Abstract: The invention provides compounds of the formulas ##STR1## which are useful as intermediates for the preparation of 6-demethyl-6-deotetracycline antibiotic agents.

Abstract: Disclosed are 17-iminomethylalkenyl and 17-iminoalkyl-14.beta.-hydroxy-5.beta.-androstane derivatives of the formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration or a Z or E configuration; A represents (CH.sub.2).sub.m or --(CH.dbd.CH).sub.n --; m represents an integer number from 1 to 6; n represents an integer number from 1 to 3; R.sup.2 represents hydrogen or hydroxy; R.sup.1 represents hydrogen, C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5, which may be the same or different, represent hydrogen, C.sub.1 -C.sub.4 alkyl or R.sup.4 and R.sup.5 may form, when taken together with the nitrogen atom, a five- or six- membered heterocyclic ring optionally containing one or more heteroatoms selected from oxygen and nitrogen; R.sup.3 represents NHC(.dbd.X)NR.sup.6 R.sup.7 or OR.sup.8 wherein R.sup.6 and R.sup.7, which may be the same or different, represent hydrogen, methyl, or C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.

Abstract: The invention presents 17.beta.-nitro and 11.beta., 17.beta.-dinitro esters of estradiol which are made from 3-acyloxy-17-keto- or 3,17-dihydroxy-1,3,5-estratrienes by processes known in the art. The compounds exhibit estrogenic activity.

Abstract: The present invention relates to intermediates for use in the preparation of taurocholanic acids. The intermediates have the following formula (IV): ##STR1## in which A completes the 5.beta.-cyclopentaneperhydrophenanthrene structure of a cholanic acid; E is hydrogen or a methyl; and R is a hydrocarbon residue bonded to the carbonyl group by a tertiary carbon.

Abstract: The invention presents compounds useful for the prevention of inflammatory or allergic reaction or the treatment of cardiovascular or haemodynamic disorders having the formula: ##STR1## where R= ##STR2## where R= ##STR3## or pharmaceutically acceptable acids or salts thereof.

Abstract: The invention relates to 11 .beta.-substituted 14,17-ethanoestratrienes of the general formula 1 ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are defined in the specification. The compound have antiestrogenic activity and are, therefore, useful for the treatment of estrogen dependent disorders.

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. Cl.sub.2 and imidazole, or PPh.sub.3 and CCl.sub.4. The disclosed process selectively forms .increment..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-.increment..sup.9,11 steroids.

Abstract: Novel steroids having a 9.alpha.-hydroxy or a 9.alpha.-carbonate substituent can be prepared from 9.alpha.-hydroxyandrostenedione and can be utilized in the synthesis of commercially valuable corticosteroids such as betamethasone. The 9.alpha.-carbonates are prepared by reaction of the corresponding 9.alpha.-hydroxy steroid with a sequence of excess base, trialkylsilyl chloride, alkyl haloformate and alkanol or by using excess base, alkyl haloformate and alkoxide. 9.alpha.-Carbonate-17-keto compounds can be treated with lithium acetylide and a lithium salt to afford the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-9.alpha.-carbonate. This compound is then esterified with a novel series of reagents to give the 17-ester which can be reduced the corresponding 17-allene. Oxidation of this allene to the bis-epoxide compound, followed by treatment with an alkali metal salt of a carboxylic acid under phase transfer conditions gives the 17.alpha.-hydroxy 21-ester 9.alpha.-carbonate. Elimination of the 9.alpha.

Abstract: The invention discloses N-alkyl-tauroursodeoxycholic acids and their pharmaceutically acceptable salts of the formula ##STR1## wherein R is a C.sub.2 -C.sub.4 alkyl group and R.sub.1 is hydrogen, an alkali metal, an alkaline earth metal or a radical of a basic amino acid.The compounds are prepared by reacting a mixed anhydride of ursodeoxycholic acid and alkyltaurine followed by percolation through two columns respectively containing a strong cationic resin in H.sup.+ form and a weakly anionic resin OH.sup.- form. The compounds are useful for the treatment of hepatic diseases.

Abstract: Compositions which, in the form of aqueous dispersions or of solutions in organic solvents, are suitable for the treatment of fiber materials can be obtained by reaction of organic phosphites and quinones and subsequent reaction with mono-, di- or polyisocyanates. Flame-retardant properties having a good permanence are imparted, above all, to fabrics comprising polyester fibers by this procedure.

Abstract: This invention relates to 8.alpha.-3-hydroxyestra-1,3,5(10),9(11)tetraen-17-one (.DELTA.9(11)-dehydro-8-isoestrone) (VI), ##STR1## to the process for its preparation, to pharmaceutical compositions containing said 8.alpha.-3-hydroxyestra-1,3,5(10),9(11)tetraen-17-one (.DELTA.9(11)-dehydro-8-isoestrone) (VI) and to the use of said 8.alpha.-3-hydroxyestra-1,3,5(10),9(11)tetraen-17-one (.DELTA.9(11)-dehydro-8-isoestrone) (VI) for modifying the balance between bone production and bone resorption, and as an antioxidant in a host animal, including man.

Abstract: There are described spontaneously dispersible agents containing sterolester and/or sterolphosphor compounds having a pronounced antitumour activity. Novel sterolesters and sterolphosphor compounds, their use for treating tumors, and processes for their preparation are disclosed.

Abstract: Vitamin D.sub.2 analogs in which a cyclopentane ring is introduced onto the 25-carbon of the side chain of 1.alpha.,25-dihydroxyvitamin D.sub.2 and its 24-epimer. 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 calcemic activity, these compounds would be useful for the treatment of diseases where bone formation is desired, such as osteoporosis.

Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.1 and Y are defined in the specification. The compounds are useful for the production of 6-demethyl-6-deoxytracycline derivatives.

Abstract: The invention provides a process for the production of compounds of the formula: ##STR1## wherein R, R.sup.3, R.sup.4 and W are defined in the specification in which a compound of the following formula: ##STR2## is reacted with a nucleophile of the formula WH in an inert atmosphere in the presence of a polar aprotic solvent. The resulting compounds are useful as antibiotics.

Abstract: The invention provides compounds of the formulas ##STR1## which are useful as intermediates for the preparation of 6-demethyl-6-deotetracycline antibiotic agents.

Abstract: The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula ##STR1## wherein R, X, R.sup.5 and R.sup.6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics.

Abstract: The invention provides a process for the production of compounds of the formula: ##STR1## wherein, R, R.sup.3, R.sup.4, X and W are defined in the specification in which a compound of the following formula: ##STR2## is reacted with a nucleophile of the formula WH in an inert atmosphere in the presence of a polar-protic or a polar-aprotic solvent. The resulting compounds are useful as antibiotics.

Abstract: Disclosed is a method of inhibiting the growth of tumors by administering an estradiol derivative-alkylating agent conjugate of the formula (I'): ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3. Also disclosed is a method of inhibiting the growth of tumors by administering a compound of the formula (II); ##STR2## wherein R.sup.1 is C.sub.1-4 alkyl 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 0 to 3; and X is hydroxy or halogen.

Abstract: Vitamin D.sub.3 analogs in which a double bond has been introduced into the side chain between carbons 20 and 22. The compounds are characterized by a marked intestinal calcium transport activity while exhibiting much lower activity than 1.alpha.,25-dihyroxyvitamin D.sub.3 their ability to mobilize calcium from bone. Because of their preferential calcemic activity, these compounds would be useful for the treatment of diseases where bone formation is desired, such as osteoporosis. The compounds also have relatively high HL-60 cell differentiation activity making them useful for the treatment of diseases characterized by abnormal cell differentiation or cell proliferation, such as psoriasis.