862667-72-9Relevant academic research and scientific papers
HETEROCYCLIC INHIBITORS OF TEAD FOR TREATING CANCER
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Paragraph 0438; 0439; 0440; 0441, (2022/02/05)
The invention relates to compounds and methods of using said compounds, as well as pharmaceutical compositions containing such compounds, for treating diseases and conditions mediated by TEAD, such as cancer.
AMINOPYRIDINE COMPOUNDS AND METHODS FOR THE PREPARATION AND USE THEREOF
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Paragraph 0423, (2018/12/02)
The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A/B (Rgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I and Formula III, as described herein, and pharmaceutically acceptable salts thereof.
CONDENSED TRICYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Page/Page column 73, (2017/03/14)
There is provided compounds of formula I, (I) wherein R1, R2, R3 R4, R5, R6, R7a and R7b have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. CDK8 and/or Haspin kinase) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
AMINONITRILES AS KYNURENINE PATHWAY INHIBITORS
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Page/Page column 92; 93, (2014/09/29)
The present application provides novel kynurenine pathway inhibitors and pharmaceutically acceptable salts and prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in regulating the kynurenine pathway and the activity of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase by administering a therapeutically effective amount of one or more of the compounds of formula (I) to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the kynurenine pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by immunosuppression, abnormal cellular proliferation and/or inflammation. In one embodiment, the disease is cancer. In another embodiment, the disease is a viral infection. In a further embodiment, the disease is depression.
INHIBITORS OF THE KYNURENINE PATHWAY
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Page/Page column 161; 162; 164, (2014/12/12)
The present application provides novel inhibitors of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase, metabolites thereof, and phannaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. A therapeutically effective amount of one or more of the compounds of formula (I) is useful in treating diseases resulting from dysregulation of the kynurenine pathway. Compounds of formula (I) act by inhibiting the enzymatic activity or expression of indoleamine 2,3-dioxygenase-1 and/or indoleamine 2,3-dioxygenase-2 and/or tryptophan 2,3-dioxygenase.
Combining metallasupramolecular chemistry with dynamic covalent chemistry: Synthesis of large molecular cages
Granzhan, Anton,Riis-Johannessen, Thomas,Scopelliti, Rosario,Severin, Kay
supporting information; experimental part, p. 5515 - 5518 (2010/09/16)
(Figure Presented) Ru-built cube: By combining metallasupramolecular chemistry with dynamic covalent chemistry, complex nanostructures can be formed. Large cages are synthesized by reaction of trinuclear metallamacrocycles containing pendant aldehyde groups (see picture; Ru blue, aldehyde linkers green) with triamines (red).
N-benzyl-3,4-dihyroxypyridine-2-carboxamide and n-benzyl-2,3-dihydroxypyridine-4- carboxamide compounds useful as hiv integrase inhibitors
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Page/Page column 22, (2010/11/27)
N-Benzyl-dihydroxypyridine carboxamide compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dihydroxypyridine carboxamides are of Formula (I) wherein Q is Formula (II) or Formula (III); T is Formula (IV); and R1, R2, X1,X2,X3, and Y1 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
FUNGAL CELL WALL SYNTHESIS GENE
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, (2008/06/13)
A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed.Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.
