Patent classifications
C07D273/02
Methods for reversing HIV latency using BAF complex modulating compounds
This disclosure provides methods of using BAF complex modulating compounds as inhibitors of BAF-mediated transcription in target cells. The BAF complex modulating compounds include 12-membered macrolactam compounds that can target a BAF-specific subunit (e.g., ARID1A) to prevent nucleosomal positioning, relieving transcriptional repression of HIV-1. The subject methods can provide for reversal of latency of HIV-1 in cells in vitro or in vivo. Use of the macrolactam BAF complex modulating compounds represent a method of HIV latency reversal with a unique mechanism of action, which can be optionally combined with other Latency Reversal Agents to improve reservoir targeting. The subject methods can be utilized in conjunction with any convenient methods of treating HIV or HIV latency, including methods related to immune system activation, antiretroviral therapies and/or anti-HIV agents.
CRYSTAL FORM OF OZANIMOD HYDROCHLORIDE, AND PREPARATION METHOD THEREFOR
The present disclosure relates to crystalline form CS3 of ozanimod hydrochloride which can be used for treating autoimmune diseases, particularly used for preparing drugs for treating multiple sclerosis and ulcerative colitis and preparation method thereof.
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CRYSTAL FORM OF OZANIMOD HYDROCHLORIDE, AND PREPARATION METHOD THEREFOR
The present disclosure relates to crystalline form CS3 of ozanimod hydrochloride which can be used for treating autoimmune diseases, particularly used for preparing drugs for treating multiple sclerosis and ulcerative colitis and preparation method thereof.
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RADIOFLUORINATED CARBOXIMIDAMIDES AS IDO TARGETING PET TRACER FOR CANCER IMAGING
Radiofluorinated carboximidamides are disclosed as selective IDO enzyme radioligands and generate specific binding in accordance with IDO expression in vitro. MicroPET experiments indicate [.sup.18F]IDO49 specifically accumulate in IDO-expressing tumors which confirmed by Western blot and IHC analysis supported. Using Hela tumor bearing models with IFN- treatment confirmed that [.sup.18F]IDO49 accumulation in the IFN- treatment tumor mouse. These results can have implications that [.sup.18F]IDO49 has substantial potential as an imaging agent that targets IDO in tumors.
MACROCYCLIC CHALCONE-AMIDE DERIVED ANTIVIRAL AGENTS
The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof:
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which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.
MACROCYCLIC CHALCONE-AMIDE DERIVED ANTIVIRAL AGENTS
The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof:
##STR00001##
which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.
Process for the preparation of raltegravir
The present invention provides a process for the preparation of crystalline anhydrous compound of Formula (X), Further, the present invention relates to the use of compound of Formula (X) preparation of Raltegravir (I) or its pharmaceutically acceptable salt thereof. ##STR00001##
Process for the preparation of raltegravir
The present invention provides a process for the preparation of crystalline anhydrous compound of Formula (X), Further, the present invention relates to the use of compound of Formula (X) preparation of Raltegravir (I) or its pharmaceutically acceptable salt thereof. ##STR00001##
MACROCYCLIC IMMUNOMODULATORS
Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I) or (II):
##STR00001## including stereoisomers and pharmaceutically acceptable salts thereof, wherein R, R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, R.sup.6c, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
PET probes of radiofluorinated carboximidamides for IDO-targeted imaging
.sup.18F labeled IDO1 imaging constructs are constructed for positron emission tomography (PET). Synthetic methodology involves the coupling of a 1-fluoro-2-halo-4-aminobenzene and a 4-mino-N-hydroxy-1,2,5-oxadiazole-3-carboximidoyl chloride wherein at least one of the coupled compounds comprises an .sup.18F. The .sup.18F labeled IDO1 imaging constructs are useful for imaging cancer cells in a patient.