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7622497 |
Derivatives of gambogic acid and analogs as activators of caspases and inducers of apoptosis
The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are...
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7615570 |
Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
Compounds having formula (I)
or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein L, A, G, R 1 , R 2 and R 3 are as defined herein. These compounds are...
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7612098 |
Amorphous hydrous esomeprazole magnesium
A hydrate of esomeprazole magnesium in the form of an amorphous solid is provided. Methods of preparation and use of, as well as formulation containing the hydrate of esomeprazole magnesium in the...
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7612094 |
Tri-substituted heteroaryls and methods of making and using the same
Compounds of formula (I) possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic...
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7598273 |
Inhibitors of the gastric H+, K+-ATPase with enhanced therapeutic properties
Chemical syntheses and medical uses of novel inhibitors of the gastric H + , K + -ATPase for the treatment and/or management of duodenal ulcers, heartburn, acid reflux, other conditions mediated by...
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7598236 |
Diazabicyclic central nervous system active agents
Compounds of formula I
pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
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7592357 |
Compounds
Novel Inhibitors of Rho-kinases are disclosed.
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7569688 |
Propane-1, 3-dione derivative
Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione...
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7569591 |
Gyrase inhibitors and uses thereof
The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions...
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7563812 |
Amorphous esomeprazole hydrate
The present invention relates to a novel amorphous form of esomeprazole hydrate, to a process for its preparation and to a pharmaceutical composition containing it. Thus, tetrahydrofuran and water...
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7560472 |
Salts of omeprazole and esomeprazole II
The present invention relates to new salts of the single enantiomers of omeprazole, i.e. salts of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methy
l]sulfinyl]-1H-benzimidazole...
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7557138 |
5-phenoxyalkoxypsoralens and methods for selective inhibition of the voltage gated Kv1.3 potassium channel
Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects,...
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7557129 |
Cyanopyridine derivatives useful in the treatment of cancer and other disorders
This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis...
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7553857 |
S-omeprazole magnesium
The present invention discloses a process for preparing a magnesium salt of S-omeprazole. The S-omeprazole salt preferably has a water content below about 4.8% by weight, a magnesium content of...
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7553856 |
Crystalline form of omeprazole
A novel crystalline form of the substrate known under the chemical name 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sul
finy]-1H-benzimidazole, and having the generic name omeprazole,...
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7553854 |
6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling
Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of...
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7553848 |
Vanilloid receptor ligands and their use in treatments
bis-Bicyclic amides and derivatives thereof and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster...
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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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7531558 |
Carboxamide derivatives
Compounds of formula (I),
or a pharmaceutically acceptable salt or solvate thereof, wherein P, W, X, Y, R 2 , R 3 , r and s are as defined in the specification, processes for preparing...
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7528158 |
Indazolone derivatives useful as 11b-HSD1 inhibitors
Compounds of formula (I)
as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 to R 7 have the significances given in the description and claims can be used in the form...
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7524862 |
Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
Alkyne compounds of formula I
wherein A, B, W, X, Y, Z, R 1 , and R 2 have the meanings given herein, which have MCH-receptor antagonistic activity and are useful for preparing pharmaceutical...
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7517897 |
Derivatives of 6,7-dihydro-5h -imidazo[1,2-a] imidazole-3-sulfonic acid
Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of...
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7517894 |
VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines
VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as...
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7511065 |
Mixed lineage kinase modulators
The present invention provides a compound of the formula: (Formula I); or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of...
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7511056 |
TGF-β inhibitors
The present invention is directed to inhibitors of TGF-β of Formula I:
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7498349 |
Biaryl compounds having anti-infective activity
Aromatic compounds exemplified by exhibit antimicrobial activity.
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7495015 |
Indazole derivatives and methods for using the same
Compounds of the formula I:
or pharmaceutically acceptable salts, solvates or prodrugs thereof,
wherein m, k, B, R 1 , R 2 and R 3 are those defined herein, and compositions comprising the...
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7494983 |
Ophthalmic compositions for treating ocular hypertension
This invention relates to potent potassium channel blocker compounds of structural Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated...
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7491738 |
Pest control agents
There is provided a pest control agent comprising a compound represented by formula (I) as active ingredient.
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7482367 |
Substituted benzimidazoles and methods of their use
New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments,...
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7482344 |
Tricyclic steroid hormone nuclear receptor modulators
The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula I in...
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7482342 |
Indazolecarboxamide derivatives, preparation and use thereof as CDK1, CDK2 and CDK4 inhibitors
Compound corresponding to general formula (I):
in which, R 1 represents a hydrogen or halogen atom, an NH 2 , NHR 2 , NHCOR 2 , NO 2 , CN, CH 2 NH 2 and CH 2 NHR 2 ; or alternatively R 1 ...
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7479500 |
Antidepressant piperidine derivatives of heterocyclefused benzodioxans
Compounds of the Formula:
are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
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7470712 |
Amino-benzazoles as P2Y1 receptor inhibitors
The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y 1 receptor. The invention also provides for various pharmaceutical...
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7446122 |
Substituted indole derivatives
Provided herein are indole derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
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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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7439258 |
Viral polymerase inhibitors
A compound of the formula I:
wherein: X is CH or N; Y is O or S; Z is OH, NH 2 , NMeR 3 , NHR 3 ; OR 3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said...
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7427414 |
Modified release oral dosage form using co-polymer of polyvinyl acetate
Once a day modified release oral dosage form comprising of granules or pellets which are either compressed into tablet or filled inside the capsule, wherein the pellet has a core of active...
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7423054 |
Therapeutic pyrazolo[3,4-b]pyridines and indazoles
The present invention provides for compounds of Formula I:
wherein R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X, and L have any of the values defined in the specification, and pharmaceutically...
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7411070 |
Form of S-omeprazole
The present invention relates to a novel form of the (−)-enantiomer of 5-methoxy-2[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sul
finyl]-1H-benzimidazole, i.e. S-omeprazole. More specifically,...
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7410982 |
Propanamine derivatives as serotonin and norepinephrine reuptake inhibitors
There is provided a heretoaryloxy/thio 3-substituted propanamine compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to...
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7410981 |
Prodrugs of imidazole derivatives, for use as proton pump inhibitors in the treatment of e.g. peptic ulcers
An imidazole compound represented by the formula (I), a salt thereof and a compound of the formula (V), which is one of the intermediates thereof. wherein each symbol is as defined in the present...
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7410980 |
Crystals of taxane derivative and process for their production
A crystal of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2-benzoyloxy-9,10-[
(1S)-2-(dimethylamino)ethylidenedioxy]-5,20-epoxy-1-hydroxyt
ax-11-en-13-yl...
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7402597 |
Activator of peroxisome proliferator-activated receptor δ
A compound represented by the formula (I) or a salt of the compound, and a PPAR-δ activator which contains the compound or salt as the active ingredient:
(wherein A represents O or S; B 1 ...
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7399772 |
Substituted benzimidazole dosage forms and method of using same
The present invention relates to pharmaceutical preparations comprising substituted benzimidazole proton pump inhibitors. There is provided a liquid or solid pharmaceutical composition consisting...
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7399765 |
Substituted diazabicycloalkane derivatives
Compounds of formula (I)
Z-Ar 1 —Ar 2 (I)
wherein Z is a diazabicyclic...
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7396841 |
Injections
An injectable composition comprises a benzimidazole compound having an antiulcer action and a strong alkali (e.g., an alkali metal hydroxide such as sodium hydroxide) in a proportion of about 1...
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7393867 |
Substituted thienopyrrole carboxylic acid amides, pyrrolothiazole carboxylic acid amides, and related analogs as inhibitors of casein kinase I
The present invention discloses and claims compounds of formula (I) and formula (II),
as inhibitors of human casein kinase Iε and methods for using said compounds for treating central nervous...
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7393866 |
Amide compounds and medications containing the same
The present invention provides to a novel compound having an ACAT inhibiting activity. The present invention relates to compounds represented by formula (I)
wherein represents an...
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7381734 |
Serine protease inhibitors
Compounds of formula (I)
where R 5 , R 6a , each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
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