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7390799 |
Apoptosis promoters
Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than...
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7358253 |
Indolylmaleimide derivatives
Provided are compounds of formula (I)
which are useful in the treatment and/or prevention of diseases or disorders mediated by T lymphocytes and/or PKC, e.g. acute or chronic rejection of organ...
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7358249 |
Heterocyclic compounds having inhibitory activity against HIV integrase
A heterocyclic compound of the formula (I):
wherein B 1 is —C(R 2 )═ or —N═; R 1 ′ is H, etc.; one of R 1 and R 2 is -Z 1 -Z 2 -Z 3 -R 5 wherein Z 1 and Z 3 are independently...
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7354924 |
Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
This invention provides Compounds I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl...
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7351708 |
Pyrrolo [2,3-b] pyridine derivatives
The present invention relates to compounds of formula I
wherein R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are...
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7351704 |
Indazole-carboxamide compounds as 5-HT4 receptor agonists
The invention provides novel indazole-carboxamide 5-HT 4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such...
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7348323 |
Pyrrolo [2,3-c] pyridine derivatives
The present invention relates to compounds of formula I
wherein R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are...
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7320985 |
Method for stabilizing arylcarboxylic acid, stabilizer thereof and aqueous solution containing stabilized arylcarboxylic acid
A method for stabilizing an arylcarboxylic acid, which comprises adding a heterocyclic base to the arylcarboxylic acid or a pharmacologically acceptable salt thereof, a stabilizer thereof and an...
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7259165 |
Heterocyclyl-3-sulfonylazaindole or-azaindazole derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
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7247634 |
Rifamycin derivatives effective against drug-resistant microbes
Rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms are claimed in this invention. The inventive rifamycin derivatives are uniquely...
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7238694 |
Rifamycin imino derivatives effective against drug-resistant microbes
The present invention relates to rifamycin 3-iminomethylenyl (—CH═N—) derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. The claimed...
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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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7186716 |
3-Pyrrol-pyridopyrazoles and 3-pyrrolyl-indazoles as novel kinase inhibitors
Compounds of Formula I are useful as mediators of protein kinases and have activity as cell proliferation inhibitors:
where X, R 1 –R 7 and R 9 are as defined herein.
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7176214 |
Imidazo-fused oxazolo[4,5-β]pyridine and imidazo-fused thiazolo[4,5-β]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I),
wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as described herein. The present invention...
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7169787 |
7-azaindoles, use thereof as phosphodiesterase 4 inhibitors and method for producing the same
The invention relates to new 7-azaindoles, their use as inhibitors of phosphodiesterase 4 and to methods for their synthesis.
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7163948 |
Heterocyclic substituted 1,4-dihydri-4ox9-1,8-naphthyridine analogs
The present invention relates to 1,4-dihydro-4-oxo-1,8-napthpyridine analogs of the formula
and pharmaceutically acceptable salts, esters, and prodrugs thereof, wherein A, X, W and Y are...
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7160888 |
[1,8]naphthyridin-2-ones and related compounds for the treatment of schizophrenia
This invention relates to compounds of the formula 1
wherein G, D, A, Z, Q, X, Y, R 1 , and R 4 through R 7 are defined as in the specification, processes for preparing the same and...
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7135469 |
Linear chain substituted monocyclic and bicyclic derivatives as factor Xa inhibitors
The present application describes linear chain substituted monocyclic and bicyclic compounds and derivatives thereof of Formula I:
P 4...
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7125888 |
Tyrosine kinase inhibitors
The present invention relates to imidazopyridine compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of...
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7125887 |
Pyrrolidine modulators of CCR5 chemokine receptor activity
Pyrrolidine compounds of Formula (I), (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6a , R 6b , R 7 and R 8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor...
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7109200 |
Carbamate derivatives, process for producing the same and use thereof
Novel carbamate derivatives which are useful as drugs because of inhibiting activated blood coagulation factor X and thus exerting an anticoagulant effect. Compounds represented by the formula:
...
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7109196 |
1,8 Naphthyridine derivatives and their use to treat diabetes and related disorders
The invention relates generally to naphthyridine derivatives of the formula
wherein one of U, X, Y and Z is nitrogen and the others are C—R, where R is hydrogen or a substituent. More...
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7094779 |
Piperazine oxime dervatives having NK-1 receptor antagonistic activity
The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity. The invention relates to compounds of the general formula (1) wherein:...
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7067515 |
Quinuclidines-substituted-multi-cyclic-heteroaryls for the treatment of disease
The invention provides compounds of Formula I:
where in W is
These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The...
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7045528 |
Benzofused heterozryl amide derivatives of thienopyridines useful as therapeutic agents, pharmaceutical compositions including the same, and methods for their use
The invention relates to compounds represented by the formula I
and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and...
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7041675 |
Heterocyclic compounds and their use as PARP inhibitors
The invention relates to compounds of the formula I
and the tautomeric forms, possible enantiomeric and diasteromeric forms thereof, and prodrugs thereof, and use thereof as PARP inhibitors.
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7026309 |
Fused bicyclic pyridine derivative as tachykinin receptor antagonist
A fused bicyclic pyridine derivative represented by the following general formula (1), or a salt thereof:
wherein the rings A and B are each a benzene ring, which may have 1 to 3...
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6977262 |
Dihydropyrazolopyridine compounds and pharmaceutical use thereof
The present invention provides dihydropyrazolopyridine compounds represented by the formula (I):
wherein each symbol is as defined in the specification, optically active forms thereof, and...
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6969712 |
Benzimidazole derivatives
This invention relates to the compounds represented by a general formula [I]:
[in which A 1 and A 2 represent optionally fluorine-substituted methine or the like; B represents halogen,...
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6969711 |
Cyclic diamine compounds and medicine containing the same
The present invention offers novel cyclic diamine compounds and a pharmaceutical composition containing the same. The present invention relates to a compound represented by the formula (I) or...
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6964971 |
1,6-naphthyridine derivatives and their use to treat diabetes and related disorders
The invention relates generally to naphthyridine derivatives of the formula
wherein one of U, X, Y and Z is nitrogen and the others are C—R, where R is hydrogen or a substituent. More...
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6964961 |
Thiophene derivatives useful as anticancer agents
The invention relates to compounds of the formula 1
or a pharmaceutically acceptable salt and to pharmaceutically acceptable salts and hydrates thereof, wherein X, Y, R 1 , R 2 and R 11 are...
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6964957 |
Fused pyrazole compounds, pharmaceutical compositions, and methods for modulating or inhibiting ERAB or HADH2 activity
Pyrazole compounds represented by the formula:
are described. The pyrazole compounds and pharmaceutical compositions containing them may be used in inhibiting ERAB or HADH2 activity and in...
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6962926 |
Antagonist of MCP-1 function, and compositions and methods of use thereof
Compounds of formula A and formula B:
and their pharmaceutically acceptable salts, compositions comprising them, methods for their use, and their use in the preparation of medicaments. The...
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6921759 |
Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV...
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6911442 |
Quinoline derivatives as antibacterials
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt and/or N-oxide thereof:
corresponding novel medicaments, pharmaceutical compositions and/or...
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6900206 |
Indole, azaindole and related heterocyclic sulfonylureido piperazine derivatives
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with sulfonylureido...
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6900205 |
1,8-Naphthyridine derivatives and their use to treat diabetes and related disorders
The invention relates generally to naphthyridine derivatives of the formula
wherein one of U, X, Y and Z is nitrogen and the others are C—R, where R is hydrogen or a substituent. More...
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6875770 |
Indole derivative having heterocycle and mono- or diazaindole derivative
There is provided a compound represented by the general formula (1):
wherein Het represents an optional substituted heterocylic group A 1 and A 2 each independently represent —CH═, etc.;...
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6861439 |
Treatment of cerebrovascular disease
A method of treating a cerebrovascular disease, particularly stroke, is described. A method of treating a cerebrovascular disease includes administering pyridoxal-5′-phosphate, pyridoxal,...
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6844354 |
Agent for prophylaxis and treatment of interstitial pneumonia and pulmonary fibrosis
An agent for the prophylaxis and treatment of interstitial pneumonia and pulmonary fibrosis, which contains a compound having a Rho kinase inhibitory activity, particularly an agent for the...
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6825201 |
Indole, azaindole and related heterocyclic amidopiperazine derivatives
The invention comprises substituted indole, azaindole and related heterocyclic amidopiperazine derivatives of general Formula I wherein: Q is —may represent a bond; A is selected from the...
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6759428 |
Indole nitriles
Compounds of the formula (I) wherein m, n, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as described herein, together with methods for making the compounds and using the compounds for treatment of...
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6756383 |
Heterocyclic derivatives of quinolinone benimidazoles
Organi c compounds having the structural formulas I, II, and III are provided where the variables have the values described herein and R 1 and R 2 in structure I join together to form a 5 to 7...
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6753331 |
Heterocyclic derivatives which inhibit factor Xa
The invention relates to heterocyclic derivatives of formula (I), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful...
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6747029 |
Dopamine D4 receptor antagonists as treatment for attention deficit-hyperactivity disorder
A method of inhibiting motor hyperactivity in a mammal exhibiting the symptoms of attention deficit-hyperactivity disorder (ADHD) includes administering to a mammal a dopamine D 4 ...
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RE38524 |
Dipeptide derivatives as growth hormone secretagogues
This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone...
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6727254 |
Heteroaryl tropane derivatives as superior ligands for nociceptin receptor ORL-1
Novel compounds of the formula wherein R is optionally substituted heteroaryl or R 1 is H or C 1 -C 6 alkyl; and R 2 and R 3 are —CH 3 , —OCH 3 or halo; or a pharmaceutically...
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6696480 |
Upregulation of type III endothelial cell nitric oxide synthase by agents that disrupt actin cytoskeletal organization
A use for agents that disrupt actin cytoskeletal organization is provided. In the instant invention, agents that disrupt actin cytoskeletal organization are found to upregulate endothelial cell...
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6680328 |
8-azabicyclo&lsqb 3.2.1&rsqb oct-2-ene and -octane derivatives
The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene and -octane derivatives which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their...
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