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Class 514/94 - Diazoles (including hydrogenated)


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the organo-phosphorus compound contains
No. of patents: 170
Last issue date: 05/15/2012


1          
NumberTitleIssue Date
8178513Heterocyclic aspartyl protease inhibitors
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W, U, X, R1, R2, R3, and R4 are as defined he...
05/15/2012
8003626Pyrazole-4-carboxamide derivatives as microbiocides
Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides. ...
08/23/2011
8003625Phosphoramidate alkylator prodrugs
Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents. ...
08/23/2011
7977323C-C-alkyl-imidazole-bisphosphonates
C2-C5-Alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, ...
07/12/2011
7947665LPA receptor agonists and antagonists and methods of use
Disclosed are compounds according to formula (I) as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA receptors; such methods including inhi...
05/24/2011
7763596Selective glucocorticoid receptor agonists
This invention is directed to a method for treating an inflammatory condition, treating haematological and other malignancies, causing immunosuppression, or preventing or treating transplant rejection in man or other animals which comprises administering to a patien...
07/27/2010
7687481Cannabinoid receptor antagonists/inverse agonists useful for treating obesity
The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders. ...
03/30/2010
73549111,3-benzodioxol compound and use of same
Containing the 1,3-benzodioxol compound represented by the formula (I): together with a pesticidal active ingredient in a pesticidal composition enhances a pest control effect of the pesticidal composition. ...
04/08/2008
7238709Therapeutic carbamates
This invention relates to hindered carbamate derivatives that are muscarinic receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds. ...
07/03/2007
7235666Process for the preparation of sodium fosphenytoin
Phosphoric acid diester 2,5-dioxo-4,4-diphenylimidazolidin-1-ylmethyl esters, both of whose ester groups can be selectively cleaved, are obtained by converting 3-(hydroxymethyl)-5,5-diphenylimidazolidine-2,4-dione to an alkylsulfonate or arylsulfonate and reacting t...
06/26/2007
7217704LPA receptor agonists and antagonists and methods of use
The present invention relates to compounds according to formula (I) as disclosed herein as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA...
05/15/2007
7211267Methods of treating acne
A method of treating acne in a human in need thereof comprising administering systemically to said human a tetracycline compound in an amount that is effective to treat acne but has substantially no antibiotic activity, without administering a bisphosphonate compoun...
05/01/2007
7208481Aminodiphosphonate 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 states. ...
04/24/2007
7172873Methods of detecting early renal disease in animals
The present invention provides a method for the detection of early renal disease in animals. The method includes the steps of (a) obtaining a sample from an animal to be tested and (b) determining the amount of albumin in the sample. An amount of albumin in the rang...
02/06/2007
7105556Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2
09/12/2006
7030103Sulfonamidomethyl phosphonate inhibitors of β-lactamase
The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel β-lactamase inhibitors, which are structurally unrelated to the natural product and...
04/18/2006
7014858Use methods of treating acne and telangiectasia
A method of treating telangiectasia in a human in need thereof comprising administering to said human a tetracycline compound in an amount that is effective to treat telangiectasia, but has substantially no antibiotic activity. ...
03/21/2006
6965033Bisamidate phosphonate prodrugs
Novel bisamidate phosphonate prodrugs of FBPase inhibitors of the Formula IA: and their use in the treatment of diabetes and other conditions associated with elevated blood glucose. ...
11/15/2005
6919322Phenyl Phosphonate 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. ...
07/19/2005
6762227Inhibition of marine biofouling of surfaces
The use of an aromatic compound substituted with at least one heterocyclic amine and possibly additional substituents, such as medetomidine and clonidine, or a functionally analogous derivative thereof, as an agent for the inhibition of marine biofouling on a surfac...
07/13/2004
6756391Antiviral compounds
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 activity in standard tests against HIV-infected cells as well as othe...
06/29/2004
6703368Peptide-containing ଱-ketoamide cysteine and serine protease inhibitors
This invention relates to peptide-containing ଱-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same....
03/09/2004
6514952Hydantoin derivatives as inhibitors of leucocyte adhesion and as VLA-4 antagonists
Compounds of the formula I ##STR1## in which B, D, E, R, W, Y, Z, b, c, d, e, f, g and have the meanings indicated in the claims, are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 which belongs ...
02/04/2003
6500811Sulfonylaminophosphinic and sulfonylaminophosphonic acid derivatives, methods for their preparation and use
Compounds of the formula I ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading enzymes is involved....
12/31/2002
6498151Aryldifluoromethylphosphonic acids with sulfur-containing substituents as PTP-1B inhibitors
The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. ##STR1## The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated d...
12/24/2002
6492410Combinations of protein farnesyltransferase and HMG CoA reductase inhibitors and their use to treat cancer
Novel combinations of inhibitors of protein farnesyltransferase enzymes and HMG CoA reductases enzymes are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in preventing or treating cancer, re...
12/10/2002
6425881Therapeutic mixture useful in inhibiting lesion formation after vascular injury
Vessels are treated with a mixture of L-arginine and an agent which enhances the biotransformation of L-arginine into NO. The incidents associated with restenosis are expected to be substantially reduced and prevented providing for a reduced incidence of ...
07/30/2002
6352985Benzimidazole compounds
A benzimidazole compound represented by the formula (I): ##STR1## wherein R3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable...
03/05/2002
6300356Method for decreasing QT dispersion or inhibiting the progression of QT dispersion with an angiotensin II receptor antagonist
Angiotensin II receptor antagonists are useful for decreasing QT dispersion or inhibiting the progression of QT prolongation in patients. Also disclosed is a method for monitoring the reduction in die risk of experiencing an adverse cardiac event, such as...
10/09/2001
6201002Method for reducing mortality with an angiotensin II antagonist
Angiotensin II receptor antagonists are useful in reducing and preventing mortality and sudden cardiac death in symptomatic heart failure patients. Losartan potassium has been shown to reduce mortality and sudden cardiac death in this patient population. ...
03/13/2001
6200961Concentrates of organophosphorous insecticides
A low volatile organic compound co-solvent system is disclosed for preparing emulsion concentrates of low melting organophosphorous insecticides wherein the bioefficacy of the insecticide active is significantly enhanced. The co-solvent system comprises a...
03/13/2001
6187752Method for treating schizophrenia employing an ace inhibitor
A method is provided for treating schizophrenia in a mammalian species by administering an ACE inhibitor, such as captopril, alone or with a neuroleptic such as cholecystokinin, fluphenazine or haloperidol....
02/13/2001
6162820Method for removing parasites and in particular ectoparasites of vertebrates, in particular of mammals, and compositions for the implementation of this method
Methods for removing parasites and in particular ectoparasites of vertebrates, in particular of mammals, and compositions for the implementation of this method. Methods for removing parasites of vertebrates, and in particular arthropods, mainly insects an...
12/19/2000
6121296Transition-state inhibitors for nucleoside hydrolase and transferase reactions
This invention is directed to transition-state analog compounds and to the use of said compounds as inhibitors of nucleoside hydrolase and transferase enzyme activity of parasites. This invention is further directed to the use of said compounds to treat i...
09/19/2000
5998390Combination of bisphosphonate and tetracycline
Tissue-destructive conditions related to excess proteinase activity in a biological system are treated or prevented by administering to the system a composition which combines a tetracycline and a bisphosphonate in synergistic proteinase inhibiting amount...
12/07/1999
5998447Heterocycles as inhibitors of leucocyte adhesion and as VLA-4 antagonists
Compounds of the formula I ##STR1## in which B, D, E, R, W, Y, Z, b, c, d, e, f, g and have the meanings indicated in the claims, are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 which belon...
12/07/1999
5972915Pesticide containing a synergistic combination of active ingredients
A pesticide comprising an active ingredient combination consisting of a) tetrahydro-3,5-dimethyl-1,3,5-thiadiazine-2-thione of the formula ##STR1## and b) O-(O-ethyl-S-n-propylphosphoryl)-O-(N-methylcarbamoyl)pyrocatechol of the formula ##STR2## ...
10/26/1999
5958905Phosphoramidates, phosphinic amides and related compounds and the use thereof to modulate the activity of endothelin
Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: ##STR1...
09/28/1999
5952305Methods for reducing risk of repeat myocardial infarction and increasing survival in heart attack victims
The invention involves a method for treating a human survivor of a heart attack and provides further improvement in survival following the heart attack by the early initiation and long-term administration of a renin-angiotensin system inhibitor, preferabl...
09/14/1999
5914351Anti-viral aromatic hydrazones
Compounds of the formula ##STR1## wherein Q is a hydrazone derivative; R1 is hydrogen, halogen, alkyl or alkoxy; R2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; a...
06/22/1999
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