85275-46-3Relevant academic research and scientific papers
PROTEIN DEGRADERS AND USES THEREOF
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Paragraph 00552; 00553, (2020/01/31)
The present invention provides compounds, compositions thereof, and methods of using the same for the targeted degradation of proteins, and the treatment of target protein-mediated disorders.
SMARCA DEGRADERS AND USES THEREOF
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Paragraph 00503-00504, (2020/12/30)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same for the modulation of one or more SWI/SNF-related matrix associated actin dependent regulator of chromatin subfamily A (SMARCA) and/o
Discovery and Evaluation of Pyrazolo[3,4-d]pyridazinone as a Potent and Orally Active Irreversible BTK Inhibitor
Zhang, Xuejun,Sheng, Xijun,Shen, Jie,Zhang, Shoubo,Sun, Wenjie,Shen, Chunli,Li, Yi,Wang, Jun,Lv, Huqiang,Cui, Minghui,Zhu, Yuchuan,Huang, Lei,Hao, Dongling,Qi, Zhibo,Sun, Guanglong,Mao, Weifeng,Pan, Yan,Shen, Liang,Li, Xin,Hu, Guoping,Gong, Zhen,Han, Shuhua,Li, Jian,Chen, Shuhui,Tu, Ronghua,Wang, Xuehai,Wu, Chengde
supporting information, p. 1863 - 1868 (2020/01/02)
The identification and lead optimization of a series of pyrazolo[3,4-d]pyridazinone derivatives are described as a novel class of potent irreversible BTK inhibitors, resulting in the discovery of compound 8. Compound 8 exhibited high potency against BTK kinase and acceptable PK profile. Furthermore, compound 8 demonstrated significant in vivo efficacy in a mouse-collagen-induced arthritis (CIA) model.
BENZOSULFONYL COMPOUNDS
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Paragraph 00343, (2019/03/12)
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
Therapeutic Combinations of a Proteasome Inhibitor and a BTK Inhibitor
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Paragraph 0472-0473, (2019/07/23)
Therapeutic combinations of a proteasome inhibitor and a Bruton's tyrosine kinase (BTK) inhibitor are described. In some embodiments, the invention provides pharmaceutical compositions comprising combinations of a proteasome inhibitor and a BTK inhibitor and methods of using the pharmaceutical compositions for treating a disease, in particular a cancer.
A N - propylene carbonyl piperidine derivatives for the preparation of
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Paragraph 0063; 0064; 0065, (2018/10/11)
The invention relates to a method for preparing an N-propylene carbonyl piperidine derivative, in particular to a new midbody for preparing ibrutinib, a preparation method of the new midbody and a method for preparing the ibrutinib, and belongs to the technical field of pharmacy. The method relates to a reaction as specified in the following formula (please see the specification for the formula). The method is easy to operate, capable of lowering cost and beneficial to industrial production.
Methods of Using BTK Inhibitors to Treat Dermatoses
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Paragraph 0428-0429, (2018/11/26)
In certain embodiments, the invention includes therapeutic methods of using a BTK inhibitor to treat dermatoses, such as psoriasis, atopic dermatitis, contact dermatitis, scleroderma, and cutaneous lupus erythematosus. In other embodiments, the methods of the invention further comprise the step of administering a therapeutically effective dose of an anti-inflammatory agent.
INHIBITOR OF BRUTON'S TYROSINE KINASE
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Paragraph 0137; 0138, (2017/03/28)
Provided are a compound represented by formula (III) or pharmaceutically acceptable salts, solvates, active metabolites, polymorphs, esters, tautomers or prodrugs thereof, pharmaceutical compositions containing the compound represented by formula (III), and the application of the pharmaceutical compositions as selective inreversible inhibitor of Bruton's tyrosine kinase for the prevention and treatment of inflammation, autoimmune diseases (such as rheumatoid arthritis) associated with aberrant B cell proliferation and cancers.
THERAPEUTIC COMBINATIONS OF A CD19 INHIBITOR AND A BTK INHIBITOR
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Paragraph 00416; 00417, (2017/04/08)
Therapeutic combinations of a CD 19 inhibitor and a Bruton's tyrosine kinase (BTK) inhibitor are described. In some embodiments, the invention provides pharmaceutical compositions comprising combinations of a CD 19 inhibitor and a BTK inhibitor and methods of using the pharmaceutical compositions for treating a disease, in particular a cancer, such as a hematological malignancy. A combination of a BTK inhibitor and a CD 19 inhibitor, such as a CD19-targeted antibody or a CD19-targeted chimeric antigen receptor expressing T cell or NK cell, and compositions and uses thereof are disclosed. Combinations of a BTK inhibitor and a CD 19 inhibitor with a programmed death- 1 (PD-1) or PD-1 ligand (PD-L1) inhibitor and compositions and uses thereof are also disclosed.
Therapeutic Combinations of an IRAK4 Inhibitor and a BTK Inhibitor
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Paragraph 0545; 0546, (2017/06/12)
Therapeutic combinations of an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor and a Bruton's tyrosine kinase (BTK) inhibitor are described. In some embodiments, the invention provides pharmaceutical compositions comprising combinations of an IRAK4 inhibitor and a BTK inhibitor, and methods of using the pharmaceutical compositions for treating a disease, in particular a cancer.
