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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...
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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.
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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.
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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...
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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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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...
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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...
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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...
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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...
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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...
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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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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...
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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 ...
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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...
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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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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...
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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...
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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...
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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...
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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...
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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,...
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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...
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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.
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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...
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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...
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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...
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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...
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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 ...
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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,...
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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.
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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...
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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)...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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 ...
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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...
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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...
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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.
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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 ...
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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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