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7417062 |
Substituted arylamides
Substituted benzamide compounds are provided along with methods for the use of those compounds for treating cancer.
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7402606 |
Derivatives of 1-(oxoaminoacetyl) pentylcarbamate as cathepsin K inhibitors for the treatment of bone loss
Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The...
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7361755 |
Transition-metal-catalyzed process for the conversion of alkenes to sterically hindered substituted n-alkoxyamines
This invention pertains to a novel process for preparing sterically hindered N-substituted alkyloxyamines from alkenes by the transition-metal-catalyzed reaction of a intermediate alkylborane with...
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7361663 |
N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa
This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing...
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7335679 |
Wortmannin analogs and methods of using same
Novel Wortmannin analogs and their use in inhibiting inhibiting PI-3-kinase activity in mammals as well as tumor formation in a subject are described herein.
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7314875 |
Tricyclic aromatic and bis-phenyl sulfinyl derivatives
The present invention provides compounds of the structure:
wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases...
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7304168 |
Photo-caged fluorescent molecules
A class of photo-caged and cell permeable fluorescent molecules having high uncaging cross sections, robust fluorescence enhancement, and flexible chemistry for bioconjugation. Some of the...
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7304081 |
Amido compounds and their use as pharmaceuticals
The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The...
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7271193 |
Inhibitors of cyclin-dependent kinases and their use
The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia),
wherein R 1 , R 2 , R 3 , R 4...
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7247646 |
Benzopyranone compounds, compositions thereof, and methods of treatment therewith
Benzopyranone Compounds having the following structure:
wherein R 1 , R 2 , X, Y and n are as defined herein, are disclosed. The Benzopyranone Compounds are useful for treating or...
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7208491 |
N-monoacylated o-phenylenediamines
Mono-acylated o-phenylendiamines derivatives of formula I
wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone...
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7189758 |
Glucocorticoid mimetics, methods of making them, pharmaceutical formulations, and uses thereof
A compound of Formula (I)
wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such...
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7186722 |
2-heteroaryl-3,4-dihydro-2h-pyrrole derivatives and the use thereof as pesticides
Novel Δ 1 -pyrrolines of the Formula (I)
in which
R 1 , R 2 , R 3 and Het have the meanings given in the description,
a plurality of processes for preparing these compounds and their use...
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7160877 |
Aliphatic nitrogen-containing 5-membered ring compound
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]:
wherein A represents —CH 2 — or —S—, R 1 represents...
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7157489 |
HIV protease inhibitors
Compounds useful for inhibiting HIV protease are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating wild-type HIV and of multidrug-resistant...
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7157454 |
Derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and the pharmaceutical compositions containing same
The invention relates to compounds of formula:
These compounds show affinity for the bradykinin receptors with selectivity towards the B 1 receptors; they may be used for the preparation of...
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7119214 |
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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7112684 |
Compounds and methods for fluorescent labeling
Dye reagents useful in labeling biological materials are provided along with methods for their use.
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7102027 |
Adamantanetricarboxylic acid derivatives
An adamantanetricarboxylic acid derivative is represented by following Formula (1):
wherein X is a hydrogen atom or a hydrocarbon group; and R 1 , R 2 and R 3 may be the same as or different...
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7098202 |
Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such...
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7034051 |
Fused bicyclic carboxamide derivatives and methods of their use
Fused bicyclic carboxamide derivatives are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.
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6989446 |
Process for the preparation of 3-aryl-benzofuranones
Process for the preparation of compounds of formula I
wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula V
wherein the general...
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6989384 |
Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
Compounds of the formula:
where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds,...
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6967216 |
Amino substituted dibenzothiophene derivatives for the treatment of disorders mediated by NP Y5 receptor
Compounds of formula (I):
wherein:
X is a group of formula (A) or (B):
and R 1 , R 2 , R 3 , R 4 , n, x, y and z are as defined within are described.
Processes for their...
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6962942 |
Azacycloalkanone serine protease inhibitors
The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and...
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6951950 |
Quaternary ammonium compounds
The invention features quaternary ammonium compounds of formula I, described herein, and their use in treating asthma, chronic obstructive pulmonary disorder, allergic rhinitis, and infectious...
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6930188 |
Stable hydrate of a muscarinic receptor antagonist
A stable solid hydrate of a muscarinic receptor antagonist is useful in the treatment of irritable bowel syndrome, diverticular disease, oesophageal achalasia, chronic obstructive airways disease,...
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6897211 |
Thienodibenzoazulene compounds as tumor necrosis factor inhibitors
The present invention relates to the dibenzoazulene compounds represented by formula I as well as to their pharmaceutical preparations for the inhibition of tumor necrosis factor alpha (TNF-α) and...
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6881733 |
Serotonergic benzofurans
The present invention provides serotonergic benzofurans of Formula (I): where A, R, R 1 , R 2 , R 3 , and R 4 are as described in the specification.
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6863843 |
Naphthopyran compounds, photoresponsive compositions and lenses
A photochromic [1,2-b] naphthopyran having a fluoro substituent in at least one of the 7-position or the 9-position of the naphthopyran provides a stable photochromic compound with a narrow range...
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6858227 |
Vitamin E conjugates
Vitamin E conjugates, methods for their preparation, and compositions that include the conjugates. The vitamin E conjugates include a tocopherol moiety covalently coupled through a linker moiety to...
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6846817 |
Nicotine receptor ligands
The invention provides nicotine receptor agonists of formula I:
wherein R 1 , x, y, and n have any of the values given in the specification, or a pharmaceutically acceptable salt thereof, as...
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6844336 |
4-fluoroalkyl-2h-benzopyrans with anti-estogenic activity
This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I,
in which
Z is a straight-chain or branched-chain alkyl group with up to 5 carbon atoms that is...
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6835727 |
Cathepsin cysteine protease inhibitors
This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of Cathepsins K and L. These compounds are useful for treating...
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6822101 |
Process for preparing amine-substituted benzofurans
The present invention relates to processes for preparing amine substituted benzofurans, and more particularly 4-(2-{2-[(2R)-2-methyl-1-pyrrolidinyl]ethyl}-1-benzofuran-5-
yl)benzonitrile, and salts...
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6784167 |
17-beta-hydroxysteroid dehydrogenase-II inhibitors
17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula wherein the phenyl group labeled A and the group —C(R 4 )(R 6 )Y are oriented cis to each other; W represents O...
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6750243 |
Amidino derivatives and their use as thrombin inhibitors
There is provided compounds of formula I wherein R 1 , R x , Y, R y , 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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6740649 |
Cyclic hydroxamic acids as inhibitors of matrix metalloproteinases and/or TNF- α converting enzyme (TACE)
The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from...
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6736998 |
Indeno-fused photochromic naphthopyrans
Described are novel reversible photochromic indenonaphthopyran compounds, examples of which are 2H-naphtho[1,2-b]pyrans characterized by having a substituted or unsubstituted indeno group fused at...
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6734206 |
3-oxa-8-azaprostaglandin analogs as agents for lowering intraocular pressure
The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective...
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6716987 |
Derivatives of benzofuran or benzodioxazole compounds
An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R 1 and R 2 independently represent hydrogen, lower alkyl, cyano, —(CH 2 ) n —E 1 —CO—G 1 ...
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6703407 |
Benzofuran compounds, compositions, and methods
The present invention provides novel, reduced benzothiophenes of formula I wherein R is —H, —OH, —O(C 1 -C 4 alkyl), —O—CO—(C 1 -C 6 alkyl), —O—CO—Ar in which Ar is...
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6653479 |
Crystalline form of 6-hydroxy-3-(4-&lsqb 2-(piperidin-1-yl)ethoxy&rsqb phenoxy)-2-(4-methoxyphenyl)benzo&lsqb b&rsqb thiophene hydrochloride
The present invention is directed to a novel crystalline hydrate of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-metho
xyphenyl)benzo[b]thiophene hydrochloride and uses for same,...
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6653328 |
3-benzyl-benzothiophenes
This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzothiophenes which are α-substituted with ether, thioether amino, cyano or halo that are...
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6632833 |
2-(2-methylphenyl)-3,4-dihydro-2H-pyrrole derivatives
The invention relates to novel 2-(2-methylphenyl)-3,4-dihydro-2H-pyrrole derivatives of the formula (I) in which Ar represents substituted phenyl, to a plurality of processes for their...
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6632825 |
Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds,...
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6620838 |
Benzopyrazone compounds, compositions thereof, and methods of treatment therewith
Benzopyranone compounds having the following structure: wherein R 1 , X, Y and n are as defined here, are disclosed. The compounds of formula (I), wherein R 1 is H, can be prepared by...
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6620837 |
Antithrombotic agents
This application relates to novel compounds of formula (I) (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical...
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6610737 |
Non-psychotropic cannabinoids
Novel non-psychotropic cannabinoids are disclosed and pharmaceutical compositions comprising these novel compounds are described for preventing neurotoxicity, neuroinflammation, immune or...
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6608089 |
Derivatives of flavones, xanthones and coumarins
Compounds having the formula (I) Z—OCH 2 —C≡CCH 2 —NRR 1 (I) or a pharmaceutically acceptable salt or solvate thereof wherein Z can represent the formula (1A) or (1B). The compounds...
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