Patent(s) and the Corresponding Patented Drug(s) |
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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) |
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) |
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 |
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[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 |
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[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) |
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 |
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[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 |
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'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 |
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 |
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] |