A61K31/5383

Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators

The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators, including their use for treating amyotrophic lateral sclerosis (ALS).

Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators

The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators, including their use for treating amyotrophic lateral sclerosis (ALS).

Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators

The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators, including their use for treating amyotrophic lateral sclerosis (ALS).

LIQUID FORMULATION COMPOSITIONS, MEDICAMENT DELIVERY DEVICES, AND METHODS OF PREPARATION AND USE THEREOF
20230147517 · 2023-05-11 ·

The invention provides liquid formulation compositions and medicament delivery devices, and methods for preparing and using the same. For example, the liquid formulation composition is an emulsion including a solvent and liquid particles, which includes surfactants and are dispersed in the solvent. The volume average particle size of the liquid particles is less than about 100 μm; the surface tension of the liquid formulation composition is less than about 60 mN/m; and the absolute value of zeta potential is greater than about 15 mV. The containment vessel may be a sprayer or a dropping device. The invention also provides methods for preparation of the liquid formulation compositions and medicament delivery devices as well as methods for using the same in treatment of various diseases and condition, for example, otitis media, otitis externa, rhinitis, sinusitis, lower respiratory tract inflammation, xerostomia (dry mouth), xerophthalmia (dry eyes) and xeromycteria (dry nose).

LIQUID FORMULATION COMPOSITIONS, MEDICAMENT DELIVERY DEVICES, AND METHODS OF PREPARATION AND USE THEREOF
20230147517 · 2023-05-11 ·

The invention provides liquid formulation compositions and medicament delivery devices, and methods for preparing and using the same. For example, the liquid formulation composition is an emulsion including a solvent and liquid particles, which includes surfactants and are dispersed in the solvent. The volume average particle size of the liquid particles is less than about 100 μm; the surface tension of the liquid formulation composition is less than about 60 mN/m; and the absolute value of zeta potential is greater than about 15 mV. The containment vessel may be a sprayer or a dropping device. The invention also provides methods for preparation of the liquid formulation compositions and medicament delivery devices as well as methods for using the same in treatment of various diseases and condition, for example, otitis media, otitis externa, rhinitis, sinusitis, lower respiratory tract inflammation, xerostomia (dry mouth), xerophthalmia (dry eyes) and xeromycteria (dry nose).

TRICYCLIC DLK INHIBITORS AND USES THEREOF

The invention relates to compounds of formula (I) and salts thereof:

##STR00001##

wherein ring A and R.sup.1-R.sup.2 have any of the values defined in the specification. The compounds and salts are useful for treating DLK mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as methods of using said compounds, salts, or compositions as DLK inhibitors and for treating neurodegeneration diseases and disorders.

TRICYCLIC DLK INHIBITORS AND USES THEREOF

The invention relates to compounds of formula (I) and salts thereof:

##STR00001##

wherein ring A and R.sup.1-R.sup.2 have any of the values defined in the specification. The compounds and salts are useful for treating DLK mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as methods of using said compounds, salts, or compositions as DLK inhibitors and for treating neurodegeneration diseases and disorders.

Targeted delivery of antimicrobial agents

A cationic antimicrobial peptide (CAMP) conjugate is disclosed. The CAMP conjugate may be made by identifying a suitable carrier peptide; identifying a suitable antimicrobial agent; creating a conjugate by conjugating the peptide with the antimicrobial agent; and evaluating and refining the conjugate. The peptide may be short peptide based on the sequence of a CAMP, such as human β-defensin-3. The peptide can be directly connected to the antimicrobial agent or through a linker segment. The antimicrobial agent may be connected to the peptide or the linker segment through stable or cleavable bonding. The peptide may carry and facilitate the delivery of the conjugated antimicrobial agent to a microbe.

Targeted delivery of antimicrobial agents

A cationic antimicrobial peptide (CAMP) conjugate is disclosed. The CAMP conjugate may be made by identifying a suitable carrier peptide; identifying a suitable antimicrobial agent; creating a conjugate by conjugating the peptide with the antimicrobial agent; and evaluating and refining the conjugate. The peptide may be short peptide based on the sequence of a CAMP, such as human β-defensin-3. The peptide can be directly connected to the antimicrobial agent or through a linker segment. The antimicrobial agent may be connected to the peptide or the linker segment through stable or cleavable bonding. The peptide may carry and facilitate the delivery of the conjugated antimicrobial agent to a microbe.

Bicyclic nitrogen-containing heterocyclic derivatives and pharmaceutical composition comprising the same

Provided are a novel compound having an antagonistic activity for the P2X.sub.7 receptor, and a pharmaceutical composition having an antagonistic activity for the P2X.sub.7 receptor. A compound represented by Formula (I): ##STR00001##
wherein Z.sup.1 is C(R.sup.4) or the like; R.sup.4 is a hydrogen atom or the like; Z.sup.2 is C(R.sup.5a)(R.sup.5a′) or the like; the dashed line represents the presence or absence of a bond; when the dashed line represents the presence of a bond, then R.sup.5a′ is absent; R.sup.5a and R.sup.5a′ are each independently a hydrogen atom or the like; Ring Q is a substituted or unsubstituted 5-membered non-aromatic heterocycle or the like; Y.sup.1 is O or the like; R.sup.2a is a group represented by the formula: —(C(R.sup.2a′)(R.sup.2b′)).sub.n—R.sup.1; R.sup.2b is a hydrogen atom or the like; R.sup.2a′ and R.sup.2b′ is each independently a hydrogen atom or the like; R.sup.1 is substituted or unsubstituted aromatic carbocyclyl or the like; X is N(R.sup.7a) or the like; R.sup.7a is a hydrogen atom or the like; R.sup.3 is substituted or unsubstituted aromatic carbocyclyl or the like; n is an integer from 0 to 4; and m is an integer from 0 to 4, or a pharmaceutically acceptable salt thereof.