Abstract: Conjugation of 4,5-Epoxymorphinan-6-ols with Bromoglucuronides in the presence of Zinc containing compounds as activator under conditions capable of forming 4,5-Epoxymorphinan-6-oxyglucuronides is disclosed. This novel approach provides an efficient method for preparation of both anomers of 4,5-Epoxymorphinan-6-oxyglucuronides. The deprotected end products are useful as analgesic agents.

Abstract: Mono-fluorinated and di-fluorinated benzothiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.

Abstract: The present invention provides amphiphilic prodrugs comprising a therapeutic compound conjugated to an PEG-oligomer/polymer and methods for using said prodrugs to enable oral drug delivery and/or delivery of drugs across the blood brain barrier into the central nervous system.

Abstract: The invention provides a novel method for synthesizing Morphine-6-Glucuronide comprising the step of reacting 3-O-pivaloyloxymorphine and methyl 1&agr;,2-ethylorthopivalate-3,4-di-O-pivaloylglucouronate.

Abstract: Compound JK represented by the general formula (1): wherein R is H or —CH3; or a pharmaceutically acceptable salt thereof. Compound JK has an excellent antimicrobial activity even against resistant strains including MRSA and is useful as an anti-microbial agent.

Abstract: The present invention relates to a process for isolating flax lignans. Specifically this invention provides a process for isolating and purifying secoisolariciresinol diglycoside (SDG) from crushed flaxseed by means of supercritical carbon dioxide extraction and chromatographic separation.

Abstract: A novel class of antitumour compounds has been recognised based on the isolation from a new marine microbe, strain PO13-046, belonging to the genus Actinomadura sp.), of a compound designated IB-00208. The class of the formulae (I) or (II) where R1 can be hydrogen, acyl, alkyl, alkenyl, aryl, benzyl, alkali metal, and/or sugar, and R2 and R3 can be hydrogen, alkyl, or together R2 and R3 form an unsaturated bond. Such compounds demonstrate an interesting activity several cancel cell lines and against Gram-positive bacteria.

Abstract: New triterpenoid derivatives with various substituents at the C-17 position of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO) were synthesized. Among them, 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-onitrile (CNDDO), 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl) imidazole, 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl)-2-methylimidazole, 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl)-4-methylimidazole show extremely high inhibitory activity (IC50=0.01-1 pM level) against production of nitric oxide induced by interferon-&ggr; in mouse macrophages. These compounds can be used in the prevention or treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, rheumatoid arthritis, and other inflammatory diseases. All the new triterpenoid derivatives are more potent than previously known CDDO.

Abstract: The present invention provides fluorescent nucleoside analogs which comprise a fluorescent cyclic compound joined to a carbon of a sugar molecule such as pentose, hexose, ribose or deoxyribose or analogs thereof in either an &agr; or &bgr; configuration. The subject compounds are useful as probes in the study of the structure and dynamics of nucleic acids and their complexes with proteins. In addition, the subject compounds are useful in any technique which uses labeled oligonucleotides for detection. Non-fluorescent spacer molecules in which a cyclohexane, cyclohexene, decalin, or benzene is joined to a carbon of a sugar moiety such as pentose, hexose, ribose or deoxyribose are also provided. Also provided are the 5′ dimethoxytrityl-3′-O-phosphoramidite derivatives, suitable for incorporation into oligonucleotides by automated synthesizers.

Abstract: The present invention provides a fluorescent substance which is represented by a formula: A-B-C wherein A is a residue of natural or synthetic nucleotide, oligonucleotide, polynucleotide, or derivative thereof, and binds to B at a base moiety in said residue, or A is a residue of avidin or streptavidin; B is a divalent linking group or a single bond; and C is a monovalent group derived from a general formula (I) and binds to B at a reactive group present in R1 or R2: wherein R1 and R2 each independently represent an alkyl group that may be substituted with a reactive group capable of covalently bonding to A-B-; R3, R4, R5, and R6 each independently represent an alkyl group, and R3 and R4, and/or R5 and R6 may bind to each other to form a saturated carbon-ring together with a carbon atom(s) to which they bind; V1, V2, V3, V4, V5, V6, V7, V8, V9 and V10 each independently represent a hydrogen atom or a monovalent substituent, and two adjacent groups thereof may bind to form a ring; L1, L2,

Abstract: A process for manufacturing morphine-6-glucuronide and related compounds of the general structure of Formula 1: wherein optionally substituted morphine is conjugated with an optionally substituted member of a new class of intermediates, namely, 1-haloglucuronate esters, in the presence of iodine or an iodinium compound. The conjugation may be followed by conversion of R1 of Formula 1 into hydrogen and/or the removal of the ester groups from the glucuronic residue at R2 of Formula 1.

Abstract: The invention provides new isoflavonoid and triterpenoid compounds isolated from a soybean phytochemical concentrate. The new compounds have exhibited cytotoxic activity against selected tumor cell lines. Pharmaceutical compositions comprising the new compounds and methods for use thereof are provided by the invention.

Abstract: Compounds according to formula I: T1—L—T2   (I), wherein T1 is a taxoid group, preferably of Formula II: wherein R1 is C6H5; R2 is O; L is a linking group; and T2 is a substituent selected from the group consisting of epipodophyllotoxin, amsacrine, ellipticine, anthracycline antibiotic, mitoxantrone, and colchicine groups, and pharmaceutically acceptable salts thereof, are provided herein. The compounds are useful in, among other things, treating tumors or cancer in subjects in need thereof, inducing cellular differentiation, and inhibiting cellular mitosis.

Abstract: The invention relates to extracts of the plant Mourera fluviatilis and to cosmetic and/or pharmaceutical preparations that contain an extract of the plant Mourera fluviatilis.

Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.

Abstract: The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X, Y, V, W1, W2, Z1 and Z2 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods of treating bacterial and protozoal infections in mammals by administering the above compounds.

Abstract: The invention concerns a novel chromogenic substrate based on Alizarin. The invention also concerns the uses to which this substrate can be put, and a formulation containing such a substrate.

Abstract: Glycosidation of 4,5-Epoxymorphinan-6-ols with a Thioglycoside as a glycoside donor is disclosed. The process comprises reacting a 4,5-Epoxymorphinan-6-ol and a Thioglycoside in the presence of a thiophilic promoter under conditions capable of forming 4,5-Epoxymorphinan-6-glycosides. This novel approach was used for preparation of pharmaceutically important 4,5-Epoxymorphinan-6-&bgr;-D-glucuronides. The process provides both high stereo-selectivity and high yields.

Abstract: This invention provides tissue selective estrogens of formula I having the structure wherein: R1 and R2 are independently, hydrogen, alkyl chain of 1-6 carbon atoms, benzyl, acyl of 2-7 carbon atoms, benzoyl, X is hydrogen, alkyl of 1-6 carbon atoms, CN, halogen, trifluoromethyl, or thioalkyl of 1-6 carbon atoms; n=1-3; with the proviso that at least one of R1 or R2 are not hydrogen, alkyl chain of 1-6 carbon atoms, benzyl, acyl of 2-7 carbon atoms, or benzoyl; or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides &bgr;-D-Glucuronidase substrates of the formula: wherein R1, R2, and R7-R12 are independently selected from the group consisting of: hydrogen, fluorine, chlorine, bromine, iodine, alkyl, hydroxyl, alkoxy, carboxyl and nitro groups; R3-R6 are independently selected from the group consisting of hydrogen, fluorine, chlorine, bromine, iodine, nitro and amino; and M+ is selected from the group consisting of: proton, lithium, sodium, potassium, magnesium, calcium, barium, and ammonium ion.

Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. In particular, this invention provides a novel class of effective compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.

Abstract: Ibuprofen-aspirin compounds useful in treating aspirin or ibuprofen-treatable conditions, hydroxymethylacylfulvene analogs useful as antitumor drugs, and L-sugar illudin analogs useful as antitumor drugs.

Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts and solvates thereof, wherein a, b, X, Y, Z, R1, R2, and R3 are as defined herein. The compounds of formula I are antibacterial and antiprotozoal agents useful for treating various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula I, to methods of treating bacterial and protozoal infections by administering the compounds of formula I, and to methods for preparing compounds of formula I.

Abstract: The compounds secoisolariciresinol (SECO), enterodiol (ED) and enterolactone (EL), which are metabolites of secoisolariciresinol diglucoside obtained from flaxseed, are used for the treatment of diseases or conditions requiring administration of an antioxidant. Diseases or conditions that may be treated include hypercholesterolemic atherosclerosis, type I and type II diabetes, ischemic heart disease, heart failure, endotoxic and hemmorhagic shock, inflammatory bowel disease, rheumatoid arthritis, Parkinson's disease, and stroke.

Abstract: The present invention provides fluorescent nucleoside analogs which comprise a fluorescent cyclic compound joined to a carbon of a sugar molecule such as pentose, hexose, ribose or deoxyribose or analogs thereof in either an &agr; or &bgr; configuration. The subject compounds are useful as probes in the study of the structure and dynamics of nucleic acids and their complexes with proteins. In addition, the subject compounds are useful in any technique which uses labeled oligonucleotides for detection. Non-fluorescent spacer molecules in which a cyclohexane, cyclohexene, decalin, or benzene is joined to a carbon of a sugar moiety such as pentose, hexose, ribose or deoxyribose are also provided. Also provided are the 5′ dimethoxytrityl-3′-O-phosphoramidite derivatives, suitable for incorporation into oligonucleotides by automated synthesizers.

Abstract: The present invention provides illudin analogs of the general formula (I): 1

Abstract: Highly specific biocatalytic reactions have been used to create a population of taxol derivatives.

Abstract: Macrolide compounds produced by culturing Saccharopolyspora species LW107129 (NRRL 30141) have insecticidal and acaricidal activity and are useful intermediates for preparing spinosyn analogs.

Abstract: The invention provides the use of the saponin derivatives, which is of the general formula (I) or the pharmaceutically acceptable salts and esters thereof: 1

Abstract: A method of treating polycystic kidney disease is described. The method involves administering soyasaponin Bb to an animal in need thereof.

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: Methods for treating, preventing, or inhibiting diseases and disorders associated with inflammation, cell-proliferation, and pain comprising the administration of a compound having the structural formula 1

Abstract: The present invention provides illudin analogs of the general formula I: 1

Abstract: A synthetic method for the preparation of the anti-tumor drug Etoposide. In one embodiment, the method includes the direct condensation of 4′-demethyl-epipodophylloxin with 2,3-di-O-dichloroacetyl-(4,6-O-ethylidene)-&bgr;-D-glucopyranose in the presence of trimethylsilyl trifluoromethane sulfonate (TMSOTf) to yield 4′-demethylepipodophyllotoxin-4-(2,3-di-O-dichloroacetyl-4,6-O-ethylidene)-&bgr;-D-glucopyranoside, followed by conversion of the same to etoposide. Other methods include use of different Lewis acids as catalyst, as well as different substituted glucopyranosides. This method provides enhanced yields over existing synthetic techniques, reduced reaction times and permits more favorable isolation reaction procedures.

Abstract: This invention provides tissue selective estrogens of formula I having the structure wherein: R1 and R2 are independently, hydrogen, alkyl chain of 1-6 carbon atoms, benzyl, acyl of 2-7 carbon atoms, benzoyl, X is hydrogen, alkyl of 1-6 carbon atoms, CN, halogen, trifluoromethyl, or thioalkyl of 1-6 carbon atoms; n=1-3; with the proviso that at least one of R1 or R2 are not hydrogen, alkyl chain of 1-6 carbon atoms, benzyl, acyl of 2-7 carbon atoms, or benzoyl; or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.

Abstract: The present invention relates to antifungal compounds having the structural formula: 1

Abstract: Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS—, HO— or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5′-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=—NH2, —OH, —COOH, —O—CO—R—COR*, —NH—CO—R—COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R* H, phenyl, alkyl with 1-6 carbon atoms.

Abstract: Use of stereoisomeric glycosidic compounds of formula (I) as pharmaceutical agents against psoriasis, compounds therefor and pharmaceutical formulations thereof wherein R1 and R2 are independently selected from —H, —OH, (1) and (2) and related esters and ethers thereto; R3 is selected from —H, (3), (4), (5), (6), (7) and (8) and related esters and ethers thereto; R4 is (9); R5 is selected from the group —CH3, —CHO, —COOH, —CH2OH and related esters and ethers thereto; R6 is selected from —OH, (10), (11), (12), (13) and (14) in the preparation of a medicament for the treatment of disease involving hyperproliferation of dermis cells.

Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1 and R2 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.

Abstract: The present invention provides a method of synthesizing an allyl pentasaccharide having the structure: as well as related oligosaccharide ceramides and other glycoconjugates useful as vaccines for inducing antibodies to epithelial cancer cells in an adjuvant therapy therefor, and in a method for preventing recurrence of epithelial cancer.

Abstract: Disclosed are novel pradimicin compounds which possess antifungal activity and, preferably, improved water solubility. The compounds of the invention are prepared by modifying the 4′-amino or 4′-alkylamino moieties of known pradimicin compounds.

Abstract: Compound of formula (I): wherein: R represents: a group of formula (i):  wherein X, Y and W are as defined in the description, or a group of formula (ii): —A—G  (ii) wherein: A represents a single bond or an optionally substituted alkylene chain, G represents a group selected from hydrogen, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, —OR2, —O—T1—NR3R4, —O—T1—NR2—T′1—NR3R4, —NR3R4, —NR2—T1—NR3R4, —NR2—T1—OR5, —NR2—T1—CO2R6, —NR2—T1—C(O)R6, —C(O)—NR3R4, —C(O)—NR2—T2, —O—C(O)T2, —O—C(S)—T2, —NR2—C(O)—T2, —NR2—C(S)—T2, —O—C(O)—O—T2, —O—C(O)—NR2—T2, —O—C(S)—O—T2, —O—C(S)—NR2—T2, —NR2—C(O)—O—T2,

Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, X1 and X2 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of treating bacterial and protozoal infections by administering the compounds of formula 1, and methods of preparing certain compounds of formula 1.

Abstract: A process is provided for obtaining diterpene glycosides which process extracts such diterpene glycosides from plant or botanical material so as to provide a product which is high in content of such diterpene glycosides, and substantially free of bitter tasting tannins. This advantageously provides a product which can be used as a sweetener material.

Abstract: The present invention provides novel, water soluble, carbohydrate derivatives of paclitaxel, methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such compounds. The compounds of the invention are modified at the 2′ or 7 position of paclitaxel and have the general formula [paclitaxel]-[link]1−2-[sugar]. These compounds show improved biological activity toward many cancer cell lines as compared to paclitaxel. Additionally, the conjugates are made from natural non-toxic materials which, when released, will be adsorbed as part of the body components.

Abstract: This invention provides a process for the preparation of a Eleutherobin derivative of the formula: wherein R1 is a hydrogen, ester, nitrile or C2H4—R wherein R4 is a carbohydrate, an alcohol an amine, an amide, an alkyne, or, R2 is a linear or branched alkyl moiety, R3 is an ester, an amide, a carbamate, an acetal compound,an ether or a urethane, R4 is a hydrogen or CH2,position C2 and C3 is cis or trans,position C8 is &agr; or &bgr; and a compound is produced having the structures: Additionally, this experiment provides a method for inhibiting growth of cancerous cells comprising contracting an amount of Eleutherobin derivative effective to inhibit the growth of said cells. Further provided is a method for treating cancer in a subject which comprises administering to the subject a therapeutically effective amount of the Eleutherobin derivative.

Abstract: A new crystalline form of morphine-6-glucuronide, referred to as Form A, characterized by its infrared spectrum pattern and/or by its x-ray powder diffraction image, the use thereof and a process for the preparation thereof.