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7615563 |
Compositions useful as inhibitors of voltage-gated sodium channels
The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of...
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7612090 |
Aryl and heteroaryl substituted tetrahydroisoquinolines and use thereof
Provided herein are compounds of the formula (I):
wherein R 1 -R 8 are as described herein, R 4 being aryl or heteroaryl Such compounds are particularly useful in the treatment of a disorder...
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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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7601739 |
Compounds having antiestrogenic and tissue selective estrogenic properties, and compounds with anti-androgenic properties for treatment of prostate cancer and androgen receptor dependent diseases
Compounds for the treatment of estrogen-receptor related maladies are provided. Compounds with anti-androgenic properties also are provided. In particular, the invention provides compounds that are...
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7601738 |
Excitatory amino acid receptor antagonists
The present invention provides novel compounds of Formula (I) and Formula (I(a)), or the pharmaceutically acceptable salts thereof; methods for treating neurological disorders and neurodegenerative...
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7598242 |
Compounds for the treatment of inflammatory disorders
This invention relates to compounds of the Formula (I):
or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions...
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7595343 |
Inhibitors of histone deacetylase
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides...
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7592331 |
Macrocyclic factor VIIa inhibitors useful as anticoagulants
The present invention relates generally to novel macrocycles of Formula (I):
or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables...
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7579347 |
Vanilloid receptor ligands and their use in treatments
Compounds having the general structure
and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster...
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7576098 |
Heterocyclic compounds as inhibitors of factor VIIa
The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable...
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7572809 |
Isoquinoline aminopyrazole derivatives
The present invention relates to the compounds of formula I:
their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of such...
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7572783 |
Substituted benzofused heterocycles
The present invention relates to the compounds of Formula I, their preparation and pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful, for...
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7566726 |
3,3-disubstituted tetrahydropyranyl cyclopentyl amide modulators of chemokine receptor activity
(wherein n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 15 , R 16 , R 17 , R 18 , Y and Z are defined herein) which are modulators of chemokine receptor activity and are useful...
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7557124 |
Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity
Compounds of Formula I:
(wherein n, R 1 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 15 , R 16 , Y and Z are as defined herein) which are modulators of chemokine receptor activity and...
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7557123 |
Heterocyclic compound and medicinal use thereof
The novel heterocyclic compound of the present invention is a novel heterocyclic compound having the formula (I)
Y:
R 15 —C(R 14 )═N—O—
wherein R 1 is H or C 1-6 alkyl, R 2 is...
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7550481 |
Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease
The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which...
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7547731 |
Formamide derivatives for the treatment of diseases
The invention relates to compounds of formula (1)
and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives....
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7541357 |
Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
The compounds of the present invention are represented by the chemical structure found in Formula (I):
wherein:
the carbon atom designated * is in the R or S configuration; and X is a fused...
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7528170 |
Sulfonamide derivatives for the treatment of diseases
The invention relates to compounds of formula (1)
and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives....
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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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7524883 |
Eponemycin and epoxomicin analogs and uses thereof
The present invention provides compounds having formula (1): wherein R 1 -R 6 , A, J, D, E, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally...
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7524861 |
Process for the preparation of a hydrate of an anthranilic acid derivative
A hydrate of an acid addition bis-salt of an anthranilic acid derivative is produced by a process which comprises:
(a) combining, in any order, the anthranalic acid derivative, a...
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7521461 |
Benzoic acid derivatives as modulators of PPAR alpha and gamma
A compound of formula (I) wherein R 1 represents aryl optionally substituted by a heterocyclic group or a heterocyclic group optionally substituted by aryl wherein each aryl or heterocyclic group...
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7511060 |
Opiate intermediates and methods of synthesis
Novel opiate intermediate compositions and methods of synthesis that include changing the substitution pattern on the aromatic ring of the pre-Grewe intermediate are provided.
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7511059 |
Thiazolidinones, their production and use as pharmaceutical agents
The invention relates to thiazolidinones of general formula (I)
their production and use as inhibitors of polo-like kinases (Plk) for treating various diseases.
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7501516 |
Quinoline derivatives and their use as tyrosine kinase inhibitors
The invention concerns quinoline derivatives of Formula (I) wherein each of Z, m, R 1 , n and R 3 have any of the meanings defined in the description; processes for their preparation,...
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7498441 |
Biaryltetrahydroisoquinoline piperidines as selective MCH receptor antagonists for the treatment of obesity and related disorders
The present invention discloses compounds which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In other aspects, the invention is...
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7488738 |
Aminophenoxyacetic acid derivatives and pharmaceutical composition containing thereof
There is provided an aminophenoxyacetic acid derivative of the following formula (I):
wherein, R 1 , R 2 , R 3 and R 4 are, independent from each other, alkoxy group, alkyl group or aryl...
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7476679 |
Octahydroisoquinoline compounds as opioid receptor modulators
Compounds which bind to opioid receptors are provided. In a preferred embodiment of the invention, the compounds are opioid receptor antagonists. The present invention also provides methods of...
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7465744 |
Triazole compounds and the therapeutic use thereof
The invention relates to triazole compounds of general formula (I), wherein A, B, R 1 , R 2 , R 3 and R 4 have the meaning cited in claim 1. The invention also relates to a pharmaceutical agent...
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7462629 |
Immunosuppressant compounds and compositions
The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds...
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7449477 |
7-phenyl-isoquinoline-5-sulfonylamino derivatives as inhibitors of akt (protein kinase B)
The present invention relates to compounds Formula (I) as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.
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7446115 |
Peptidomimetic ligands for cellular receptors and ion channels
One aspect of the present invention relates to novel peptidomometic compounds. A second aspect of the present invention relates to the use of the novel peptidomimetic compounds as...
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7446103 |
Bicyclic benzamide compound as histamine H3 receptor ligand useful in the treatment of neurological diseases
The present invention relates to novel bicyclic benzamide derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the...
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7442710 |
Substituted phenyl methanones
The present invention relates to compounds of general formula IA or IB
wherein
X 1 and X 2 are each independently N or C—R″ and R 1 , R 2 ,R 3 , R 4 , R 5 , and R 6 are as defined in...
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7439270 |
Drugs for spinal anesthesia
Spinal anesthetics for intrathecal administration to produce spinal anesthesia are provided with use of 6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinolone-3-car
boxylic acid or its...
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7439257 |
Aryloxyalkylcarbamate-type derivatives, preparation method thereof and use of same in therapeutics
The invention relates to a compound of formula (I):
Wherein m, n, X, Y, R 1 , R 2 , R 3 and R 4 are as defined herein. The invention also relates to the use of same in therapeutics.
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7435750 |
Method of using substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I:
wherein Ar 1 , Ar 3 , A, B and D are defined herein. The...
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7435729 |
Compounds and methods for modulation of estrogen receptors
Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for...
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7429592 |
Cyanoanthranilamide derivatives and the use thereof as medicaments
Substituted cyanoanthranilamide derivatives, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described. The compounds...
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7417062 |
Substituted arylamides
Substituted benzamide compounds are provided along with methods for the use of those compounds for treating cancer.
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7414063 |
Inhibitors of Akt (protein kinase B)
The present invention relates to compounds Formula (I): as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.
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7407989 |
Compounds useful for modulating abnormal cell proliferation
There is described compounds of Formula I, and salts, solvates and hydrates thereof:
wherein: R 1 , R 2 and R 3 are each independently selected from OH, C 1-6 alkyl, OC 1-6 alkyl, OC(O)C 1-6...
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7407976 |
Thiazoles and oxazoles useful as modulators of ATP-Binding Cassette transporters
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions...
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7402594 |
Sulfated bis-cyclic agents
Sulfated bis-cyclic compounds that are potent anticoagulants and methods for their manufacture are provided. The sulfated compounds are bis-cyclic moieties comprised of an isoquinoline ring joined...
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7390798 |
Carboxamide spirolactam CGRP receptor antagonists
The present invention is directed to compounds of Formula I: I (where variables A 1 , A 2 , B, J, K, m, n, R 4 , R 5a , R 5b and R 5c are as defined herein) useful as antagonists of CGRP...
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7388017 |
Inhibitors of serine proteases, particularly hepatitis C virus NS3 protease
The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds,...
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7384957 |
3,4-dihydro-1H-isoquinolin-2-yl-derivatives
The present invention relates to novel compounds of formula I wherein the variable groups are as defined in the claims or a pharmaceutically acceptable acid addition salt thereof. The compounds of...
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7378428 |
Nitrogen-containing bicyclic compounds and drugs containing the same as the active ingredient
A nitrogen-containing bicyclic compound of formula (I) or a pharmaceutically acceptable salt thereof (wherein the symbols have the same meanings as described in the specification).
The compound...
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7354944 |
Thiadiazole compounds and methods of use
The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and...
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