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: 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 invention provides methods of preventing and treating pulmonary bacterial infection or symptomatic pulmonary exposure to endotoxin and related conditions in a patient by administering to the patient antiendotoxin compounds by inhalation.

Abstract: wherein when Y is  or heteroaryl; A is —O(CH2)m, S, —NH(CH2)m, or (CH2)n where n is 0-3 and m is 0-2; and R1 to R6 are as defined herein. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with one, two or more other antidiabetic agents, and/or one, two or more hypolipidemic agents.

Abstract: This invention provides novel substrate compounds that selectively inhibit the proliferation of pathological cells, for example, pathological calls that endogenously overexpress a target enzyme that confers resistance to biologic and chemotherapeutic agents. The enzyme acts on a substrate compound to 1) convert it to a cellular toxin and/or 2) release a toxic byproduct. In one embodiment, the activity of the target enzyme has been greatly enhanced in a target cell as a result of loss of tumor suppressor function and/or selection resulting from previous exposure to chemotherapy. In another embodiment, the pathological cell contains a target enzyme that is an expression product of an infectious agent in the cell. Further provided by this invention is a method for treating a subject by delivering to the subject a prodrug as described herein. The prodrugs of this invention may be used alone or in combination with other chemotherapeutics or alternative anti-cancer therapies such as radiation.

Abstract: The present invention discloses new and novel substituted anthracyclines with modified alkyl-aromatic ring substitutions on the C-3′ of the sugar moiety or modified or unmodified alkyl-aromatic ring substitutions at the C-4′ of the sugar moiety. It also discloses novel methods for the preparation of sugar substrates and methods for the preparation of anthracycline antibiotics. These anthracycline analogs show high cytotoxicity in vitro against several tumor cell lines.

Abstract: This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure wherein R1-R13 are as defined herein.

Abstract: Disclosed is an invention concerning triazolyloligosaccharides, oligosaccharides wherein the bonding between the saccharide groups is via a triazole group and methods for their preparation.

Abstract: The invention provides single-dose oral formulations for controlling an ectoparasite infestation on a companion animal for a prolonged time, said formulations comprising a spinosyn component, or a physiologically acceptable derivative or salt thereof, and a carrier in oral dosage form. It also provides methods for controlling such infestations comprising orally administering a single dose of these formulations to the animal.

Abstract: A medicament for treatment of a viral infection which comprises as an active ingredient a compound represented by the following formula (I) or its Pharmaceutically acceptable salt, or a hydrate thereof or a solvate thereof.

Abstract: Disclosed herein is a process for preparing highly pure acarbose of formula (I) useful as medicine for the treatment of diabetes. The disclosed process comprises prepurifying an acarbose-containing solution using a synthetic adsorbent to produce a prepurified acarbose having an acarbose content of a predetermined level or more; and contacting the prepurified acarbose with a monodispersed, strongly acid cation exchanger, in one step, to absorb acarbose.

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: 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 present invention relates to biscarbodiimides, thiourea derivatives, urea derivatives, and cross-linked hyaluronan derivatives having at least one intramolecular disulfide bond, and methods of preparation thereof. The invention also includes thiolated hyaluronan derivatives and salts thereof having at least one pendant thiol group or a modified pendant thiol group, and methods of preparation thereof. An example of a modified pendant thiol group is a sulfhydryl group linked to a small molecule such as a bioactive agent, for example a drug or pharmaceutically active moiety. A hyaluronan derivative having a sulfhydryl group linked to a pharmaceutically active moiety is useful as a sustained or controlled release drug delivery vehicle. Compositions containing the hyaluronan derivatives of the invention can reversibly viscosify in vivo or in vitro, in response to mild changes in condition, and are thus useful in ophthalmic surgery and in tissue engineering.

Abstract: Modified polysaccharides (such as starches, gums, chitosans, celluloses, alginates, sugars, etc.), which are commonly used in the paper industry as strengthening agents, surface sizes, coating binders, emulsifiers and adhesives, can be combined into a single molecule with amphiphilic hydrocarbons (e.g. surface active agents) which are commonly utilized in the paper industry to control absorbency, improve softness, enhance surface feel and function as dispersants. The resulting molecule is a modified polysaccharide having surface active moieties which can provide several potential benefits, depending on the specific combination employed, including: (a) strength aids that do not impart stiffness; (b) softeners that do not reduce strength; (c) wet strength with improved wet/dry strength ratio; (d) debonders with reduced linting and sloughing; (e) strength aids with controlled absorbency; and (f) surface sizing agents with improved tactile properties.

Abstract: Derivatives of sphingolipids of the formula: are provided wherein the substituents are as defined in the specification and wherein there is at least one R2 substituent in the sphingolipid derivative. The compounds are useful in the treatment of of abnormal cell proliferation, including benign and malignant tumors, the promotion of cell differentiation, the induction of apoptosis, the inhibition of protein kinase C, and the treatment of inflammatory conditions, psoriasis, inflammatory bowel disease as well as proliferation of smooth muscle cells in the course of development of plaques in vascular tissue. The invention also includes a method for triggering the release of cytochrome c from mitochondria that includes administering an effective amount of a sphingolipid or its derivative or prodrug to a host in need thereof.

Abstract: The present invention discloses novel sulfenate derivatives and their bioconjugates for phototherapy of tumors and other lesions. The sulfenates of the present invention are designed to absorb low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of free radicals, the reactive intermediate produced upon photofragmentation of the sulfenate moiety, with the tissue of interest.

Abstract: The present invention provides an agent for treatment of arthritic diseases such as rheumatoid arthritis that has for its active ingredient a complex of hyaluronic acid and zinc. This complex synergistically inhibits proliferation of synovial cells and suppresses matrix metalloproteinase MMP-9, which is produced by synovial cells, as compared with its constituents, hyaluronic acid and zinc, alone.

Abstract: Antibody-mediated xenograft rejection is attenuated by (1) removing preformed antibodies to various identified carbohydrate xenoantigens from the recipient's circulation prior to transplantation by extracorporeal perfusion of the recipient's blood over a biocompatible solid support to which the xenoantigens are bound and/or (2) parenterally administering a xenoantibody-inhibiting amount of an identified xenoantigen to the recipient shortly before graft revascularization and thereafter.

Abstract: The present invention provides novel thermoprecipitating polymers of formula 1, processes for the preparation thereof respectively and to the use thereof for the separation of enzymes. In formula 1 R is hydrogen or methyl, and x and y are integers greater than 1.

Abstract: Maltoligosaccharide derivatives represented by the general formula: wherein n is an integer of 0 to 3 and X is a hydrogen atom or a hydrophobic group) or their hydrates or physiologically acceptable salts, and an &agr;-amylase inhibitor and a prophylactic or therapeutic agent for hyperglycemia such as diabetes containing them as an active ingredient.

Abstract: Apoptosis inducers, anticancer drugs and carcinostatic drugs containing sulfated-fucose-containing polysaccharide(s) and/or degradation product(s) thereof, and a method for inducing apoptosis by using sulfated-fucose-containing polysaccharide(s) and/or degradation product(s) thereof as the active ingredient. A degrading enzyme which is useful in the production of the degradation products of sulfated-fucose-containing polysaccharides.

Abstract: Camptothecin derivatives of camptothecin of formula (I): wherein the groups R1, R2 and R3 are as defined in the description are disclosed. The compounds of formula (I) are endowed with antitumor activity and show a good therapeutic index. Processes for the preparation of the compounds of formula (I) and their use in the preparation of medicaments useful in the treatment of tumors, viral infections and antiplasmodium falciparum are also disclosed.

Abstract: Method for enhancing in a mammalian cell the activity of an enzyme associated with a lysosomal storage disorder by administering a competitive inhibitor of the enzyme in an amount effective to enhance the activity of the enzyme. Preferred compounds for use in the method are imino sugars and related compounds.

Abstract: This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-&agr;-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-&agr;-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.

Abstract: An improved process for the purification of crude aqueous solutions of acarbose by passing such solutions through a strong acid cation-exchange resin, saturating such resin and recovering as an eluate a substantially pure acarbose solution. Purities of more than 98%, and preferably about 99% or higher, are thus obtained.

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: Oligosaccharides including those usable as anti-inflammatory agent or anti-allergy agent, represented by the following general formula (3): wherein R10 and R11 each independently represent a hydrogen atom or —SO3M where M represents a proton or a monovalent cation, Ac represents an acetyl group, R12 represents a hydrogen atom or an anomeric substituent (a 6-O-sulfated N-acetylglucosamine residue, an alkyl group, a glycerol residue, an O-alkylglycerol residue, a cholesterol residue, a cholestanyl group, a ceramide residue, a phospholipid residue, a biotin residue, or a peptide residue), and Z represents an oxygen atom or —NHCO—.

Abstract: Processes for the preparation of 3′,4′-cyclic acetals of pentopyranosylnucleosides, in which the pentopyranosyl nucleoside is reacted with an aldehyde, ketone, acetal, or ketal under reduced pressure of less than about 500 mbar.

Abstract: Polysaccharide derivatives derived from a polysaccharide or a derivative thereof by substituting a part or all of the hydrogen atoms of the hydroxyl groups of the polysaccharide or the derivative thereof with the groups represented by the following formula (1): —E1—(OA)n—E2—R  (1) wherein E1 represents a divalent saturated C1-6 hydrocarbon group which may be substituted with one or more hydroxyl groups or oxo groups, n stands for a number of from 8 to 300, n numbers of As may be the same or different and each independently represent a divalent saturated C1-6 hydrocarbon group, E2 represents an ether bond or an oxycarbonyl group, and R represents a C4-30 alkyl group which may be substituted with one or more hydroxyl groups, in which the H(s) of one or more hydroxy groups in each of said groups (1) may be further substituted with the groups (1); thickeners and emulsifiers comprising these polysaccharide derivatives; as well as aqueous compositions containing said polysacchari

Abstract: A synthetic polysaccharide including an antithrombin III binding domain consisting of a concatenation of five monosaccharides supporting a total of two carboxylic acid functions and at least four sulpho groups, said domain being directly bound at the non-reducing end by a thrombin binding domain including a concatenation of 10-25 monosaccharide units selected from hexoses, pentoses or deoxy sugars of which all the hydroxyl groups are etherified by a C1-6 alkyl group or esterified in the form of sulpho groups, as well as salts and particularly pharmaceutically acceptable salts thereof, are disclosed.

Abstract: Glycosylated polyamines comprising of mono- or oligo-saccharides that are glycosidically linked to an aliphatic polyamine, and pharmaceutically acceptable salts, prodrugs and derivatives thereof are provided. An exemplary glycosylated polyamine has the following structure: Glycosylated polyamines, their pharmaceutically acceptable salts, prodrugs and derivatives are useful, for example, as anticancer compounds for the treatment of a variety of cancers. Methods for synthesis of glycosylated polyamines are disclosed. In addition, metal complexes of glycosylated polyamines, the preparation of such metal complexes, analytical methods using the metal complexes are provided. Methods for detecting equatorial and axial conformation of a group other than hydrogen at the C2 position of a saccharide molecule are also provided. The compounds of the invention can be used as anti-cancer agents (e.g., against breast, ovarian, colon or renal cancers).

Abstract: This invention provides compounds containing a 2-deoxy-2-amino-&bgr;-D-glucopyranose (glucosamine) glycosidically linked to an cyclic aminoalkyl (aglycon) group. The invention further provides methods for inducing an immune response using the compounds of the present invention in the presence or absence of an antigen. In addition, methods for treating disease with the compounds of the present invention with or without an antigen are also provided in this invention.

Abstract: Modified polysaccharides (such as starches, gums, chitosans, celluloses, alginates, sugars, etc.), which are commonly used in the paper industry as strengthening agents, surface sizes, coating binders, emulsifiers and adhesives, can be combined into a single molecule with amphiphilic hydrocarbons (e.g. surface active agents) which are commonly utilized in the paper industry to control absorbency, improve softness, enhance surface feel and function as dispersants. The resulting molecule is a modified polysaccharide having surface active moieties which can provide several potential benefits, depending on the specific combination employed, including: (a) strength aids that do not impart stiffness; (b) softeners that do not reduce strength; (c) wet strength with improved wet/dry strength ratio; (d) debonders with reduced linting and sloughing; (e) strength aids with controlled absorbency; and (f) surface sizing agents with improved tactile properties.

Abstract: An SGLT2 inhibiting compound is provided having the formula A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with another antidiabetic agent or other therapeutic agent.

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: The present invention relates to glycoconjugates of 20(S)-camptothecin, in which a 3-O-methylated &bgr;-L-fucose unit is linked to the 20-hydroxyl group of a camptothecin derivative via a thiourea-modified peptide spacer. The invention furthermore relates to processes for the preparation of the compounds according to the invention and to their use as medicaments, in particular in connection with oncoses.

Abstract: The invention relates to a compound of formula (I) wherein R1 is a sugar; R2 is —CH2—O—(R7)m, R7 representing a sugar, or is —COOH; R3 is an epoxide-comprising group, or is C1-C6-alkyl or C2-C6-alkenyl, unsubstituted or substituted by at least one OH; R5 is H, C1-C6-alkyl, C2-C6-alkenyl or C2-C6-alkynyl; R4R6, R8 and R10 independently of one another are H; C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, —X2H, or —X2R12, or R4 and R6 together and/or R8 and R10 together are =X2; X2 is O, NH, N—C1-C6-alkyl, N—C2-C6-alkenyl, N-C2-C6-alkynyl or S; R12 is C1-C6-alkyl, C2-C6—alkenyl, C2-C6-alkynyl, aryl or acyl; and m and n are 1 or 2; in any of its stereochemical forms and mixtures of these forms in any ratio, and a physiologically acceptable salt or derivative thereof. The compounds are obtainable from a culture of the microorganism Actinomycetales species HAG 003959, DSM 12931, by fermentation.

Abstract: A series of 2-(Purin-9-yl)-tetrahydrofuran-3,4-diol derivatives with broad anti-inflammatory properties which inhibit leukocyte recruitment and activation and which are agonists of the adenosine 2a receptor are described.

Abstract: An immunosuppressant comprising Glucopyranose derivatives of the formula (I): wherein R is H, OH etc; G is —CH2CH(R1—R2)(R3—R4), in which R1 is a single bond, OCO-alkyl; R2, R4 is H, phenyl which may be substituted by halogen atoms etc.; R3 is alkylene; R5 is OCO-alkyl, R6 is H, phenyl which may be substituted by halogen atoms etc. or R5—R6 is OCO—Z-(dialkoxyphenyl); R7 is H, CH2OH etc; or non-toxic salts thereof as active ingredient. Glucopyranose derivatives of the formula (I) or non-toxic salts thereof possess an activity of immunosuppression, and being useful as the prevention and/or treatment of diseases caused by abnormal enhancement of immunity, e.g. allergic diseases, autoimmune diseases.

Abstract: The subject invention lies in the field of vaccines. Specifically new compounds that can be used as adjuvants are provided. Recombinant LPS having a reduced number of secondary acyl chains per molecule of LPS vis a vis the corresponding non modified LPS molecule, said secondary acyl chains being bound to primary acyl chains, said primary acyl chains being bound to the glucosamine of said recombinant LPS molecule, said recombinant LPS being homogenous in acylation pattern is an example of such a compound. Also recombinant LPS having a phosphate group attached to the glucosamine at the non reducing end of the LPS molecule and a phosphate group attached to the glucosamine at the reducing end of the molecule per recombinant LPS molecule provides a further example.

Abstract: Glucosamine compositions comprising the compounds glucosamine sulfate metal chloride, wherein the metal, i.e., the cation is potassium, sodium, magnesium, lithium, calcium, zinc or manganese. The compounds have purity levels of at least about 97%, with water present in a maximum amount of about 10 wt. %, based on the weight of the composition. The compounds are prepared by contacting glucosamine hydrochloride with a hydroxide of the metal in the presence of water to form a first aqueous solution of the free glucosamine base and a chloride of the metal, acidifying the first aqueous solution with sulfuric acid to form a second aqueous solution of glucosamine sulfate and the chloride of the metal, and thereafter freeze-drying the second aqueous solution at a temperature and at a reduced pressure for such period of time that at least about 90 wt. % of the water is removed and decomposition of the compound glucosamine sulfate metal chloride is limited to a maximum of about 3%.

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

Abstract: The invention provides amine-protecting groups for use in solution phase or solid-phase oligosaccharide synthesis, in which a 2-substituted 1,3-dioxo compound is used to protect one or more primary amine groups of an aminosugar or gylycosylamine. The invention provides reagents, reagent kits, and methods for solution phase, solid-phase oligosaccharide synthesis.

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: Benzimidazole derivatives useful for treating or preventing viral infections such as those caused by herpes viruses or in the treatment of restenosis following surgical techniques. Methods of preparing these benzimidazole derivatives and pharmaceutical compositions containing them are described.

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: The disclosed invention is a composition agonists and/or antagonists of V2, V1a or both receptors, in a host, including animals, and especially humans, using a small molecule or its pharmaceutically acceptable salt or prodrug.

Abstract: The present invention has multiple aspects. In particular, in one aspect, the present invention is directed to a unit dose composition comprising 0.2 &mgr;g/kg to 48 &mgr;g/kg of an FGF-2 of SEQ ID NO: 2, or an angiogenically active fragment or mutein thereof in a pharmaceutically acceptable carrier. In another aspect, the present invention is directed to a method for treating a human patient for coronary artery disease, comprising administering into one or more coronary vessels or a peripheral vein of a human patient in need of treatment for coronary artery disease a safe and angiogenically effective dose of a recombinant FGF-2, or an angiogenically active fragment or mutein thereof. The single unit dose composition of the present invention provides an angiogenic effect in a human CAD patient that lasts six months before re-treatment is required. In another aspect, the present invention is directed to a method of administration which optimizes patient's safety.

Abstract: The present invention relates to novel prodrugs of gabapentin and to pharmaceutical formulations and sustained release formulations containing the prodrugs.