Patent classifications
C07J1/0011
Small molecules active against gram-negative bacteria
Disclosed are compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.
CYCLIN-DEPENDENT KINASE DEGRADERS AND METHODS OF USE
The present application provides bifunctional compounds of Formula (Ia): (Ia), or an enantiomer, diastereomer, stereoisomer, or pharmaceutically acceptable salt thereof, which act as protein degradation inducing moieties for one or mor of cyclin-dependent kinase 8 (CDK8) and cyclin-dependent kinase 19 (CDK19). The present application also relates to methods for the targeted degradation of CDK8 and/or CDK19 through the use of the bifumtional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK8 and/or CDK19 which can be utilized in the treatment of disorders modulated by CDK8 and/or CDK19.
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AQUEOUS SUSPENSION COMPOSITIONS, FORMULATIONS, AND WATER DISPERSIBLE DRY COMPOSITIONS COMPRISING 16ALPHA-BROMO-3BETA-HYDROXY-5ALPHA-ANDROSTAN-17-KETONE AND HYDRATES, DERIVATIVES, AND ANALOGS THEREOF
Method of treating a subject in need of a treatment for modulating immune system or anti-microbial infection, comprising administering a stable aqueous suspension formulation, which may be reconstituted from a water dispersible dry composition, comprising compound of Formula I in the form of particles stabilized in an aqueous suspension. It causes little or no injection site irritation and has superior properties over non-aqueous formulations. It stimulates autophagy, enhance innate immunity, down-regulates unproductive inflammation and exerts a Th1 immune bias. It demonstrates better efficacy in both in vitro and in vivo models.
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AQUEOUS SUSPENSION COMPOSITIONS, FORMULATIONS, AND WATER DISPERSIBLE DRY COMPOSITIONS COMPRISING 16ALPHA-BROMO-3BETA-HYDROXY-5ALPHA-ANDROSTAN-17-KETONE AND HYDRATES, DERIVATIVES, AND ANALOGS THEREOF
Composition comprising a stable aqueous suspension formulation, which may be reconstituted from a water dispersible dry composition, comprising compound of Formula I in the form of particles stabilized in an aqueous suspension. It causes little or no injection site irritation and has superior properties over non-aqueous formulations. It stimulates autophagy, enhance innate immunity, down-regulates unproductive inflammation and exerts a Th1 immune bias. It demonstrates better efficacy in both in vitro and in vivo models.
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HYDROXYSTEROID COMPOUNDS, THEIR INTERMEDIATES, PROCESS OF PREPARATION, COMPOSITION AND USES THEREOF
The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds.
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Small molecules active against gram-negative bacteria
Disclosed are novel compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.
CHEMILUMINESCENT ANDROSTENEDIONE CONJUGATES
Chemiluminescent androstenedione conjugates are disclosed. These chemiluminescent androstenedione conjugates may be used as chemiluminescent tracers in immunoassays for the quantification and identification of certain analytes.
INHIBITORS OF GLUCOCORTICOID RECEPTOR
The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer and hypercortisolism.
COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
Described herein are neuroactive steroids of the Formula (I):
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or a pharmaceutically acceptable salt thereof; wherein , A, R.sup.1, R.sup.2, R.sup.3a, R.sup.4a, R.sup.4b, R.sup.5, R.sup.7a, and R.sup.7b are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.
NEUROACTIVE STEROIDS AND COMPOSITIONS THEREOF
Provided herein is a compound of Formula (I):
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or a pharmaceutically acceptable salt thereof, wherein R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7a, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.16a, R.sup.16b, R.sup.19, R.sup.11a, R.sup.22, R.sup.X, R.sup.Y and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.