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6878737 |
Reversal of multidrug resistance in human colon carcinoma cells
The present invention describes the use of fumitremorgin A, B and C and a series of diketopiperazines of Formula (I) to resensitize multidrug resistant (MDR) cancer cells to the cytotoxic effects...
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6875439 |
Formulation containing amphipathic weak base and/or amphipathic cation and multiple drug resistance inhibitor
Methods are provided relating to the enhanced cytoplasmic accumulation of amphipathic weakly basic or amphipathic cationic molecules in prokaryotes and eukaryotes under conditions of high...
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6844353 |
Fungicidal properties of sampangine and its analogs to agriculturally important fungal plant pathogens
It has been found that sampangine and related analogs such as benzo[4,5]sampangine, 4-bromosampangine and 4-methoxysampangine may be used as effective fungicidal agents for plants. Fungicidal plant...
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6828327 |
Macroheterocylic compounds useful as kinase inhibitors
This invention is directed to macroheterocyclic compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or...
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6825206 |
Camptothecin compounds with a thioether group
Camptothecin compounds which are effective anti-tumor compounds are disclosed. These conjugates inhibit the enzyme topoisomerase I and enhance the stability of the topoisomerase I-DNA cleavable...
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6815438 |
Heteroaryl-diazabicycloalkanes
The present invention relates to novel heteroaryl-diazabicycloalkanes which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the...
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6806291 |
Analgesic compounds, their synthesis and pharmaceutical compositions containing them
New analgesic compounds, which are prepared by the hydrolysis of N-acylated 4-hydroxyphenylamine derivatives, their synthesis and pharmaceutical compositions containing them are disclosed. These...
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6790847 |
Topical application of cetirizine and loratadine
The present invention relates to a drug composition containing the non-sedating H 1 antihistamines cetirizine, loratadine, mixtures or pharmaceutically acceptable salts thereof for topical...
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6784186 |
Therapeutic compounds
This invention relates to novel structural analogues and derivatives of compounds with general analgesic or related pharmacological activity. In particular the invention relates to derivatives of...
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6770654 |
Indole derivatives and use thereof in medicines
This invention relates to: an indole derivative or a pharmaceutically acceptable salt thereof represented by formula (I): wherein R 1 is, for example, hydrogen or C 1-5 alkyl; R 2 is, for...
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6767888 |
Neuroprotective methods and reagents
One aspect of the present application relates to a method for limiting damage to neuronal cells by ischemic or epoxic conditions, e.g., such as may be manifest by a reduction in brain infarct...
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6703398 |
Orally administered analgesic compositions containing nalbuphine
The present invention provides orally administered pharmaceutical compositions which contains an effective amount of free base or pharmaceutcially acceptable salts of nalbuphine and/or nalbuphine...
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6696480 |
Upregulation of type III endothelial cell nitric oxide synthase by agents that disrupt actin cytoskeletal organization
A use for agents that disrupt actin cytoskeletal organization is provided. In the instant invention, agents that disrupt actin cytoskeletal organization are found to upregulate endothelial cell...
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6689788 |
Method and composition for treatment of inflammatory bowel disease
A composition in unit dosage form for the inhibition, prevention or treatment of inflammatory bowel disease comprising an effective amount of a compound having the formula: and a...
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6642248 |
Benzo&lsqb b&rsqb pyrano&lsqb 3,2-h&rsqb acridin-7-one compounds
A compound selected from those of formula (I): wherein: X and Y represent group selected from hydrogen, halogen, mercapto, cyano, nitro, alkyl, trihaloalkyl, trihaloalkylcarbonylamino, —ORa,...
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6638941 |
Conformationallly constrained peptidomimetics as β-turn templates and modulators of SH3 domains
Spirolactam compounds useful as inhibitors of protein-protein interactions modulated by SH3 domains are disclosed. Compounds of the invention are also useful as β-turn mimetics. Also disclosed are...
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6613313 |
Aniline compound-containing hair dye composition and method of dyeing hair
A hair dye composition containing at least one of the following compounds: or analogues thereof; and a method for dyeing hair which comprises a step of applying to the hair the hair dye...
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6608073 |
Intranasal codeine for the rapid suppression of cough and rapid relief of pain
This invention provides a method of rapidly and reliably delivering codeine, alone or in combination with other compounds, to the systemic circulation by administration via the nasal route to...
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6602896 |
p38MAPK inhibitor and uses thereof
The present invention demonstrates that p38 MAPK inhibitor induces low density lipoprotein receptor expression 6-8 fold, and further provides the application of such inhibitor in the treatment of...
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6534514 |
Kappa opioid receptor antagonists
Compounds of the formula: are provided, which are selective kappa opioid receptor antagonists, wherein R 1 is (C 1 -C 5 )alkyl, C 3 -C 6 (cycloalkyl)alkyl, C 5 -C 7 (cycloalkenyl)alkyl, (C 6 -C...
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6528518 |
Treatment of depression with kappa receptor antagonists
The invention features the treatment of depression using kappa opioid receptor antagonists.
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6528517 |
Synthesis of quinobenzoxazine analogues with topoisomerase II and quadruplex interactions for use as antineoplastic agents
The present invention discloses a novel quinobenzoxazine self-assembly complex on DNA and on the topoisomerase II-DNA complex. The related model is used to design a new series of quinobenzoxazines,...
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6503919 |
Compounds of 7-oxo-2,3,7,14-tetrahydro-1H-benzo&lsqb b&rsqb pyrano&lsqb 3,2-h&rsqb acridin carboxylate
A compound selected from those of formula (I): wherein: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino,...
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6500824 |
Kappa (OP2) opioid receptor antagonists
The invention provides kappa receptor antagonists of formula (I), wherein R 1 -R 6 X and Y have any of the meanings given in the specification, as well as compositions comprising them, and methods...
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6465479 |
Pyridomorphinans and use thereof
Compounds represented by the formula: wherein each of Y, X and R individually is H, OH, alkyl, alkoxy, aryl, halo, CF 3 and NO 2 , provided that at least one of Y, X and R is other than H; and...
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6410041 |
Culturing cells in presence of amphipathic weak bases and/or cations and multiple drug resistance inhibitor containing reserpine
Methods are provided relating to the enhanced cytoplasmic accumulation of amphipathic weakly basic or amphipathic cationic molecules in prokaryotes and eukaryotes under conditions of high...
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6407089 |
Triazatrinaphthyrins and the use thereof
A novel class of macrocycles, termed triazatrinaphthyrins, is disclosed having general Formula I: or a solvate, hydrate, ester or salt thereof; wherein R 1 , R 2 , R 3 , R a , R a′ , R a″ ,...
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6407115 |
Hexa-cyclic compound
Accordingly, an object of this invention is to provide a hexa-cyclic compound represented by the following general formula: wherein R 1 and R 2 individually represent a hydrogen atom, a...
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6383528 |
Pharmaceutical composition comprising ticlopidine and Ginkgo biloba extract
The invention herein relates to a pharmaceutical composition comprising ticlopidine and Ginkgo biloba extract. In detail, as an anti-thrombotic preparation, the pharmaceutical composition...
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6365594 |
Heterocycle-condensed morphinoid derivatives (II)
Heterocycle-condensed morphinoid derivatives of formula (I), or solvates or salts thereof, are potent and selective delta opioid agonists and antagonists and are useful as i.a. analgesics....
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6323038 |
Diagnostic reagent for complications associated with diabetes or renal failure
In view of the situation of the prior art, the present invention specifies the structure of a late-stage product of Mailard reaction in vivo having a close relation with various tissue disorders,...
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6291470 |
Indole derivatives process for producing the same and medicinal uses of the same
A novel compound which is a δ-opioid antagonist having high selectivity and activity, that exhibits immunosuppressive action, antiallergic action, anti-inflammatory action and brain...
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6288074 |
Method of treating lymphoproliferative syndrome
Lymphoproliferative syndrome, including such diseases as malignant lymphoma, chronic lymphocytic leukemia, Hodgkin's lymphoma, and non-Hodgkin's lymphoma, is treated in human patients by the...
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6288072 |
Camptothecin β-alanine esters with topoisomerase I inhibition
β-Alanine esters of camptothecin compounds which are effective anti-tumor compounds are disclosed. These compounds inhibit the enzyme topoisomerase I and may alkylate DNA of the associated...
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6288073 |
Acronycine derivatives, preparation method and pharmaceutical compositions
A compound selected from those of formula (I): ##STR1## in which: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino,...
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6284769 |
Nonpeptide kappa opioid receptor antagonists
The compounds of structural formulae (I) and (II) ##STR1## and use of the compounds and salts and hydrates thereof, as therapeutic agents, is disclosed. A compound of formula (I) or (II) is an...
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6277829 |
Process for preparing of aqueous formulation for opthalmic use
The present invention describes a process for the preparation of aqueous formulations containing azithromycin for ophthalmic use, as well any formulations obtained by this process and their topical...
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6271264 |
Polymers containing spirobicyclic ammonium moieties as bile acid sequestrants
The present invention relates to a method for sequestering bile acids in a patient and to particular polymers for use in the method. The method comprises administering a therapeutically effective...
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6268375 |
10, 11-difluoromethylenedioxycamptothecin compounds with topoisomerase I inhibition
Camptothecin compounds having a C 10 11 O--(CF 2 ) n O group where n is 1 or 2 are effective anti-tumor compounds. These compounds inhibit the enzyme topoisomerase I and may alkylate DNA of the...
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6268377 |
Method for treating androgen-related conditions
The present invention provides for the combined use of 5α-reductase inhibitors together with calcium channel blockers for the treatment of benign prostatic hyperplasia (BPH), prostate cancer,...
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6265413 |
Camptothecin compounds and a method of preparation thereof
Camptothecin derivatives and pharmaceutically acceptable salts thereof, its manufacturing method and an antineoplastic agent containing it. The camptothecin derivatives are modified in B-ring and...
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6258856 |
Method for preventing or controlling cataract
A method for preventing or treating pathological changes which occur in association with cataract formation in the mammalian eye by protecting lens cells against the cataractogenic effects of...
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6218398 |
Nocathiacin antibiotics
Novel thiazolyl peptide antibiotic compounds, including nocathiacin I, II and III, are disclosed. Also, novel microorganism ATCC-202099 is disclosed.
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6214835 |
Dihalopropene compounds insecticides containing them as active ingredients, and intermediates for their production
The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R 1 is C 1 -C 10 alkyl or the like; L is C(O)NH or the like; R 2 , R 3 and R 4 are...
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6194422 |
Anthracycline derivatives
The present invention provides imino aza-anthracyclinones and a method of treating amyloidoses using the same.
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6187783 |
Phenanthridinium derivatives
A novel phenanthridinium derivative represented by general formula (A): ##STR1## wherein R 1 is a substituted or unsubstituted lower aliphatic hydrocarbon group; R is an aliphatic hydrocarbon...
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6187782 |
Morphinane derivatives and medicinal use thereof
Novel morphinan derivatives and pharmaceutically acceptable acid addition salts thereof as compounds having abilities to bind to opioid ε-receptor, which have agonist or antagonist activities, are...
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6172078 |
Quinolinomorphinane derivatives and medicinal use thereof
The present invention provides a quinolinomorphinan derivative or a pharmacologically acceptable acid addition salt thereof, and an agent for curing or preventing cerebral disorders composed of the...
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6156762 |
Indolomorphinan derivative and agent for curing and preventing cerebral disorder
The present invention provides an indolomorphinan derivative or a pharmacologically acceptable acid addition salt thereof, and an agent for curing and preventing cerebral disorders composed of the...
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6156754 |
Glycoconjugates of modified camptothecin derivatives (A-or B-ring linkage)
The present invention relates to glycoconjugates of camptothecin derivatives in which at least one carbohydrate component is linked via suitable spacers with the A or B ring of a camptothecin...
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