C07F9/65522

Heteroaryl compounds useful as inhibitors of SUMO activating enzyme

Disclosed are chemical entities which are compounds of formula (I): ##STR00001##
or pharmaceutically acceptable salts thereof; wherein Y, R.sup.a, R.sup.a, R.sup.b, R.sup.c, X.sub.1, X.sub.2, X.sub.3, R.sup.d, Z.sub.1, and Z.sub.2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.

Antioxidant compound having anti atherosclerotic effect and preparation thereof

The present invention relates to an antioxidant compound having anti atherosclerotic effect and preparation thereof. The present invention more particularly relates to the synthesis of TPP+ coupled esculetin (mitochondria-targeted esculetin [Mito-Esc]) followed by the biological evaluation of Mito-Esc for its ability to attenuate Angiotensin-II-induced atherosclerosis in apolipoproteinE knockout (ApoE.sup./ mice along with the endothelial cell age-delaying effects of Mito-Esc.

Prodrugs of tetrahydrocannabinol, compositions comprising prodrugs of tetrahydrocannabinol and methods of using the same

Described herein are ?.sup.9-THC prodrugs, methods of making ?.sup.9-THC prodrugs, formulations comprising ?.sup.9-THC prodrugs and methods of using ?.sup.9-THC. One embodiment described herein relates to the transdermal administration of a ?.sup.9-THC prodrug for treating and preventing diseases and/or disorders.

Modified ionic liquids containing bicyclophosphate moiety

A bicyclophosphate-modified ionic liquid compound, the synthesis thereof, an electrochemical electrolyte containing a bicyclophosphate-modified ionic liquid compound, and energy storage device containing the electrolyte are disclosed.

Stabilized CRISPR complexes

Provided herein are polynucleotides and CRISPR effector proteins configured to be covalently bound together in a CRISPR complex. The polynucleotides can be further modified to modulate the activity of the CRISPR complex. Modification of the polynucleotide and CRISPR effector protein can be used to improve the efficacy of target binding and/or cleavage.

TOCOPHEROL PHOSPHORIC ACID ESTER SALT, METHOD FOR MANUFACTURING THE SAME, AND SKIN EXTERNAL PREPARATION
20180086779 · 2018-03-29 · ·

A tocopherol phosphoric acid ester salt in which the tocopherol phosphoric acid ester salt is represented by Formula (1), and in the Formula (1), R1, R2, and R3 each independently represents a hydrogen atom or a methyl group, M represents an alkali metal, and a is 1.10 or more and 2.00 or less.

##STR00001##

Stabilized CRISPR Complexes

Provided herein are polynucleotides and CRISPR effector proteins configured to be covalently bound together in a CRISPR complex. The polynucleotides can be further modified to modulate the activity of the CRISPR complex. Modification of the polynucleotide and CRISPR effector protein can be used to improve the efficacy of target binding and/or cleavage.

PRODRUGS OF TETRAHYDROCANNABINOL COMPOSITIONS COMPRISING PRODRUGS OF TETRAHYDROCANNABINOL AND METHODS OF USING THE SAME

Described herein are .sup.9-THC prodrugs, methods of making .sup.9-THC prodrugs, formulations comprising .sup.9-THC prodrugs and methods of using .sup.9-THC. One embodiment described herein relates to the transdermal administration of a .sup.9-THC prodrug for treating and preventing diseases and/or disorders.

Functionalizing nanofibres
09814786 · 2017-11-14 ·

Methods of preparing a functionalized nanofiber preparing a dispersion of a polymer and a water soluble synthetic construct of the structure F-S-L in admixture in a liquid medium; and then electrospinning the polymer from the liquid medium to provide the functionalized nanofiber. F is the functional moiety, L is a lipid and S is a spacer linking F to L via covalent bonds.

SUBSTITUTED BICYCLIC COMPOUNDS

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):

##STR00001##

and/or a salt thereof, wherein R.sub.1 is OH or OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.