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7034042 |
N-(4-aryloxypiperidin-1-ylalkyl) cinnamic amides as CCR33 receptor antagonists
Compounds of formula (I) in free or salt form, where Ar 1 is phenyl substituted by one or more substituents selected from halogen, cyano, nitro, and C 1 –C 8 -alkyl optionally substituted by...
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7034018 |
Substituted pyrrole mannich bases to combat pain and allergic reactions
The invention relates to substituted pyrrole Mannich bases of general formula (I), wherein R 1 =H, a C 1-10 -alkyl-, aryl, a heteroaryl- or an aryl, heteroaryl-, CN, Br—, Cl or OH radical bound...
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7030114 |
Compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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7026335 |
Melanocortin receptor ligands
The present invention relates to compounds which comprise a 4-substituted piperidine ring linked to a substituted or unsubstituted hydrocarbyl ring. The compounds, including all enatiomeric and...
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7026316 |
Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in...
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7022715 |
4-(phenyl-piperidin-4-ylidene-methyl)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders
Compounds of general formula I: R 1 is selected from any one of phenyl, pyridinyl, pyrrolyl, thienyl, furanyl, imidazolyl, triazolyl, thiazolyl and pyridine N-oxide; where each R 1 phenyl ring...
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7022716 |
Cyclic amine phenyl beta-3 adrenergic receptor agonists
This invention provides compounds of Formula I having the structure
wherein,
R 1 , R 2 , R 3 , R 4 , R 5 , T, T 1 , T 2 , and X are as defined hereinbefore, or a pharmaceutically...
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7019033 |
2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives
Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula
where R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are hydrogen or substituent groups such as alkyl, and...
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7019007 |
CCR-3 receptor antagonists (I)
The invention provides compounds of Formula (I):
wherein: R 1 –R 4 , A, D, and L have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical...
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7015218 |
Amide compounds and medicinal use thereof
The present invention relates to a compound of the formula
wherein R 1 is substituted aryl, heteroaryl and the like, R 2 and R 3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q...
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7005437 |
Substituted aryl and heteroaryl derivatives, the preparation thereof and the use therof as pharmaceutical compositions
The present invention relates to new substituted aryl and heteroaryl derivatives of general formula
wherein
A, Ar, n, X, Y 1 , Y 2 , Y 3 , Y 4 , R 1 and R 5 are defined as in claim 1...
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7001901 |
Tetrazolylpropionamides as inhibitors of Aβ protein production
This invention relates to novel tetrazolyl-propionamides in which the amide group comprises an aminoazepinone, and related structures, of Formula (I):
or pharmaceutically acceptable salt...
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6992091 |
N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
The present application describes N-ureidoalkyl piperidines as modulators of chemokine receptors, or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other...
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6984637 |
Cyclic amine derivatives-CCR-3 receptor antagonists
This invention relates to certain cyclic amine derivatives of Formula (I)
that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods...
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6984627 |
Peptide derivatives
Pharmaceutical preparation containing an effective amount of acetylsalicylic acid and a compound of Formula I.
A 1 —A 2 —NH—(CH 2 )...
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6982264 |
Substituted alcohols useful in treatment of Alzheimer's disease
The invention relates to substituted alcohol compounds of the formula (I):
wherein X, R 1 , R 2 , R 3 , R N , R 20 and R C are defined herein. The compounds are useful in the treatment or...
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6977263 |
Chemical compounds
Provided herein are novel and useful compounds having a tryptase inhibition activity, pharmaceutical compositions comprising such compounds, and methods treating subjects suffering from a...
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6977265 |
Piperidine CCR-3 receptor antagonists
The invention provides compounds of Formula (I):
wherein: R 1 -R 5 , A, L, and X have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical...
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6974810 |
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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6960602 |
Piperidine derivatives as modulators of chemokine receptors
The invention provides a compound of formula (I): wherein R 1 , R 2 , R 3 , R 3a , R 4 , R 4a , R 5 , and R 6 are as defined; or a pharmaceutically acceptable salt thereof or a solvate thereof;...
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6960601 |
Preparation and use of imidazole derivatives for treatment of obesity
This invention relates to substituted imidazole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds,...
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6958350 |
Chemical compounds
The invention provides a compound of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , N, X and Y are as defined in the specification, processes, for their preparation, pharmaceutical compositions...
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6953793 |
Substituted pyrazoles
Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.
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6949570 |
Compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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6949546 |
N-ureidoheterocycloalkyl-piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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6946477 |
3-Substituted piperidines comprising urea functionality, and methods of use thereof
One aspect of the present invention relates to novel heterocyclic compounds comprising urea functionality. A second aspect of the present invention relates to the use of the novel heterocyclic...
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6946466 |
Aromatic sulfonamides as peroxynitrite-rearrangement catalysts
The invention relates to the use of aromatics sulfonamides of the general formula I as peroxynitrite rearrangement catalysts, to the preparation thereof and to the use thereof as medicament for the...
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6939880 |
Compounds with growth hormone releasing properties
Compounds of peptide mimetic nature having the general formula I
wherein a and b are independently 1 or 2, R 1 and R 2 are independently H or C 1-6 alkyl, G and J are independently, inter...
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6939867 |
β3 agonists and uses thereof
Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with β-adrenergic receptors, such as obesity,...
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6930122 |
Use of central cannabinoid receptor antagonist for preparing medicines designed to facilitate smoking cessation
The invention relates to the use of N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-met
hylpyrazole-3-carboxamide for helping to quit tobacco consumption.
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6927217 |
HIV protease inhibitors
The present invention relates to novel dihydropyrones of Formula I
wherein X is NH or NR 8 , which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in...
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6919356 |
N-substituted heterocyclic amines as modulators of chemokine receptor activity
The present application describes modulators of chemokine receptors of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic...
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6908922 |
Linear cyclic ureas
Compound of formula (I):
wherein:
V represents a single bond or an alkylene chain, M represents a single bond or an alkylene chain, A and E each represents nitrogen or CH, but at least...
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6906085 |
Tetrahydropyran derivatives as neurokinin receptor antagonists
The present invention relates compounds of the formula (I):
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 represent a variety of substituents; and pharmaceutically acceptable salts...
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6903118 |
Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides
The invention relates to new piperazinyl-substituted pyridylalkane, alkene, and alkine acid amides substituted with saturated or one or several-fold unsaturated hydrocarbon residue in the...
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6903119 |
Amino acid derivatives and drugs containing the same as the active ingredient
The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification).
The compounds of the formula (I)...
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6900228 |
Opiate compounds, methods of making and methods of use
The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.
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6890928 |
Aromatic sulfone hydroxamic acids and their use as protease inhibitors
This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix...
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6887865 |
N-heterocyclic derivatives as NOS inhibitors
N-Heterocyclic derivatives of the formula (I):
are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these...
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6884809 |
Method and compositions for reducing cardiac dysfunctions with a selective histamine H3 receptor agonist
The invention provides a method for reducing cardiac dysfunctions in a human. The method comprises administration to the human of an effective amount of a selective histamine H 3 Receptor agonist....
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6884801 |
Imidazoline derivatives as alpha-1A adrenoceptor ligands
Compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof are disclosed. Such compounds are useful in the treatment of Alpha-1A mediated diseases or conditions such as...
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6878723 |
LTA4 hydrolase inhibitors
The invention concerns compounds inhibiting LTA 4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.
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6872735 |
LFA-1 antagonist compounds
The invention relates to novel compounds having formula (I)
wherein Cy, X, Y, L and R 1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte...
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6872734 |
Use of tiagabine for treatment of diabetic neuropathy and migraine
(R)-N-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]nipecotic acid and salts thereof are effective GABA uptake inhibitory compounds and exert pharmacological effects on pain associated with diabetic...
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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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6864249 |
Piperidine and azetidine thrombin inhibitors
The present invention relates to a compound having formula I:
and pharmaceutically acceptable salts thereof. The compounds of formula I and pharmaceutical compositions containing them are of...
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6852713 |
Lactam derivatives and methods of their use
Lactam derivatives of the general formula
are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.
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6852745 |
Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists
Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as...
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6852719 |
Glucocorticoid receptor modulators
The present invention provides non-steroidal compounds of Formula I, including prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial...
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6838479 |
Amidine inhibitors of serine proteases
Inhibitors of serine proteases are provided having formula (I)
wherein X, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. In particular, the compounds bind to factor VIIa, tissue...
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