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6596728 |
Substituted 1,3-diaryl-2-pyrid-2-yl-3-(pyrid-2-ylamino)propanol derivatives, process for their preparation, pharmaceuticals comprising these compounds and their use
Substituted 1,3-diaryl-2-pyridin-2-yl-3-(pyridin-2-ylamino)propanol derivatives of the formula (I), and salts thereof, in which the radicals have the meanings given in the specification, and...
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6579880 |
Isoxazoles and oxadiazoles as anti-inflammatory inhibitors of IL-8
The invention relates to isoxazole and oxadiazole compounds of Formulae I and II, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds...
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6579871 |
Methods of using novel compounds as neuro-protective agents
This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
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6562843 |
Substituted 3-pyridyl-4-arylpyrroles, and related therapeutic and prophylactic methods
This invention provides novel substituted 3-pyridyl-4-arylpyrroles, and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by reducing TNF-α production and/or...
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6548519 |
Pyridoxine and pyridoxal analogues: novel uses
The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions...
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6541491 |
4-mercaptopyrrolidine derivatives as farnesyl transferase inhibitors
Pharmaceutical compositions comprising an inhibitor of ras farnesylation of formula (I) wherein, R 1 is for example H and further values as defined in the specification; R 2 is for example H and...
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6537991 |
Method of treating a peripheral neuropathic pain
The invention provides methods for treating and preventing neuropathic pain which comprise the administration of an effective amount of an antagonist of the pain-enhancing effects of E-type...
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6528503 |
Thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g....
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6525076 |
Selective factor Xa inhibitors
Novel 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 treating...
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6521643 |
Pyridine compounds and their pharmaceutical use
A compound of formula (I) wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically...
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6518267 |
Protease inhibitors
The present invention provides bis-aminomethyl carbonyl protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K,...
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6514998 |
2-&lsqb 1′, 2′, 4′-triazol-3′-yloxymethlene&rsqb anilides, their preparation and their use
2-[1′,2′,4′-Triazol-3′-yloxymethylene]anilides of the formula I where the index and the substituents have the following meanings: n is 0, 1, 2, 3 or 4; X is a direct bond, O or NR a ; R...
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6514997 |
Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
Compounds of the formula: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the picornaviral 3C protease. Also...
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6506747 |
Substituted 1-(4-aminophenyl)pyrazoles and their use as anti-inflammatory agents
1-(4-aminophenyl)pyrazoles optionally substituted on the 3- and 5-positions of the pyrazole ring and on the amino group at the 4-position of the phenyl ring are disclosed and described, which...
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6500847 |
Inhibition of matrix metalloproteases by substitued biaryl oxobutyric acids
Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the...
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6495578 |
Sulfonamide derivatives having oxadiazole rings
Sulfonamide derivatives having a matrix metalloprotease inhibiting effect, which are compounds represented by general formula (I), optical isomers of the same, pharmaceutically acceptable salts of...
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6492397 |
N-arylheteroarylalkyl imidazol-2-one compounds for treatment of arteriosclerosis
A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of arteriosclerosis. Compounds of particular interest are angiotensin II antagonists of Formula I: ...
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6482833 |
Immunotherapeutic anti-cancer pharmaceutical compositions
There is disclosed a class of pharmaceutical compositions useful for the treatment of cancer, particularly solid tumors, and having a mechanism of action as spermine antagonists. The present...
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6479520 |
Method of treating a patient having precancerous lesions with phenyl pyridinone derivatives
Derivatives of phenyl pyridinone are useful for the treatment of patients having precancerous lesions. These compounds are also useful to inhibit the growth of neoplastic cells.
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6476042 |
Combination therapy for the treatment of migraine
The present invention relates to a method of treating migraine in a mammal, including a human, by administering to the mammal a 5HT 1 receptor agonist in combination with caffeine and a...
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6472392 |
Triazole compounds and the use thereof as dopamine-D3 -ligands
Triazole compounds of the following formula: where Ar 1 , A, B and Ar 2 have the meanings given in the description, possess a high affinity for the dopamine D 3 receptor and can therefore be...
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6465493 |
Triarylimidazoles
Compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R 1 , R 2 and R 3 are various substituent groups; and one of X 1 and X 2 is N or CR′, and the other is NR′...
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6465492 |
Heterocyclic compounds
A heterocyclic compound has the following formula (I) wherein Y represents a substituted or unsubstituted ethylene group or a trimethylene group, W represents the group —SO 2 R 1 , X...
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6458805 |
Formulation of sulfonamides for treatment of endothelin-mediated disorders
Formulations of pharmaceutically-acceptable salts of thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides using the...
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6458813 |
Substituted pyridine compounds and methods of use
Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF-α, IL-1β, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain...
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6455560 |
Isoxazoline fibrinogen receptor antagonists
This invention relates to novel isoxazolines of formula (I): or a pharmaceutically acceptable salt form thereof. This invention also relates to novel isoxazolines of formula (I) which are useful...
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6451820 |
Substituted 1-(4-aminophenly)triazoles and their use as anti-inflammatory agents
Compounds of formula I wherein: R 1 is pyridyl optionally substituted with halogen, C 1-4 alkyl, C 1-4 alkenyl, CN, Me 2 N, CO 2 Me, OMe, aryl, heterocyclyl, or R 4 ; R 2 is CF 3 ; halogen;...
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6448238 |
Inhibitors of β-lactamases and uses therefor
The invention provides novel non-β-lactam inhibitors of β-lactamases. In particular, the invention provides such inhibitors which are boronic acids of formula (1) which is set forth in the...
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6441005 |
Oxazolidinone compounds and compositions, and methods of using the same
Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising...
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6432960 |
Squarate derivatives of dihydropyridine NPY antagonists
A series of antagonists of NPY have been synthesized and are comprised of squarate derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). As antagonists of NPY-induced behavior, these...
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6429213 |
Cyclic hydroxamic acids as metalloproteinase inhibitors
The present application de gibes 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 0-2...
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6420395 |
Azacyclooctane and heptane derivatives, their preparation and use in therapy
The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen,...
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6417187 |
1,2,4-triazole based compounds that can be used as insecticides or acaricides and processes
3-(Substituted aryl)-5-{substituted aryl-(alkynyl-aryl)}-[1,2,4]- triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the...
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6417204 |
Pyridoxine AMD pyridoxal analogues: cardiovascular therapeutics
The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions...
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6414003 |
Oxazolone derivatives and their use as anti-helicobacter pylori agents
An anti- Helicobacter pylori agent comprising a compound represented by the formula: wherein A represents an aromatic ring group which may be substituted; R 1 and R 2 , whether identical or...
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6413992 |
3-(substituted pyridyl)-1,2,4-triazole compounds
Compounds of the formula wherein one of X and Y is lower alkyl, haloalkyl, lower alkenyl, lower alkynyl, or alkoxyalkyl; and the other of X and Y is optionally substituted phenyl, pyridyl,...
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6399606 |
Neuroprotective agents and methods related thereto
Neuroprotective agents are disclosed having the following structure: wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Such compounds have utility in the treatment of conditions...
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6399619 |
Pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and n are defined herein) which are useful as modulators of chemokine...
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6391327 |
Pesticidal composition
A pesticidal composition comprising prallethrin and a neonicotinoid compound given in the following formula (1), (2) or (3), as an active ingredient wherein, A represents a 6-chloro-3-pyridyl,...
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6391897 |
Biphenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
This invention provides substituted compounds of the general formulae: wherein B and E are C or N; D, G and W are O, S, or N; or salt forms thereof, and methods and pharmaceutical compositions...
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6380213 |
Compounds useful as neuro-protective agents
This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
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6369084 |
Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment
This invention encompasses the novel compounds of formula A, which are useful in the treatment of prostaglandin mediated diseases, or a pharmaceutically acceptable salt, hydrate or ester...
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6369083 |
2-methoxyimino-2 (pyrinyloxymethyl) phenyl acetamides with polyether derivatives on the pyridine ring
The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl) phenyl acetamide compounds with polyether substituents on the pyridine ring, their use as fungicidal compounds, and their...
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6365607 |
Anticachectic composition
A medicinal composition for the prophylaxis and treatment of cachexia which comprises a compound of the formula: wherein R represents a hydrocarbon group that may be substituted or a...
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6365603 |
Aromatic compounds and pharmaceutical compositions containing them
Compounds of formula I useful for inhibiting the pain enhancing effects of E-type prostaglandins are disclosed wherein A is a ring system in which the —CH(R 3 )N(R 2 )B—R 1 and —OR 4 ...
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6358942 |
Phenyloxazolidinones having a c-c bond 4-8 membered heterocyclic rings
A compound of Formula (I): or pharmaceutical acceptable salts thereof wherein X is NR 1 ; R 1 is H, C 1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R 1 is —(CH 2 ) h...
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6355653 |
Amino-triazolopyridine derivatives
The invention relates to compounds of formula wherein R 1 is a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally...
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6355659 |
4-(4-Chlorophenyl)-1236-tetrahydro-1(1H-124-triazol-1-yl)butty)pyrideine and salts thereof; pharmaceutical compositions and method of treating psychoses utilizing same
Antipsychotic compound 4-(4-chlorophenyl)-1,2,3,6-tetrahydro-1-[4-(1H-1,2,4-triazol
-1-yl) butyl]pyridine, or one of its physiologically acceptable salts, pharmaceutical compositions containing...
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6340697 |
Oxime derivatives and agricultural chemicals containing the same
Various oxime derivatives are provided, which do not cause any chemical damage to plants and which exhibit sufficient effectiveness against various plant diseases. The oxime derivatives are...
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6337394 |
Compounds
There is provided compounds of formula I, wherein R 1 , R 2 , R 3 , R x , Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases,...
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