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7635684 |
Pyrazole derivatives, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof
The present invention provides pyrazole derivatives represented by the general formula:
wherein R 1 represents H, an optionally substituted C 1-6 alkyl group etc.; one of Q and T represents a...
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7622449 |
Anti-hypercholesterolemic compounds
This invention provides cholesterol absorption inhibitors of Formula I:
and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol...
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7605136 |
Effector conjugates, methods for their preparation and their pharmaceutical use
Conjugates of epothilones and epothilone derivatives (as effectors) with suitable saccharides or saccharide derivatives (as recognition units) are described. Their production is carried out by the...
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7598286 |
[(1H-indazol-3-yl)methyl]phenols and (hydroxyphenyl)(1H-indazol-3-yl)methanones
This invention provides anti-inflammatory agents of formula I, having the structure
wherein A and R 1 -R 10 are as defined in the specification, or a N-oxide thereof or a pharmaceutically...
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7589068 |
Inhibitors of Akt activity
The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for...
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7569679 |
Tanaproget derivatives, metabolites, and uses thereof
A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples...
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7566699 |
Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof
The present invention provides fused heterocyclic derivatives represented by the general formula:
wherein R 1 represents H, halogen, OH, etc.; R 2 represents H, halogen or an alkyl group; R 3...
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7556967 |
Foldable polymers as probes
Disclosed herein are novel probes, which can be used to detect and identify target molecules of interest in a sample. The disclosed probes can be used to monitor conformational changes induced by...
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7504489 |
Inhibitors of ADP-ribosyl transferases, cyclases, and hydrolases, and uses thereof
The present invention provides compounds having the formula:
wherein A is chosen from a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group; both B and C are...
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7439343 |
Aminoglycoside-polyamine displacers and methods of use in displacement chromatography
Aminoglycoside-polyamines are disclosed along with methods of use thereof in displacement chromatography and as DNA-binding ligands. The aminoglycoside-polyamines are derivatives of carbohydrates,...
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7423133 |
Fluorescent glycosides and methods for their use
Fluorescent glycosides containing aromatic hydrocarbon groups are useful in labelling and detection methods for a wide array of chemical and biological molecules. Assembly of multiple analogs to...
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7375213 |
Methods of producing C-aryl glucoside SGLT2 inhibitors
Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with...
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7375090 |
Glucopyranosyloxy-pyrazoles, pharmaceutical compositions containing these compounds, the use thereof and processed for the preparation thereof
The present invention relates to glucopyranosyloxy-pyrazoles of general formula
wherein
R 1 to R 6 and R 7a , R 7b , R 7c are defined as in claim 1 , the tautomers, the stereoisomers, the...
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7365055 |
Derivatives of morphine-6-glucuronide, pharmaceutical compositions containing them, their preparation method and their uses
The invention relates to novel derivatives of morphine-6-glucuronide, the preparation method thereof and the uses of same in therapy, for example, as analgesics.
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7361744 |
Oligosaccharide derivative
Compounds having the formula (I):
wherein A represents a group such as a cyclic group, R 1 and R 2 represent groups such as alkyl groups or hydroxymethyl groups, and n represents 1 or 2, or...
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7288528 |
Aromatic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof
Novel aromatic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof. The invention relates to substituted aromatic fluoroglycoside derivatives of the formula I...
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7217697 |
Glucopyranosyloxypyrazole derivative medicinal composition containing the same medicinal use thereof and intermediate therefor
The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula:
wherein R 1 is a hydrogen atom or a hydroxyalkyl group; one of Q and T is a group...
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7189702 |
Glucopyranosyloxypyrazole derivatives and medicinal use thereof
The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula:
wherein one of Q and T represents a group represented by the general formula:
while...
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7157432 |
Tetraphenylbacteriochlorin derivatives and compositions containing the same
Provided is a tetraphenylbacteriochlorin derivative represented by the formula (I):
[wherein R 1 , R 2 , R 3 and R 4 , independently from each other, are a residue of a monosaccharide...
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7129220 |
Substituted indole-O-glucosides
Substituted indole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed.
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7129221 |
6,11-bicyclic erythromycin derivatives
The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof:
which exhibit antibacterial properties. The present invention further...
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7122526 |
Indolocarbazole anticancer agents and methods of using same
The present invention relates to anti-tumor compounds, compositions and methods. In particular, the invention relates to indolocarbazole analogues of the following general formulas that inhibit...
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7112671 |
Non-symmetric tripyrranes in the synthesis of novel macrocycles
The present invention provides certain non-symmetric tripyrranes; that is, tripyrranes that do not contain a mirror plane of symmetry perpendicular to the plane containing the tripyrrane. Further,...
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7098327 |
Dual-functional ion exchange resins from agricultural by-products
A process for the production of dual-functional ion exchange resins from lignocellulosic agricultural material involving anionization of the lignocellulosic agricultural material with citric acid...
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7094764 |
Substituted benzimidazole-, Benztriazole-, and benzimidazolone-O-glucosides
This invention relates to to substituted benzimidazole-O-glucosides, benztriazole-O-glucosides, and benzimidazolone-O-glucosides, compositions containing them, and methods of using them, for...
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7087579 |
Glucopyranosyloxypyrazole derivatives and medicinal use thereof
The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula:
wherein one of Q and T represents a group represented by the general formula:
while...
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7084123 |
Glucopyranosyloxypyrazole derivatives and use thereof in medicines
The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula:
wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug:...
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7084124 |
Substituted indazole-O-glucosides
Substituted indazole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed.
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7071181 |
Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors
The present invention provides methods of treating diabetes and associated conditions by administering a composition including at least one sterol or 5α-stanol absorption inhibitor or compositions...
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7067494 |
Antimitotic eleuthesides
This invention provides analogs of eleutherobin and the eleuthesides modified at the C-11 position or comprising an epoxide functionality from C-11 to C-12. C-11 to C-12 is an ideal location for...
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7056906 |
Combinations of hormone replacement therapy composition(s) and sterol absorption inhibitor(s) and treatments for vascular conditions in post-menopausal women
The present invention provides compositions, therapeutic combinations and methods including: (a) at least one hormone replacement therapy composition; and (b) at least one sterol absorption...
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7053080 |
Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors
The present invention provides methods for the treatment of obesity using sterol or 5α-stanol absorption inhibitors and compositions and therapeutic combinations including sterol or 5α-stanol...
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7022678 |
Pregabalin lactose conjugates
In accordance with the present invention, there is provided pregabalin lactose conjugate compounds. Also provided as part of the present invention is a novel method of central nervous system...
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7019131 |
Programmable one-pot oligosaccharide synthesis
The reactivity of a number of p-methylphenyl thioglycoside (STol) donors which are either fully protected or have one hydroxyl group exposed has been quantitatively determined by HPLC in...
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6982251 |
Substituted 2-azetidinones useful as hypocholesterolemic agents
Hypocholesterolemic substituted 2-azetidinone compounds of the formula:
are disclosed, as well as a methods of lowering cholesterol by administering said compounds, pharmaceutical compositions...
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6958395 |
Method for producing water-soluble saccharide conjugates and saccharide mimetics by Diels-Alder reaction
The present invention relates to a method by which saccharide compounds can be prepared in a very easy way. This method comprises the steps of:
(a) attaching at least one saccharide to a cyclic or...
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6939858 |
Malto-oligosaccharide derivatives and use thereof
The present invention provides a substance which strongly inhibits human α-amylase and is effective for the prevention and treatment of hyperglycemia, for example, diabetes and the diseases caused...
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6916937 |
Carbohydrate prodrugs of fluorooxindoles
The present invention provides novel prodrug derivatives of fluorooxindoles having the general Formula I
wherein the wavy bond (
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6908905 |
N-substituted pyrazole-O-glycoside derivatives and therapeutic agent for diabetes containing the same
The present invention relates to pyrazole derivatives represented by the following formulas and analogues thereof, which can be used for a therapeutic agent for diabetes.
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6908989 |
Process for the production of perbenzylated 1-O-glycosides
The invention relates to a process for the production of perbenzylated 1-O-glycosides of general formula I or salts thereof
in which
sugar 1 is a monosaccharide that is functionalized...
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6887854 |
Compounds as dynamic organ function monitoring agents
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...
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6875755 |
Antithrombotic compound
The present invention relates to compounds of the formula (I), wherein R is independently SO 3 − or CH 3 ; the spacer is a flexible spacer of a length of 13-25 atoms; the charge of the...
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6858624 |
Aryl fused azapolycyclic compounds
This invention is directed to compounds of the formula (I):
and their pharmaceutically acceptable salts, wherein R 1 , R 2 , and R 3 are as defined herein; intermediates for the synthesis of...
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6849607 |
Galectin recognized photosensitizers for photodynamic therapy
Purpurin-carbohydrate conjugates and their method of preparation and use for treatment of cancer cells. The conjugates have the general formula:
wherein R 6 and R 7 taken together are ═NR...
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6844346 |
Chromogenic substrates of sialidase and methods of making and using the same
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...
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6841536 |
Prodrugs and conjugates of thiol- and selenol-containing compounds and methods of use thereof
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...
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6800742 |
Method for producing β-D-ribofuranose derivatives or optical isomers thereof
The present invention provides a method for efficiently producing β-D-ribofuranose derivatives or optical isomers thereof, useful as synthetic intermediates of pharmaceutical nucleic acid-series...
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6780616 |
Antibiotic caprazamycins and process for producing the same
There have been obtained, by cultivation of Streptomyces sp. MK730-62F2 (deposit number of FERM BP-7218), antibiotic caprazamycins A to F having by the following general formula (I) wherein R is...
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6774112 |
Amino acid complexes of C-aryl glucosides for treatment of diabetes and method
Crystalline complexes are obtained from a 1:1 or 2:1 mixtures of either the (D) or (L) enantiomer of natural amino acids and compounds of formula wherein R 1 , R 2 and R 2a are independently...
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6737518 |
Process for preparation of 4,5-epoxymorphinan-6-oxyglucuronides
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...
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