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7601845 |
Optically detectable organophosphonates
The invention relates to compounds having general formula I
in which X represents an optically detectable moiety, n is an integer with 1≦n≦20, R 1 is an unbranched or branched alkyl group...
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7589211 |
Zoledronic acid crystal forms, zoledronate sodium salt crystal forms, amorphous zoledronate sodium salt, and processes for their preparation
The invention relates to polymorphs of zoledronic acid and zoledronate sodium salts, amorphous zoledronate sodium salt, processes for making the polymorphs and amorphous zoledronate sodium salt,...
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7582768 |
Zoledronic acid crystal forms, zoledronate sodium salt crystal forms, amorphous zoledronate sodium salt, and processes for their preparation
The invention relates to polymorphs of zoledronic acid and zoledronate sodium salts, amorphous zoledronate sodium salt, processes for making the polymorphs and amorphous zoledronate sodium salt,...
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7557095 |
Therapeutic compounds
Disclosed herein is a compound having a structure
or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are...
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7550448 |
Therapeutic compounds
Disclosed herein is a compound having a structure
or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also...
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7521436 |
Modified phosphocalcic compound, injectable composition containing same
The invention concerns a phosphocalcic compound modified by a gem-bisphosphonic acid or one of its salts, a method for preparing same, as well as its use for preparing an injectable composition....
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7479502 |
2-(2-hydroxybiphenyl-3-yl)-1H-benzoimidazole-5-carboxamidine derivatives as factor VIIA inhibitors
The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these...
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7435827 |
Zoledronic acid crystal forms, zoledronate sodium salt crystal forms, amorphous zoledronate sodium salt, and processes for their preparation
The invention relates to polymorphs of zoledronic acid and zoledronate sodium salts, amorphous zoledronate sodium salt, processes for making the polymorphs and amorphous zoledronate sodium salt,...
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7427636 |
Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
The invention is related to phosphorus substituted IMPDH inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as...
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7410956 |
Caspase 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...
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7361786 |
Bisphosphines as bidentate ligands
The present invention relates to ligands of the general formula (I).
In addition, a process for the production thereof and the use thereof are demonstrated.
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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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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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7329758 |
Imidazolidine-based metal carbene metathesis catalysts
The present invention relates to novel metathesis catalysts with an imidazolidine-based ligand and to methods for making and using the same. The inventive catalysts are of the formula
wherein:
...
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7323572 |
Process for controlling the hydrate mix of a compound
This invention relates to a process for controlling the hydrate mix of a compound, or a composition comprising the compound, the compound being capable of forming a plurality of hydration forms of...
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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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7304163 |
Benzotriazole-1-yl-N-oxy phosphonium coupling agent
Novel phosphonium salts of benzotraizoles, which are highly reactive coupling agents, and are particularly useful in peptide synthesis, are disclosed. Further disclosed is a process of preparing...
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7253154 |
Substituted thiazolopyrimidines as xanthine oxidase inhibitors
The invention relates to compounds of the following formula (I) or their salts:
in which R 1 represents OR 4 or others, in which R 4 is an alkyl group having 1-8 carbon atoms which may have...
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7241790 |
Compounds active in spinigosine 1-phosphate signaling
The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor...
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7235666 |
Process 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...
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7205404 |
Phosphorus-containing prodrugs
Novel cyclic phosphoramidate prodrugs of drugs of formula I
in their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are...
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7141672 |
Oxazole-aryl-carboxylic acids useful in the treatment of insulin resistance and hyperglycemia
This invention provides compounds of Formula I having the structure
or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance...
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7112684 |
Compounds and methods for fluorescent labeling
Dye reagents useful in labeling biological materials are provided along with methods for their use.
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7109186 |
HIV integrase inhibitors
The present invention describes novel compounds of Formula I which inhibit HIV integrase. The invention also describes compositions and treatments of AIDS or ARC by using these compounds
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7081536 |
Isoxazoline derivatives as P N ligands
The invention relates to novel ligands of the phosphanylbenzothiophenyl-dihydroisoxazoline, phosphanyl-dihydrooxazolyl-indole and phosphanyl-dihydrooxazolyl-benzofuran type, especially compounds of...
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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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6977302 |
Triazole derivatives useful in therapy
The invention provides compounds of formula I,
R 1 —OP(O)(OH) 2 I
wherein...
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6951944 |
Production of imidazole derivatives and novel intermediates of the derivatives
An improvement in the production of imidazole derivatives including histamine H 3 agonist immepip and histamine H 3 antagonist VUF4929. Desired imidazole derivatives can be easily obtained in...
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6906006 |
N-arly-substituted nitrogen-containing heterocycles, processes and novel intermediates for their preparation, and their use as herbicides and plant growth regulators
Substituted triazolinone compounds of the formula:
wherein the variables R 1 , R 2 , R 7 , R 8 , R 12 and X are as defined in the specification are useful as herbicides, plant growth...
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6706698 |
α-Substituted β-aminoethyl phosphonate derivatives
The present invention relates to novel α-substituted-β-aminoethylphosphonate and α-substituted-β-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a),...
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6632954 |
Phosphinite-oxazolines and metal complexes
Compounds of formulae I and Ia, wherein X 1 is secondary phosphino; R 3 is hydrogen, a hydrocarbon radical having from 1 to 20 carbon atoms, a heterohydrocarbon radical, bonded via a carbon...
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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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6531607 |
Immobilized palladium complexes
The invention relates to immobilized palladium complexes, to a process for their preparation, to their use as catalysts and to a process for the preparation of arylamines using immobilized...
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6528500 |
Azole derivatives or salts thereof
Described is an azole derivative represented by the following formula (1): wherein, R 1 represents a substituted phenyl group, R 2 and R 3 each represents a fluorine atom, an alkyl group or...
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6509364 |
Interphenylene 7-oxabicyclic &lsqb 2.2.1&rsqb heptane oxazoles as prostaglandin F2α antagonists
The present invention provides novel compounds represented by the general formula I. and pharmaceutically acceptable salts thereof wherein m, n, X, R, R 1 and R 2 are as defined in the...
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6500811 |
Sulfonylaminophosphinic and sulfonylaminophosphonic acid derivatives, methods for their preparation and use
Compounds of the formula I 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...
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6498256 |
Phosphinite-oxazolines and metal complexes thereof
Compounds of formulae I and Ia, wherein X 1 is secondary phosphino; R 3 is hydrogen, a hydrocarbon radical having from 1 to 20 carbon atoms, a heterohydrocarbon radical, bonded via a carbon...
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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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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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6448401 |
Process for water soluble azole compounds
An improved process is provided for preparing water-soluble prodrugs of triazole antifungal compounds containing a secondary or tertiary hydroxyl group. More particularly, the improved process is...
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6399782 |
Benzimidazole inhibitors of fructose 1,6-bisphosphatase
Novel benzimidazole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described
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6380393 |
Ligands, transition metal complexes and methods of using same
Compositions including at least one organic ligand including a first hetero atom and a second hetero atom directly bonded to the first hetero atom or located one carbon atom away from the first...
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6362172 |
Water soluble prodrugs of azole compounds
Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided...
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6352985 |
Benzimidazole compounds
A benzimidazole compound represented by the formula (I): wherein R 3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl...
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6255492 |
Diesters of phosphoric acid 2,5-dioxo-4,4-diphenyl-imidazolidin-1-ylmethyl ester
An improved process for the preparation of a diester of phosphoric acid 2,5-dioxo-4,4-diphenyl-imidazolidin-1-ylmethyl ester is described where an alkali metal phosphate is treated with a...
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6235728 |
Water-soluble prodrugs of azole compounds
Water soluble prodrugs of azole antifungal agents are provided by quaternizing a nitrogen atom of the azole ring with a phosphonooxymethyl group.
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6194576 |
Process for preparing antiviral 2-phosponate nucleotide analogs
Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: ##STR1## wherein n is 0 or an integer; X is O or S, CH 2 , CH-halogen, CH--N 3 , or CCH 2 ; ...
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6054464 |
Azabicyclic esters of carbamic acids useful in therapy
A compound of formula ##STR1## X is O or S; Y is O or S; G and D are independently nitrogen or carbon with the proviso that no more than one of G, D, or E is nitrogen; E is N or C--R 4 ; R 1 is...
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6030960 |
Method of treating hepatitis virus infections
A method of treating hepatitis virus infection is disclosed. The method comprising administering to a human subject in need of such treatment an effective hepatitis virus-combatting amount of an...
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