1333384-43-2Relevant articles and documents
ANTI-HUMAN VISTA ANTIBODIES AND USE THEREOF
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, (2021/10/30)
The invention provides anti-VISTA antibody drug conjugates which may be used for targeted delivery of anti-inflammatory agents such as steroids to immune cells, e.g., myeloid cells. The invention also provides methods of using anti-VISTA antibody drug conjugates in the treatment of inflammatory and/or autoimmune conditions and/or for alleviating the toxicity of anti-inflammatory agents such as steroids.
Nitrogen-containing ring derivative regulator as well as preparation method and application thereof
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, (2021/05/12)
The invention relates to a nitrogen-containing ring derivative regulator as well as a preparation method and an application thereof. In particular, the present invention relates to a compound represented by general formula (I), a preparation method thereof, a pharmaceutical composition containing the compound, and an application of the compound as a G-protein coupled receptor modulator in the treatment or prevention of central nervous system diseases and/or mental diseases.
SSAO INHIBITORS AND USE THEREOF
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, (2021/05/07)
Provided are a compound of formula (I') or (I), a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of formula (I') or (I), and a method of treating or preventing a disease in which SSAO plays a role.
Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway
Alper, Phil B.,Betschart, Claudia,Buffet, David,Collignon Zipfel, Géraldine,Deane, Jonathan,Gordon, Perry,Hampton, Janice,Hawtin, Stuart,Ibanez, Maureen,Jiang, Tao,Junt, Tobias,Knoepfel, Thomas,Liu, Bo,Maginnis, Jillian,McKeever, Una,Michellys, Pierre-Yves,Mutnick, Daniel,Nayak, Bishnu,Niwa, Satoru,Richmond, Wendy,Rush, James S.,Syka, Peter,Zhang, Yi,Zhu, Xuefeng
supporting information, (2020/07/03)
Antagonism of the Toll-like receptors (TLRs) 7 and TLR8 has been hypothesized to be beneficial to patients suffering from autoimmune conditions. A phenotypic screen for small molecule antagonists of TLR7/8 was carried out in a murine P4H1 cell line. Compound 1 was identified as a hit that showed antagonistic activity on TLR7 and TLR8 but not TLR9, as shown on human peripheral blood mononuclear cells (hPBMCs). It was functionally cross reactive with mouse TLR7 but lacked oral exposure and had only modest potency. Chemical optimization resulted in 2, which showed in vivo efficacy following intraperitoneal administration. Further optimization resulted in 8 which had excellent in vitro activity, exposure and in vivo activity. Additional work to improve physical properties resulted in 15, an advanced lead that had favorable in vitro and exposure properties. It was further demonstrated that activity of the series tracked with binding to the extracellular domain of TLR7 implicating that the target of this series are endosomal TLRs rather than downstream signaling pathways.
COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF ENDOSOMAL TOLL-LIKE RECEPTORS
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Page/Page column 91, (2020/07/16)
The invention disclosed herein relates to 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridinyl compounds and 4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridinyl compounds of Formula (A), pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of autoimmune diseases.
IMIDAZOPYRROLOPYRIDINE AS INHIBITORS OF THE JAK FAMILY OF KINASES
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Page/Page column 119, (2018/07/05)
2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF ENDOSOMAL TOLL-LIKE RECEPTORS
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Page/Page column 63, (2018/03/28)
The invention disclosed herein relates to 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridinyl compounds and 4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridinyl compounds of Formula (A), pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of autoimmune diseases.
BRIDGED BICYCLIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Page/Page column 66, (2013/03/26)
Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.