1383446-28-3Relevant academic research and scientific papers
INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7)
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, (2018/02/28)
The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
Janus kinase inhibitor synthesis and use
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Paragraph 0044; 0045, (2016/10/08)
The formula (I) compound, wherein R1, R2 and Y defined in the formula, the compounds are inhibitors of Janus kinase (JAK), itself as immunosuppressants, can be used in organ transplantation, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, type
Design and optimization of selective protein kinase C θ (PKCθ) inhibitors for the treatment of autoimmune diseases
Jimenez, Juan-Miguel,Boyall, Dean,Brenchley, Guy,Collier, Philip N.,Davis, Christopher J.,Fraysse, Damien,Keily, Shazia B.,Henderson, Jaclyn,Miller, Andrew,Pierard, Francoise,Settimo, Luca,Twin, Heather C.,Bolton, Claire M.,Curnock, Adam P.,Chiu, Peter,Tanner, Adam J.,Young, Stephen
supporting information, p. 1799 - 1810 (2013/04/24)
Protein kinase C θ (PKCθ) has a central role in T cell activation and survival; however, the dependency of T cell responses to the inhibition of this enzyme appears to be dictated by the nature of the antigen and by the inflammatory environment. Studies in PKCθ-deficient mice have demonstrated that while antiviral responses are PKCθ-independent, T cell responses associated with autoimmune diseases are PKCθ-dependent. Thus, potent and selective inhibition of PKCθ is expected to block autoimmune T cell responses without compromising antiviral immunity. Herein, we describe the development of potent and selective PKCθ inhibitors, which show exceptional potency in cells and in vivo. By use of a structure based rational design approach, a 1000-fold improvement in potency and 76-fold improvement in selectivity over closely related PKC isoforms such as PKCδ were obtained from the initial HTS hit, together with a big improvement in lipophilic efficiency (LiPE).
INHIBITORS OF INFLUENZA VIRUSES REPLICATION
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, (2012/06/30)
Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
