Abstract: The present invention comprises peptidomimetic compounds which comprise a suitably aniline and aminoalkylbenzene moieties. The instant compounds inhibit the farnesyl-protein transferase enzyme and the farnesylation of certain proteins. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: The compounds (I) are useful as intermediates in the synthesis of hexahydroareno(e)cyclopropa(c)indol-4-ones with antitumoral activity.

Abstract: This invention relates to perhydroisoindole derivatives of 08/448,402 formula (I), wherein radicals R are phenyl radicals optionally 2-or 3-substituted by a halogen atom or a methyl radical; R.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxy, alkylthio, acyloxy, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; and R.sub.3 is optionally 2-substituted phenyl; optionally salts thereof where applicable; and preparation thereof. Said derivatives are particularly useful as neurokinin A antagonists.

Abstract: Novel cyclohexanes of formulas (I) and (II) are described herein. They inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production: these compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV.

Abstract: There are disclosed novel tannins, lipase inhibitors containing the same as active constituent and a method for producing the same, wherein said tannins have the formula: ##STR1## wherein n is 2 or an integer more than 2.

Abstract: Trifluoromethylpyrroloindolecarboxylic acid ester derivatives, and optical isomers and pharmaceutically acceptable salts thereof are provided which are represented by the general formula (1): ##STR1## or the general formula (2): ##STR2## The compounds are antineoplastic agents which are selective to cancer cells, effective also to solid cancer, and less toxic.

Abstract: The present invention relates to compounds of formula (I): ##STR1## wherein A, x, y, R.sub.1, R.sub.2 and R.sub.3 are as defined in the description. The compounds are useful for treating diseases requiring a selective serotonin reuptake site and 5-HT.sub.2c or 5-HT.sub.3 ligand.

Abstract: A phthalide compound of general formula (I) and a near infrared absorber and a recording material each utilizing the phthalide compound are disclosed. ##STR1## wherein ring A represents a substituent group of the following formula ##STR2## where the other substituents are as defined in the disclosure. The near infrared absorber and the recorded image on the recording material absorb strongly the near infrared region with no appreciable absorption in the visible region of the spectrum. The near infrared absorber is colorless or pale in color and yet highly capable of absorbing near infrared radiation. The recorded image on the recording material can hardly be read with the eye but can be read with the OCR. Moreover, the effect on the developed shade of any concomitant color former in a recording material is minimal.

Abstract: Compounds of formula I ##STR1## wherein the substituents are as defined herein, are disclosed as treatments for disorders linked to CCK and gastrin. Processes for preparing the compounds are also taught.

Abstract: Perhydroisoindole derivatives of formula I, wherein the substituents are as defined in the specification, are particularly suitable as substance P antagonists. Several processes for preparing the compounds are also taught.

Abstract: A process for the preparation of side chain-fluorinated alkyloxazoles, wherein hydroxyalkyloxazoles are reacted with an .alpha.,.alpha.-difluoroalkylamine at pressures of under 2 bar, in the presence of an inert solvent boiling at above 100.degree. C. (at normal pressure), and new fluorinated alkyloxazoles.

Abstract: Nitric esters with pharmacological activity having general formula (I), their pharmaceutical utilisation and process for their preparation.

Abstract: An object of the present invention is to provide a safe method of commercially producing optically active aminoalcohol derivatives, which serve as intermediates for the synthesis of medicinal chemicals such as the immunopotentiating anticancer agent bestatin, in a simple and easy manner in high yields and with high levels of selectivity.The present invention consists in a method of producing 3-amino-1-nitro-4-phenyl-2-butanol derivatives of the general formula (1) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents a hydrogen atom or an amino group protecting group, and a method of producing 3-amino-2-hydroxy-4-phenylbutyric acid derivatives derivable therefrom.

Abstract: 3-Amino-5-methylpyrazole is prepared by reaction of cyanoacetone or an alkali metal salt thereof with hydrazine, a hydrazinium salt, or hydrazine hydrate.

Abstract: The invention is directed to a process for preparing a 1,3-dialkyl-5-hydroxyoxindole of formula 1: ##STR1## comprising heating an N-alkyl-p-alkoxy-(.alpha.-haloacyl)anilide of formula 2: ##STR2## wherein the substituents are as defined herein, in the presence of an anhydrous zinc halide to a temperature in the range from about 120.degree. C. to about 160.degree. C., and isolating the 1,3-dialkyl-5-hydroxyoxindole prepared.

Abstract: Novel compounds of Formula (I) ##STR1## where X.sub.4 is a substituted cyclohexane or cyclohexane group and the other radicals are defined herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production. The compounds of the present invention are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.

Abstract: Diaziridinylpolyamines useful as anti-cancer agents; compositions containing the same, and methods of using the same for the treatment of cancer are described.

Abstract: Angiotensin II receptor antagonists for the treatment and prophylaxis of coronary heart disease.Antagonists for angiotensin II receptors of the AT.sub.1 subtype can be employed for the prophylaxis and combating of coronary heart disease.Furthermore these compounds, such as, for example, azoles of the formula (I) ##STR1## can also be used for the therapy of cognitive and erectile dysfunction.

Abstract: The invention provides a pharmaceutical composition comprising a particular physical form of N-[4-[5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-yl-methyl]-3-methoxy benzoyl]-2-methylbenzenesulphonamide and polyvinylpyrrolidone. It also provides methods for preparing this physical form, and another physical form of N-[4-[5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-yl-methyl]-3-methoxy benzoyl]-2-methylbenzenesulphonamide useful in the preparation of the first mentioned physical form. The compositions are useful in the treatment of diseases in which leukotrienes are implicated, for example asthma.

Abstract: A process for the preparation of (-)-eserethole, of formula (I) starting from (+)-eserethole, or from mixtures of (.+-.)-and (-)-eserethole in which the latter enantiomer prevails, by treating (.+-.)-eserethole or mixtures of (+)-and (-)-eserethole enriched in the latter enantiomer, with 0.5-0.7 mole (per mole of the enantiomeric mixture) of a resolution agent, to yield a (-)-eserethole salt less soluble than the corresponding (+)-eserethole salt.