3528-45-8Relevant academic research and scientific papers
Growth Factor Receptor antagonists. Preparation method and application thereof
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Paragraph 0133-0138, (2021/11/27)
The invention relates to a small molecule antagonist for transforming growth factor β receptors, a method for preparing the small molecule antagonist, and application of the small molecule antagonist in preparation of drugs. The small molecule antagonist for transforming the growth factor β receptor has the application of treating and/or preventing various diseases mediated by ALK5, and has great clinical application potential.
INHIBITORS OF BRUTON'S TYROSINE KINASE
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Page/Page column 108-109, (2018/06/06)
The present invention relates to a new compound of formula I: or pharmaceutically acceptable salt, solvate or stereoisomer thereof, wherein: V1 is C or N, V2 is C(R2) or N, whereby if V1 is C then V2 is N, if V1 is C then V2 is C(R2), or if V1 is N then V2 is C(R2); each n, k is independently 0, 1; each R2, R11 is independently H, D, Hal, CN, NR'R", C(O)NR'R", C1-C6 alkoxy; R3 is H, D, hydroxy, C(O)C1-C6 alkyl, C(O)C2-C6 alkenyl, C(O)C2-C6 alkynyl, C1-C6 alkyl; R4 is H, Hal, CN, CONR'R", hydroxy, C1-C6 alkyl, C1-C6 alkoxy; L is CH2, NH, O or chemical bond; R1 is selected from the group of the fragments, comprising: Fragment 1, Fragment 2, Fragment 3 each A1, A2, A3, A4 is independently CH, N, CHal; each A5, A6, A7, A8, A9 is independently C, CH or N; R5 is H, CN, Hal, CONR'R", C1-C6 alkyl, non-substituted or substituted by one or more halogens; each R' and R" is independently selected from the group, comprising H, C1-C6 alkyl, C1-C6 cycloalkyl, aryl; R6 is selected from the group: [formula II] each R7, R8, R9, R10 is independently vinyl, methylacetylenyl; Hal is CI, Br, I, F, which have properties of inhibitor of Bruton's tyrosine kinase (Btk), to pharmaceutical compositions containing such compounds, and their use as pharmaceuticals for treatment of diseases and disorder.
INHIBITORS OF BRUTON'S TYROSINE KINASE
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Paragraph 00558, (2016/01/25)
Disclosed herein are compounds that inhibit Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. 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.
THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
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Paragraph 0802; 0803, (2014/07/23)
The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
6-(4-HYDROXY-PHENYL)-1H-PYRAZOLO[3,4-B]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS
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, (2013/05/21)
The present invention relates to 1 H-pyrazolo[3,4-b]pyridine compounds of the formula (I) in which R1, R2, R3 and R4 are defined as indicated below. The compounds of the formula I are protein kinase C (PKC) inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
AMIDO-BENZYL SULFONE AND SULFOXIDE DERIVATIVES
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Page/Page column 132, (2013/09/12)
The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
PYRIDINYL AND PYRIMIDINYL SULFOXIDE AND SULFONE DERIVATIVES
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Page/Page column 83, (2013/09/12)
Disclosed are certain pyridinyl and pyrimidinyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds and methods of treatment using such compounds.
AMIDO SPIROCYCLIC AMIDE AND SULFONAMIDE DERIVATIVES
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Page/Page column 145, (2013/09/12)
Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5- carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT)
Zheng, Xiaozhang,Bair, Kenneth W.,Bauer, Paul,Baumeister, Timm,Bowman, Krista K.,Buckmelter, Alexandre J.,Caligiuri, Maureen,Clodfelter, Karl H.,Feng, Yezhen,Han, Bingsong,Ho, Yen-Ching,Kley, Nikolai,Li, Hong,Liang, Xiaorong,Liederer, Bianca M.,Lin, Jian,Ly, Justin,O'Brien, Thomas,Oeh, Jason,Oh, Angela,Reynolds, Dominic J.,Sampath, Deepak,Sharma, Geeta,Skelton, Nicholas,Smith, Chase C.,Tremayne, Jarrod,Wang, Leslie,Wang, Weiru,Wang, Zhongguo,Wu, Hongxing,Wu, Jiansheng,Xiao, Yang,Yang, Guangxing,Yuen, Po-Wai,Zak, Mark,Dragovich, Peter S.
supporting information, p. 5488 - 5497 (2013/10/01)
Potent, 1H-pyrazolo[3,4-b]pyridine-containing inhibitors of the human nicotinamide phosphoribosyltransferase (NAMPT) enzyme were identified using structure-based design techniques. Many of these compounds exhibited nanomolar antiproliferation activities a
AMIDO-BENZYL SULFONE AND SULFONAMIDE DERIVATIVES
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Page/Page column 61;62, (2013/09/12)
Disclosed are certain amido-benzyl sulfone and sulfonamide compounds, pharmaceutical compositions comprising such compounds, land methods of treatment using such compounds.
