C07J41/0038

COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
20240101592 · 2024-03-28 ·

Provided herein is a compound of Formula (I)

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or a pharmaceutically acceptable salt thereof, wherein ring D and the substituents are defined herein. Also provided are pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and methods of using the compound of Formula (I) in the treatment of CNS-related disorders.

CATIONIC STEROID ANTIMICROBIAL DIAGNOSTIC, DETECTION, SCREENING AND IMAGING METHODS
20180280550 · 2018-10-04 · ·

The invention relates to diagnostic, detection, screening and imaging methods. In various embodiments, methods of diagnosis, detection, screening and imaging include administering a cationic steroid antimicrobial or CSA to a subject having or at risk of having an infection or a hyperproliferative disorder (e.g., a tumor, cancer or neoplasia) in an amount effective to diagnose or detect the infection or the hyperproliferative disorder (e.g., a tumor, cancer or neoplasia) in the subject. In a particular aspect, a detectable CSA, namely CSA-13 labeled with .sup.99mTc is used to detect the presence of an infection.

Amphiphilic compounds with neuroprotective properties

Amphiphilic compounds with tetradecahydrophenanthrene skeleton and their enantiomers, exhibiting neuroprotective effects, their use in methods of treatment of neuropsychiatric disorders associated with an imbalance in glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post-traumatic stress disorder and diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addiction, multiple sclerosis, epilepsy, glioma, and a pharmaceutical composition containing compound.

Cationic steroid antimicrobial diagnostic, detection, screening and imaging methods
09943614 · 2018-04-17 · ·

The invention relates to diagnostic, detection, screening and imaging methods. In various embodiments, methods of diagnosis, detection, screening and imaging include administering a cationic steroid antimicrobial or CSA to a subject having or at risk of having an infection or a hyperproliferative disorder (e.g., a tumor, cancer or neoplasia) in an amount effective to diagnose or detect the infection or the hyperproliferative disorder (e.g., a tumor, cancer or neoplasia) in the subject. In a particular aspect, a detectable CSA, namely CSA-13 labeled with .sup.99mTc is used to detect the presence of an infection.

SELECTIVE ISONITRILE INHIBITORS OF CYTOCHROME P450 SUBTYPES

Described herein are steroid or steroid-like compounds including at least one isonitrile group and which inhibit the activity of a cytochrome P450 enzyme, as well as compositions including the compounds. Also included are methods of inhibiting activity of a cytochrome P450 in a subject having a steroid-responsive cancer, a Mycobacterium tuberculosis infection, a fungal infection, or a trypanosome infection, the method comprising administering to the subject the compound including at least one isonitrile group or a pharmaceutically acceptable salt thereof, in an amount effective to inhibit the CYP activity in the subject.

5-β, 14-β-androstane derivatives useful for the treatment of proteinuria, glomerulosclerosis and renal failure

Compound of formula (I), wherein the symbol have the meaning reported in the text; for preparing a medicament for the prevention and/or treatment of proteinuria, glomerulosclerosis or renal failure.

Testosterone derivatives with a carboxyalkyl substitution in position 3 and use thereof for the production of labelled steroids for determining the concentration of testosterone in a biological sample
09676811 · 2017-06-13 · ·

A testosterone derivative of formula (I): ##STR00001##
where n is an integer in a range of from 1 to 10, and Y represents an activated or ready-to-be-activated group allowing formation of an amide bond with a primary amine of a molecule. Conjugates including the testosterone derivatives and a marker, methods for determining the concentration of testosterone in a biological sample, and methods for preparing the testosterone derivatives are also provided.

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.

##STR00001##

Method for preparing carbonyl sulfone

Disclosed is a method for preparing -carbonyl sulfones. The method comprises: by taking an -carbonyl diazo compound and sodium arylsulfinate as reaction substrates, cheap silver nitrate as an optimal catalyst, 1,10-phenanthroline as a ligand, and potassium persulfate as an oxidant, carrying out coupling reaction in a mixed solvent of acetonitrile and water to obtain a -carbonyl sulfones compound. Compared with the prior art, the method has the following advantages: a wide range of reaction substrates, short reaction time, a relatively high reaction yield, a mild reaction condition, etc. In the present invention, non-toxic and harmless reagents are used as reaction raw materials, so that it has no harm to the environment and satisfies the requirements of contemporary green chemistry development. Post-reaction treatment is relatively simple, and is convenient for separation and purification. In addition, the reaction can achieve gram-scale synthesis, and lays a foundation for actual applications.

COMPOUNDS AND METHODS FOR THE TREATMENT OF DERMAL AND OCULAR DISORDERS

Described herein are compositions and methods for the treatment or prevention of dermal or ocular surface disorders. Ocular surface disorders include ocular allergy, dry eye disease, ocular manifestation of graft versus host disease and other inflammatory and/or infectious diseases of the (e.g., anterior) surface of the eye(s). Said compositions and methods comprise keratolytic conjugates which demonstrate immunological, keratolytic, anti-inflammatory, and/or other desirable activities. Topical administration of said compositions to the eyelid margin or surrounding areas provides therapeutic benefit to patients suffering from ocular surface disorders.