Abstract: Described is a process for the regioselective dehydration of 11-hydroxy steroids using PCl.sub.5, PCl.sub.3, POCl.sub.3 or either SO.sub.2 Cl.sub.2 and imidazole, or PPh.sub.3 and CCl.sub.4. The disclosed process selectively forms .DELTA..sup.9,11 steroids from either 11-.alpha.- or 11-.beta.-hydroxy steroids, and can also be used for the one-step conversion of 11,21-dihydroxy steroids to 21-chloro-.DELTA..sup.9,11 steroids.Also disclosed are processes for the regioselective conversion of 11-.beta.-chloro steroids to .DELTA..sup.9,11 steroids, and for regioselectively converting an 11,17,21-trihydroxy streoid to a 21-chloro-11,17-dihydroxy steroid.

Abstract: Cyclohexylidene compounds of the structure: ##STR1## where X.sup.1 and X.sup.2, which may be the same or different, is hydrogen or a hydroxy-protecting group, and Y is --POPh.sub.2, or --PO (OAlkyl).sub.2, or --SO.sub.2 Ar, or --Si(Alkyl).sub.3. The compounds are used as intermediates in the preparation of 19-nor-vitamin D compounds.

Abstract: A compound of formula I ##STR1## wherein R stands for a straight or branched, saturated or unsaturated alkyl group containing from 4 to 12 carbon atoms optionally substituted with a hydroxy group, and possibly containing a ring structure, and in which at least one of the carbon atoms not bearing hydroxyl group is substituted with one or more halogen atoms or an azido group; and prodrugs of I in which one or more of the hydroxy groups are masked as groups which can be reconverted to hydroxy groups in vivo, in pure form or in mixtures. The compounds show antiinflammatory and immunomodulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells. The compounds are prepared by oxidizing 1(S),3(R)-bis-(tert-butyldimethylsilyloxy)-20(S)formyl-9,10-seco-pregna-5( E),7(E),10(19)-triene, reducing the resulting product; alkylating the reduction product and then subjecting the alkylated product to triplet-sensitized photoisomerization.

Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine, and X is H.sub.2 or .dbd.CH.sub.2 are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of cancer, such as, leukemia, and as agents for the treatment of sebaceous gland diseases, such as, acne and seborrheic dermatitis.

Abstract: New steroidal polyamines have the structure of formula I or formula II: ##STR1## wherein R.sub.1 and R.sub.2 are independently N(R').sub.3.sup.+ or H in the .alpha.- or .beta.- position except both R.sub.1 and R.sub.2 are not H;R.sub.3 is N(R').sub.3.sup.+ in the .alpha.- position or hydrogenR.sub.4 is OH, N(R').sub.3, or NHC(NH.sub.2)NH.sub.2.sup.+R' is hydrogen, alkyl of one to four carbons, aralkyl, or combinations thereof.

Abstract: This invention is directed to 2-aminoalkyl-5-aminoalkylamino substituted isoquino[8,7,6-cd]indazole-6-(2H)-ones and to 2-aminoalkyl-5-aminoalkylamino substituted-isoquino[5,6,7-cd]indazole-6(2H)-ones. These compounds have been shown to have antitumor activity.

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 dimethyl formamide; at a temperature within the range of about -78.degree. to about 0.degree. C., under anhydrous conditions under an inert atmosphere.

Abstract: The invention describes hydrazino and hydroxyamino-14.beta.-hydroxyandrostane derivatives having general formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration and A, B, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 have the meanings given in the description and their use in the treatment of cardiovascular disorders such as heart failure and hypertension.

Abstract: A synthesis of 1.alpha.-hydroxy-19-nor-vitamin D compounds comprises (a) the construction of a 5,8-diol-6-yne intermediate by joining ring-A and ring-C/D portions of the desired end product via the condensation of an acetylenic derivative containing the C/D-ring portion of the desired end product with a cyclic dihydroxy ketone representing the A-ring of the desired end product; (b) the partial reduction of the 6,7 acetylenic triple bond linkage between the A and C/D ring portions to obtain a 5,8-diol-6-ene intermediate; and (c) the reductive removal of the 5,8-oxygen functions to generate the required 5,7-diene end product from which the desired 7-trans(7E)-isomer is purified directly, or after optional double bond isomerization of the 7-cis(7Z)-isomer employing a novel thiophenol-promoted isomerization step.

Abstract: The invention is drawn to a compound having the following formula ##STR1## in which X.sup.1 and X.sup.2, which may be the same or different, represent hydrogen or a hydroxy-protecting group, X.sup.4 is hydrogen, A is selected from --COOAlkyl and CH.sub.2 OH, and B is a hydroxy group, or A and B, when taken together, represent an oxo group. These compounds are useful as intermediates in the production of 19-nor vitamin D derivatives.

Abstract: A new process for the preparation of 16.beta.-methyl-steroids of the formula ##STR1## and novel intermediates therefor which compounds are intermediates for betamethasone.

Abstract: An improvement in a process for producing 3.beta.,14.beta.-dihydroxyethianaldehyde is disclosed wherein the oxidation of the lactone ring of digitoxigenin-3-acetate is conducted with an alkaline periodate in the presence of a catalytic amount of ruthenium tetroxide obtained in situ by reacting RuO.sub.2 hydrate or RuCl.sub.3 with the alkaline periodate.

Abstract: Agents for enhancing the contrast in a diagnostic ultrasound procedure comprise colloidal dispersions of the liquid-in-liquid type, i.e., emulsions or microemulsions, in which the dispersed liquid phase is a high vapor pressure chemical which undergoes a phase change from a dispersed liquid to a highly echogenic dispersed gaseous foam or kugelschaum following administration to an organism. The liquid state of the dispersed phase allows one to manufacture extremely stable, pharmaceutically acceptable emulsions with particle sizes typically below 1000 nm. The gaseous state at body temperature yields highly echogenic microbubbles, typically below 10,000 nm in diameter, which are effective as ultrasound contrast agents. Intravenous, intraarterial, oral, intraperitoneal, and intrauterine dosage forms, methods of administration, and imaging techniques are described.

Abstract: The invention describes a process for the preparation of the polymorph A form of a compound having the structure ##STR1## which involves triturating, crystallizing, or precipitating crude N-t-butyl-androst-3,5-diene-17.beta.-carboxamide-3-carboxylic acid from an ethyl acetate or t-butyl methyl ether solvent, followed by isolation of the polymorph A.

Abstract: Compounds of formula ##STR1## wherein Q is a --CH.sub.2 --, --CH.dbd.CH-- or --C.dbd.C--; U is a C.sub.1 -C.sub.6 alkylene; R.sup.1 is hydrogen, a C.sub.1 -C.sub.4 alkyl or YR' in which Y stands for the radicals --SO-- or --SO.sub.2 -- and R' stands for a C.sub.1 -C.sub.4 alkyl; R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1 -C.sub.4 alkyl, and additionally R.sup.2 and R.sup.3, when taken together with the starred carbon atom, may form a C.sub.3 -C.sub.6 carbocyclic ring; Z is hydrogen or hydroxy; and derivatives thereof. The compounds show antiinflammatory and immunomodulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells. The compounds are prepared by adding an anion R.sup.- to 1(S),1(R)-bis-(tert-butyldimethylsilyl-oxy)-9,10-secopregna-5(E),7(E),10(1 9)-triene-20-one and the resulting compound is alkylated or acylated with R.sup.1 X.sup.1 where X.sup.

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 vitamin D compounds have the formula: ##STR1## where X.sup.1 and X.sup.2 are each hydrogen or a hydroxy protecting group and R is a side chain.

Abstract: The present invention is directed toward the use of 20-epi-vitamin D.sub.3 analogs to treat low bone turnover osteoporosis. The 20-epi compounds are characterized by a marked intestinal calcium transport activity while exhibiting much higher activity than 1.alpha.,25-dihydroxyvitamin D.sub.3 in their ability to mobilize calcium from bone.

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 discloses steroid conjugates having the following structure: ##STR1## where Y is NHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, NH(CH.sub.2).sub.3 NH(CH.sub.2).sub.4 NH(CH.sub.2).sub.3 NH.sub.2, or NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2, and each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is individually H, OH and OSO.sub.3 H. These conjugates posses antimicrobial properties and are, therefore, useful as antibiotics.

Abstract: New 25-carboxylic acid derivatives of general formula I, ##STR1## R.sup.19 and R.sup.19a each mean a hydrogen atom or together form an exocyclic methylene group,R.sup.21 and R.sup.21a independently of one another mean a hydrogen atom, a chlorine or fluorine atom, an alkyl group with 1 to 4 carbon atoms, together a methylene group, together with quaternary carbon atom 20 mean a 3-7 membered, saturated or unsaturated carboxylic ring,Y preferably means a derivatized carboxyl radical, and the other substituents have the meanings indicated in the description as well as process for their production, are described.The new compounds have vitamin D activity as well as proliferation-inhibiting and cell-differentiating effects and are suitable for the production of pharmaceutical agents.