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7605172 |
Thiazolo-naphthyl acids
The present invention relates to thiazolo-naphthyl acids of the formula
and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.
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7605171 |
(3,4-disubstituted)propanoic carboxylates as S1P (Edg) receptor agonists
The present invention encompasses compounds of Formula I:
as well as the pharmaceutically acceptable salts thereof. The compounds are S1P 1 /Edg1 receptor agonists and thus have...
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7605164 |
Compositions and methods for treating heart failure
Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including...
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7601742 |
Pyrrolidones with anti-HIV activity
The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using...
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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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7595332 |
Amides that inhibit vanilloid receptor subtype 1 (VR1)
The present invention relates to compounds of formula (I)
that are novel VR1 antagonists useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.
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7595321 |
Compounds having selective inhibiting effect at GSK3
The present invention relates to new compounds of formula (I) wherein Z is N; Y is CONR 5 , NR 5 CO, SO 2 NR 5 , NR 5 SO 2 , CH 2 NR 5 , NR 5 , NR 5 CONR 5 , CH 2 CO, CO, O or CH 2 O; X is CH or N;...
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7589216 |
Process for preparing N-hydroxyformamido-propyl pyrrolidin compounds and intermediates
The present invention is directed to a process for preparing intermediates that are useful to prepare certain antibacterial N-formyl hydroxylamine compounds which are peptide deformylase...
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7585882 |
Phosphodiesterase 4 inhibitors
Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I:
wherein R 1 , R 2 ,...
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7585881 |
Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
The present invention relates to new compounds of formula I,
to pharmaceutical formulations containing the compounds, and to the use of the compounds in the prevention and/or treatment of...
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7585880 |
Phenylpropanoic acid derivatives
The present invention provides a novel compound having a GPR40 receptor function modulating action, which is useful as an insulin secretagogue, a drug for the prophylaxis or treatment of diabetes...
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7582659 |
Cyclopropyl group substituted oxazolidinone antibiotics and derivatives thereof
This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and...
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7579355 |
Inhibitors of Akt activity
The present invention is directed to compounds which contain a substituted pyridine moeity which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to...
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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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7576079 |
Viral polymerase inhibitors
An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I:
wherein:
A is O, S, NR 1 , or CR 1 , wherein R 1 is defined herein; represents either a single...
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7572816 |
Therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders
The present invention is directed to compounds having the structure wherein R 1 , R 2 , R 3 , R 4 , R 5 and m are as defined herein. The compounds of this invention are novel therapeutic agents...
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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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7566730 |
Substituted aminoethers for the treatment of Alzheimer's disease
The invention provides compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful...
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7560564 |
Heterocyclic diamide invertebrate pest control agents
This invention provides compounds of Formula (I), N-oxides and suitable salts thereof, wherein A and B are independently O or S; each J is independently a phenyl ring, a naphthyl ring system, a 5-...
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7560456 |
Pesticidal pyridinecarboxamide derivatives
The invention relates to 3-pyridylcarboxamide derivatives of formula (I):
wherein the various symbols are as defined in the description, compositions thereof, methods for controlling pests by...
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7557131 |
Substituted triazole derivatives as oxytocin antagonists
The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility...
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7544704 |
Aryl-4-ethynyl-isoxazole derivatives
The present invention is concerned with aryl-4-ethynyl-isoxazole derivatives of formula I
wherein R 1 to R 5 are as described in the specification and pharmaceutically acceptable salt...
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7524873 |
Calcium receptor modulating agents
The compounds of the invention are represented by the following general structure
or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are...
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7524872 |
Method and composition for treating cancer using cellular organelle crystallizing agents
This invention provides a method for treating cancer in mammals through cellular-organelle-crystallization-induced-death (herein defined as “Cocid”), a method for treating cancer using cellular...
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7524870 |
Biaryloxymethylarenecarboxylic acids as glycogen synthase activators
The present invention relates to compounds of formula (I)
wherein Ar, Ar 2 , R 2 , R 3 , R 4 , m, p and s are as defined in the description and claims, and pharmaceutically acceptable salts...
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7524864 |
Methods of treating sleep disorders
The invention relates to novel antihistamines and methods of modulating sleep by administering a doxepin analog or a pharmaceutically effective salt thereof.
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7504420 |
Compounds which inhibit beta-secretase activity and methods of use
The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.
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7504402 |
Triazole derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase-1
Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as...
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7498350 |
Oxazolidinones as antibacterial agents
A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof: Wherein C is selected from (D) and (E), R 2 a, R 6 a, and R 3 a are independently...
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7495016 |
Pyrrolidones with anti-HIV activity
The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using...
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7485653 |
1,4-dihydropyridine compounds, pharmaceutical compositions, and methods for the treatment of cardiovascular disease
The present invention provides certain substituted 1,4-dihydropyridine compounds, including pure enantiomeric forms and pharmaceutical formulations thereof. These compounds provide for elevation of...
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7485652 |
Indolyl derivatives as liver-X-receptor (LXR) modulators
The invention relates to compounds of formula (I):
and pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A, m, n and...
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7476684 |
Compounds for the treatment of neurological, psychiatric or pain disorders
The present invention is directed to novel compounds, their use in therapy and pharmaceutical compositions comprising said novel compounds.
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7476683 |
Glycinamide derivatives as raf-kinase inhibitors
The present invention relates to glycinamide derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the...
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7462633 |
Cyclopropyl group substituted oxazolidinone antibiotics and derivatives thereof
This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and ...
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7456200 |
Compounds
The present invention relates to new compounds of formula I,
a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing compounds of the...
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7452885 |
Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I
The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and...
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7442713 |
2-thio-substituted imidazole derivatives and their use in pharmaceutics
The invention relates to 2-thio-substituted imidazole derivatives of the formula I
in which the radicals R 1 , R 2 , R 3 , R 4 and p are as defined in the description. The compounds according...
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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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7435748 |
Gamma-secretase inhibitors
Compounds of formula I:
inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease.
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7432287 |
Heteroarylcarbamoylbenzene derivative
Compounds represented by formula (I):
as well as their pharmaceutically acceptable salts are disclosed. The compounds are useful as glucokinase activating agents for the treatment of diabetes...
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7429605 |
Phenylpyridine derivatives
The present invention relates to the compounds of formula I:
their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned...
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7425570 |
Pyridoxine and pyridoxal analogues: new uses
The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions...
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7423012 |
Phosphinyloxy, oxime and carboxylic acid derivatives which are useful as carboxypeptidase U inhibitors
The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts,
which compounds inhibit carboxypeptidase U and...
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7420055 |
Aryl sulfonamides
Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9....
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7414065 |
Methods to modulate conditions mediated by the CXCR4 receptor
The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have...
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7414055 |
Inhibitors of Akt activity
The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to...
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7410979 |
Synergistically effective combinations of dihaloacetamide compounds and interferon or ribavirin against HCV infections
The present invention relates to anti-HCV dihaloacetamide compounds in synergistic combination with an interferon and/or ribavirin and pharmaceutical compositions thereof for inhibition of the...
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7407972 |
Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I):
wherein A, B, C, G, and W 1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are...
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7399773 |
Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid and phenylamide
An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-
pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxy
lic acid phenylamide by a novel...
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