C07J5/0053

Neuroactive steroids, compositions, and uses thereof

Described herein are neuroactive steroids of the Formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof; wherein R.sup.1a and R.sup.1b 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.

17ALPHA-MONOESTERS OF CORTEXOLONE FOR USE IN THE TREATMENT OF TUMORS
20190175618 · 2019-06-13 · ·

The present invention provides certain cortexolone derivatives, and the same for use as antitumor active ingredients for the curative or adjuvant, or neoadjuvant or palliative treatment of precancerous lesions, dysplasias, metaplasias and tumor diseases, including malignant neoplasias and metastasis. The present invention also provides pharmaceutical compositions comprising the cortexolone derivatives as active ingredients and at least one physiologically acceptable excipient, and to the use of said pharmaceutical compositions as antitumor medicinal products.

COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS

Described herein are neuroactive steroids of the Formula (I):

##STR00001##

or a pharmaceutically acceptable salt thereof; wherein custom-character, 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.

QUANTITATIVE PROFILING OF PROGESTERONE METABOLITES FOR THE PREDICTION OF SPONTANEOUS PRETERM DELIVERY
20190137507 · 2019-05-09 ·

Disclosed are methods for identifying a pregnant female who is susceptible to spontaneous preterm delivery. In particular, disclosed are methods for identifying a pregnant female who is susceptible to spontaneous preterm delivery based on ratios of steroids in samples obtained from the pregnant female.

METHODS FOR THE PURIFICATION OF DEOXYCHOLIC ACID

Synthetic methods for preparing deoxycholic acid and intermediates thereof, high purity synthetic deoxycholic acid, compositions and methods of use are provided. Also, provided are processes for the synthesis of 12-keto or 12--hydroxysteroids from -9,11-ene, 11-keto or 11-hydroxy--steroids. This invention is also directed to novel compounds prepared during the synthesis. This invention is also directed to the synthesis of deoxycholic acid starting from hydrocortisone.

NON-HORMONAL STEROID MODULATORS OF NF-kB FOR TREATMENT OF DISEASE
20190125763 · 2019-05-02 ·

Provided herein is a pharmaceutical composition comprising a compound having the structural formula

##STR00001##

wherein the compound is present in an amount effective to treat or reduce the symptoms of muscular dystrophy. The therapeutically effective amount may be between 10 mg to 200 mg, or may be between 0.01 mg/kg to 10.0 mg/kg. Also provided are methods of treating or reducing the symptoms of muscular dystrophy, comprising the administration, to a patient in need thereof, of a therapeutically effective of the above compound.

17A-MONOESTERS AND 17A,21-DIESTERS OF CORTEXOLONE FOR USE IN THE TREATMENT OF TUMORS
20190091240 · 2019-03-28 · ·

The present invention relates to certain cortexolone derivatives of formula (I)

##STR00001##

and the use of the same as antitumor active ingredients for the curative or adjuvant, or neoadjuvant or palliative treatment of precancerous lesions, dysplasias, metaplasias and tumor diseases, including malignant neoplasias and metastasis. The present invention also relates to pharmaceutical compositions comprising cortexolone derivatives of formula (I) as active ingredients and at least one physiologically acceptable excipient, and to the use of the pharmaceutical compositions as antitumor medicinal products.

ENZYMATIC PROCESS FOR OBTAINING 17 ALPHA-MONOESTERS OF CORTEXOLONE AND/OR ITS 9,11-DEHYDRODERIVATIVES
20190083511 · 2019-03-21 ·

The present invention refers to a new enzymatic process for obtaining 17?-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17?,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone-17?-propionate and 9,11-dehydro-cortexolone 17?-butanoate.

Cortexolone 17alpha-benzoate for use in the treatment of tumours
10231980 · 2019-03-19 · ·

The present invention provides certain cortexolone derivatives of formula (I), and the same for use as antitumor active ingredients for the curative or adjuvant, or neoadjuvant or palliative treatment of precancerous lesions, dysplasias, metaplasias and tumor diseases, including malignant neoplasias and metastasis. Another aspect of the invention relates to pharmaceutical compositions comprising cortexolone derivatives of formula (I) as active ingredients and at least one physiologically acceptable excipient, and to the use of said pharmaceutical compositions as antitumor medicinal products.

Non-hormonal steroid modulators of NF-kB for treatment of disease

The present invention relates to compounds and methods which may be useful as treatments of neuromuscular diseases such as muscular dystrophy, and as inhibitors of NF-?B for the treatment or prevention of muscular wasting disease, including muscular dystrophy.