Abstract: To provide novel steroid derivatives having an antitumor action which can be synthesized efficiently and stereoselectively by means of synthetic organic chemistry. A steroid derivative represented by the formula: ##STR1## wherein R is an alkyl group having 1 to 13 carbon atoms, A is a hydroxyl group or a group easily hydrolyzable to a hydroxyl group, X and Y together form an oxo group or an alkylenedioxy group having 2 or 3 carbon atoms, X is a hydroxyl group, an alkoxy group having 1 to 5 carbon atoms or a group easily hydrolyzable to a hydroxyl group, Y is a hydrogen atom or an alkoxy group having 1 to 5 carbon atoms, with the proviso that when X is a hydroxyl group or a group easily hydrolyzable to a hydroxyl group, Y is a hydrogen atom, and when X is an alkoxy group having 1 to 5 carbon atoms, Y is an alkoxy group having 1 to 5 carbon atoms, or a salt thereof.

Abstract: Sialic acid derivatives represented by the general formula (I): ##STR1## wherein R.sup.1 is a steroidal compound residue; R.sup.2 is H or alkyl;R.sup.3 is alkyl; ##STR2## wherein each of R.sup.6 and R.sup.7 is H, alkyl or the like and I is an integer of 0 to 6; or the like;X is O or S;R.sup.4 is H or acyl; and R.sup.5 is R.sup.14 O-- (R.sup.14 is H or acyl) or R.sup.15 NH--(R.sup.15 is acyl or the like);their salts, hydrates or solvates are provided.Sialic acid derivatives of the present invention are expected to be effective medicines for the prevention and therapy of senile dementia including Alzheimer's disease and the like, because they increase ChAT activity in cholinergic neurons.

Abstract: The present invention relates to a method of using a perchloric acid catalyzed reaction to make acyl derivatives of norprogesterone compounds and, in particular, 16-methylene-17.alpha.-hydroxy-19-norpregn-4-ene-3,20-dione.

Abstract: The invention relates to 20(S)-vitamin D compounds having the following formula ##STR1## where U and R' are as defined in the specification. The compounds have strong antiinflammatory and immunomodulating activity. There are also useful in the inhibition of proliferation of undesirable cells.

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.

Abstract: A 19-nor-steroid having a formula selected from the group consisting of ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2##

Abstract: To remove the unsaturated impurities (in particular 1-chloro-2,2-difluoroethylene and polyfluoropropenes) present in crude 1,1,1,2-tetrafluoroethane (F134a), a gaseous mixture of crude F134a, of hydrofluoric acid and of chlorine is treated in gaseous phase in the presence of a fluorination catalyst at a temperature of between 100.degree. and 300.degree. C. and at a pressure between atmospheric pressure and 2.5 MPa, the molar ratio HF/F134a being between 0.05 and 0.5 and the molar ratio Cl.sub.2 /F134a between 0.0001 and 0.1.

Abstract: The present invention is directed to steroidal or terpenoidal compounds which inhibit farnesyl-protein transferase (FPTase). The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.

Abstract: In this invention, the new etheno- and ethano-19,11-bridged 4-estrenes of general formula I ##STR1## are described, in whichW, R.sup.1, R.sup.2, R.sup.6a, R.sup.6b, R.sup.7, R.sup.14, R.sup.15, R.sup.16, R.sup.11, R.sup.11' and R.sup.19 have the meaning indicated in the description, as well as a process for their production.The new compounds have strong progestational activity and are suitable for the production of pharmaceutical agents.

Abstract: The invention relates to vitamin D derivatives, modified in 20-position, of general formula I ##STR1## in which X, Y, Z, R.sub.1, R.sub.2 as well as R.sub.3 have the meaning indicated in the description, process for their production and their use as agents for treatment of hyperproliferative diseases of the skin.

Abstract: The invention recites a process for preparing 9,10-secocholesta-5,7,10(19)-trienes of formula (I) ##STR1## where R.sup.1 is hydrogen or a hydroxy-protecting group and R.sup.2 and R.sup.3 are independently hydrogen or OR.sup.1. The compounds are prepared from epoxides of the following formulas ##STR2## by reaction with a low-valent metal reagent formed by reducing a metal halide, M(z)X.sub.z, preferably WCl.sub.6.

Abstract: The invented compound ##STR1## is useful for the production of steroidal-17-amides that have 5.alpha.-reductase inhibitory activity.

Abstract: Angiostatic steroids for use in controlling ocular hypertension are disclosed. Pharmaceutical compositions of the angiostatic steroids and methods for their use in treating ocular hypertension, including controlling the ocular hypertension associated with primary open angle glaucoma, are disclosed. In addition, the combination of the compounds with glucocorticoids for the prevention of elevated IOP during the treatment of inflammation is disclosed.

Abstract: This invention relates to an improved process for the single step oxidation of 3-phenoxytoluene to 3-phenoxybenzaldehyde using molecular oxygen as the oxidant by employing a Ti.sub.2 VMoP.sub.6 O.sub.24 catalyst having particular infrared spectral bands.

Abstract: A progesterone compound represented by the following formula (1): ##STR1## ?wherein R.sup.1 represents a C1-C23 hydrocarbon group!, and a neovascularization inhibitor containing the same as the active ingredient.The compound (1) has a potent neovascularization inhibitory effect and is hence useful in the treatment of malignant tumors, diabetic retinitis, rheumatism, etc.

Abstract: The invention is a method of controlling fertility in male warm-blooded animals by administering a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 12 carbon atoms and aralkyl of 7 to 15 carbon atoms or taken together form a saturated heterocycle of 5 to 6 ring members optionally having a second ring heteroatom selected from the group consisting of sulfur, oxygen and nitrogen, R.sub.3 is an .alpha.-alkyl of 1 to 8 carbon atoms, n is an integer from 2 to 15, R.sub.4 is alkyl of 1 to 12 carbon atoms, R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and acyl of an organic carboxylic acid of up to 12 carbon atoms and the wavy lines indicate that the 17- and 20- asymmetrical centers are independent of the absolute R and S configurations and their non-toxic, pharmaceutically acceptable acid addition salts.

Abstract: Polyamines having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are alkyl, aralkyl or aryl having up to 10 carbon atoms; anda and b may be the same or different and are integers from 1 to 8; or a salt thereof with a pharmaceutically acceptable acid. Anti-neoplastic, anti-diarrheal, anti-peristaltic, gastrointestinal anti-spasmodic, anti-viral, anti-retroviral, anti-psoriasis and insecticidal compositions comprising biologically effective amounts of the above-described amines and biologically acceptable carriers therefor are also disclosed, as well as methods of treatment, administration or application of biologically effective amounts of the polyamines of the invention. Also disclosed are methods for preparing the polyamines of the invention.

Abstract: Disclosed is a process for producing a compound of the formula: ##STR1## by reacting a compound of the formula: ##STR2## with: (1) a chlorinating reagent selected from an N-chloroimide or an N-chloroamide; (2) an anhydrous strong acid selected from orthophosphoric acid, alkylsulfonic acids, fluoroalkylsulfonic acids or arylsulfonic acids; and (3) anhydrous dimethylformamide; at a temperature within the range of about -78.degree. to about 0.degree. C.

Abstract: A pharmaceutical compound of the formula ##STR1## in which R is hydrogen, halo or F.sub.2 HCO--; or a salt, amide or ester thereof, useful in the treatment of skeletal diseases.

Abstract: Bile acid derivatives of the formula IW--X--Gin which G is a bile acid radical, W is an active compound moiety of a medicament and X is a bonding member between a bile acid radical and active compound moiety, are outstandingly suitable for introducing active compounds into the enterohepatic circulation. The compounds I are absorbed and pass into the bloodstream. It is possible in this way, using the natural reabsorption of the bile acids, to achieve improved absorption of non-absorbable or poorly absorbable pharmaceuticals.W may be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a hepatoprotective agent, an antihyperlipidemic, a diuretic, a hypotensive, a renin inhibitor, a substance for the treatment of cirrhosis of the liver or a substance for the treatment of diabetes.G is a bile acid radical in the form of the free natural or chemically modified acids, the esters and amides, the salt forms and forms derivatized on alcohol groups.