Abstract: This invention relates to 1-substituted-phenyl-3-substituted-2-thioxo-4,5-imidazolidinediones and 2,4,5-imidazolidinetriones which have activity as herbicides, to compositions which contain these compounds and to methods of use of these compounds. In particular, the present invention pertains to 2-thioxo-4,5-imidazolidinediones or 2,4,5-imidazolidinetriones wherein a 2,4,5,6-tetrasubstituted phenyl ring is linked to the heterocyclic ring.

Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.

Abstract: Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.

Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.

Abstract: The present invention relates to oxygen-containing heterocyclic compounds represented by the following formula (I): wherein m represents an integer of 0 to 4; R1, R2, R3 and R4 independently represent a hydrogen atom, substituted or unsubstituted lower alkyl, etc.; R5 represents substituted or unsubstituted lower alkoxy etc.; R6 represents a hydrogen atom etc.; and Y represents the following formula (II): wherein R9 represents cyano etc., R10 represents a hydrogen atom etc., R11 represents carboxy etc., and R12 represents a hydrogen atom etc.; and the like; or pharmaceutically acceptable salts thereof.

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 invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.

Abstract: Optically active alcohols of formulae (1) and (2) which are useful as intermediates for the synthesis of (RRR)-optical isomers of 1,4-benzodioxin-2-carboxylic acid derivatives which are useful as a prophylactic and therapeutic agent for diabetes, hyperglycemia and the like.

Abstract: The subject invention provides novel biologically active compounds which are useful for inhibiting cellular proliferation. Because of the biological activity of these compounds, they can be used for immunomodulation and/or treating cancer. In a preferred embodiment, the novel compounds, compositions and methods of use of the subject invention can advantageously be used to inhibit the growth of tumor cells in a mammalian host. More particularly, the subject compounds can be used for inhibiting in a human the growth of tumor cells, including cells of breast, colon, CNS, ovarian, renal, prostate, bone, gastrointestinal, stomach, testicular, or lung tumors, as well as human leukemia or melanoma cells. Specifically exemplified are discalamides A and B.

Abstract: The present invention features compounds able to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders using such compounds. Preferred compounds can mimic or block the effect of extracellular calcium on a cell surface calcium receptor.

Abstract: The present invention relates to oxygen-containing heterocyclic compounds represented by the following formula (I): 1

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

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: Optically active alcohols of formulae (1) and (2) which are useful as intermediates for the synthesis of (RRR)-optical isomers of 1,4-benzodioxin-2-carboxylic acid derivatives which are useful as a prophylactic and therapeutic agent for diabetes, hyperglycemia and the like.

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: Indane and indene compounds are described which are endothelin receptor antagonists.

Abstract: 1-phenyl-3 -dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.

Abstract: The present invention relates to a process for preparing fluorine-containing phenethylamines which is characterized in that, in a first step, a substituted bromobenzene is reacted with an N-vinylimide in the presence of a palladium catalyst, in a second step, the resulting substituted &bgr;-iminovinylbenzene is hydrogenated catalytically and in a third step, the substituted &bgr;-iminovinylbenzene obtained in the second step is cleaved. This process also provides access to novel &bgr;-iminovinyl- and &bgr;-iminoethylbenzenes.

Abstract: The enzyme substrate according to this invention has within its molecule both a group to be cleaved by an enzyme reaction and a group that forms a strongly fluorescent coumarin derivative through intramolecular lactonization when cleaved by the enzyme reaction. Furthermore, the method for determining an enzyme activity according to this invention comprises conducting the enzyme reaction by the use of the enzyme substrate of the invention and determining the enzyme activity by means of the measurement of fluorescence of the coumarin derivative formed.

Abstract: A process for preparing compounds of the formula: and intermediates for use in the process.

Abstract: Described are novel photochromic benzopyrano-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted benzopyran group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds.

Abstract: What is described here are photochromic naphthopyrane dyes with different substituents whose properties can be set by controlled selection of the substituents. In this manner it is possible to take an influence on the migration characteristics, the absorption characteristics and the brightening rate and kinetics. The inventive compounds display good darkening and brightening properties at a very good service life.The invention excels itself by the fact that a method is made available which is substantially improved over prior art, in addition to the surprising influence on specific properties of the inventive compounds. The described compounds are suitable for application in synthetic materials of any kind.A photochromic object is also the subject matter of the invention, which comprises one or several photochromic naphthopyrane dyes as well as at least one polymer material, with the photochromic object being producible by mass-dyeing or superficial dyeing.

Abstract: A process for preparing a benzo fused heterocyclic sulfonyl halide comprising reacting a benzo fused heterocyclic compound with an SO.sub.3 complex in the presence of a water immiscible, non-reactive solvent, at a temperature of from about 0.degree. C. to about 75.degree. C., cooling, if necessary, to a temperature of from about -25.degree. C. to about 65.degree. C. and then adding oxalyl halide.

Abstract: A 1,4-benzodioxin derivative represented by formula (I) ##STR1## wherein A is an aryl group or a (C.sub.3 -C.sub.8)cycloalkyl group, R.sub.1 and R.sub.2 individually are a hydrogen atom, a halogen atom, an alkyl group, a trifluoromethyl group, an alkoxy group, an aryl group, an aryloxy group, or R.sub.1 and R.sub.2 together form a methylenedioxy group, R.sub.3 is a hydrogen atom or an alkyl group, R.sub.4 is a hydrogen atom or CO.sub.2 R.sub.5, R.sub.5 is a hydrogen atom or an alkyl group, X is a radical of formula (II) or (III) ##STR2## wherein n is 1 or 2. The compounds are useful for a prophylactic or therapeutic agent for diabetes, hyperglycemia and obesity.

Abstract: Described are novel photochromic polymerizable polyalkoxylated naphthopyran compounds, examples of which are certain 2H-naphtho[1,2-b]pyrans, 3H-naphtho[2,1-b]pyrans and indeno[2,1-f]naphtho[1,2-b]pyrans each having at least one polyalkoxylated substituent of from 1 to 50 alkoxy units per substituent which is end-capped with a polymerizable group. Specific substituents are also present on the naphtho, indeno and pyrano portions of the compounds. These compounds may be represented by the following graphic formulae: ##STR1## Also described are various substrates, e.g., paper, glass, polymeric organic materials, etc., that contain or that are coated with such compounds. Optically clear articles such as contact lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, indenonaphthopyrans, benzopyrans, oxazine-type compounds, etc., are also described.

Abstract: The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.

Abstract: New benzimidazole derivatives of the formula in whichR represents cyano or the group ##STR1## X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are identical or different and represent halogen;Y represents alkyl, alkenyl or alkinyl, each of which is optionally substituted by halogen; or represents optionally substituted phenylalkyl or in each case optionally substituted cycloalkyl and cycloalkenyl; andZ represents hydrogen or halogen,a process for the preparation of these substances, and their use for controlling pests.New intermediates and processes for their preparation.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: A 1-bromoalkylbenzene derivative is prepared by reacting a phenylalkene derivative with hydrogen bromide in the presence of a non-polar solvent. The phenylalkene derivative is prepared by reacting an alkenyl halide with metal magnesium to form a Grignard reagent, and then reacting the Grignard reagent with a benzyl halide derivative. An allyl Grignard reagent is prepared by reacting continuously an allyl halide derivative with metal magnesium in an organic solvent, in which the allyl halide derivative and metal magnesium are continuously added to the reaction system and the allyl Grignard reagent formed is continuously removed from the reaction system. The processes provide the intended compounds in high yields, high selectivities and high purities.

Abstract: A process for preparing compounds of formula (B) wherein:one of A.sub.1 ' or A.sub.2 ' represents hydrogen and the other represents a group CF.sub.3 --Y-- wherein Y represents --CF.sub.2 --, >C.dbd.O, or --CH(OH)--, or A.sub.1 ' and A.sub.2 ' are groups convertible to A.sub.1 and A.sub.2 respectively.Y.sub.1 represents --O--, --CH.sub.2 -- or NR.sup.O wherein R.sup.O is hydrogen, alkyl or alkylcarbonyl; R.sub.1 and R.sub.2 independently represent hydrogen or alkyl; orR.sub.1 and R.sub.2 together represent a C.sub.2-7 polymethylene moiety;R.sub.3 represents hydrogen, hydroxy, alkoxy or acyloxy and R.sub.4 is hydrogen or R.sub.3 and R.sub.4 together represent a bond;which process comprises reacting a compound of formula (C): ##STR1## wherein the variable A.sub.1 ', A.sub.2 ', Y.sub.1, R.sub.1 and R.sub.2 are as defined above, in the presence of an oxygen source and a chiral catalyst as defined in WO/91/14694.

Abstract: Described are novel photochromic benzopyrano-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted benzopyran group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, nenzopyrans, and spiro(indoline)type compounds.

Abstract: Dienoic retinoids having activity for retinoid X receptors or are panagonists on retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their therapeutic use.

Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.

Abstract: The invention relates to new substituted biphenyloxazolines of the formula (I) ##STR1## in which R.sup.1 represents C.sub.1 -C.sub.6 -halogenoalkylthio andR.sup.2 represents hydrogen, orR.sup.1 and R.sup.2 together with the carbon atoms to which they are bonded form a halogen-substituted 5- or 6-membered heterocyclic ring,X represents hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.

Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.

Abstract: Novel derivatives of benzodioxa alkylene ethers are provided which are useful as melatonergic agents.

Abstract: 4-Cyano-4-deformylsordarin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.

Abstract: Described are novel photochromic polyalkoxylated naphthopyran compounds, examples of which are certain 2H-naphtho?1,2-b!pyrans, 3H-naphtho?2,1-b!pyrans and indeno?2,1-f!naphtho?1,2-b!pyrans, each having at least one polyalkoxylated substituent of from 2 to 50 alkoxy units per substituent. Specific substituents may also be present on the naphtho, indeno and pyrano portions of the compounds.

Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.

Abstract: Described are novel photochromic indeno-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted indeno group, the 2,1 positions of which are fused to the f side of the naphtho portion of the naphthopyran, and having certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 6, 7, 8, 9, 10, 11, 12 or 13 carbon atoms of the compounds. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans and spiro(indoline)type compounds, are also described.

Abstract: The present invention is drawn to a process for preparing a 2,2,3,3-tetrafluoro-1,4-benzodioxane, by cyclocondensing a o-(2-bromo-tetrafluoroethoxy)-phenol in the presence of an acid binder.

Abstract: A compound of formula ##STR1## wherein Z is a tetrahydro-pyrano group selected from ##STR2## having antifungal activity processes for their preparation and their use in medicines.

Abstract: Amino acid derivatives of formula (Ia) and (Ib) and pro-drugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as inhibitors of these enzymes.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

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: The present invention is concerned with compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1--6 alkyl; R.sup.2 is hydrogen or C.sub.1- 6 alkyl; R.sup.3 is C.sub.1-6 alkyl, hydroxy, cyano, halo, C.sub.1-6 alkyloxy, aryloxy, arylmethoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkyl--S--, C.sub.1-6 alkyl(S.dbd.O)--, C.sub.1-6 alkylcarbonyl; R.sup.4 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl, or C.sub.1-6 alkyloxy; or R.sup.3 and R.sup.4 taken together form a bivalent radical; R.sup.5 and R.sup.6 each independently are hydrogen, halo, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.7 is hydrogen; Alk.sup.1 is C.sub.2-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## Pharmaceutical compositions, preparations and use as a medicine are described.

Abstract: Described are novel pentahydrophenanthro?9,10-b!pyrans and tetrahydrocyclopenta?c!-naphtho?1,2-b!pyrans. Also described are polymeric organic host materials that contain or that are coated with such compounds.

Abstract: A novel process for preparing a 1,4 benzodioxane derivative shown by the formula (1) which is a useful intermediate of circulatory drugs and drugs for psychoneurosis, characterized in sulfonating a phenoxypropanediol with a sulfonyl halide, eliminating the protective group, and then cyclizing the sulfonated compound by treating with a base followed by, if necessary, further sulfonation. ##STR1## In the above formula, R.sup.1 is H, RSO.sub.2, R is alkyl, phenyl which may be substituted with alkyl, R.sup.2, R.sup.3, R.sup.4 are H, halogen, OH, nitro, cyano, formyl, COOH, alkoxycarbonyloxy, alkyl, alkoxy, haloalkyl, N,N-dialkylamino, alkylcarbonyl, alkoxycarbonyl, phenyl which may be substituted by alkyl, etc.

Abstract: Selected sulfonylalkanoylamino 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: A light-stable cosmetic composition for protection from UV rays having a wavelength of between 280 and 400 nm, which contains at least one tetraalkylquercetin in a cosmetically acceptable oil-based medium, and new tetraalkylquercetins.