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7618994 |
Fluoro substituted cycloalkanoindoles, compositions containing such compounds and methods of treatment
Fluoro substituted cycloalkanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.
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7605274 |
Carvedilol
This invention relates to an improved process of preparing carvedilol, as well as a new crystalline hydrate and solvate and forms of carvedilol, processes for the manufacture thereof, and...
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7595337 |
Mitotic kinesin inhibitors
The present invention relates to tricyclic pyrazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting...
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7595336 |
Isatine derivatives with neurotrophic activity
The present invention relates to novel isatin derivatives, pharmaceutical compositions comprising the isatin derivatives of the invention, methods of preparing the isatin derivatives of the...
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7576119 |
Supports for oligomer synthesis
Universal linkers, their facile processes of manufacture and methods of using the same are provided.
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7576118 |
Asymmetric hydrogenation process
The present invention provides an asymmetric hydrogenation process for the preparation of chiral cycloalkanoindole DP receptor antagonists in high enantiomeric excess.
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7550500 |
Bicyclic and tricyclic amines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I):
A—E—NR 1 —G (I)
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7528164 |
Substituted 4-aryl-4h-pyrrolo[2,3-h]chromenes and analogs as activators of caspases and inducers of apoptosis and the use thereof
The present invention is directed to substituted 4H-chromenes and analogs thereof, represented by the Formula (I): wherein R 1 , R 3 -R 5 , A, D, Y and Z are defined herein. The present invention...
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RE40707 |
Use of carbazole compounds for the treatment of congestive heart failure
A method of treatment using carvedilol is disclosed, wherein the carvedilol decreases the risk of mortality caused by congestive heart failure in patients. The patients are titrated with low...
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7517904 |
Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions...
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7517903 |
Cytotoxic compounds and conjugates
The present disclosure provides drug-cleavable substrate conjugates that are potent cytotoxins. The disclosure is also directed to compositions containing the drug-cleavable substrate conjugates,...
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7517880 |
Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.
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7514467 |
Crystalline solids of carvedilol and processes for their preparation
This invention relates to a novel crystalline solid of carvedilol or a solvate thereof, to processes for its preparation, to compositions containing it and to its use in medicine. This invention...
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7465721 |
2-hydroxytetrahydrofuran derivatives and use thereof as medicaments
A hydroxytetrahydrofuran of formula
wherein A is
with the substituents as defined in the specification, having a calpain inhibiting activity and/or an activity which traps the reactive...
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7446122 |
Substituted indole derivatives
Provided herein are indole derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
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7442808 |
Antidiabetic bicyclic compounds
Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof,...
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7429578 |
Tricyclic inhibitors of poly(ADP-ribose) polymerases
Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma,...
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7427638 |
(+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione:, and methods of synthesis and compositions thereof
Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4
-acetylaminoisoindoline-1,3-dione, substantially free of its (−) isomer, and prodrugs, metabolites, polymorphs,...
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7425553 |
Triheterocyclic compounds, compositions, and methods for treating cancer or viral diseases
The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder...
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7423056 |
Tricyclic heteroaryl piperazines, pyrrolidines and azetidines as serotonin receptor modulators
The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More...
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7410951 |
Biologically active peptides and compositions, their use
Derivatives of hemiasterlin or Geodiamolide G having anti-mitotic activities and useful in treating cancer. These derivatives are represented by formula I
wherein Y, n, R 1 , R 2 , R 3 , R 7 ,...
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7388026 |
Prodrugs of CC-1065 analogs
Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the...
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7384946 |
M3 muscarinic acetylcholine receptor antagonists
Novel dimeric benzoazabicyclohepatane compounds, pharmaceutical compositions, processes for their preparation and use thereof in treating M 3 muscarinic acetylcholine receptor mediated diseases...
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7384933 |
Derivatives of 2-hydroxytetrahydrofuran and their use as medicaments
A hydroxytetrahydrofuran of formula
wherein A is
with the substituents as defined in the specification, having a calpain inhibiting activity and/or an activity which traps the reactive...
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7375127 |
Tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCRs)
The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the...
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7361680 |
Indole compounds useful for the treatment of cancer
The present invention provides novel indole derivatives useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti-cancer treatments.
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7354948 |
Methods for treatment of chronic uveitis using cyclopropyl-n-{2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-3-oxoisoindoline-4-yl}carboxamide
Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass...
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7351733 |
Tetrahydrocarbazole derivatives and their pharmaceutical use
The present invention relates to novel compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds.
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7351702 |
Caspase inhibitors and uses thereof
This invention provides compounds of formula I:
wherein Z is oxygen or sulfur; R 1 is hydrogen, —CHN 2 , R, CH 2 OR, CH 2 SR, or —CH 2 Y; next to R 3 represents a single or double bond;...
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7345062 |
Substituted acylhydroxamic acids and method of reducing TNFαlevels
Imido and amido substituted acylhydroxamidic acids which reduce the levels of TNFα and inhibit phosphodiesterase in a mammal. A typical embodiment is...
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7332520 |
Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to fused indole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention...
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7332516 |
Geminally di-substituted NSAID derivatives as Aβ42 lowering agents
The present invention encompasses compounds of Formula I (I)
or pharmaceutically acceptable salts thereof, wherein A is the base molecule of a propionic acid or acetic acid NSAID, or a...
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7323487 |
Condensed indoline derivatives and their use as 5HT, in particular 5HT2C, receptor ligands
A chemical compound of formula (I) wherein R 1 and R 2 are independently selected from hydrogen and alkyl; R 3 is alkyl; R 4 and R 5 are selected from hydrogen and alkyl; R 6 and R 7 are...
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7317036 |
Fluoro substituted cycloalkanoindoles, compositions containing such compounds and methods of treatment
Fluoro substituted cycloalkanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.
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RE40000 |
Method of treatment for decreasing mortality resulting from congestive heart failure
A method of treatment using a compound of Formula I:
wherein:
R 1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl; R 2 is hydrogen,...
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7314886 |
Tetrahydropyrano-indole derivatives
Provided herein are indole derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
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7288561 |
Sulfonyltetrahydro-3H-benzo(E)indole-8-amine compounds as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a CNS disorder related to or affected by the 5-HT6 receptor
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7288560 |
Spirocyclic cyclohexane derivatives
The present invention relates to spirocyclic cyclohexane compounds, to methods for their production, to pharmaceutical compositions containing these compounds, to methods of treatment using such...
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7282514 |
Reactive probes for two-photon fluorescent imaging and sensing
Fluorescent dyes and probes are key components in multiphoton based fluorescence microscopy imaging of biological samples. In order to address the demand for better performing dyes for two-photon...
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7268157 |
Substituted arylalcanoic acid derivatives as PPAR pan agonists with potent antihyperglycemic and antihyperlipidemic activity
Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, R 1 , R 2 , R 3 , R 4 , R 5 , X, Alk 1 , Alk 2 , Ar 1 , and Ar...
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7268156 |
Carvedilol phosphate salts and/or solvates thereof, corresponding compositions and/or methods of treatment
The present invention relates to carvedilol phosphate salts, which include novel crystalline forms of carvedilol dihydrogen phosphate (i.e., dihydrogen phosphate salt of...
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7265146 |
Integrin receptor inhibitors
Provided are compounds of formula (I)
wherein A, Q, W, X, Y, Z, R 1 to R 4 , m and n are as defined herein. Compounds of the invention bind to α 4 integrin receptors and thereby inhibit...
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7250441 |
Carbazole and cyclopentaindole derivatives to treat infection with Hepatitis C virus
The invention is directed to a method of treating, preventing, or inhibiting a Hepatitis C viral infection in a mammal comprising contacting the mammal with an effective amount of a compound of the...
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7250440 |
(Hydroxyphenyl)-1H-indole-3-carbaldehyde oxime derivatives as estrogenic agents
This invention provides estrogen receptor modulators of formula I, having the structure
where R 1 , R 2 , R 3 , and R 4 are as defined in the specification, or a pharmaceutically acceptable...
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7250439 |
Matrix metalloproteinase inhibitors
Compounds of formula (I):
wherein:
Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, NR 5 or CR 6 R 7 ; Y represents CHOH, CHSH, NOR 8...
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7250409 |
Ningalin B analogs employable for reversing multidrug resistance
Anlogs of ningalin B lacking inherent cytotoxic activity may be employed to reverse multi-drug resistant (MDR) phenotype and to resensitize transformed cells, including a human colon cancer cell...
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7247650 |
Macrolides and methods for producing same
This invention relates, in part, to macrolide compounds, actinomycete strains for producing them, and pharmaceutical compositions containing them.
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7241796 |
Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A protease. As such, they act by interfering...
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7238718 |
Method for treating myolytic disease and method for screening antimyolytic agent
An object of the present invention is to provide a method which is able to prevent or improve the progress of myolytic diseases such as muscular dystrophy. Such an object is able to be solved by a...
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7238374 |
Process and substances for the release of a growth-regulating factor from endothelial cells
Endothelial cells have the natural property of releasing soluble factors into the fluid surrounding them, said factors altering the behavior of immune cells. In cell systems containing at least...
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