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6696437 |
Heterocyclically substituted benzimidazoles, the production and application thereof
The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.
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6689381 |
Liposomal benzoquinazoline thymidylate synthase inhibitor formulations
Liposomal encapsulated benzoquinazoline thymidylate synthase inhibitor formulations are provided. The liposomes have improved pharmacokinetics and enhanced efficacy as anti-tumor agents compared to...
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6680326 |
Polycyclic compounds
Novel polycyclic compounds of the formula [I], wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , ring A, ring B, X, Y and Z are as defined herein and the pharmaceutically acceptable salts...
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6677333 |
2H-phthalazin-1-one derivatives and drug containing its derivatives as active ingredient
Poly(ADP-ribose)polymerase inhibitors containing as the active ingredient 2H-phthalazin-1-one derivatives represented by general formula (I) (wherein each symbol is as defined in the description)...
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6670360 |
Optically active pyrrolopyridazine derivatives
An optically active pyrrolopyridazine compound of the formula (I) or a pharmaceutically acceptable salt thereof: wherein R 1 is alkyl; R 2 and R 3 are each independently alkyl; R 4 is...
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6667302 |
Heterocyclic topoisomerase poisons
The invention provides compounds of formula I: wherein R 1 to R 5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds,...
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6656964 |
Method of inhibiting phosphodiesterases with substituted alkanohydroxamic acids
Imido and amido substituted alkanohydroxamic acids reduce the levels of TNFα and inhibit phosphodiesterase in a mammal. A typical embodiment is...
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6653320 |
Imidazopyridine derivatives
The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel...
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6645965 |
Nitrate salts of antihypertensive medicines
Nitric acid salts with medicines having an antihypertensive activity.
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6646013 |
Nutrient formulations for disease reduction
The instant invention provides a combination of multiple nutrients useful to reduce colon rectal cancer in a mannalian or human subject. Further, the combination provides synergistic ratios of the...
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6638938 |
Method for preventing tissue injury from hypoxia
There is disclosed a method for preventing tissue injury caused by tissue hypoxia and reoxygenation, comprising administering a compound that inhibits signal transduction by inhibiting cellular...
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6635641 |
Amide compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
Amide compounds represented by the formula: wherein: R 1 is a moiety represented by the formula where X is selected from the group consisting of CH 2 , O, S, and NH; and Y is selected from...
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6635642 |
PARP inhibitors, pharmaceutical compositions comprising same, and methods of using same
The present invention relates to PARP inhibitors, pharmaceutical compositions comprising the same, and methods of using the same to treat tissue damage resulting from cell damage or death due to...
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6635643 |
Bicyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives
The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R 1 and R 2 ...
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6630471 |
Substituted triazolo-pyridazine derivative, pharmaceutical compositions made therefrom
7-(1,1 -Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(
2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine, and pharmaceutically acceptable salts thereof are selective ligands for GABA A ...
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6627630 |
Condensed pyridazine derivatives, their production and use
A condensed pyridazine derivative which is useful as a pharmaceutical composition for preventing or treating allergic skin diseases such as contact dermatitis, pruritus, dried dermatitis, acute...
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6624159 |
Heterocycle carboxamides as antiviral agents
The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
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6624160 |
4-oxo-1,4-dihydro-3-cinnolinecarboxamides as antiviral agents
This invention provides compounds of formula I; which are useful as antiviral agents.
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6617325 |
Biphenyl derivatives, production thereof and uses as medicines
The present invention relates to biphenyl derivatives of general formula wherein R a to R g and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically...
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6613772 |
Substituted 2-aryl-4-amino-chinazolines, method for the production and use thereof as medicaments
Compounds of the formula I in which R 1 , R 2 , R 3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and...
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6613766 |
Pentaaza-cyclopental&lsqb a&rsqb naphthalene derivatives as ligands for GABAa α5 receptors
A class of 1,2,3a,4,x-pentaaza-cyclopenta[a]naphthalene compounds (x=6, 7, 8 or 9) is described. The compounds have a high affinity for the GABA A α5 receptors and show inverse agonist activity...
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6610692 |
Thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is NY...
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6610694 |
Condensed pyridazine compounds, their production and use
A condensed pyridazine derivative which exhibits anti-allergic activity, anti-histaminic activity and/or eosinophil chemotaxis-inhibiting activity, anti-inflammatory activity, anti-PAF...
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6605611 |
Base analogues
Nucleoside analogues or base analogues having structure (I), where X=O or NH or S, Y=N or CHR 6 or CR 6 , W=N or NR 6 or CHR 6 or CR 6 or S, n=1 or 2; each R 6 is independently H or O or alkyl...
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6602882 |
Quinoline derivatives and their use as antibacterial agents
Piperidine derivatives and pharmaceutical derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
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6593325 |
Pyrido-pyridazine derivatives as ligands for GABA receptors
A class of pyrido[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 8-position, a substituted alkoxy moiety at the 2-position,...
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6589951 |
Phthalazine derivatives as phosphodiesterase 4 inhibitors
Compounds of formula (I) wherein B is alkylene, amino, CONH or a bond; Cy is optionally substituted phenyl or heteroaryl; R is H, phenyl or (C 1-4 )alkyl optionally substituted; R 1 is (C 1-6...
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6586478 |
Methods and compositions for improving sleep
Methods and compositions for improving sleep in individuals with sleep disorders or other conditions which interfere with normal sleep via administration of a NO-mimetic are provided.
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6583134 |
Aza- indolyl derivatives for treating obesity
Novel compounds of formula (I): wherein X 1 , X 2 , X 3 and X 4 , n, R 1 , R 2 and R 3 are defined in the specification, and pharmaceutically acceptable salts and prodrugs of the compounds of...
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6583155 |
Method for treating allergies using substituted pyrazoles
A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
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6579876 |
Imidazo-pyridines, -pyridazines, and -triazines as corticotropin releasing factor antagonists
The present invention describes novel compounds of formula (Ib): wherein D is aryl or heteroaryl or pharmaceutically acceptable salt forms thereof, which are useful as corticotropin releasing...
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6566357 |
Spirocyclic-6,7-dihydro-5H-pyrazolo&lsqb 1,2-a&rsqb pyrazol-1-ones which control inflammatory cytokines
The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms...
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6562319 |
Radiolabeled irreversible inhibitors of epidermal growth factor receptor tyrosine kinase and their use in radioimaging and radiotherapy
Radiolabeled epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors and their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and...
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6562822 |
Heterocyle carboxamides as antiviral agents
The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
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6548512 |
Nitrogen containing heteroaromatics as factor Xa inhibitors
The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and...
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6548521 |
Inhibitors of metazoan parasite proteases
Compositions and methods for treating a patient infected with a metazoan parasite by inhibiting the enzymatic action of the metazoan parasite protease, wherein there is employed at least one...
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6548501 |
Composition and methods for stimulating gastrointestinal motility
The present invention is directed to methods for stimulating the motility of the gastrointestinal system in a patient which comprises administering a growth hormone secretagogue, a prodrug thereof...
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6544993 |
Tetrahydrothiopyranphthalazinone derivatives as PDE4 inhibitors
The compounds of formula (I) in which R1, R2, A and Ar have the meanings as given in the description are novel effective PDE4 inhibitors.
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6537991 |
Method of treating a peripheral neuropathic pain
The invention provides methods for treating and preventing neuropathic pain which comprise the administration of an effective amount of an antagonist of the pain-enhancing effects of E-type...
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6534505 |
Therapeutic polymorphs of a GABA-A alpha-5 inverse agonist and pamoate formulations of the same
There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)met
hyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate,...
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6525054 |
Cyanoiminoquinoxaline derivatives
A cyanoiminoquinoxaline derivative of the formula (II) is useful as a preventive or therapeutic agent for diseases due to hyperexcitation of glutamate receptors. (wherein, X and Y each is...
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6525055 |
Tricyclic phthalazine derivatives as phosphodiesterase 4 inhibitors
Tricyclic phthalazine compounds of formula (I) wherein A is a 5-7 membered heterocycle containing from 1 to 4 nitrogen atoms, optionally partially or totally unsaturated, and optionally...
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6518270 |
Heterocyclic compounds for inhibition of gastric acid secretion, processes for their preparation and pharmaceutical compositions thereof
The present invention relates to heterocyclic compounds of the formula (I), in which the phenyl moiety is substituted with lower alkyl in 2- and 6-position, which inhibit exogenously or...
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6514971 |
Cinnoline derivatives and use as medicine
The invention relates to the use of cinnoline derivatives of formula (I) wherein Z represents —O—, —NH—, —S— or —CH 2 —; m is a n integer from 1 to 5; R 1 represents hydrogen,...
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6514934 |
Imidazoline α-adrenergic receptor antagonist compounds in combination with nitric oxide donors, compositions and methods of use
The present invention is directed to nitrosated or nitrosylated α-adrenergic receptor antagonists, compositions comprising α-adrenergic receptor antagonists that are optionally substituted with...
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6512004 |
Promoters of neural regeneration
The invention provides methods and compositions for promoting neural cell growth and/or regeneration. The general methods involve contacting with an activator of a cyclic nucleotide dependent...
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6498159 |
Phthalazine derivatives and remedies for erectile dysfunction
The present invention provides a phthalazine compound as a therapeutic agent for erectile dysfunction represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate...
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6492366 |
Cyano-indole serotonin-reuptake inhibitor compound
A compound selected from those of formula (I): wherein: R 1 and R 2 each independently represent hydrogen or, alkyl, T 1 and T 2 each independently represent alkylene, G represents a...
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6489326 |
Medicinal preparation and process for manufacturing thereof
The present invention can be used in medical practice specifically in chemical and pharmaceutical production of medicinal agents capable of modulating the immune system. This invention essentially...
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6486158 |
&lsqb 4,5&rsqb -fused-3,6-disubstituted-pyridazines with sulfur-containing substituents in position three for the treatment of neoplasia
[4,5]-Fused-3,6 disubstituted-pydidazines of Formula I are useful for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in...
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