Patent classifications
C07F9/5728
STAT6 inhibitors
The present disclosure provides compounds that are useful for inhibiting the STAT6 pathway. Also provided are related pharmaceutical compositions and methods of using the compounds. In some embodiments, the compounds may be used to treat a disease such as, e.g., an allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease, or a cancer.
USE OF PHOSPHOROUS-CONTAINING ORGANIC OXYIMIDES AS FLAME RETARDANTS AND/OR AS STABILIZERS FOR PLASTICS, FLAME-RETARDANT AND/OR STABILIZED PLASTIC COMPOSITIONS, METHOD FOR THE PRODUCTION THEREOF, MOULDED PART, PAINT AND COATINGS
The present invention relates to the use of phosphorous-containing organic oxyimides according to the general formula (I) as flame retardant for plastic materials, as radical generators in plastic materials and/or stabilisers for plastics. In addition, the present invention relates to a flame-retardant plastic material moulding compound in which the previously described phosphorous-containing organic oxyimides are integrated, and also to a method for the production of the previously mentioned plastic material composition. Furthermore, the present invention relates to a moulded article, a paint or a coating from the previously mentioned flame-retardant plastic material composition.
METHODS AND COMPOSITIONS COMPRISING PSYCHOACTIVE COMPOUNDS FROM PSYCHOACTIVE ORGANISMS
This invention relates to the extraction of psychoactive compounds from organisms for use in medicine. Extraction is carried out with a strong acid or strong base to either promote or inhibit dephosphorylation. The extract in the slurry form is standardized with added excipient so that when it is dried the powdered composition has a specified total psychoactive alkaloid concentration, with a known ratio of phosphorylated to dephosphorylated psychoactive alkaloids.
Aminopeptidase A inhibitors and pharmaceutical compositions comprising the same
The present invention relates to a novel compound, to a composition comprising the same, to methods for preparing the compound, and the use of this compound in therapy. In particular, the present invention relates to a compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma.
PHENYLPYRROLIDINONE FORMYL PEPTIDE 2 RECEPTOR AGONISTS
The disclosure relates to compounds of Formulae (I)-(IX), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.
##STR00001##
Salts of prodrugs of piperazine and substituted piperidine antiviral agents
This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. ##STR00001##
wherein: X is C or N with the proviso that when X is N, R.sup.1 does not exist; W is C or N with the proviso that when W is N, R.sup.2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of ##STR00002## Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. ##STR00003##
wherein: L and M are independently selected from the group consisting of C.sub.1-C.sub.6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
Reagents based on a tertiary amine backbone to introduce chemical functionality in nucleic acids and sequence-controlled polymers
It is provided an achiral, non-nucleosidic backbone for phosphoramidites that can be inserted with high yields in nucleic acid strands and sequence-controlled oligo(phosphodiester)s through solid phase synthesis (SPS) using a DNA synthesizer. From this backbone, platforms with useful chemical handles were synthesized, further functionalized, transformed into phosphoramidites and attached to nucleic acid strands and sequence-controlled oligo(phosphodiester)s. The backbone is based on a tertiary amine with a 3-6 carbon spacer between the central nitrogen and the two external hydroxyls. The spacer has been optimized to increase coupling yields and stability.
METHODS OF TREATING NEUROCOGNITIVE DISORDERS, CHRONIC PAIN AND REDUCING INFLAMMATION
- Derek John Londesbrough ,
- Christopher Brown ,
- Julian Scott Northen ,
- Gillian Moore ,
- Hemant Kashinath PATIL ,
- David E. Nichols ,
- Megan CROAL ,
- Hans Ake ERIKSSON ,
- George GOLDSMITH ,
- Molly Tabitha HICKEY ,
- Shaun HURLEY ,
- Ekaterina MALIEVSKAIA ,
- Lindsey MARWOOD ,
- Drummond E-Wen Joe MCCULLOCH ,
- Laurie Emma MEDHURST ,
- Nathan POULSEN ,
- Aslihan SELIMBEYOGLU ,
- Anais SOULA ,
- Amanda Tan SHUXIANG ,
- Manon Cecile Elisabeth VERAART ,
- Tobias Patrick WHELAN ,
- Lars Christian WILDE ,
- Stephen WRIGHT
The disclosure provides methods for treating a subject in need thereof comprising administering to the subject a therapeutically-effective dose of psilocybin. The methods described herein may be used to treat a variety of diseases, disorders, and conditions. For example, the methods may be used to treat neurocognitive disorders (e.g., Alzheimer's disease, Parkinson's disease), ADHD, Epilepsy, Autism, Sleep-wake disorders, Chronic pain, Inflammatory Disorders, IBD, Stroke, ALS, and/or Multiple Sclerosis.
PROGRAMMABLE POLYMERIC DRUGS
Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.a, L.sup.b, L.sup.1, L.sup.2, L.sup.3, M, m, and n are as defined herein. Methods associated with preparation and use of such compounds is also provided.
##STR00001##
PROGRAMMABLE POLYMERIC DRUGS
Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L, L.sup.1, L.sup.2, M and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.
##STR00001##