Patent classifications
C07D333/20
PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
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).
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SULFUR AND AMIDE TROPOLONE INHIBITORS OF NUCLEOTIDYL TRANSFERASES AND USES THEREFOR
The present disclosure provides inhibitors of microorganisms including viruses and fungi of the formula (I) or (II) wherein the variables are defined herein. Also provided are methods of treatment using these agents in the treatment of infections of microorganisms such as viruses and fungi.
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SULFUR AND AMIDE TROPOLONE INHIBITORS OF NUCLEOTIDYL TRANSFERASES AND USES THEREFOR
The present disclosure provides inhibitors of microorganisms including viruses and fungi of the formula (I) or (II) wherein the variables are defined herein. Also provided are methods of treatment using these agents in the treatment of infections of microorganisms such as viruses and fungi.
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CYCLOOXYGENASE-2 INHIBITORS AND USES THEREOF
The present disclosure describes compounds of the formula: (I), (II), (III), (IV), (V). The compounds described herein may be cyclooxygenase (COX) (e.g., cyclooxygenase 2 (COX2)) inhibitors. The compounds may be radiolabeled. The compounds (e.g., radiolabeled compounds) may be useful (e.g., as positron emission tomography (PET) imaging agents) for diagnosing a disease. The compounds may also be useful for treating or preventing a disease. The present disclosure also describes pharmaceutical compositions and kits including the compounds; and methods of using the compounds.
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CYCLOOXYGENASE-2 INHIBITORS AND USES THEREOF
The present disclosure describes compounds of the formula: (I), (II), (III), (IV), (V). The compounds described herein may be cyclooxygenase (COX) (e.g., cyclooxygenase 2 (COX2)) inhibitors. The compounds may be radiolabeled. The compounds (e.g., radiolabeled compounds) may be useful (e.g., as positron emission tomography (PET) imaging agents) for diagnosing a disease. The compounds may also be useful for treating or preventing a disease. The present disclosure also describes pharmaceutical compositions and kits including the compounds; and methods of using the compounds.
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COMPOUND AND PREPARATION METHOD THEREFOR AND USE THEREOF
Provided are a novel impurity compound of rotigotine behenate, rotigotine behenate or a preparation thereof containing less than 0.5 wt % of the impurity compound and use of the impurity compound as a reference substance in the impurity detection of the rotigotine behenate or the preparation thereof.
Rotigotine-containing patch
The present invention provides a rotigotine-containing patch comprising: a backing layer; and an adhesive agent layer, wherein the adhesive agent layer contains rotigotine and/or a pharmaceutically acceptable salt thereof, the adhesive agent layer further contains a styrene-based thermoplastic elastomer, a petroleum-based resin and/or a terpene-based resin, an aliphatic alcohol, and a cross-linked polyvinylpyrrolidone, and in the adhesive agent layer, a mass ratio of a content of the rotigotine and/or the pharmaceutically acceptable salt thereof in terms of rotigotine free form and a content of the cross-linked polyvinylpyrrolidone (content of the rotigotine and/or the pharmaceutically acceptable salt thereof in terms of rotigotine free form:content of the cross-linked polyvinylpyrrolidone) is 10:3 to 1:3.
Photoswitchable HDAC inhibitors
This invention relates to photoswitchable inhibitors of histone deacetylases and methods of using the same.
Photoswitchable HDAC inhibitors
This invention relates to photoswitchable inhibitors of histone deacetylases and methods of using the same.
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.