C07D495/10

NITROGEN CONTAINING HETEROCYCLES AS CDK12 INHIBITORS

Provided is a compound that may have a superior CDK12 inhibitory action and is expected to be useful as a prophylactic or therapeutic drug for cancer and the like. A compound represented by the following formula (I):

##STR00001##

wherein each symbol is as described in the DESCRIPTION, or a salt thereof.

Heteroaryl compounds as inhibitors of programmed necrosis pathway, composition and method using the same
20230121233 · 2023-04-20 ·

The present disclosure provides heteroaryl compounds of Formula I, processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from or related to the programmed necrosis pathway. Formula I is:

##STR00001##

PHOTOCHROMIC COMPOUND, PHOTOCHROMIC ARTICLE AND EYEGLASSES

The photochromic compound is represented by general formula (1):

##STR00001## wherein, X denotes an oxygen atom, or a nitrogen atom unsubstituted or substituted by a substituent selected from Y.sup.1 group: —R.sup.1, -A.sup.1(B.sup.1).sub.l(A.sup.2).sub.m(B.sup.2).sub.nR.sup.2, -A.sup.3A.sup.4, -A.sup.5R.sup.3 R.sup.1 denotes a cyano group or the like, R.sup.2 denotes an alkyl group or the like, R.sup.3 denotes a halogen atom or the like, A.sup.1, A.sup.2, A.sup.3, and A.sup.5 each independently denote an alkylene group or the like, A.sup.4 denotes a naphthyl group which may be substituted, B.sup.1 and B.sup.2 each independently denote a divalent group selected from the following group:

##STR00002## l, m, and n are each independently 0 or 1, provided that n is 0 when m is 0, Y.sup.2 denotes a hydrogen atom or the like, R denotes a hydrogen atom or the like, and

##STR00003##

denotes a norbornylidene group, a bicyclo[3.3.1]nonylidene group, or an adamantylidene group which may each be substituted.

PHOTOCHROMIC COMPOUND, PHOTOCHROMIC ARTICLE AND EYEGLASSES

The photochromic compound is represented by general formula (1):

##STR00001## wherein, X denotes an oxygen atom, or a nitrogen atom unsubstituted or substituted by a substituent selected from Y.sup.1 group: —R.sup.1, -A.sup.1(B.sup.1).sub.l(A.sup.2).sub.m(B.sup.2).sub.nR.sup.2, -A.sup.3A.sup.4, -A.sup.5R.sup.3 R.sup.1 denotes a cyano group or the like, R.sup.2 denotes an alkyl group or the like, R.sup.3 denotes a halogen atom or the like, A.sup.1, A.sup.2, A.sup.3, and A.sup.5 each independently denote an alkylene group or the like, A.sup.4 denotes a naphthyl group which may be substituted, B.sup.1 and B.sup.2 each independently denote a divalent group selected from the following group:

##STR00002## l, m, and n are each independently 0 or 1, provided that n is 0 when m is 0, Y.sup.2 denotes a hydrogen atom or the like, R denotes a hydrogen atom or the like, and

##STR00003##

denotes a norbornylidene group, a bicyclo[3.3.1]nonylidene group, or an adamantylidene group which may each be substituted.

ORGANIC COMPOUND AND APPLICATION THEREOF

Provided are an organic compound and an application thereof The organic compound of the present disclosure has a structure similar to a spiro ring. The structure can enable the compound to obtain relatively high thermal stability and a relatively high glass transition temperature Tg. The skeleton has an electron-donating ability, and a group having an electron withdrawing ability is linked to the skeleton so that the skeleton has the electron withdrawing ability, which is more conducive to the transport and recombination of electrons and holes in this region. The compound having the structure similar to the spiro ring also has suitable steric distortion and can reduce a molecular acting force and intermolecular stacking, which is conducive to reducing concentration quenching and efficiency roll-off and preparing an organic light-emitting diode (OLED) device. Therefore, the compound of the present disclosure also enables the device to achieve a longer lifetime.

ORGANIC COMPOUND AND APPLICATION THEREOF

Provided are an organic compound and an application thereof The organic compound of the present disclosure has a structure similar to a spiro ring. The structure can enable the compound to obtain relatively high thermal stability and a relatively high glass transition temperature Tg. The skeleton has an electron-donating ability, and a group having an electron withdrawing ability is linked to the skeleton so that the skeleton has the electron withdrawing ability, which is more conducive to the transport and recombination of electrons and holes in this region. The compound having the structure similar to the spiro ring also has suitable steric distortion and can reduce a molecular acting force and intermolecular stacking, which is conducive to reducing concentration quenching and efficiency roll-off and preparing an organic light-emitting diode (OLED) device. Therefore, the compound of the present disclosure also enables the device to achieve a longer lifetime.

GALACTOKINASE INHIBITORS

Described herein are compounds that inhibit galactokinase (GALK) and other kinases and methods for producing the same. Also described are methods for using Structure-Activity Relationships (SAR) to develop compounds with enhanced activity.

DELIVERY OF THERAPEUTIC ALKALOID COMPOUNDS
20230159455 · 2023-05-25 ·

Disclosed are prodrug compounds that can be converted to mesembrine under biologically relevant conditions, such as hydrolysis in vivo; and related methods of preparing and using these compounds. Stable preparations of isolated mesembrine stereoisomers are also provided.

DELIVERY OF THERAPEUTIC ALKALOID COMPOUNDS
20230159455 · 2023-05-25 ·

Disclosed are prodrug compounds that can be converted to mesembrine under biologically relevant conditions, such as hydrolysis in vivo; and related methods of preparing and using these compounds. Stable preparations of isolated mesembrine stereoisomers are also provided.

METHODS FOR THE PREPARATION OF 1,3-BENZODIOXOLE HETEROCYCLIC COMPOUNDS

The present invention relates to novel methods for the preparation of 1,3-benzodioxole heterocyclic compounds and intermediates for the same. The compounds are useful as PDE4 inhibitors.