Ribozyme Pharmaceuticals, Incorporated

Mbc Pharma, Inc.

Sirna Therapeutics, Inc.

Maxwell Biotech Group Ltd.

Mbc Research, Inc.

Alexander Karpeisky

Leonid Beigelman

James A McSwiggen

Chandra Vargeese

Shawn Patrick Zinnen

Jasenka Matulic-Adamic

David Sweedler

Nassim Usman

Peter Haeberli

Alex B Burgin

Amber Beaudry

Anil Modak

Thale Jarvis

Francine E Wincott

Anthony DiRenzo

Lisa Lynn Caralli

Tod M Woolf

Andrei P Guzaev

James D Thompson

Vladimir Serebryany

Mark Reynolds

Ekaterina Alekseevna Ivanova

Rina Diana Fong

Laurent Bellon

Nelly Padioukova

Sergey Mikhailov

Grigorii Tzeitline

Christopher Shaffer

Nilabh Chaudhary

John Min

Hbf Dixon

Michael Zwick

Vladmir Serebryany

Vladimir Y Vvedensky

Murali Urlam

Shawn Zinnen

Shawn P Zinnen

Rina Diana Salurialam

Lawrence Blatt

Provided herein is a novel method for creating fixed, non-antagonistic molar ratios of drugs in and around the bone environment for desired periods of time. This method enables treating bone and bone-related disease by administering a pharmaceutical composition comprising a bone-targeted therapeutic agent able to release a drug payload from the bone surface, in addition to a second therapeutic agent. Such methods are useful in the treatment of bone and bone-related diseases, such as cancer-induced bone disease, osteomyelitis and bone infection, bone pain and inflammatory bone disease, metabolic disease, as well as others.

Drug combination treatments using bone-targeting therapeutics for bone and bone-related disease

Provided herein are conjugates of nucleoside antimetabolites and their analogs with ibandronate, pharmaceutical compositions including one or more of said conjugates, methods of synthesizing the same as well as methods of treating diseases and or conditions using the same.

Ibandronate conjugates of nucleoside antimetabolites

The invention relates to the field of medicine and pharmaceuticals and particularly to a novel dosage form of an antitumor preparation, which ensures the hydrolytic and physical stability of said preparation, as well as to a method for producing a dosage form of this type. The stable dosage form is a lyophilizate comprising an etidronate-cytarabine conjugate or a pharmaceutically acceptable salt thereof, and a stabilizer, which is a divalent metal salt, in a molar ratio of stabilizer to conjugate of 1:1 to 20:1. A dosage form of this type ensures the hydrolytic and physical stability of the conjugate during long-term storage, and the stability of solutions of the conjugate for parenteral administration during clinical use.

Stable dosage form of etidronate-cytarabine conjugate, and use thereof

This invention relates to oncology, and specifically to a novel medicinal drug and a method for treating bone lesions caused by malignant neoplasms. A medicinal drug that represents a lyophilisate for solution for parenteral administration, including the following components: pharmaceutically acceptable salt of the divalent metal and 1-((((((2R,3S,4S,5R)-5-(4-amino-2-oxopyrimidine-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methoxy))(hydroxy)phosphoryloxy)(hydroxy)phosphoryl)-1-hydroxyethylphosphonic acid or pharmaceutically acceptable salt hereof with a molar ratio of the components ranging from 1:1 to 20:1 is proposed for this purpose. The treatment method includes the drug solution administration according to the invention in the form of intravenous drop infusions in a dose ranging from 0.01 to 5 mg/kg of the active component per 1 kg of the patient's weight in the form of intravenous drop infusions. The treatment with the medicinal drug according to the invention allows to reduce the metabolic activity of bone lesions caused by malignant tumours up to 100%.

Pharmaceutical preparation treating bone lesions caused by malignant neoplasms

The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.

Bone targeted therapeutics and methods of making and using the same

Compounds and compositions are provided, as are methods of using them to treat infections, neoplastic disease, including pancreatic cancer, inflammatory disease, and pain. Such compounds are nucleotides, acyclonucleotides, and ANP phosphonates conjugated with forms and/or moieties of Vitamin Bfor delivery past the cell membrane and into the cell.

Vitamin B6 derivatives of nucleotides, acyclonucleotides and acyclonucleoside phosphonates

This invention features permeability enhancer molecules, and methods, to increase membrane permeability of various molecules, such as nucleic acids, polynucleotides, oligonucleotides, enzymatic nucleic acid molecules, antisense nucleic acid molecules, 2-5A antisense chimeras, triplex forming oligonucleotides, decoy RNAS, dsRNAs, siRNAs, aptamers, or antisense nucleic acids containing nucleic acid cleaving chemical groups, peptides, polypeptides, proteins, carbohydrates, steroids, metals and small molecules, thereby facilitating cellular uptake of such molecules.

Compositions for the delivery of negatively charged molecules

Process for chemical synthesis of methoxy nucleosides.

Chemical synthesis of methoxy nucleosides

The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.

Biphosphonate conjugates and methods of making and using the same

The present invention provides methods for the chemical synthesis of nucleosides and derivatives thereof, including 2&prime;-amino, 2&prime;-N-phthaloyl, 2&prime;-O-methyl, 2&prime;-O-silyl, 2&prime;-OH nucleosides, C-nucleosides, nucleoside phosphoramidites, C-nucleoside phosphoramidites, and non-nucleoside derivatives.

Methods for synthesizing nucleosides, nucleoside derivatives and non-nucleoside derivatives

This invention relates to novel chemically-modified nucleic acid molecules having specific formulae that exhibit increased resistance to nucleases and increased binding affinity to target nucleic acid molecules. The invention further relates to methods of modulating gene expression using the novel chemically modified nucleic acid molecules, and compositions and cells comprising said molecules.

Nucleic acid molecules with novel chemical compositions capable of modulating gene expression

Novel nucleotide triphosphates, methods of synthesis and process of incorporating these nucleotide triphosphates into oligonucleotides, and isolation of novel nucleic acid catalysts (e.g., ribozymes) are disclosed. Also, described are the use of novel enzymatic nucleic acid molecules to inhibit HER2/neu/ErbB2 gene expression and their applications in human therapy.

Oligoribonucleotides with enzymatic activity

An enzymatic nucleic acid molecule comprising a 5&prime;- and/or a 3&prime;-cap structure, wherein said structure is not a 5&prime;-5&prime;-linked inverted nucleotide or a 3&prime;-3&prime;-linked inverted nucleotide.

Enzymatic nucleic acids containing 5&prime;-and or 3&prime;-cap structures

Growing community of inventors

Lafayette, CO, United States of America

Alexander Karpeisky