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6387902 |
Phenazine compounds, methods and pharmaceutical compositions for inhibiting PARP
This invention relates to compounds, pharmaceutical compositions, and methods of using compounds of the formula: wherein R 1 -R 9 and Z are independently. hydrogen, hydroxy, halo, haloalkyl,...
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6387896 |
Bicyclic oxazolidinones as antibacterial agents
The present invention provides compounds of formula I useful as antimicrobial agents wherein W, X, Y, R 1 , R 2 and n are as defined in thereof.
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6380235 |
Benzimidazolones and analogues
The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR 4 ; B...
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6380193 |
Fused tricyclic compounds, methods and compositions for inhibiting PARP activity
A compound of formula I: or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof.
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6380195 |
Method of treating heart failure with endothelin antagonists
A composition for preventing and/or treating heart failure and ventricular dysfunction in a warm blooded animal comprising a therapeutically effective amount of an endothelin antagonist of the...
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6380209 |
4-(4-piperidylmethylamino) substituted heteroaryl fused pyridines: GABA brain receptor ligands
Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: R is hydrogen, alkyl, or(un)substituted alkoxy or amino; and W is (un)substituted...
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6380267 |
Composition and method for decreasing neurologic symptomatology
A method of decreasing the signs or symptomatology in a patient with a neurologic condition or disease, or in a patient due to effects of exposure to an exogenous substance, such as a...
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6376490 |
Quinoxalinediones
The invention provides compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 5-membered ring heteroaryl group containing 3 or 4 nitrogen heteroatoms which is...
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6372752 |
Inha inhibitors and methods of use thereof
The invention relates to compounds which inhibit the Mycobacterial enoyl-ACP reductase required for cell wall biosynthesis. The invention also relates to pharmaceutical compositions comprising...
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6369057 |
Quinoxalines, processes for their preparation and their use
Compounds of the formula I or Ia in which n and the substituents R 1 , R 5 and x have the meaning mentioned have an antiviral activity.
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6369058 |
Brain delivery of folic acid for the prevention of alzheimer's disease and stroke
This invention provides a method of rapidly and reliably delivering folic acid, alone or in combination with other compounds, to the systemic circulation by administration via the nasal route to...
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RE37650 |
Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
This invention relates to the treatment of intimation in a patient suffering from such disorder. More specifically, the invention relates to mono- and/or bicyclic aryl or heteroaryl quinazoline...
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6365578 |
Drug cominbations containing AZT
Combinations of 3′-azido-3′-deoxythymidine (AZT) with 5-fluorouracil (FUra) or its precursor 5-fluoro-2′-deoxyuridine (FUDR) or methoxtrexate (MTX) exhibit increased cytotoxicity and...
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6365199 |
Hair growth stimulant
A hair growth formulation. The two basic main ingredients are castor oil and a special lemon extract. The special lemon extract is made from fresh lemon peel. The peel, including the bioflavonoids...
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6358953 |
Pterin antineoplastic agents
Disclosed are novel metal pterin and pterin analog complexes and compositions useful as antineoplastic and antiviral agents.
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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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6355614 |
Cyclic boroproline compounds
Substantially pure preparations of cyclic boroProline compounds that bind, in cyclic or linear form, to CD26 are provided. Methods for using the cyclic compounds to stimulate the activation and/or...
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6353010 |
Bicyclic aryl carboxamides and their therapeutic use
Compounds of the formula (i) have therapeutic utility via inhibition of TNF or phosphodiesterase.
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6350769 |
Gaba alpha receptors mediate inhibition of T cell responses
The present invention provides new methods for modulating immune responses. The methods are based on the discovery that GABA A receptors are present on peripheral lymphocytes. Thus, GABA agonists...
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6348461 |
6,7-asymmetrically disubstituted quinoxalinecarboxylic acid derivatives, addition salts thereof, and processes for the preparation of both
The present invention provides 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid compounds and their addition salts, and processes for preparing them, which have antagonism against...
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6348485 |
Method for treating or preventing sleep disorders
The present invention provides a pharmaceutical composition for treating or preventing sleep disorders which comprises (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethy
l]propionamide in...
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6348464 |
Pyrrolecarbonylimino derivatives as naaladase inhibitors
The present invention relates to pharmaceutical compositions and methods of using pyrrolecarbonylimino derivatives to inhibit N-Acetylated α-Linked Acidic Dipeptidase (NAALADase) enzyme activity,...
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6340682 |
Diamide compound and drugs containing the same
The present invention provides diamide derivatives represented by the following general formula (1): wherein A is a phenyl group or the like, which may be substituted, B is —CH═CH—,...
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6333326 |
Quinoxalinediones
This invention relates to 2,3(1H,4H)-quinoxalinedione derivatives which are selective antagonists of N-methyl-D-aspartate receptors. More particularly, this invention relates to...
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6329369 |
Methods of treating pain and other conditions
Methods of treating glaucoma or elevated pressure and other diseases with reduced side effects by treating a mammal in need thereof an agonist of the alpha 2B or alpha 2B/2C adrenergic receptor(s)....
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6329342 |
Treatment of congestive heart failure with growth hormone secretagogues
The present invention is directed to methods for the modulation of cardiac function which comprise the administration of certain compounds, as defined herein, having growth hormone secretagogue...
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6323229 |
N-acyl and N-aroyl aralkylamides
A compound of the formula ##STR1## wherein m, R 1 , R 2 , R 3 , R 4 , R 5 and X are as defined, useful in treating or preventing migraine, depression and other disorders for which a 5-HT 1 ...
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6323204 |
Methods for using (2-imidazolin-2-ylamino) quinoxaline derivatives
A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those...
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6323203 |
Composition and method for treating diabetes
A pharmaceutical composition for treating diabetes, contains more than 600 mg of a compound of formula (I): ##STR1## where Y is O; R is NHCONR 4 R 5 ; or NC(NR 4 R 5 ) 2 . Also, another...
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6322821 |
Veterinary pharmaceutical composition
A composition for preventing and treating milk fever in freshening cows, and a method of administering the composition. The basic composition is a mixture of water, calcium chloride, propylene...
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6323205 |
Combinations of 10-propargyl-10-deazaaminopterin and taxols and methods of using same in the treatment of tumors
Preliminary clinical studies in humans have now been done which show both the efficacy of 10-propargyl-10dAM and a preferred dosage schedule for such treatments. In addition, it has now been...
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6319925 |
O-benzyl oxime ether derivatives and their use in crop protection compositions
##STR1## Oxime ethers of formula (I) in which a) X is an N atom and Y is an oxygen atom or NH, or b) X is CH and Y is an oxygen atom, in which furthermore R 1 is C 1 -C 4 alkyl; R 2 is...
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6319926 |
Optically active 5H-pyrrolo[3, 4-B]pyrazine derivative, its preparation and pharmaceutical compositions containing it
Dextrorotatory isomer of 6-(5-chloro-2-pyridyl)-5[(4-methyl-1-piperazinyl)carbonyloxy
]-7-oxo-6,7-di hydro-5H-pyrrolo[3,4-b]pyrazine, its preparation and pharmaceutical compositions containing it...
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6316444 |
SRC kinase inhibitor compounds
Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same,...
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6310039 |
Antineoplastic conjugates of transferrin, albumin and polyethylene glycol
Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at...
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6300329 |
Pharmaceutical agents for the treatment of Parkinson's disease, ADHD and microadenomas
The present invention is directed to the use of certain pyrido[1,2-a]-pyrazine derivatives, also described as bis-azabicyclic compounds and defined by the formula (I) herein, in the treatment of...
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6300342 |
Antithrombotic phenylalkyl derivatives
Antithrombotic phenylalkyl derivatives of the formula ##STR1## Exemplary compounds are: (a) 1-[3-(4-amidino-phenyl)propionyl]-6-(4-fluoro-phenylsulphona
mido)-1,2,3,4- tetrahydro-quinoline, ...
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6297244 |
Stable drug composition
A stabilized pharmaceutical composition comprising (R)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2
-a]pyrazine-4- spiro-3'-pyrrolidine-1,2',3,5'-tetrone (hereinafter, referred to as...
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6297224 |
Method for treatment, preventing and reduction of elevated serum metabolite levels
A method for orally administering vitamin preparations is described which combine vitamin B 12 (B 12 , cobalamin) and folic acid (folate), with and without pyridoxine (B 6 ), for preventing and...
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6288065 |
Quinoxaline-carboxylic acid derivatives
The disclosure relates to quinoxaline derivates of Formula I ##STR1## wherein R 1 , R 4 , R 5 , R 6 , R 7 and R 8 are defined in the disclosure, as well as their production and use in...
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6284757 |
Pyrrolo[1,2-a]pyrazine derivatives as 5HT1A ligands
This invention relates to the use of compounds of formula I ##STR1## wherein R 1 , R 2 , R 3 , X, m and n are defined as in the specification, and their pharmaceutically acceptable salts, for...
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6277849 |
N-sulphonyl and N-sulphinyl amino acid amides as microbiocides
The invention relates to novel pesticidally active compounds of the general formula I ##STR1## as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and ...
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6277850 |
Pyrrolyl quinoxalindiones their production and use as AMPA receptor antagonists
Pyrrolylquinoxalinediones of the formula I ##STR1## and their tautomeric and isomeric forms, and their physiologically tolerated salts are described, where the variables have the following meaning:...
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6274570 |
Pesticidal compositions
A liquid pesticidal composition, which is substantially free of water, comprising a hydrophobic pesticide or mixture of pesticides dissolved in an organic solvent and comprising as surfactants (a)...
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6274581 |
Blocking induction of tetrahydrobiopterin to block induction of nitric oxide synthesis
Guanosine triphosphate pathway tetrahydrobiopterin synthesis antagonist and/or pterin salvage pathway tetrahydrobiopterin synthesis antagonist are administered to inhibit nitric oxide synthesis...
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6271264 |
Polymers containing spirobicyclic ammonium moieties as bile acid sequestrants
The present invention relates to a method for sequestering bile acids in a patient and to particular polymers for use in the method. The method comprises administering a therapeutically effective...
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6271233 |
Method for treating ocular neovascular diseases
The invention relates to the use of certain phthalazines in the preparation of medicaments for the treatment of ocular neovascularization.
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6271232 |
Collagenase-1 and stromelysin-1 inhibitors, pharmaceutical compositions comprising same and methods of their use
Novel inhibitors of metalloproteases, in particular collagenase-1 and stromelysin-1, are disclosed. Such compounds are useful in pharmaceutical compositions and methods for treating or controlling...
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6271231 |
Pharmaceutically active compounds
The present invention provides optionally substituted and/or annulated compounds of formula (I) ##STR1## wherein X, Y, Z and A is each independently carbon or nitrogen, and at least two of X, Y, Z...
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6268366 |
Amide derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists
A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the...
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