Abstract: Described is a new process for producing 7.beta.-substituted-4-aza-5.alpha.-androstan-3-ones and related compounds which are 5.alpha.-reductase inhibitors, consisting of reducing the corresponding androsteneone with lithium and liquid ammonia, contacting the product with an isomerizing agent, oxidizing the product to a seco acid and reacting that seco acid with an amine to cyclize to form 4-aza-5.alpha.-androstan-3-ones.

Abstract: Compounds are provided of the formula: ##STR1## wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, (C.sub.6 -C.sub.12)aryl, (C.sub.6 -C.sub.12)aralkyl, trans(C.sub.4 -C.sub.5)alkenyl, allyl or furan-2-ylalkyl, R.sup.2 is H, OH or O.sub.2 C(C.sub.1 -C.sub.5)alkyl; R.sup.3 is H, (C.sub.6 -C.sub.10)aralkyl, (C.sub.1 -C.sub.5)alky or (C.sub.1 -C.sub.5)alkylCO; X is O, S or NY, wherein Y is H, benzyl or (C.sub.1 -C.sub.5)alkyl; R is CH(Z)CO.sub.2 Y, wherein Z is H, CH.sub.2 CO.sub.2 Y or (CH.sub.2).sub.n N(R.sup.4)(R.sup.5), wherein n is 1-5 and R.sup.4 and R.sup.5 are individually H, (C.sub.1 -C.sub.4)alkyl, phenyl, (C.dbd.NH)NH.sub.2, benzyloxycarbonyl or (C.dbd.NHNO.sub.2); and the pharmaceutically acceptable salts thereof.

Abstract: Disclosed are pharmaceutical compositions that comprise gallium complexes of 3-hydroxy-4-pyrones. These compositions provide enhanced gallium bioavailability particularly when orally administered as compared to the gallium bioavailability achieved by use of pharmaceutical compositions containing gallium salts. Compositions included in this invention are useful in providing gallium to humans and other mammals for a wide variety of medical and veterinary applications, including the treatment, prevention, or diagnosis of hypercalcemia, certain cancers, certain disorders of calcium homeostasis, and certain bone diseases including osteoporosis, osteopenia, and Paget's disease.

Abstract: The present invention relates to compounds of the formula: ##STR1## wherein R is H or alkyl;Y.sup.1 is --CH.dbd. or --N.dbd.; andY.sup.2 --CH.dbd., --C(OH).dbd., --C(NO.sub.2).dbd., --C(NH.sub.2).dbd., --C(Hal).dbd., --N.dbd.;X is cycloalkenyl; bicyclo[2.2.1]hept-2-yl, optionally substituted by phenyl-2-oxo-5 -methoxymethyl-oxazolidinyl; bicyclo[2.2.1]-hept-5 -en-2-yl; adamantyl; or cycloalkyl or piperidinyl, optionally substituted by amino, alkyl, --CN, oxo hydroxyimino, ethylenedioxyor by --OR.sup.1,R.sup.1 is --CH(C.sub.6 H.sub.5).sub.2, --(CH.sub.2).sub.n C.sub.6 H.sub.5, alkyl, H, --(CH.sub.2).sub.n NHCOCH.sub.3, --(CH.sub.2).sub.n NH.sub.2, --(CH.sub.2).sub.n CN, --(CH.sub.2).sub.n SCH.sub.3 --(CH.sub.2).sub.n SO.sub.2 CH.sub.3, --CO-lower-alkyl, --COC.sub.6 H.sub.5, optionally substituted by oxazolidine;or by .dbd.CR.sup.2 R.sup.3,R.sup.2 is alkylR.sup.3 is H, --CN, alkyl, phenyl or COO-alkyl;or by --(CH.sub.2).sub.n R.sup.4R.sup.4 is --CN, amino, --NHCOCH.sub.3, --COC.sub.6 H.sub.

Abstract: The compound (-)-[[4-(1,4,5,6 tetrahydro-4-methyl-6-oxo-3 pyridazinyl) phenyl]-hydrazono] propane dinitrile and its salts are prepared and used for treating congestive heart failure.

Abstract: Replacement with fluorine of the primary hydroxy group of 1-phenyl-2-amino-1,3-propanediol compounds wherein the secondary hydroxy group and the amino group have been suitably protected.The reaction is carried out with an inorganic fluoride in a polyglycol.New oxazoline compounds particularly useful in said process.

Abstract: Compounds of formula (I): ##STR1## wherein R.sub.3, R.sub.4, R.sub.5, R.sub.6, X and Y are defined in the description.Those compounds are used therapeutically in the treatment of cancerous tumours.

Abstract: The present invention relates to the compound of formula (I), ##STR1## also known as 17.beta.-N-(2,5-bis(Trifluoromethyl))phenylcarbamoyl-4-aza-5.alpha.-andros t-1-en-3-one, solvates thereof, its preparation, intermediates used in its preparation, pharmaceutical formulations thereof and its use in the treatment of androgen responsive and mediated diseases.

Abstract: An ellipticine derivative of the formula [I]: ##STR1## wherein R is a substituted lower alkyl group, a substituted or unsubstituted lower alkoxy group or a heteromonocyclic group,or a pharmaceutically acceptable salt thereof, which show excellent antitumor activity, less side effects, less toxicity and/or high solubility in water and are useful as antitumor agent, and a process for preparing the same.

Abstract: Novel oxazolidinone derivatives of the formula I ##STR1## in which R.sup.1 is a phenyl radical which is unsubstituted or is monosubstituted by CN, H.sub.2 N--CH.sub.2 --, A.sub.2 N--CH.sub.2 --, H.sub.2 N--C(.dbd.NH)--, H.sub.2 N--C(.dbd.NH)--NH--, H.sub.2 N--C(.dbd.NH)--NH--CH.sub.2 --, HO--NH--C(.dbd.NH)-- or HO--NH--C(.dbd.NH)--NH--,X is O, S, SO, SO.sub.2, --NH-- or --NA--,B is ##STR2## or ##STR3## A is alkyl having from 1 to 6 C atoms,R.sup.2 is H, A, Li, Na, K, NH.sub.4 or benzyl,R.sup.3 is H or (CH.sub.2).sub.n --COOR.sup.2,E is, in each case independently of each other, CH or N,Q is O, S or NH,m is 1, 2 or 3, andn is 0, 1, 2 or 3,and physiologically compatible salts thereof are provided, which inhibit the binding of fibrinogen to the corresponding receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and also tumors.

Abstract: An oxazoline derivative having the formula: ##STR1## which is useful for control of insects, mites and/or ticks.

Abstract: The biologically active enantiomer of .gamma.-methylene-10-deazaaminopterin (L-MDAM) possessing the L configuration at the .gamma.-methyleneglutamate moiety, which is identical to the absolute configuration at the .alpha.-position of the .gamma.-methyleneglutamic acid isolated from peanut seedlings is provided as well as procedures for its preparation. The compound does not undergo polyglutamylation, is twice as effective as an inhibitor of recombinant human dihydrofolate reductase, and exhibits outstanding growth inhibitory activity in a large variety of human tumor cells in culture. The biochemical and pharmacological results established the utility of L-MDAM as a therapeutic agent for the treatment of human neoplastic diseases.

Abstract: 3(2H)-Pyridazinone derivatives of the general formula I ##STR1## where R.sup.1 is alkyl, R.sup.2 is hydrogen or alkyl, X is halogen, W is oxygen or sulfur and Z is a hetaryl-substituted isoxazolyl radical or a substituted or unsubstituted cyclohexyl or cyclopentyl radical, plant-tolerated salts thereof, processes for their manufacture, and their use as pesticides.

Abstract: The present invention is directed to a new class of beta-ketone, beta oxime and beta hydrazine phosphonate NMDA antagonists.

Abstract: Disclosed are certain 3-pyrazolyloxypyridazines, compositions thereof which are herbicidal and methods of using such composition for controlling undesired plants. Also disclosed are mixtures of such pyridazines and acetanilide herbicides, to which mixture a safener may be added, if desired. Intermediate compounds useful in preparing the pyrazolyloxypyridazines are also disclosed.

Abstract: Compounds of Formula I ##STR1## wherein Z contains an ether or thioether moeity, are inhibitors of the 5.alpha.-reductase enzyme and isozymes thereof. The compounds are useful for the treatment of hyperandrogenic disease conditions and diseases of the skin and scalp.

Abstract: Retinold-like activity is exhibited by compounds of the formula ##STR1## where X is S, O or NR'; where R' is hydrogen or lower alkyl; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is pyridazinyl, pyrazinyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.

Abstract: Polycyclic vat dyes of the general formula I ##STR1## where X is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, halogen or nitro, obtainable by reacting (9)-benzo-5-aminoanthraquinonyl(2,1-h)-8-azapyrenone-3(II) ##STR2## with a benzoyl chloride of the formula III ##STR3## in a dipolar aprotic solvent.

Abstract: Described are new 7.beta.-substituted 4-aza-5.alpha.-cholestan-3-ones and related compounds as 5.alpha.-reductase inhibitors.

Abstract: Invented are 17.beta.-substituted acyl-4-aza analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates and processes used in preparing these compounds.