A class of cyanosteroid compounds that efficiently inhibit ghrelin acylation by ghrelin O-acyltransferase. The compounds have a steroid scaffold with ,-unsaturated ketone in the A ring position such an -cyanoenone. Exemplary compounds include (5S,8S,9S,10S,13S,14S)-10,13-dimethyl-3-oxo-4,5,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-3H-cyclopenta[a]phenanthrene-2-carbonitrile.

Methods of using 7,11-dimethyl-17-hydroxy-4-estren-3-one bucyclate (I) and 7,11-dimethyl-17-hydroxyestr-4-en-3-one 17-undecanoate (II) ##STR00001##
for various hormonal therapies, dosage forms comprising 7,11-dimethyl-17-hydroxy-4-estren-3-one bucyclate and 7,11-dimethyl-17-hydroxyestr-4-en-3-one 17-undecanoate, and processes for their preparation.

Novel selective synthesis route to introduce primary alkyl groups on aromatic compounds is disclosed. The synthesis route is based on electrophilic aromatic substitutions of thionium ion species that are generated in-situ from aldehydes and thiols, affording benzyl sulfide that can be reduced with triethylsilane.

This disclosure provides 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 comprises (i) a diazonium salt that contains a diazonium ion; (ii) an amine and nitrous acid; and/or (iii) a nitrite and an acid.

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.

Disclosed are compounds of the formula:

##STR00001##

and the respective enantiomers, stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of such compounds; which can be useful in the treatment of various types of cancer.

A conjugate for delivery of drugs, such as genetic drugs, (e.g., siRNA or antisense oligonucleotides (ASO) across biological membranes is provided. The conjugates of the Invention are capable of delivering drugs in both presence and absence of plasma proteins.

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.

The invention relates to a process for the preparation of 11-methylene steroids through selective olefination of the ketone at position 11. The resulting products are useful intermediates in the preparation of several pharmaceutically active agents, such as Etonogestrel and Desogestrel.

Disclosed are compounds of the formula: ##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen, C.sub.1-C.sub.6 alkyl, halo, a sulfate, a glucuronide, OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, N(CH.sub.2).sub.n; a phosphate group, and a phosphinate group; R.sub.9 is hydrogen, halogen or alkyl; R.sub.11 is selected from the group consisting of H, C.sub.1-C.sub.6 alkyl, halogen, a sulfate, a glucoronide, SO.sub.2NH.sub.2, COOH, CN, CH.sub.2CN, NHCN, CHO, CHOCH.sub.3, COO salt, OSO.sub.2alkyl, NH.sub.2, and NHCO(CH.sub.2).sub.n; R.sub.12 is selected from the group consisting of H, a C.sub.1-C.sub.6 alkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X is selected from the group consisting of C.sub.1-C.sub.12 alkyl, C.sub.2-C.sub.12 alkenyl, C.sub.2-C.sub.12 alkynyl, halogen, a glucoronide, NH.sub.2, SO.sub.2NH.sub.2, COOH, CN, CH.sub.2CN, NHCN, CHO, COOsalt, OSO.sub.2alkyl, SH, SCH.sub.3, CH[(CH.sub.2).sub.nCH.sub.3]COOCH.sub.3, (CH.sub.2).sub.mCOOCH.sub.3, (CH.sub.2).sub.mOCH.sub.3, (CH.sub.2).sub.mO(CH.sub.2).sub.nCH.sub.3, (CH.sub.2).sub.mSCH.sub.3, (CH.sub.2).sub.mS(CH.sub.2).sub.nCH.sub.3, (CH.sub.2).sub.mNH(CH.sub.2).sub.nCH.sub.3, C.sub.2-C.sub.8 alkenyl-O(CH.sub.2).sub.nCH.sub.3, C.sub.2-C.sub.8 alkenyl-S(CH.sub.2).sub.nCH.sub.3, C.sub.2-C.sub.8 alkenyl-N(CH.sub.2).sub.nCH.sub.3, C.sub.2-C.sub.8 alkynyl-O(CH.sub.2).sub.nCH.sub.3, C.sub.2-C.sub.8 alkynyl-S(CH.sub.2).sub.nCH.sub.3, C.sub.2-C.sub.8 alkynyl-N(CH.sub.2).sub.nCH.sub.3, (CH.sub.2).sub.mOH, (CH.sub.2).sub.mONH.sub.2, (CH.sub.2).sub.mSNH.sub.2, NH(CH.sub.2).sub.mCH.sub.3, NH(CH.sub.2).sub.mOCH.sub.3, NH(CH.sub.2).sub.mCHOHCOOH, N(CH.sub.3).sub.2, (CH.sub.2).sub.m(NH)CH.sub.2OH, NHCOOH, (CH.sub.2).sub.mNHCOOH, NO.sub.2, SCN, SO.sub.2alkyl, B(OH).sub.2, (CH.sub.2).sub.mN(CH.sub.3)SO.sub.2NH.sub.3, (CH.sub.2).sub.mNHSO.sub.2NH.sub.2, NHC(S) CH.sub.3, and NHNH.sub.2; and Y is selected from hydrogen, O, OCO(R.sub.6) and OH; wherein m is an integer between 0-20, n is an integer between 0-8, the symbol represents either a single or a double bond capable of forming a keto group at position 3 or 17; and the symbol represents any type of bond regardless of the stereochemistry; and the respective enantiomers, othe