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Class 514/89 - Hetero ring is six-membered and includes only one ring nitrogen


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the organo-phosphorus compound contains
No. of patents: 502
Last issue date: 12/06/2011


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NumberTitleIssue Date
8071573Bisphosphonate 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 context of functional assays such as Leishmania major farnesyl di...
12/06/2011
8012949Bisphosphonate 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 are capable of selectively inhibiting one or more of farnesyl diphosph...
09/06/2011
7964583Salts 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+ represents an am...
06/21/2011
7960365Compounds 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 (1C-4C)alkyl; R
06/14/2011
7875597Treatment 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 of bisphosphonate. ...
01/25/2011
7786097Tricyclic 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 treatment of conditions mediated ...
08/31/2010
7781419Use 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 in the treatment of otosclerosis. Particularly, the method involves ad...
08/24/2010
7745422Bisphosphonate 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 context of functional assays such as Leishmania major farnesyl di...
06/29/2010
7704977Solid 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 underlying circulation. Preferably, the enhancer is a medium chain fat...
04/27/2010
7678778Salts 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+ represents an am...
03/16/2010
7618953Amorphous 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. ...
11/17/2009
7612050Drug 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 he used to prevent the onset of osteonecrosis and/or osetonecrosis dissecans and any complications associated with both diseases. ...
11/03/2009
7598231Tricyclic compound, 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 treatment of conditions mediated ...
10/06/2009
7589081Nitrogen-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 compounds. ...
09/15/2009
7563782T-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 and R2
07/21/2009
7541346Pancratistatin 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 found to provide an efficient route to a new series (3b-3d) of promising ...
06/02/2009
7511028Use 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 in the treatment of otosclerosis. Particularly, the method involves ad...
03/31/2009
7498319Phosphinic acid derivatives
The present invention relates to phosphinic acid derivatives as GABAB antagonists, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them. ...
03/03/2009
7468359Compositions 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 ingredient in these compositions is an alpha-oxo- or alpha-thioxophos...
12/23/2008
7442689Cardioprotective phosphonates and malonates
The present invention provides for pyridoxine phosphonate analogues, pharmaceutical compositions, and methods for treatment of cardiovascular and related diseases. ...
10/28/2008
7425549Drug 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 complications associated with both diseases. ...
09/16/2008
7423012Phosphinyloxy, 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 can be used in the preventio...
09/09/2008
7410956Caspase 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 caspase inhibitors from these compounds through selective bond cleavage. ...
08/12/2008
7403883Three-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 a passageway that substantially mimics the size, shape, and structure...
07/22/2008
7371739Aryl 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. ...
05/13/2008
7361666Heterocyclic 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 cellular receptors, including opiate receptors, other G-protein-couple...
04/22/2008
7358360Risedronate sodium having a very low content of iron
The present invention relates to a method of making risedronate sodium substantially free of iron including the steps of refluxing, especially with mechanical agitation, a combination of risedronic acid, a sodium base, especially sodium hydroxide, and an iron-reduci...
04/15/2008
7354895Phosphinyloxy, 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 can be used in the preventio...
04/08/2008
7348440Mitotic kinesin inhibitors
The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comp...
03/25/2008
7348318α-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 group or the like; W, X, Y an...
03/25/2008
7342122Bisphosphonate complexes
Bisphosphonate compounds are disclosed, particularly bisphosonate conjugates useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis. ...
03/11/2008
7320993Aryl-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 several-fold unsaturated hydrocarbon residue in the carboxylic acid group, ...
01/22/2008
7294637Method of treating addiction or dependence using a ligand for a monamine receptor or transporter
One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substitute...
11/13/2007
7288535Methods and compositions for stimulating bone growth using nitric oxide releasing bisphosphonate conjugates
The invention relates to compositions and methods for use in treating skeletal system disorders in a vertebrate at risk for bone loss, and in treating conditions that are characterized by the need for bone growth, in treating fractures, and in treating cartilage dis...
10/30/2007
7288588Polymer binder for intumescent coatings
The present invention discloses a copolymer composition for use in or as a polymeric binder in an intumescent coating, said copolymer composition comprising a blend of a Newtonian copolymer and of a reticulated copolymer, wherein the Newtonian copolymer is comprised...
10/30/2007
7276604Crystalline form of the sodium salt of 3-pyridyl-1-hydroxyethylidene-1,1-bisphosphonic acid
The present invention relates to a crystalline, hydrated form of the sodium salt of 3-pyridyl-1-hydroxyethylidene-1,1-bisphosphonic acid. The hydrate contains from 6.4 up to 22 weight % of sodium and 15 up to 23 weight % of crystalline water if the sodium content is...
10/02/2007
7268124Geranylgeranyl 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. ...
09/11/2007
7259143Method of extending the dose range of vitamin D compounds
Inhibitors of bone calcium resorption are administered to allow high doses of vitamin D compounds or mimetics to be given with the intent of treating non-calcium related diseases such as cancer, psoriasis, and autoimmune disease without the dangers of calcification ...
08/21/2007
7256159Fluid loss reducer for high temperature high pressure water based-mud application
The present invention concerns a water-based drilling mud for utilization in the drilling of oil wells comprising an aqueous phase wherein the aqueous phase contains an oil soluble polymer in the form of a gel as a fluid loss reducer. The subject invention further r...
08/14/2007
7241745Pyridyl 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 well as their m...
07/10/2007
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