Abstract: The invention relates to a new method for preparing all trans retinoyl CoA.

Abstract: The invention provides new seco-sterol compounds which are effective in inducing the differentiation of malignant cells and are therefore useful for the treatment of malignancies such as leukemia.

Abstract: This invention provides novel side chain homologs of 1.alpha.,25-dihydroxyvitamin D.sub.3 which exhibit enhanced and highly selective activity in inducing differentiation of malignant cells. It also provides a general method of synthesis applicable to the preparation of a variety of vitamin D side chain analogs, and a method of treatment of neoplastic diseases which takes advantage of the selective differentiation activity of the new vitamin D homologs.

Abstract: This invention provides novel 1.alpha.-hydroxyvitamin D compounds, methods for their preparation, and pharmaceutical compositions of these compounds. The new compounds, which are characterized structurally by having a cyclopentane ring as part of their side chains, exhibit highly pronounced biological activity, both in terms of their effect on calcium metabolism and their effect on differentiating malignant cells to normal cells. By virtue of their biological properties, the new vitamin D analogs are effective as calcium-regulating, or differentiation-inducing agents, and thus find application as therapeutic agents in the treatment or prophylaxis of bone-related as well as neoplastic diseases.

Abstract: The invention relates to a method for preparing vitamin D-related compounds and to certain intermediate compounds in such process. The intermediate compounds are characterized by an aldehyde or ester in the C-22 position in the side chain. The presence of such groups permit facile side chain additions for the preparation of vitamin D derivatives.

Abstract: The invention relates to a new method for preparing all trans- and 13-cis retinoyl CoA.

Abstract: The invention provides a method for inducing the differentiation of malignant cells utilizing certain seco-sterol compounds, such as the differentiation of leukemia cells to normal macrophages and thereby affords a method for treating leukemic disorders.

Abstract: The invention is directed to the preparation of hydroxylated compounds of the vitamin D.sub.2 series and specifically to a process for synthesizing 1.alpha.,25-dihydroxyvitamin D.sub.2, 1.beta.,25-dihydroxyvitamin D.sub.2, their corresponding 5,6-trans isomers and the C-24 epimers of these compounds.The hydroxylated vitamin D.sub.2 compounds obtained exhibit vitamin D-like activity and can be substituted for vitamin D.sub.3 or various of its known metabolites where such compounds are applied.

Abstract: The invention relates to new coenzyme A and N-hydroxysuccinimidyl esters of all-trans- and 13-cis-retinoic acid and to methods for preparing the same. A new method for preparing all-trans-retinoic acid anhydride is also disclosed.

Abstract: The invention relates to ring A-diol units suitable for synthesizing 1.alpha.-hydroxyvitamin D compounds by subsequent condensation with appropriate .sup.C /.sub.D -ring fragments and to methods for preparing such ring A-diol units.

Abstract: The invention provides, as novel vitamin D derivatives, analogs of vitamin D.sub.2 compounds which lack the 24-methyl substituent and are identified as 1.alpha.-hydroxy-28-norvitamin D.sub.2 and 1.alpha.,25-dihydroxy-28-norvitamin D.sub.2.The compounds of the invention are characterized by unexpectedly high vitamin D-like activity as well as a novel activity pattern. Because of such activity they would find ready application as substitutes for vitamin D or various of the known vitamin D metabolites in their various application for the treatment of calcium disorders.

Abstract: Novel 1-hydroxylated vitamin D compounds containing a 22, 23-cis double bond in the side chain are provided. The compounds are characterized by an unexpectedly high binding affinity for the protein receptor forecasting their ready applicability as substitutes for vitamin D or various of its metabolites in their various known applications and in the treatment of various metabolic bone diseases.

Abstract: This invention relates to a method for enhancing cell differentiation in malignant cells by exposing the cells to a 1.alpha.-hydroxylated vitamin D derivative characterized by a 17-side chain greater in length than the cholesterol or ergosterol side chains.The method finds application in the treatment of neoplastic diseases including leukemoid diseases and, specifically, leukemia.

Abstract: The invention provides a novel vitamin D derivative, 1.alpha.,25-dihydroxy-22Z-dehydrovitamin D.sub.2.The compound is characterized by unexpectedly high ability to raise serum calcium levels. The compound could therefore, find ready application as a substitute for vitamin D or its metabolites in the treatment of metabolic bone diseases or in other of their known applications.

Abstract: A method for treating or preventing metabolic bone disease characterized by loss of bone mass in mammals by administering 24-epi-1.alpha.,25-dihydroxy vitamin D.sub.2 alone or in combinations thereof with bone mobilization-inducing vitamin D derivatives to said mammals.

Abstract: The invention relates to a process for preparing 1-hydroxyvitamin D compounds by acid-catalyzed solvolysis of the corresponding 1-hydroxy-3,5-cyclovitamin D compound in an organic solvent medium whereby the free, non-acylated, 5,6-cis and 5,6-trans-1-hydroxylated vitamin D compounds are obtained in admixture.

Abstract: The invention relates to a process for separating 1.alpha.-hydroxyvitamin D compounds from their corresponding 1.alpha.-hydroxy-5,6-trans isomers in a mixture thereof by treating the mixture with a dienophile and then separating the resulting dienophil-adduct of the 1.alpha.-hydroxy-5,6-trans vitamin D isomer from the unreacted 1.alpha.-hydroxyvitamin D compound.

Abstract: This invention provides novel 1,23-dihydroxyvitamin D compounds, a process for preparing such compounds of novel intermediates in such process.As indicated by its binding affinity for the 1.alpha.,25-dihydroxyvitamin D.sub.3 receptor protein, the compounds of this invention would function as effective substitutes for vitamin D and certain vitamin D metabolites for the regulation of calcium and phosphorous metabolism and for treatment of bone-related diseases.

Abstract: The invention provides, as novel vitamin D derivatives, isomers of 25-hydroxyvitamin D.sub.2 and 1.alpha.,25-dihydroxyvitamin D.sub.2 characterized by a double bond at the 23,24-position.The compounds are characterized by vitamin D-like activity as assessed by competitive binding assays and would therefore, find application as substitutes for vitamin D or various of its metabolites in their various known applications and in the treatment of vitamin D-responsive bone diseases.

Abstract: This invention provides a novel vitamin D derivative, namely a 24-oxime derivative of vitamin D.sub.3, and a process for its preparation. The compound of this invention is an effective inhibitor of vitamin D-25-hydroxylation and markedly suppresses the formation of the physiologically active vitamin D metabolites. The compound would thus find use as an effective antagonist of vitamin D activation, and for treating hypercalcemic conditions resulting from metabolic, bone, or neoplastic diseases, or from vitamin D intoxication.