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8071573 |
Bisphosphonate compounds and methods for bone resorption diseases, cancer, bone pain, immune disorders, and infectious diseases
Bisphosphonate compounds and related methods of making and using are disclosed, including pyridinium-1-yl, quinolinium-1-yl, and related compounds. The activity of compounds is disclosed in the...
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8044037 |
Modified phosphocalcic compound, injectable composition containing same
A phosphocalcic compound modified by a gem-bisphosphonic acid or one of its salts, a method for preparing same, as well as its use for preparing an injectable composition. The modified...
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8012949 |
Bisphosphonate compounds and methods with enhanced potency for multiple targets including FPPS, GGPPS, and DPPS
The disclosure provides, inter alia, novel bisphosphonate compounds and methods of making and using such compounds. In certain embodiments, compounds of the invention include bisphosphonates that...
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8008329 |
Method of treating or preventing osteoporosis comprising administering to a patient in need thereof an effective amount of pharmacuetical composition comprising benzamidine derivative or it's salt, and bisphosphonate
The present invention provides a method of treating or preventing osteoporosis comprising administering to a patient in need thereof an effective amount of pharmaceutical composition comprising...
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8003624 |
Functionally selective ALPHA2C adrenoreceptor agonists
In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical ...
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7989434 |
Heterocyclic self-immolative linkers and conjugates
The present invention provides heterocyclic linker compounds useful for linking drug moieties to ligands. The compounds also include drug-ligand conjugates comprising a ligand capable of targeting...
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7973083 |
Pesticidally active compounds
A pesticidally active combination comprising an HPPD-inhibiting herbicide in the form of an agrochemically acceptable salt and an insecticide is disclosed, provided that the HPPD inhibiting...
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7964583 |
Salts of isophosphoramide mustard and analogs thereof as anti-tumor agents
The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula wherein A+...
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7960365 |
Compounds with medicinal effects due to interaction with the glucocorticoid receptor
The invention provides for compounds having the structure according to the formula I wherein: X is a carbon or nitrogen atom; Ar is phenyl or heteroaromatic ring; R1 is hydrogen, halogen, CN or...
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7960354 |
Synergistic pesticidal mixtures
Synergistic pesticidal mixtures are provided.
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7875597 |
Treatment of spinal mechanical pain
The invention is directed to a method of treating chronic spinal mechanical pain by intravenous administration to a subject in need of chronic spinal mechanical pain relief of an effective amount...
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7807659 |
Caspase inhibitors and uses thereof
The present invention relates to novel classes of compounds of formula I which are caspase and TNF-alpha inhibitors. This invention also relates to pharmaceutical compositions comprising these...
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7786097 |
Tricyclic compounds, compositions and methods
The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the...
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7781419 |
Use of bisphosphonates for otosclerosis
A method of treating otosclerosis in a human in need thereof by administering a bisphosphonate in a defined dosing schedule. The invention demonstrates an effective response and sustained benefit...
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7772198 |
CFTR channel modulators
The invention concerns pharmaceutical formulas designed for the treatment of diseases related to CFTR channel dysfunction, such as cystic fibrosis, asthma or diarrhoea. These formulas contain a...
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7767204 |
Method and composition for protecting neuronal tissue from damage induced by elevated glutamate levels
A method of reducing extracellular brain glutamate levels. The method comprises administering to a subject in need thereof a therapeutically effective amount of an agent capable of reducing blood...
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7749984 |
Computer-based model for identification and characterization of non-competitive inhibitors of nicotinic acetylcholine receptors and related ligand-gated ion channel receptors
A computer readable medium holding data of a molecular model of a ligand-gated ion channel receptor and/or a computer system for modeling said receptor are provided by the instant invention. The...
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7745422 |
Bisphosphonate compounds and methods for bone resorption diseases, cancer, bone pain, immune disorders, and infectious diseases
Bisphosphonate compounds and related methods of making and using are disclosed, including pyridinium-1-yl, quinolinium-1-yl, and related compounds. The activity of compounds is disclosed in the...
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7718633 |
Prodrugs of HIV protease inhibitors
A compound of the formula is disclosed as a prodrug of an HIV protease inhibitor. Methods and compositions for inhibiting HIV protease activity and treating HIV infection are also disclosed.
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7704977 |
Solid oral dosage form containing an enhancer
The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to enhance intestinal delivery of the bisphosphonate to the...
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7691871 |
Multivitamin syrup for children or young adults
The invention relates to an improved pharmaceutical or dietary composition in form of an aqueous syrup, consisting essentially of (a) vitamins recommended for consumption by children or young...
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7678778 |
Salts of isophosphoramide mustard and analogs thereof as anti-tumor agents
The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula wherein A+...
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7645459 |
Dosage forms of bisphosphonates
Oral dosage forms of a bisphosphonate comprised of a safe and effective amount of a pharmaceutical composition comprising a bisphosphonate, a chelating agent, and, means for effecting delayed...
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7635708 |
Methods and pharmaceutical compositions for inhibiting tumor cell growth
The present invention is based on the finding that activation of PPARγ plays a key role in inducing growth arrest and differentiation of certain actively proliferating cells. We show that ...
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7618953 |
Amorphous forms of risedronate monosodium
The monosodium salt of 3-pyridyl-1-hydroxyethylidene-1,1-bisphosphonic acid in new amorphous forms, methods of preparation and a pharmaceutical formulation.
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7589081 |
Nitrogen-containing monodentate phosphines and their use in catalysis
The present invention relates to novel nitrogen-containing monodentate phosphane ligands of formula (I) and to their use in catalytic reactions, especially in the improvement of haloaromatic...
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7563782 |
T-type calcium channel blocker
There is provided a T-type calcium channel blocker that is optically active 1,4-dihydropyridine compound, a pharmaceutically acceptable salt thereof or a solvate thereof, of formula (1) wherein R1...
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7550488 |
Application methods to rapidly alter disease and injury states using molecular transport of B6
The present invention discloses methods of application employing B5/B6 vitamins in molecular transport creams or gels to deliver B6 in a high dose to bring about therapeutic ways in human or mammal...
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7541346 |
Pancratistatin cyclic phosphate prodrugs and phenpanstatin cyclic phosphate prodrugs
Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexylcarbodiimide in pyridine followed by cation exchange chromatographic procedures was...
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7521436 |
Modified phosphocalcic compound, injectable composition containing same
The invention concerns a phosphocalcic compound modified by a gem-bisphosphonic acid or one of its salts, a method for preparing same, as well as its use for preparing an injectable composition....
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7511028 |
Use of bisphosphonates for otosclerosis
A method of treating otosclerosis in a human in need thereof by administering a bisphosphonate in a defined dosing schedule. The invention demonstrates an effective response and sustained benefit...
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7498319 |
Phosphinic acid derivatives
The present invention relates to phosphinic acid derivatives as GABAB antagonists, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.
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7494983 |
Ophthalmic compositions for treating ocular hypertension
This invention relates to potent potassium channel blocker compounds of structural Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated...
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7468359 |
Compositions comprising oxophosphonate-based metalloproteinase inhibitors
The present invention relates to compositions useful for treating or controlling disease states or conditions associated with zinc containing proteinases, especially metalloproteinases. The active...
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7459444 |
Inhibitors of chymase
The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and...
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7425549 |
Drug for the treatment of osteonecrosis and for the management of patients at risk of developing osteonecrosis
A bisphosphonate for the treatment of osteonecrosis and/or osteonecrosis dissecans. The drug may further be used to prevent the onset of osteonecrosis and/or osteonecrosis dissecans and any...
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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 thus...
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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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7403883 |
Three-dimensional in-vitro spinal models and methods of analyzing substance distribution therein
An in-vitro model apparatus of a human spine and methods for detecting and analyzing substance distribution patterns therein. In one embodiment, the model apparatus includes a column body defining...
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7371739 |
Aryl fructose-1,6-bisphosphatase inhibitors
Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
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7348318 |
α-Amino-N-(diaminophosphinyl)lactam derivatives
There are disclosed a novel α-amino-N-(diaminophosphinyl)lactam derivative represented by general formula (1): wherein, for example, A is a hydrogen atom or a substituent such as a lower alkyl ...
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7320993 |
Aryl-substituted pyridylalkane, alkene, and alkine carboxamides useful as cytostatic useful as cytostatic and immuosuppressive agents
The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or...
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7268124 |
Geranylgeranyl pyrophosphate synthase inhibitors
The invention provides novel pyrophosphate synthase inhibitors of formula I as well as compositions comprising such inhibitors and methods for their use.
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7241745 |
Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as...
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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 are each as defined in...
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7208481 |
Aminodiphosphonate apolipoprotein E modulators
The present invention relates to methods of use of aminodiphosphonate to modulate apolipoprotein E levels and the use of such compounds in therapy, including cardiovascular and neurological disease...
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7192905 |
Organophosphate insecticide synergists for fly and tick control
Combination of a cytochrome P450 monooxygenase inducer with an organophosphate pesticide (insecticide or acaracide) provides effective control of ticks and flies, particularly against...
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7129228 |
Heterocyclic analgesic compounds and methods of use thereof
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various...
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7109184 |
Phosphate transport inhibitors
Disclosed is a phosphate transport inhibiting compound represented by Structural Formula (I): R1 and R2 are independently —H, an electron withdrawing group or a C1–C10 alkyl group.Y is a cov...
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7071175 |
Pyridine mercapto carboxylic acids 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 thus...
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