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7485651 |
Compounds with activity on muscarinic receptors
Compounds and methods are provided for the alleviation or treatment of diseases or conditions in which modification of muscarinic m1 receptor activity has a beneficial effect. In the method, a...
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7485641 |
Substituted 3-amino-pyrrolidino-4-lactams
The invention provides compounds of formula (1),
and the pharmaceutically acceptable salt thereof, wherein R 1 , n and R 2 are as described herein; compositions thereof; and uses thereof.
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7482472 |
Substituted isoindoles and their use
The invention relates to coagulation of the blood. Disclosed are novel compounds of formula (I),
a method for the production of these compounds, pharmaceutical compositions containing them, and...
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7476690 |
Thio-substituted tricyclic and bicyclic aromatic methanesulfinyl derivatives
The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of...
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7476676 |
Methods for increasing bone formation using inhibitors of glycogen synthase kinase-3β
This invention relates to the use of inhibitors of glycogen synthase kinase-3β to increase bone formation.
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7462640 |
Indol-6yl sulfonamide derivatives, their preparation and their use as 5-HT-6 as modulators
The present invention refers to new sulfonamide derivatives, of general formula (Ia, Ib, Ic) optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their...
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7459478 |
Substituted dihydropyrano indole-3,4-dione derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
Compounds of formula (I) and II) are provided
wherein: X is an alkali metal or a basic amine moiety; R 1 is alkyl, cycloalkyl, —CH 2 -cycloalkyl, pyridinyl, —CH 2 -pyridinyl, phenyl or...
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7459585 |
Benzene derivatives and pharmaceutical use thereof
The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory...
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7455864 |
Melatonin-based composition for improved sleep
A method for improving sleep in an individual comprising the administration of a composition comprising melatonin, lavender flower extract and Ferula extract is provided. The composition may be...
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7456209 |
IAP binding compounds
IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in...
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7453010 |
Phenylcyclohexylpropanolamine derivatives, preparation and therapeutic application thereof
The invention relates to compounds of general formula (I):
where R 1 represents H or a (C 1 -C 4 )alkyl, —CO(C 1 -C 4 )alkyl, (C 1 -C 4 )alkylphenyl or —CO-phenyl group, said phenyl...
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7449489 |
Indolylalkylamino-methylidenecarbamate derivatives useful as GnRH antagonists
The invention relates to a group of novel indole compounds of Formula (I): wherein: R 1 , R 2 , R 4 , R 6 , R 6a , R 7 , R 8 , R 9 , R 10 , and A are as defined in the specification, which are...
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7446103 |
Bicyclic benzamide compound as histamine H3 receptor ligand useful in the treatment of neurological diseases
The present invention relates to novel bicyclic benzamide derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the...
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7435729 |
Compounds and methods for modulation of estrogen receptors
Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for...
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7429612 |
Indoline compound and medicinal use thereof
The present invention provides an indoline compound represented by the formula (I)
wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and a...
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7419986 |
Antidepressant azaheterocyclylmethyl derivatives of heterocycle-fused benzodioxans
Compounds of the Formula:
are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
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7414070 |
Indol-7-YL sulfonamide derivatives, their preparation and their use in pharmaceutical compositions
The present invention refers to new sulfonamide derivatives, of general formula (Ia, Ib, Ic), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their...
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7407983 |
Indole derivatives substituted with long-chain alcohols and medicaments containing them
Provided is an indole long-chain alcohol, or a hydrate or an isomer thereof, represented by the following formula (I):
wherein R 1 , R 2 , R 3 and R 4 each independently represent a hydrogen...
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7405236 |
Indole derivatives comprising an acetylene group
This invention is directed to compounds of the formula (I):
wherein one of R 6 , R 7 , R 8 and R 9 is
and X, R 1 to R 12 , m, n and o are as defined in the description, and...
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7402603 |
Cyclooxygenase-2 inhibitor/histone deacetylase inhibitor combination
The invention relates to a combination which comprises (a) a cyclooxygenase-2 inhibitor (“COX-2 inhibitor”) and (b) a histone deacetylase inhibitor (“HDAI”) for simultaneous, concurrent,...
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7399780 |
3-Heterocyclyl-indole inhibitors of glycogen synthase kinase-3
The present invention provides new compounds of formula Ia and Ib: as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said...
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7384973 |
Materials and methods for treating hypercholesterolemia
The subject invention provides novel HMG-CoA-reductase inhibitors. In a preferred embodiment, the HMG-CoA reductase inhibitors of the subject invention can be deactivated to a primary inactive...
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7381739 |
2,4-substituted indoles and methods of use
The present invention provides a compound of the formula:
a pharmaceutically acceptable salt or a prodrug thereof, where R 1 , R 2 , R 3 , R 4 , p and n are those defined herein. The present...
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7381740 |
Melatonin analogue prodrugs
Disclosed are compounds that can serve as melatonin analogue prodrugs and that are soluble in aqueous solvents. Melatonin or melatonin analogues having modifications to the indole moiety are...
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7381731 |
Pharmaceutical composition comprising citrulline
Embodiments of the present invention include compositions and pharmaceutical compositions comprising citrulline and Hmg-CoA reductase inhibitors. Further embodiments relate to the use of such...
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7375113 |
Nitrogenous fused-ring derivatives, medicinal compositions containing the derivatives, and use thereof as drugs
The present invention provides nitrogen-containing fused-ring derivatives represented by the following general formula, or pharmaceutically acceptable salts thereof, or prodrugs thereof, which...
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7375118 |
Phenyl-indole compounds for modulating IgE and Inhibiting cellular proliferation
The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic....
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7368470 |
Substituted 3-pyrrolidine-indole derivatives
Substituted 3-pyrrolidine-indole derivatives and methods for their production. Also pharmaceutical compositions containing these compounds and the use of these substances in methods of treatment,...
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7365090 |
Substituted phenylindoles for the treatment of HIV
This invention is in the area of phenylindoles that are useful for the treatment of HIV infection, and, in particular, phenylindoles that exhibit significant activity against resistant strains of...
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7365091 |
Derivatives of succinic and glutaric acids and analogs thereof useful as inhibitors of PHEX
The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula:
useful as inhibitors of PHEX. These derivatives are...
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7361681 |
Method of treating amytrophic lateral sclerosis using melatonin
The present invention relates to the treatment of amyotrophic lateral sclerosis (ALS) and/or the improvement of motor function in individuals in need of such improvement using a melatonin compound...
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7351730 |
Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
This invention provides PAI-1 inhibiting compounds of Formula I:
wherein: R 1 , R 2 , R 3 , and R 4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R 8 ,...
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7351719 |
Amide compounds having MCH-antagonistic activity and medicaments comprising these compounds
The present invention relates to amide compounds of general formula I
wherein the groups and residues A, B, b, W, X, Y, Z, R 1 , R 2 and R 3 have the meanings given in claim 1 . Moreover the...
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7348354 |
Cyclohexylurea compounds
Cyclohexylurea compounds corresponding to formula I
a method for producing them, pharmaceutical compositions containing them, and the use of such compounds as pharmaceutically active agents...
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7348352 |
Diindolylmethane for the treatment of HPV infection
New methods and compositions are disclosed that comprise the phytochemical Diindolylmethane, alone or in combination with immune potentiating steroids. These methods and compositions are utilized...
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7345083 |
Hydroisoindoline tachykinin receptor antagonists
The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The...
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7345082 |
Phosphinic acids
The present invention relates to phosphinic acid derivatives of formula I
wherein R 1 , R 2 , R 3 and R 4 are described hereinabove. These compounds can be used in the treatment or prevention...
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7342029 |
Substituted indoles
Compounds of the formula I
are suitable for preparing pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NFκB is involved.
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7342040 |
5-fluorooxindole-3-carboxylic acid ester
A 5-fluorooxindole-3-carboxylic acid ester represented by a formula (2):
wherein R 1 is a group selected from the group consisting of an unsubstituted or substituted alkyl group having 1...
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7342038 |
Substituted diphenyl indanone, indane and indole compounds and analogues thereof useful for the treatment or prevention of diseases characterized by abnormal cell proliferation
The present invention provides substituted 3,3-diphenyl indole compounds, as well as analogues thereof, which are specific potent and safe inhibitors of mammalian cell proliferation. The compounds...
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7342039 |
Substituted indole oximes
The present invention relates to substituted indole oximes and methods of using them.
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7335678 |
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1(VR1) receptor
Compounds of formula (I)
are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity, wherein X 1 , X 2 , X 3 ,...
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7332521 |
Substituted indoles
The present invention relates generally to substituted indoles such as substituted 1H-indole-2-carboxylic acid derivatives, and methods of using them.
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7323494 |
Compounds and methods
Disclosed is a compound of having the formula:
pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables...
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7323488 |
Chromogenic enzyme substrates
This invention provides novel chromogenic enzyme substrates which are indoxyl β-D-ribofuranosides. A process for their production is provided. Methods for detecting β-D-ribofuranosidase activity...
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7319090 |
Methods of treating cerebral ischemia
The present invention provides methods of treating cerebral ischemia in mammals comprising inducing hypothermia in a mammal before, during, or following cerebral ischemia in the mammal. The...
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7317025 |
Non-peptidic NPY Y2 receptor inhibitors
The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to...
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7307088 |
Substituted anthranilic amide derivatives and methods of use
Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically...
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7307098 |
Indole derivatives and drugs containing the same
An indole derivative represented by the following general formula (1):
wherein at least one of R 1 , R 2 , R 3 , and R 4 represents an alkoxy group containing 1 to 20 carbon atoms, and...
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7294648 |
Anthranyl derivatives having an anticholecystokinin activity (anti-cck-1), a process for their preparation, and pharmaceutical use thereof
Anthranylic compounds having anti-CCK activity of general formula (I) in which, n is a whole number lying between 0 and 7; R 1 is chosen independently from the groups (II), in which X 1 is chosen...
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