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Class 546/23 - Polycyclo ring system having the six-membered hetero ring as one of the cyclos


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the six-membered hetero ring is one of
No. of patents: 312
Last issue date: 04/24/2012


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NumberTitleIssue Date
8163911Arylsulfonylaminomethylphosphonic acid derivatives, the preparation thereof and the use thereof as pharmaceutical compositions
The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a me...
04/24/2012
8163910Amide-substituted xanthene dyes
The present invention provides amide-substituted xanthene fluorescent dyes and reagent for the introduction of phosphonate or sulfo groups into the fluorescent dyes. ...
04/24/2012
7994320Narcistatin prodrugs
The present invention provides prodrugs derived from the sparingly soluble anticancer isocarbostyril narciclasine, a component of various Narcissus species, said prodrugs having potential for use against animal and human cancers. Also disclosed is an efficien...
08/09/2011
7893264Antiviral phosphinate compounds
The invention is related to anti-viral phosphinate compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. ...
02/22/2011
7709643Synthesis of sodium narcistatin and related compounds
The present invention involves use of the compounds narciclasine (2a) and 7-deoxy-narciclasine (2c), which are obtained via isolation from the medicinal plant species Narcissus (Amaryllidaceae), as precursors in a novel synthesis method in which each of these...
05/04/2010
7514556Inhibitors 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...
04/07/2009
7423049Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceut...
09/09/2008
7420059HMG-CoA reductase inhibitors and method
Compounds are provided having the following structure and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, U, V, W, Y...
09/02/2008
7411087Process for preparation of bisphosphonic acid compounds
The present invention provides a novel process for preparation of bisphosphonic acids or salts thereof, e.g. alendronic acid, by reacting a carboxylic acid, phosphorous acid and a halophosphorous compound in a water miscible neutral solvent. ...
08/12/2008
7361761Process for the preparation of bisphosphonic acid
The present invention is to relate an improved process using anisole as solvent for the preparation of compound of formula (I) and its pharmaceutically acceptable salts thereof. wherein R represents —NR1R2...
04/22/2008
7358361Biophosphonate 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...
04/15/2008
7351830Pancratistatin cyclic phosphate prodrugs and phenpanstatin cyclic phosphate prodrugs
Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexyl-carbodiimide in pyridine followed by cation exchange chromatographic procedures was found to provide an efficient mute to a new series (3
04/01/2008
7351698Androgen 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, as well as in a method of agonizing the androgen receptor in a patien...
04/01/2008
7332603Preparation of biphosphonic acids and salts thereof
A process for preparing alendronate sodium includes the reaction of gammabutyric acid with phosphorous acid and phosphorus trichioride and subsequent treatment with an aqueous solution of an alkali metal hydroxide, in which the reaction is conducted in liquid ionic ...
02/19/2008
7312219Heteroaromatic inhibitors of fructose 1,6-bisphosphatase
Novel FBPase inhibitors of the formula I and X are useful in the treatment of diabetes and other conditions associated with elevated blood glucose. ...
12/25/2007
7312326Fluorescent labeled nucleotide derivatives
Fluorescent labeled reporter compounds having a modified cyanine dye that is coupled to a nucleotide derivative through a linker are disclosed. The compounds are useful for nucleic acid sequence analysis. The fluorescent labeled reporter compounds are ring-locked cy...
12/25/2007
7253180Pre-organized tricyclic integrase inhibitor compounds
Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. A1 and A2 are moieties forming a five, six, or...
08/07/2007
7247726Compounds for generating chemiluminescence with a peroxidase
Novel compounds comprising a C—C double bond substituted at one carbon with two sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence rapidly by reaction with a peroxidase enzyme and a pe...
07/24/2007
7119104Activator of peroxisome proliferator-activated receptor delta
A compound represented by the formula (I) or a salt of the compound, and a PPAR-δ activator which contains the compound or salt as the active ingredient: (wherein A represents O or S; B
10/10/2006
7083986Near infrared chemiluminescent acridinium compounds and uses thereof
A method for the detection or quantitation of an analyte in a biological sample is disclosed. The method comprises the steps of selecting a biological sample suspected of containing a target analyte and binding the target analyte in the sample to a binding partner c...
08/01/2006
7060290Phosphocholine linked prodrug derivatives
Disclosed are compounds of general formula (I) that function as prodrugs, thereby increasing bioavailabilities of the linked therapeutic agents, wherein the LINKER is (i) substituted or unsubstituted alkyl, (ii) substituted or unsubstituted alkenyl, (iii) substitute...
06/13/2006
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
7019139Quinolinones and uses thereof
The invention relates to compounds of the general formula (and pharmaceutically acceptable derivatives thereof): in which RA, RB, RC, RD, R5, R7, R9...
03/28/2006
7009054Quinolines and uses thereof
This invention relates to compounds of the general formula: in which RA, RB, RC and RD are as defined herein, and to their preparation and use. ...
03/07/2006
7001911Fused cyclic modulators of nuclear hormone receptor function
The invention pertains to fused cyclic compounds having the formula, wherein G is an optionally substituted aryl or heterocyclo, L is an optional linker, M is a bond, O, CR7R7′ or NR10
02/21/2006
6962996Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceut...
11/08/2005
6921756Inhibitors of β-lactamase
The invention 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...
07/26/2005
6903111Isoquinuclidine derivative process for producing the same, and medicinal composition containing the same
An isoquinuclidine derivative represented by the following general formula (I): (I) [wherein A1 is methylene or carbonyl]: R1 is hydrogen or methyl: R2 is —(CH2)n-A2-Ph (n is an integer of 0 to 3 an...
06/07/2005
6893668Process for isolation of anticancer agent camptothecin from Nothapodytes foetida
The present invention relates to an improved and economical process for the isolation of anticancer agent Camptothecin from the twigs and stem of Nothapodytes foetida using hot extraction 20(S) Camptothecin is an alkaloid, which contains a pentacyclic ring sy...
05/17/2005
6884791Inhibitors 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...
04/26/2005
6872828Compounds for generating chemiluminescence with a peroxidase
Novel compounds comprising a C—C double bond substituted at one carbon with two sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence rapidly by reaction with a peroxidase enzyme and a pe...
03/29/2005
6867215Cardioprotective phosphonates and malonates
The present invention provides for pyridoxine phosphonate analogues such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)alkylphosphonates, and (2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)azaalkylphosphonates) and to pyridoxine malonate analogues, ...
03/15/2005
6858733Compounds for generating chemiluminescence with a peroxidase
Novel compounds comprising a C—C double bond substituted at one carbon with two sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence rapidly by reaction with a peroxidase enzyme and a pe...
02/22/2005
6841559Pyridinones 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 by which these derivatizations occur is described. Two regioselectiv...
01/11/2005
6825181Aminoisoquinoline derivatives
Aminoisoquinoline derivatives of the following formulae or analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an excellent effect of inhibiting activated blood-coagulation factor X, and they are useful as anticoagulants ...
11/30/2004
68186323-(anilinomethylene)oxindoles
Compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims, exhibit protein tyrosine kinase and protein serin/threonine kinase inhibitory activity. ...
11/16/2004
6812345HMG-CoA reductase inhibitors and method
Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hyperchol...
11/02/2004
6759535Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceut...
07/06/2004
6727361Phosphino substituted pyridine amine ligands
New ligands, compositions, metal-ligand complexes and arrays with pyridyl-amine ligands are disclosed that catalyze the polymerization of monomers into polymers. Certain of these catalysts with hafnium metal centers have high performance characteristics, including h...
04/27/2004
6720281Chiral phosphorus ligands and the use thereof in the production of optically active products
The present invention relates to novel chiral phosphorus compounds which can be readily prepared from quinoline derivatives as inexpensive starting compounds and have the general formula I wherein R1, R2
04/13/2004
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