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Class 548/413 - Phosphorus attached indirectly to the five-membered hetero ring by nonionic bonding


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein phosphorus is attached indirectly to the
No. of patents: 290
Last issue date: 04/29/2008


1                
NumberTitleIssue Date
7365092Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they ac...
04/29/2008
7365091Derivatives of succinic and glutaric acids and analogs thereof useful as inhibitors of PHEX
The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula: useful as inhibitors of PHEX. These derivatives are useful fo...
04/29/2008
7351730Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8,...
04/01/2008
7345082Phosphinic acids
The present invention relates to phosphinic acid derivatives of formula I wherein R1, R2, R3 and R4 are described hereinabove. These compounds can be used in the treatment or prev...
03/18/2008
7339066Intermediates for the synthesis of polypropionate antibiotics
The invention relates to intermediate compounds of the formula wherein R1 is H or a protecting group, R2 and R3 each independently represent H, methyl, or a leaving group, provided that at l...
03/04/2008
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
7314941Synthesis of phosphono-substituted porphyrin compounds for attachment to metal oxide surfaces
A method of making a phosphono-substituted dipyrromethane comprises reacting an aldehyde or acetal having at least one phosphono group substituted thereon with pyrrole to produce a phosphono-substituted dipyrromethane; and wherein the phosphono is selected from the ...
01/01/2008
7297807Intermediates for the synthesis of polypropionate antibiotics
The invention relates to intermediate compounds of the formula wherein R1 is H or a protecting group, R2 and R3 each independently represent H, methyl, or a leaving group, provided that at l...
11/20/2007
7268124Geranylgeranyl pyrophosphate synthase inhibitors
The invention provides novel pyrophosphate synthase inhibitors of formula I as well as compositions comprising such inhibitors and methods for their use. ...
09/11/2007
7223879Ligands for metals and improved metal-catalyzed processes based thereon
One aspect of the present invention relates to ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. ...
05/29/2007
7148361Synthesis of phosphono-substituted porphyrin compounds for attachment to metal oxide surfaces
A method of making a phosphono-substituted dipyrromethane comprises reacting an aldehyde or acetal having at least one phosphono group substituted thereon with pyrrole to produce a phosphono-substituted dipyrromethane; and wherein the phosphono is selected from the ...
12/12/2006
7141377Process for discrimination of nucleic acid sequence variants
A process of detecting a target nucleic acid using labeled oligonucleotides uses the 5′ to 3′ nuclease activity of a nucleic acid polymerase to cleave annealed labeled oligonucleotide from hybridized duplexes and release labeled oligonucleotide fragments for det...
11/28/2006
7119090Pyrrole substituted 2-indolinone protein kinase inhibitors
The present invention relates to novel pyrrole substituted 2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of prot...
10/10/2006
7115738Hydroxyproline/phosphono oligonucleotide analogues, methods of synthesis and methods of use
Compounds are described and claimed comprising general formula: The compounds have substituents as described herein and are useful, e.g., for their ability to bind nucleic acids and thereby effect purifications, ...
10/03/2006
7078532Process for manufacture of fosinopril sodium
The present invention discloses a process for the synthesis of fosinopril as a single desired isomer of high purity in two steps comprising of (a) preparation of fosinopril as a mixture of four diastereomers and (b) separation of the desired isomer from the mixture ...
07/18/2006
7045511Fosinopril formulation
A pharmaceutical formulation is provided comprising fosinopril which is the prodrug of an angiotensin converting enzyme (ACE) inhibitor, fosinoprilat. The formulation is characterized by comprising in the range of about 0.25 to about 5% glyceryl dibehenate which has...
05/16/2006
7026498Ligands for metals and improved metal-catalyzed processes based thereon
One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming react...
04/11/2006
70054428-azaprostaglandin carbonate and thiocarbonate analogs as therapeutic agents
The present invention provides a compound represented by the general formula I; wherein A, Ar, X, Z, n, x, y, R and R3 are as defined in the specification. ...
02/28/2006
6977303Highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using same
The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence,...
12/20/2005
69518832H-1-benzopyran derivatives processes for their preparation and pharmaceutical compositions thereof
2H-1-Benzopyran derivatives, processes for their preparation and use thereof for the preparation of pharmaceutical compositions for the prevention and treatment of postmenopausal pathologies. ...
10/04/2005
6946560Ligands for metals and improved metal-catalyzed processes based thereon
One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming react...
09/20/2005
6939886Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor Type-1 (PAI-1)
This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8
09/06/2005
69060978-azaprostaglandin analogs as agents for lowering intraocular pressure
The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I;
06/14/2005
6878830Catalytic boronate ester synthesis from boron reagents and hydrocarbons
A process for producing a ring-substituted arene borane which comprises reacting a ring-substituted arene with an HB organic compound in the presence of a catalytically effective amount of an iridium or rhodium complex with three or more substituents, excluding hydr...
04/12/2005
68122408-azaprostaglandin carbonate and thiocarbonate analogs as therapeutic agents
The present invention provides a compound represented by the general formula I; wherein A, Ar, X, Z, n, x, y, R and R3 are as defined in the specification. ...
11/02/2004
6800654Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are eachH, alkyl,, alkanoyl, halo, OH, aryl optionally substituted with R8
10/05/2004
6784191Benzamidine derivatives
A benzamidine derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an effect of inhibiting the blood coagulation based on their excellent effect of inhibiting activated blood-coagulation factor X. Thus, a blood-coag...
08/31/2004
6753431Production of mixed acid anhydride and amide compound
There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)pā€ƒā€ƒ(1) wherein R1, R2 and Y denote the same as defined bel...
06/22/2004
67342018-Azaprostaglandin carbonate and thiocarbonate analogs as therapeutic agents
The present invention provides a compound represented by the general formula I; wherein A, Ar, X, Z, n, x, y, R and R3 are as defined in the specification. ...
05/11/2004
67342063-oxa-8-azaprostaglandin analogs as agents for lowering intraocular pressure
The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I;
05/11/2004
6699884Fluoro-substituted benzenesulfonyl compounds for the treatment of inflammation
Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: ##STR1## wherein A, X, n, R1...
03/02/2004
6696081Carbohydrate based lipid compositions and supramolecular structures comprising same
Novel lipid compounds and compositions comprising carbohydrate backbones are used to make supramolecular structures such as vesicles, liposomes (single lamellar, multilamellar, and giant), micelles, hexagonal phases, microemulsions and others. The novel c...
02/24/2004
6686477Highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using same
The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reactio...
02/03/2004
6555567Substituted spiroheterocyclic 1H-3-aryl-pyrrolidine-2,4-dione derivatives, processes for their preparation, and their use as pesticides
The invention concerns substituted spiro heterocyclic 1H-3-arylpyrrolidine-2,4-dione derivatives depicted by the formula: ##STR1## X is alkyl, halogen or alkoxy; Y is hydrogen, alkyl, halogen, alkoxy or alkyl halide; Z is alkyl, halogen or alkoxy; n is 0,...
04/29/2003
6509359Pyrrolidin-2-one compounds and their use as neuraminidase inhibitors
A compound having the formula: ##STR1## wherein all variables are as defined in the specification, for use as a neuramninidase inhibitor....
01/21/2003
6492351Kappa agonist compounds, pharmaceutical formulations and method of prevention and treatment of pruritus therewith
The compounds of formulae IIA, the structure: ##STR1## wherein R1, R2, and X4, X5, n are as described in the specification....
12/10/2002
6485886Oxime derivatives and the use thereof as latent acids
New oxime derivatives of formula (I) or. (II), wherein m is 0 or 1; R1 inter alia is phenyl, naphthyl, anthracyl, phenanthryl or a heteroaryl radical; R'1 is for example C2 -C12 alkylene, phenylene, naphthylene;...
11/26/2002
6479471NAALADase inhibitors
The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit N-Acetylated ଱-Linked Acidic Dipeptidase (NAALADase) enzym...
11/12/2002
64724191-H-3-aryl-pyrrolidine-2, 4-dione derivatives as pest-control agents
The present invention relates to new 1-H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, G, X, Y and Z have the meanings given in the description, to processes for their preparation, and to intermediates therefor. The ...
10/29/2002
6452004Cyclopentenecarboxamide derivative, method for preparing the same bicycloamide derivative used therein
A cyclopentenecarboxamide derivative represented by the formula (I): ##STR1## and a method for preparing the cyclopentencarboxamide derivative. A bicycloamide derivative represented by the formula (II): ##STR2## and a method for preparing the bicycloamide...
09/17/2002
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