39806-89-8Relevant academic research and scientific papers
BTK Inhibitors and uses thereof
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Paragraph 1619; 1628-1630, (2020/05/02)
The invention discloses a bruton's tyrosine kinase (BTK) inhibitor and use thereof. Specifically, the invention provides heteroaromatic compounds or stereoisomers, geometrical isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the heteroaromatic compounds; the invention also discloses use of the heteroaromatic compounds or the pharmaceutical compositions containing the heteroaromatic compounds in preparation of medicines; the medicines can be used for treating autoimmune diseases, inflammatory diseases or proliferative diseases.
PI3 KINASE INHIBITORS AND USES THEREOF
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Paragraph 00222, (2019/02/15)
Described herein are PI3 Kinase inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer, cardiovascular diseases, and inflammatory diseases.
Visible-Light-Induced [4+2] Annulation of Thiophenes and Alkynes to Construct Benzene Rings
Song, Chunlan,Dong, Xin,Wang, Zhongjie,Liu, Kun,Chiang, Chien-Wei,Lei, Aiwen
supporting information, p. 12206 - 12210 (2019/07/31)
The [4+2] annulation represents an elegant and versatile synthetic protocol for the construction of benzene rings. Herein, a strategy for visible-light induced [4+2] annulation of thiophenes and alkynes, to afford benzene rings, is presented. Under simple and mild reaction conditions, the ready availability and structural diversity of thiophenes and alkynes permit the facile synthesis of several substituted aromatic rings. Valuable drugs and amino acids are also well tolerated. Moreover, DFT calculations explain the high regioselectivity of the reaction.
Deprotonation of 4-ethynylpyrazolium salts
Ahlburg, Nils Lennart,Doppleb, Olivia,Hillrichs, Kai,Namyslo, Jan C.,Hübner, Eike G.,Schmidt, Andreas
, p. 1203 - 1215 (2018/08/06)
4-Ethynyl-1,2-dimethylpyrazolium salts were prepared by methylation of the corresponding 4-ethynyl-1-methylpyrazoles with trimethyloxonium tetrafluoroborate and were deprotonated to give the corresponding pyrazolium-4acetylenides, which are mesomeric betaines. These can be represented as alkynyl- or mesoionic allenylidene-type resonance forms. Calculations and spectroscopic investigations were performed to determine the contribution of each canonical form to the overall structure. Ylides and N-heterocyclic carbenes are tautomers of the betaines. Their relative stabilities have been compared.
COMPOUNDS, DEVICES, AND USES THEREOF
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Paragraph 00544, (2018/04/21)
The present invention provides compounds, e.g., compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are implantable elements (e.g., devices and materials) comprising the same, as well as methods of use thereof, e.g., for treating or preventing a disease, disorder, or condition.
SOLID FORMS OF ISOQUINOLINONE DERIVATIVES, PROCESS OF MAKING, COMPOSITIONS COMPRISING, AND METHODS OF USING THE SAME
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Paragraph 001137; 001143; 001149-001154; 001156, (2017/04/11)
Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphic forms, cocrystals, and amorphous forms thereof, and pharmaceutical compositions thereof.
HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Paragraph 00605, (2016/04/26)
Compounds of formula I' and formula II' and their pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity for the treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity.
PI3 kinase modulators and methods of use thereof, and use thereof
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Paragraph 0413; 0461; 0462, (2016/10/07)
The invention belongs to the field of medicines, concretely relates to a compound for treating cancer, a composition and an application of the composition and particularly relates to a PI3 kinase regulator as well as a use method and application of the PI3 kinase regulator. The invention provides a compound as shown in the formula (I), a pharmaceutically accepted salt of the compound and a pharmaceutical preparation of the compound, wherein the compound is used for regulating the activity of protein kinase and intercellular or intracellular signal response. The invention also relates to a pharmaceutical composition containing the compound and a method for treating high-proliferative diseases of mammals and particularly human beings by using the pharmaceutical composition as shown in the formula (I).
PI3 KINASE MODULATORS AND METHODS OF USE
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Paragraph 0176; 0188, (2014/02/16)
This invention relates to the field of lipid kinases and modulators thereof. In particular, the invention relates to modulators of phosphatidylinositol 3-kinases (PI3 kinases or PBKs) signaling pathways, and methods of their use. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in modulating of PI3K signaling pathways and their related disorders in mammals, especially humans.
Structure-based design of orally bioavailable 1 h -Pyrrolo[3,2- C ]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1)
Naud, Sébastien,Westwood, Isaac M.,Faisal, Amir,Sheldrake, Peter,Bavetsias, Vassilios,Atrash, Butrus,Cheung, Kwai-Ming J.,Liu, Manjuan,Hayes, Angela,Schmitt, Jessica,Wood, Amy,Choi, Vanessa,Boxall, Kathy,Mak, Grace,Gurden, Mark,Valenti, Melanie,De Haven Brandon, Alexis,Henley, Alan,Baker, Ross,McAndrew, Craig,Matijssen, Berry,Burke, Rosemary,Hoelder, Swen,Eccles, Suzanne A.,Raynaud, Florence I.,Linardopoulos, Spiros,Van Montfort, Rob L. M.,Blagg, Julian
, p. 10045 - 10065 (2014/01/17)
The protein kinase MPS1 is a crucial component of the spindle assembly checkpoint signal and is aberrantly overexpressed in many human cancers. MPS1 is one of the top 25 genes overexpressed in tumors with chromosomal instability and aneuploidy. PTEN-defic
