Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: A process is provided for the preparation of cyclohexene derivatives of general formula I or II: 1

Abstract: 7-substituted fused ring tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted fused ring tetracycline compounds are described.

Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.

Abstract: The claimed invention relates to cyclic dienol ethers of formula (III). wherein R3 is hydrogen and R4 is C1-4 alkoxy or R3 and R4 together form an optionally substituted methylenedioxy group —O—C(R5)(R6)—O—, wherein R5 and R6 are each independently hydrogen, C1-4 alkyl or phenyl.

Abstract: The present invention regards a three-step process for the synthesis of 5-(&agr;-hydroxyalkyl) benzo[1,3]dioxols. The process comprises: (i) the reaction of pyrocatechin (1,2-dihydroxybenzene) with a dihalo or di-alkoxyalkane, with the formation of a benzo[1,3]dioxol derivative; (ii) 5-selective catalytic acylation of the benzo[1,3]dioxol, with formation of a 5-alkanoylbenzo[1,3]dioxol and its subsequent (iii) reduction to 5-(&agr;-hydroxyalkyl) benzo[1,3]dioxol. Also described are new benzodioxols obtainable using the above-mentioned process. The process of the invention is industrially simple and has low environmental impact; it allows to obtain in high yields derivatives of considerable interest, in particular for the perfumery industry, and in the sector of insecticides.

Abstract: Retinoid antagonist compounds have been found to be useful in the prevention and/or minimization of surgical adhesion formation. Also provided by the invention are certain novel substituted (5,6)-dihydronaphthalenyl compounds which are retinoid antagonists and possess the above-mentioned property in addition to their use as antiinflammatory agents for chronic skin inflammatory diseases, as agents for the treatment of rheumatic diseases and as agents for the treatment of various tumors as well as non-malignant proliferative skin conditions.

Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: Intermediate compounds, including 2-(t-butyldimethylsilyloxymethyl)-3,4-[(dimethylmethylene)dioxy]-5-hydroxy-tricyclo[5.2.1.02,6]dec-8-ene, which are useful for the synthesis of neplanocin A having strong antitumor activity. Improved processes for the preparation of neplanocin A, starting from optically active 2-hydroxymethyl-5-hydroxy-tricyclo[5.2.1.02,6]deca-3,8-diene and via a key step comprising a retro-Diels-Alder reaction of the above intermediate.

Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: The present invention provides compounds represented by the general formula (I): and a salt thereof, and anti-inflammatory agents and antitumor agents containing the compounds as the active ingredients.

Abstract: The fungicidal compound 4,5-dimethyl-N-2-propenyl-2-(trimethylsilyl)-3-thiophenecarboxamide (Formula (I)) has shown superior and unexpected control of the growth of the soil-borne fungus Gaeumannomyces graminis (Gg). The present invention provides a novel compound for synthesizing the compound of Formula (I) which uses the compound 4-hydroxy-4,5-dimethyl-2-trimethylsilanyl-dihydrothiophene-3-carboxylic acid allylamide (Formula (II)) as well as novel compounds of synthesizing the allylamide. In addition, Formula (II) itself has unexpectedly been found to provide control of Gg.

Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.

Abstract: The novel two-stage process described here makes it possible to obtain substituted benzyl compounds and toluene derivatives in a simple manner and in high yields by means of Suzuki-type coupling reactions of an aromatic with an organoboron compound, followed by a reduction. The process is particularly useful for preparing ortho-substituted benzyl compounds and toluene derivatives. The process can be applied to both intermolecular and intramolecular coupling reactions. Catalysts used for the coupling reaction are palladium compounds and/or nickel compounds. An advantageous aspect is that only very small amounts of catalyst are required.

Abstract: The invention relates to novel cyclic imines of the formula (I) in which Ar1 and Ar2 each represent substituted phenyl and n represents 1, to a process for their preparation and to their use as pesticides.

Abstract: The following description refers to a new process for the synthesis of 5-alkylated benzo[1,3]dioxole, comprising the following steps in sequence: catalytic hydrogenation of 4-acylphenol; acylation; displacement catalysed by Lewis acids; treatment with an inorganic basic compound and hydrogen peroxide; reaction with alkyl dihalides or dialkoxyalkanes. The process described herein, which yields 5-alkylbenzo[1,3]dioxoles, is economic and can be easily scaled up to industrial size.

Abstract: Retinoid antagonist compounds have been found to be useful in the prevention and/or minimization of surgical adhesion formation.

Abstract: Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.

Abstract: A process for the preparation of 3-substituted 4-cyano-pyrrole compounds of the formula (I) in which Ar has the meaning given in the description, by reaction in a 1st stage of bromides (II) Ar—Br  (II) with acrylonitrile in the presence of a solvent and a suitable reaction auxiliary to give acrylonitrile derivatives (III) Ar—CH═CH—CN  (III) and in a 2nd stage with a phenylsulphonylmethyl isocyanide (IV) Ph—SO2—CH2—CN  (IV) in the presence of a solvent and optionally in the presence of a suitable reaction auxiliary, characterised in that the the 1st stage is carried out in the presence of a palladium catalyst and the 2nd stage in the presence of a 1.2- to 1.8-fold molar excess of alkali metal alcoholate or alkali metal hydroxide.

Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: The present invention is directed to chiral intermediates in a synthetic route for preparing endothelium receptor antagonists of formulae (7B) and (7A).

Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganism, eukaryoic cells, whole animals and human being. R' and R" are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R'" is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.

Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: The present invention provides a method for the preparation of triarylmethyl protecting group reagents. The reagents are prepared from reaction effluent from the cleavage step of oligonucleotide synthetic regimes.

Abstract: The present invention is directed to a synthetic route for preparing endothelium receptor antagonists of formulae (7B) and (7A) and to the chiral intermediates ##STR1##

Abstract: Disclosed are novel .alpha.-aryl-N-alkylnitrone compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for preventing and/or treating neurodegenerative, autoimmune and inflammatory conditions in mammals and as analytical reagents for detecting free radicals.

Abstract: This invention relates to derivatives of furan and thiophene, their composition, process of making and method of use as endothelin receptor antagonists.

Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: Process for isolation of 1-(3,4-methylenedioxy-phenyl)-1E-tetradecene from Piper longum. Processes for synthesis of 1-(3,4-methylenedioxy-phenyl)-1E-tetradecene; its stereoisomers and analogues are disclosed. The compounds isolated and synthesized according to this invention have immunomodulatory properties and can be used to treat tumors and infections.

Abstract: The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula II ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock, reperfusion injury, Alzheimer's disease, shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.

Abstract: Disclosed herein are substituted vinylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.3 are independently a phenyl group which may be substituted, R.sup.2 is a phenyl group which may be substituted, or a cycloalkyl group, and wave lines mean that the bonding state may be either E or Z, with the proviso that the cases where R.sup.1, R.sup.2 and R.sup.3 are unsubstituted phenyl groups, and where R.sup.1 and R.sup.2 are unsubstituted phenyl groups and R.sup.3 is a 4-ethoxyphenyl group are excluded, or salt thereof, and medicines comprising such a derivative as an active ingredient as well as a method of preventing and treating arteriosclerosis with such a medicine. The derivatives or salts thereof selectively and strongly inhibit ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

Abstract: The present invention relates to the derivatives of formula: ##STR1## and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.

Abstract: Compounds of the formula ##STR1## wherein the variables are defined as in the specification, are capable of lowering introaocular pressure in the eye of a mammal.

Abstract: Disclosed are novel pancratistatins and methods for their total asymmetric synthesis. In particular embodiments, processes for the total asymmetric synthesis of (+)-pancratistatin, (-)-pancratistatin, (+)-7-deoxypancratistatin, (-)-7-deoxypancratistatin, truncated pancratistatins, and related derivatives are provided.

Abstract: Novel carbocyclic compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.

Abstract: An economical process for producing .alpha.-L-aspartyldipeptide amide derivatives useful as sweeteners, by using amino protecting groups which can be removed by hydrolysis under acidic conditions, resulting in conversion of a .beta.-carboxyl acid ester to a carboxylic acid.

Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.

Abstract: The invention concerns tachykinin antagonists. The compounds are nonpeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included.The compounds are expected to be especially useful in asthma and rheumatoid arthritis.

Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.

Abstract: The present invention relates to the carbocyclic diarylmethylene derivatives of formula (I): ##STR1## and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.

Abstract: According to the invention, a new process for the preparation of fluorine-substituted aminobenzodioxoles and -benzodioxanes of the formula (I) ##STR1## in which n represents an integer 1 or 2, has been found, in which fluorine-substituted nitro-halogeno-benzodioxoles and -benzodioxanes, which are likewise new, are hydrogenated. The novel intermediates are obtained from fluorine-substituted benzodioxoles and benzodioxanes by halogenation and subsequent nitration. The amino compounds are important starting materials for highly active biocides.

Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.

Abstract: 2,2-Difluorobenzo[1.3]dioxole-carbaldehydes are prepared in a particularly advantageous manner if methylbenzo[1.3]dioxoles are chlorinated, the resulting dichloromethyl-2,2-dichlorobenzo[1.3]dioxole is fluorinated with hydrogen fluoride and the dichloromethyl-2,2-difluorobenzo[1.3]dioxole obtained by this procedure is reacted with a carboxylic acid.

Abstract: Methods of producing carboxylic acid ester derivatives of formulae (I) and (II), which are useful, for instance, as intermediates for producing an anti-hypercholesterolemic agent having an inhibitory effect on HMG-CoA Reductase: ##STR1## wherein R.sup.1 and R.sup.2 are independently a protective group for hydroxyl group, or R.sup.1 and R.sup.2 integrally constitute a protective group for hydroxyl groups; R.sup.3 is an alkyl group, or an aryl group; and R.sup.4 is a substituted aryl group, a substituted heterocyclic group, a substituted vinyl group, or a substituted cycloalkenyl group; and ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are respectively the same as defined in the above formula (I), are disclosed. In addition, intermediates for use in these methods of producing the carboxylic acid ester derivatives are disclosed.

Abstract: This invention provides certain sulfonamide derivatives, their pharmaceutical formulations, and their use in the treatment of susceptible neoplasms in mammals.

Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.

Abstract: A compound of formula: ##STR1##

Abstract: According to the invention, a new process for the preparation of fluorine-substituted aminobenzodioxoles and -benzodioxanes of the formula (I) ##STR1## in which n represents an integer 1 or 2, has been found, in which fluorine-substituted nitro-halogeno-benzodioxoles and -benzodioxanes, which are likewise new, are hydrogenated. The novel intermediates are obtained from fluorine-substituted benzodioxoles and benzodioxanes by halogenation and subsequent nitration. The amino compounds are important starting materials for highly active biocides.