- AZETIDINE DERIVATIVE, AND PRODRUG THEREOF
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An object of the present invention is to provide a compound useful as a therapeutic or prophylactic drug for a disease involving the immune system, by suppressing a function of immune cells by suppressing proliferation of activated T cells or suppressing production of interferon alpha (IFN-α) by activated plasmacytoid dendritic cells (pDC), particularly an autoimmune disease such as systemic lupus erythematosus (SLE) and lupus nephritis in SLE patients. The present invention provides a compound represented by general formula (I) : [wherein X, R1, R2, R3, R4, R5 and R6 are as described in the description], or a pharmaceutically acceptable salt thereof.
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Paragraph 0152; 0156
(2021/04/16)
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- RAS INHIBITORS
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The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.
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Paragraph 1288; 1293
(2021/05/07)
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- RAS INHIBITORS
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The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.
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Paragraph 1128-1129
(2021/05/07)
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- THERAPEUTIC COMPOUNDS FOR THE TREATMENT OF VIRAL INFECTIONS
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Compounds of formula I or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therape
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Paragraph 0221; 0222
(2014/07/23)
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- Functionalization of aromatic amino acids via direct C-H activation: Generation of versatile building blocks for accessing novel peptide space
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Functionalized α-amino acid building blocks have been prepared in good yield with high regiocontrol and preservation of stereochemistry via iridium-catalyzed borylation of suitably protected aromatic α-amino acid derivatives. The utility of these systems
- Meyer, Falco-Magnus,Liras, Spiros,Guzman-Perez, Angel,Perreault, Christian,Bian, Jianwei,James, Keith
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supporting information; experimental part
p. 3870 - 3873
(2010/11/05)
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- Macrocyclic Compounds Useful as Bace Inhibitors
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The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
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Page/Page column 45
(2008/12/05)
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- MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS
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The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
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Page/Page column 87
(2008/06/13)
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- SUBSTITUTED AMIDE BETA SECRETASE INHIBITORS
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Disclosed are novel compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula (I). Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula (I) and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula (I), HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
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Page/Page column 36
(2010/10/19)
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- MACROCYCLIC COMPOUNDS AND COMPOSITIONS USEFUL AS BACE INHIBITORS
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The invention relates to novel macrocyclic compounds of the formula in which R1, R3, V1, V2, X1, X2, Y, Z, Ar, AA and n are as defined in the specification, the number of ring atoms include
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Page/Page column 24
(2008/06/13)
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