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7638549 |
Mitotic kinesin inhibitors
The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for...
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7569599 |
Intermediates for the production of optically active cyclopropylamine derivatives and process for the production of the intermediates
A process for producing an optically active compound represented by formula (4), or a salt thereof,
wherein R 1 represents a protecting group.
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7557137 |
Gamma-lactams as beta-secretase inhibitors
There is provided a series of novel substituted gamma-lactams of Formula (I)
wherein R 1 , R 2 , R 3 , R 4 and R 5 are defined herein, their pharmaceutical compositions and methods of use....
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7550448 |
Therapeutic compounds
Disclosed herein is a compound having a structure
or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also...
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7504432 |
Ester derivatives
This invention relates to compounds which exhibit selective muscarinic M 3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of...
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7482475 |
Therapeutic lactams
Disclosed herein is a compound having a structure
Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
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7476747 |
Substituted gamma lactams as therapeutic agents
A compound comprising
or a pharmaceutically acceptable salt, prodrug, or a metabolite thereof is disclosed herein. Y, A, and B are as described herein.
Methods, compositions, and medicaments...
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7423059 |
Pharmaceutically active compounds and methods of use
The present invention relates to certain imine-substituted heterocyclic compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds....
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7419936 |
Optically active 2,5-bisaryl-Δ1-pyrrolines and their use as pest control agents
Novel optically active Δ 1 -pyrrolines of the formula (I)
in which
R 1 , R 2 , R 3 , R 4 , and m are each as defined in the description, a plurality of the processes for preparing these...
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7408071 |
N-aryl pyrrolidine derivatives as beta-secretase inhibitors
There is provided a series of substituted N-aryl pyrrolidine derivatives of Formula (I)
or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R...
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7399773 |
Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid and phenylamide
An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-
pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxy
lic acid phenylamide by a novel...
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7396828 |
PI-3 kinase inhibitor prodrugs
The invention provides prodrugs of inhibitors of PI-3 kinase. The compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.
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7368462 |
Melanin concentrating hormone antagonists
The present invention relates to compounds capable of serving as moderators of human and mammalian appetite and as such provide a means for reducing body mass and controlling obesity.
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7348356 |
Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
Disclosed are compounds of formula (I)
which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is...
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7345082 |
Phosphinic acids
The present invention relates to phosphinic acid derivatives of formula I
wherein R 1 , R 2 , R 3 and R 4 are described hereinabove. These compounds can be used in the treatment or prevention...
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7332516 |
Geminally di-substituted NSAID derivatives as Aβ42 lowering agents
The present invention encompasses compounds of Formula I (I)
or pharmaceutically acceptable salts thereof, wherein A is the base molecule of a propionic acid or acetic acid NSAID, or a...
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7323492 |
7-pyrollyl 9-aminoacyl tetracycline compounds and methods of use thereof
A compound of formula (I):
wherein:
A represents an aromatic 5 membered heterocycle, optionally containing, in addition to the nitrogen atom indicated in formula (I), one to three...
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7323490 |
Pyrrole compounds and uses thereof
The invention provides pyrrole-containing compounds and methods of use thereof. Kits and pharmaceutical compositions comprising the pyrrole compounds of the invention are also provided. The...
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7235580 |
Mitotic kinesin inhibitors
The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for...
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7214701 |
Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising
(a) compounds of the formula (I)
in which W, X, Y, Z, A, B, D and G...
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7199081 |
Aqueous compositions for seed treatment
An aqueous composition suitable for applying fungicides to plant propagation materials is provided, comprising water and a blend of the following components, by weight:
a) 2–10% of a...
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7176229 |
Cyclic AMP-specific phosphodiesterase inhibitors
Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases...
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7144881 |
Arylcyclopropylcarboxylic amides as potassium channel openers
The present invention provides novel arylcyclopropylcarboxylic amides and related derivatives having the general Formula I
wherein R, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as defined...
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7105507 |
Cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and...
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7094431 |
Method of healing skin wounds in mammals and a composition therefor
This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or...
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7074785 |
Δ1-pyrrolines used as pesticides
Novel Δ 1 -pyrrolines of the formula (I)
in which
R 1 , R 2 , R 3 , A, R 4 and m have the meanings given in the description,
a number of processes for preparing these substances, and their...
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7056945 |
Selective inhibition of neuronal nitric oxide synthase
Compositions, prodrugs and methods for inhibiting neural Nitric Oxide Synthase (nNOS). By inhibiting nNOS, the compounds, prodrugs and methods of the presnet invention are useable to treat or...
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7034045 |
Monofluoroalkyl derivatives
The present invention provides certain monofluoroalkyl derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions,...
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7034052 |
7-Amido-isoindolyl compounds and their pharmaceutical uses
The invention encompasses 7-amido-isoindolyl compounds and methods of using these compounds and compositions in mammals for treatment, prevention or management of various diseases and disorders....
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7026440 |
Branched polymers and their conjugates
The present invention is directed to branched reactive water-soluble polymers comprising at least two polymer arms, such as poly(ethylene glycol), attached to a central aliphatic hydrocarbon core...
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6995185 |
Δ1-pyrrolines used as pesticides
Novel Δ 1 -pyrrolines of the formula (I)
in which
Ar 1 , Ar 2 and Q are each as defined in the description, a plurality of processes for preparing these substances and their use for...
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6989088 |
Perfluorocyclicamine, constant boiling composition and process for producing the same
A process for producing a perfluorocyclicamine which includes electrolytically fluorinating a triallylamine in anhydrous liquid hydrogen fluoride. A constant boiling composition and process for...
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6911456 |
Use of estrogen antagonists and estrogen agonists in inhibiting pathological conditions
The present invention provides novel methods of inhibiting pathological conditions related to organ systems which respond to estrogen agonists comprising administering to a mammal in need of such...
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6867236 |
Method of preventing of delaying the onset and progression of Alzheimer's disease and related disorders
The present invention relates, in general, to a method of preventing or delaying the onset of Alzheimer's disease and related neurodegenerative disorders. The invention also relates to a method of...
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6867200 |
(Hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors
The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a...
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6821998 |
Arylamines as inhibitors of chemokine binding to US28
Methods for treating CMV and CMV-related diseases are provided that use compounds having the formula: wherein the subscripts m and n are each independently integers from 1 to 2; and the R groups...
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6806290 |
Stabilized pharmaceutically effective composition and pharmaceutical formulation comprising the same
Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The...
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6780858 |
Antibacterial agents
Hydroxyamidines and related compounds are provided which are suitable as antibacterial agents.
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6680341 |
Stable pharmaceutical formulation comprising a HMG-CoA reductase inhibitor
Atorvastatin and pravastatin may be destabilized by the environmental factors, their degradation may also be accelerated by interactions with other pharmaceutical ingredients, such as fillers,...
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6653337 |
Therapy of auto-immune disease by a photochemotherapeutical method
As a novel photochemotherapeutical method for the treatment or prevention of an auto-immune disease, there is provided a method for treating an auto-immune disease, which comprises administering to...
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6649658 |
(−)-Verbenone derivatives
A description is given here of novel solid and stable derivatives of (−)-verbenone having formula (I) wherein, when X=O Z=H, ═CHAr, ═C(OH)COOEt, ═NOR; Y=H, NH 2 , NH 3 +X 1 −, NHCOAr,...
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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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6630504 |
Phenoxyphenylheterocyclyl derivatives as SSRIs
The invention provides compounds of general formula (I) wherein R 1 is H or C 1 -C 6 alkyl; R 2 and R 3 , together with the interconnecting atoms form a 4 to 8-membered saturated ring containing...
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6608050 |
Lyophilizate of lipid complex of water insoluble porphyrins
The present invention relates to a pharmaceutically acceptable dosage form of water insoluble porphyrins, particularly metal containing porphyrins such as tin porphyrin, which can be complexed with...
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6605634 |
Aryl and heteroaryl substituted fused pyrrole anti-inflammatory agents
The present invention comprises a new class of novel aryl and heteroaryl substituted fused pyrrole compounds useful for the prophylaxis and treatment of diseases or conditions, such as TNF-α,...
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6576632 |
Biaryl compounds useful as anticancer agents
The present invention relates to compounds of formula I and to pharmaceutically acceptable salts, hydrates and prodrugs thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 10 , R 11 , b, m, n, p...
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6548532 |
Indolecarboxylic compounds for treating seborrhea and complications thereof
Indolecarboxylic acid compounds and derivatives thereof are useful for treating seboarhea and the dermatitides associated therewith, especially acne and/or blackheads and/or comedones.
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6548533 |
Ureido substituted pyrrolidines
The invention is directed to physiologically active compounds of formula (I): wherein one of A 1 , A 2 and A 3 represents NR 2 and the others represent C(R 3 )(R 4 ); R 1 represents R 5 Z 1...
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6541507 |
Indolecarboxylic compounds for inducing/stimulating hair growth and/or retarding hair loss
Indolecarboxylic acid compounds and derivatives thereof, notably 4,6-dimethoxyindole-2-carboxylic acid and derivatives thereof, are especially useful for inducing/stimulating mammalian hair growth...
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6534546 |
Aniline derivatives possessing an inhibitory effect of nitric oxide synthase
Compounds represented by the general formula (1): (where R 1 is SR 6 or NR 7 R 8 , where R 6 is typically an alkyl group having 1-6 carbon atoms, R 7 is a hydrogen atom, an alkyl group...
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