The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds. ##STR00001##

Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.

In one aspect, the present disclosure provides methods of preparing a primary or secondary amine and hydroxylated aromatic compounds. In some embodiments, the aromatic compound may be unsubstituted, substituted, or contain one or more heteroatoms within the rings of the aromatic compound. The methods described herein may be carried out without the need for transition metal catalysts or harsh reaction conditions.

Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.

A compound of formula (I)

##STR00001##

in which R represents a group (CR.sub.aR.sub.b).sub.nX(CR.sub.cR.sub.d).sub.m[Y(CR.sub.eR.sub.f).sub.o].sub.tNR.sub.9R.sub.10 and X and Y independently represent a group NR11-, a group O or a divalent 5-membered or 6-membered heterocyclic group comprising at least one nitrogen atom, and also the stereoisomers, mixtures of stereoisomers, and/or pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical or veterinary compositions containing same, which may be used as a medicament, more particularly, in the treatment of bacterial, fungal, viral or parasitic infections. In certain aspects, these pharmaceutical or veterinary compositions include the compound of formula (I) in combination with an antibiotic other than such a compound of formula (I).

Described herein are neuroactive steroids or a pharmaceutically acceptable salt thereof. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.

A compound having a chemical formula according to Formula (I) is disclosed where one of Z.sub.1, Z.sub.2 and Z.sub.3 is and one of the Z.sub.1, Z.sub.2, and Z.sub.3 that is bonded to a carbon atom that is adjacent to the carbon atom bonded to is P(AR.sub.1)(AR.sub.2). Metal-based catalyst and pre-catalysts, such as nickel-based catalysts and precatalysts, where the metal is complexed to the compound are also disclosed. Methods of forming C(sp2)-N bonds are also disclosed.

Disclosed are compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.

The invention relates to an antagonist of CB1 receptor for use in the treatment of a pathologic condition or disorder selected from the group consisting of bladder and gastrointestinal disorders; inflammatory diseases; cardiovascular diseases; nephropathies; glaucoma; spasticity; cancer; osteoporosis; metabolic disorders; obesity; addiction, dependence, abuse and relapse related disorders; psychiatric and neurological disorders; neurodegenerative disorders; autoimmune hepatitis and encephalitis; pain; reproductive disorders and skin inflammatory and fibrotic diseases.

Compounds are provided according to Formula (I):

##STR00001##

and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v):

##STR00002##

and wherein L.sup.1, L.sup.2, L.sup.3, X.sup.1, X.sup.2, Y, R.sup.Z4, R.sup.Z5, R.sup.Z6, n, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.14, R.sup.17, R.sup.19, R.sup.20, R.sup.23a, R.sup.23b, and R.sup.24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.