Abstract: The unsaturated 17.alpha.-cyanomethyl-17.beta.-hydroxy steroids of the formula I, ##STR1## in which R.sub.1 =Me, Eth; R.sub.2 =H, Me; R.sub.3 =H, OH, an acetoxy or alkoxy group; R.sub.4 =H, R.sub.5 =OH, an acetoxy, alkoxy group of R.sub.4 and R.sub.5 together represent a keto- or ketal group and double bonds are contained in the basic structure of the steroid, particularly between the 15 and 16 position in the steroid ring, from unsaturated 17-ketosteroids of the general formula II as described herein with the aforementioned meanings of R.sub.1 to R.sub.5 by reacting the unsaturated 17-ketosteroids with LiCH.sub.2 CN and subsequently hydrolyzing.The compounds of formula I are pharmacologically interesting steroid compounds or also intermediate products for the synthesis of highly-effective steroid products which can be used in human and veterinary medicine for the treatment of endocrine disorders and for reproductive control based on their specific hormonal/anti-hormonal actions.

Abstract: The present invention relates to 3-aryl-oxirane derivatives of the formula ##STR1## wherein Ar is 4'-quinoline or 5'-quinoline; each of R and R.sub.1 independently is hydrogen or C.sub.1 -C.sub.6 alkoxy; one of X and Y is hydrogen, cyano, --COOR.sub.2 or --CONR.sub.3 R.sub.4, and the other of X and Y is cyano, --COOR.sub.2 or --CONR.sub.3 R.sub.4, wherein R.sub.2 is C.sub.1 -C.sub.6 alkyl and each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.6 alkyl, and pharmaceutically acceptable salts thereof, which are useful in therapy as tyrosine kinase inhibitors, in particular as anti-proliferative agents, typically as anti-cancer agents, in the treatment of psoriasis and in inhibiting the development of atheromatous plaque.

Abstract: Methods of treating an immune disease, cell proliferation, restenosis and vascular smooth muscle cells using the pharmaceutical compounds of the formula ##STR1## in which R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl; and salts thereof.

Abstract: Reaction products of dialkyltin oxide and polyhydric phenols.These reaction products are suitable as catalysts with improved properties for curing coating binders.

Abstract: The object of the invention is to provide a novel compound having serotonin antagonist activity.The invention is directed to an indolecarboxamide derivative of the following general formula [I] and a serotonin antagonist composition comprising the same derivative as an active ingredient. ##STR1## (wherein R.sup.1 is a lower alkyl and R.sup.2 is hydrogen, a halogen, a lower alkyl or a lower alkoxy.)The compound of the invention is effective as a gastrointestinal motor activity regulator, antimigraine, antipsychotic or antianxiety drug. The compound is also effective as a therapeutic drug for dementia or orthostatic hypotension.

Abstract: Dioxetane compounds reactable with an enzyme to release optically detectable eneregy are disclosed. These compounds have the formula: ##STR1## wherein T is a carboxylic acid or methoxy substituted adamantyl group bound to the ring through a spiro bond, Y is phenoxy or napthyloxy and X is methoxy, ethoxy or propoxy. Z is an enzyme cleavable group such that when cleaved by an enzyme, an electron rich moiety is left bound to the dioxetane ring.

Abstract: The invention relates to the compounds of formula (I): ##STR1## in which: R.sub.1 represents a linear or branched, lower or higher alkoxy group or a substituted or unsubstituted amino group,R.sub.2 represents a lower alkyl group unsubstituted or substituted with an amino group,R.sub.3 represents an amino, lower or higher alkoxy or a hydroxyl group, with the proviso, however, that at least one amino group is present in R.sub.1 or R.sub.3,R.sub.4 represents a hydrogen atom or an aryl group,m is equal to 1 or 2,n is between 1 and 6, andRa and Rb, which may be identical or different, represent a hydrogen atom when m=1, or a hydrogen atom or an alkyl group when m=2 andmedicinal products.

Abstract: An antitumor substance BE-12406 or a pharmaceutically acceptable salt thereof, which is represented by the general formula ##STR1## and a method of producing the novel substance.

Abstract: Novel 1-substituted 1H-imidazo-[4,5-c]quinolin-4-amines are disclosed. These compounds function as antiviral agents, and they are potential synthetic intermediates in the preparation of known antiviral agents and labeled known antiviral agents. This invention also provides intermediates for preparing such compounds, pharmaceutical compositions containing such compounds, and pharmacological methods of using such compounds.

Abstract: A pyrazole derivative having the formula: ##STR1## wherein A is alkyl, alkenyl or alkynyl; B is hydrogen, alkyl, halogen, haloalkyl, alkoxy, alkylthio, alkoxyalkyl, alkylthioalkyl or alkoxycarbonyl; X is alkyl, alkoxy, halogen, nitro, cyano, haloalkyl, alkoxyalkyl, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl substituted by hydrogen or alkyl, haloalkoxy, alkylthio or alkylthioalkyl; Y is --COOR1 (wherein R1 is hydrogen, alkyl, etc.), --COO--L--OR1 (wherein L is alkylene which may be substituted), --COO--L--R2 (wherein R2 is phenyl group which may be substituted), --COO--M (wherein M is 3 to 6-membered alicyclic residue containing not more than 2 sulfur or oxygen atoms), --COO--L--M, --COO--L--O--L--R2, --COO--L--S(O).sub.n --CON (R3) (R4) (wherein each of R3 and R4 is hydrogen, alkyl, etc.), a --CON--(CH.sub.2).sub.n, ##STR2## wherein R5 is alkyl), ##STR3## --CONHSO.sub.2 CH.sub.3, --CONHSO.sub.2 CF.sub.3, --COO--L--N(R3) (R4), --COO--L--CO--R1, --COO--L--CO--O--R1, --COO--L--CN, --Coo--L--NO.sub.

Abstract: Methods and compositions are provided to facilitate the transportation and combustion of highly viscous hydrocarbons by forming reduced viscosity hydrocarbon-in-water emulsions, and in particular, bioemulsifier-stabilized hydrocarbon-in-water emulsions.

Abstract: A conditioning agent is disclosed, for the pre-treatment of base materials for subsequent complete and uniform chemical metallization, characterized by a content of a quaternary organic nitrogen compound. Also disclosed is a process for the pre-treatment of base materials, employing said conditioning agent. Preferred embodiments include as active agent at least one compound of the general formula ##STR1## represents a cyclical nitrogen compound, R is hydrogen, C.sub.1 -C.sub.4 -alkyl or hydroxy-C.sub.1 -C.sub.2 -alkyl,n is 0 or 1, andX.sup.(-) is the anion of an inorganic or an organic acid.

Abstract: A reference liquid for calibration or quality control of instruments which determine ionized calcium and pH. The reference liquid contains both a particular calcium ion activity and a pH-buffer and can therefore be used for calibration of both the calcium-sensitive electrode and the pH-electrode in the instruments. The pH-buffer is a nitrogen-containing organic sulphonic acid and the salt of this acid, the acid having a pK in the range of 6.6-7.6. The reference liquid has an ionic strength of 0.15-0.17, a buffer capacity .beta. in the range of 0.04-0.10 and is packed in glass ampoules.

Abstract: N-Alkyl-benzenesulphonamides, the alkyl group of which is open-chain C.sub.1 -C.sub.12 -alkyl or C.sub.5 -C.sub.7 -cycloalkyl and the benzene nucleus of which can be substituted by C.sub.1 -C.sub.4 -alkyl, can be heat-stablized by 10-1,000 ppm of one or more 2-mercapto-benzimidazole compounds of the formula ##STR1## wherein R.sup.1 denotes hydrogen of a C.sub.1 -C.sub.4 -alkyl group andX.sup.1 denotes hydrogen or 1 equivalent of the metals Zn, Cd or Mn(II).Such stabilized N-alkyl-benzenesulphonamides can be used as plasticizers for polymers having polar groups.

Abstract: Vaccines are provided which are composed of (a) non-toxic and highly effective adjuvants obtained from microbial sources, together with (b) tumor antigens. A wide variety of antigens can be employed in the vaccines and include, antigens obtained from tumors or cultures of tumor cells, such as ovarian cancers, melanomas, colorectal cancers, pancreatic cancers, renal cancers and the like. By adding tumor antigens to potent but non-toxic immunostimulants, a protective and lasting tumor immunity can be obtained.

Abstract: Penetration-enhancing pharmaceutical compositions for topical transepidermal and percutaneous application are disclosed which are non-irritating to the skin. These compositions are made up of a safe and effective amount of an active pharmaceutical permeant, including hydrophilic salt forms, contained in a novel penetration-enhancing vehicle comprising, (i) 1-95% w. of a cell-envelope disordering compound selected from the group consisting of oleic acid, oleyl alcohol, glycerol monoleate, glycerol dioleate, glycerol trioleate and mixtures thereof, (ii) 5-75% w., and preferably 5-49% w., of a lower alkanol selected from the group consisting of ethanol, propanol and isopropanol and mixtures thereof and (iii) 0-45% w., and preferably 1-45% w., of an inert diluent which, according to properties of the permeant used, may range from hydrophilic to hydrophobic. Water, polyethylene or polypropylene glycols and mineral oil are exemplary diluents.