C07J1/0011

NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, PRODRUGS THEREOF, AND METHODS OF TREATMENT USING SAME
20200113916 · 2020-04-16 ·

The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

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##

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.

Compositions and methods for treating CNS disorders

Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein (II), 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. ##STR00001##
custom character (II)

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.

NEUROACTIVE STEROIDS SUBSTITUTED IN POSITION 10 WITH A CYCLIC GROUP FOR USE IN THE TREATMENT OF CNS DISORDERS

Provided herein is a compound of Formula (I)

##STR00001##

or a pharmaceutically acceptable salt thereof, wherein n, R.sup.19, R.sup.5, R.sup.3a, R.sup.6a, R.sup.6b, R.sup.1, R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.17b, R.sup.15a, R.sup.15b, R.sup.16a and R.sup.16b 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.

METHOD OF PREPARING ESTRADIOL DERIVATIVES BY SOLID-PHASE SYNTHESIS
20240116978 · 2024-04-11 ·

The present invention relates to a method of preparing estradiol derivatives and/or estrone derivatives, which are suitable for radiolabeling. The present invention further relates to the estradiol derivatives and/or estrone derivatives, preferably obtained by the method of the present invention, as well as to the use of the estradiol derivatives and/or estrone derivatives for radiolabeling with diagnostic and/or therapeutic radionuclides. The present invention further relates to a method of imaging and/or diagnosis of breast cancer as well as to a method of treatment of breast cancer.

Methods for preparation of bile acids and derivatives thereof

The present application relates to a method of preparing compounds of Formula (I) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, R.sub.1 is H, -OH, -OH, or an oxo group. ##STR00001##

CRYSTAL FORM OF BRASSINOSTEROID (BR) ANALOGUE, AND PREPARATION METHOD AND USE THEREOF
20240158434 · 2024-05-16 ·

The present disclosure provides a novel brassinosteroid (BR) analogue, a novel crystal form, and a preparation method and use thereof. The BR analogue has a chemical formula of C.sub.27H.sub.46O.sub.7, a chemical name of (20R,22R)-2?,3?,14?-14,20,22,25-hexahydroxy-5?,8?,9?-cholestan-6-one, and a structural formula of:

##STR00001##

In the present disclosure, a novel crystal form with a high bioactivity is obtained by improving a recrystallization process of a naturally extracted BR analogue. This novel crystal form can be applied in the field of agriculture to promote the growth of plants.

Ultrasonic-assisted pretreatment method for extraction of multiple steroid hormones in sediment

The disclosure discloses an ultrasonic-assisted pretreatment method for extraction of multiple steroid hormones in a sediment, including the following steps: (1) lyophilizing the sediment, grinding the sediment, and passing the ground sediment through a 40-60-mesh sieve; (2) placing the sample obtained in step (1) in a container; (3) adding an extractant to the container in step (2), shaking the mixture for 15 s-30 s, centrifuging the mixture to collect an supernatant after ultrasonication, and repeating extraction three times; where the extractants used in the three times of extraction are two of methanol, acetonitrile and acetone; and (4) after mixing the supernatants of the three times of extraction obtained in step (3), concentrating the mixture under a nitrogen flow at 20-30? C., passing the concentrated mixture through a filter, and performing detection. By using the method of the disclosure, the maximum recovery can be up to 100%. The application range is wide, and a recovery of the plurality of steroid hormones each can be up to 73% or above.