Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: The invention relates to Siglec inhibitors that have an increased affinity for the receptor molecule. The Siglec inhibitors provided by the invention are preferably selective of a given Siglec molecule. The invention further relates to a method for producing Siglec inhibitors and to a method for increasing the binding selectivity for a given Siglec molecule. The invention also relates to pharmaceutical compositions that contain the Siglec inhibitors and to medical indications for the Siglec inhibitors.

Abstract: The present invention is directed to a continuous process for the preparation of fructopyranose sulfamate derivatives of the general formula (I) 1

Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.

Abstract: The present invention relates to a process to prepare semi synthetic statins, to intermediates formed during said process and to highly purified simvastatin produced by the process.

Abstract: The present invention relates to 2-(4-sulphonylphenyl)pyran-4-one derivatives of general formula 1

Abstract: The present invention relates to a process for the preparation of compounds of formula I 1

Abstract: Novel, enantiopure, substituted 4-deoxypentenosides (4-DPs) and related dihydropyrans (DHPS) are prepared from common carbohydrates via a novel process. The 4-DPs and related DHPs are amenable to a broad range of stereoselective transformations and are used as synthetic intermediates to prepare a variety of enantiopure tetrahydropyrans (THPs), including rare or exotic sugars and other complex THPs of commercial or medicinal value. In one embodiment of the instant invention, 4-DPs are converted to L-sugars in a novel process that offers distinct advantages over known synthetic methods.

Abstract: A compound of the formula wherein R1-R13, X, Z and Q are as defined above, useful in the treatment of arthritis, cancer, and other diseases involving the dysregulated production/release of reprolysins such as Aggrecanase and other diseases characterized by matrix metalloproteinase activity. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID's), COX-2 inhibitors and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.

Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.

Abstract: The present invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having anti-proliferative activities, as well as methods for treating various diseases associated with abnormal cell proliferation, including cancer, by administering said compounds. It further deals with pharmaceutical compositions comprising said compounds, more particularly useful to treat cancers.

Abstract: This invention relates to compositions, compounds, and methods for lightening skin, using active compounds having the general structure: wherein each X is halo; m is 1 to 4; each R′ and R″ is independently selected from hydrogen, halo, C1-C10 alkyl, substituted C1-C10 alkyl, substituted or unsubstituted phenyl, substituted or unsubstituted naphthyl, OR, OCOR, OCRROR, COR, CR(OR)OR, CONRR, COOR, CRROR, CN, SR, and NRR; each R is selected from hydrogen, C1-C10 alkyl, substituted C1-C10 alkyl, substituted or unsubstituted phenyl, and substituted or unsubstituted naphthyl; n is 1 to 5; Z is O; in an amount effective to lighten skin; and a pharmaceutically-acceptable carrier therefor.

Abstract: The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.

Abstract: The invention relates to a new process for preparing optically active dihydropyrones, new intermediate products which may be obtained by this synthesis, and their use as starting compounds in the preparation of pharmaceutically active compounds.

Abstract: The present invention relates to compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.

Abstract: An E-isomeric fulleropyrrolidine compound of formula (I): is disclosed. Also disclosed is a method for preparing and polymers prepared from such a compound.

Abstract: Compounds of formula (I) or their salts or esters: [wherein R1 is alkyl or haloalkyl; R2 and R3 each represents hydrogen or aliphatic acyl; X is hydroxy, halogen, alkoxy, or a group of formula RaO—, where Ra is aliphatic acyl; Y is a group of formula RbRcN— or RbRcN—O—, where Rb and Rc each is hydrogen or alkyl; and Z is oxygen or sulfur] have excellent sialidase inhibitory activity and are therefore useful for the treatment and prevention of influenza and other viral diseases where the replication of the virus is susceptible to sialidase inhibitors.

Abstract: One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.

Abstract: The invention is related to a preparation method of arbutin intermediate (chemical formula I). It is characterized by the glycosylation of hydroquinone or mono-protectected hydroquinone (chemical formula II) with pentaacetyl-&bgr;-D-glucose (chemical formula III) in the presence of Lewis acid and base as catalysts. where Ac is acetyl group, R is hydrogen, alkyl or cycloalkyl group with 1 to 10 carbon, or aliphatic or aromatic acyl group with 1 to 10 carbon.

Abstract: A process is provided for the preparation of anhydrosugar alcohols. The process involves heating a sugar alcohol or a monoanhydrosugar alcohol starting material in the presence of an acid catalyst, and subsequent purification of the anhydrosugar alcohol. Very high purities are achieved, without the use of organic solvents in the process.

Abstract: The method of this invention prepares acylated cyclic compounds by contacting phenyl esters as acylating agents with cyclic compounds in the presence of a cyanide or fluoride catalyst.

Abstract: 2-Phenylpyran-4-one derivatives of formula (I): 1

Abstract: Compounds of formula (I) or their salts or esters: have excellent sialidase inhibitory activity and are therefore useful for the treatment and prevention of influenza and other viral diseases where the replication of the virus is susceptible to sialidase inhibitors.

Abstract: The present invention has its object to provide a noble antifungal substance which is use of as clinical medicine in the therapy of fungal infectious diseases. The present invention is related to an antibiotic TKR459 having the following chemical formula (1) or its pharmacologically acceptable salt.

Abstract: Compounds of the formula I in which R1, R2, R3, R4, R5, m and n have the meanings cited in the description, are novel effective PDE-inhibitors.

Abstract: The present invention has its object to provide a noble antifungal substance which is use of as clinical medicine in the therapy of fungal infectious diseases.

Abstract: The present invention relates to novel compounds of the formula (I) in which Het represents one of the groups in which A, B, D, G, V, W, X, Y and Z are as defined in the description, processes and intermediates for their preparation, and to their use as pesticides and herbicides.

Abstract: The present invention relates to new compounds of the formula (I) in which X represents alkyl, Y represents halogen or alkyl and Z represents halogen or alkyl, with the proviso that one of the radicals Y and Z always represents halogen and the other alkyl, Het represents one of the groups in which A, B, D and G have the meanings given in the description, a plurality of processes for their preparation and their use as pesticides and herbicides.

Abstract: A process for the isolation of the pseudomonic acid A antibiotic of pharmaceutical quality from the culture broth of one of the pseudomonic acid A-producing species of the Pseudomonas bacterium genus comprising the extraction of the biosynthesized pseudomonic acid A from the culture broth at acidic pH with a chlorinated aliphatic hydrocarbon or isobutyl acetate, followed by purification, is disclosed.

Abstract: 11-hydroxysordarin, biotransformation product of a fermentation with sordarin and Actinomyces spp., (Merck Culture Collection MA7235) ATCC No. 202103 is an antifungal agent. This compound may be useful in the treatment of diseases caused by fungal pathogens such as Candida albicans.

Abstract: Novel polyketides and novel methods of efficiently producing both new and known polyketides, using recombinant technology, are disclosed. In particular, a novel host-vector system is described which is used to produce polyketide synthases which in turn catalyze the production of a variety of polyketides.

Abstract: Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: wherein at least one of R1, R2, R3, R4, or R5 comprises a functional group which is chemically similar to that found in the peptide of interest.

Abstract: It is shown that the potency of anti-cancer drugs, here exemplified by doxorubicin, can be increased by the use of polyunsaturated fatty acid amides and in particular specific combinations of such compounds, forming complexes with doxorubicin. Further, a modified form of doxorubicin is presented.

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

Abstract: The present invention relates to a process for stereoselective cycloaddition reactions which generally comprises a cycloaddition reaction between a pair of chiral or prochiral substrates that contain reactive .pi.-systems, in the present of a non-racemic chiral catalyst, to produce a stereoisomerically enriched product.

Abstract: Novel cyclic ether vitamin D3 compounds having a cyclic ether side chain are disclosed. These compounds were first identified as metabolites of 3-epi vitamin D3 produced via a tissue-specific metabolic pathway which catalyzes the formation of a cyclic ether structure. Also disclosed are 1.alpha.(OH) 3-epi vitamin D3 compounds, which are produced via the epimerization of a 3-.beta.-hydroxyl group of 1.alpha.(OH) vitamin D3 precursor in vivo. The vitamin D3 compounds of the present invention can be used as substitutes for natural and synthetic vitamin D3 compounds.

Abstract: There is disclosed a novel compound having a fluoromethyl group which itself has a large electron attractive property at an asymmetric carbon atom on a tetrahydropyran ring, which is expected to be a novel type of a liquid crystal.

Abstract: There is disclosed a novel compound having a fluoromethyl group which itself has a large electron attractive property at an asymmetric carbon atom on a tetrahydropyran ring, which is expected to be a novel type of a liquid crystal.

Abstract: Compounds of the formula (I) ##STR1## and pharmaceutically acceptable salts or metabolically labile derivatives thereof, processes for their preparation, their use as antifungal agents and intermediates for use in their preparation.

Abstract: This invention provides sweetener blends comprising N-[N-(3,3-dimethylbutyl)-L-.alpha.-aspartyl]-L-phenylalanine 1-methyl ester and another sweetener. The sweetener blends of this invention exhibit isobole synergy.

Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and a blocking group, characterized by the presence of a covalent bond which is cleaved at pH values below 7.0. The prodrug may be used in a technique for treating a condition or disease in a mammal related to elevated hydrogen ion concentrations, whereby on administering it to a mammal having such a condition or disease, the pharmacologically active compound is activated selectively within tissues having such elevated hydrogen ion concentrations.

Abstract: The present invention addresses compounds which inhibit Mur D. The compounds are represented by structural formula 1: ##STR1## wherein: X represents OH, OC.sub.1-6 alkyl, O-aryl, O-Har, uridinyl, 5-iodouridinyl or O--Y.sup.+, wherein Y.sup.+ represents a charge balancing group; R.sup.1 and R.sup.2 independently represent H or C.sub.1-6 alkyl, or R.sup.1 and R.sup.2 taken together represent C.sub.1-6 alkylene unsubstituted or substituted with from 1-2 aryl or Har groups; W represents H, aryl, C.sub.1-6 alkyl or a charge balancing group; each M independently represents a member selected from the group consisting of: H, a charge balancing group and a protecting group.Salts and hydrates thereof are included.Also included are pharmaceutical compositions and methods of treatment.

Abstract: Novel methods for the treatment and/or prophylaxis of diseases caused by tissue-adhering bacteria are disclosed. By interacting with periplasmic molecular chaperones it is achieved that the assembly of pili is prevented or inhibited and thereby the infectivity of the bacteria is diminished. Also disclosed are methods for screening for drugs as well as methods for the de novo design of such drugs, methods which rely on novel computer drug modelling methods involving an approximative calculation of binding free energy between macromolecules. Finally, novel pyranosides which are believed to be capable of interacting with periplasmic molecular chaperones are also disclosed.

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: Triene-containing compounds which mimic the chemical and/or biological activity of the spongistatins are provided, as are methods and intermediates useful in their preparation.

Abstract: Compounds of the formula Iglycosyl-Y?--C(.dbd.Y)--X--!.sub.p --W(R).sub.n --Z--C(.dbd.Y)-active compound (I)are described which are suitable for the treatment of carcinomatous diseases, autoimmune diseases and chronic inflammatory diseases such as rheumatoid arthritis.

Abstract: Maltol and ethyl maltol can be produced from a haloenone intermediate by reacting the intermediate with acid in a reaction medium comprising an aprotic solvent.

Abstract: Process for the preparation of 6-(substitutedaminopropionyl)-derivatives of forskolinProcess for the manufacture of 6.beta.

Abstract: Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.

Abstract: A process for producing a compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen or alkyl, and R is hydrogen or alkyl, which comprises removing the protective group (P) of hydroxyl of a compound of the formula (II): ##STR2## wherein P is a protective group of hydroxyl, .about. indicates an E-isomer, Z-isomer or a mixture thereof, and the other symbols are as defined above; and an intermediate for the production of the compound of the formula (I).