102877-50-9Relevant articles and documents
Potent P2Y1 urea antagonists bearing various cyclic amine scaffolds
Ruel, Réjean,L'Heureux, Alexandre,Thibeault, Carl,Lapointe, Philippe,Martel, Alain,Qiao, Jennifer X.,Hua, Ji,Price, Laura A.,Wu, Qimin,Chang, Ming,Zheng, Joanna,Huang, Christine S.,Wexler, Ruth R.,Rehfuss, Robert,Lam, Patrick Y.S.
, p. 6825 - 6828 (2013)
A number of new amine scaffolds with good inhibitory activity in the ADP-induced platelet aggregation assay have been found to be potent antagonists of the P2Y1 receptor. SAR optimization led to the identification of isoindoline 3c and piperidine 4a which showed good in vitro binding and functional activities, as well as improved aqueous solubility. Among them, the piperidine 4a showed the best overall profile with favorable PK parameters.
Synthesis of substituted 5-aminomethyl tetrahydro-isoquinolines and dihydro-isoindoles
Fray, M. Jonathan,Allen, Paul,Bradley, Paul R.,Challenger, Clare E.,Closier, Michael,Evans, Tim J.,Lewis, Mark L.,Mathias, John P.,Nichols, Carly L.,Po-Ba, Yvonne M.,Snow, Hayley,Stefaniak, Mark H.,Vuong, Hannah V.
, p. 6869 - 6875 (2006)
The synthesis of ten substituted aminomethylene tetrahydro-isoquinolines is described, proceeding in eight steps from 5-hydroxyisoquinoline via reductive amination of N-Boc tetrahydro-isoquinoline 5-carboxaldehyde. Likewise, reductive amination was used to prepare four substituted dihydro-isoindoles from the corresponding aldehyde. The dihydro-isoindole ring system was conveniently accessed via a 2+2+2 cycloaddition reaction.
PRMT5 INHIBITORS AND USES THEREOF
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Paragraph 0455-0456, (2019/04/05)
Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
Preparation method of tetrahydroisoquinoline derivative
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Paragraph 0025; 0026, (2018/03/24)
The invention discloses a preparation method of a tetrahydroisoquinoline derivative which is N-Fmoc-1,2,3,4-tetrahydroisoquinoline-5-alcohol. The preparation method comprises the following steps: taking isoquinoline as a starting raw material, loading sulfonic acid groups, hydrolyzing, hydrogenating and carrying out Fmoc protection to obtain a target product. The compound is used as an important medical intermediate.
PRMT5 INHIBITORS CONTAINING A DIHYDRO- OR TETRAHYDROISOQUINOLINE AND USES THEREOF
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Paragraph 00353, (2014/07/08)
Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5- mediated disorders are also described.
Tetrahydroisoquinoline PPARγ agonists: Design of novel, highly selective non-TZD antihyperglycemic agents
Henry, James R.,Li, Yihong,Warshawsky, Alan M.,Brozinick, Joseph T.,Hawkins, Eric D.,Misener, Elizabeth A.,Briere, Daniel A.,Montrose-Rafizadeh, Chahrzad,Zink, Richard W.,Yumibe, Nathan P.,Ajamie, Rose T.,Wilken, Brad,Devanarayan, Viswanath
, p. 6293 - 6297 (2007/10/03)
Novel tetrahydroisoquinolines have been developed as potent PPAR ligands. Evaluation of these compounds in PPARγ responsive models of type 2 diabetes is described.
HETEROCYCLIC COMPOUNDS AS MODULATORS OF PEROXISOME PROLIFERATOR ACTIVATED RECEPTORS, USEFUL FOR THE TREATMENT AND/OR PREVENTION OF DISORDERS MODULATED BY A PPAR
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Page/Page column 196, (2010/02/11)
The present invention is directed to a compound of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.