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6933304 |
Heteroarylalkanoic acids as integrin receptor antagonists
The present invention relates to a class of compounds represented by the Formula I
or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the...
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6933305 |
Amide compounds and use thereof
The present invention relates to an amide compound of the formula
wherein R 1 is a hydrogen and the like, R 2 is a hydrogen and the like, X is SO 2 and the like, Y is the formula (III) and...
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6930115 |
Antitumor effect potentiators
When used concurrently with an antitumor agent, a compound having a Rho kinase inhibitory activity, such as (R)-(+)-N-(4-pyridyl)-4-(1-aminoethyl)benzamide, reinforces an antitumor effect of the...
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6927226 |
Antidepressant azaheterocyclymethyl derivatives of 7,8-dihydro-3H-6,9-dioxa-1,3-diazacyclopenta[a]naphthalene
Compounds of the formula:
are useful for the treatment of depression and other diseases such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety...
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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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6919352 |
Pyrazolopyridinyl pyridine and pyrimidine therapeutic compounds
The present invention provides compounds of formula (I):
wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and...
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6916826 |
Substituted imidazo[1,2-a]pyridine derivatives
The present invention is a series of novel compounds of formula I and a method of treatment or prevention of a mGluR5 receptor mediated disease by administering an therapeutically effective amount...
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6916810 |
αν integrin receptor antagonists
The present invention relates to cyclic urea derivatives, their synthesis, and their use as αv integrinreceptor antagonists. More particularly, the compounds of the present invention are...
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6908930 |
4-substituted 7-AZA-indolin-2-ones and their use as protein kinase inhibitors
This invention relates to 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors. Particular 4-substituted 7-aza-indolin-2-ones disclosed herein are of Formula 1
and...
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6903112 |
Heterocyclylindazole and -azaindazole compounds as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
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6887881 |
Bispidine compounds useful in the treatment of cardiac arrythmias
There is provided compounds of formula I,
wherein R 1 , R 2 , R 3 , R 4 , R 5a , R 5b , R 6 , X, A, B and D have meanings given in the description, which are useful in the prophylaxis and in...
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6881736 |
Vitronectin receptor antagonists
Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis:
wherein
R 1 is Het or Ar R 2 is
or a...
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6878714 |
Substituted alkylamine derivatives and methods of use
Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically...
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6875761 |
Certain 1,3-disubstituted isoquinoline derivatives
Condensed pyridine compounds represented by formula (I):
wherein: R 1 and R 3 are, independently, hydrogen, lower alkyl, or lower alkoxy; R 2 represent an amino substituent; ring A is a...
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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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6872731 |
Imidazo-pyridine derivatives as ligands for GABA receptors
A class of 3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or...
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6872730 |
Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists
The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (αv) integrins, for example α v β 3 and α v β 5 integrins, their...
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6869945 |
Pyrrolyl-and imidazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
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6867208 |
Vitronectin receptor antagonists, their preparation and their use
The present invention relates to compounds of the formula I
A—B—D—E—F—G (I)
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6867217 |
Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods...
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6858613 |
Fused bicyclic-N-bridged-heteroaromatic carboxamides for the treatment of disease
The invention provides compounds of Formula I:
These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful...
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6855721 |
Methods and compositions for alleviating stuttering
Methods of treating stuttering include treating people with gamma-aminobutyric acid (GABA) receptor modulators, including cyclopyrrolones. A second active agent may be used with GABA receptor...
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6852739 |
Methods using proton pump inhibitors and nitric oxide donors
The present invention describes novel nitrosated and/or nitrosylated proton pump inhibitor compounds, and novel compositions comprising at least one proton pump inhibitor compound that is...
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6852721 |
Pharmaceutical compositions and methods for use
The present invention relates to diazabicyclic compounds, preferably to N-aryl diazabicyclic compounds. Of particular interest are 2-pyridinyl diazabicyclic compounds, such as...
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6852753 |
Alkyl/aryl hydroxy or keto thiepine compounds as inhibitors of apical sodium co-dependent bile acid transport (ASBT) and taurocholate uptake
Thiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as...
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6849644 |
Isoquinoline derivatives useful in the treatment of CNS disorders
The invention relates to novel tetrahydroquinoline compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of...
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6849622 |
Aliphatic nitrogenous five-membered ring compounds
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]:
wherein
A represents —CH 2 — or —S—, R 1 ...
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6849642 |
Bicyclic imidazo-3-yl-amine derivatives substituted on the 6-membered ring
Bicyclic imidazo-3-yl-amine derivatives substituted on the 6-membered ring, and pharmaceutical compositions containing these compounds, useful, inter alia, as analgesics.
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6849641 |
Azaindole tyrosine kinase inhibitors
The present invention relates to novel 3-hetero-arylideneazaindolin-2-one compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein...
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6846833 |
Vitronectin receptor antagonist bicyclic compounds, preparation method and compositions containing same
Compounds of formula (1):
wherein:
G represents an optionally substituted phenyl or optionally substituted heterocycle, G 1 and G 2 being N or C, T 1 represents —CH 2 —CH 2 —,...
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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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6844342 |
Heterocyclic substituted 2-methyl-benzimidazole antiviral agents
The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides...
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6828330 |
Quinuclidine-substituted hetero-bicyclic aromatic compounds for the treatment of disease
The invention provides compounds of Formula I: wherein W 0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric...
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6818643 |
Neurotrophic bicyclic diamides
The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel bicyclic diamide compounds that are neuroprotective...
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6818632 |
3-(anilinomethylene)oxindoles
Compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims, exhibit protein tyrosine kinase and protein serin/threonine kinase...
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6815440 |
Cyclic and heterocyclic N-substituted α-iminohydroxamic and -carboxylic acids
Cyclic and heterocyclic N-substituted α-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course...
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6815438 |
Heteroaryl-diazabicycloalkanes
The present invention relates to novel heteroaryl-diazabicycloalkanes which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the...
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6815451 |
1,2,3,4-Tetrahydroisoquinolines derivatives as urotensin II receptor antagonists
The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions....
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6806256 |
Taste masked liquid pharmaceutical compositions
This invention is directed to a taste masked liquid pharmaceutical composition comprising a pharmaceutically active agent and a taste masking composition. In particular, the taste masking...
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6800639 |
Pharmaceutical combination for the treatment of cancer
In accordance with the present invention there is provided a pharmaceutical combination useful for the treatment of cancer comprising at least one active compound of formula (I): and at least...
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6780874 |
Enamine derivatives
Enamine derivatives of formula (1) are described: wherein R 1 is a group Ar 1 L 2 Ar 2 Alk- in, which Ar 1 is an aromatic or heteroaromatic group, L 2 is a covalent bond or a linker atom or...
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6780887 |
Anti-ischemic compounds
The present invention is related to a compound of formula (I), salts and pro-drugs of the compound (I) and methods for treating and/or preventing partial or total ischemia, methods for treating...
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6777404 |
Use of corticotropin releasing factor antagonists and related compositions
The present invention relates to compositions and methods of achieving a therapeutic effect including, the treatment or prevention of Syndrome X in an animal, preferably a mammal including a human...
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6762192 |
Tetrahydronaphthyridinyl-carboxamides having anti-convulsant activity
Compounds of formula (I) and pharmaceutically acceptable salts and solvates: where R 1 is hydrogen, C 1-6 alkyl (optionally substituted by hydroxy or C 1-4 alkoxy), phenyl-C 1-4 alkyl-, C 1-6...
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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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6750240 |
Methods of using bis-indolylquinones
The present invention relates to novel synthetic methods for the preparation of indolylquinones. The methods of the present invention are directed to synthetic reactions involving indoles and...
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6743802 |
Alkyne-aryl phosphodiesterase-4 inhibitors
Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation.
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6743793 |
Indole derivatives, process for preparation of the same and use thereof
Indole derivatives represented by formula (I): (wherein all symbols are described in the description), a process for the preparation of the same and a DP receptor antagonist comprising it as an...
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6743803 |
Medicines for the prevention and treatment of neurodegenerative diseases
Medicines for the prevention and treatment of neurodegenerative diseases such as Alzheimer's disease and schizophrenia of mammals (including human beings) through the retardation or inhibition of...
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6740662 |
Naphthyridine derivatives
2-Oxo-1,2-dihydro-1,8-naphthyridine derivatives characterized by bearing a specific substituent, —X—R 6 , at the 3-position and a cyclic substituent, R 5 , at the 4-position; or salts thereof....
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