C07F9/59

CYCLOPROPYLAMINES AS LSD1 INHIBITORS
20180000805 · 2018-01-04 ·

This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.

CYCLOPROPYLAMINES AS LSD1 INHIBITORS
20180000805 · 2018-01-04 ·

This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.

ANTISENSE COMPOUNDS AND USES THEREOF

The present disclosure provides oligomeric compounds. The present disclosure provides metabolically stable linkers that do not rapidly degrade in vivo. In certain embodiments, the present disclosure provides metabolically stable linkers for use in attaching a conjugate group to an oligonucleotide.

Inhibitors of the WNT/beta-catenin pathway

The present disclosure relates to compounds that are capable of modulating the WNT/Beta-Catenin pathway. The disclosure further relates to methods of treating colorectal cancer and other WNT/Beta-Catenin mediated cancers.

CHIRAL SYNTHESIS OF A TERTIARY ALCOHOL

Disclosed herein are methods for preparing tertiary alcohols from an optionally substituted phenyl ketone or an optionally substituted pyridinyl ketone that includes the use of a chiral ligand and boron trifluoride diethyl etherate. Tertiary alcohols can be used to prepare synthetic versions of natural products and/or pharmaceuticals.

CHIRAL SYNTHESIS OF A TERTIARY ALCOHOL

Disclosed herein are methods for preparing tertiary alcohols from an optionally substituted phenyl ketone or an optionally substituted pyridinyl ketone that includes the use of a chiral ligand and boron trifluoride diethyl etherate. Tertiary alcohols can be used to prepare synthetic versions of natural products and/or pharmaceuticals.

Benzimidazol derivatives for treating filovirus infection

The present invention relates to compounds comprising a benzimidazole scaffold, and the use of such compounds for the treatment of viral diseases. The invention also relates to pharmaceutical compositions comprising said compounds as an active ingredient. In particular the compounds of the invention comprising a benzimidazole scaffold are used for the treatment of filoviruses or retroviruses, and preferably for the treatment of Ebola virus or HIV virus.

THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF

The invention provides a compound of formula (I): or a salt thereof, wherein A, B, R.sup.1, R.sup.2, R.sup.3 and X have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as therapeutic agents for treating diastolic dysfunction.

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THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF

The invention provides a compound of formula (I): or a salt thereof, wherein A, B, R.sup.1, R.sup.2, R.sup.3 and X have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as therapeutic agents for treating diastolic dysfunction.

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MASP-2 inhibitors and methods of use

The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.