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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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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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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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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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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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6653313 |
1,4-dihydropyridine compounds as bradykinin antagonists
The present invention relates to compounds of the formula wherein each A is independently halo; Y is —(CH 2 ) m —, —C(O)— or —S(O)—; R 1 and R 2 are independently C 1-4 alkyl; R 3...
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6653320 |
Imidazopyridine derivatives
The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel...
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6642225 |
Diazacycloalkanedione derivatives
Compounds of formula I wherein R is carboxy, esterified carboxy or amidated carboxy; R 1 and R 3 are independently lower alkyl, (hydroxy, lower alkoxy, amino, acylamino, mono- or di-lower...
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6642237 |
Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof
γ-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanam
ide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or...
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6635647 |
Decahydro-isoquinolines
The invention provides compounds of formula (I) wherein A, B and R are as defined herein and the preparation thereof. The compounds of formula (I) are useful as somatostatin antagonists.
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6613770 |
Quinoline derivatives as NK-2 and NK-3 receptor ligands
A compound, or a solvate or a salt thereof, of formula (I): wherein R is linear or branched alkyl; R 1 represents hydrogen or up to four optional substituents selected from the list consisting...
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6573262 |
Composition and antiviral activity of substituted indoleoxoacetic piperazine derivatives
The invention comprises substituted indoleoxoacetic piperazine derivatives of general Formula I, compositions thereof and their use as antiviral agents, and particularly for treating HIV infection.
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6559186 |
Compositions and methods of treatment of sympathetically maintained pain
Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other...
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6552015 |
Azabicycloalkane derivatives and therapeutic uses thereof
The present invention is directed to a compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , Y, U, W, k, A, E, V, R 4 and R 5 are as defined herein,...
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6531468 |
Diazabicyclooctane derivatives and therapeutic uses thereof
The present invention provides diazabicyclooctane derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein the group represents R 1 and R 2 are selected...
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6514988 |
Condensed-ring thiophene derivatives, their production and use
A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or...
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6506772 |
Substituted &lsqb 1,2,4&rsqb triazolo&lsqb 1,5a&rsqb pyridine derivatives with activity as adenosine receptor ligands
Substituted [1,2,4]triazolo[1,5a]pyridine derivatives and pharmaceutically active salts thereof with activity as adenosine receptor ligands are disclosed. These compounds are useful for treatment...
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6476022 |
Oxathiepino&lsqb 6,5-b&rsqb dihydropyridines, and related compositions and methods
This invention provides novel oxathiepino[6,5-b]dihydropyridines. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstriction activity....
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6448244 |
Water soluble azoles as broad-spectrum antifungals
The present invention concerns novel water-soluble azole compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof;...
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6423711 |
Heterocyclic amino substituted heteroaryl fused pyridines; GABA brain receptor ligands
Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: n is an integer from 0 to 3; the C ring is aryl or heteroaryl; X is CH, N, or O Z...
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6399616 |
Pyridine compounds
A compound selected from those of formula (I): wherein: W represents optionally substituted naphthyl, n represents an integer from 2 to 3 inclusive, Z represents a single bond, A represents...
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6362180 |
Imidazopyridines for the treatment of neurological disorders
Corticotropin releasing factor (CRF) antagonists of formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress...
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6358970 |
Integrin receptor antagonists
The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are...
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6326379 |
Fused pyridine inhibitors of cGMP phosphodiesterase
Compounds of the formulas ##STR1## are useful as inhibitors of cGMP PDE, especially type V.
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6316445 |
Carboxy substituted acylic carboxamide derivatives
The present invention relates to novel carboxy substituted acyclic carboxamide derivatives of formula (1)): ##STR1## and stereoisomers and pharmaceutically acceptable salts thereof and their use as...
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6310063 |
Aminoalkyl substituted pyrrolo [3,2-E]pyridine and pyrollo [2,3-b]pyrimidine derivatives: modulators of CRF1 receptors
Disclosed are compounds of the formula: ##STR1## wherein Ar, Q 1 , Q 2 , R 1 , W and X are substituents as defined herein, which compounds are water-soluble CRF 1 receptor antagonists, and are...
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