Method of targeting a specific location in a body using phospholipid and cholesterol liposomes which encapsulate an agent
Granted: August 14, 2001
Patent Number:
6274115
Micellular particles such as small unilamellar vesicles of less than 2000 A° loaded with 111In are administered to BALB/c mice in which EMT6 tumors had been induced. Whole body scintographs of the mice to which either neutral or positively or negatively charged vesicles had been administered show a substantial quantity of the vesicle entrapped 111In localized in the tumor. Blocking of macrophages in the liver and spleen by first administering unlabeled, aminomannose substituted…
Truncation selex method
Granted: July 17, 2001
Patent Number:
6261774
This invention is directed to a method for identifying nucleic acid ligands by the SELEX method wherein the participation of fixed sequences is eliminated or minimized.
Homogeneous detection of a target through nucleic acid ligand-ligand beacon interaction
Granted: July 17, 2001
Patent Number:
6261783
A method for detecting a target molecule in a test mixture suspected of containing said target molecule is described. The nucleic acid ligand capable of binding to the target molecule has a first sequence A and a second sequence B, which are partially complementary sequences that form an imperfect intramolecular duplex, which unwinds upon the binding of the target to the nucleic acid ligand. Sequences A and B are able to participate in extramolecular hybridization reactions only when the…
Tenascin-C nucleic acid ligands
Granted: May 15, 2001
Patent Number:
6232071
Methods are described for the identification and preparation of nucleic acid ligands to tenascin-C. Included in the invention are specific RNA ligands to tenascin-C identified by the SELEX method. Further included in the invention are methods for detecting the presence of a disease condition in a biological tissue in which tenascin-C is expressed.
Compounds and methods for synthesis and therapy
Granted: May 1, 2001
Patent Number:
6225341
Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and…
Nucleotide analogs
Granted: May 1, 2001
Patent Number:
6225460
Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.
Antibiotic formulation and use for bacterial infections
Granted: April 24, 2001
Patent Number:
6221388
A liposomal aminoglycoside formulation comprising a neutral lipid, a negatively charged lipids and a sterol. The formulation contains unilamellar vesicles having an average size below 100 nm. A process of making liposomes containing an aminoglycoside is also provided. A method is also provided for the treatment of drug susceptible and drug resistant bacteria.
Preparation of cyclohexene carboxylate derivatives
Granted: March 20, 2001
Patent Number:
6204398
The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates such as those having formulas (I)-(IV), useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.
Polypeptides and coagulation therapy
Granted: August 29, 2000
Patent Number:
6110721
Novel polypeptides (NPs) are provided which are capable of protein C activation without significant fibrinogen clotting activity, and vice versa. NPs having enhanced protein C activating properties in relation to fibrinogen clotting are useful in particular as anticoagulants and in screening for substances that agonize or antagonize this property and in diagnostic procedures to determine the status of patients' activated protein C-mediated anticoagulant pathway. Procoagulant NPs are…
Compounds and methods for synthesis and therapy
Granted: August 29, 2000
Patent Number:
6111132
Novel compounds of Formula (I) are described. R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are described in this specification.Synthetic intermediates and pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Assay methods for detecting neuraminidase activity are also described.
Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability
Granted: May 30, 2000
Patent Number:
6069249
Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure --OC(R.sup.2).sub.2 OC(O)X(R).sub.a, wherein R.sup.2 independently is H, C.sub.1 -C.sub.12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR.sup.3 in which R.sup.3 is C.sub.1 -C.sub.12 alkyl; X is N or O; R is…
Preparation of carbocyclic compounds
Granted: May 2, 2000
Patent Number:
6057459
The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.
Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability
Granted: March 28, 2000
Patent Number:
6043230
Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure -OC(R.sup.2).sub.2 OC(O) X(R).sub.a, wherein R.sup.2 independently is H, C.sub.1 -C.sub.12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR.sup.3 in which R.sup.3 is C.sub.1 -C12 alkyl; X is N or O; R is…
Thiepane compounds
Granted: March 7, 2000
Patent Number:
6034118
Tri- and tetra substituted thiepane compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositions are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled…
Pyrimidine derivatives and oligonucleotides containing same
Granted: February 22, 2000
Patent Number:
6028183
Compounds having structure (1) ##STR1## wherein R.sup.1 is --H a protecting group, a linker or a binding partner; and R.sup.2 and R.sup.34 are as defined in the specification. The invention also provides intermediates and methods make the structure (1) compounds, as well as methods to use the compounds as labels in diagnostic assays and to enhance binding to complementary bases.
Pyrimidine derivatives for labeled binding partners
Granted: December 28, 1999
Patent Number:
6007992
Compounds having structure (1) ##STR1## wherein R.sup.1 is --H a protecting group, a linker or a binding partner; and R.sup.2 and R.sup.34 are as defined in the specification. The invention also provides intermediates and methods make the structure (1) compounds, as well as methods to use the compounds as labels in diagnostic assays and to enhance binding to complementary bases.
Pyrimidine derivatives
Granted: December 21, 1999
Patent Number:
6005096
A compound having the structure ##STR1## wherein R.sup.1 is H or a linker group; R.sup.24 is independently halo or C.sub.1 -C.sub.2 haloalkyl;R.sup.25 is independently --SH, --OH, .dbd.S or .dbd.O;A is independently N or C; andM, taken together with the radical --A--C(--R.sup.25), completes an aryl or heteroaryl ring structure comprising 5 or 6 ring atoms wherein the heteroaryl ring comprises a single O ring heteroatom, a single N ring heteroatom, a single S ring heteroatom, a single O…
Piperidine compounds
Granted: November 30, 1999
Patent Number:
5994377
Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and…
Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability
Granted: November 2, 1999
Patent Number:
5977089
Compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure --OC(R.sup.2).sub.2 OC(O)X(R).sub.a, wherein R.sup.2 independently is H, C.sub.1 -C.sub.12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR.sup.3 in which R.sup.3 is C.sub.1 -C.sub.12 alkyl; X is N or O; R is…
Polyhydroxy benzoic acid derivatives and their use as neuraminidase inhibitors
Granted: September 28, 1999
Patent Number:
5958973
The present invention is directed to compositions of the formula: ##STR1## wherein: R.sub.2 is H, or an alkyl group having 1 to 3 carbon atoms and 0 to 2 hydroxyls;R.sub.3 is H, or hydroxyl;R.sub.4 is H, or forms a hydrolyzable ester or amide with --CO.sub.2 --;R.sub.5 are H, or are taken together to form .dbd.NH; andR.sub.6 comprises an amine, or a group having 1 to 12 carbon atoms and 1 to 3 amine groups. The invention is also directed to methods of inhibiting the activity of…
