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7618987 |
Acylated piperidine derivatives as melanocortin 4-receptor agonists
Certain novel N-acylated piperidine 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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7618961 |
Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the...
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7615549 |
Substituted pyrrolidinones, their manufacture and their use as medicaments
The present invention relates to new substituted pyrrolidinones of general formula
wherein A, X, B and R 1 to R 9 are as defined above, or a tautomer or salt thereof, particularly the...
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7612068 |
Aromatic oxyphenyl and aromatic sulfanylphenyl derivatives
The present invention relates to compounds of formula I wherein the substituents are as defined below. The compounds of formula I are useful for the treatment of diseases such as schizophrenia,...
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7608718 |
4,5-dihydro-1H-pyrazole derivatives having potent CB1-antagonistic activity
The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB 1 ) receptor antagonists with utility for the treatment of diseases connected...
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7608629 |
(Piperidinyloxy)phenyl, (piperidinyloxy)pyridinyl, (piperidinylsulfanyl)phenyl and (piperidinylsulfanyl)pyridinyl compounds as 5-HT1F agonists
The present invention relates to compounds of formula 1: and pharmaceutically acceptable acid addition sails thereof. The compounds of the present invention are useful for activating 5-HT 1F ...
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7608619 |
Substituted oxazole compounds with analgesic activity
Substituted oxazole derivatives corresponding to formula I:
a method for producing such compounds, pharmaceutical compositions containing such compounds, and the use of such compounds to treat...
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7608617 |
Naphthaline derivatives as H3 inverse agonists
The present invention relates to compounds of formula I:
and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The...
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7595312 |
Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions
The present invention relates to CGRP antagonists of general formula
wherein A, U, V, W, X and R 1 to R 3 are defined as in claim 1,
the tautomers, diastereomers, enantiomers, hydrates,...
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7592336 |
Hepatitis C virus inhibitors
Hepatitis C virus inhibitors having the general formula
are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
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7589110 |
Delivery of modulators of glutamate-mediated neurotransmission to the inner ear
The invention features methods and devices for local delivery of agents that modify glutamate-mediated neurotransmission to the inner ear for treatment of inner ear disorders caused by...
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7585859 |
PDE4B inhibitors and uses therefor
Compounds active on phosphodiesterase PDE4B are provided. Also provided herewith are compositions useful for treatment of PDE4B-mediated diseases or conditions, and methods for the use thereof.
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7585858 |
N-sulfonylcarboximidamide apoptosis promoters
Compounds having the formula
are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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7582654 |
Heterocyclo inhibitors of potassium channel function
Novel heterocyclo compounds useful as inhibitors of potassium channel function (especially inhibitors of the K v 1 subfamily of voltage gated K + channels, especially inhibitors K v 1.5 which has...
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7582629 |
Derivatives of isothiazol-3(2H)-one 1,1-dioxides as liver X receptor modulators
The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X...
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7579352 |
Retinoic acid mimetic anilides
The present invention is concerned with compounds of formula
the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents...
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7579340 |
Phenylenediamine urotensin-II receptor antagonists and CCR-9 antagonists
The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.
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7576218 |
4-phenylpiperdine-pyrazole CCR1 antagonists
Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful...
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7576106 |
Piperidine derivatives and methods of use
Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful...
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7576105 |
Benzyl substituted (piperidin-4-yl)aminobenzamido derivatives
The present invention is directed to N-benzyl substituted (piperidin-4-yl)aminobenzamido derivatives which are delta-opioid receptor modulators.
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7576102 |
Biaryl substituted nitrogen containing heterocycle inhibitors of LTA4H for treating inflammation
The present invention relates to a chemical genus of biaryl substituted nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general...
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7572921 |
Substituted benzylimidazoles useful for the treatment of inflammatory diseases
The invention comprises a class of derivatives of substituted benzylimidazoles of the formula (I) and methods for making the same. These compounds are useful for the treatment of inflammatory...
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7572792 |
Azetidine glycine transporter inhibitors
The present invention is directed to azetidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with...
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7572785 |
Substituted imidazoles as cannabinoid receptor modulators
The use of compounds of the present invention as antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor particularly in the treatment, prevention and suppression of diseases...
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7569568 |
Cytokine inhibitors
Disclosed are compounds of formula (I)
Where Ar 1 , X, R 3 , R 4 , R 5 and R 6 are defined herein. The compounds of the invention inhibit production of cytokines involved in inflammatory...
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7557219 |
Methods for making 4-tetrazolyl-4-phenylpiperidine compounds
Methods, composition, and intermediates are disclosed that are useful for making 4-Tetrazolyl-4-phenylpiperidine Compounds according to Formula I,
where Ar 1 is —C 3 -C 8 cycloalkyl,...
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7557126 |
Diphenylmethyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I:
wherein a, b, c, e, m, n, Ar 1 , R 1 , R 2 , R 3 , R 4a , R 4b , R 5 and R 6 are as defined in the specification. The compounds of formula...
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7557102 |
Pyrazolidine-1,2-dicarboxyldiphenylamide derivatives as coagulation factor Xa inhibitors for the treatment of thromboses
Novel compounds of the formula (I), in which R, R 1 , R 2 and R 3 have the meanings indicated in Patent Claim 1 , are inhibitors of coagulation factor Xa and can be employed for the prophylaxis...
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7550486 |
N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
The present application describes modulators of chemokine receptor activity of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other...
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7544700 |
Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein JunKinases
The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds....
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7541368 |
Pyrazoles as inhibitors of tumor necrosis factor
The present invention provides compounds of Formula (I)
and ester prodrugs, pharmaceutically acceptable salts or solvates of such compounds; or ester prodrugs of such salts or solvates;...
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7538122 |
Heterocyclic antiviral compounds
This invention relates to piperidine derivatives of formulae Ia and Ib with substituents as defined herein useful in the treatment of a variety of disorders, including those in which the modulation...
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7531535 |
Lactam-containing compounds and derivatives thereof as factor Xa inhibitors
The present application describes lactam-containing compounds and derivatives thereof of Formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7...
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7528162 |
4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB 1 ) receptor antagonists with utility for the treatment of diseases connected...
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7528136 |
Prolinamide derivatives as NK3 antagonists
The present invention relates to a compound of formula I
wherein
R 1 , R 2 , R 3 , R 4 , R 5 , X, n, and o are as defined herein and to a pharmaceutically acceptable acid addition salt thereof...
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7524868 |
Substituted pyrazoline compounds, their preparation and use as medicaments
The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for...
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7524867 |
Tetrasubstituted imidazole derivatives as cannabinoid CB1 receptor modulators with a high CB1/CB2 receptor subtype selectivity
The present invention relates to 1,2,4,5-tetrasubstituted imidazole derivatives as selective cannabinoid CB 1 receptor modulators, in particular CB 1 receptor antagonists or inverse agonists...
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7524838 |
Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them
The present invention relates to the novel derivatives of formula (I) in which
A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7)...
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7521473 |
Inhibitors of protein tyrosine phosphatase 1B
Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted thiophene compounds such as, for...
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7521462 |
4-Amino-piperidine derivatives as monoamine uptake inhibitors
The present invention provides compounds of formula (I) where n, R1, R2, R3, R4, R5 and Heteroaryl are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected...
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7517892 |
Ligands for monoamine receptors and transporters, and methods of use thereof
One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian...
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7514439 |
Oxime derivative and preparations thereof
The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]:
wherein Ring A is aryl or heteroaryl;
...
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7514068 |
Biphenyl-pyrazolecarboxamide compounds
The present invention relates to biphenyl-pyrazole compounds and in particular biphenyl-pyrazolecarboxamides. The invention further provides compositions comprising a compound of this invention and...
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7507753 |
Biaryl compound and use thereof
The present invention provides a compound having melanocortin receptor agonist activity or antagonist activity, which is a novel biaryl compound represented by the formula (I):
wherein...
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7504400 |
MTP inhibiting aryl piperydines or piperazines substituted with 5-membered heterocycles
The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant...
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7498348 |
1 H-imidazole derivatives as cannabinoid receptor modulators
The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid receptors, to methods for the preparation of these compounds, to novel intermediates useful for the...
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7491737 |
Heterarylpiperidine modulators of chemokine receptor activity
The present invention is directed to compounds of the formula (I): (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 10 and n are defined herein) which are useful as modulators of chemokine receptor...
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7491724 |
Substituted cyclic hydroxamates as inhibitors of matrix metalloproteinases
The present invention provides compounds of the formula I:
its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof,...
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7482365 |
Piperidylcarboxamide derivatives and their use in the treatment of tachykinin-mediated diseases
The present invention relates to piperidine derivatives of formula (I):
wherein R, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X, Y, m and n are as defined herein; and pharmaceutically acceptable salts...
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7482364 |
Phenylalkynes
Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
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