Abstract: Disclosed is a prodrug of the formula: where A is a sulfur or a selenium, and R is derived from a mono- di- or oligo- saccharide. Also disclosed is a prodrug of the formula: where A is sulfur or selenium, R? is derived from a sugar and R? has the formula (CHOH)nCH2OH, where n is 1 to 5, or R? is an alkyl or aryl group, or R? is ?O, and the R? groups may be the same or different and may be hydrogen, alkyl, alkoxy, carboxy. Also disclosed is a conjugate of an antioxidant vitamin and a thiolamine or selenolamine. Also disclosed is a prodrug of the formula; where A is sulfur or selenium, and R? is derived from a sugar and R? has the formula (CHOH)nCH2OH, where n is 1 to 5, or R? is also be an alkyl or aryl group, or R? is ?O, and R‡ is an alkoxy, or an amine group. Also disclosed is a prodrug of the formula: where R is COOH or H, and R? is derived from a sugar and R? has the formula (CHOH)nCH2OH,where n is 1 to 5, or R? is an alkyl or aryl group, or R? is ?O.

Abstract: The invention relates to the field of pharmacology. More particularly, the invention relates to the treatment of prostate conditions, such as BPH. The invention provides new therapeutic compositions and methods for treating BPH, as well as chronic prostatitis, prostadynia, and irritative bladder conditions, other than interstitial cystitis. The compositions and methods according to the invention, which may be administered orally, efficaciously and safely treat the designated conditions by causing regression of established lesions and reduction of bladder irritation. In particular, the compositions and methods of the invention treat BPH by reducing the size of the prostate gland and decreasing the associated obstructive symptoms.

Abstract: A pharmaceutical composition for the regulation of cytokine activity in a subject. The composition features an effective amount of an oligosaccharide to inhibit the cytokine activity, preferably through inhibition of TNF-alpha activity. The oligosaccharide is more preferably up to four saccharide units in length, and optionally and more preferably, is N-sulfated with at least one other sulfur moeity. The compositions are useful for the treatment of various pathological conditions related to, caused by or promoted through, cytokine activity.

Abstract: The present invention is to obtain novel anti-inflammatory agents having decreased antibacterial activity and increased anti-inflammatory action, and is psedoerythromycin derivatives represented by the following general formula [I], wherein R1 and R2 are same or different and each represents H, alkyl, alkynyl, acyl or sulfonyl, in which these groups may optionally have substituents, and Me indicates methyl.

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: 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: Polysaccharides, which are widely used as an anticoagulation drugs, especially heparin, are clinically administered only by intravenous or subcutaneous injection because of their strong hydrophilicity and high negative charge. Amphiphilic heparin derivatives were synthesized by conjugation to bile acids, sterols, and alkanoic acids, respectively. These heparin derivatives were slightly hydrophobic, exhibited good solubility in water, and have high anticoagulation activity. These slightly hydrophobic heparin derivatives are efficiently absorbed in the gastrointestinal tract and can be used in oral dosage forms. Methods of using these amphiphilic heparin derivatives and similarly modified macromolecules for oral administration are also disclosed.

Abstract: The present invention is a compound of general formula (I) or a pharmaceutically acceptable salt of, wherein W represents carbon chain from 9 to 17 which containing double bond or hydroxy group occasionally; X represents carbon chain from 11 to 25 which containing double bond or hydroxy group occasionally; Y represents —(CH2)a—CH═CH—(CH2)a′—, —(CH2)a— (a, a′ denotes an integer of 0-5 and a+a′ is 5 and under.), —S(O)0-2CH2—, —NHCH2—; Z represents —CO—, —SO2—; R represents —CH2OH, CO2H, CH2OCH2CO2SO3H; R0 represents —OH, —NH2, —NHAc.

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: Formulations for enhanced mucosal absorption of heparin are disclosed. In one embodiment, a powdered heparin composition is made by dissolving an amphiphilic heparin derivative including heparin covalently bonded to a hydrophobic agent in a water phase, dispersing the water phase in an organic phase such that an emulsion is formed, and drying the emulsion. In another embodiment, an amorphiphilic heparin derivative dispersed in an oil phase is made by dissolving the amphiphilic heparin derivative in water or a water/organic co-solvent, dispersing the water or co-solvent in the oil phase, and evaporating the water or co-solvent. In another embodiment, heparin-containing nanoparticles having surfactant molecules associated with a hydrophobic agent on the outside of the nanoparticles are made by dissolving the amphiphilic heparin derivative in an aqueous solvent, mixing the surfactant with the aqueous solvent, and disrupting nanoparticles of the amphiphilic heparin derivative.

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

Abstract: SGLT2 inhibiting compounds are provided having the formula where R1, R2, and R2a are independently hydrogen, OH, OR5, lower alkyl, CF3, OCHF2, OCF3, SR5i or halogen, or two of R1, R2 and R2a together with the carbons to which they are attached can form an annelated five, six or seven membered carbocycle or heterocycle; R3 and R4 are independently hydrogen, OH, OR5a, OAryl, OCH2Aryl, lower alkyl, cycloalkyl, CF3, —OCHF2, —OCF3, halogen, —CN, —CO2R5b, —CO2H, —COR6b, —CH(OH)R6c, —CH(OR5h)R6d, —CONR6R6a, —NHCOR5c, —NHSO2R5d, —NHSO2Aryl, Aryl, —SR5e, —SOR5f, —SO2R5g, —SO2Aryl, or a five, six or seven membered heterocycle, or R3 and R4 together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle; R5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h and R5i are independently lower alkyl; R6, R6a, R6b, R6c and R6d are independently hydrogen, alkyl,

Abstract: Disclosed are prodrugs as follows: (I) a prodrug of the formula where A is a sulfur or a selenium, and R is a mono- di- or oligo-saccharide; (II) a prodrug of the formula where A is sulfur or selenium, R′ is a sugar, or ═O, and the R″ groups are hydrogen, alkyl, alkoxy, carboxy; (III) a conjugate of an antioxidant vitamin and a thiolamine or selenolamine; (IV) a prodrug of the formula where A is sulfur or selenium, and R′ is a sugar, or an alkyl or aryl group, or ═O, and R‡ is an alkoxy, or an amine group; (V) a prodrug of the formula R is COOH or H, and R′ is a sugar or ═O.

Abstract: The present invention relates to a new kind of heavy metal chelating agents and a preparation process and uses thereof. The said heavy metal chelating agents are expressed in &agr;-[D(+)glucose-1-yl-amino]-&bgr;3-mercapto-(S)-propanoic acid (abbreviated to NGP,I) and/or N,N′-di[D(+)glucose-1-yl]-L-cystine (abbreviated to NGCD,II). In the process of preparation, glucose and cysteine are reacted with a base, with a reducing agent, and the obtained products are acidified to give NGP,I, which can be used in and/or as drugs, health foods and food additives for accelerating the excretion of heavy metals including Pb, Cd, Hg, Al, Sb, As, etc. The structural feature of the compounds of the present invention is that they contain glucose and cysteirie in their molecules.

Abstract: The present invention relates to a novel class of glycoside indoles. More specifically, the present invention relates to a novel class of glycoside indoles isolated from Calanthe discolor Lindl. and derivatives thereof.

Abstract: A combinatorial chemical library of compounds structurally related to the moenomycin class of antibiotics has the formula wherein D is a donor mono- or disaccharide, A is an acceptor monosaccharide, and P-R is a lipophosphoglycerate mimetic group. Members of the library have a glycosidic linkage between the anomeric carbon of D and the C2 carbon of A, and the D-A moiety is in turn covalently linked through the anomeric carbon of A to the P-R group. Members of the library exhibit their greatest structural diversity in terms of substitutions occurring at the C3 position of the A residue, substitutions at the C2 position of the D residue, and different P-R groups used in assembling the compounds. Members of the library are preferably synthesized by solid phase techniques involving stepwise coupling of the respective units to a support, functionalizing the A and/or D saccharides either before or after immobilizing them on the support, and cleaving the assembled compounds from the support.

Abstract: This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure wherein W is S, SO, SO2, NR; Y is O, S, NR, or CH2; R is hydrogen or alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, acyl of 2-7 carbon atoms, perfluoroacyl of 2-7 carbon atoms; R1 and R7 are each, independently, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, haloalkyl of 1-6 carbon atoms, nitroalkyl of 1-6 carbon atoms, cyanoalkyl of 1-6 carbon atoms, alkoxyalkyl of 2-12 carbon atoms, nitriloalkyl of 1-6 carbon atoms, phenyl mono-, di-, or tri-substituted with R8, phenylalkyl of 7-10 carbon atoms, wherein the phenyl ring is mono-, di-, or tri-substituted with R8, pyridyl substituted with R8, furyl substituted with R8, thienyl substituted with R8, and thiazolyl substituted with R8; R2 is hydrogen, R3, R4, R5, and R6 are each, independently, hydrogen, acyl of 2-7 carbon atoms, perfluoroacyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, p

Abstract: Polysaccharides, which are widely used as an anticoagulation drugs, especially heparin, are clinically administered only by intravenous or subcutaneous injection because of their strong hydrophilicity and high negative charge. Amphiphilic heparin derivatives were synthesized by conjugate to bile acids, sterols, and alkanoic acids, respectively. The hydrophobicity of the heparin derivatives depended on the feed mole ratio of heparin to hydrophobic agent. The heparin derivatives were slightly hydrophobic and exhibited good solubility in a water-acetone solvent, as well as water. The heparin derivatives have a high anticoagulant activity. These slightly hydrophobic heparin derivatives can be absorbed in gastric intestinal tract and can be used as oral dosage form. Also, the heparin derivatives can be used for the surface modification to prevent anticoagulation for medical devices such as extracorporeal devices and implanted devices.

Abstract: Synthesis of an amino-disaccharide, amino-oligosaccharide or a derivative thereof, characterized in that a monosaccharide, a disaccharide, an oligosaccharide, a glycoside or a derivative thereof, in the presence of a glycosidase as catalyst, is reacted with an amino-deoxy-saccharide or a glycoside or derivative thereof, and that the amino-saccharide is optionally isolated from the product mixture directly or after chemical/enzymatic modification.

Abstract: Novel substituted liposaccharides useful as in the prophylactic and affirmative treatment of endotoxemia including sepsis, septicemia and various forms of septic shock and methods of using these agents are provided. Also provided are methods of preparing these agents and intermediates useful therein.