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7410956 |
Caspase inhibitor prodrugs
The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of...
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7407946 |
Quinazoline compounds
Quinazoline derivatives of formula (I) wherein A is 5-membered heteroaryl containing a sulphur atom and optionally containing one or more nitrogen atoms; compositions containing them, processes for...
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7365096 |
Methods for selectively inhibiting Janus tyrosine kinase 3 (Jak3)
Methods are disclosed for inhibiting or disrupting Janus tyrosine kinase 3 (Jak3) dependent function in cells of lymphoid or myeloid origin, especially for blocking proliferation and function of...
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7365091 |
Derivatives of succinic and glutaric acids and analogs thereof useful as inhibitors of PHEX
The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula:
useful as inhibitors of PHEX. These derivatives are...
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7351698 |
Androgen receptor modulators and methods of use thereof
Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation,...
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7345082 |
Phosphinic acids
The present invention relates to phosphinic acid derivatives of formula I
wherein R 1 , R 2 , R 3 and R 4 are described hereinabove. These compounds can be used in the treatment or prevention...
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7345032 |
Methods for the preparation of {2-[(8,9)-dioxo-2,6-diaza-bicyclo[5.2.0]-non-1(7)-en-2-yl]ethyl}phosphonic acid and esters thereof
The present invention provides methods for the preparation of {2-[(8,9)-dioxo-2,6-diaza-bicyclo[5.2.0]-non-1(7)-en-2-yl]et
hyl}phosphonic acid, and esters thereof.
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7300924 |
Anti-infective phosphonate analogs
The invention is related to phosphorus substituted anti-infective compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as...
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7282514 |
Reactive probes for two-photon fluorescent imaging and sensing
Fluorescent dyes and probes are key components in multiphoton based fluorescence microscopy imaging of biological samples. In order to address the demand for better performing dyes for two-photon...
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7268123 |
Derivatives of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)alkyl]phosphonic acid and methods of making them
Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided:
wherein: A is alkylenyl of 1 to 4 carbon atoms, or alkenylenyl of 2 to 4 carbon atoms; R 1 and R 2 ...
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7253153 |
Derivatives of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)alkyl] phosphonic acid and methods of use thereof
Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided
where at least one of R 2 or R 3 is not hydrogen. The compounds of the present invention are...
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7247610 |
Use of glutamate antagonists for the treatment of cancer
Disclosed are methods for treating cancer by administering an inhibitor of the interaction of glutamate with the KA receptor complex.
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7235537 |
N3 alkylated benzimidazole derivatives as MEK inhibitors
Disclosed are compounds of the formula I
and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R 1 , R 2 , R 7 , R 8 , R 9 and R 10 are as defined in the specification. Such...
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7226915 |
Diaminopyrroloquinazolines compounds as protein tyrosine phosphatase inhibitors
This invention relates to diaminopyrroloquinazoline compounds which are useful for inhibiting protein tyrosine phosphatases, particularly PTP1B, and are useful for lowering blood glucose...
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7214701 |
Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising
(a) compounds of the formula (I)
in which W, X, Y, Z, A, B, D and G...
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7202234 |
Compounds and methods for treating Toll-like receptor 2-related diseases and conditions
The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation.
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7176196 |
Bicyclic heterocycles as HIV integrase inhibitors
The invention encompasses a series cyclic bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds...
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7157447 |
Bicyclic heterocycles as HIV integrase inhibitors
The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for...
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7138388 |
Methods to treat autoimmune and inflammatory conditions
This invention provides methods for treating inflammatory or autoimmune diseases by contacting the affected cell or tissue with a therapeutic compound as described herein. Such pathologies include,...
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7132427 |
Quinazolines and uses thereof
This invention relates to compounds of the general formula:
in which R A , R B , R C and R D are as defined herein, and to their preparation and use.
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7129225 |
Protection against and treatment of hearing loss
The present invention provides a method for protecting against or treating hearing loss in a subject. This method involves administering an effective amount of a protein tyrosine kinase inhibitor...
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7098196 |
Regulators of the hedgehog pathway, compositions and uses related thereto
The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract...
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7041658 |
Method of inhibiting hair growth
Disclosed herein are a method of inhibiting hair growth, which comprises administering an inhibitor of elastase-like enzymes or a neutral endopeptidase inhibitor, and use of an inhibitor of...
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7018988 |
Pharmaceutically active pyrrolidine derivatives as Bax inhibitors
The present invention is related to new substituted pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine...
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6987100 |
Pharmaceutical compositions for treating bone lesions in multiple myeloma
Pharmaceutical compositions for treating bone lesions in multiple myeloma or pharmaceutical compositions for treating multiple myeloma which contain as an active ingredient a compound having both...
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6930101 |
Thiazolopyrimidines useful as TNFα inhibitors
The invention provides derivatives of thiazolo[4,5-dl]pyrimidine and their use as inhibitors of proinflammatory cytokines.
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6930100 |
Phosphate prodrugs of fluoroxindoles
The present invention provides novel phosphate derivatives having the general Formula I
wherein the wavy bond ( ) represents the racemate, the (R)-enantiomer or the (S)-enantiomer and A, B, R...
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6908908 |
Biologically active 4H-benzo [1,4] oxazin-3-ones
The invention is directed to 4h-benzo[1,4]oxazin-3-ones useful as peroxisome proliferator activated receptor gamma (PPARγ) agonists or antagonists. Pharmaceutical compositions comprising compounds...
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6867200 |
(Hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors
The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a...
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6864276 |
Active substance combinations having insecticidal and acaricidal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising
(a) compounds of the formula (I)
in which W, X, Y, Z, A, B, D and G are each as...
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6841559 |
Pyridinones to treat and prevent bacterial infections
Novel pyridinones and their derivatives which are effective in treating or preventing Gram-negative bacterial infections are provided. The pyridinones are stable and easily derivatized; the methods...
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6825211 |
Bicyclic metabotropic glutamate receptor ligands
The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and methods for their use.
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6797692 |
Use of glutamate antagonists for the treatment of cancer
Glutamate antagonists (NMDA, AMPA and kainate receptor antagonists) and their physiologically compatible salts can be used for the preparation of drugs for treatment of cancer.
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6794371 |
Aminoalkylenephosphonates for treatment of bone disorders
A method for preventing loss of bone mineral in mammals which method comprises administering to a mammal an amount of an aminoalkylenephosphonate which is effective to prevent or minimize loss of...
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6777445 |
Fullerene pharmaceutical compositions for preventing or treating disorders
The present invention relates to a method for treating a disease, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a fullerene. The diseases...
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6727233 |
Medicinal compositions for treating osseous lesion in multiple myeloma
Pharmaceutical compositions for treating bone lesions in multiple myeloma or pharmaceutical compositions for treating multiple myeloma which contain as an active ingredient a compound having both...
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6716828 |
Compounds, methods and pharmaceutical compositions for treating cellular damage, such as neural or cardiovascular tissue damage
This invention relates to compounds, pharmaceutical compositions, and methods for the treatment or prevention of neural or cardiovascular tissue damage related to cerebral ischemia and reperfusion...
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6706698 |
α-Substituted β-aminoethyl phosphonate derivatives
The present invention relates to novel α-substituted-β-aminoethylphosphonate and α-substituted-β-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a),...
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6699896 |
Oxazole-aryl-carboxylic acids useful in the treatment of insulin resistance and hyperglycemia
This invention provides compounds having the structure wherein A is OR 5 , or R 1 is alkyl, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, pyridyl, R 2 is H, alkyl, or aryl; R 3 and R 4 ...
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6699855 |
Inhibitors of hepatitis C virus NS3 protease
The present invention relates to compounds of Formula (I): wherein A 1 is methylene, ethylene or propylene group and A 2 is N or CR 5 , or stereoisomeric forms, stereoisomeric mixtures, or...
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6683082 |
Bicyclic protein kinase inhibitors
The present invention relates to novel 3-hetero-arylidene-2-indolinone compounds and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are...
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6673781 |
Tricyclic compounds having sPLA2-inhibitory activities
The present invention provides a compound having sPLA 2 inhibiting activity. The compound represented by the formula (I): wherein R 1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20...
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6673780 |
Sulfoxide and bis-sulfoxide compounds and compositions for cholesterol management and related uses
The present invention relates to novel sulfoxide and bis-sulfoxide compounds, compositions comprising sulfoxide and bis-sulfoxide compounds, and methods useful for treating and preventing...
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6656926 |
Phosphoramide compounds
The invention provides a compound of formula I: wherein R 1 , R a , R b , R c , and R d have any of the values defined in the specification, as well as pharmaceutical compositions comprising...
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6645950 |
Benzimidazole vascular damaging agents
Vascular damaging agents composed of substituted 5(6)-substituted benzimidazole-2-carbamates are provided. These agents are useful in the preparation of medicaments for the treatment of diseases...
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6638960 |
Halogenobenzimidazoles and their use as microbicides
New halogenobenzimidazoles of the formula in which A, R 1 , R 2 , R 3 , R 4 and X have the meanings given in the description, and their acid addition salts and metal salt complexes, a process...
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6635626 |
Imidazoquinoxaline protein tyrosine kinase inhibitors
Novel imidazoquinoxalines and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated...
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6596709 |
6-sulphanoyl-3-quinolylphosphonic acid compounds
The invention relates to a compound of formula (I): wherein: X represents chlorine or fluorine or CF 3 , R represents hydrogen or a group and methods for using the same.
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6555536 |
Biologically active 4H-benzo &lsqb 1,4&rsqb oxazin-3-ones
The invention is directed to 4h-benzo[1,4]oxazin-3-ones useful as peroxisome proliferator activated receptor gamma (PPARγ) agonists or antagonists. Pharmaceutical compositions comprising compounds...
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6555528 |
Derivatized biotin compounds and methods of use
An efficient synthesis for the selective and efficient 1′-N derivatization of biotin is reported. The derivatized biotin acts as a stable analog of the carboxyphosphate intermediate in...
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