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7598422 |
Production of chirally pure amino alcohol intermediates, derivatives thereof, and uses thereof
A method of selectively preparing a chiral 2S-amino alcohol useful in preparation of an amide sulfonated or acylated with alkyl, substituted aryl or substituted heteroaryl is described. The method...
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7560573 |
Process for the preparation of (S)-(-)-N,N-dimethyl-3-(2-thienyl)-3-hydroxypropananine, a duloxetine intermediate
A chiral resolution process for the preparation of (S)-AT-OL, and a process for the racemization of AT-OL are provided.
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7547725 |
Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof
Compounds of Formula (I),
are provided where T is CHO, COR 8 , or C(OH)R 1 R 2 ; R 1 and R 2 are hydrogen, optionally substituted lower alkyl, CF 3 , optionally substituted alkenyl, or...
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7524859 |
(2-carboxamido)(3-amino)thiophene compounds
A method of treatment of hyperproliferative disorders comprises a step of administering an effective amount of a compound represented by
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7482376 |
Conjugated complement cascade inhibitors
The present invention is directed to conjugated complement cascade inhibitors, and a method of treating a patient using a conjugated complement cascade inhibitor.
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7446213 |
Detection of negatively charged polymers using water-soluble, cationic, polythiophene derivatives
Novel methods allowing for the simple optical detection and electrochemical detection of doubled-straded oligonucleotides are disclosed. The methods are rapid, selective and versatile....
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7365196 |
Sulphonamido-substituted bridged bicycloalkyl derivatives
A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of...
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7358375 |
Low molecular weight conjugated nitrogen compounds and devices fabricated using the same
Low molecular weight conjugated nitrogen compounds having linear conjugated chains, and devices fabricated using the conjugated nitrogen compounds as organic semiconductor materials, hole...
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7351825 |
Cyclopropane compounds and pharmaceutical use thereof
The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the...
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RE39530 |
3-amino-3-arylpropan-1-ol-compounds, their preparation and use
3-amino-3-arylpropan-1-ol compounds corresponding to the formula I
in which R 1 to R 5 , A and X have the meanings according to claim 1, and their preparation and use as medicaments.
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7161006 |
Sulphones for inhibition of gamma secretase
The invention provides compounds of formula I:
which are inhibitors of γ-secretase and hence useful in the treatment or prevention of Alzheimer's disease.
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7138530 |
Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such...
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7105545 |
N-p-propargyloxyphenethyl-thioacetic acid amides
The invention relates to N-propargyloxy-phenethyl thioacetic acid amide derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R 1 is...
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7094911 |
Biphenyl and biphenyl-analogous compounds as integrin antagonists
The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of...
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7091219 |
Bis-sulfonamide hydroxyethyl-amino retroviral protease inhibitors
Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease...
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7083928 |
Detection of negatively charged polymers using water-soluble, cationic, polythiophene derivatives
Novel methods allowing for the simple optical and electrochemical detection of double-stranded oligonucleotides are disclosed. The methods are rapid, selective and versatile. Advantageously, they...
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7084170 |
Thiophene-amd thiazolesulfonamides as antineoplastic agents
The present invention provides antineoplastic compounds of the formula:
and antineoplastic methods.
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7026339 |
Inhibitors of HCV NS5B polymerase
The present invention relates to compounds, process for their synthesis, compositions and methods for the treatment and prevention of hepatitis C virus (HCV) infection. In particular, the present...
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7019024 |
Pharmaceutical for treatment of neurological and neuropsychiatric disorders
The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula:
or a pharmaceutically acceptable salt thereof.
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6960688 |
Use of compounds for the elevation of pyruvate dehydrogenase activity
The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said...
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6949563 |
(2-carboxamido)(3-amino)thiophene compounds
Compounds represented by Formula (I):
or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1 is
R2 is
and R3 is C 0-4 alkyl, are useful in the treatment of cancer.
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6949536 |
Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
This invention provides a compound of the formula:
or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially...
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6919369 |
Serine protease inhibitors
Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of...
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6916837 |
Amidino derivatives and anticoagulants and thrombosis therapeutic agents containing them
Amidino derivatives represented by the following general formula (I):
{where X is a group represented by R 1 SO 2 NR 2 — (wherein R 1 represents optionally substituted C 6-14 aryl, etc....
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6890942 |
Acyl sulfonamides as inhibitors of HIV integrase
The present invention relates a series of compounds of Formula I
wherein R 1 , R 2 , R 3 , and B are as defined in the specification. The compounds are useful for the inhibition of HIV...
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6878742 |
Heterocyclic sulfonamide inhibitors of beta amyloid production
Compounds of Formula (I),
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or...
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6878723 |
LTA4 hydrolase inhibitors
The invention concerns compounds inhibiting LTA 4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.
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6800764 |
Process for the synthesis of chirally pure beta-amino-alcohols
A process is provided for preparing chirally pure S-enantiomers of α-amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the formula (R) 2 CH(CH 2 )...
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6768024 |
Triamine derivative melanocortin receptor ligands and methods of using same
The invention provides triamine derivative melanocortin receptor ligands of the formula: wherein R 1 to R 8 and n have the meanings provided herein. The invention further provides methods of...
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6743929 |
Sulfonylalkanoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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6706755 |
Cyclopentane heptan(ene) acyl sulfonamide, 2-alkyl or 2-arylalkyl, or 2-heteroarylalkenyl derivatives as therapeutic agents
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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6686478 |
Thienylsulphonylamino(thio)carbonyl compounds
The invention relates to novel thienylsulphonylamino(thio)carbonyl compounds of the formula (I), in which Q represents oxygen or sulphur, R 1 represents cyano, halogen or in each case...
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6677360 |
Biphenyl and biphenyl-analogous compounds as integrin antagonists
The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of...
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6657070 |
Production of chirally pure α-amino acids and N-sulfonyl α-amino acids
Methods for production of chirally pure α-amino acids and N-sulfonyl α-amino acids are described. An aldehyde and a cyanide salt are reacted with an α-methylbenzylamine to afford product. The...
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6566375 |
Elevation of HDL cholesterol by 4-&lsqb (aminothioxomethyl)-hydrazono&rsqb -N-(substituted)-4-arylbutanamides
Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis. These...
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6562842 |
Protease inhibitors
The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or...
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6545154 |
Method for the production of N-(5-amino-2-cyano-4-fluoro-phenyl)-sulphonamides and new intermediate products
The invention relates to a process for preparing N-(5-amino-2-cyano-4-fluoro-phenyl)-sulphonamides in which, in a first step, 2-amino-4,5-difluoro-benzonitrile is reacted with sulphonyl halides in...
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6509499 |
Nitromethylthiobenzene derivatives as inhibitors of aldose reductase
The invention concerns novel compound of general formula (1) in which: P, T 1 , T 2 , X and n are as defined in claim 1, their tautomeric forms, and their additive salts with pharmaceutically...
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6506780 |
Benzophenones and sulfones as inhibitors of glycine uptake
This invention relates to a series of substituted benzophenone and sulfone compounds of the formula I wherein ring A, Z, Y, R and X are defined as in the specification, that exhibit activity as...
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6465060 |
Tetrahydrothiophene derivatives, and their use in liquid-crystalline mixtures
Tetrahydrothiophene derivatives of the formula (I) R 1 —X—(A 1 —M 1 ) a —(A 2 —M 2 ) b —A 3 —Y—T—Z—R 2 (I) where the symbols and indices have the following meanings, for...
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6451791 |
Amidoaromatic ring sulfonamide hydroxamic acid compounds
An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a...
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6441177 |
Tertiary amines
Tertiary amines of the formula wherein A 1 , A 2 , A 3 , A 4 , M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.
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6433009 |
Sulfonyl urea derivatives and their use in the control of interleukin-1 activity
A compound of the formula wherein R 1 and R 2 are as defined above, useful in the treatment and condition selected from the group consisting of meningitis and salpingitis, septic shock,...
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6391918 |
N-sulphonyl and N-sulphinyl phenylglycinamide
Novel α-amino acid amides of formula (I) as well as possible isomers and mixtures of isomers thereof, wherein the substituents are defined as follows: n is the number zero or one; R 1 is...
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6369273 |
Chemical compounds and their use to elevate pyruvate dehydrogenase activity
The use of a compound of the formula (I): wherein: ring C is phenyl or carbon-linked heteroaryl selected from pyridyl, pyrazinyl, pyrimidinyl and pyridazinyl; and wherein said phenyl or...
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6355673 |
Substituted diaminocarboxylic acids
Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading...
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6350909 |
Methoxymino-phenylacetamide derivatives and their utilization as pesticides
The invention relates to new imides, to a plurality of processes for their preparation and to their use as fungicides.
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6350761 |
Benzenamine derivatives as anti-coagulants
This invention is directed to benzenamine derivatives of formula (I): wherein A, W, m, n, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are defined herein. These compounds are useful as anti-coagulants.
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6342610 |
N-aryl thienyl-, furyl-, and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides,...
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6323315 |
Dolastatin peptides
The present invention provides compounds of the formula ##STR1## where R 1 -R 5 are each, independently, a hydrogen atom or a normal or branched C 1 -C 6 -alkyl group; A is a methionyl,...
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