164147-66-4Relevant academic research and scientific papers
TETRAHYDROISOQUINOLINE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
-
Page/Page column 95, (2017/11/06)
Described herein are tetrahydroisoquinoline compounds with estrogen receptor modulation activity or function having the Formula I structure: I and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
1,2,3,4-TETRAHYDROISOQUINOLINE COMPOUNDS AND COMPOSITIONS AS SELECTIVE ESTROGEN RECEPTOR ANTAGONISTS AND DEGRADERS
-
Paragraph 00328, (2015/07/07)
The present invention relates to compounds of formula (I) in which n, R1, R2, R3, R4and R5 are as defined in the claims; capable of being both potent antagonists and degraders of estrogen receptors. Also described is a process for the preparation of compounds of the invention, and the invention further provides pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.
Synthesis and initial evaluation of novel, non-peptidic antagonists of the αv-integrins αvβ3 and αvβ5
Letourneau, Jeffrey J.,Liu, Jinqi,Ohlmeyer, Michael H.J.,Riviello, Chris,Rong, Yajing,Li, Hong,Appell, Kenneth C.,Bansal, Shalini,Jacob, Biji,Wong, Angela,Webb, Maria L.
scheme or table, p. 352 - 355 (2011/03/18)
The discovery, synthesis and preliminary SAR of a novel class of non-peptidic antagonists of the αv-integrins αvβ3 and αvβ5 is described. High-throughput screening of an extensive series of ECLiPS com
NITROGEN HETEROCYCLE BIARYLS FOR OSTEOPOROSIS AND OTHER DISEASES
-
Page/Page column 52; 53, (2010/11/25)
Nitrogen heterocycle biaryls having a carboxylate terminus are useful for treating endometriosis, osteoporosis, restenosis following angioplasty, rheumatoid arthritis, cancer, macular degeneration and obesity. Compounds of formula: (I) are disclosed. A re
Nitrogen heterocycle biaryls for osteoporosis and other diseases
-
Page/Page column 19-20, (2010/02/14)
Nitrogen heterocycle biaryls having a carboxylate terminus are useful for treating endometriosis, osteoporosis, restenosis following angioplasty, rheumatoid arthritis, cancer, macular degeneration and obesity. Compounds of formula: are disclosed. A representative example is
Non-peptide RGD surrogates which mimic a Gly-Asp β-turn: Potent antagonists of platelet glycoprotein IIb-IIIa
Fisher, Matthew J.,Gunn, Bruce,Harms, Cathy S.,Kline, Allen D.,Mullaney, Jeffrey T.,Nunes, Anne,Scarborough, Robert M.,Arfsten, Ann E.,Skelton, Marshall A.,Um, Suzane L.,Utterback, Barbara G.,Jakubowski, Joseph A.
, p. 2085 - 2101 (2007/10/03)
Cyclic heptapeptide 1, which contains an Arg-Gly-Asp sequence, has good affinity for the platelet receptor GPIIb-IIIa and was chosen for study by 1H NMR techniques. The key RGD sequence of this molecule was found to reside in a conformationally defined type II' Gly-Asp β-turn, and this information was used in the design of simple non-peptide RGD mimics. Disubstituted isoquinolones, bearing an acidic side chain at position 2 and a basic side chain at position 6, were prepared and were found to have modest affinity for GPIIb-IIIa. Systematic modification of the basic residue contained in these molecules yielded compounds with high affinity for GPIIb-IIIa.
