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7320978 |
Oxazole derivatives, preparation and therapeutic use thereof
This invention relates to compounds of formula (I):
Wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as described herein. The invention further relates to a method for prevention...
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7317010 |
Thieno-pyrrole compounds as antagonists of gonadotropin releasing hormone
The invention relates to a group of novel thieno-pyrrole compounds of Formula (I), wherein: R 1 , R 2 , R 4 , R 5 , R 6 , R 6a , R 7 , R 8 , A and B are as defined in the specification, which are...
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7300936 |
α-(N-sulfonamido)acetamide derivatives as β-amyloid inhibitors
There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I)
wherein R, R 1 , R 2 and R 3 are defined herein, which are inhibitors of β-amyloid peptide...
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7297697 |
4-(diarylmethyl)-1-piperazinyl derivatives
A compound of formula I
wherein X, Y, X′ & Y′ are selected from hydrogen, halogen, substituted or unsubstituted alkyl (linear, branched or cyclo), aryl, alkyloxy and haloalkyl group; R...
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7291633 |
6H-oxazolo[4,5-e]indole derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands
Compounds of the formula I in which R 1 , R 2 , R 3 and R 4 are as defined in claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the...
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7279475 |
Fluorinated di-aryl urea compounds
Disclosed are compounds of formula(I):
wherein R 1 , R 2 , W and X of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are...
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7279478 |
Cathepsin cysteine protease inhibitors
This invention relates to class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating...
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7259186 |
Salts of fenofibric acid and pharmaceutical formulations thereof
In one aspect, the present invention relates to a formulation in the form of molecular dispersion comprising i) fenofibric acid, a physiologically acceptable salt or derivative thereof and...
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7250412 |
PH sensitive prodrugs of 2,6-Diisopropylphenol
The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby...
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7232817 |
α- and β-amino acid hydroxyethlamino sulfonyl urea derivatives useful as retroviral protease inhibitors
α- and β-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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7232821 |
(2-((2-alkoxy)-phenyl) -cyclopent-1enyl) aromatic carbo and heterocyclic acid and derivatives
Compounds of formula (I) or a pharmaceutically acceptable derivative thereof:
wherein A, R 1 , R 2 , R x , R 8 , R 9 and n are as defined in the specification, a process for the preparation of...
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7217705 |
Combination of a CB1 receptor antagonist and of a product which activates dopaminergic neurotransmission in the brain, the pharmaceutical compositions comprising them and their use in the treatment of parkinson's disease
The present invention relates to the combination of one or more CB1 antagonist azetidine derivatives and of one or more products which activate dopaminergic neurotransmission in the brain, to the...
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7199158 |
Succinoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula:
wherein R 1 –R 6 , R 7 , R 7′ , R 8 , R 30 –R 34 , X′, Y, Y′, t, x, and n are as defined herein, are...
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7189727 |
Guanidino compounds
Compounds having the general structure III are provided:
where D is N or C; W is selected from
Z 1 , Z 2 , and Z 3 are independently selected from CR 8 and N; and the other variables have...
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7186723 |
Tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to...
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7183284 |
Aminium salts of 1,2,3-triazoles as prodrugs of drugs including antiviral agents
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with new aminium salts...
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7166605 |
Probucol nitro-derivatives
Probucol derivatives and pharmaceutical compositions containing the same to be employed in treatment or prophylaxis of diseases.
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7160887 |
Aromatic amine derivatives, their production and use
Compounds of a formula:
wherein Ring A represents an optionally-substituted aromatic ring; Ring B represents an optionally-substituted cyclic hydrocarbon group; Z represents an...
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7153857 |
Arylpiperazines and arylpiperidines and their use as metalloproteinase inhibiting agents
Compounds of the formula I
useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.
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7148208 |
Pharmaceutical compositions for headache, migraine, nausea and emesis
S-alkylsiothiouronium derivatives such as S-ethylisothiouronium diethylphosphate are used for the treatment of headaches, in particular, migraines, as well as for the prevention or treatment of...
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7141573 |
Polypharmacophoric agents
One aspect of the present invention relates to polypharmacophoric compounds. In certain embodiments, the polyphamacophore compounds comprise individual pharmacophore units selected from the group...
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7122539 |
Nitric esters and nitrate salts of specific drugs
Nitric acid salts with medicines active in the respiratory system pathology treatment.
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7105504 |
Combination of a CB1 receptor antagonist and of a product which activates dopaminergic neurotransmission in the brain, the pharmaceutical compositions comprising them and their use in the treatment of parkinson's disease
The present invention relates to the combination of one or more CB1 antagonist azetidine derivatives and of one or more products which activate dopaminergic neurotransmission in the brain, to the...
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7105540 |
Cholinesterase inhibitors to treat disorders of attention
The present invention provides novel methods of treating disorders of attention or improving attention in humans by administering an effective amount of a cholinesterase inhibitor.
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7094785 |
Method of treating polycythemia vera
The invention is directed to the use of imatinib mesylate for treating polycythemia vera. Imatinib mesylate is surprisingly effective at controlling the symptoms of polycythemia vera and reducing...
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7084144 |
Sulfonyl group containing compounds and their use for the treatment of erectile dysfunction
A compound having the general formula (I):
wherein: X is N or C; R 0 is H, a lower alkyl group, a lower O-alkyl group,
lower alkyl group, a benzyl group, a phenyl group, a heterocyclic...
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7078407 |
4-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them
The present invention relates to 4-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them. More particularly, it relates to 4-hydroxycinnamamide derivatives...
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7074794 |
Proline derivatives and the use thereof as drugs
The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that...
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7071180 |
Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases
The invention relates to compounds of the general formula (I):
wherein
Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO 2 —, —NH—, (ii) a C 1-4...
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7067517 |
Use of compounds 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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7067555 |
Sertraline oral concentrate
The present invention provides an essentially nonaqueous, liquid pharmaceutical concentrate composition for oral administration containing sertraline or a pharmaceutically acceptable salt thereof...
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RE39088 |
Amide compounds and use of the same
An amide compound of the formula (I):
wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R 1 , R 2 , R 3 and R 4 are H,...
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7030110 |
Cyclic oxyguanidine pyrazinones as protease inhibitors
Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I:
wherein R 3 , R 4 , R 5 , W, and A are as set forth in the specification, as well as hydrates,...
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7030111 |
Compounds that abrogate DNA-damage-induced cell cycle G2 checkpoint and/or augment the anti-cancer activity of DNA damaging treatments
The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically,...
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7022707 |
Piperazine derivatives
The present invention is a chemical compound of formula (I)
or a pharmaceutically acceptable salts, solvates and esters thereof, wherein R 1 to R 4 , A 1 , A 2 m and n are as described in the...
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7001907 |
Peptide-containing α-ketoamide cysteine and serine protease inhibitors
This invention relates to peptide-containing α-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.
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6972289 |
Cell division inhibitor and a production method thereof
The present invention relates to a cell division inhibitor comprising various dehydrodiketopiperazines such as dehydrophenylahistin, or analogs thereof as an active ingredient, and a dehydrogenase...
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6969713 |
Piperidine and piperazine acetamide derivatives
The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the...
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6964963 |
Preparation of 4-amino-1-naphthol ethers
The present invention describes a process for preparing 4-amino-1-naphthol ethers which is characterized in that naphthol ethers are first prepared from 1-naphthols, the former are then converted...
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6951860 |
Calcium channel blockers
The invention involves the identification of a family of compounds which block calcium channels. The compounds can be formulated in pharmaceutical carriers and administered to subjects. The...
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6949553 |
Aliphatic compounds, their synthesis method, and utilization of the same
The present invention relates to aliphatic compounds of the formula I, or stereoisomers thereof, or their pharmaceutically acceptable salts:
wherein A represents an optionally substituted CH 3...
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6939881 |
Methods for prevention of ulcers and improving physiological performance
Methods for preventing ulcers, such as gastric ulcers, in a horse about to undergo stress that causes gastric ulcers and prior to occurrence of a gastric ulcer condition in the horse involving...
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6936600 |
Sorbitol dehrydrogenase inhibitors
This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I,
wherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to...
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6916797 |
α-arylethylpiperazine derivatives as neurokinin antagonists
The invention relates to new α-arylethylpiperazine of the formula
wherein
Z represents 0 or S; n′ represents 1 or 2; R 2 represents a hydrogen atom or a methyl group; W, Ar 1 and...
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6916816 |
Phenanthryl piperazinyl dicarboxylic acids as selective NMDA receptor modulating agents
Disclosed are compounds of formula (I) wherein: L is (a) optionally substituted by replacement of one or more of the hydrogen atoms on the phenanthrene ring system by one or more groups other than...
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6887876 |
Benzamidine derivatives
Benzamidine derivatives
are useful delta-opioid receptor modulators, agonists useful as analgesics and antagonists useful as immunosuppressants, antiinflammatory agents, agents for the...
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6887872 |
Propenecarboxylic acid amidoxime derivatives, a process for the preparation thereof, and pharmaceutical compositions containing the same
The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition...
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6887903 |
N-(2-aryl-propionyl)-sulfonamides and pharmaceutical preparations containing them
The compounds of formula 1
wherein R and R 2 are as defined in the disclosure, are useful in the prevention and treatment of tissue damage due to exacerbated recruitment of polymorphonuclear...
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6881738 |
Analogs of choline for neuroprotection and cognitive enhancement in neurodegenerative disorders
The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease,...
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6875765 |
Arylsulfonamide ethers, and methods of use thereof
The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1β converting enzyme and other cysteine proteases in the ICE family are...
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