates to a compound inhibiting the kinase activities of Bruton&#039;s tyrosine kinase (BTK) and/or Janus kinase 3 (JAK3), a pharmaceutical composition of the compound, pharmaceutica.
Applicant(s) Beijing Hanmi Pharmaceutical Co., Ltd
Representative Drug(s) D00BYK Drug Info IC50 < 50 nM [3]
Patent ID WO2015022926
Title Novel Fused Pyrimidine Compound or Salt Thereof.
Abstract The objective of the present invention is to provide a novel compound which has a BTK inhibitory action and a cytostatic effect. Additionally, the objective of the present invention is also to provide.
Applicant(s) Taiho Pharmaceutical Co., Ltd
Representative Drug(s) D0R9HP Drug Info IC50 = 0.836 nM [1]
Patent ID WO2014064131
Title Inhibitors of Bruton'S Tyrosine Kinase.
Abstract This application discloses compounds according to generic Formula I wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D05UXK Drug Info IC50 = 0.11 nM [1]
Patent ID WO2013157021
Title Bicyclic Compounds, Compositions and Medicinal Applications Thereof.
Abstract The present disclosure relates to a class of substituted bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts and pharmaceutical compositions containing them. The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.
Applicant(s) Advinus Therapeutics Limited
Representative Drug(s) D0WN2X Drug Info IC50 = 0.7 nM [1]
Patent ID WO2013118986
Title Triazolopyridine Derivatives As A Tyrosine Kinase Inhibitor.
Abstract Provided is a novel triazolopyridine derivative having irreversible tyrosine kinase inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of inflammatory diseases, autoimmune diseases, proliferative diseases or hyperproliferative diseases, immunologically mediated diseases, cancers or tumors.
Applicant(s) Hanmi Pharm Co., Ltd
Representative Drug(s) D0NK1R Drug Info IC50 = 73 nM [2]
Patent ID WO2013100631
Title Novel Imidazopyridine Derivatives As A Tyrosine Kinase Inhibitor.
Abstract Provided is a novel imidazopyridine derivative having irreversible tyrosine kinase inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of inflammatory diseases, autoimmune diseases, proliferative diseases or hyperproliferative diseases, immunologically mediated diseases, cancers or tumors.
Applicant(s) Hanmi Pharm. Co., Ltd
Representative Drug(s) D0P3UH Drug Info IC50 < 50 nM [2]
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 = 12 nM [2]
Patent ID WO2013010380
Title Btk Inhibitors.
Abstract Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0CG3V Drug Info IC50 < 10 nM [1]
Patent ID WO2013008095
Title Novel Pyrrolo Pyrimidine Derivatives.
Abstract The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.
Applicant(s) Novartis Ag
Representative Drug(s) D05YNZ Drug Info IC50 = 5 nM [1]
Patent ID WO2015089327
Title Biaryl Compounds Useful for The Treatment of Human Diseases In Oncology, Neurology and Immunology.
Abstract The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
Applicant(s) Biogen Ma Inc
Representative Drug(s) D0W3BE Drug Info N.A. [1]
Patent ID WO2014055928
Title Substituted N-(3-(Pyrimidin-4-Yl)Phenyl)Acrylamide Analogs As Tyrosine Receptor Kinase Btk Inhibitors.
Abstract In one aspect, the invention relates to substituted N-(3-(pyrimidin-4- yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Applicant(s) University of Utah Research Foundation
Representative Drug(s) D0J8UO Drug Info N.A. [1]
Patent ID WO2014025486
Title Novel Pyrrolopyrimidine Compounds As Inhibitors of Protein Kinases.
Abstract The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3(D835Y), ITK, JAKl, JAK2, JAK3, TEC and TXK) and/or the respective pathways.
Applicant(s) Acea Biosciences Inc
Representative Drug(s) D09IOW Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US2015064196
Title Substituted Hetero-Bicyclic Compounds, Compositions and Medicinal Applications Thereof.
Representative Drug(s) D0TI0R Drug Info IC50 = 4 nM [1]
European Patent Office (EPO)
Patent ID EP3042903
Title Substituted Hetero-Bicyclic Compounds, Compositions and Medicinal Applications Thereof.
Representative Drug(s) D0SR0U Drug Info N.A. [1]
Intellectual Property Office of United Kingdom (IPOUK)
Patent ID GB2515785
Title Compounds.
Representative Drug(s) D0Q8LH Drug Info IC50 < 15 nM [1]
References  Top
REF 1 Pyrrolo[2,3-d]pyrimidines active as Btk inhibitors.Expert Opin Ther Pat. 2017 Dec;27(12):1305-1318.
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 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.

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