C07C235/60

METHOD FOR PREPARING BENZOIC ACID AMIDE COMPOUND

The present invention relates to a method for preparing a benzoic acid amide compound in a high yield by presenting a novel method for preparing a benzyl amine compound to be used as a reactant and delimiting the reaction condition of each step by using the same, and the method is economically advantageous since mass production is possible.

METHOD FOR PREPARING BENZOIC ACID AMIDE COMPOUND

The present invention relates to a method for preparing a benzoic acid amide compound in a high yield by presenting a novel method for preparing a benzyl amine compound to be used as a reactant and delimiting the reaction condition of each step by using the same, and the method is economically advantageous since mass production is possible.

Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors

A compound of formula (1a), (1b) or (1c) wherein: n is 1 or 2; R.sup.N is H or Me; R.sup.1 is optionally one or more halo or methyl groups; R.sup.2a and R.sup.2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.2c and R.sup.2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.3a and R.sup.3b are independently selected from H and Me; R.sup.4a is selected from OH, NH.sub.2, C(O)NH.sub.2, and CH.sub.2OH; R.sup.4b is either H or Me; R.sup.5 is either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C.sub.5-12 heteroaryl. ##STR00001##

Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors

A compound of formula (1a), (1b) or (1c) wherein: n is 1 or 2; R.sup.N is H or Me; R.sup.1 is optionally one or more halo or methyl groups; R.sup.2a and R.sup.2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.2c and R.sup.2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.3a and R.sup.3b are independently selected from H and Me; R.sup.4a is selected from OH, NH.sub.2, C(O)NH.sub.2, and CH.sub.2OH; R.sup.4b is either H or Me; R.sup.5 is either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C.sub.5-12 heteroaryl. ##STR00001##

PROLYL HYDROXYLASE INHIBITORS AND METHODS OF USE

The present disclosure relates to HIF-la prolyl hydroxylase inhibitors, compositions which comprise the HIF-la prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.

PROLYL HYDROXYLASE INHIBITORS AND METHODS OF USE

The present disclosure relates to HIF-la prolyl hydroxylase inhibitors, compositions which comprise the HIF-la prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.

Histone acetyltransferase modulators and uses thereof

The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.

Composition of 5-nitrobenzoate derivatives as anti-metastatic agent that inhibits tumor cell-induced platelet aggregation
09956191 · 2018-05-01 ·

Disclosed are 5-nitrobenzoate derivatives of Formula I, ##STR00001##
and the preparation method therefor, wherein R is referred to hydrogen (H), unsubstituted, mono-substituted, di-substituted or tri-substituted benzoyl moiety. 5-Nitrobenzoare derivatives of Formula I do not affect the platelet aggregation, possesses the inhibitory activity related to the tumor cell-induced platelet aggregation (TCIPA), and further specifically inhibits podoplanin-induced platelet aggregation. Therefore, 5-nitrobenzoates of the invention are applicable in its therapeutic use as the novel therapeutic agent in preventing tumor metastasis.

NOVEL CANNABIDIOL DERIVATIVE, METHOD FOR PREPARING SAME, AND COMPOSITION FOR COGNITIVE FUNCTION IMPROVEMENT COMPRISING SAME

Provided are a cannabidiol derivative, a method for preparing same, and a composition for cognitive function improvement comprising same, in which cannabidiol derivative exhibits acetylcholinesterase inhibitory activity and butyrylcholinesterase inhibitory activity, as well as inhibitory activity against monoamine oxidase B, therefore it is possible to simultaneously treat a decrease in acetylcholine levels in brain tissue and a decrease in blood butyrylcholine levels, which are seen in patients with dementia, and to provide a more effective cognitive function improvement treatment by preventing brain cell damage.

Complexes and ligands

The present application provides ligands and fluorescent or luminescent complexes comprising these ligands.