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8168631 |
3-(4-fluorophenyl)-3-hydroxy-2-amino-propionic acid amides and related compounds having analgesic activity
Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
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8106191 |
Synthetic multimerizing agents
New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic...
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8093266 |
Rho kinase inhibitors
Substituted amide and urea derivatives useful as inhibitors of Rho kinase are described, which inhibitors can be useful in the treatment of various disorders such as cardiovascular diseases,...
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8088763 |
Cyclohexyl-1, 4-diamine compounds
Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical...
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8071625 |
Certain chemical entities, compositions, and methods
Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin...
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8071603 |
Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula...
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7985861 |
Piperidinyl derivatives as modulators of chemokine receptor activity
The present application describes substituted piperidinyl modulators of MIP-1α or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and ...
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7973055 |
Crystalline forms of a biphenyl compound
The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-[2-({3-[2-(4-hydroxybenzylamino)ethylcarbamoyl]benzoyl}met
hylamino)ethyl]piperidin-4-yl ester, and pharmaceutically...
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7943775 |
Small molecules for imaging protein-protein interactions
A tissue is imaged to detect the presence of amyloid deposits or other target proteins prior to their aggregation into plaques, with the assistance of the administration of a labeled bifunctional...
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7932269 |
Sulfonamides as orexin antagonists
The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3 and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful...
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7906556 |
Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors
The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and...
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7884102 |
Substituted piperidine compounds and methods of their use
3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are...
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7872021 |
LXR receptor modulators
Benzenesulfonamide derivative compounds corresponding to the general formula (I): and their pharmaceutically acceptable addition salts; a process for preparation of such compounds; pharmaceutical...
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7872028 |
Diaminopropanol renin inhibitors
Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated. levels of...
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7868009 |
N-hydroxyamide derivatives and use thereof
The present invention is related to N-hydroxyamide derivatives of Formula (I): and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases,...
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7858624 |
Piperidine and morpholine renin inhibitors
Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also...
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7807672 |
Compounds that are ERK inhibitors
Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The...
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7772251 |
N-sulphonylated amino acid derivatives, method for the production and use thereof
The present invention relates to N-sulfonylated amino acid derivatives, where an aryl radical is linked via the sulfonyl group N-terminally to the amino acid and a radical which comprises at least...
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7767623 |
Siliconated phenyl amides derivatives useful as microbiocide
A fungicidal compound of formula (1): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring...
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7754737 |
Diaminoalkane aspartic protease inhibitors
Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases...
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7745441 |
Urokinase inhibitors
New urokinase inhibitors having a triisopropylphenylsulfonyl residue as an Nα-substituent for 3-amidinophenylalanine are provided. The introduction of the triisopropylphenylsulfonyl residue ...
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7737127 |
2-propynyl adenosine analogs having A2A agonist activity and compositions thereof
The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described here.
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7723307 |
Amino acid derivatives and pharmaceutical uses thereof
Novel Amino Acid Derivatives and Pharmaceutical Uses Thereof Provided are novel compounds of Formula I: wherein ‘X’ represents an amino acid group, ‘n’ is an integer between 1 and 4, ‘R1’ re...
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7718673 |
Isonipecotamides for the treatment of integrin-mediated disorders
The invention is directed to novel isonipecotamide derivatives of Formula (I): which are useful in treating integrin-mediated disorders.
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7713979 |
Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention...
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7678826 |
Organic compounds for the treatment of inflammatory or allergic conditions
Compounds of formula (I) in free or pharmaceutically acceptable salt form, where R1, R2, R3, R4, R5, R6, R7, m, n, w, X, and Y have the meanings as indicated in the specification, are useful for...
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7671055 |
Insecticidal 3-(dihaloalkenyl) phenyl derivatives
Certain novel 3-(dihaloalkenyl)phenyl derivatives have unexpected insecticidal activity. These compounds are represented by formula (I), where R through R5, a, b, D, E, G and U are fully described...
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7645774 |
Cannabinoid receptor ligands
There are disclosed compounds of the formula I: or a pharmaceutically acceptable salt of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are...
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7625929 |
Oxophenyl-cyclohexyl-propanolamine derivatives, production and use thereof in therapeutics
The invention relates to the compounds of general formula (I) where R1 represents H, a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl being optionally sub...
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7595401 |
Therapeutic compounds and their use in cancer
The invention relates to compounds of Formula I and their therapeutic uses, wherein substituent A is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carboxylic group,...
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7482365 |
Piperidylcarboxamide derivatives and their use in the treatment of tachykinin-mediated diseases
The present invention relates to piperidine derivatives of formula (I): wherein R, R1, R2, R3, R4, R5, R6, X, Y, m and n are as defined herein; and pharmaceutically acceptable salts and solvates...
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7435851 |
Puleganic amides
The present invention provides substituted puleganic amides and compositions thereof, which are both useful as a topical treatment for skin, such as a repellant for insects and arthropods.
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7425641 |
Carboxylic acid amides, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to carboxylic acid amides of general formula wherein R1 to R5, Ar, m and n are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof, the prodrugs and...
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7390905 |
Piperidine compound and process for preparing the same
The present invention relates to a piperidine compound represented by the formula [I]: wherein Ring A represents an optionally substituted benzene ring, Ring B represents an optionally substituted...
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7381721 |
Substituted piperidine compounds
3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are...
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7378440 |
Substituted benzoylureido-o-benzoylamides, process for their preparation and their use
The invention relates to substituted benzoylureido-o-benzoylamides and to their physiologically tolerated salts and physiologically functional derivatives. The invention relates to compounds of the...
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7361666 |
Heterocyclic analgesic compounds and methods of use thereof
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various...
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7323563 |
Hydroxamic acid derivatives as antibacterials
A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a...
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7309714 |
Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or pre...
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7285568 |
Biaromatic compounds which activate PPARgamma type receptors and cosmetic/pharmaceutical compositions comprised thereof
Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and...
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7262208 |
Hydroxypropyl amides for the treatment of Alzheimer's disease
The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that...
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7259157 |
N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
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7253171 |
Urea derivatives as integrin α4 antagonists
Novel antagonists of ∝4β1 integrin and/or ∝4β7 integrin of the general Formula I: wherein R1, R2, R5, L1, L2, Rb, W and Z are as defined in any one of claims 1 to 13, A represents —CH— or a nitroge...
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7247748 |
Amide compounds and methods of using the same
Disclosed is a compound having the formula (I) pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as...
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7247730 |
Process for the preparation of dexmethylphenidate hydrochloride
The present invention provides a new and efficient process for the preparation of the dexmethylphenidate hydrochloride with high optical purity, the process comprising: (a) reacting a solution of...
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7241757 |
Amidino derivatives and their use as thrombin inhibitors
There is provided compounds of formula I wherein R1, Rx, Y, Ry, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as...
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7238709 |
Therapeutic carbamates
This invention relates to hindered carbamate derivatives that are muscarinic receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.
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7132539 |
Melanocortin receptor ligands
The present invention relates to compounds which comprise a nitrogen-containing ring scaffold substituted by an R1 alkyl units selected from the group consisting of C1–C12 linear or branched a...
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7030115 |
N-sulfonylurea apoptosis promoters
Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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7012084 |
Acylated piperidine derivatives as melanocortin-4 receptor agonists
Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor...
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