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7619110 |
Amino acid derived prodrugs of propofol, compositions, uses and crystalline forms thereof
The present invention provides a prodrug of propofol and crystalline forms thereof, methods of making the propofol prodrug and crystalline forms thereof, pharmaceutical compositions of the propofol...
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7612087 |
Heterocyclic compounds as inhibitors of beta-lactamases
This invention discloses and claims methods for inhibiting bacterial β-lactamases and treating bacterial infections by inhibiting bacterial β-lactamases in man or an animal comprising...
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7612085 |
Sigma 2 receptor ligands and therapeutic uses therefor
A series of N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs are disclosed, as well as methods of their preparation. Their affinities for sigma (σ1 and σ2) receptors are...
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7612084 |
Amine derivatives for the treatment of asthma and COPD
The invention relates to compounds of formula (1)
and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives....
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7608626 |
Substituted indolizines and derivatives as CNS agents
Compounds of formula 1 or pharmaceutically acceptable salts thereof are provided:
which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and...
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7601735 |
Antiviral compounds
Use of certain castanospermine esters in the treatment of diseases caused by flaviviruses, in particular in the treatment of disease caused by the hepatitis C virus (HCV) and compositions...
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7598233 |
Method for treating thrombosis
This invention relates to a method for treating thrombosis by combined administration of a pitavastatin with aspirin.
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7592337 |
Di-aryl substituted tetrazole modulators of metabotropic glutamate receptor-5
Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring,...
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7585874 |
Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives
The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives of formula I:
wherein
R 1 to R 5 are as defined in the specification and pharmaceutically...
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7582650 |
Tricyclic opioid modulators
The invention is directed to compounds of Formula (I) useful as delta and mu opioid receptor modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and...
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7572798 |
Combi-molecules having signal transduction inhibitory properties and DNA damaging properties
The present invention relates to a series of new chemical agents that demonstrate anti-tumor activity. More particularly, the present invention relates to molecules, referred to as...
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7563774 |
Combination of FBPase inhibitors and antidiabetic agents useful for the treatment of diabetes
A combination therapy of at least one FBPase inhibitor and at least one other antidiabetic agent is disclosed.
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RE40838 |
2-azabicyclo[3.3.1]nonane derivatives
The subject invention relates to 2-azabicyclo[3.3.1]nonane derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states,...
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7553846 |
2-alkylbenzoxazole carboxamides as 5-HT3 modulators
Compounds of formulae I and II:
are disclosed as 5-HT 3 inhibitors. Those compounds are useful in treating CINV, IBS-D and other diseases and conditions.
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7553845 |
Substituted indolizine 1,2,3,6,7,8 derivatives, FGFs inhibitors, a method for the preparation thereof and pharmaceutical compositions containing said derivatives
The invention is directed to a compound of formula I,
wherein R, R 1 , R 2 , R 3 and R 4 are as defined herein, or a pharmaceutically acceptable salt thereof, and its pharmaceutically...
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7553844 |
Methods for treatment of HIV or malaria using combinations of chloroquine and protease inhibitors
The present invention relates to a drug combination capable of conferring therapeutic benefits in the treatment of both AIDS and malaria. In particular, it relates to a drug combination including...
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7524958 |
Certain 9-aza-bicyclo[3.3.1] nonane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
This invention relates to novel 9-aza-bicyclo[3.3.1]nonane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these...
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7524858 |
Substituted pyrroline kinase inhibitors
The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder.
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7517988 |
Hydroxamates as therapeutic agents
The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore...
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7511058 |
Heterocyclic inhibitors of MEK and methods of use thereof
Disclosed are compounds of the Formula III
and pharmaceutically acceptable salts and prodrugs thereof, wherein R 1 , R 2 , R 7 , R 8 , R 9 R 10 , and W are as defined in the specification....
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7488735 |
Quinuclidine amide derivatives
New quinuclidine amide derivatives having the chemical structure of general formula (I) and pharmaceutically acceptable salts thereof including quaternary salts of formula (II) are disclosed; as...
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7479498 |
Treatments for viral infections
The present invention relates to improved methods and compositions for treating viral infections and other diseases and conditions that induce a cytokine storm. More particularly, the present...
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7449582 |
Compounds and compositions as protein kinase inhibitors
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated...
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7442708 |
1,2,3-substituted indolizine derivatives, inhibitors of fgfs, method for making same and pharmaceutical compositions containing same
Compounds of formula I or salts thereof:
in which
R 1 represents —OH, (C 1 -C 5 )alkoxy, carboxyl, (C 2 -C 6 )alkoxycarbonyl, —NR 5 R 6 , —NH—SO 2 -Alk, —NH—SO 2 -Ph,...
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7435742 |
Quinuclidine derivatives and pharmaceutical compositions containing the same
Carbamates of formula (I) or pharmaceutically acceptable salts thereof, including quaternary ammonium salts of formula (II) are disclosed; as well as processes for their preparation, pharmaceutical...
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7425561 |
3-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof
The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally...
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7417041 |
Imidazopyrimidines as transforming growth factor (TGF) inhibitors
Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described....
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7411076 |
Coumarin derivative
A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the following general formula...
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7410978 |
Once daily dosage forms of trospium
A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (C...
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7410961 |
2,6-disubstituted piperiddines as modulators
The present invention is further directed to compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 16 , R 17 , R 18 , R 19 , R 20 , R 21 and R 22 are as...
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7402592 |
Pharmaceutical compositions and methods for relieving pain and treating central nervous system disorders
Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release...
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7399769 |
Aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives
The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives of formula
wherein:
R 1 , R 2 , and R 3 are as defined herein and pharmaceutically acceptable...
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7399749 |
Substituted prolines as inhibitors of hepatitis C virus NS3 serine protease
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses...
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7393857 |
Use of 5-HT3 receptor antagonists for treating musculoskeletal diseases
The present invention relates to a new use for compounds having 5-HT 3 (serotonin M) receptor antagonist activity, especially tropisetron, for the manufacture of a pharmaceutical composition for...
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7388018 |
4-Piridinylmethylsulphonamide derivatives as fungicidal plant protein agents
Sulfonamides of the formula I
where the substituents are as follows:
R 1 is hydrogen, alkyl, alkoxy, alkenyl or alkynyl; and R 2 , R 3 , R 4 , R 5 are hydrogen, halogen, alkyl, alkoxy or...
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7384954 |
4-substituted imidazoles
Compounds of formula I:
wherein A and R 1 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in...
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7342028 |
Medical use for tachykinin antagonists
The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel...
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7320987 |
6-Alkoxy-pyrido-pyrimidines
The present invention provides compounds of the Formula I:
wherein R 1 is alkyl, cycloalkyl, cycloalkylalkyl, or —CH 2 -alkenyl, X 1 is O, NH, N(alkyl), S or —C(═O), Z is N or CH; and R...
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7314870 |
Compounds, their preparation and use
The present invention relates to novel compounds that are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due...
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7312230 |
Carboxylic acid derivatives as IP antagonists
This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I:
wherein:
R 1 , R 2 , and R 3 are each independently in each...
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7297693 |
Nitrogen-containing heterocyclic compounds and their use as Raf inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac...
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7276520 |
Bicyclic piperidine derivatives as melanocortin-4 receptor agonists
Certain novel bicyclic N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R)....
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7273885 |
Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life...
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7273865 |
Thiazolopyridine
The present invention relates to compounds of formula I
wherein R 1 and R 2 are described hereinbelow. These compounds have high affinity to A 2A receptors and good selectivity to A 1 and A...
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7241773 |
3-quinuclidinyl heteroatom bridged biaryl derivatives
Compounds of formula:
or pharmaceutically acceptable salts, esters, amides, or prodrugs thereof, wherein: A and G are each independently N or N + —O − ; m and n are each independently 0, 1,...
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7230009 |
Pyridoxal analogues and methods of treatment
Pyridoxal analogues can be useful for treating B 6 deficiency and related diseases; cardiovascular and related diseases; melanoma and related diseases; and symptoms thereof. One such analogue is a...
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7214701 |
Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising
(a) compounds of the formula (I)
in which W, X, Y, Z, A, B, D and G...
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7205328 |
Oxindoles with anti-HIV activity
The present invention relates to inhibition of viruses, e.g., HIV using oxindoles and compounds related to oxindoles. The invention further relates to methods for identifying and using agents,...
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RE39558 |
5-Substituted-6-cyclic-5,6,7,8-tetrahydronaphthalen 2-ol compounds which are useful for treating osteoporosis
Compounds of this formula
are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.
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7176198 |
1H-pyrazole and 1H-pyrrole-azabicyclic compounds for the treatment of disease
The invention provides compounds of Formula I:
wherein Azabicyclo is
where the variables have the definitions discussed herein. These compounds may be in the form of pharmaceutical salts or...
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