Abstract: The present invention provides compounds of formula I 1

Abstract: 3-Descladinosyl-6-O-carbamoyl and 6-O-carbonoyl macrolide antibacterial agents of the formula: 1

Abstract: Camptothecin derivatives of camptothecin of formula (I) 1

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: Compounds having activity against methicillin-resistant staphylococcus aureus (MRSA), the compounds having formula (I) 1

Abstract: Substantially pure isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A having the Formula I: 1

Abstract: A macrolide antibiotic of the formula 1

Abstract: Antibacterial compounds having formula (I) 1

Abstract: The present invention provides pyrazole-O-glycoside derivatives represented by the following formulae, used as a diabetic medicine.

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: One aspect of the invention relates to novel complexes of technetium (Tc) with various heteroaromatic ligands, e.g., pyridyl and imidazolyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to novel pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the technetium complexes are also described. Another aspect of the invention relates to novel pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.

Abstract: This invention provides for labeling reagents, labeled targets and processes for preparing labeling reagents. The labeling reagents can take the form of cyanine dyes, xanthene dyes, porphyrin dyes, coumarin dyes or composite dyes. These labeling reagents are useful for labeling probes or targets, including nucleic acids and proteins. These reagents can be usefully applied to protein and nucleic acid probe based assays. They are also applicable to real-time detection processes.

Abstract: 6-O-Acyl ketolide antibacterials of the formula: 1

Abstract: Antibacterial compounds with improved pharmacokinetic profiles having formula (I) 1

Abstract: A therapeutic composition is provided that comprises a 1-R1-phenyl, 4-R2-phenyl substituted 1,2,3,6-tetrahydropyrimidine-2-one sensory nerve receptor agonist in a therapeutically effective amount. The sensory nerve receptor agonist may be represented by the general formula 1-[R1-phenyl]-4-[R2-phenyl]-1,2,3,6-tetrahydropyrimidine-2-one wherein: R1 may be -hydroxy, -chloro, -fluoro, -alkyl, -acetoxy, -trifluoromethyl ; and R2 is -nitro, -chloro, -fluoro, -alkyl, -trifluoromethyl. Therapeutic compositions of the invention reduce pain, a sense of abdominal distension, tenesmus, and abnormal bowel function when formulated for oral delivery to human gastrointestinal tract and are useful to alleviate gastrointestinal dysfunction.

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: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.

Abstract: The invention relates to novel magnetic resonance imaging contrast agents and methods of detecting physiological signals or substances.

Abstract: The present invention relates to sodium channel blockers. The present invention also relates to a variety of methods of treatment using the sodium channel blockers.

Abstract: Substituted propanolamine derivatives, their pharmaceutically tolerated salts and physiologically functional derivatives thereof are described.

Abstract: The present invention relates to sodium channel blockers. The present invention also relates to a variety of methods of treatment using these sodium channel blockers.

Abstract: The use of azetidinone compounds that are inhibitors of cholesterol absorption as tools for discovering and characterizing proteins involved in trafficking or absorption of cholesterol and/or cholesteryl esters in biological systems is presented. These compounds can serve as tools for competitive binding assays to discover and characterize other chemical agents useful as cholesterol absorption inhibitors. New compounds of the present invention are also highly efficacious inhibitors of cholesterol absorption.

Abstract: A 2-oxoquinoline compound or its pharmaceutically acceptable salt of general formula [I]: 1

Abstract: Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and phototoxic agent to diseased tissues A combination of these elements takes full advantage of the unique and efficient properties of each component for an effective patient care management.

Abstract: Nucleic acid labeling compounds containing heterocyclic derivatives are disclosed. The heterocyclic derivative containing compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.

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: Molecular conjugates for the treatment and prevention of infectious diseases due to pathogenic microorganisms are provided. These conjugates comprise at least one photosensitizer coupled to a microorganism receptor (vector) that binds selectively to the surface of a microorganism, such as bacteria, viruses, mycoplasma, fungi, parasites and others. Complex aggregates formed by self-association of carbohydrate-photosensitizer conjugates or that are constructed on the base of a carrier form multiple interactions with the binding sites on the surface of the selected microorganism due to their polyligand carbohydrate surrounding. The property of the conjugates to bind selectively to sites on targeted microbes and to block these sites defines their ability to act as inhibitors of microbial cell adhesion and thereby provides an ability to prevent infectious disease. Methods for treatment and prevention of infectious diseases due to pathogenic microorganisms are also provided.

Abstract: Provided is a tetraphenylbacteriochlorin derivative represented by the formula (I): 1

Abstract: This invention is directed to compounds of the formula (I): 1

Abstract: A DDS compound in which amino group at 1-position of (1S,9S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H-benzo[de]pyrano[3′,4′:6,7]-indolizino[1,2-b]quinoline-10,13(9H,15H)-dione as a drug compound is bound to a carboxyl group of a carboxymethyldextran polyalcohol with a spacer containing one amino acid or two to eight amino acids linked by peptide bond(s); characterized in that an introduced amount of residue of the drug compound is in a range of from 3.2% to 8.4% by weight; a weight-average molecular weight of the carboxymethyldextran polyalcohol is in a range of from 240,000 to 480,000; and degree of carboxymethylation is in a range of from 0.14 to 0.47; and a method for preparing said DDS compound, which comprises the steps of, for example, adding an aqueous solution containing sodium periodate to an aqueous solution containing dextran at a temperature of 4° C.±2° C.

Abstract: The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.

Abstract: The present invention is directed to an aryl-substituted propanolamine derivative of formula I 1

Abstract: The present invention is related to polysaccharide esters of N-derivatives of glutamic acid (N-GA derivatives). These polysaccharidic esters have antiproliferative activity and are characterized by a low systemic toxicity. The esters of the invention are used in the prevention and therapy of diseases caused by cellular hyperproliferation, particularly psoriasis, tumors, rheumatoid arthritis, or intestinal inflammatory pathologies.

Abstract: Methods are provided for cancer and pre-cancer detection by increased uptake of fluorophore glucose or deoxyglucose conjugates in cancerous and pre-cancerous cells relative to normal cells.

Abstract: The present invention relates to anti-tumor compounds, compositions and methods.

Abstract: A pharmaceutical composition having an ensured preservation stability, which contains a compound, wherein a polysaccharide derivative having a carboxyl group is bonded to a camptothecin derivative via a spacer or without mediated by any spacer, and a sugar or a sugar alcohol optionally together with a pH-adjusting substance.

Abstract: The invention provides polymer conjugates of protein kinase C (PKC) inhibitors comprising a polymer, such as poly(ethylene glycol), covalently attached to a PKC inhibitor, such as a bisindolylmaleimide molecule. The linkage between the polymer and the PKC inhibitor is preferably hydrolytically degradable. The invention also includes a pharmaceutical composition comprising a polymer conjugate of a PKC inhibitor and a method of treating any condition responsive to a PKC inhibitor by administering a polymer conjugate of the invention.

Abstract: Cyanine dye bioconjugates useful for diagnostic imaging and therapy are disclosed. The conjugates include several cyanine dyes with a variety of bis- and tetrakis (carboxylic acid) homologues. The compounds may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350-1300 nm, the exact range being dependent upon the particular dye. Use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The inventive compounds are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities, for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.

Abstract: The synthesis of deuterated analogues of rapamycin is disclosed together with a method for use for inducing immunosupression and in the treatment of transplantation rejection, graft vs host disease, autoimmune diseases, diseases of inflammation leukemia/lymphoma, solid tumors, fungal infections, hyperproliferative vascular disorders. Also described is a method for the synthesis of water soluble deuteratred rapamycin compounds and their use as described above.

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: The invention relates to novel bicyclic aromatic compounds which have the general formula (I): 1

Abstract: Novel compounds of Formula (I) 1

Abstract: 6-O-Carbamate-11,12-lacto-ketolide antimicrobials of the formula: 1

Abstract: The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of benzimidazole compounds as inhibitors of membrane fusion associated events, such as viral transmission. In another embodiment, the invention encompasses processes for making benzimidazole compounds, methods of using the benzimidazole compounds and compositions comprising the benzimidazole compounds. Finally, the invention provides methods for treating, preventing or ameliorating symptoms associated with respiratory infection, particularly that caused by Respiratory Syncytial Virus utilizing the novel benzimidazole compounds of the invention.

Abstract: The present invention relates to compounds of the formula (I), wherein R is independently SO3− or CH3; the spacer is a flexible spacer of a length of 13-25 atoms the charge of the pentasaccharide residue is compensated by positively charged counterions; and the total number of sulfate groups in the pentasaccharide residue is 4, 5 or 6; or a pharmaceutically acceptable salt, a prodrug or a solvate thereof. The compounds of the invention have antithrombotic activity and can be used in treating or preventing thrombin-related diseases.

Abstract: Fungicidal 5,5-disubstituted thiazolidine derivatives are provided having the formula; 1

Abstract: The invention relates to compounds of Formula 1 1

Abstract: Hypocholesterolemic substituted 2-azetidinone compounds of the formula: 1

Abstract: Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and phototoxic agent to diseased tissues. A combination of these elements takes full advantage of the unique and efficient properties of each component for an effective patient care management.