In an embodiment of the invention, a composition for treating a cell population comprises a medicant. The medicant moiety can be an illudofulvene analog. In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The affinity moiety can be an antibody, an antibody fragment, a receptor protein, a peptidic growth factor, an anti-angiogenic protein, a specific binding peptide, protease cleavable peptide, a glycopeptide, a peptide, a peptidic toxin, a protein toxin and an oligonucleotide. The affinity moiety can be covalently bound to the medicant via a linker.

Disclosed are methods of purifying the compound (22E)-(24R)-2-methylene-22-dehydro-1α,24,25-trihydroxy-19-nor-vitamin D.sub.3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving (22E)-(24R)-2-methylene-22-dehydro-1α,24,25-trihydroxy-19-nor-vitamin D.sub.3 in a solvent comprising ethyl acetate and hexane to form a solution, allowing crystals of (22E)-(24R)-2-methylene-22-dehydro-1α,24,25-trihydroxy-19-nor-vitamin D.sub.3 to form and precipitate from the solution, and recovering the crystals of (22E)-(24R)-2-methylene-22-dehydro-1α,24,25-trihydroxy-19-nor-vitamin D.sub.3 from the solution.

In an embodiment of the invention, a composition for treating a cell population comprises a medicant. The medicant moiety can be an illudofulvene analog. In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The affinity moiety can be an antibody, an antibody fragment, a receptor protein, a peptidic growth factor, an anti-angiogenic protein, a specific binding peptide, protease cleavable peptide, a glycopeptide, a peptide, a peptidic toxin, a protein toxin and an oligonucleotide. The affinity moiety can be covalently bound to the medicant via a linker.

The present disclosure relates to polycyclic (e.g., tetracyclic) glucocorticoid receptor (GR) modulators, synthetic methods for preparing such GR modulators, and methods of using such GR modulators to treat a glucocorticoid-dependent condition, such as cancer or hypercortisolism. Exemplary compounds have quaternary centers at C9 and C13 in which the quaternary center at C9 projects a substituent on the opposite face of the tetracycle as the substituent at C13.

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 disclosure relates to a method for labeling a biomolecule, a fluorescent dye, or a nanoparticle compound with a radioisotope, comprising: (a) providing a cyclooctyne compound represented by the following formula (I) comprising the biomolecule, the fluorescent dye, or the nanoparticle compound which is bound to a cyclooctyne moiety of the cyclooctyne compound; and (b) reacting the cyclooctyne compound of formula (I) with a quinone compound represented by the following formula (II) to give a biomolecule, a fluorescent dye, or a nanoparticle compound labeled with the radioisotope: ##STR00001## in formula (I), (Z is the biomolecule, the fluorescent dye, or the nanoparticle compound) ##STR00002## in formula (II), (b is 0 or an integer from 1 to 10; L is CH.sub.2, —COO—, or —CONH—; M is the radioisotope).

The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.

A new and improved method for preparing maxacalcitol and an intermediate therefor is provided. The method is an efficient and cost-effective process for preparing maxacalcitol and an intermediate therefor.

It is an object of the present invention to provide methods for producing vitamin D that gives improved yields and reduced side product contamination. In various aspects, these methods provide for production of vitamin-D.sub.2 using ergosterol as provitamin D.sub.2 or a dihydroxy derivative thereof as a starting material, or production of vitamin-D.sub.3 using 7-dehydrocholesterol as provitamin D.sub.3 or a dihydroxy derivative thereof as the starting material. The methods described herein comprise irradiating the starting material in a solution including an organic or inorganic base with light in the wavelength range 245-360 nanometers (nm) to obtain a product containing pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3, and heating the product to convert the resulting pre-vitamin-D.sub.2 or pre-vitamin-D.sub.3 to vitamin D.sub.2 or vitamin D.sub.3. In various embodiments, these methods further comprise recovering vitamin D.sub.2 or vitamin D.sub.3 from this reaction as a purified product.

Methods of preparing unsaturated compounds or analogs through dehydrogenation of corresponding saturated compounds and/or hydrogenation of aromatic compounds are disclosed.