C07D333/24

FLUORESCENT SYSTEMS FOR BIOLOGICAL IMAGING AND USES THEREOF
20220347299 · 2022-11-03 ·

The invention discloses a dye sensitizer molecule taking triazole as a core and a preparation method of the dye sensitizer molecule. According to the dye molecule, a triazole ring is introduced to the design of a molecular structure, and the electronic absorption and transmission capability among D-pi-A dye molecules are greatly improved by substituting donors with different carbon chain lengths and receptors with triple bonds at the periphery, so that a novel triazole dye with high efficiency is obtained. The preparation method of the compound comprises: click chemical reaction, detrimethylsilyl reaction, Sonogashira coupling reaction and the like; and the prepared dye molecule can be applied to a dye-sensitive solar cell and can show favorable photoelectric conversion property so as to have wide application prospects on the aspects of energy development and utilization. In addition, the material also has liquid crystal property under a certain condition so as to also have a huge potential on the aspect of application to photoelectric devices.

FLUORESCENT SYSTEMS FOR BIOLOGICAL IMAGING AND USES THEREOF
20220347299 · 2022-11-03 ·

The invention discloses a dye sensitizer molecule taking triazole as a core and a preparation method of the dye sensitizer molecule. According to the dye molecule, a triazole ring is introduced to the design of a molecular structure, and the electronic absorption and transmission capability among D-pi-A dye molecules are greatly improved by substituting donors with different carbon chain lengths and receptors with triple bonds at the periphery, so that a novel triazole dye with high efficiency is obtained. The preparation method of the compound comprises: click chemical reaction, detrimethylsilyl reaction, Sonogashira coupling reaction and the like; and the prepared dye molecule can be applied to a dye-sensitive solar cell and can show favorable photoelectric conversion property so as to have wide application prospects on the aspects of energy development and utilization. In addition, the material also has liquid crystal property under a certain condition so as to also have a huge potential on the aspect of application to photoelectric devices.

PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
20220347176 · 2022-11-03 ·

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO.sub.2— or —SO.sub.2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.1 is H or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, C land alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.12R.sub.13, heteroaryl, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; and R.sub.9 is H, alkyl or halo; R.sub.10 and R.sub.11 are each independently H or alkyl; and R.sub.12 and R.sub.13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).

##STR00001##

PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
20220347176 · 2022-11-03 ·

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO.sub.2— or —SO.sub.2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.1 is H or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, C land alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.12R.sub.13, heteroaryl, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; and R.sub.9 is H, alkyl or halo; R.sub.10 and R.sub.11 are each independently H or alkyl; and R.sub.12 and R.sub.13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).

##STR00001##

Small molecule modulators of the BTB domain of Keap1

The present application relates to compounds of formula (I′) or formula (I), such as formula (Ia), and their pharmaceutical compositions/preparations. This application further relates to methods of treating or preventing neurodegenerative disorders, such as Alzheimer's disease (AD), Parkinson's disease (PD), Huntington disease (HD) and other CAG-triplet repeat (or polyglutamine) diseases, amyotrophic lateral sclerosis (ALS; Lou Gehrig's disease), diffuse Lewy body disease, chorea-acanthocytosis, primary lateral sclerosis, multiple sclerosis (MS), frontotemporal dementia, Friedreich's ataxia, acute head injury, and epilepsy (repression of microglia activation).

Opioid receptor modulators

Provided herein are opioid receptor modulators and pharmaceutical compositions comprising said compounds.

Opioid receptor modulators

Provided herein are opioid receptor modulators and pharmaceutical compositions comprising said compounds.

SMALL MOLECULE MODULATORS OF THE BTB DOMAIN OF KEAP1

The present application relates to compounds of formula (I′) or formula (I), such as formula (Ia), and their pharmaceutical compositions/preparations. This application further relates to methods of treating or preventing neurodegenerative disorders, such as Alzheimer's disease (AD), Parkinson's disease (PD), Huntington disease (HD) and other CAG-triplet repeat (or polyglutamine) diseases, amyotrophic lateral sclerosis (ALS; Lou Gehrig's disease), diffuse Lewy body disease, chorea-acanthocytosis, primary lateral sclerosis, multiple sclerosis (MS), frontotemporal dementia, Friedreich's ataxia, acute head injury, and epilepsy (repression of microglia activation).

L-PAG DERIVATIVES FOR TREATMENT OF SLEEP DISORDERED BREATHING (SDB)

Described herein are novel γ- and δ-propargyl carboxylic acids and esters. The novel compositions are antagonists of CSE and may be used to modulate of the activity of the carotid body, therefore providing therapeutic benefits for sleep-related breathing disorders and related conditions.

L-PAG DERIVATIVES FOR TREATMENT OF SLEEP DISORDERED BREATHING (SDB)

Described herein are novel γ- and δ-propargyl carboxylic acids and esters. The novel compositions are antagonists of CSE and may be used to modulate of the activity of the carotid body, therefore providing therapeutic benefits for sleep-related breathing disorders and related conditions.