Patent classifications
C07J1/007
19-NOR NEUROACTIVE STEROIDS AND METHODS OF USE THEREOF
Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I):
##STR00001##
and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, status epilepticus.
19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof
Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein, , R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, and R.sup.4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5-to6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus. ##STR00001##
19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof
Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof; wherein , R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, and R.sup.4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5- to 6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
COMPOUNDS FOR TREATING CNS DISORDERS
##STR00001##
Provided herein in part is a compound of Formula (I): or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of using the compounds, e.g, in the treatment of CNS- related disorders.
REAGENT KIT FOR LC-MS ANALYSIS OF AROMATIC COMPOUNDS
A method for analyzing aromatic compounds, and a reagent kit for LC-MS analysis of aromatic compounds. The method includes preparing a diazonium reagent, contacting aromatic compounds in a sample with the diazonium reagent to form an analyte; and measuring an amount or ratio of the analyte. The reagent kit includes a diazonium reagent, wherein the diazonium reagent includes (i) a diazonium salt that contains a diazonium ion; (ii) an amine and nitrous acid; and/or (iii) a nitrite and an acid.
PROCESS FOR PREPARING (15ALPHA,16ALPHA,17BETA)-ESTRA-1,3,5(10)-TRIENE-3,15,16,17-TETROL MONOHYDRATE (ESTETROL MONOHYDRATE)
The present invention relates to a process for preparing (15α,16α,17(β)-Estra-1,3,5(10)-triene -3,15,16,17-tetrol monohydrate, also known as Estetrol monohydrate.
2-METHOXYESTRADIOL DERIVATIVES AND MEDICAL USES THEREOF
The present invention relates to novel 2-Methoxyestradiol derivatives and their medical use. In particular, the novel derivatives of the present invention are useful for the treatment or prevention of liver or lung fibrosis. Accordingly, the present invention also provides medical uses of the 2-Methoxyestradiol derivatives of the present invention. The present invention also provides a method of treating or preventing liver or lung fibrosis comprising administering an effective amount of the 2-Methoxyestradiol derivatives of the present invention.
INDUSTRIAL PROCESS FOR THE PREPARATION OF HIGH PURITY ESTETROL
The invention relates to the preparation of estetrol of formula (I), derivatives thereof protected at positions 3,15α,16α,17β of general formula (III), and 3-hydroxy derivatives thereof protected at positions 15α,16α,17β of general formula (IV), and to the intermediates of general formulae (III) and (IV) applied in the process. Another aspect of the invention is the use of estetrol of formula (I) obtained by the process of the invention for the preparation of a pharmaceutical composition.
##STR00001##
19-NOR C3, 3-DISUBSTITUTED C21-N-PYRAZOLYL STEROIDS AND METHODS OF USE THEREOF
Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I):
##STR00001##
and pharmaceutically acceptable salts thereof; wherein , R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6, and R.sup.7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
Quantitative profiling of progesterone metabolites for the prediction of spontaneous preterm delivery
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.