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7381719 |
Diaryl ethers as opioid receptor antagonist
A compound of the formula (I) wherein the variables X 1 to X 10 , R 1 to R 7 including R 3′ , E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer,...
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7365073 |
3-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by VLA-4
Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a...
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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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7319099 |
Benzoyl-piperazine derivatives
The invention relates to compounds of formula
wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such...
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7317013 |
Cyclic pyrazinoylguanidine sodium channel blockers
The present invention provides sodium channel blockers represented by formula (I):
where the structural variables are defined herein. The compounds of the present invention may be used for...
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7307081 |
Piperidine derivatives useful as CCR5 antagonists
The present invention provides a compound of the formula
or a pharmaceutically acceptable salt or solvate thereof, wherein the various moieties are as defined in the specification. The present...
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7300930 |
Therapeutic acridone and acridine compounds
The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ═O, L is —H, alpha is a single bond, beta is a double bond, gamma is a single bond...
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7262197 |
Phospholipase C inhibitors for use in treating inflammatory disorders
This invention is directed to heterocyclyl-substituted anilino phospholipase C inhibitor compounds useful in treating or ameliorating an inflammatory disorders and/or restenosis of the general...
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7259162 |
Benzazole derivatives and their use as JNK modulators
The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said...
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7253168 |
Substituted 1-benzyl-4-substituted piperazine analogues
Compounds of Formula I are provided, in which variables are as described herein:
Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly...
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7244722 |
Amino-substituted 1H-pyrazin-2-ones and 1H-quinoxalin-2-ones
Compounds of the general formula (I):
wherein m, n, R 1 , R 2 , R 3 and R 4 are as described in the specification.
Further included are pharmaceutical compositions comprising the...
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7238693 |
Aryl carbamate derivatives, preparation and use thereof
The present invention relates to novel compounds, the preparation and use, particularly therapeutic, thereof. More specifically, it relates to compounds derived from aryl carbamates, the...
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7238688 |
Piperidine compounds
Disclosed are novel compounds of the formula
Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or...
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7226925 |
Compounds, their use and preparation
The invention relates to compounds of the general Formula (I):
The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from...
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7196080 |
Phenylpyridinecarbonylpiperazinederivative
The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. ...
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7189715 |
Compositions comprising zopiclone derivatives and methods of making and using the same
The invention is directed to racemic and stereomerically pure compounds of Formula 3:
and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation.
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7186715 |
Piperazine- and piperidine-derivatives as melanocortin receptor agonists
The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction
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7179807 |
5-substituted-2-arylpyrazines
Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators or CRF receptors. Compounds of the invention are provided by the following formula:
The...
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7160886 |
Acylated piperazine derivatives as melanocortin-4 receptor agonists
Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are...
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7153858 |
Arylpiperazinyl compounds
The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formulae I: and II, and synthesis and uses of those compounds for treating...
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7153856 |
Cyclic protein tyrosine kinase inhibitors
Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders...
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7122544 |
Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure:
wherein R 1 ...
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7119086 |
Phenylsulfonyl-1,3-dihydro-2h-indole-2-one derivatives, their preparation and their therapeutic use
The invention relates to compounds of formula:
and also to the salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, with affinity for and selectivity towards...
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7105519 |
Inhibitors of macrophage migration inhibitory factor and methods for identifying the same
Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF...
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7101886 |
Phenylalkyl and pyridylalkyl piperazine derivatives
This invention relates to compounds of the formula 1
wherein R 1 , R 3 , R 4 , X 1 , and X 2 are defined as in the specification, pharmaceutical compositions containing them and their use in...
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7098213 |
CCR5 antagonists useful for treating AIDS
Compounds of the formula
or a pharmaceutically acceptable salt or isomer thereof, wherein:
Q, X and Z are CH or N; R, R 4 –R 7 and R 13 are H or alkyl; R 1 is H, alkyl, fluoroalkyl,...
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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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7084141 |
Inhibitors of macrophase migration inhibitory factor and methods for identifying the same
Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF...
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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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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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7026314 |
Therapeutic chromone compounds
Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating,...
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7015216 |
Heteroaryl-β-alanine derivatives as alpha 4 integrin inhibitors
Disclosed are a series of heteroaryl-β-alanine derivatives, compositions containing them, processes for their preparation and their use in medicine.
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7008946 |
CCR5 antagonists useful for treating AIDS
Compounds of the formula
or a pharmaceutically acceptable salt or isomer thereof, wherein:
Q, X and Z are CH or N; R, R 4 –R 7 and R 13 are H or alkyl; R 1 is H, alkyl, fluoroalkyl,...
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6960580 |
Nitrogenous heterocyclic substituted quinoline compounds
The present invention relates to nitrogen-containing heterocyclic quinoline compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases,...
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6958331 |
Bradykinin receptor antagonists
The invention relates to sulfonyl amine derivatives of formula IA
wherein R 5A , X 1 , X 2 , R 9 and R 10 are as defined herein, which derivatives are useful as bradykinin B 1 receptor...
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6949552 |
Remedial agent for anxiety neurosis or depression and piperazine derivative
There are provided a therapeutic preparation for anxiety neurosis or depression which comprises a MC 4 receptor antagonist as an effective ingredient; and a piperazine derivative represented by...
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6939884 |
Pharmaceutical agents containing acyclovir, fusaric acid and derivatives thereof
Compositions are provided, which comprise at least one nucleoside analogue inhibitor, pharmaceutically acceptable salts, solvates, or prodrugs thereof and fusaric acid, derivatives, or...
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6916804 |
Pyrimidine A2b selective antagonist compounds, their synthesis and use
The subject invention provides compounds having the structure:
wherein R 1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5...
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6861432 |
Piperazine derivatives that destabilize androgen receptors
This invention relates to new piperazine derivatives of general formula I,
in which V, W, n, R, R′, i, j, Y and Z have the meaning that is indicated in the description.
The compounds...
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6838461 |
N-(indolcarbonyl-)piperazine derivatives
Compounds of the formula I
in which R 1 , R 2 , R 4 and R 5 have the meanings indicated in claim 1 , are potent 5-HT 2A antagonists and are suitable for the treatment of psychoses,...
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6833369 |
Angiogenesis inhibiting 5-substituted-1,2,4,-thiadiazolyl derivatives
This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R 1 is...
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6797709 |
Aromatic nitrogen-containing 6-membered cyclic compounds
An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): wherein Ring A is a substituted or unsubstituted nitrogen-containing heterocyclic group; R 1 is a substituted or...
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6787546 |
Heterocycle derivatives and drugs
The object of the invention is to provide an excellent compound as a drug. The invention relates to a heterocyclic compound shown by the following formula: A—B—D—E [ 1] wherein A is...
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6780863 |
Bis-basic compounds with tryptase-inhibitory activity
Compounds of which the following are exemplary: These have tryptase-inhibiting activity and are useful for the treatment of inflammatory and allergic disease conditions.
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6747030 |
Piperazine derivatives as 5-HT1B antagonists
Piperazine derivatives of formula(1), processes for their preparation, pharmaceutical compositions containing them in the treatment of CNS and other disorders and in their use in therapy as 5-HT...
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6740661 |
Farnesyl protein transferase inhibitors
Disclosed are compounds of the formula: wherein R 13 represents an imidazole ring; R 14 represents a carbamate, urea, amide or sulfonamide group; R 8 represents H when the alkyl chain between...
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6734183 |
Compounds
Compounds of the formula I useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.
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6727253 |
Treatment of accidental extravasation of anthracyclines
The present invention relates to a method for pharmacological treatment of accidental extravasation of topoisomerase II poisons, such as anthracyclines. In particular, the invention relates to the...
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6716871 |
Cyclic AMP-specific phosphodie sterase inhibitors
Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases...
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6713472 |
Thiazine or pyrazine derivatives
A compound which is a chymase inhibitor and which is represented by a formula [I] and salts thereof. In the formula [I], X is R 6 —(A 2 ) n —N, R 1 and R 2 are H, alkyl, cycloalkyl or aryl, R...
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