Abstract: The present invention discloses a process for making 1-.alpha.-(carboxyalkyl)testosterone having the following formula: ##STR1## The process involves protecting the 17 position of 1,4-androstadien-17 .beta.-ol-3-one with TBDMS, alkylating with an alkenylmagnesium bromide and ozonolyzing the resulting ether. The resulting product is oxidized with sodium hypochloride followed by removal of the TBDMS protecting group with aqueous hydrofluoric acid in acetonitrile to produce the 1-.alpha.-(carboxyalkyl)-testosterone.

Abstract: A convergent synthesis of 19-nor-vitamin D compounds, specifically 19-nor-1.alpha.,25-dihydroxyvitamin D.sub.3, is disclosed. The synthesis can also readily be utilized for preparing other 1.alpha.-hydroxylated 19-nor-vitamin D compounds. The key step in the synthesis is a suitable application of Lythgoe's procedure i.e. a Horner-Wittig reaction of the lithium anion of a phosphine oxide with a Windaus Grundmann ketone to give, after any necessary deprotection, the desired 19-nor-vitamin D compound.

Abstract: The invention is drawn to a method for suppressing an immunoresponse in animals by administering an estradiol derivative-chlorambucil conjugate of the formula (I): ##STR1## wherein R.sup.1 is alkyl or alkoxyl of 1 to 4 carbon atoms; R.sup.2 is acyl, dansyl, or alkyl; R.sup.3, R.sup.4, and R.sup.5 independently are H, oxo, OH, or acyloxy; m is an integer of 1 to 3; and n is an integer of 0 to 3; provided that when n is 0, all of R.sup.3, R.sup.4, and R.sup.5 are not H at the same time, and at least one of R.sup.3, R.sup.4, and R.sup.5 is a group other than H and OH; and further, when n is 2 or 3, the groups R.sup.1 are the same or different.

Abstract: This invention relates to new 11-benzaldoxime-estra-diene derivatives of the general formula I ##STR1## wherein Z is --CO--CH.sub.3, --CO--O--C.sub.2 H.sub.5, --CO--NH-phenyl, --CO--NH--C.sub.2 H.sub.5, --CO--C.sub.2 H.sub.5, --CH.sub.3, or --CO-phenyland their pharmaceutically acceptable salts, a method for their production, and pharmaceuticals containing such compounds. The compounds of the general formula I are produced by esterifying or etherizing a compound of the general formula II ##STR2## The compounds described show strong antigestagenic effects combined with reduced glucocorticoid activity.

Abstract: This invention discloses compounds useful as steroid inhibitors. The compounds comprise the formula (5) ##STR1## wherein (a) R.sub.1 is hydrogen and R.sub.2 is selected from the group consisting of SO.sub.2 CF.sub.3, SO.sub.2 NH.sub.2, SO.sub.2 (C.sub.1 -C.sub.6 -alkyl), COCF.sub.3, CONH.sub.2, CO(C.sub.1-C.sub.6 -alkyl); and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiol, estradiolester, pregnenolone, substituted estrones, substituted dehydroepiandrosterone, substituted estradiols, substituted estradiolesters and substituted pregnenolone. Preferably the steroid nucleus is selected from the group consisting of estrone, dehydropeiandrosterone and pregnenolone. The invention also discloses methods of treating a patient therapeutically and prophylactically for estrogen dependent diseases with the compounds of this invention.

Abstract: Use of a compound selected from the group consisting of pentoxifylline, propentofylline and torbafylline for topical treatment of psoriasis or atopic dermatitis and pharmaceutical compositions comprising them.

Abstract: The invention relates to a process for stabilizing pharmaceutically active derivatives of vitamin D2 and D3. At least one pharmaceutically active vitamin D derivative is dissolved in a solvent with an antioxidant. This solution is mixed with a pharmaceutically acceptable stabilizer and at least one solid pharmaceutical excipient or carrier which is present in an amount sufficient to impart the characteristics of a solid to the composition. Finally, the solvent is removed.

Abstract: The invention is drawn to 17-formyl vitamin D compounds having the following formula ##STR1## The compounds are intermediates in the production of 5,6-trans-(E)-20(22)-Dehydrovitamin D compounds which are useful for the treatment of diseases where bone formation is desired, such as osteoporosis, and for the treatment of diseases characterized by abnormal cell differentiation or cell proliferation, such as psoriasis.

Abstract: A process is described for the preparation of taurocholanic acids of formula (I): ##STR1## in which A completes the 5.beta.-cyclopentaneperhydrophenanthrene structure of a cholanic acid and E is hydrogen or a methyl group, by reacting the corresponding cholanic acid with the chloride of an acid having a tertiary carbon in the alpha-position, and treating the resulting mixed anhydride with taurine.

Abstract: A process is disclosed for the removal of the 4-protected hydroxy group from compounds of the following formula: ##STR1## where A is --COOAlkyl and B is hydroxy, or A and B together represent either oxo or .dbd.CHCOOAlkyl, where X.sup.1 and X.sup.2 are the same or different and represent hydrogen or a hydroxy-protecting group, and where X.sup.3 is ##STR2## with a hydrogen radical source, such as tributyltin hydride or tris(trimethylsilyl)silane, and a radical initiator, such as AIBN or irradiation.

Abstract: The invention relates to substituted 17.alpha.-acyl steroidal 5.alpha.-reductase inhibiting compounds. The invention also relates to pharmaceutical compositions containing these compounds and their use for reducing prostate size and treating prostate adenocarcinoma. Further, the invention describes a process for making these compounds by heating the corresponding substituted 17.beta.-acyl steroid in a solvent, such as ethylene glycol or dimethyl sulfoxide (DMSO), in a base, such as sodium or potassium hydroxide.

Abstract: Estradiol derivatives of the formula: ##STR1## wherein R.sup.1 is C.sub.1-4 alky or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; n is an integer of 1 to 3; and X is hydroxy or halogen are useful as tumor growth inhibiting agents.

Abstract: This invention provides a novel class of vitamin D-related compounds, namely the 1.alpha.-hydroxy-19-nor-vitamin D analogs, as well as a general method for their chemical synthesis. The compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells, including malignant cells, and in inducing their differentiation, and thus represent novel therapeutic agents for the treatment of malignant and other diseases characterized by the proliferative growth of undifferentiated cells. Formulations for therapeutic use and treatment methods are also provided. The 19-nor analogs useful herein are of the general formula ##STR1## where X.sup.1 and X.sup.2 each hydrogen, acyl, alkylisilyl or alkoxyalkyl, and where R is any of the typical side chains known for vitamin D type compounds.

Abstract: The invention relates to a process for the preparation of tetrachloro-1,4-benzoquinone of high purity by the action of chlorine and concentrated hydrochloric acid on hydroquinone, which involves introducing a portion of the hydroquinone to be employed into initially introduced hydrochloric acid containing catalytic amounts of iron(III) ions and an anionic dispersant, introducing chlorine gas into this solution at a temperature from 20.degree. to 107.degree. C., then adding the residual quantity of hydroquinone as a solid or in solution, raising the temperature to from 80.degree. to 107.degree. C. while continuing to pass in gaseous chlorine, adding, after the introduction of gaseous chlorine has ended, a relatively high-boiling organic solvent which is not miscible with hydrochloric acid, and subsequently subjecting the reaction mixture to thermal aftertreatment.

Abstract: Chlorinated violanthrones or isoviolanthrones are prepared by reacting violanthrone or isoviolanthrone with chlorine in the presence of a diluent, using aliphatic carboxylic acids and/or aliphatic halo carboxylic acids as diluent for this purpose.

Abstract: The disclosed invention is drawn to the organometallic oestrogen complex of formula (I): ##STR1## in which A is a C.sub.1-7 alkylene radical or C.sub.2-7 alkenylene or alkynylene radical; M.sub.x is one or more identical or different transition metals; L'.sub.y is one or more identical or different ligands complexing the metal(s) of M.sub.x ; and L is a ligand for covalently coupling M.sub.x to A; and R is H or a C.sub.1-7 alkyl or alkoxy group which may be optionally substituted, particularly with one or more halogens. These complexes are useful for the treatment of hormone-dependent cancers. Also, when the metals of the complex M.sub.x are radioactive isotopes suitable for imaging, the complexes are useful as imaging agents.

Abstract: The present invention relates to compounds of the following formula ##STR1## in which Y is sulfur, S(O), or S(O).sub.2 ; R stands for C.sub.1 -C.sub.3 alkyl, or can form a C.sub.3 -C.sub.8 carbocyclic ring. Q is a C.sub.1 -C.sub.8 hydrocarbylene diradical; and derivatives thereof. The compounds can be made by reacting a 20(S)-formyl vitamin D derivative with tert-butyl hypochlorite to form the corresponding acid chloride which is then reacted with potassium O-ethyl dithiocarbonate followed by photochemical reaction and decarbonylation, treatment with aminoethanol, and conversion to the 22-thiol. The 22-thiol is then alkylated to form the desired sidechain. The compounds show antiinflammatory and immunomodulating effects. They also exhibit strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells.

Abstract: The invention discloses a method for treating hypoparathyroidism with vitamin D.sub.3 analogs of the following formula: ##STR1## The methyl group in these compounds which is normally attached to the side chain at carbon 20 has been exchanged with the hydrogen atom attached to carbon 20 to form the 20-epi configuration. The compounds are useful for the treatment of hypoparathyroidism because of their high activity for mobilizing calcium form the bone.

Abstract: 21-norvitamin D.sub.3 analogs in which the methyl group normally attached to the side chain at carbon 20 has been replaced by a hydrogen atom. The compounds are characterized by a marked intestinal calcium transport activity while exhibiting much lower activity than 1.alpha.,25-dihydroxyvitamin D.sub.3 in their ability to mobilize calcium from bone. Because of their preferential calemic activity, these compounds would be useful for the treatment of diseases where bone formation is desired, such as osteodystrophy. Novel intermediates formed during the synthesis of the end products are also disclosed.

Abstract: The invention relates to vitamin D compounds of formula (I) ##STR1## in which X is hydrogen or hydroxy; R.sup.1 and R.sup.2 stand for hydrogen or a C.sub.1-6 hydrocarbyl radical which is optionally substituted with one or more deuterium or fluorine atoms, or taken together with the carbon atom bearing the group X can form a C.sub.3-8 carbocyclic ring; Q is a single bond or a C.sub.1-8 hydrocarbylene diradical which is optionally substituted with one or more deuterium or fluorine atoms; and derivatives of formula I. The compounds show anti-inflammatory and immunomodulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells.