Patents
Literature
Hiro is an intelligent assistant for R&D personnel, combined with Patent DNA, to facilitate innovative research.
Hiro

8754 results about "Prodrug" patented technology

A prodrug is a medication or compound that, after administration, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Inactive prodrugs are pharmacologically inactive medications that are metabolized into an active form within the body. Instead of administering a drug directly, a corresponding prodrug might be used instead to improve how a medicine is absorbed, distributed, metabolized, and excreted (ADME). Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects.

Polymer-based, sustained release drug delivery system

Disclosed is a sustained release system that includes a polymer and a prodrug having a solubility less than about 1 mg / ml dispersed in the polymer. Advantageously, the polymer is permeable to the prodrug and may be non-release rate limiting with respect to the rate of release of the prodrug from the polymer. This permits improved drug delivery within a body in the vicinity of a surgery via sustained release rate kinetics over a prolonged period of time, while not requiring complicated manufacturing processes.
Owner:PSIVIDA INC

Pentapeptide compounds and uses related thereto

Pentapeptide compounds are disclosed. The compounds have biological activity, e.g., cytotoxicity. Prodrugs having targeting groups and pentapeptide moieities, as well as precursors thereof are also disclosed. For example, precursors having a reactive linker that can serve as a reaction site for joining to a targeting agent, e.g., an antibody, as disclosed.
Owner:SEAGEN INC

Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of myeloproliferative diseases

Methods of treating, preventing and / or managing a myeloproliferative disease are disclosed. Specific methods encompass the administration of an immunomodulatory compound, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active agent, and / or the transplantation of blood or cells. Particular second active agents are capable of suppressing the overproduction of hematopoietic stem cells or ameliorating one or more of the symptoms of a myeloproliferative disease. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
Owner:CELGENE CORP

Modified fluorinated nucleoside analogues

The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2′R)-2′-deoxy-2′-fluoro-2′-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.
Owner:GILEAD SCI INC

Elongated and multiple spacers in activatible prodrugs

This invention is directed to prodrugs that can be activated at the preferred site of action in order to selectively deliver the corresponding therapeutic parent drugs to target cells or to the target site. This invention will therefore primarily but not exclusively relate to tumor cells as target cells. More specifically the prodrugs are compounds of the formula V—(W)k—(X)l—A—Z, wherein: V is a specifier; (W)k—(X)l—A is an elongated self-elimination spacer system; W and X are each a 1,(4+2n) electronic cascade spacer, being the same or different; A is either a spacer group of formula (Y)m wherein: Y is a 1,(4+2n) electronic cascade spacer, or a group of formula U being a cyclization elimination spacer; Z is a therapeutic drug; k, l and m are integers from 0 (included) to 5 (included); n is an integer of 0 (included) to 10 (included), with the provisos that: —when A is (Y)m: k+l+m≧1, and if k+l+m=1; —when A is U: k+l≧1.
Owner:BYONDIS BV

Methods of using and compositions comprising immunomodulatory compounds for treatment and management of macular degeneration

Methods of treating, preventing and / or managing macular degeneration are disclosed. Specific embodiments encompass the administration of an immunomodulatory compound, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active agent and / or surgery. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
Owner:CELGENE CORP

Macrocyclic hepatitis C serine protease inhibitors

The present invention relates to compounds of Formula I, II or Ill, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: wherein W is a substituted or unsubstituted heterocyclic ring system. The compounds inhibit serine protease activity, particularly the activity of hepatitis c virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis c virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Owner:ENANTA PHARM INC

Single-molecule selection methods and compositions therefrom

InactiveUS20020034757A1Highly specific controlImprove complianceNanotechSugar derivativesNucleotideAdhesive
Single-molecule selection methods are provided for identifying target-binding molecules from diverse sequence and shape libraries. Complexes and imprints of selected target-binding molecules are also provided. The subject selection methods are used to identify oligonucleotide and nonnucleotide molecules with desirable properties for use in pharmaceuticals, drug discovery, drug delivery, diagnostics, medical devices, cosmetics, agriculture, environmental remediation, smart materials, packaging, microelectronics and nanofabrication. Single oligonucleotide molecules with desirable binding properties are selected from diverse sequence libraries and identified by amplification and sequencing. Alternatively, selected oligonucleotide molecules are identified by sequencing without amplification. Nonnucleotide molecules with desirable properties are identified by single-molecule selection from libraries of conjugated molecules or nucleotide-encoded nonnucleotide molecules. Alternatively, target-specific nonnucleotide molecules are prepared by imprinting selected oligonucleotide molecules into nonnucleotide molecular media. Complexes and imprints of molecules identified by single-molecule selection are shown to have broad utility as drugs, prodrugs, drug delivery systems, willfully reversible cosmetics, diagnostic reagents, sensors, transducers, actuators, adhesives, adherents and novel multimolecular devices.
Owner:MOLECULAR MACHINES

Pentapeptide compounds and uses related thereto

Pentapeptide compounds are disclosed. The compounds have biological activity, e.g., cytotoxicity. Prodrugs having targeting groups and pentapeptide moieities, as well as precursors thereof are also disclosed. For example, precursors having a reactive linker that can serve as a reaction site for joining to a targeting agent, e.g., an antibody, as disclosed.
Owner:SEAGEN INC

Administration of TLR7 ligands and prodrugs thereof for treatment of infection by hepatitis C virus

This invention relates to methods for treating or preventing hepatitis C virus infections in mammals using Toll-Like Receptor (TLR)7 ligands and prodrugs thereof. More particularly, this invention relates to methods of orally administering a therapeutically effective amount of one or more prodrugs of TLR7 ligands for the treatment or prevention of hepatitis C viral infection. Oral administration of these TLR7 immunomodulating ligands and prodrugs thereof to a mammal provides therapeutically effective amounts and reduced undesirable side effects.
Owner:ANDADYS PHARMA INC

Indole and azaindole inhibitors of fructose-1,6-bisphosphatase

InactiveUS6054587AReduce riskFasting hyperglycemiaPhosphorus organic compoundsFructoseNitrogen
Novel indole and azaindole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described: and pharmaceutically acceptable prodrugs and salts thereof.
Owner:METABASIS THERAPEUTICS INC

Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of myelodysplastic syndromes

Methods of treating, preventing and / or managing myclodysplastic syndromes are disclosed. Specific methods encompass the administration of an immunomodulatory compound, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active ingredient, and / or the transplantation of blood or cells. Specific second active ingredients are capable of affecting or blood cell production. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
Owner:CELGENE CORP

Purine inhibitors of fructose 1,6-bisphosphatase

InactiveUS6284748B1Reduce riskFasting hyperglycemiaBiocideOrganic active ingredientsFructosePurine
Novel purine compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described.whereinA is selected from the group consisting of -NR82, -NHSO2R3, -OR5, -SR5, halo, lower alkyl, -CON(R4)2, guanidino, amidino, -H, and perhaloalkyl;E is selected from the group consisting of -H, halo, lower alkylthio, lower perhaloalkyl, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, -CN, and -NR72;X is selected from the group consisting of -alk-NR-, alkylene, alkenylene, alkynylene, arylene, heteroarylene, -alk-NR-alk-, -alk-O-alk-, -alk-S-alk-, -alk-S-, alicyclicene, heteroalicyclicene, 1,1-dihaloalkylene, -C(O)-alk-, -NR-C(O)-NR'-, -alk-NR-C(O)-, -alk-C(O)-NR-, -Ar-alk-, and -alk-Ar-, all optionally substituted, wherein each R and R' is independently selected from -H and lower alkyl, and wherein each "alk" and "Ar" is an independently selected alkylene or arylene, respectively;Y is selected from the group consisting of -H, alkyl, alkenyl, alkynyl, aryl, alicyclic, heteroalicyclic, aralkyl, aryloxyalkyl, alkoxyalkyl, -C(O)R3, -S(O)2R3, -C(O)-OR3, -CONHR3, -NR22, and -OR3, all except H are optionally substituted; andpharmaceutically acceptable prodrugs and salts thereof.
Owner:METABASIS THERAPEUTICS INC

Ocular delivery of polymeric delivery formulations

The present invention provides a flowable composition suitable for use as a controlled release implant. The flowable composition can be administered into the ocular region of a mammal. The composition includes: (a) a biodegradable, biocompatible thermoplastic polymer that is at least substantially insoluble in aqueous medium, water or body fluid; (b) a biological agent, a metabolite thereof, a biological agently acceptable salt thereof, or a prodrug thereof; and (c) a biocompatible organic liquid, at standard temperature and pressure, in which the thermoplastic polymer is soluble. The present invention also provides methods of medical treatment that include administering the flowable composition into the ocular region of a mammal.
Owner:QLT USA INC

6-amino-1,4-dihydro-benzo[d][1,3] oxazin-2-ones and analogs useful as progesterone receptor modulators

Compounds having the structure of formula I are provided. In formula I, R1 is H, OH, substituted or unsubstituted C1 to C3 alkyl, C1 to C3 perfluoroalkyl, or COR6; R6 is H, substituted or unsubstituted C1 to C4 alkyl, aryl, substituted or unsubstituted C1 to C4 alkoxy, substituted or unsubstituted C1 to C3 aminoalkyl; R2 and R3 are H, substituted or unsubstituted C1 to C6 alkyl, C1 to C6 perfluoroalkyl, substituted or unsubstituted C2 to C6 alkenyl, substituted or unsubstituted C2 to C6 alkynyl, substituted or unsubstituted C3 to C6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic; or R2 and R3 are fused to form spirocyclic rings; R4 is NHR7, OR7, NHSO2R7, or OSO2R7; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt, ester, or prodrug thereof. Such compounds are useful as progesterone receptor modulators and for treating progesterone receptor related conditions.
Owner:WYETH LLC

Matrices for drug delivery and methods for making and using the same

In one aspect, biocompatible matrices such as sol-gels encapsulating a reaction center may be administered to a subject for conversion of prodrugs into biologically active agents. In certain embodiments, the biocompatible matrices of the present invention are sol-gels. In one embodiment, the enzyme <SMALLCAPS>L< / SMALLCAPS>-amino acid decarboxylase is encapsulated and implanted in the brain to convert <SMALLCAPS>L< / SMALLCAPS>-dopa to dopamine for treatment of Parkinson's disease.
Owner:MOLECULAR INSIGHT PHARMA

Methods of using 3-(4-amino-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myelodysplastic syndromes

Methods of treating, preventing and / or managing myclodysplastic syndromes are disclosed. Specific methods encompass the administration of an immunomodulatory compound, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active ingredient, and / or the transplantation of blood or cells. Specific second active ingredients are capable of affecting or blood cell production. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
Owner:CELGENE CORP

Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of skin diseases or disorders

Methods of treating, preventing, correcting and / or managing skin diseases or disorders characterized by overgrowths of the epidermis, keratoses, scleroderma, cutaneous vasculitis, acne or wrinkles are disclosed. Specific embodiments encompass the administration of an immunomodulatory compound, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active agent. Specific second active ingredients are capable of affecting or inhibiting cell growth or proliferation, removing or improving acne scars, or reducing or correcting wrinkle lines. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
Owner:CELGENE CORP

Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of asbestos-related diseases and disorders

InactiveUS20050100529A1Heavy metal active ingredientsBiocideActive agentAsbestos-related diseases
Methods of treating, preventing and managing an asbestos-related disease or disorder are disclosed. Specific embodiments encompass the administration of an immunomodulatory compound, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active agent and / or chemotherapy, surgery, or radiation therapy. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in the methods of the invention are also disclosed.
Owner:CELGENE CORP

Antibody methods for selectively inhibiting VEGF

Disclosed are antibodies that specifically inhibit VEGF binding to only one (VEGFR2) of the two VEGF receptors. The antibodies effectively inhibit angiogenesis and induce tumor regression, and yet have improved safety due to their specificity. The present invention thus provides new antibody-based compositions, methods and combined protocols for treating cancer and other angiogenic diseases. Advantageous immunoconjugate and prodrug compositions and methods using the new VEGF-specific antibodies are also provided.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST

Amine Compounds

InactiveUS20080200535A1Potent immunosuppressive actionBiocideSenses disorderUveitisAutoimmune disease
There is provided a compound exhibiting an activity of suppressing immune response with reduced adverse drug reactions, which compound is useful in the chemotherapy for preventing or treating, for example, a wide range of various autoimmune diseases including systemic erythematodes, chronic rheumatoid arthritis, Type I diabetes, inflammatory bowel disease, biliary cirrhosis, uveitis, multiple sclerosis or other disorders, or chronic inflammatory diseases, or cancers, lymphoma or leukemia, or resistance to organ or tissue transplantation or rejection against transplantation.Novel amine compounds having an S1P1 / Edg1 receptor agonist effect, possible stereoisomers or racemic bodies of the compounds, or pharmacologically acceptable salts, hydrates or solvates of the compound, the stereoisomers or the racemic bodies, or prodrugs of the compounds, the stereoisomers, the racemic bodies, the salts, the hydrates or the solvates, are provided.
Owner:ASAHI KASEI PHARMA

Antibody kits for selectively inhibiting VEGF

Disclosed are antibodies that specifically inhibit VEGF binding to only one (VEGFR2) of the two VEGF receptors. The antibodies effectively inhibit angiogenesis and induce tumor regression, and yet have improved safety due to their specificity. The present invention thus provides new antibody-based compositions, methods and combined protocols for treating cancer and other angiogenic diseases. Advantageous immunoconjugate and prodrug compositions and methods using the new VEGF-specific antibodies are also provided.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST

2′-fluoronucleosides

A class of 2′-fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: wherein[0001]Base is a purine or pyrimidine base;[0002]R1 is OH, H, OR3, N3, CN, halogen, including F, or CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy, and base refers to a purine or pyrimidine base;[0003]R2 is H, phosphate, including monophosphate, diphosphate, triphosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of providing a compound wherein R2 is H or phosphate; sulfonate ester including alkyl or arylalkyl sulfonyl including methanesulfonyl, benzyl, wherein the phenyl group is optionally substituted with one or more substituents as described in the definition of aryl given above, a lipid, an amino acid, peptide, or cholesterol; and[0004]R3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of being cleaved to the parent compound, or a pharmaceutically acceptable salt thereof.
Owner:EMORY UNIVERSITY

Methods and compositions using immunomodulatory compounds for the treatment and management of central nervous system disorders or diseases

Methods of treating, preventing and / or managing central nervous system disorders, such as Amyotrophic Lateral Sclerosis (ALS or Lou Gehrig's Disease) and related syndromes are disclosed. Specific methods encompass the administration of an immunomodulatory compound of the invention, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active ingredient. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
Owner:CELGENE CORP

Substituted nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases

InactiveUS20040229839A1Sufficient inhibitionBiocideSugar derivativesPurinePolymerase L
Provided are compounds represented by: X is O, S or NR6, R1 is H or (CH2)mR5, R2, R2', R3 and R3' are independently NO2, N3 or (CH2)mR5, OH R4 is H, OR6, SR6, NR6R6a, CN, C(O)OR6, C(O)NR6R6a, R6, OR7 or (CH2)nR7, R5 is H, halo, OR6, SR6, NR6R6a, CN, C(O)OR6, C(O)NR6R6a, R6, OR7 or (CH2)mR7, R6 and R6a are individually H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl or substituted aryl, R7 is: R8 is H, F, SR9 or OR9, R9 is H, alkyl, alkenyl, alkynyl, aryl or hydroxyprotecting group, Y is H, CH3 or (CH2)mR5, Z is O or S W is CH2, CF2, CHF or O, m is 0-4, B is adenine, guanine, cytosine, uracil, thymine, modified purines and pyrimidines substituted pyridines, five membered heterocycles substituted by at least one of amines, substituted amines, amides, substituted amides, esters, halogens, alkyls, ethers; and pharmaceutically acceptable salts thereof and prodrugs thereof. These ring systems may be substituted.
Owner:BIOCRYST PHARM INC
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products