| Patent Number |
Title Of Patent |
Date Issued |
| 6861521 |
Stereoselective transacetalization of steroidal C-22 acetonide |
March 1, 2005 |
| The present invention is a process for the preparation of rofleponide of formula (II) ##STR1##where the 22R/22S ratio is 90/10 or greater which comprises contacting an acetonide of formula (I) ##STR2##with CH.sub.3 --CH.sub.2 --CH.sub.2 --CHO (III) in the presence of perchloric a |
| 6861433 |
Oxazolidinone photoaffinity probes |
March 1, 2005 |
| The present invention provides compounds of the formula: ##STR1##compositions comprising such compounds, and methods for using the same. |
| 6861420 |
N-substituted 1,2,4,5-tetrahydro-1H-benzo[d]azepine compounds |
March 1, 2005 |
| The present invention provides compounds of Formula I: ##STR1##wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therape |
| 6858635 |
Oxazolidinone photoaffinity probes |
February 22, 2005 |
| Disclosed are novel compounds that are useful and effective as photoaffinity probes and methods of using oxazolidinone photoaffinity probes. |
| 6858385 |
Pseudorabies virus protein |
February 22, 2005 |
| The present invention provides recombinant DNA molecules comprising a sequence encoding a pseudorabies virus (PRV) glycoprotein selected from the group consisting of gI, gp50, and gp63, host cells transformed by the recombinant DNA molecule sequences, the gI, gp50 and gp63 polypeptides. |
| 6855709 |
Pyridyl sulfone derivatives |
February 15, 2005 |
| The invention provides compounds of the formula ##STR1##and methods of using those compounds for treating a disease or condition in a mammal wherein a 5-HT receptor, such as a 5-HT.sub.6 receptor, is implicated and modulation of a 5-HT function is desired, wherein A, G and W.sub.1 -W |
| 6849640 |
Therapeutic 1H-pyrido [4,3-b] indoles |
February 1, 2005 |
| The present invention provides 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indoles and 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. These compounds are 5-HT ligands that are useful for treating diseases wherein modulation of 5-HT activity is desired. |
| 6846813 |
Compounds to treat alzheimer's disease |
January 25, 2005 |
| The present invention is disubstituted amines of formula (I) ##STR1##and disubstituted amines of formula (II) ##STR2##useful in treating Alzheimer's disease and other similar diseases. |
| 6846640 |
Time-resolved fluorescence assay for the detection of multimeric forms of A-beta 1-40 |
January 25, 2005 |
| The present invention provides for a polypeptide aggregation screening assay for the purpose of detecting modulators of polypeptide aggregation, which can provide for new therapies in pathologic states associated with polypeptide aggregation, especially considered is Alzheimer's Disease. |
| 6844148 |
Alzheimer's disease secretase, APP substrates therefor, and uses therefor |
January 18, 2005 |
| The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. An enzyme that cleaves the .alpha.-secretase site of APP also is |
| 6835565 |
Alzheimer's disease secretase |
December 28, 2004 |
| The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. |
| 6835546 |
Drosophila G protein coupled receptors, nucleic acids, and methods related to the same |
December 28, 2004 |
| The present invention provides a Drosophila melanogaster GPCR (DmGPCR) polypeptides and polynucleotides which identify and encode such a DmGPCR. In addition, the invention provides expression vectors, host cells and methods for its production. The invention also provides methods for the |
| 6833453 |
Methods of producing oxazolidinone compounds |
December 21, 2004 |
| Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-hal |
| 6833248 |
Human caspase-12 materials and methods |
December 21, 2004 |
| The present invention provides novel human caspase-12 polynucleotides and polypeptides; constructs and recombinant host cells incorporating the polynucleotides; the human caspase-12 polypeptides encoded by the polynucleotides; antibodies to the polypeptides; and methods of making and |
| 6828330 |
Quinuclidine-substituted hetero-bicyclic aromatic compounds for the treatment of disease |
December 7, 2004 |
| The invention provides compounds of Formula I: ##STR1##wherein W.sup.0 is a bicyclic moiety and is ##STR2##These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful to treat diseases or conditions |
| 6828317 |
Antimicrobial thiadiazinone derivatives and their application for treatment of bacterial infecti |
December 7, 2004 |
| The present invention provides certain thiadiazinone derivatives of oxazolidinones of the following formula I: ##STR1##or pharmaceutically acceptable salts thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for prepa |
| 6828117 |
Alzheimer's disease secretase, APP substrates therefor, and uses therefor |
December 7, 2004 |
| The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. The invention further provides a modified APP protein and associa |
| 6825225 |
Bicyclic isoxazolinones as antibacterial agents |
November 30, 2004 |
| The present invention provides compounds of formula I useful as anti microbial agents ##STR1##wherein X, Y, R.sup.1, and n are as defined in thereof. |
| 6825023 |
Alzheimer's disease secretase, APP substrates therefor, and uses therefor |
November 30, 2004 |
| The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. The invention further provides a modified APP protein and associa |
| 6821970 |
Oxazinocarbazoles for the treatment of CNS diseases |
November 23, 2004 |
| The present invention provides oxazinocarbazole derivatives having a ring connecting position 8 (C-8) and position 9 (N-9), and more specifically, provides compounds of formula (I) wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are described herein. ##STR1##These compounds are 5-HT li |
| 6821969 |
Thioxazinoquinolones as antiviral agents |
November 23, 2004 |
| The present invention provides a compound of formula I ##STR1##These compounds are useful as antiviral agents, in particular, as agents against viruses of the herpes family. |
| 6814319 |
Laboratory scale milling process |
November 9, 2004 |
| There is provided a process for reducing particle size of a drug, the process comprising (a) a step of dispersing about 10 g or less of the drug in a suitable volume of a liquid dispersion medium to form a suspension; (b) a step of bringing together in a vessel grinding media, magnetical |
| 6809112 |
Method of treating sexual disturbances |
October 26, 2004 |
| The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) ##STR1##in a dosage range where the sexually therapeutic amount is from about 0.2 thru 8 mg/person/dose and where the sexually matin |
| 6797834 |
Phosphoric acid isomerization of A 5 (10), 9 (11)--diene steroid to the corresponding 4, 9-diene |
September 28, 2004 |
| The invention is a process for the preparation of a .DELTA..sup.4,9 -steroid of formula (II) ##STR1##which comprises contacting a .DELTA..sup.5(10),9(11) -steroid of formula (I) ##STR2##with a phosphorous containing acid. |
| 6797003 |
Aspheric soft lens |
September 28, 2004 |
| An aspheric soft intraocular lens, having an optical power surface, which may have multiple radii portions or aspherical portions, as well as spherical portions, intended to replace the crystalline lens of a patient's eye, in particular after a cataract extraction. Such an aspheric s |
| 6796975 |
Container for linezolid intravenous solution |
September 28, 2004 |
| The present invention is a container for an IV aqueous solution of a Gram-positive oxazolidinone agent, such as linezolid a the compound of formula: ##STR1##which comprises having the container-solution contact surface material be a polyolefin. |
| 6790950 |
Anti-bacterial vaccine compositions |
September 14, 2004 |
| Gram negative bacterial virulence genes are identified, thereby allowing the identification of novel anti-bacterial agents that target these virulence genes and their products, and the provision of novel gram negative bacterial mutants useful in vaccines. |
| 6790610 |
Alzheimer's disease, secretase, APP substrates therefor, and uses therefor |
September 14, 2004 |
| The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. The invention further provides a modified APP protein and associa |
| 6774231 |
Method for the preparation of oxazolidinones |
August 10, 2004 |
| The present invention relates to a process for making a compound of structure 4 ##STR1##which comprises reacting a compound of structure 1 with vinyl sulfone in the presence of a Lewis-acid at a temperature in a range of from 40.degree. C. to 170.degree. C., wherein each R.sup.1 is i |
| 6764858 |
Methods for creating a compound library |
July 20, 2004 |
| A method for developing a library of compounds, the compound library, a method for identifying ligands for target molecules, and a method for identifying lead chemical templates, which, for example, can be used in drug discovery and design are provided. Certain embodiments of these m |
| 6764823 |
Antimicrobial methods and materials |
July 20, 2004 |
| The present invention provides methods of identifying antimicrobial agents that target genes essential for the survival of Staphylococcus bacteria, including antimicrobial agents that interfere with the expression of essential coding sequence products and antimicrobial agents that interf |
| 6762191 |
Therapeutic compounds |
July 13, 2004 |
| The present invention provides compounds of formula (I): ##STR1##wherein: R.sub.1, R.sub.2, R.sub.3 R.sub.4, R.sub.5, R.sub.6, X, - - - , m, and n have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts thereof. The |
| 6757618 |
Chemical structure identification |
June 29, 2004 |
| A method for generating a numeric or alpha-numeric identifier representative of a chemical structure having at least two atoms connected by a bond includes the step of assigning a numerical value to each atom and a numerical bond value to each bond. The method updates the numerical v |
| 6753163 |
Alzheimer's disease secretase, APP substrates therefor, and uses therefor |
June 22, 2004 |
| The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. The invention further provides a modified APP protein and associa |
| 6743811 |
Oxazalidinone compounds and methods of preparation and use thereof |
June 1, 2004 |
| Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used |
| 6740754 |
Process to produce oxazolidinones |
May 25, 2004 |
| The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)and processes for production of pharmacologically useful oxazolidinones. |
| 6740652 |
Oxazolidinones to treat eye infections |
May 25, 2004 |
| The present invention involves a method of treating an ophthalmic infection in a useful warm blooded mammal who is in need of such treatment which comprises topical administration of an ophthalmologically effective amount of an OXAZOLIDINONE. |
| 6737510 |
Alzheimer's disease secretase, APP substrates therefor, and uses thereof |
May 18, 2004 |
| The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. The invention further provides a modified APP protein and associa |
| 6734301 |
2,3,4,5-Tetrahydro-1H-[1,4]diazepino[1,7-a]indole compounds |
May 11, 2004 |
| Certain 2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,7-a]indoles are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired. |
| 6734005 |
Matrix metalloproteinases |
May 11, 2004 |
| The present invention provides genes encoding novel matrix metalloproteinases termed MMP; constructs and recombinant host cells incorporating the genes; the MMP polypeptides encoded by the genes; antibodies to the MMP polypeptides; and methods of making and using all of the foregoing |
| 6730682 |
Heterocycle carboxamides as antiviral agents |
May 4, 2004 |
| The present invention provides a compound of formula I ##STR1##which is useful as antiviral agents, in particular, as agents against viruses of the herpes family. |
| 6727274 |
Arylsulphonyl substituted-tetrahydro- and hexahydro-carbazoles |
April 27, 2004 |
| The invention provides compounds of formula I for use in treating conditions in which 5-HT.sub.6 receptors are involved such as in anxiety, depression, schizophrenia, Alzheimer's disease, stress-related disease, panic, a phobia, obsessive compulsive disorder, obesity, post-traumatic |
| 6727248 |
Substituted quinolinecarboxamides as antiviral agents |
April 27, 2004 |
| The present invention discloses disubstiuted 4-oxo-1,4-dihydro-3-quinolinecarboxamide derivatives. The compounds are useful as antiviral agents, in particular, as agents against viruses of the herpes family. |
| 6727074 |
Alzheimer's disease secretase, APP substrates therefor, and uses therefor |
April 27, 2004 |
| The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. The invention further provides a modified APP protein and associa |
| 6720316 |
Therapeutic 5-HT ligand compounds |
April 13, 2004 |
| The present invention provides compounds of Formula (I) ##STR1##wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and Z have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention als |
| 6716980 |
Process to produce oxazolidinones |
April 6, 2004 |
| The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)and processes for production of pharmacologically useful oxazolidinones. |
| 6716870 |
Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives |
April 6, 2004 |
| The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases ("PKs"). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity ut |
| 6713260 |
Methods of identifying compounds that bind to target species under isothermal denaturing conditi |
March 30, 2004 |
| The present invention provides a method for identifying a test compound that binds to a target species. The method includes: incubating at least one test mixture under isothermal denaturing conditions, each test mixture comprising at least one test compound, and at least one target speci |
| 6710067 |
Mannich base prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives |
March 23, 2004 |
| The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases ("PKs"). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK |
| 6706485 |
Method of identifying agents that inhibit APP processing activity |
March 16, 2004 |
| The present invention provides methods of identifying agents that inhibit the amyloid precursor protein (APP) processing activity of Asp2 polypeptide. |
