23561 results about "Pharmaceutical drug" patented technology

Drug-Linker-Ligand Conjugates are disclosed in which a Drug is linked to a Ligand via a peptide-based Linker unit. In one embodiment, the Ligand is an Antibody. Drug-Linker compounds and Drug compounds are also disclosed. Methods for treating cancer, an autoimmune disease or an infectious disease using the compounds and compositions of the invention are also disclosed.

Multimolecular devices and drug delivery systems prepared from synthetic heteropolymers, heteropolymeric discrete structures, multivalent heteropolymeric hybrid structures, aptameric multimolecular devices, multivalent imprints, tethered specific recognition devices, paired specific recognition devices, nonaptameric multimolecular devices and immobilized multimolecular structures are provided, including molecular adsorbents and multimolecular adherents, adhesives, transducers, switches, sensors and delivery systems. Methods for selecting single synthetic nucleotides, shape-specific probes and specifically attractive surfaces for use in these multimolecular devices are also provided. In addition, paired nucleotide-nonnucleotide mapping libraries for transposition of selected populations of selected nonoligonucleotide molecules into selected populations of replicatable nucleotide sequences are described.

Methods of monitoring and evaluating the status of a tumor undergoing treatment includes monitoring in vivo at least one physiological parameter associated with a tumor in a subject undergoing treatment, transmitting data from an in situ located sensor to a receiver external of the subject, analyzing the transmitted data, repeating the monitoring and transmitting steps at sequential points in time and evaluating a treatment strategy. The method provides dynamic tracking of the monitored parameters over time. The method can also include identifying in a substantially real time manner when conditions are favorable for treatment and when conditions are unfavorable for treatment and can verify or quantify how much of a known drug dose or radiation dose was actually received at the tumor. The method can include remote transmission from a non-clinical site to allow oversight of the tumor's condition even during non-active treatment periods (in between active treatments). The disclosure also includes monitoring systems with in situ in vivo biocompatible sensors and telemetry based operations and related computer program products.

The present invention provides heterocyclic linker compounds useful for linking drug moieties to ligands. The compounds also include drug-ligand conjugates comprising a ligand capable of targeting a selected cell population, and a drug connected to the ligand by a heterocyclic linker moiety. The linker moiety comprises a peptide sequence that is a substrate for an intracellular enzyme, for example a cathepsin, that cleaves the peptide at an amide bond. The peptide further contains a self-immolating moiety which connects the drug and the protein peptide sequence. Upon cleavage of the peptide sequence by an intracellular enzyme the self-immolating moiety cleaves itself from the drug moiety such that the drug moiety is in an underivatized and active form.

Light- and/or UV-radiation protective coatings for drug delivery devices, such as, for instance, drug eluting vascular stents, where the drugs being delivered via the stents are light sensitive. A method of fabricating a medical article, such as a drug eluting vascular stent, that includes the light- and/or UV-radiation protective coating.

According to the present invention, a method for enhancing transdermal transport is disclosed. The method includes the steps of increasing a permeability of an area of a membrane with a permeabilizing device. The membrane may be, inter alia, biologic skin or synthetic skin. The permeabilizing device may be an ultrasound-producing device. A substance is transported into and through the area of the membrane. The substance may be a drug, a vaccine, or a component of interstitial fluid.

[Summary]

[Problem] Provided is a substituted spiropyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, which is useful as an anti-HIV agent.

[Solving Means] The present invention relates to a compound represented by the following formula [I] or [II] or a pharmaceutically acceptable salt thereof:

wherein each symbol is as defined in the specification.

The present invention provides treatment regimens for treating diseased prostate tissue, including the steps of chemically ablating prostate tissue and coadministering an antiandrogen. In some embodiments, prostate tissue is chemically ablated by injection of ethanol, or an injectable gel comprising ethanol, into prostate tissue. Steroidal and non-steroidal antiandrogens are suitable antiandrogens. One suitable non-steroidal antiandrogen is bicalutamide. The treatment regimen is suitable for treatment of prostate tissue diseases including benign prostatic hyperplasia and prostatic carcinoma. The invention further provides a treatment regimen for treating benign prostatic hyperplasia, including the steps of damaging prostate tissue and coadministering an antiandrogen. Also provided by the present invention is a kit for treating a human male, including a means for necrosing prostate tissue, an antiandrogen drug, and a means for administering the antiandrogen drug. A kit including a first surgical device for delivering a chemoablation fluid to prostate tissue transurethrally, an antiandrogen drug such as bicalutamide, and a second surgical device for administering the antiandrogen drug, is further provided.

A new dry powder inhaler is developed as a pulmonary medicine delivery device for dispersing precise tiny dosages (10 μg-50 mg) of pure carrier-free ultra-fine powdered medicament (<5 μm aerodynamics particle size) into a patient's lung. The powder is drawn from the blister cell and dispersed through an outlet tube assisted by two air streams. The first air stream goes through a the blister cell from its upstream side, to significantly fluidize the medicament in the dose to flow upward. The second one extracts the fluidized powder from downstream of the blister cell for further deagglomeration and dispersion of the medicament powder by shear force. The rotating multi-dose blister can hold up to 60 doses, which are pre-metered with pure ultra-fine powdered medicament. So that it has higher drug loading capability in small volumes, compared to most current dry powder inhalers, which usually use some excipient. The inhaler efficiently disperse the aerosolized medicament in the air stream to the deep interior of patient's lung. The fine particle fraction (<4.7 μm) is reported to reach as high as 80% using this inhaler.

The present invention relates to tripeptide compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. In particular, the present invention provides novel tripeptide analogs, pharmaceutical compositions containing such analogs and methods for using these analogs in the treatment of HCV infection.

A pharmaceutical composition and formulations comprise preventative, prophylactic or therapeutic amounts of an oligo(s) anti-sense to a specific gene(s) or its corresponding mRNA(s), and a glucocorticoid and/or non-glucocorticoid steroid or a ubiquinone or their salts. The agents, composition and formulations are used for treatment of ailments associated with impaired respiration, bronchoconstriction, lung allergy(ies) or inflammation, and abnormal levels of adenosine, adenosine receptors, sensitivity to adenosine, lung surfactant and ubiquinone, such as pulmonary fibrosis, vasoconstriction, inflammation, allergies, allergic rhinitis, asthma, impeded respiration, lung pain, cystic fibrosis, bronchoconstriction, COPD, RDS, ARDS, cancer, and others. The present treatment is effectively administered by itself for conditions without known therapies, as a substitute for therapies exhibiting undesirable side effects, or in combination with other treatments, e.g. before, during and after other respiratory system therapies, radiation, chemotherapy, antibody therapy and surgery, among others. Each of the agents of this invention may be administered directly into the respiratory system so that they gain direct access to the lungs, or by other effective routes of administration. A kit comprises a delivery device, the agents and instructions for its use.

A system for managing delivery of pharmaceutical drugs is formed of a blister package that includes a plurality of cells arranged in a grid. Each of the cells is sealed by a breakable wall and holds a unit-dose of medication. A user gains access to the medication in a given cell by puncturing the breakable wall associated with the given cell. A severable conductor is positioned proximate to each breakable wall. The severable conductor associated with a given cell ruptures upon puncturing of the breakable wall associated with the given cell. A computer chip is electrically connected to the severable conductors. The computer chip senses the puncturing of each cell in the grid by monitoring the rupturing of each of the severable conductors. An RF transmitter is coupled to the computer chip. The RF transmitter sends information corresponding to usage of each of medications stored in the blister package to a remote information transceiver.

Cells derived from postpartum tissue such as the umbilical cord and placenta, pharmaceutical compositions comprising such cells, and methods for using such cells and pharmaceutical compositions to treat patients having a neurodegenerative condition of the substantia nigra or striatum, such as Parkinson's disease, are provided.

The present disclosure provides antibody-drug conjugates that are potent cytotoxins, wherein the drug is linked to the antibody through a linker. The disclosure is also directed to compositions containing the antibody-drug conjugates, and to methods of treatment using them.

Methods and devices for ablating portions of a tissue volume with electromagnetic radiation (EMR) to produce lattices of EMR-treated ablation islets in the tissue are disclosed, including lattices of micro-holes, micro-grooves, and other structures. Also, methods and devices for using the ablated islets are disclosed, including to deliver chromophores, filler, drugs and other substances to the tissue volume.

The invention is an inhaler for aerosolization of medicament with a unique dosage counter. The dosage counter has a first and second counting ring and a coupling device that interconnects the counting rings. The counter being advanced by a unique armature mechanism that is interconnected with the actuation mechanism of the inhaler to insure accurate counting of doses.

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.

A compound of formula (I):

Conjugates of a cereblon-binding compound and compounds having modulatory activity against G12C mutant KRAS, HRAS or NRAS G12C proteins are provided. Methods associated with preparation and use of such conjugates, pharmaceutical compositions comprising such conjugates and methods to modulate the activity of G12C mutant KRAS, HRAS or NRAS G12C proteins for treatment of disorders, such as cancer, are also provided.

The present invention relates to a polymeric drug conjugate with one or more biologically active agents conjugated via an enzymatically cleavable linker to either a regular repeating linear unit comprising a water soluble polymer segment and a multifunctional chemical moiety, or a branched polymer comprising two or more water soluble polymer segments each bound to a common multifunctional chemical moiety, as well as to methods of making such conjugates. The present invention is also directed to pharmaceutical compositions comprising such conjugates and to the use of such conjugates to treat pathological conditions.

A drug delivery device that is suitable for delivery of a therapeutic agent to limited access regions of the eye is provided. Preferred devices of the invention are minimally invasive, refillable and may be easily fixed to the treatment area.

The invention discloses an anti-SARS-CoV-2 fully-humanized monoclonal antibody against SARS-CoV-2. The antibody is obtained by screening through a flow sorting-single cell PCR technology, and has a unique CDR partition. The invention further discloses an application of the antibody in preparation of medicines for treating the 2019-coronavirus disease. The monoclonal antibody disclosed by the invention has efficient and specific anti-SARS-COV-2 activity, also has the characteristics of high expression, complete humanization and good stability, and is suitable for industrial production.

The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

Absorbable polyurethanes, polyamides and polyester urethanes prepared from at least one compound selected from:

or the diamines and diisocyanates thereof, wherein each X represents a member independently selected from —CH₂COO— (glycolic acid moiety), —CH(CH₃)COO— (lactic acid moiety), —CH₂CH₂OCH₂COO— (dioxanone), —CH₂CH₂CH₂CH₂CH₂COO— (caprolactone moiety), —(CH₂)_yCOO— where y is one of the numbers 2, 3, 4 or 6-24 inclusive, and —(CH₂CH₂O)_z′CH₂COO— where z′ is an integer between 2 and 24, inclusive; each Y represents a member independently selected from —COCH₂O— (glycolic ester moiety), —COCH(CH₃)O— (lactic ester moiety), —COCH₂OCH₂CH₂O— (dioxanone ester), —COCH₂CH₂CH₂CH₂CH₂O— (caprolactone ester), —CO(CH₂)_mO— where m is an integer between 2, 3, 4 or 6-24 inclusive, —COCH₂O(CH₂CH₂O)_n— where n is an integer between 2 and 24, inclusive; R′ is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; p is an integer between 1 and 4, inclusive; and Rn represents one or more members selected from H, alkoxy, benzyloxy, aldehyde, halogen, carboxylic acid and —NO₂, which is attached directly to an aromatic ring or attached through an aliphatic chain. Absorbable polymers prepared from these compounds are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention and other implantable medical devices.

The present invention generally relates to the field of intravascular medical devices, and more specifically to the field of balloon catheters and other similar diagnostic or therapeutic catheters within the body for treatment and diagnosis of diseases. In particular, the present invention relates to reinforced balloon catheters and drug-eluting balloon catheters and corresponding methods for producing same.

The present disclosure provides drug-ligand conjugates and drug-cleavable substrate conjugates that are potent cytotoxins. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.

A pharmaceutical composition comprising therapeutically effective amount of rifaximin or pharmaceutically acceptable salt or enantiomer or polymorph thereof, pharmaceutically acceptable excipient(s) and release controlling agent(s). Pharmaceutical composition of rifaximin comprising: at least two entities wherein one entity is an immediate release or fast release and the other is controlled release. The pharmaceutical composition in the form of multilayer tablet comprising, at least one layer comprising, therapeutically effective amount of rifaximin or pharmaceutically acceptable salt or enantiomer or polymorph thereof, pharmaceutically acceptable excipient(s); said layer providing controlled release rifaximin; and at least one layer which provides increased residence time of the dosage form in the gastrointestinal tract. The pharmaceutical formulation comprising rifaximin having an in vitro dissolution profile, wherein about 70% of rifaximin is released in about 24 hours. The composition comprising therapeutically effective amount of rifaximin or pharmaceutically acceptable salt(s) or enantiomer(s) or polymorph(s) thereof, one or more release controlling agent(s) and pharmaceutically acceptable excipient(s) causing pathogenic eradication.

This invention relates to a pharmaceutical composition comprising or consisting essentially of the phytocannabinoids cannabidivarin (CBDV) and cannabidiol (CBD). The composition is particularly safe and efficacious for use in the treatment of neurological conditions, characterized by hyper-excitability of the central nervous system, convulsions or seizures such as occur in epilepsy. Preferably the CBDV and the CBD are present with at least one non-cannabinoid component of cannabis such as one or more terpenes or a terpene fraction. More particularly the composition further comprises one or more cannabichromene type compounds. Particularly cannabichromene propyl variant (CBCV) and/or cannabichromene (CBC). More particularly still the composition is absent or substantially absent of other cannabinoids, including in particular tetrahydrocannabinol (THC) and tetrahydrocannabivarin (THCV), which would normally be present in significant amounts in cannabis chemotypes bred to contain a significant amount of CBDV and/or CBD.

In its many embodiments, the present invention discloses novel compounds, as inhibitors of HDM2 protein, methods for preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of treatment, prevention, inhibition, of one or more diseases associated with the HDM2 protein or P53 using such compounds or pharmaceutical compositions.

The present invention relates to chemically modified, linked double-stranded (ds)RNA compositions comprising two or more double-stranded (ds) oligoribonucleotides linked by at least one linking moiety and methods of formulating and delivering such compositions to modulate gene expression through target-specific RNA co-interference (RNAco-i). The compositions of the invention may optionally comprise a conjugation or a complex with one or more small molecule drugs, protein therapeutics, or other dsRNA molecules. The present invention is directed at the methods of production for, methods of use of, and therapeutic utilities for RNAi co-interference therapy utilizing the compositions of the invention.