58009-66-8Relevant academic research and scientific papers
Discovery of clinical candidate (1 R,4 r)-4-((R)-2-((S)-6-Fluoro-5 H-imidazo[5,1-A[isoindol-5-yl)-1-hydroxyethyl)cyclohexan-1-ol (Navoximod), a potent and selective inhibitor of indoleamine 2,3-dioxygenase 1
Kumar, Sanjeev,Waldo, Jesse P.,Jaipuri, Firoz A.,Marcinowicz, Agnieszka,Van Allen, Clarissa,Adams, James,Kesharwani, Tanay,Zhang, Xiaoxia,Metz, Richard,Oh, Angela J.,Harris, Seth F.,Mautino, Mario R.
, p. 6705 - 6733 (2019/08/20)
A novel class of 5-substituted 5H-imidazo[5,1-a]isoindoles are described as potent inhibitors of indoleamine 2,3-dioxygenase 1 (IDO1). A structure-based drug design approach was used to elaborate the 5H-imidazo[5,1-a]isoindole core and to improve potency and pharmacological properties. Suitably placed hydrophobic and polar functional groups in the lead molecule allowed improvement of IDO1 inhibitory activity while minimizing off-target liabilities. Structure-activity relationship studies focused on optimizing IDO1 inhibition potency and a pharmacokinetic profile amenable to oral dosing while controlling CYP450 and hERG inhibitory properties.
DERIVATIVES OF PYRROLOIMIDAZOLE OR ANALOGUES THEREOF WHICH ARE USEFUL FOR THE TREATMENT OF INTER ALIA CANCER
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Page/Page column 100; 101, (2017/12/28)
Present invention relates to novel heterocyclic compounds as indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) modulators. Compounds of the present invention inhibit tryptophan degradation by modulating IDO and/or TDO. Formula (I) The invention further relates to the process of their preparation, pharmaceutical composition and their use in modulating the activity of indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3- dioxygenase (TDO). The compounds of the invention can be used alone or in combination for the treatment of conditions that benefits from the inhibition of tryptophan degradation.
COMPOUNDS FOR THE INHIBITION OF INDOLEAMINE-2,3-DIOXYGENASE
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Paragraph 0222-0223, (2016/04/09)
The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of IDO, and for the treatment of IDO-related disorders.
4H-IMIDAZO[1,5-A]INDOLE DERIVATIVES AND THEIR USE AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) AND/OR TRYPTOPHAN 2,3-DIOXYGENASE (TD02) MODULATORS
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Paragraph 00177, (2016/06/28)
This invention relates to novel compounds of formula (I) wherein wherein ?' is a 5 or 6 membered aryl or heteroaryl group, unsubstituted or substituted with 1, 2 or 3 groups as defined in claim 1; X is a bond or -(CRA1R81)n/sub
Use of certain prostaglandin analogues to treat glaucoma and ocular hypertension
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, (2008/06/13)
Certain prostaglandin analogues are useful in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandin analogues.
2,5,6,7-tetranor-4,8-inter-m-phenylene PGI2 derivatives
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, (2008/06/13)
Disclosed herein are novel prostaglandin I2 (PGI2) derivatives exhibiting excellent in vivo duration and activities, said derivatives being represented by the general formula: STR1 wherein R1, X, R2 and R3 are as defined herein.
15-Cycloaliphatic derivatives of 13,14-didehydro-carboprostacyclins and process for their preparation
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, (2008/06/13)
13, 14 didehydro-15 cyclic prostacyclins have been prepared.
9-Substituted carbacyclin analogs
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, (2008/06/13)
Novel compounds of the following formula: STR1
9-Substituted carbacyclin analogs
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, (2008/06/13)
Novel compounds of the following general formula: STR1
9-Substituted carbacyclin analogs
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, (2008/06/13)
Novel compounds of the following general formula: STR1
