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8163911 Arylsulfonylaminomethylphosphonic 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...
8163910 Amide-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.
8158797 Oxazolidinone-quinolone hybrid antibiotics  
The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria.
8026388 Process for making 1-hydroxyalkylidene-1,1-biphosphonic acids  
Synthesis of biphosphonate compounds can be advantageously carried out in a solvent/diluent comprising a compound of formula (3) wherein R is hydrogen or a C1-C6 alkyl group; each of R1 is a C1-C6...
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...
7994320 Narcistatin 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...
7893264 Antiviral 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...
7888336 Indole compounds bearing aryl or heteroaryl groups having sphingosine 1-phosphate (S1P) receptor biological activity  
The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful...
7872144 Process for producing biphosphonic acids and forms thereof  
Disclosed herein is a process for producing bisphosphonic acids and salts thereof. The process comprising reacting a carboxylic acid of Formula [I] with phosphorous acid and halophosphorus compound...
7723330 Heterobicyclic pyrazole compounds and methods of use  
Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine...
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.
7709643 Synthesis 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...
7514556 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 ...
7462609 Narcistatin 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...
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...
7423049 Inhibitors 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...
7420059 HMG-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, and n are as defined above, which compounds are HMG CoA...
7411087 Process 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...
7361761 Process 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...
7358361 Biophosphonate 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...
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,...
7332603 Preparation 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...
7312219 Heteroaromatic 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.
7312326 Fluorescent 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...
7253180 Pre-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...
7247726 Compounds 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 c...
7060290 Phosphocholine 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...
7030103 Sulfonamidomethyl 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 ...
7019139 Quinolinones 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, R9a, AK, p, q, r and X are as defined herein,...
7009054 Quinolines 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.
6903111 Isoquinuclidine 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 a...
6893668 Process 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)...
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...
6825181 Aminoisoquinoline 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...
6818632 3-(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...
6812345 HMG-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...
6727361 Phosphino 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...
6720281 Chiral 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...
6660860 Process for the selective oxidation of alcohols using readily removable nitroxyl radicals  
The invention relates to a process for the selective oxidation of alcohols to ketones or to aldehydes by means of an alkali hypohalite under alkaline conditions, which comprises carrying out the...
RE38333 Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability  
Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure —OC(R2)2OC(O)X(R)a, wherein R2 i...
6653296 Antiretroviral enantiomeric nucleotide analogs  
Resolved enantiomers of the formula (IA) and (IB) wherein B is a purine or pyrimidine base or aza and/or deaza analogs thereof are useful in antiviral pharmaceutical compositions to treat...
6605612 Cardioprotective phosohonates and malonates  
The present invention provides for pyridoxine phosphonate analogues such as, for example, ((2-methyl-3-hydroxy-4-hydroxymethyl-5-pyridyl)alkylphosphon ates, and and...
6576760 Processes for synthesis of cyclic and linear polyamine chelators containing N-monosubstituted coordinating arms  
Polyamines containing at least two nitrogen atoms monosubstituted with pendant arms capable of coordinating metal cations, or with precursors of such pendant arms, all nitrogen atoms of the...
6531484 Pyrrolidine modulators of CCR5 chemokine receptor activity  
Pyrrolidine compounds of Formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, j, k, 1, m, and n are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor...
6506734 20(S) camptothecin glycoconjugates  
The present invention relates to glycoconjugates of 20(S)-camptothecin, in which a 3-O-methylated β-L-fucose unit is linked to the 20-hydroxyl group of a camptothecin derivative via a ...
6498151 Aryldifluoromethylphosphonic 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. The invention also encompasses pharmaceutical compositions and...
6492335 Glycoconjugates from modified camptothecin derivatives (20-O-linkage)  
The present invention relates to glycoconjugates of camptothecin derivatives in which at least one carbohydrate component is linked via suitable spacers with the 20-hydroxyl group of a camptothecin...
6489476 Heteroaromatic compounds containing a phosphonate group that are inhibitors of fructose-1,6-bisphosphatase  
FBPase inhibitors of the formula I and X are useful in the treatment of diabetes and other conditions associated with elevated blood glucose or excess glycogen storage.
6472406 Sulfonamidomethyl phosphonate inhibitors of beta-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 ...
6410505 Dimeric non-azo naphthalimides and uses for the same  
A class of predominantly hydrophilic 1,8-naphthalimide dyes. The dye contains at least two 1,8-naphthalimide ring systems, joined by a spacer moiety. Each of the 1,8-naphthalimide ring system has a...
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