850156-39-7Relevant academic research and scientific papers
INHIBITING USP36
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Paragraph 0152; 0157, (2020/11/13)
The present disclosure is directed to compounds of formulas (I) - (VI), which are useful as modulators of USP36. The compounds are further useful in the inhibition of USP36 and the treatment of diseases or disorders associated with the inhibition of USP36
A Dipolar Cycloaddition Reaction to Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate
Chrovian, Christa C.,Soyode-Johnson, Akinola,Peterson, Alexander A.,Gelin, Christine F.,Deng, Xiaohu,Dvorak, Curt A.,Carruthers, Nicholas I.,Lord, Brian,Fraser, Ian,Aluisio, Leah,Coe, Kevin J.,Scott, Brian,Koudriakova, Tatiana,Schoetens, Freddy,Sepassi, Kia,Gallacher, David J.,Bhattacharya, Anindya,Letavic, Michael A.
supporting information, p. 207 - 223 (2018/02/10)
A single pot dipolar cycloaddition reaction/Cope elimination sequence was developed to access novel 1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridine P2X7 antagonists that contain a synthetically challenging chiral center. The structure-activity relati
Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor
Swanson, Devin M.,Savall, Brad M.,Coe, Kevin J.,Schoetens, Freddy,Koudriakova, Tatiana,Skaptason, Judith,Wall, Jessica,Rech, Jason,Deng, Xiahou,De Angelis, Meri,Everson, Anita,Lord, Brian,Wang, Qi,Ao, Hong,Scott, Brian,Sepassi, Kia,Lovenberg, Timothy W.,Carruthers, Nicholas I.,Bhattacharya, Anindya,Letavic, Michael A.
, p. 8535 - 8548 (2016/10/03)
The synthesis and SAR of a series of 4,5,6,7-tetrahydro-imidazo[4,5-c]pyridine P2X7 antagonists are described. Addressing P2X7 affinity and liver microsomal stability issues encountered with this template afforded methyl substituted 4,5,6,7-tetrahydro-imidazo[4,5-c]pyridines ultimately leading to the identification of 1 (JNJ 54166060). 1 is a potent P2X7 antagonist with an ED50 = 2.3 mg/kg in rats, high oral bioavailability and low-moderate clearance in preclinical species, acceptable safety margins in rats, and a predicted human dose of 120 mg of QD. Additionally, 1 possesses a unique CYP profile and was found to be a regioselective inhibitor of midazolam CYP3A metabolism.
Concise preparation of a stable cyclic sulfamidate intermediate in the synthesis of a enantiopure chiral active diamine derivative
Rousseau, Jean-Francois,Chekroun, Isaac,Ferey, Vincent,Labrosse, Jean Robert
, p. 506 - 513 (2015/04/27)
A classical resolution was studied and developed from 2-benzoyl-pyridine in order to prepare SSR504734, a novel antipsychotic derivative. The key step of this route is the substitution of a sulfamidate derivative by a benzamide anion with complete inversi
P2X7 MODULATORS
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Paragraph 0209, (2014/09/29)
The present invention is directed to a compound of Formula (I): The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invent
P2X7 MODULATORS
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Paragraph 0284, (2014/09/29)
The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.
P2X7 MODULATORS
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Paragraph 0404; 0405; 0406, (2014/09/30)
The present invention is directed to a compound of Formula (I) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
PYRROLIDINE SUBSTITUTED FLAVONES FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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Page/Page column 33, (2011/09/30)
The present invention relates to the use of a compound of formula 1, a stereoisomer or a tautomer thereof, or a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, for the treatment of an inflammatory disorder. The invention further relates to a pharmaceutical composition comprising a compound of formula 1 and at least one pharmaceutically acceptable carrier, for use in the treatment of an inflammatory disorder. The invention also relates to a method for the treatment of an inflammatory disorder by administering a therapeutically effective amount of the compound of formula 1 to a subject in need thereof.
2-AZA-BICYCLO[2.2.2]OCTANE COMPOUNDS AND USES THEREOF
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Page/Page column 82, (2010/08/09)
This invention relates to 2-aza-bicyclo [2.2.2] octane compounds (and salts thereof), the process for making such a compound and pharmaceutical compositions comprising such a compound. The invention also relates to the use of the compounds for modulating
Novel Compounds 894
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Page/Page column 30, (2009/02/11)
The invention relates to 2-aza-bicyclo[2.2.2]octane compounds and uses thereof. Particularly the invention relates to such compounds and their uses as pharmaceuticals in treating pyshoses such as schizophrenia and other diseases, disorders, or conditions.
