C07D239/06

CHIRAL 1,3-DIARYLIMIDAZOLIUM SALT CARBENE PRECURSOR, SYNTHESIS METHOD THEREFOR, METAL SALT COMPOUND AND APPLICATION THEREOF
20200369620 · 2020-11-26 ·

Chiral 1, 3-diarylimidazole salt carbene precursors, their methods of preparation, particularly transition metal complexes and their use in chemical synthesis are provided. In particular, an air and moisture stable chiral 1, 3-diarylimidazole carbene precursor Cu (I) complex has been prepared and applied to highly regio- and enantioselective Markovnikov hydroboration of unactivated terminal alkenes to form chiral boronic esters. Moreover, these new chiral NHCs can be potentially applied in various metal-catalyzed asymmetric transformations.

##STR00001##

Spiroheptane salicylamides and related compounds as inhibitors of ROCK

The present invention provides compounds of Formula (I): ##STR00001##
or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

Spiroheptane salicylamides and related compounds as inhibitors of ROCK

The present invention provides compounds of Formula (I): ##STR00001##
or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

PHENYL IMIDAZOLINE COMPOUND HAVING AMINOMETHYL GROUP OR SALT THEREOF, OR PHENYL TETRAHYDROPYRIMIDINE COMPOUND HAVING AMINOMETHYL GROUP OR SALT THEREOF, AND PRODUCTION METHOD FOR SUCH COMPOUNDS OR SALTS THEREOF

In order to provide a novel phenyl imidazoline compound having an aminomethyl group, a novel phenyl tetrahydropyrimidine compound having an aminomethyl group, or the like, a compound according to the present invention or a salt thereof is represented by the following formula (1):

##STR00001## wherein R.sub.1 and R.sub.2 each independently represent hydrogen or a substituent selected from the group consisting of an alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, an aryloxy group having 6 to 10 carbon atoms, a hydroxyl group, an amide group, and a halogen atom; and n is an integer of 1 or 2.

PHENYL IMIDAZOLINE COMPOUND HAVING AMINOMETHYL GROUP OR SALT THEREOF, OR PHENYL TETRAHYDROPYRIMIDINE COMPOUND HAVING AMINOMETHYL GROUP OR SALT THEREOF, AND PRODUCTION METHOD FOR SUCH COMPOUNDS OR SALTS THEREOF

In order to provide a novel phenyl imidazoline compound having an aminomethyl group, a novel phenyl tetrahydropyrimidine compound having an aminomethyl group, or the like, a compound according to the present invention or a salt thereof is represented by the following formula (1):

##STR00001## wherein R.sub.1 and R.sub.2 each independently represent hydrogen or a substituent selected from the group consisting of an alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, an aryloxy group having 6 to 10 carbon atoms, a hydroxyl group, an amide group, and a halogen atom; and n is an integer of 1 or 2.

AMIDINE CATALYST FOR CURABLE COMPOSITIONS
20200231548 · 2020-07-23 · ·

The present invention relates to an amidine of the formula (I) and its use as a catalyst for crosslinking a curable composition. The amidine of the formula (I) contains at least one aliphatic amidine group. It is substantially odorless and nonvolatile at room temperature and accelerates the crosslinking of curable compositions very efficiently, without impairing the storage stability of the compositions. It is particularly suitable for compositions based on polymers containing silane groups, with which it is compatible, as a result of which such compositions do not have a tendency to separation or migration or evaporation of the catalyst.

AMIDINE CATALYST FOR CURABLE COMPOSITIONS
20200231548 · 2020-07-23 · ·

The present invention relates to an amidine of the formula (I) and its use as a catalyst for crosslinking a curable composition. The amidine of the formula (I) contains at least one aliphatic amidine group. It is substantially odorless and nonvolatile at room temperature and accelerates the crosslinking of curable compositions very efficiently, without impairing the storage stability of the compositions. It is particularly suitable for compositions based on polymers containing silane groups, with which it is compatible, as a result of which such compositions do not have a tendency to separation or migration or evaporation of the catalyst.

Inhibitors of creatine transport and uses thereof
10717704 · 2020-07-21 · ·

This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

Inhibitors of creatine transport and uses thereof
10717704 · 2020-07-21 · ·

This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

GEM-DISUBSTITUTED PYRROLIDINES, PIPERAZINES, AND DIAZEPANES, AND COMPOSITIONS AND METHODS OF MAKING THE SAME

Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of -substituted lactams, such as -lactams. The use of various electrophiles and ligands are described, and result in the construction of -quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).