156237-78-4Relevant academic research and scientific papers
Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology
Lu, Min,Zhang, Hongjun,Li, Derun,Childers, Matthew,Pu, Qinglin,Palte, Rachel L.,Gathiaka, Symon,Lyons, Thomas W.,Palani, Anandan,Fan, Peter W.,Spacciapoli, Peter,Miller, J. Richard,Cho, Hyelim,Cheng, Mangeng,Chakravarthy, Kalyan,O'Neil, Jennifer,Eangoor, Padmanabhan,Beard, Adam,Kim, Hai-Young,Saurí, Josep,Gunaydin, Hakan,Sloman, David L.,Siliphaivanh, Phieng,Cumming, Jared,Fischer, Christian
supporting information, p. 1380 - 1388 (2021/08/06)
Recent data suggest that the inhibition of arginase (ARG) has therapeutic potential for the treatment of a number of indications ranging from pulmonary and vascular disease to cancer. Thus, high demand exists for selective small molecule ARG inhibitors wi
ERK INHIBITOR AND USE THEREOF
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Paragraph 0098-0099, (2021/04/16)
Disclosed are a compound (as shown in formula I) as an extracellular signal-regulated kinase (ERK) inhibitor, a pharmaceutical composition thereof, a preparation method therefor, and use thereof in treating ERK-mediated diseases. Said compound plays a role by regulating a plurality of processes such as cell proliferation, apoptosis, migration and angiogenesis.
PRC1 INHIBITORS AND METHODS OF TREATMENT THEREWITH
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Page/Page column 94; 95, (2019/12/28)
Provided herein are small molecule inhibitors of Polycomb Repressive Complex 1 (PRC1) activity, and methods of use thereof for the treatment of disease, including leukemia and other cancers, as well as other diseases dependent on the activity of PRC1.
PYRROLOPYRAZINE DERIVATIVES AS ALPHA V INTEGRIN INHIBITORS
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Page/Page column 40-41, (2019/05/30)
The disclosure relates to compounds of formula I: Formula I which inhibit αv-containing integrins, and includes pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of αV-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders.
ARGINASE INHIBITORS AND METHODS OF USE
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Page/Page column 112, (2019/10/04)
Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.
PYRROLE AMIDES AS ALPHA V INTEGRIN INHIBITORS
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Page/Page column 69, (2018/05/27)
The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are inhibitors to αv-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of αv-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
FUSED QUADRACYCLIC COMPOUNDS, COMPOSITIONS AND USES THEREOF
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Paragraph 0185, (2017/08/01)
Provided herein are substituted fused quadracyclic compounds useful as inhibitors of MK2. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention also provides medical uses of substituted fused quadracyclic compounds.
NOVEL PYRROLE DERIVATIVES FOR THE TREATMENT OF CANCER
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Page/Page column 29, (2014/10/15)
The invention provides a method for the treatment of cancer, which method comprises the general formula (I) wherein R1, R2, R3, R4 and W are as described herein.
Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a] quinoxaline derivatives as inhibitors of the human protein kinase CK2
Guillon, Jean,Le Borgne, Marc,Rimbault, Charlotte,Moreau, Stéphane,Savrimoutou, Solène,Pinaud, No?l,Baratin, Sophie,Marchivie, Mathieu,Roche, Séverine,Bollacke, Andre,Pecci, Adali,Alvarez, Lautaro,Desplat, Vanessa,Jose, Joachim
, p. 205 - 222 (2013/10/01)
Herein we describe the synthesis and properties of substituted phenylaminopyrrolo[1,2-a]quinoxaline-carboxylic acid derivatives as a novel class of potent inhibitors of the human protein kinase CK2. A set of 15 compounds was designed and synthesized using
Oxidative radical cyclization of (ω-iodoalkyl)indoles and pyrroles. Synthesis of (-)-monomorine and three diastereomers
Artis,Cho,Jaime-Figueroa,Muchowski
, p. 2456 - 2466 (2007/10/02)
Addition of excess hydrogen peroxide (10 equiv) to a sonicated solution of FeSO4:7H2O (1 equiv) in DMSO containing the N-(ω-iodoalkyl)indoles 4, 5, 11, and 13 effected oxidative radical cyclization to 6, 7, 14, and 15, respectively. The (ω-iodoalkyl)pyrroles 21, 22, 27, 38, and 49 underwent analogous cyclization reactions to 23, 24, 28, 39, and 50, respectively. The regiochemistry of these radical cyclization reactions was correctly predicted by FMO calculations in all cases but one. For compound 38, FMO calculations indicated that radical attack should take place at both C-3 and C-5. Only the product of cyclization at C-5, i.e., 39, was observed. The enantiomerically pure bicyclic ketone 42, prepared by the above technique from the iodide 53, was converted into 55 which, on catalytic reduction (H2/Rh-Al2O3), gave a mixture of (-)-monomorine (40) and three of its diastereomers 56-58.
