77111-77-4Relevant academic research and scientific papers
COMPOUNDS AS INHIBITORS OF MACROPHAGE MIGRATION INHIBITORY FACTOR
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, (2020/09/27)
The present invention provides compounds of Formula (I) shown above and their pharmaceutically acceptable salt, solvates, isomers, or prodrugs, as well as pharmaceutical compositions containing these compounds. Also provided by the invention is a method for treating a disorder mediated by macrophage migration inhibitory factor in a subject, comprising administering to the subject in need thereof a compound or a pharmaceutical composition of this invention.
COMPOSITIONS CONTAINING, METHODS AND USES OF ANTIBODY-TLR AGONIST CONJUGATES
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Paragraph 00636; 00647, (2020/08/28)
Disclosed herein are Trastuzumab-linked TLR-agonist derivative analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The Trastuzumab-linked TLR-agonist derivative analogs can includ
PURINE AND 3-DEAZAPURINE ANALOGUES AS CHOLINE KINASE INHIBITORS
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Page/Page column 116; 117, (2018/02/28)
There are provided substituted purine and 3-deazapurine analogues, which modulate the activity of Choline Kinase (ChoK). The compounds of this invention are therefore useful in treating diseases caused by an altered choline metabolism, such as cancer, cell proliferative disorders, infectious diseases of different origin, immune-related disorders and neurodegenerative disorders. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
ADENINE DERIVATIVES WHICH ARE USEFUL IN THE TREATMENT OF ALLERGIC DISEASES OR OTHER INFLAMMATORY CONDITIONS
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, (2016/06/13)
Compounds of formula (I).
Structural requirements for TLR7-selective signaling by 9-(4-piperidinylalkyl)-8-oxoadenine derivatives
Bazin, Hélène G.,Li, Yufeng,Khalaf, Juhienah K.,Mwakwari, Sandra,Livesay, Mark T.,Evans, Jay T.,Johnson, David A.
, p. 1318 - 1323 (2015/04/14)
We report the synthesis and biological evaluation of a new series of 8-oxoadenines substituted at the 9-position with a 4-piperidinylalkyl moiety. In vitro evaluation of the piperidinyl-substituted oxoadenines 3a-g in human TLR7- or TLR8-transfected HEK293 cells and in human PBMCs indicated that TLR7/8 selectivity/potency and cytokine induction can be modulated by varying the length of the alkyl linker. Oxoadenine 3f containing a 5-carbon linker was found to be the most potent TLR7 agonist and IFNα inducer in the series whereas 3b possessing a 1-carbon linker was the most potent TLR8 agonist.
NITROGEN CONTAINING HETEROCYCLIC COMPOUNDS AS PIK3 -DELTA INHIBITORS
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Page/Page column 60, (2012/01/15)
Substituted bicyclic heteroaryls of the following formulae and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory o
PROCESS FOR PREPARING ADENINE COMPOUNDS AND INTERMEDIATES THEREOF
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Page/Page column 22;23, (2012/02/05)
The present invention relates to a process for preparing a compound of Formula (III), or a salt thereof; wherein R1 is C1-6 alkyl; R2 and R3 are each independently hydrogen or C1-4 alkyl, or R2 and R3 combine together with the nitrogen atom to which they are attached to form a pyrrolidine ring, a morpholine ring, a piperidine ring, or a piperazine ring; and n is 1, 2 or 3.
6-AMINO-2-{ [ (1S)-1-METHYLBUTYL] OXY}-9-[5-(1-PIPERIDINYL)-7,9-DIHYDRO-8H-PURIN-8-ONE MALEATE
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, (2011/09/15)
A compound which is 6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one: Formula (I) in the form of a maleate salt, may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
PURINE DERIVATIVES AND THEIR PHARMACEUTICAL USES
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Page/Page column 20; 27, (2011/09/15)
Compounds of formula (I), wherein; R1 represents hydrogen or C1-3alkyl; n is an integer having a value of 1 to 5; X represents O or NH; Y represents C or N; or a pharmaceutically acceptable salt thereof, have been shown to be inducers of human interferon
PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES
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Page/Page column 41, (2010/04/03)
Compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; m is an integer having a value of 3, 4, or 5; n is an integer having a value of 0 to 3; p is an integer having a value of 1 or 2 and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
