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7619094 |
Ketoamides with cyclic P4's as inhibitors of NS3 serine protease of hepatitis C virus
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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7615647 |
Process for producing atorvastatin hemicalcium
A process is provided for preparing pharmaceutical grade atorvastatin hemicalcium salt comprising:
(a) deesterifying,
wherein R is an ester protecting group to
...
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7615572 |
Pyrrole and pyrazole DAAO inhibitors
Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia,...
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7612103 |
Pleuromutilin derivatives as antimicrobials
Compounds of formula
wherein
R 1 and R 1 ′ are hydrogen or deuterium, R 2 , R 3 and R 4 are hydrogen or deuterium, R 5 is the residue of an amino acid, X is S or N-ALK,
is...
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7612068 |
Aromatic oxyphenyl and aromatic sulfanylphenyl derivatives
The present invention relates to compounds of formula I wherein the substituents are as defined below. The compounds of formula I are useful for the treatment of diseases such as schizophrenia,...
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7608677 |
Method for preparing polymeric organic iridium compositions
The present invention provides a method for the preparation of polymeric organic iridium complexes useful in electronic devices such as OLEDs. The method provides polymeric organic iridium...
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7605289 |
Benzamide derivatives and uses related thereto
Benzamide derivatives of formula I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described...
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7605177 |
Effects of glycyl-2 methyl prolyl glutamate on neurodegeneration
This invention provides analogs and peptidomimetics of glycyl-L-prolyl-L-glutamic acid (GPE). In particular, this invention relates to GPE analogs and peptidomimetics that are anti-apoptotic,...
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7601753 |
Pyrrolidine melanocortin-specific compounds
Melanocortin receptor-specific pyrrolidine compounds having the structure:
and stereoisomer and pharmaceutically acceptable salts thereof, where R 1 , R 2 , and R 3 are as described in the...
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7601752 |
Pyrrolidine derivatives
The invention is concerned with novel pyrrolidine derivatives of formula (I)
wherein X, Y, R 1 , R 2 and R 3 are as defined in the description and in the claims, as well as physiologically...
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7601742 |
Pyrrolidones with anti-HIV activity
The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using...
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7601360 |
Excitatory amino acid inhibitors for treating sensitive skins
Sensitive human skin/scalp/mucous membrane conditions, for example skin irritation and/or dry patches and/or erythemas and/or dysaesthesic sensations and/or sensations of heating and/or pruritus,...
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7592365 |
Substituted pyrroles, compositions containing same, method for making same and use thereof
The disclosure concerns substituted pyrroles of formula (I):
wherein A, L, Ar, R1, R2, R5, and Ra are as defined in the disclosure, compositions containing the same, methods for making the same...
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7592336 |
Hepatitis C virus inhibitors
Hepatitis C virus inhibitors having the general formula
are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
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7589118 |
IAP BIR domain binding compounds
Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I:
or a salt thereof, in which R 1 , R 2 , R 100 , R 200 , A, A 1 , B, B 1 , BG, n, Q and Q...
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7589076 |
Substituted aryl piperidinylalkynyladenosines as A2AR agonists
A 2A agonists of formula (I) is provided, wherein R 1 , R 2 , R 4 , R 5 , X, Y, Z, n, p, and q are as described herein.
Also provided are compositions comprising and methods of using compounds...
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7585886 |
Pyrrolidine derivative or salt thereof
[Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism. [Means for Resolution] It was found...
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7579369 |
CB 1 receptor inverse agonists
The present invention relates to compounds of formula (I)
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , m and X are as defined in the description and claims, and pharmaceutically acceptable salts...
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7579320 |
IAP BIR domain binding compounds
Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I or II
or a salt thereof, in which R 1 , R 2 , R 3 , R 100 , R 200 , R 300 , A, A 1 , BG, Q...
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7572770 |
Use of an interleukin 1 receptor antagonist and/or pyrrolidinedithiocarbamate for the treatment or prophylaxis of type 2 diabetes
Substances that inhibit the action of the members of the IL-1β/NF-κB pathway can be used for protecting and preserving β-cell mass and function in prediabetic and diabetic type 2 patients....
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7560446 |
Use of angiotensin II receptor antagonists for treating acute myocardial infarction
The invention relates to the use of an angiotensin II receptor antagonist or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of acute MI and for the...
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7557136 |
Pyrrolidine derivatives as oxytocin antagonists
The present invention relates to novel pyrrolidine derivatives of Formula (I), its geometrical isomers, its optically active forms as enantiomers, diastercomers, mixtures of these and its racemate...
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7550487 |
Pyrrolidine-3,4-dicarboxamide derivatives
The invention is concerned with novel pyrrolidine-3,4-dicarboxamide derivatives of formula (I)
wherein R 1 to R 9 and X are as defined in the description and in the claims, as well as...
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7550453 |
2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof
The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.
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7547724 |
IAP BIR domain binding compounds
Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I:
or a salt thereof, in which R 1 , R 2 , R 100 , R 200 , A, A 1 , B, B 1 , BG, n, Q and Q...
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7547722 |
Chemical compounds
The invention relates to a group of novel thieno-pyrrole compounds of Formula (I):
wherein: R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the specification, which are useful as...
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7544714 |
Lipid-amino acid conjugates and methods of use
N-fatty acid-amino acid conjugates and J 2 prostanoid-amino acid conjugates are disclosed along with methods for making such conjugates and methods of using these conjugates in the treatment of...
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7538136 |
Crystalline forms of atorvastatin
The present invention is directed to new crystalline forms of Atorvastatin calcium (2:1), referred to hereinafter as polymorphic Forms X, A, B1, B2, C, D and E. Furthermore, the present invention...
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7538128 |
Dipeptidyl peptidase IV inhibitors, process for their preparation and compositions containing them
The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula:
wherein X, Y, a, R 1 , and R 2 are as defined herein.
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7534810 |
Salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β, δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid
Novel salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylet
hyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptano
ic acid characterized by their X-ray powder diffraction...
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7514571 |
Bicyclo derivative
A novel bicyclo derivative represented by the following general formula (1), or a pharmaceutically acceptable salt thereof, acts as an effective DPP-IV inhibitor:
One example is...
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RE40667 |
[R-(R*R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid, its lactone form and salts thereof
[R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-((1-methyle
thyl)-3-phenyl-4-[(phenylamino)-carbonyl)]-1H-pyrrole-1-hept
anoic acid or...
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7495016 |
Pyrrolidones with anti-HIV activity
The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using...
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7488750 |
Crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms
The present invention provides novel forms of atorvastatin designated Forms VI, VIII, IX, X, XI and XII and novel processes for their preparation as well as processes for preparing atorvastatin...
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7488747 |
Pyrrole and pyrazole DAAO inhibitors
Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia,...
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7488725 |
Pyrrolidinyl beta-amino amide-based inhibitors of dipeptidyl peptidase IV and methods
Compounds are provided having the formula:
wherein R 1 , R 2 , R 2′ , R 3 , R 3′ , R 4 , R 4′ , R 5 , X, Y and Z are as defined herein.
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7485626 |
Combinations of enzyme inhibitor-containing preparations and the use thereof
The invention comprises a process wherein the DNA synthesis and, thus, the proliferation of mononuclear cells (MNZ) and of T cells as well is inhibited by the simultaneous and combined inhibition...
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7482026 |
Compositions and methods directed towards sore muscles and joints
Chemical formulations and methods for reducing muscle and joint soreness are disclosed. A representative chemical formulation includes compounds such as a selenium-compound, chondroitin sulfate,...
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7462641 |
(2S,4S)-4-fluoro-1-[4-fluoro-beta-(4-fluorophenyl)-L-phenylalanyl]-2-pyrrolidinecarbonitrile p-toluenesulfonic acid salt and anhydrous crystalline forms thereof
The present invention includes anhydrous crystalline forms of (2S,4S)-4-fluoro-1-[4-fluoro-β-(4-fluorophenyl)-L-phenylala
nyl]-2-pyrrolidinecarbonitrile p-toluenesulfonic acid salt.
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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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7459473 |
N-linked sulfonamides of N-heterocyclic carboxylic acids or carboxylic acid isosteres
This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including...
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7459428 |
Method of regulating glucose metabolism, and reagents related thereto
One aspect of the present invention relates to a method for treating Type II diabetes in an animal, comprising conjointly administering to the animal metformin and an inhibitor of...
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7449479 |
Hepatitis C virus inhibitors
Hepatitis C virus inhibitors are disclosed having the general formula:
wherein R 1 , R 2 , R 3 , R′, B, Y and X are described in the description.
Compositions comprising the compounds and...
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7446125 |
Derivatives of nitroproline compounds, processes of manufacture and uses in the treatment of integrin mediated disorders
This invention relates to nitroproline derivative compounds and procedures for their preparation and the preparation of pharmaceutical compositions containing the compounds. The invention also...
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7439257 |
Aryloxyalkylcarbamate-type derivatives, preparation method thereof and use of same in therapeutics
The invention relates to a compound of formula (I):
Wherein m, n, X, Y, R 1 , R 2 , R 3 and R 4 are as defined herein. The invention also relates to the use of same in therapeutics.
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7429613 |
Process for the preparation of atorvastatin and intermediates
A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phe
nylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptano
ic acid, R-substituted ester 9...
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7427619 |
Formulation of amino acids and riboflavin useful to reduce toxic effects of cytotoxic chemotherapy
Pharmaceutical compositions effective in alleviating or reducing the effects of fatigue and weakness associated with cancer and cancer chemotherapy are disclosed. The pharmaceutical compositions of...
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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
R 1 to R 5 , Ar, m and n are defined as in claim 1 , the tautomers, stereoisomers, mixtures thereof,...
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7425576 |
Compounds 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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7423170 |
Anticancer agents based on regulation of protein prenylation
Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is...
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