425394-89-4Relevant academic research and scientific papers
Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors
Bajrami, Bekim,Bame, Eris,Gu, Chungang,Hoemberger, Marc,Hopkins, Brian T.,Huang, Jiansheng,Ma, Bin,Metrick, Claire M.,Mingueneau, Michael,Murugan, Paramasivam,Santoro, Joseph C.,Tang, Hao,Wang, Ti
supporting information, (2022/02/01)
BTK is a tyrosine kinase playing an important role in B cell and myeloid cell functions through B cell receptor (BCR) signaling and Fc receptor (FcR) signaling. Selective inhibition of BTK has the potential to provide therapeutical benefits to patients su
LPXC INHIBITOR AND METHODS OF MAKING
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Paragraph 00260; 00261, (2021/10/02)
Provided herein is an LpxC inhibitor compound, as well as methods of making and pharmaceutical compositions comprising said compound, and methods of use thereof in the treatment of disease that would benefit from treatment with an LpxC inhibitor, including gram-negative bacterial infections such as urinary tract infections and the like.
ANTIBACTERIAL COMPOUNDS
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Paragraph 00193, (2020/06/05)
Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting the growth of gram-negative bacteria. Furthermore, the subject compounds and compositions are useful for the treatment of bacterial infection, such as urinary tract infection and the like.
PYRAZOLYL COMPOUNDS AND METHODS OF USE THEREOF
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Paragraph 0633-0636, (2020/05/14)
Compounds having activity as chemotherapeutic agents are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R1a, R1b, R1c, R1d, L, and are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods for treating cancer (e.g., hematological cancers) are also provided.
ANTIBACTERIAL COMPOUNDS
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Paragraph 00178, (2018/12/02)
Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting the growth of gram-negative bacteria. Furthermore, the subject compounds and compositions are useful for the treatment of bacterial infection, such as urinary tract infection and the like.
NOVEL INHIBITORS OF MAP4K1
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Page/Page column 47, (2018/12/13)
The invention relates to novel inhibitors of MAP4K1 (HPK1) useful for the treatment of diseases or disorders characterised by dysregulation of the signal transduction pathways associated with MAPK activation, including hyperproliferative diseases, diseases of immune system dysfunction, inflammatory disorders, neurological diseases, and cardiovascular diseases. The invention further relates to pharmaceutical compositions comprising the same and methods of treatment of said diseases and disorders. The inhibitors are of formula (I) wherein the definitions for A, D, E, F, R5, R6, R7, Z, ring Q, n, x and y are as given in the application.
LABELED AMINO PYRIMIDINE DERIVATIVES
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Page/Page column 45, (2016/06/15)
The present invention describes novel radioactive amino pyrimidine derivatives, their preparation and their use as radiotracers / radiomarkers for imaging techniques and as diagnostic tools in the field of BTK receptor susceptible diseases and/or disorder
COMBINATION OF CHIMERIC ANTIGEN RECEPTOR THERAPY AND AMINO PYRIMIDINE DERIVATIVES
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Page/Page column 280, (2017/04/29)
The invention provides compositions and methods for treating diseases associated with expression of CD19, e.g., by administering a recombinant T cell comprising the CD19 CAR as described herein, in combination with a BTK inhibitor, e.g., an amino pyrimidi
NOVEL AMINO PYRIMIDINE DERIVATIVES
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Paragraph 0366; 0367; 0368, (2015/06/10)
The present invention describes new amino pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino 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.
NOVEL AMINO PYRIMIDINE DERIVATIVES
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Page/Page column 76; 77, (2015/06/11)
The present invention describes new amino pyrimidine derivatives of formula (I) and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino 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.
