This present disclosure is directed to novel prodrugs of activated vitamin D.sub.3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.

##STR00001##

The invention pertains to a process for producing a compound of formula (11) wherein R.sup.7 and R.sup.8 are each independently selected from H, halogen, alkyl, aryl, or alkylaryl, R.sup.42 is H or a protective group, R.sup.43 is H or R.sup.3, wherein R.sup.3 is a protective group, by contacting a compound of formula (10) with an olefmation reagent, wherein compound of formula (10) comprises a counter acid X.sup.1 when R.sup.42H and R.sup.43H.

Compounds of formula (I):

##STR00001##

where R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6 and R.sup.7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

Compounds include compounds of the Formula I, namely, (R.sup.1).sub.p-(L).sub.q-Z wherein R.sup.1, L, p and q are as defined herein.

Compounds of formula (II): ##STR00001##
wherein ##STR00002##
R.sup.1, R.sup.2, R.sup.5 and R.sup.13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

Disclosed are methods of preparing unsaturated carbocyclic compounds through dehydrogenation of corresponding saturated carbocyclic compounds.

The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds, and methods of using such compounds to treat a disease, such as a brain tumor and, particularly, a glioma.

The present invention relates to a process for labeling compounds comprising thiol moieties with 3-arylpropiolonitrile compounds, to 3-arylpropiolonitrile compounds substituted with tag moieties and to specific 3-arylpropiolonitrile linkers.

This invention relates to compositions, methods and kits for determining the presence and/or amount of vitamin D analytes, including vitamin D isomers, and metabolites thereof in a sample suspected of containing the same. Compounds include compounds of the Formula I, namely, (R.sup.1).sub.p-(L).sub.q-Z wherein R.sup.1, L, p and q are as defined herein. These compounds are capable of binding specifically to corresponding antibodies. Compounds and antibodies in accordance with the principles described herein can have therapeutic activity. These compounds may be administered in therapeutically effective amount, which is an amount to provide treatment of a particular disease state associated with vitamin D. Administration of the examples of compounds in accordance with the principles described herein can be by means of any of the accepted modes of administration for agents that serve similar utilities.

The present invention pertains to novel octahydro-indene compounds and their unexpected advantageous use thereof in enhancing, improving or modifying the fragrance of perfumes, colognes, toilet waters, fabric care products, personal products, and the like.