- HPK1 ANTAGONISTS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.
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Paragraph 1316; 1317
(2021/03/19)
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- COMPOUNDS MODULATING PROTEIN RECRUITMENT AND/OR DEGRADATION
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The invention provides cereblon binders for the degradation of proteins by the ubiquitin proteasome pathway for therapeutic applications.
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Paragraph 0407; 0408
(2021/06/26)
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- PYRROLIDINE-3-YLACETIC ACID DERIVATIVE
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A compound represented by formula (1) or a pharmaceutically acceptable salt thereof has an inhibitory effect in the fractalkine-CX3CR1 pathway: wherein R represents a C1-6 alkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, a C3-8 cycloalkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, or a C3-8 cycloalkenyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, X represents a C1-6 alkyl group, Y and Z are the same or different from each other and each represents a halogen atom or a C1-6 alkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group B, n represents 0 or 1, Substituent Group A consists of halogen atoms, and Substituent Group B consists of halogen atoms.
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Paragraph 0214
(2014/08/06)
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- PYRROLIDIN-3-YLACETIC ACID DERIVATIVE
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A compound represented by formula (1) or a pharmaceutically acceptable salt thereof has an inhibitory effect in the fractalkine-CX3CR1 pathway: wherein R represents a C1-6 alkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, a C3-8 cycloalkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, or a C3-8 cycloalkenyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, X represents a C1-6 alkyl group, Y and Z are the same or different from each other and each represents a halogen atom or a C1-6 alkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group B, n represents 0 or 1, Substituent Group A consists of halogen atoms, and Substituent Group B consists of halogen atoms.
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Paragraph 0336; 0337
(2013/03/28)
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- Isosteric analogs of lenalidomide and pomalidomide: Synthesis and biological activity
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A series of analogs of the immunomodulary drugs lenalidomide (1) and pomalidomide (2), in which the amino group is replaced with various isosteres, was prepared and assayed for immunomodulatory activity and activity against cancer cell lines. The 4-methyl and 4-chloro analogs 4 and 15, respectively, displayed potent inhibition of tumor necrosis factor-α (TNF-α) in LPS-stimulated hPBMC, potent stimulation of IL-2 in a human T cell co-stimulation assay, and anti-proliferative activity against the Namalwa lymphoma cell line. Both of these analogs displayed oral bioavailability in rat.
- Ruchelman, Alexander L.,Man, Hon-Wah,Zhang, Weihong,Chen, Roger,Capone, Lori,Kang, Jian,Parton, Anastasia,Corral, Laura,Schafer, Peter H.,Babusis, Darius,Moghaddam, Mehran F.,Tang, Yang,Shirley, Michael A.,Muller, George W.
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p. 360 - 365
(2013/02/23)
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- THIAZOLOPYRIMIDINONE DERIVATIVES AS PI3 KINASE INHIBITORS
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This invention relates to the use of thiazolopyrimidinone derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3' OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ
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Page/Page column 42
(2010/12/18)
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- ARYL FLUOROETHYL UREAS ACTING AS ALPHA 2 ADRENERGIC AGENTS
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The invention provides well-defined aryl fluoroethyl ureas that are useful as selective alpha2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of alpha2 adrenergic receptors.
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Page/Page column 22
(2008/12/07)
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- COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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This invention relates to compounds of the Formula (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-α or combinations thereof.
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Page/Page column 559
(2010/02/15)
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- TETRAHYDROISOQUINOLINE OR ISOCHROMAN COMPOUNDS AS ORL-1 RECEPTOR LIGANDS FOR THE TREATMENT OF PAIN AND CNS DISORDERS
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This invention provides the compounds of formula (I), or its a pharmaceutically acceptable ester or amide of such compound, or a pharmaceutically acceptable salt thereof, wherein X1 is NH; R1, R2, R4 through Rs
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Page/Page column 68-69
(2010/02/10)
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- ISOQUINOLINONE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
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This invention is directed to isoquinolinone derivatives and their use in modulating the activity of orphan nuclear receptors, pharmaceutical compositions containing such derivatives, and methods of using such derivatives in treating disease-states associ
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- ENDOTHELIN RECEPTOR ANTAGONISTS
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Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
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Page column 24
(2008/06/13)
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- ENDOTHELIN RECEPTOR ANTAGONISTS
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Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
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