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7625944 |
Inhibitors of plasma kallikrein
The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease...
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7625896 |
Pyridylsulfonamide derivatives
The present invention relates to the compounds of formula I:
their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of such compounds,...
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7622486 |
Pyridine compounds, process for their preparation and compositions containing them
The present invention provides new heterocyclic compounds, particularly substituted pyridines, methods and compositions for making and using these heterocyclic compounds, and methods for treating a...
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7619096 |
3-Aminopyrrolidines as inhibitors of monoamine uptake
The present invention provides compounds of formula (I)
and pharmaceutically acceptable salts thereof, which are useful for the inhibition of the uptake of one or more physiologically active...
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7601720 |
Nicotinic receptor agonists for the treatment of inflammatory diseases
This invention relates to the use of nicotine receptor agonists for treating inflammatory diseases, including a variety of pulmonary diseases. Such agonists have fewer side effects than other...
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7598275 |
Nicotine in therapeutic angiogenesis and vasculogenesis
Methods are provided for induction of angiogenesis by administration of nicotine or other nicotine receptor agonist. Induction of angiogenesis by the methods of the invention can be used in...
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7598274 |
Pyrrole derivatives
Compounds of the formula (I), in which X, Y, Z and Ar have the meanings indicated in claim 1 , are inhibitors of Raf kinase and can be employed, inter alia, for the treatment of tumours
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7592358 |
Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
Alkyne compounds having MCH-receptor antagonistic activity, which are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly...
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7579355 |
Inhibitors of Akt activity
The present invention is directed to compounds which contain a substituted pyridine moeity which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to...
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7557127 |
HDAC inhibitor
Compounds having the formula (I):
wherein
R 1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl,...
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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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7550481 |
Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease
The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which...
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7547712 |
Methods for decreasing the toxic effects of nicotine on fetuses in pregnant women
The present invention relates methods for reducing the adverse effects of nicotine. This application describes the use of nicotine carrier conjugates in decreasing the toxic effects of nicotine on...
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7547444 |
Methods for controlling fungi and bacteria
The present invention includes compounds of pyridinium salts and methods of their use for agricultural purposes. The present invention also relates to methods of controlling fungi and/or bacteria.
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7494989 |
Pyridine compounds useful as N-type calcium channel antagonists
Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when...
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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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7462612 |
Pyridine inhibitors of ERK2 and uses thereof
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
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7456202 |
Marked maleimide compounds, method for preparing same and use thereof for marking macromolecules
Fluorine-18-labelled maleimide compounds of general formula (I):
in which:
m represents an integer from 0 to 10; n represents an integer from 1 to 10; Y represents a group selected from...
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7456190 |
Compositions useful as protein kinase inhibitors
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
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7452906 |
Pyridine derivatives as Raf kinase 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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7452541 |
Hapten-carrier conjugates and uses thereof
The present invention provides compositions comprising a conjugate of a hapten with a carrier in an ordered and repetitive array, and methods of making such compositions. The conjugates and...
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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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7446106 |
Pyridylfurans and pyrroles as Raf kinase 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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7442702 |
Prostaglandin agonists
This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such...
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7435749 |
Beverage treated with nicotine
The present application is directed to a method for preparing a solution containing processed nicotine and beverages made according to such method. The beverage produced according to this method...
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7432288 |
Pyrrole-2,5-dione derivatives as Liver X receptor modulators
The present invention relates to certain novel compounds of the Formula I
to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X...
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7414055 |
Inhibitors of Akt activity
The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to...
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7407974 |
Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I):
wherein A, B, C, G, and W 1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are...
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7407972 |
Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I):
wherein A, B, C, G, and W 1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are...
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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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7396843 |
5′-carbamoyl-1,1′-biphenyl-4-carboxamide derivatives and their use as p38 kinase inhibitors
Compounds of formula (I):
or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
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7387788 |
Pharmaceutical compositions of nicotine and methods of use thereof
The present invention comprises non occlusive compositions for transdermal delivery of nicotine, and more particularly pharmaceutically acceptable salts thereof, and methods of making same. The...
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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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7358263 |
Fused bicyclic-substituted amines as histamine-3 receptor ligands
Compounds of formula (I)
are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising...
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7354939 |
Pyrrole inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
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7345063 |
Amides, preparation and therapeutic use as modulators of CCR-receptor activity
The invention provides compounds of general formula (I), wherein R 1 , X, Y, n, R 2 , Z 1 , Z 2 , A 1 , A 2 , Q, R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , t and R 16 are as defined in the specification,...
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7312235 |
Benzamide inhibitors of factor Xa
Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian Factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or...
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7312218 |
Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If:
or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic...
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7300934 |
Benzamide nitriles
Compounds of the formula (I)
wherein m, n, A, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as described herein, together with methods for making the compounds and using the compounds for treatment...
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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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7288541 |
Propylcarbamate derivatives as inhibitors of serine and cysteine proteases
The present invention includes ketone derivatives (I) and (II), which are useful as cathepsin K inhibitors. The described invention also includes methods of making such ketone derivatives as well...
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7282510 |
Small molecule inhibitors of rotamase enzyme activity
This invention relates to neurotrophic N-glyoxyl-prolyl ester compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated...
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7279470 |
Compounds and uses thereof for decreasing activity of hormone-sensitive lipase
Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The...
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7276524 |
Pyridyl alkane acid amides as cytostatics and immunosuppressives
The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical...
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7276500 |
Substituted amides, their preparation and use
An amide of the formula I
and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the...
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7262207 |
Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as...
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7259163 |
4-(6-membered)-heteroaryl acyl pyrrolidine derivatives as HCV inhibitors
Novel anti-viral agents of Formula
wherein:
A represents OR 1 , NR 1 R 2 , or R 1 wherein R 1 and R 2 are hydrogen, C 1-6 alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R 1 and...
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7253187 |
Heterocyclic inhibitors of ERK2 and uses thereof
Described herein are compounds that are useful as protein kinase inhibitors having the formula:
wherein Z 1 and Z 2 are each independently nitrogen or CH and Ring A, T m R 1 , QR 2 , U n R 3...
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7247648 |
N-alkyl-4-methyleneamino-3-hydroxy-2-pyridones
Compounds of Formula (I)
are effective in the treatment of a microbial infection.
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7247502 |
Hapten-carrier conjugates for treating and preventing nicotine addiction
Novel hapten-carrier conjugates are capable of inducing the production of antibodies, in vivo, that specifically bind to nicotine. These conjugates comprise a nicotine hapten conjugated to an...
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